Drug abuse and their effect
1. INTRODUCTION
DefinitionsAddiction is a word that’s used to describe a variety of conditions which are all characterized by
an abnormally strong need to act in predictable ways to try to satisfy the intense driving forces
that are felt by anyone with an addiction.
Substance abuse, which can also be called drug abuse, is one form of addiction. It involves the
intense craving and need to consume, inject, sniff or smoke, one or more of a wide variety of
psycho-active drugs. A psycho-active drug is any chemical which has the property of changing
how the brain functions.
The word Addiction is also used to describe some behavioral disorders such as pathological
gambling or abnormal eating behavior, where no psycho-active substance use is involved, but
the features of this sort of addiction, still closely resemble those of substance abuse addiction.
“loss of control is the hallmark of all addictions”
People with an addiction do not have control over what they are doing, taking or using. Their
addiction may reach a point at which it is harmful. Addictions do not only include physical things
we consume, such as drugs or alcohol, but may include virtually anything, such abstract things
as gambling to seemingly harmless products, such as chocolate - in other words, addiction may
refer
to
a substance
dependence (e.g.
drug
addiction)
or
behavioural
addiction (e.g.gamblingaddiction).
In the past addiction used to refer just to psychoactive substances that cross the blood-brain
barrier, temporarily altering the chemical balance of the brain; this would include alcohol,
tobacco and some drugs. A considerable number of psychologists, other health care
professionals and lay people now insist that psychological dependency, as may be the case
with gambling, sex, internet, work, exercise, etc. should also be counted as addictions, because
they can also lead to feelings of guilt, shame, hopelessness, despair, failure, rejection, anxiety
and/or humiliation.When a person is addicted to something they cannot control how they use it,
and become dependent on it to cope with daily life.
Addiction - there is a psychological/physical component; the person is unable to control the
aspects of the addiction without help because of the mental or physical conditions involved
Addiction is Habitual psychological or physiologic dependence on a substance or practice that is
beyond voluntary control.
Addiction has long been understood to mean an uncontrollable habit of using alcohol or
other drugs. Because of the physical effects of these substances on the body, and particularly
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Drug abuse and their effect
the brain, people have often thought that “real” addictions only happen when people regularly
use these substances in large amounts.
More recently, we have come to realize that people can also develop addictions to behaviours,
such as gambling, and even quite ordinary and necessary activities such
as exercise and eating. What these activities have in common is that the person doing them
finds them pleasurable in some way.
There is some controversy about which of the “behavioural” addictions constitute scientifically
validated “true” addictions, with both professionals and the public failing to reach an agreement.
More research is needed to clarify this issue....
2. TYPES OF ADDICTION
1. Alcohol Addiction
Alcohol is a substance that is perfectly legal for adults to buy and consume, and has the
potential to become addictive. We tend to use euphemisms like "drinking problem" or say that
someone likes to "bend the elbow" when talking about an addiction to alcohol. It's a polite way
of talking about an addiction that can have serious health consequences, including cirrhosis of
the liver and brain damage. It is no coincidence that thousands of alcohol treatment
centres exist across the world.
2. Nicotine Addiction
If you have ever wondered why giving up smoking is so difficult, blame the fact that nicotine is
one of the most addictive substances on the planet. Every time a smoker lights up, they are
getting a "hit" of nicotine that works on the pleasure centre in their brain. Cravings are just the
body's way of looking for more of the same. Unfortunately, smoking has been linked to several
types of cancer, heart disease, and stroke.
3. Cocaine Addiction
Cocaine is a highly-addictive stimulant that is made from the leaves of the coca plant. Whether
you call it "coke," "blow," or "nose candy," it gives the user a relatively brief, but very intense,
high. This drug also causes the user's heart rate and blood pressure to increase rapidly,
sometimes with tragic results in the form of a heart attack or a stroke.
4 .Opiate Addiction
Codeine, morphine, and heroin are all powerful painkilling drugs derived from the opium poppy.
Not only can they alleviate pain, but they also produce a feeling of euphoria, which opens up the
door to addiction. Someone who is in the throes of an addiction to these kinds of drugs may lose
the ability to make good decisions for themselve. They also run the risk of contracting HIV/AIDS
if they are using needles to inject themselves. Often, a visit to a drug detox centre is necessary
even before entering a treatment facility for opiate addiction treatment.
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5. Heroin Addiction
Heroin is known by several names, including "smack," "horse," and "brown sugar" due to its
varying forms and colors.. It produces a feeling of euphoria for the more than half a million
people in the United States who use it. Heroin can cause physical dependency in users within
days of being used regularly, which means that trying to give it up can be very difficult.
6. Meth Addiction
Some people turn to meth, a type of amphetamine, as their drug of choice because it is an
appetite suppressant. It also produces an intense "high" when injected, smoked, snorted, or
swallowed. Addiction can happen very quickly, and it's possible to become addicted after using
meth only once.
7. Methadone Addiction
In a twist of irony, methadone, which is used to treat people who are addicted to heroin, is itself
a highly-addictive drug. Like heroin, methadone is an opiate, and it is used to relieve the
cravings that a recovering heroin addict may experience. Many wonder whether trading one
addiction for another is such a good idea.
8. Marijuana Addiction
More than three million people in the United States use marijuana on either a daily or an almostdaily basis, making it the most popular illegal drug in the country. There are more than 200
different names used to describe the leaves, stems, and flowers of the hemp plant, which are
dried and rolled prior to being smoked. The question of whether marijuana is addictive remains
a popular debate with opposing viewpoints.
9. Caffeine Addiction
Do you enjoy your morning Java? Many people do, but there are some for whom caffeine isn't
just something that helps them feel alert through the day. They develop a full-blown addiction,
including withdrawal symptoms when they try to switch to decaf or cut back on caffeine-laden
soft drinks and chocolate.
10. Steroid Addiction
Athletes and body builders who want to increase muscle mass may be tempted to use steroids
to get bigger, faster. They may not realize that the sense of well-being they experience when
using them is from the 'roids’ themselves. An addiction to steroids may be more difficult to
recognize than someone using a substance to achieve a "high" though there are typically signs
that can be detected.
11. Vicodin Addiction
Vicodin is usually prescribed for moderate pain. This opiate not only relieves pain, but also
produces a feeling of euphoria. Approximately one person in five in the United States has taken
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Drug abuse and their effect
a prescription medication for a purpose other than the one for which it was prescribed,
and vicodin is the drug most often used in this way.
12. Prescription Drug Addiction
Using prescription drugs for a long time or taking more than the recommended dose may lead to
an addiction. This is the reason doctors limit the amount of medication they prescribe. Any
prescription drug taken to relieve pain has the potential to create a physical dependency.
3. HARMFUL EFFECTS OF DRUG ABUSE
Drug abuse can affect individuals, relationships and society, but the specific effects depend on
the specific drug of abuse. Both street drugs and legal drugs, such as prescription medication or
legally purchased alcohol, can be abused and can contribute to problems for the individual
involved. Drug addicts may have extreme difficulty quitting and in some cases it may be nearly
impossible without the intervention of treatment programs and psychological counseling.
Nonetheless, the harmful effects of drug abuse are serious enough that efforts to prevent drug
dependence and help individuals who desire to stop using drugs are worthwhile.
1. HEALTH PROBLEMS
Depending on the specific type of drug abused, health problems may take a range of forms,
according to Medline Plus. Some drug abusers become addicted, suffering withdrawal
symptoms if they attempt to quit using the drug. Amphetamines, for example, cause immediate
health issues including a rapid heart rate, weight loss and sleep disturbances. On the other
hand, alcoholics may develop liver disease over long periods of use. Injected drugs such as
heroin raise the risk of an individual contracting infectious diseases such as HIV or hepatitis.
Hallucinogens such as LSD remain within the body for years after the initial use, potentially
causing flashbacks. Many drugs can cause death if the user takes too much of them.
2. RELATIONSHIP EFFECTS
Because drugs often alter the behavior of the user, relationships frequently suffer from the
effects of drug abuse. Some drugs, such as cocaine, may cause some users to become violent,
making domestic abuse more likely. In other cases, the drug user may shirk off responsibilities,
upsetting friends and family members. Because drug addicts often must spend large amounts of
money to continue to acquire drugs, drug users frequently find themselves in financial trouble,
which can add to marital stress. Drugs that alter inhibitions, such as alcohol, can contribute to
unwise decisions that can stress relationships, including imprudent sexual activity and risktaking behavior.
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3. SOCIAL EFFECTS
Many individuals who abuse drugs end up committing criminal acts to support their drug habit.
The National Drug Intelligence Center maintains that parents who abuse drugs often neglect or
abuse, either physically or mentally, the children in their care. Children of addicts tend to go
without proper dental and medical care, including not receiving all of their childhood
vaccinations on schedule. These children are also more likely to go without proper food and
shelter and may be inadvertently exposed to the drugs that their parents are using. The
maintenance of law enforcement programs to combat community drug use requires taxpayer
money at both the local and federal levels.
(a) Effects of Drug Addiction in Adolescents
1. Criminal
•
One of the fastest ways for an adolescent's drug use or addiction to affect his life is through the
criminal consequences associated with the drug use. The law does not make exceptions for
teen drug users. Even if a teenager is not caught using drugs, living a drug-filled life can lead to
many other criminal problems, including gang activity and drug-related criminal offenses. Some
teenagers turn to selling to support their habits. Addiction can also compel an adolescent to take
part in criminal activity such as theft to get money to buy drugs. Studies have shown that drug
use automatically raises the chances that a teenager will commit a criminal offense. In fact, the
Bureau of Justice Statistics found that nearly two-thirds of released jail inmates were using
drugs within 4 to 6 months before they committed their offenses.
2. Education
•
According to a 2005 survey by the U.S. Census Bureau, school dropout rates varied by state
from 5 percent to nearly 11 percent of all high school students. Though not all high school
dropouts do so because of drug addictions, drugs can be a dominating factor. Once a teenager
has become addicted to a drug, whether it be alcohol or meth or marijuana, her drug addiction
can take precedence over any other activities in her life. This is especially true if the adolescent
comes from a broken family who may not be aware, or care, that their child is skipping school.
As the addiction strengthens, it can be hard for the teenager to function while high. Even if she
does attend school, she may be disruptive or just unable to learn because of the influence of the
drugs in her system. This can lead to either voluntary removal from school through dropping out
or forced removal from school by expulsion. Drug use can also allow criminal activity to spread
onto school property.
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Drug abuse and their effect
3.Family
•
A drug-addicted adolescent can quite often go through a complete change in character because
of his using. A once-friendly who is hard to live with. Many teenage drug users become defiant
against authority figures, including their own parents. They may also turn to lying and even
stealing from their families to support their habits. This can easily lead to a host of problems in
the home, even completely splitting apart family relationships.
4. Health
•
One of the most devastating effects of an adolescent drug addiction is the health problems that
come with drug use. Even in small doses, both illicit and legal drugs can have severe effects on
a teenager, ranging from early onset of liver problems to cardiac arrest. However, the most
dangerous health consequence comes with a drug overdose, which in many cases leads to
death. Teenagers are especially at risk for drug overdose, since drug use often becomes a
competition among younger users. This competitive atmosphere is especially true with binge
drinking.
5. Costs
•
For every adolescent addict, there is an increased price for health care and drug treatment. With
the average treatment program costing thousands of dollars per month, and much of that bill
being covered by health care programs, the cost of addiction is staggering. Teen drug use also
contributes to other drains on the health care and financial system. These include an increased
risk for the contraction of sexually transmitted diseases, an increased risk of drug-related car
accidents and an increase in drug-related crimes.
(b) OTHER EFFECTS
•
•
•
•
•
•
•
•
Physical deterioration
Psychiatric problems
Intellectual impairment
Personality deterioration
Increased risk of accidents and higher susceptibility to high
risk behaviour in the form of unprotected sex or use of
unsterile needles
Legal risks.
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Drug abuse and their effect
4. Category of Abused Drug
Drugs and medications of abuse can be grouped together into categories based on similarities
between how they work and what effects they will produce in the human body and brain. A
useful categorization scheme follows. We'll consider each class of drugs in turn, but if you want
to, you can skip ahead to read about the particular drug class that interests you most.
•
•
•
Central Nervous System Depressants
Alcohol
Barbiturates ['ludes, sleepers, downers, tranquilizers]
Benzodiazepines (Valium, Ativan, Librium, Xanax) [sleepers, downers, tranquilizers]
•
•
•
•
Central Nervous System Stimulants
Cocaine (Crack, Blow, Nose, Snow, Toot, White, Rock, Flake)
Amphetamine & Methamphetamine (Ritalin, Meth, Bennies, Crank, Crystal)
Caffeine (Coffee)
Nicotine (Cigarettes, Chew)
•
•
•
•
Opiates
Heroin (Horse, Junk, Smack, Snow, "H", Brown, Black)
Morphine
Codeine (OxyContin, Tylenol with Codeine)
Methadone, LAAM
•
•
Cannabinols
Marijuana (Marinol, Pot, Grass, Weed, Brick, Joint, Thai Stick, Mary Jane)
Hashish (Hash, Ganja, Rope)
•
•
•
•
Hallucinogens
LSD (Acid)
Mescaline (Cactus)
Psilocybin, ('Shrooms, Mushrooms)
MDMA (Love Drug, "X", Esctacy)
•
•
•
•
Solvents
Aerosol sprays
Glues
Paint Thinner
Gasoline
Other Drugs of Abuse
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Drug abuse and their effect
•
PCP (Angel Dust)
5. Classification of Addictive Drugs
a)
b)
c)
d)
e)
f)
g)
Narcotic Analgesics
Stimulants
Depressants
Hallucinogens
Cannabis
Volatile Solvents
Other drugs of abuse
(a) NARCOTIC ANALGESICS
Pain killing or pain relieving drugs with opium like effects
Natural sources – Opium – Morphine, Codeine
Semi synthetic : Heroin (brown sugar)
Synthetic : Buprenorphine (tidigesic), Methadone, Pentazocine
Mode of intake
� Opium – oral, inhalation
� Morphine – injection
� Codeine – oral (tablets and cough syrups)
� Heroin – injection, inhalation, chasing
� Buprenorphine – oral, injection
Short – term effects
� Euphoria
� Thought process impairment, drowsiness, apathy
� Feelings of hunger and pain are not felt
� Overdose of heroin can cause convulsions, coma and death
Long – term effects
� Mood instability
� Reduced libido
� Constipation
� Respiratory impairments
� Physical deterioration
Infections like serum hepatitis and HIV can occur among IV users due to use of unsterile
needles. In female abusers, menstrual irregularity and fetal addiction / abnormality can
occurs.
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Tolerance and dependence develop Withdrawal symptoms
� Feeling of unpleasantness
� Aches and pains all over the body
� Diarrhoea
� Dilation of pupils
� Insomnia
(b) STIMULANTS
Drugs which excite or speed up the central nervous system
Type and mode of intake
� Amphetamines – oral
� Cocaine – snorted
Short – term effects
� A heightened feeling of well being, euphoria
� A sense of super-abundant energy
� Increased motor and speech activity
� Suppression of appetite
� Increased wakefulness
Long-term effects
� Chronic sleep problem
� Poor appetite
� Rapid and irregular heart beat
� Mood swings
� `Amphetamine psychosis’ may occur
Tolerance and dependence develop Withdrawal symptoms – No major physiological
disruptions
� Extreme fatigue
� Disturbed sleep
� Voracious appetite
� Moderateto severe depression
(c) DEPRESSANTS
Drugs which depress or slow down the functions of the central nervous system
Type and mode of intake
Sedative-hypnotics – Barbiturates, Benzodiazepines (oral tablets) Alcohol
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Drug abuse and their effect
Short – term effects
� Relief from anxiety and tension
� Euphoria
� Lowering of inhibitions
� Poor motor coordination
� Impaired concentration and judgement
� Slurred speech and blurred vision
� Sedation, sleep with larger doses
Long – term effects
� Depression
� Chronic fatigue
� Respiratory impairments
� Impaired sexual function
� Decreased attention span
� Poor memory and judgement
� Chronic sleep problems
Tolerance and dependence
� Tolerance does not develop uniformly
� Cross tolerance can develop
� Physical and psychological dependence develop
Withdrawal symptoms
� Tremors
� Insomnia
� Irritability and restlessness
� Hallucinations
� ConvulsiONS
(d) HALLUCINOGENS
Hallucinogens are drugs which affect perception, emotions and mental processes
Type and mode of intake
LSD -Lysergic acid diethylamide (oral tablets)
PCP –Phencyclidine (snorted / smoked)
Mescaline (oral tablets)
Psilocybin (smoked)
Short – term effects
� Alterations of mood
� Distortion of the sense of direction, distance and time
� ‘Pseudo’ hallucinations
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Drug abuse and their effect
� Synesthesia – melding of two sensory modalities
� Feelings of depersonalization
Long-term effects
� Flash back or spontaneous recurrence of on LSD experience can occur
� Amotivational syndrome
� LSD precipitated psychosis
(e) CANNABIS
Drugs from cannabis plant come under this category
� Ganja / Marijuana
� Hashish / Charas
� Hashish oil
� Bhang
Mode of intake- Smoking
Short – term effects
� Mild euphoria
� Lowering of inhibitions
� Reddening of eyes
� Sense of smell, touch and taste are often enhanced
� Altered sense of time perception
� Impaired short-term memory
� Impairment of ability to perform complex motor tasks
Long-term effects
� Decreased cognitive ability
� Amotivational syndrome
� Psychosis
� Respiratory problems
� Sterility / impotence
� In women abusers, fetal damage can occur
Tolerance and psychological dependence develop Withdrawal symptoms
� Sleep disturbances
� Loss of appetite, irritability
� Tremors
� Depression or psychotic symptoms may become prominent
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Drug abuse and their effect
(f) VOLATILE SOLVENTS
Drugs under this category are volatile hydrocarbons, Petroleum derivatives Type and mode of
intake Glue and solvents like varnish and eraser fluids and petrol through sniffing.
Short – term effects
� Euphoria
� Clouded thinking
� Slurred speech
� Staggering gait
� Hallucinations
� Sudden death
Long – term effects
� Psychosis
� Permanent brain damage
� Liver, kidney and heart damage
(g) OTHER DRUGS OF ABUSE
Medically used drugs that do not fall into any of the above categories
� Muscle relaxants
� Painkillers
� Anti-histamines, prescribed for allergies
� Anti-emetics
� Anti-depressants / anti-psychotics
These drugs are taken orally as tablets or used in the form of injections. The effects and
subsequent dependence and withdrawal symptoms vary.
6. LIST OF ABUSED DRUGS
(a) Tobacco
Category
& Name
Examples of Commercial
DEA Schedule
& Street Names
Nicotine
Found cigarettes, cigars, Not scheduled
bidis
&
smokeless
tobacco
(snuff,
spit
tobacco, chew)
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How Administered*
Smoked, snorted, chewed
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Drug abuse and their effect
Acute Effects - Increased blood pressure and heart rate
Health Risks - Chronic lung disease; cardiovascular disease; stroke; cancers of the
mouth, pharynx, larynx, esophagus, stomach, pancreas, cervix, kidney, bladder, and
acute myeloid leukemia; adverse pregnancy outcomes; addiction.
(b) Alcohol
Category & Name
Exampleof commercial
DEA Schedule
& street name
Alcohol
(ethylalcohol)
Found in liquor, beer, Not scheduled
and wine
How Administered*
Swallowed
Acute Effects - In low doses, euphoria, mild stimulation, relaxation, lowered inhibitions; in
higher doses, drowsiness, slurred speech, nausea, emotional volatility, loss of coordination,
visual distortions, impaired memory, sexual dysfunction, loss of consciousness
Health Risks - Increased risk of injuries, violence, fetal damage (in pregnant women);
depression; neurologic deficits; hypertension; liver and heart disease; addiction; fatal overdose
(c) Cannabinoids
Category
& Name
Examples of Commercial & DEA
Street Names
Schedule
Marijuana
Blunt, dope, ganja, grass, I ?
herb, joint, bud, Mary Jane,
pot, reefer, green, trees,
smoke, sinsemilla, skunk,
weed
Boom, gangster, hash, hash I ?
oil, hemp
Hashish
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How Administered*
Smoked, swallowed
Smoked, swallowed
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Drug abuse and their effect
Acute Effects - Euphoria; relaxation; slowed reaction time; distorted sensory perception;
impaired balance and coordination; increased heart rate and appetite; impaired learning,
memory; anxiety; panic attacks; psychosis
Health Risks - Cough, frequent respiratory infections; possible mental health decline; addiction
(d) Opioids
Category
& Name
Examples of Commercial DEA
& Street Names
Schedule
Heroin
Diacetylmorphine:
I?
smack,
horse,
brown
sugar, dope, H, junk, skag,
skunk, white horse, China
white; cheese (with OTC
cold
medicine
and
antihistamine)
Laudanum,
paregoric: II, III, V ?
big O, black stuff, block,
gum, hop
Opium
How Administered*
Injected, smoked, snorted
Swallowed, smoked
Acute Effects - Euphoria; drowsiness; impaired coordination; dizziness; confusion; nausea;
sedation; feeling of heaviness in the body; slowed or arrested breathing
Health Risks - Constipation; endocarditis; hepatitis; HIV; addiction; fatal overdose
(e) Stimulants
Category & Name
Cocaine
Examples of Commercial
DEA schedule
& Street Names
Cocaine hydrochloride: II ?
blow, bump, C, candy,
Charlie, coke, crack,
flake, rock, snow, toot
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How Administered*
snorted,
injected
smoked,
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Drug abuse and their effect
Amphetamine
Biphetamine,
II ?
Dexedrine:
bennies,
black beauties, crosses,
hearts, LA turnaround,
speed, truck drivers,
uppers
Methamphetamine
Desoxyn: meth, ice, II ?
crank, chalk, crystal, fire,
glass, go fast, speed
swallowed,
snorted,
smoked, injected
swallowed,
snorted,
smoked, injected
Acute Effects - Increased heart rate, blood pressure, body temperature, metabolism; feelings
of exhilaration; increased energy, mental alertness; tremors; reduced appetite; irritability;
anxiety; panic; paranoia; violent behavior; psychosis
Health Risks - Weight loss, insomnia; cardiac or cardiovascular complications; stroke; seizures;
addiction
Also, for cocaine – Nasal damage from snorting
Also, for methamphetamine – Severe dental problems
(f) Club drugs
Category & Name
MDMA
Flunitrazepam**
GHB**
Examples of Commercial &
DEA
Street Names
Schedule
Ecstasy, Adam, clarity, I ?
Eve, lover's speed, peace,
uppers
Rohypnol: forget-me pill, IV ?
Mexican Valium, R2, roach,
Roche, roofies, roofinol,
rope, rophies
Gamma-hydroxybutyrate: I ?
G, Georgia home boy,
grievous bodily harm, liquid
ecstasy, soap, scoop, goop,
liquid X
How Administered*
swallowed,
injected
snorted,
swallowed, snorted
Swallowed
Acute Effects,for MDMA - Mild hallucinogenic effects; increased tactile sensitivity; empathic
feelings; lowered inhibition; anxiety; chills; sweating; teeth clenching; muscle cramping
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Drug abuse and their effect
Also, for Flunitrazepam - Sedation; muscle relaxation; confusion; memory loss; dizziness;
impaired coordination
Also, for GHB - Drowsiness; nausea; headache; disorientation; loss of coordination; memory
loss
Health Risks, for MDMA - Sleep disturbances; depression; impaired memory; hyperthermia;
addiction
Also, for Flunitrazepam - Addiction
Also, for GHB - Unconsciousness; seizures; coma
(g) Dissociative drugs
Category & Name
Ketamine
PCP and analogs
Salvia divinorum
Dextromethorphan
(DXM)
Examples
Of Commercial
& Street Names
Ketalar
SV: cat
Valium, K, Special K,
vitamin K
Phencyclidine:ange
l dust, boat, hog, love
boat, peace pill
Salvia,
Shepherdess's Herb,
Maria Pastora, magic
mint, Sally-D
Found in some
cough
and
cold
medications:
Robotripping, Robo,
Triple C
DEA
Schedule
How Administered*
III ?
injected, snorted, smoked
I, II ?
swallowed, smoked, injected
Not
Scheduled
chewed, swallowed, smoked
Not
Scheduled
Swallowed
Acute Effects - Feelings of being separate from one’s body and environment; impaired motor
function
Also, for ketamine - Analgesia; impaired memory; delirium; respiratory depression and arrest;
death
Also, for DXM - Euphoria; slurred speech; confusion; dizziness; distorted visual perceptions
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Drug abuse and their effect
Health Risks - Anxiety; tremors; numbness; memory loss; nausea
(h) Hallucinogens
Category & Name
LSD
Mescaline
Psilocybin
Examples
of Commercial & Street
Names
Lysergic
acid
diethylamide:acid,
blotter,
cubes,
microdot
yellow
sunshine, blue heaven
Buttons,
cactus, mesc,
peyote
Magic mushrooms, purple
passion, shrooms, little smoke
DEA
Schedule
I?
How Administered*
swallowed,
absorbed
through mouth tissues
I?
swallowed, smoked
I?
swallowed
Acute Effects - Altered states of perception and feeling; hallucinations; nausea
Also, for LSD - Increased body temperature, heart rate, blood pressure; loss of appetite;
sweating; sleeplessness; numbness, dizziness, weakness, tremors; impulsive behavior; rapid
shifts in emotion
Also, for Mescaline - Increased body temperature, heart rate, blood pressure; loss of appetite;
sweating; sleeplessness; numbness, dizziness, weakness, tremors; impulsive behavior; rapid
shifts in emotion
Also, for Psilocybin - Nervousness; paranoia; panic
Health Risks, for LSD - Flashbacks, Hallucinogen Persisting Perception Disorder
(i) Other compounds
Category & Examples of Commercial & Street
DEA
Name
Names
Schedule
LSD
Mescaline
Lysergic acid diethylamide:acid, I ?
blotter, cubes, microdot yellow
sunshine, blue heaven
Buttons, cactus, mesc, peyote
I?
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How Administered*
swallowed,
absorbed
through mouth tissues
swallowed, smoked
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Drug abuse and their effect
Psilocybin
Magic
mushrooms,
purple I ?
passion, shrooms, little smoke
Swallowed
Acute Effects, for Anabolic steroids - No intoxication effects
Also, for Inhalants (varies by chemical) - Stimulation; loss of inhibition; headache; nausea or
vomiting; slurred speech; loss of motor coordination; wheezing
Health Risks, for Anabolic steroids - Hypertension; blood clotting and cholesterol changes;
liver cysts; hostility and aggression; acne; in adolescents—premature stoppage of growth; in
males—prostate cancer, reduced sperm production, shrunken testicles, breast enlargement; in
females—menstrual irregularities, development of beard and other masculine characteristics
Also, for Inhalants - Cramps; muscle weakness; depression; memory impairment; damage to
cardiovascular and nervous systems; unconsciousness; sudden death
7. TOP 10 Abused Drugs (Prescribed)
1. Ambien (Zolpidem)
Zolpidem is a nonbenzodiazepine (similar to a benzo, but with a different molecular structure)
drug with powerful hypnotic and sedative effects. It’s prescribed by doctors for treatment of
insomnia, and in rarer cases as a muscle relaxant. Due to its GABA antagonist properties, it is
similar to alcohol in its ability to relax inhibitions and promote sociability. In especially high
doses, the onset of amnesia can be quite potent, resulting in the user having a “night they can’t
remember”. With adolescents having limited access to alcohol, abusing their parents’ Ambien
isn’t uncommon. Although it would be a legitimate medicine that a doctor saw fit, those
prescribed it should keep in mind driving, or yielding heavy machinery (such as chainsaws) is,
by no means, a good idea while influenced by this drug. Eminem had a reasonably publicized
affair with zolpidem in 2009, after he started using it to help him sleep through the stresses of
his life.
2. Seroquel (Quetiapine)
Although antipsychotics are rarely thought of as “drugs of abuse”, quetiapine deserves
recognition on this list due to its huge recreational value in prison. Prescribed for schizophrenia,
bipolar disorders, and insomnia, Seroquel doesn’t seem, at all, like a drug you’d want anyone to
even know you’re prescribed. However, the tranquilizer has earned the name “Jailhouse Heroin”
among our citizens who are paying their debts to society. Abusers seek its anxiolytic (anxiety
reducing) effects, as well as its tendency to reduce feelings and provide a careless state of
mind. Prisoners commonly trade their meals and money for these pills, only to find their benefit
outweighed by the price they paid after the effects have ended. Even though this is a prison
drug if there ever was one, note that is also serves recreational use among the outside, as well.
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3. Dilaudid (hydromorphone)
Often prescribed for pain (and occasionally bad cough), Dilaudid is known as more of an “all or
nothing pharmaceutical”. This is because abusers can take well above the allowed dose and not
feel a bit of the euphoric opiate heaven he’s used to, or the said person may claim it’s the
closest to heaven they’ve ever been with a moderately low dose. The oral bioavailability (the
fraction of a substance that can be used by the bodily systems before it’s lost en route) of
hydromorphone is very low, therefore popping three 4mg “dilly dallies” may not blow one’s mind
in the least, but administering it through a needle could well be compared to intravenous heroin.
With all opiates being able to be injected via one method or another, Dilaudid may not seem
special, but it does have one unique property. It can be liquefied through “cold shaking”,
meaning hydromorphone requires no heat for water solubility. This factor is taken advantage of
by many heroin addicts in need of a shot; however the difficulty of abuse via oral administration
makes it one of the safer opiates to have around a house with adolescents.
4. Xanax (alprazolam)
Benzodiazepine abuse is very common among those self-medicating for stress and anxiety, but
one particular benzo, by the name of alprazolam, is also very common among recreational
users seeking a “high”. A physician will prescribe a patient Xanax for panic disorders, insomnia,
and, more rarely, social anxiety. Although it’s available in doses of .25, .5, and 1 milligram, the
most popular tablet on the street is the 2mg Xanax “bar”. They are either crushed and
insufflated or popped. With intranasal use especially, the onset is very rapid and instills
relaxation, reduced, alcohol-like inhibitions, and potent apathy in the user. Alprazolam, and
other benzodiazepines, like Valium, Klonopin, and Ativan, are abused to enhance sociability and
to let one “be themself” around social gatherings, like malls and parties. What makes benzos
more dangerous to abuse, versus opiates, are the withdrawals. A long time addicted user will
get panic attacks and seizures when he can’t redose.
5. Desoxyn (Methamphetamine)
No, you didn’t just misread that subtitle. Methamphetamine, or “speed”, “crank”, “ice”, ext. is
available by prescription in the United States, New Zealand, and Canada for ADHD treatment,
as well as obesity, due to its appetite suppressing effects. Good luck trying to get it legally
though, if you’re persuasive enough to convince a doctor that your ADHD is so bad, that only
meth can control you, you should seek a career in law. I bet Johnny Cochrane could’ve gotten a
script! Okay, not to get off topic. When Desoxyn is obtained, it obviously has very high street
value, for its drug and for its consistent dosing. A meth user never knows what he’s getting in a
bag he got off the street, but a 10mg Desoxyn tablet would be seen as a “good batch” all day.
6. Narcotic Syrups (Codeine & hydrocodone)
Prescription cough syrups (such as Tussoinex and Phenergan) containing narcotics such as
codeine and hydrocodone have become very popular among young adults through pop culture.
Several rappers have made it clear that they not only enjoy recreationally drinking “purple
drank”, but they encourage it, almost as much one would normally encourage a safer drug, like
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marijuana. Like other opiates, they instill euphoric, pleasantly itchy, and relaxing effects within
the drinker. A popular term “lean” describes putting a jolly rancher in your bottle for flavor.
Although codeine and hydrocodone are very rarely abused to the point of overdose, it should be
noted that the syrups are often combined with drugs like acetaminophen and guaifenesin, which
will cause bodily harm much more rapidly. Codeine and hydrocodone are also available in pill
form, under brand names Tylenol 1-4 and Vicodin, respectively.
7. Adderall (Mixed amphetamine salts)
The all-too-famous “speed in a pill”, Adderall is provided to adolescents like candy it seems. By
combining l-amp and d-amp in a 25% to 75% ratio, it can provide people with trouble
concentrating miraculous relief. But attention disorders are exceptionally easy to fake, and,
therefore, many high school entrepreneurs acquire it just to make extra cash from their friends
at
school.
Amphetamines,
ranging
from
Adderall
to
meth
to
Ecstasy
(methylenedioxymethamphetamine), are valued for their energetic, stimulating, and oftentimes
euphoric effects. Adderall, along with Ritalin, abuse is rampant among high school and college
students during exams, due to their ability to exponentially increase focus and motivation
8. Laudanum (Tincture of opium)
Adding a little history to our list, Laudanum was coined in early 17th century London, although
preparations of opium extractions date back quite a bit further. It is an alcoholic mixture of
powdered opium, varying in potency. The active ingredients, therefore, include codeine,
morphine, and ethanol. This potent mixture was treated as an alternative poison to English
users, viewed as more socially acceptable than smoking opium, which a good fraction of the
Chinese were addicted to at the time. Long before our modern Rx system, this medicine was
readily available to anyone, and was soon found to be no less harmful than nature’s own
narcotic preparation. The tincture continued to be used pharmaceutically in the States by many,
until the early 20th century when it was deemed unfit to consume without a doctor’s overseeing.
Its history in Europe and America is well known, but what is not is that it is actually still available
today. Laudanum remains available by prescription, and is most commonly used for newborns
that were born to opiate addicted mothers.
9. OxyContin (Oxycodone)
Also branded as Percocet with acetaminophen, as well as several others, oxycodone has
probably been responsible for more harm, in the past twenty years, than any other pill on this
list. It was synthesized by German scientists in the early 1900s, but not used widely in medicine
until much later. The drug gives users a blissful, heavenly euphoria that is almost unmatched in
the narcotic world. In the mid-90s Purdue manufactured OxyContin; a time released tablet
containing enough oxycodone to get a user high many times over, in the higher milligram doses.
When taken orally this provided chronic pain patients, with cancer and disabilities, a new
outlook on life. They could live pain free without taking pills consistently throughout the day.
When abused by chewing, insufflation, or injection this pill was the ultimate score until quite
recently. OxyContin is now manufactured via a formula that is much harder to abuse; however,
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Drug abuse and their effect
other preparations of oxycodone (e.g. Roxicodone) are still very popular in the opiate
community.
10. Opana (Oxymorphone)
The common Joe may have never heard of Opana before, but it is number one on this list
because it is becoming significantly more popular with abusers, now that OxyContin is nearly
useless to them. In the near future oxymorphone will likely be one of the most misused
painkillers on the market. It is similar to other narcotics, providing pain relief for those in need,
but its euphoria not only exceeds that of oxycodone, but some will argue heroin as well. A
person with a low tolerance will get an indescribably rich high off about one-eighth of a high
dose (40mg ER) Opana through insufflation. As more thrill seekers spread the word of Opana’s
potential, we will see oxymorphone become the new pharmaceutical dope; the drug of choice
for anyone with access to an unlocked medicine cabinet.
8. LIST OF ABUSED DRUGS (USED IN INDIA)
DRUG
COREX
COMPANY
PFIZER
MOLECULE
CODEINE
PHASPHATE
DOSAGE
SYRUP
AMOUNT
10mg/5ml
TOSSEX
PIRAMAL
HEALTH CARE
CODEINE
PHASPHATE
SYRUP
10mg/5ml
VILIUM
PIRAMAL
HEALTH CARE
DIGEPAM
TAB
2,5,10 mg /TAB
TRIKA
UNICAM
ALPRAZOLAM
TAB
0.25,0.5,1 mg/TAB
IODEX
GSK
GANDAPURO TEL
2gm, TURPINE TEL
400mg
OINTMENT
PER 10 gm
LOPEZ
PIRAMAL
HEALTH CARE
LORAZEPAM
TAB
1,2 mg/TAB
AVIL
AVENTIS
PHENIRAMINE
MALEATE
TAB
25,50 mg/TAB
NITROSON
SUN
NITRAZEPAM
TAB
5mg,10mg/TAB
FORTWIN INJ
RANBAXY
PANTOZOCINE
LACTATE
INJECTION
30mg/ml
GARDENAL
PIRAMAL
HEALTH CARE
PHENOBARBITONE
TAB
30,60 mg/TAB
LONAZEP
SUN PHARMA
CLONAZEPAM
TAB
0.25,0.5,1,2
mg/TAB
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Drug abuse and their effect
LIBRIUM
PIRAMAL
CHLORDIZEPOXIDE
TAB
10 mg/TAB
TEGRITAL
NOVARTIS
CARBAMAZEPINE
TAB
100,200,400
mg/TAB
ZOLFRESH
ABBOTT
ZOLPIDEM TITRATE
TAB
5,10 mg/TAB
EPTOIN
ABBOTT
PHENYTOIN
TAB
50,100 mg/TAB
PRAZOPRESS
SUN
PRAZOSIN
TAB
1,2 mg/TAB
CALMPOSE
RANBAXY
DIZEPAM
INJECTION
10 mg/2 ml
ATIVAN
WYETH
LORAZEPAM
TAB
1,2mg/TAB
NOOTROPIL
UCB
PIRACETAM
TAB
800mg/TAB
9. DESCRIPTION
(a) MOLECULAR AND CELLULAR BIOLOGY OF
ADDICTION
Addiction to alcohol, tobacco, and illegal drugs represents a substantial burden to
societies worldwide. In terms of health-related outcomes, addiction results in enormous direct
medical costs, premature mortality (tobacco alone may be responsible for 450,000 deaths
yearly in the United States), and disability. In terms of broader social costs, addiction results in
crime, negative impacts on families, derailed lives, and personal suffering. The major categories
of drugs most likely to produce addiction are psychostimulants (including cocaine and
amphetamines), opiates, ethanol, nicotine, marijuana, and phencyclidine-like drugs.
Understanding the molecular and cellular actions of addictive drugs is obligatory if we are to
better understand pathophysiology and develop potent pharmacotherapies to treat addiction. Of
course, the molecular and cellular information presented in this chapter cannot be applied
directly to the behavioural expression of addiction.
Acutely, addictive drugs are both rewarding (i.e., interpreted by the brain as intrinsically positive)and
reinforcing (i.e., behaviors associated with drug use tend to be repeated). With repeated use,
however, addictive drugs produce molecular changes that, within a vulnerable brain, promote
continued drug-taking behavior in a manner that becomes increasingly difficult to control. The central
feature of addiction is compulsive drug use—the loss of control over the apparently voluntary acts of
drug seeking and drug taking. Once it has taken hold, addiction tends to follow a chronic course with
periods of abstinence (that may or may not follow treatment), followed by relapse to active drug use.
Even after extended periods of drug abstinence, the risk of relapse remains high.
MOLECULAR TARGETS OF ADDICTIVE DRUGS
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The overall effect of each of the addictive drugs depends on the particular neurons and circuits that
express their molecular targets, and the nature of those targets. Thus, for example, morphine-like
opiates are analgesic and sedating, whereas cocaine is a
psychomotor stimulant; these
different properties are based on differences in localization and functional properties of the proteins
with which they interact,the -opioid receptor for morphine and the dopamine reuptake transporter
(DAT)for cocaine. However, as described in other chapters in this section, addictive drugs share the
ability to activate mesocorticolimbic dopamine projections that are critical substrates for both
rewarding and reinforcing effects of natural stimuli. Mesocorticolimbic dopamine projections originate
in the ventral tegmental area (VTA) of the ventral midbrain and project to structures that include the
nucleus accumbens (NAc)(a complex structure within the ventral striatum that is the best-established
substrate for reinforcement), and the prefrontal cerebral cortex.In vivo microdialysis studies have
indicated that most if not all addictive drugs, including cocaine, amphetamines, opiates, nicotine, and
ethanol, cause selective elevation of extracellular dopamine levels in the NAc, and blockade of
dopamine neurotransmission in this region attenuates most measurable reinforcing and rewarding
effects of addictive drugs. The powerful control over behavior exerted by addictive drugs is thought
to result from the brain’s inability to distinguish between the activation of reward circuitry by drugs
and natural activation of the same circuitry by useful behaviors (e.g., behavioral related to eating or
reproduction). Any activity, whether related to drug taking or survival, that activates this circuitry
tends to be repeated; however, activation of reward circuitry by addictive drugs can be much more
reliable and powerful than activation triggered by natural reinforcers, facilitating repetitive drug use,
and with it, the initiation of molecular mechanisms that may produce tolerance, dependence,
sensitization, and compulsive use. Although the mesocorticolimbic dopamine system is a site of
convergence for the rewarding effects of virtually all major classes of addictive drugs, these drugs
act by very different mechanisms.
PSYCHOSTIMULANTS
The best-characterized and most widely abused psychostimulants are cocaine and the
amphetamines. The details of their mechanisms of actions differ, but both result in increases of
extracellular dopamine and other monoamines and produce similar effects on behavior. In humans,
psychostimulants increase alertness and produce a sense of well being. In animal studies,
psychostimulants produce a dosedependent increase in locomotor activity at low doses and
stereotypies at high doses. If cocaine or amphetamine is used repeatedly, some acute drug effects
may diminish (tolerance), whereas others are enhanced (sensitization). Cocaine and amphetamines
produce their effects by potentiating monoaminergic transmission through actions on dopamine,
serotonin, and norepinephrine reuptake transporters. These proteins normally transport previously
released neurotransmitter back into the presynaptic nerve terminal, and thereby terminate
transmitter action. Cocaine binds to these transporters and competitively inhibits their functioning,
thereby increasing the duration of action of neurotransmitter released into the synaptic cleft.
Amphetamines and related drugs increase dopamine, serotonin, and
norepinephrine neurotransmission by acting as a substrate for their transporters. Amphetamines are
transported into the presynaptic terminal where they cause neurotransmitter release by reversing the
usual direction of transport (i.e.,causing transmitter to move into the synapse).
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(b) DESCRIPTION OF DRUGS
(1) Alprazolam (trade name Xanax)
It is a short-acting anxiolytic of the benzodiazepine class of psychoactive drugs. Alprazolam like
other benzodiazepines, binds to specific sites on the GABA (gamma-amino-butyric acid)
receptor. Alprazolam is commonly used and FDA approved for the medical treatment of panic
disorder, and anxiety disorders, such asgeneralized anxiety disorder (GAD) or social anxiety
disorder (SAD). Alprazolam is available for oral administration in compressed tablet(CT)
and extended-release capsule (XR) formulations. Alprazolam
possesses anxiolytic, sedative, hypnotic, skeletal muscle relaxant,anticonvulsant,
and amnestic properties.
Alprazolam has a fast onset of action and symptomatic relief. Ninety percent of peak benefits
are achieved within the first hour (Although onset may begin at 8-25 minutes of ingestion) of
using either preparation for panic disorder, and full peak benefits are achieved in 1.5 and 1.6
hours respectively. Peak benefits achieved for generalized anxiety disorder (GAD) may take up
to a week. Tolerance does not appear to develop to the anxiolytic effects but may develop to
the sedative effects within a couple of days. Withdrawal symptoms or rebound symptoms may
occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and
may necessitate a gradual dose reduction.
Medical uses
Alprazolam is mostly used to treat anxiety disorders, panic disorders, and nausea due
to chemotherapy. The FDA label advises that the physician should periodically reassess the
usefulness of the drug.
Panic disorder
Alprazolam is effective in the relief of moderate to severe anxiety and panic attacks. It however
is not a first line treatment, since the development of selective serotonin reuptake inhibitors, due
to concerns regarding tolerance, dependence and abuse. Evidence supporting the effectiveness
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of alprazolam in treating panic disorder has been limited to 4 to 10 weeks. However, people with
panic disorder have been treated on an open basis for up to 8 months without apparent loss of
benefit.
In the US alprazolam is FDA-approved for the treatment of panic disorder with or
without agoraphobia. Alprazolam is recommended by the World Federation of Societies of
Biological Psychiatry (WFSBP) for treatment-resistant cases of panic disorder where there is no
history oftolerance or dependence, as of 2002.
Anxiety disorders
In the US alprazolam is FDA-approved for the management of anxiety disorders (a condition
corresponding most closely to the APA Diagnostic and Statistical Manual DSM-III-R diagnosis of
generalized anxiety disorder) or the short-term relief of symptoms of anxiety. Anxiety associated
with depression is responsive to alprazolam. Demonstrations of the effectiveness by systematic
clinical study are limited to 4 months duration for anxiety disorder.
In the UK, alprazolam is recommended for the short-term treatment (2–4 weeks) of severe
acute anxiety. In one study, some long term, high-dosage users of alprazolam developed
reversible depression.
Nausea due to chemotherapy
Alprazolam may be used in combination with other medications for chemotherapy-induced
nausea and vomiting.
Pregnancy and lactation
Benzodiazepines cross the placenta, enter into the fetus and are also excreted with breast milk.
The use of benzodiazepines during pregnancy or lactation has potential risks. The use of
alprazolam
in
pregnancy
is
believed
to
be
associated
with congenital
abnormalities. Diazepam and chlordiazepoxide have a better safety profile in pregnancy than
alprazolam.
Women who are pregnant or are planning on becoming pregnant should avoid starting
alprazolam. Use in the last trimester may cause fetal drug dependence and withdrawal
symptoms in the post-natal period as well as neonatal flaccidity and respiratory
problems. However, in long-term users of benzodiazepines abrupt discontinuation due to
concerns of teratogenesis has a high risk of causing extreme withdrawal symptoms and a
severe rebound effect of the underlying mental health disorder. Spontaneous abortions may
also result from abrupt withdrawal of psychotropic medications including benzodiazepines.
Benzodiazepines, including alprazolam, are known to be excreted in human milk. Chronic
administration of diazepam to nursing mothers has been reported to cause their infants to
become lethargic and to lose weight.
Contraindications
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Benzodiazepines require special precaution if used in children and in alcohol- or drugdependent individuals. Particular care should be taken in pregnant or elderly patients, patients
with substance abuse history, particularly alcohol dependence and patients with comorbid
psychiatric disorders. Use of alprazolam should be avoided or carefully monitored by medical
professionals in individuals with the following conditions: myasthenia gravis, acute narrowangle glaucoma, severe liver deficiencies (e.g., cirrhosis), severe sleep apnea, pre-existing
respiratory
depression,
marked
neuromuscular
respiratory
weakness
including
unstable myasthenia gravis, acute pulmonary insufficiency, chronic psychosis, hypersensitivity
or allergy to alprazolam or other drugs in the benzodiazepine class, borderline personality
disorder (may induce suicidality and dyscontrol).
Like all central nervous system depressants, including alcohol, alprazolam in larger-than-normal
doses can cause significant deterioration in alertness, combined with increased feelings of
drowsiness, especially in those unaccustomed to the drug's effects. People driving or
conducting activities that require vigilance should exercise caution in using alprazolam or any
other depressant. Elderly individuals should be cautious in the use of alprazolam due to the
possibility of increased susceptibility to side-effects, especially loss of coordination and
drowsiness
Adverse effect
Xanax (alprazolam) 2 mg tri-score tablets
Allergic reactions are unlikely to occur. The only common side effect is sleepiness when
treatment is initiated.
Possible side effects include:
1. Disinhibition
2. Change in libido
3. Jaundice (very rare)
4. Hallucinations (rare)
5. Dry mouth (infrequent)
6. Ataxia, slurred speech
7. Suicidal ideation (rare)
8. Urinary retention (infrequent)
9. Skin rash, respiratory depression, constipation
10. Anterograde amnesia and concentration problems
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Drug abuse and their effect
11. Drowsiness, dizziness, lightheadness, fatigue, unsteadiness and
impaired coordination, vertigo
Paradoxical reactions
Although unusual, the following paradoxical reactions have been shown to occur:
1. Aggression
2. Rage, hostility
3. Twitches and tremor
4. Mania, agitation, hyperactivity and restlessness
Food and drug interactions
Alprazolam is primarily metabolised via CYP3A4. Combining CYP3A4 inhibitors such
as cimetidine, erythromycin, fluoxetine, fluvoxamine, itraconazole, ketoconazole, nefazodone,pr
opoxyphene, and ritonavir delay the hepatic clearance of alprazolam, which may result in
excessive accumulation of alprazolam. This may result in exacerbation of its adverse effect
profile.
Imipramine and desipramine have been reported to be increased an average of 31% and 20%,
respectively, by the concomitant administration of alprazolam tablets in doses up to 4 mg/day.
Combined oral contraceptive pills reduce the clearance of alprazolam, which may lead to
increased plasma levels of alprazolam and accumulation.
Alcohol is one of the most important and common interactions. Alcohol and benzodiazepines
such as alprazolam taken in combination have a synergistic effect on one another, which can
cause severe sedation, behavioral changes, and intoxication. The more alcohol and alprazolam
taken the worse the interaction. Combination of alprazolam with the herb kava can result in the
development of a semi-comatose state. Hypericum conversely can lower the plasma levels of
alprazolam and reduce its therapeutic effect.
Overdose
Overdoses of alprazolam can be mild to severe depending on how much of the drug is taken
and any other drugs that have been taken.
1. Alprazolam overdoses cause excess central nervous system (CNS) depression and may
include one or more of the following symptoms:
2. Somnolence (sleepy state)
3. Hypotension (low blood pressure)
4. Hypoventilation (shallow breathing)
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Drug abuse and their effect
5. Impaired motor functions
6. Dizziness
7. Impaired balance
8. Muscle weakness
9. Impaired or absent reflexes
10. Fainting
11. Coma
12. Death (very rare)
Dependence and withdrawal
Alprazolam, like other benzodiazepines, binds to specific sites on the GABA gamma-aminobutyric acid receptor. When bound to these sites, which are referred to as benzodiazepine
receptors, it modulates the effect of GABA A receptors and, thus, GABAergic neurons. Longterm use causes adaptive changes in the benzodiazepine receptors, making them less sensitive
to stimulation and less powerful in their effects.
Withdrawal and rebound symptoms occur commonly and necessitate a gradual reduction in
dosage to minimize withdrawal effects when discontinuing.
Not all withdrawal effects are evidence of true dependence or withdrawal. Recurrence of
symptoms such as anxiety may simply indicate that the drug was having its expected antianxiety effect and that, in the absence of the drug, the symptom has returned to pretreatment
levels. If the symptoms are more severe or frequent, the patient may be experiencing a rebound
effect due to the removal of the drug. Either of these can occur without the patient's actually
being drug-dependent.
Alprazolam and other benzodiazepines may also cause the development of physical
dependence, tolerance, and benzodiazepine withdrawal symptoms during rapid dose reduction
or cessation of therapy after long-term treatment. There is a higher chance of withdrawal
reactions if the drug is administered in a higher dosage than recommended, or if a patient stops
taking the medication altogether without slowly allowing the body to adjust to a lower-dosage
regimen.
Pharmacology
Alprazolam is classed as a high-potency benzodiazepine and is a
triazolobenzodiazepine, namely a benzodiazepine with a triazole ring attached to its structure.
Benzodiazepines produce a variety of therapeutic and adverse effects by binding to the
benzodiazepine receptor site on the GABAA receptor and modulating the function of the GABA
receptor, the most prolific inhibitory receptor within the brain. The GABA chemical and receptor
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Drug abuse and their effect
system mediates inhibitory or calming effects of alprazolam on the nervous system. The
GABAA receptor is made up of 5 subunits out of a possible 19, and GABAA receptors made up
of different combinations of subunits have different properties, different locations within the
brain, and, importantly, different activities with regard to benzodiazepines. Benzodiazepines and
in particular alprazolam causes a marked suppression of the hypothalamicpituitary-adrenal axis.
The therapeutic properties of alprazolam are similar to other benzodiazepines and
include anxiolytic, anticonvulsant, muscle relaxant, hypnotic and amnesic.
Pharmacokinetics(ADME)
Absorption
Following oral administration, alprazolam is readily absorbed. Peak concentrations in the
plasma occur in one to two hours following administration. Plasma levels are proportionate to
the dose given; over the dose range of 0.5 to 3.0 mg, peak levels of 8.0 to 37 ng/mL were
observed. Using a specific assay methodology, the mean plasma elimination half-life of
alprazolam has been found to be about 11.2 hours (range: 6.3 to 26.9 hours) in healthy adults.
Distribution
In vitro, alprazolam is bound (80 percent) to human serum protein. Serum albumin accounts for
the majority of the binding.
Metabolism/Elimination
Alprazolam is extensively metabolized in humans, primarily by cytochrome P450 3A4 (Cyp3A4),
to two major metabolites in plasma: 4-hydroxyalprazolam and α- hydroxyalprazolam. A
benzophenone derived from alprazolam is also found in humans. Theirs half-lives appear to be
similar to that of alprazolam. The plasma concentrations of 4-hydroxyalprazolam and αhydroxyalprazolam relative to unchanged alprazolam coincentration were always less than 4%.
The reported relative potencies in benzodiazepines receptor binding experiments and in animals
models of induced seizure inhibition are 0.2 and 0.66, respectively, for 4-hydroxyalprazolam and
α-hydroxyalprazolam. Such low concentrations and lesser potencies of 4-hydroxyalprazolam
and α-hydroxyalprazolam suggest that they are unlikely to contribute much to the
pharmacological effects of alprazolam. The benzophenone metabolite is essentially inactive.
Alprazolam and its metabolites are excreted primarily in the urine.
Chemistry
Alprazolam is a chemical analog of triazolam that differs by the absence of a chlorine atom in
the o-position of the 6-phenyl ring. The same scheme that was used to make triazolam can be
used to make alprazolam, with the exception that it begins with 2-amino-5chlorobenzophenone. However, a non-standard way of making alprazolam has been suggested,
which comes from 2,6-dichloro-4-phenylquinoline, the reaction of which with hydrazine gives 6chloro-2-hydrazino-4-phenylquinoline. Boiling this with triethyl orthoacetate in xylene leads to
the heterocyclization into a triazole derivative. The resulting product undergoes oxidative
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cleavage using sodium periodate and ruthenium dioxide in an acetone–water system to give 2[4-(3′-methyl-1,2,4-triazolo)]-5-chlorobenzophenone. Oxymethylation of the last
using formaldehyde and subsequent substitution of the resulting hydroxyl group by phosphorus
tribromide,gives 2-[4-(3′-methyl-5′-bromomethyl-1,2,4-triazolo)]-5-chlorobenzophenone.
Substitution of the bromine atom with an amino group using ammonia and the spontaneous,
intramolecular heterocyclization following that reaction gives alprazolam.
History
Alprazolam was first released by Upjohn (now a part of Pfizer). It is covered under U.S. Patent
3,987,052, which was filed on 29 October 1969, granted on 19 October 1976, and expired in
September 1993. Alprazolam was released in 1981. The first approved indication was panic
disorder.
(2) AVIL
Pheniramine maleate (fen-eye-r-a-mean mal-e-ate)
uses
Avil Tablets contain pheniramine maleate, a medicine used to treat allergic conditions such as hayfever,
runny nose, itching skin and skin rashes. It is also used in the prevention and treatment of inner ear
disorders (eg Meniere's disease) and travel sickness.
Avil is one of a group of medicines called 'antihistamines' which works by blocking the action of histamine.
When you must not take it
1. Do not take Avil if you:
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2. are taking an antidepressant medicine known as a MAO Inhibitor
3. are male and you have an enlarged prostate
4. Do not take Avil if you are allergic to it or any of the ingredients listed at the end of this leaflet.
5. Some symptoms of an allergic reaction include skin rash, itching, asthma, wheezing, shortness of
breath or swelling of the fact, lips or tongue, which may cause difficulty in swallowing or
breathing, fainting.
6. Do not take it after the expiry date (EXP) printed on the pack.
7. If you take it after the expiry date has passed, it may not work as well.
8. Do not take it if the packaging is torn or shows signs of tampering.
9. Do not give Avil to a premature or newborn baby.
Before you take it
1. Tell your doctor or pharmacist if you have allergies to:
2. any of the ingredients listed at the end of this leaflet
3. any other medicines
4. any other substances, such as foods, preservatives or dyes
5. Tell your doctor or pharmacist if you are pregnant or intend to become pregnant.
6. Your doctor or pharmacist will discuss the risk and benefits of taking it if you are pregnant.
7. Tell your doctor or pharmacist if you are breastfeeding or planning to breastfeed.
8. If there is a need to consider Avil while you are breastfeeding, your doctor or pharmacist will
discuss with you the benefits and risks of taking it.
9. Tell your doctor or pharmacist if you have or have had any medical conditions, especially the
following:
10. an enlarged prostate
11. glaucoma (high pressure in the eye)
12. breathing problems, including asthma or bronchitis
13. heart disease
14. Tell your doctor or pharmacist if you plan to have surgery.
15. If you have not told your doctor or pharmacist about any of the above, tell them before you take
Avil.
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Taking other medicines
1. Tell your doctor or pharmacist if you are taking any other medicines, including any that you buy
without a prescription from your pharmacy, supermarket or health food store.
2. Some medicines and Avil may interfere with each other. These include:
3. antidepressants known as MAO inhibitors
4. atropine and other anticholinergic drugs
5. alcohol
6. sedative drugs
7. Avil may cause drowsiness and may increase the effects of alcohol and other sedative drugs. If
affected, do not drive a motor vehicle or operate machinery.
8. You might get used to the sedative effect after a few days of treatment, however you may prefer
to change to a non-sedating antihistamine.
9. Please discuss this option with your pharmacist.
How much to take
1. Adults and children over 10 years:
2. Half to 1 tablet up to 3 times daily.
3. Children 5 - 10 years:
4. Half a tablet up to 3 times daily.
5. Not recommended for children under 5 years of age.
6. To prevent travel sickness, it is recommended that the first dose be taken at least 30 minutes
before travelling.
7. Ask your doctor or pharmacist if you are unsure of the correct dose for you.
8. They will tell you exactly how much to take.
Side Effects
All medicines can have some unwanted side effects. Sometimes they are serious, most of the time they
are not. Your doctor or pharmacist has weighed the risks of using this medicine against the benefits they
expect it will have for you. Do not be alarmed by this list of possible side effects. You may not experience
any of them.
1. Drowsiness nervousness, irritability, incoordination, lack of concentrationdizziness
2. nausea and vomiting
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3. difficulty passing urine
4. Tell your doctor immediately if you notice any of the following:
5. changes in your usual behaviour or mood
6. severe sedation, confusion or restlessness
7. hallucinations
8. vision problems
9. irregular heart beat
10. If any of the following happen, stop taking this medicine and tell your doctor immediately, or go to
Accident and Emergency at your nearest hospital:
11. swelling of the face, lips, mouth or throat, which may cause difficulty in swallowing or breathing
12. hives
13. fainting
14. yellowing of the skin and eyes (jaundice)
15. These may be serious side effects. You may need urgent medical attention. Serious side effects
are rare.
16. Ask your doctor or pharmacist to answer any questions you may have.
Storage
1. Keep your tablets in the blister pack until it is time to take them.
2. If you take the tablets out of the box or the blister pack, they may not keep well.
3. Keep Avil in a cool dry place where the temperature stays below 30 degrees C. Do not store Avil
or any other medicine in the bathroom or near a sink. Do not leave it in the car or on window sills.
4. Heat and dampness can destroy some medicines.
5. Keep it where children cannot reach it.
6. A locked cupboard at least one-and-a-half metres above the ground is a good place to store
medicines.
Disposal
If your doctor or pharmacist tells you to stop taking or giving Avil or the expiry date has passed, ask your
pharmacist what to do with any medicine which is left over.
Return any unused medicine to your pharmacist.
Product description
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What it looks like
Avil tablets are round white tablets with a single breakline on one face and DAR inscribed on both sides
of the line. They come in packs of 10 and 50 tablets.
Ingredients
Active Ingredient
Avil tablets contain the active ingredient pheniramine maleate. There is 45.3 mg of pheniramine maleate
in every tablet.
Inactive Ingredients
maize starch
sodium starch glycollate
lactose
colloidal silica
microcrystalline cellulose
magnesium stearate
Avil preparations do not contain gluten, tartrazine or azo dyes.
(3) Diazepam Valium
GENERIC NAME- diazepam
BRAND NAME- Valium, Diastat
DRUG CLASS:
Diazepam is an anti-anxiety medication in the benzodiazepine family, the same family that
includes alprazolam (Xanax), clonazepam (Klonopin), lorazepam (Ativan), flurazepam
(Dalmane), and others. Diazepam and other benzodiazepines act by enhancing the effects of
gamma-aminobutyric acid (GABA) in the brain. GABA is a neurotransmitter (a chemical that
nerve cells use to communicate with each other) that inhibits activity in the brain. It is believed
that excessive activity in the brain may lead to anxiety or other psychiatric disorders.
PREPARATIONS:
Tablets: 2, 5, and 10 mg. Solution: 5 mg/ml. Injection: 5 mg/ml. Rectal Gel: 2.5, 10, and 20 mg.
STORAGE:
Diazepam should be stored at room temperature, 15-30°C (59-86°F).
PRESCRIBED FOR:
Diazepam is used for the treatment of anxiety disorders. Diazepam also is used for the
treatment of agitation, tremors, delirium, seizures, and hallucinations resulting from alcohol
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withdrawal. It is used for the treatment of seizures and relief of muscle spasms in some
neurological diseases.
DOSING:
Diazepam may be taken with or without food. Diazepam is metabolized by the liver and
excreted mainly by the kidney. Dosages of diazepam may need to be lowered in patients with
abnormal kidney function. The usual oral diazepam dose is 2-10 mg given 2-4 times daily. The
usual rectal dose is 0.2-0.5 mg/kg and depends on the age of the patient.
DRUG INTERACTIONS:
Alcohol or medications that cause sedation may add to the sedative effects of diazepam.
Patients taking benzodiazepines should avoid such combinations.
Cimetidine (Tagamet), ketoconazole (Nizoral), omeprazole (Prilosec,
Rapinex), fluvoxamine (Luvox), and fluoxetine (Prozac) may prolong the effects of diazepam by
inhibiting liver enzymes that break down diazepam. Dosages may need to be decreased when
these drugs are used with diazepam.
PREGNANCY:
Benzodiazepines, such as diazepam, can cause fetal abnormalities and should not be used
during pregnancy.
NURSING MOTHERS:
Diazepam is excreted in breast milk and can affect nursing infants. Therefore, diazepam should
not be used by women who are nursing.
SIDE EFFECTS:
The most frequent side effects of diazepam are drowsiness, fatigue, and ataxia (loss of
balance). Rarely, diazepam causes a paradoxical reaction with excitability, muscle spasm, lack
of sleep, and rage.Confusion, depression, speech problems, and double vision are also rare
side effects of diazepam.
Diazepam can lead to addiction (dependency), especially when higher dosages are used over
prolonged periods of time. In patients addicted to diazepam or after prolonged use, abrupt
discontinuation of the medicine may cause symptoms of withdrawal
(insomnia, headaches, nausea, vomiting, lightheadedness, sweating, anxiety, and fatigue).
Seizures can occur in more severe cases of withdrawal. Therefore, after extended use,
diazepam should be slowly tapered under a doctor's supervision rather than abruptly stopping
the medication.
Muscle Cramps
Muscle cramps are involuntarily and forcibly contracted muscles that do not relax. Extremely
common, any muscles that have voluntary control, including some organs, are subject to cramp.
Since there is such variety in the types of muscle cramps that can occur, many causes and
preventative medications are known. Stretching is the most common way to stop or prevent
most muscle cramps.
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Dizziness
Dizziness is a symptom that is often applies to a variety of sensations including lightheadedness
and vertigo. Causes of dizziness include low blood pressure, heart problems, anemia,
dehydration, and more. Treatment of dizziness depends on the cause.
Muscle Spasms
Muscle spasms are involuntary muscle contractions that come on suddenly and are usually
quite painful. Dehydration, doing strenuous exercise in a hot environment, prolonged muscle
use, and certain diseases of the nervous system may cause muscle spasms. Symptoms and
signs of a muscle spasm include an acute onset of pain and a possible bulge seen or felt
beneath the skin where the muscle is located. Gently stretching the muscle usually resolves a
muscle spasm.
Anxiety
Anxiety is a feeling of apprehension and fear characterized by physical symptoms. Anxiety
disorders are serious medical illnesses that affect approximately 19 million American adults.
Temporomandibular Joint Disorder (TMJ)
Temporomandibular joint disorder, or TMJ, is a disorder of the temporomandibular joint(s) that
causes signs and symptoms including ear pain, bite problems, headaches, dizziness, clicking
sounds in the jaw, tinnitus and/or locked jaws. Behaviors or conditions that can lead to TMJ
include teeth grinding or clenching, fingernail biting, habitual gum chewing, trauma to the jaw,
stress, and occupational hazards. Treatment for TMJ may include heat, ice, a soft diet,
antiinflammatory medications, physical therapy, stress management, occlusal therapy,
correction of bite abnormalities, and surgery.
Stress
Stress occurs when forces from the outside world impinge on the individual. Stress is a normal
part of life. However, over-stress, can be harmful. There is now speculation, as well as some
evidence, that points to the abnormal stress responses as being involved in causing various
diseases or conditions.
Seizure (Epilepsy)
Epilepsy is a brain disorder in which the person has seizures. There are two kinds of seizures,
focal and generalized. There are many causes of epilepsy. Treatment of epilepsy (seizures)
depends upon the cause and type of seizures experienced.
Wisdom Teeth
Wisdom teeth are the third set of molars that people get in their late teens or early twenties.
Impacted wisdom teeth that only partially erupt allows for an opening for bacteria to enter
around the tooth and cause an infection, which results in pain, swelling, jaw stiffness, and
general illness. Before your wisdom teeth are pulled, the teeth and the surrounding tissue will be
numbed with a local anesthetic. Recovery from wisdom tooth removal depends upon the
difficulty of the extraction.
Cerebral Palsy
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Cerebral palsy (CP) is an abnormality of motor function and postural tone acquired at an early
age (even before birth). Cerebral palsy is generally caused by brain trauma. Types of cerebral
palsy include: spastic, dyskinetic (dystonic or choreoathetoid), hypotonic, and mixed types.
There is no cure for cerebral palsy, and treatment is generally managing the symptoms of the
condition.
Dislocated Shoulder
The shoulder is the most often dislocated joint in the body due to its mobility. Dislocation occurs
when the head of the humerus is dislocated from its socket. Symptoms and signs of a shoulder
dislocation include nausea and vomiting, lightheadedness, weakness, and sweating. There are
various methods of reducing a dislocation and returning the humeral head to its normal place.
The method for reduction of a shoulder dislocation depends upon the type of dislocation, the
patient, the situation, and the clinician's experience. Intravenous narcotics and muscle relaxants
are often administered to relax the muscles and relieve pain.
Insomnia
Insomnia is the perception or complaint of inadequate or poor-quality sleep because of difficulty
falling asleep; waking up frequently during the night with difficulty returning to sleep; waking up
too early in the morning; or unrefreshing sleep. Secondary insomnia is the most common type of
insomnia. Treatment for insomnia include lifestyle changes, cognitive behavioral therapy, and
medication.
Agoraphobia
Agoraphobia is a fear of being outside or of being in a situation from which escape would be
impossible. Symptoms include anxiety, fear, disorientation, rapid heartbeat, diarrhea, or
dizziness. Treatment may incorporate psychotherapy, self-exposure to the anxiety-causing
situation, and medications such as SSRIs, benzodiazepines, and beta blockers.
Meniere's Disease
Meniere disease (idiopathic endolymphatic hydrops) is an inner ear disorder with symptoms that
include vertigo, tinnitus, hearing loss, and the sensation of ear fullness. Diuretics, anti-vertigo,
anti-nausea and low salt diets are the primary treatment for Meniere disease. Surgery may be
recommended if the vertigo cannot be controlled with medication.
Phobias
Phobias are unrelenting fears of activities (social phobias), situations (agoraphobia), and
specific items (arachnophobia). There is thought to be a hereditary component to phobias,
though there may be a cultural influence or they may be triggered by life events. Symptoms and
signs of phobias include having a panic attack, shaking, breathing troubles, rapid heart beat,
and a strong desire to escape the situation. Treatment of phobias typically involves
desensitization, cognitive behavioral therapy, and medications such as selective serotonin
reuptake inhibitors and beta blockers.
Dystonia
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Dystonia disorders cause involuntary movements and prolonged muscle contraction, resulting in
twisting body motions, tremor, and abnormal posture. There are many forms of dystonia. Some
types of dystonia respond to dopamine, or can be controlled with
Brief Psychotic Disorder
Brief psychotic disorder dedative-type medications, or surgery. is a short-term mental illness
that features psychotic symptoms. There are three forms of brief psychotic disorder. The
first occurs shortly after a major stress, the second has no apparent trauma that triggers the
illness, and the third is associated with postpartum onset. Symptoms include hallucinations,
delusions, unusual behavior, disorientation, changes in eating and sleeping, and speech that
doesn't make sense. Treatment typically involves medication and psychotherapy.
Nerve Disease and Bladder Control
A nerve problem might affect your bladder control if the nerves that are supposed to carry
messages between the brain and the bladder do not work properly. Such problems include urine
retention, poor control of sphincter muscles, and overactive bladder. Treatment depends upon
the cause of the nerve damage and resulting type of bladder control problem.
Stiff-Person Syndrome
Stiff-Person syndrome is a neurological disorder associated with features of an autoimmune
disease. Signs and symptoms of Stiff-Person syndrome include a heightened sensitivity to
stimuli (noise, touch, emotional distress) and fluctuating muscle rigidity of the trunk and limbs.
Conditions associated with Stiff-Person syndrome include thyroiditis, vitiligo, pernicious anemia,
and diabetes. Treatment for Stiff-Person syndrome is generally medication to control symptoms.
The most obvious symptoms of brief psychotic disorder include:
1. Hallucinations: Hallucinations are sensory perceptions of things that aren't actually
present, such as hearing voices, seeing things that aren't there, or feeling sensations on
your skin even though nothing is touching your body.
2. Delusions: These are false beliefs that the person refuses to give up, even in the face of
contradictory facts.
Other symptoms of brief psychotic disorder include:
1. Disorganized thinking
2. Speech or language that doesn't make sense
3. Unusual behavior and dress
4. Problems with memory
5. Disorientation or confusion
6. Changes in eating or sleeping habits, energy level, or weight
7. Inability to make decisions
(4) Lorazepam
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Lorazepam (initially marketed under the brand names Ativan and Temesta) is a high-potency,
short- to intermediate-acting, 3-hydroxybenzodiazepine drug that has all six intrinsic
benzodiazepine.
Effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant, antiemetic and muscle
relaxant. Lorazepam is used for the short-term treatment of anxiety, insomnia, acute seizures
including status epilepticus and sedation of hospitalized patients, as well as sedation of
aggressive patients.
IUPAC name
(RS)-9-chloro-6-(2-chlorophenyl)-4-hydroxy2,5-diazabicyclo[5.4.0]undeca5,8,10,12-tetraen-3-one
Medical uses
1. Lorazepam has relatively potent anxiolytic effects and its best-known indication is the
short-term management of severe anxiety; the FDA advises against use of
benzodiazepines such as lorazepam for longer than two to four weeks. It is fast acting,
and useful in treating fast onset panic anxiety.
2. Lorazepam has strong sedative/hypnotic effects, and the duration of clinical effects from
a single dose makes it an appropriate choice for the short-term treatment of insomnia, in
particular in the presence of severe anxiety. It has a fairly short duration of action.
Withdrawal symptoms, includingrebound insomnia and rebound anxiety, may occur after
only seven days' administration of lorazepam.
3. Lorazepam is sometimes used for individuals receiving mechanical ventilation. However,
in critically ill patients, propofol has been found to be superior to lorazepam both in
effectiveness and overall cost; as a result, the use of propofol for this indication is now
encouraged, whereas the use of lorazepam is discouraged.
4. Its relatively potent amnesic effect, with its anxiolytic and sedative effects, makes
lorazepam useful as premedication. It is given before a general anaesthetic to reduce
the amount of anaesthetic agent required, or before unpleasant awake procedures, such
as in dentistry or endoscopies, to reduce anxiety, to increase compliance, and to induce
amnesia for the procedure. Oral lorazepam is given 90 to 120 minutes before
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procedures, andintravenous lorazepam as late as 10 minutes before
procedures. Lorazepam is sometimes used as an alternative to midazolam in palliative
sedation. In intensive care units lorazepam is sometimes used to
produce anxiolysis, hypnosis, and amnesia.
5. Intravenous diazepam or lorazepam are first-line treatments for convulsive status
epilepticus. Lorazepam is more effective than diazepam in the treatment of status
epilepticus. However, phenobarbitol has a superior success rate compared to lorazepam
and other drugs, at least in the elderly.
Formulation
1. Pure lorazepam is an almost white powder that is nearly insoluble in water and oil. In
medicinal form, it is mainly available as tablets and a solution for injection, but, in some
locations, it is also available as a skin patch, an oral solution, and a sublingual tablet.
2. Lorazepam tablets and syrups are administered by mouth only. Lorazepam tablets of the
Ativan brand also contain lactose, microcrystalline cellulose, polacrilin, magnesium
stearate, and colouring agents (indigo carmine—E132—in blue tablets and tartrazine—
E102— in yellow tablets).
3. Lorazepam injectable solution is administered either by deep intramuscular injection or
by intravenous injection. The injectable solution comes in 1 mlampoules containing 2 or
4 mg of lorazepam. The solvents used are polyethylene glycol 400 and propylene glycol.
As a preservative, the injectable solution contains benzyl alcohol. Toxicity from
propylene glycol has been reported in the case of a patient receiving a continuous
lorazepam infusion. Intravenous injections should be given slowly and patients closely
monitored for side effects, such as respiratory depression, hypotension, or loss of airway
control.
4. Peak effects roughly coincide with peak serum levels, which occur 10 minutes after
intravenous injection, up to 60 minutes after intramuscular injection, and 90 to 120
minutes after oral administration, but initial effects will be noted before this. A clinically
relevant lorazepam dose will normally be effective for six to 12 hours, making it
unsuitable for regular once-daily administration, so it is usually prescribed as two to four
daily doses when taken regularly, but this may be extended to five or six, especially in
the case of elderly patients who could not handle large doses at once.
Adverse effects
Any of the five intrinsic benzodiazepine effects possessed by lorazepam (sedative/hypnotic,
muscle relaxant, anxiolytic, amnesic, and anticonvulsant) may be considered as adverse or side
effects if unwanted. Adverse effects can include sedation and hypotension; the effects of
lorazepam are increased in combination with other CNS depressant drugs. Other adverse
effects include confusion, ataxia, anterograde amnesia and hangover effects. With long-term
use of benzodiazepines, it is unclear whether cognitive impairments fully return to normal after
cessation of therapy; cognitive deficits persist for at least six months after withdrawal, but longer
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than six months may be required for recovery of cognitive function. Lorazepam appears to have
more profound adverse effects on memory than other benzodiazepines; it impairs
both explicit and implicit memory. In the elderly, falls may occur as a result of benzodiazepines.
Adverse effects are more common in the elderly, and they appear at lower doses than in
younger patients. Benzodiazepines can cause or worsen depression. Paradoxical effects can
also occur, such as worsening of seizures, or paradoxical excitement; paradoxical excitement is
more likely to occur in the elderly, children, those with a history of alcohol abuse and in people
with a history of aggression or anger problems. Lorazepam's effects are dose-dependent,
meaning the higher the dose, the stronger the effects (and side effects) will be. Using the
smallest dose needed to achieve desired effects lessens the risk of adverse effects.
Sedation is the side effect for which most patients complain. In a group of around 3500 patients
treated for anxiety, the most common side effects complained of from lorazepam were sedation
(15.9%), dizziness (6.9%), weakness (4.2%), and unsteadiness (3.4%). Side effects such as
sedation and unsteadiness increased with age. Cognitive impairment, behavioural disinhibition
and respiratory depression as well as hypotension may also occur.
1. Paradoxical effects: In some cases, paradoxical effects can occur with benzodiazepines,
such as increased hostility, aggression, angry outbursts, and psychomotor agitation. These
effects are seen as more common with lorazepam than other benzodiazepines. Paradoxical
effects are more likely to occur with higher doses, in patients with pre-existing personality
disordersand those with a psychiatric illness. Frustrating stimuli may trigger such reactions,
though the drug may have been prescribed to help the patient cope with such stress and
frustration in the first place. As paradoxical effects appear to be dose-related, they usually
subside on dose reduction or on complete withdrawal of lorazepam.
2. Suicidality: Benzodiazepines may sometimes unmask suicidal ideation in depressed
patients, possibly through disinhibition or fear reduction. The concern is that, though
relatively nontoxic in themselves, benzodiazepines may inadvertently become facilitators of
suicidal behaviour. Lorazepam should, therefore, not be prescribed in high doses or as the
sole treatment in depression, but only with an appropriate antidepressant
3. Amnesic effects: Among benzodiazepines, lorazepam has relatively strong amnesic effects,
but patients soon develop tolerance to this with regular use. To avoid amnesia (or excess
sedation) being a problem, the initial total daily lorazepam dose should not exceed 2 mg.
This also applies to use for night sedation. Five participants in a sleep study were
prescribed lorazepam 4 mg at night, and the next evening, three subjects unexpectedly
volunteered memory gaps for parts of that day, an effect that subsided completely after two
to three days' use. Amnesic effects cannot be estimated from the degree of sedation
present, since the two effects are unrelated.
Contraindications
Lorazepam should be avoided in people with:
1. Allergy or hypersensitivity – Past hypersensitivity or allergy to lorazepam, to any
benzodiazepine, or to any of the ingredients in lorazepam tablets or injections
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2. Severe respiratory failure – Benzodiazepines, including lorazepam, may depress central
nervous system respiratory drive and are contraindicated in severe respiratory failure. An
example would be the inappropriate use to relieve anxiety associated with acute severe
asthma. The anxiolytic effects may also be detrimental to a patient's willingness and ability
to fight for breath. However, if mechanical ventilation becomes necessary, lorazepam may
be used to facilitate deep sedation.
3. Acute intoxication – Lorazepam may interact synergistically with the effects of alcohol,
narcotics, or other psychoactive substances. It should, therefore, not be administered to a
drunk or intoxicated person.
4. Ataxia – This is a neurological clinical sign, consisting of unsteady and clumsy motion of the
limbs and torso, due to failure of gross muscle movement coordination, most evident on
standing and walking. It is the classic way in which acute alcohol intoxication may affect a
person. Benzodiazepines should not be administered to already-ataxic patients.
5. Acute narrow-angle glaucoma – Lorazepam has pupil-dilating effects, which may further
interfere with the drainage of aqueous humour from the anterior chamber of the eye, thus
worsening narrow-angle glaucoma.
6. Sleep apnea – Sleep apnea may be worsened by lorazepam's central nervous system
depressant effects. It may further reduce the patient's ability to protect his or her airway
during sleep.
7. Myasthenia gravis – This condition is characterised by muscle weakness, so a muscle
relaxant such as lorazepam may exacerbate symptoms.
8. Pregnancy and breast feeding – Lorazepam belongs to the Food and Drug
Administration (FDA) pregnancy category D, which means it is likely to cause harm to the
developing baby, if taken during the first trimester of pregnancy. Evidence is inconclusive
whether lorazepam, if taken early in pregnancy, results in reduced intelligence,
neurodevelopmental problems, physical malformations in cardiac or facial structure, or other
malformations in some newborns.
Tolerance and dependence
Dependence typified by a withdrawal syndrome occurs in about one-third of individuals who are
treated for longer than four weeks with a benzodiazepine. Higher doses and longer periods of
use increase the risk of developing a benzodiazepine dependence. Potent benzodiazepines,
such as lorazepam, alprazolam, and triazolam, have the highest risk of causing a dependence.
Tolerance to benzodiazepine effects develops with regular use. This is desirable with amnesic
and sedative effects, but undesirable with anxiolytic, hypnotic, and anticonvulsant effects.
Patients at first experience drastic relief from anxiety and sleeplessness, but symptoms
gradually return, relatively soon in the case of insomnia, but more slowly in the case of anxiety
symptoms. After four to six months of regular benzodiazepine use, evidence of continued
efficacy declines. If regular treatment is continued for longer than this, dose increases may be
necessary to maintain effects, but treatment-resistant symptoms may in fact be benzodiazepine
withdrawal symptoms. Due to the development of tolerance to the anticonvulsant effects,
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Drug abuse and their effect
benzodiazepines are generally not recommended for long-term use for the management of
epilepsy. Increasing the dose may overcome tolerance, but tolerance may then develop to the
higher dose and adverse effects may persist and worsen. The mechanism of tolerance to
benzodiazepines is complex and involves GABA HYPERLINK "http://en.wikipedia.org/wiki/GABAA_receptor" HYPERLINK
"http://en.wikipedia.org/wiki/GABAA_receptor" HYPERLINK "http://en.wikipedia.org/wiki/GABAA_receptor"A HYPERLINK
"http://en.wikipedia.org/wiki/GABAA_receptor" HYPERLINK
"http://en.wikipedia.org/wiki/GABAA_receptor" HYPERLINK
"http://en.wikipedia.org/wiki/GABAA_receptor" HYPERLINK
"http://en.wikipedia.org/wiki/GABAA_receptor" HYPERLINK
"http://en.wikipedia.org/wiki/GABAA_receptor" HYPERLINK
"http://en.wikipedia.org/wiki/GABAA_receptor"receptor downregulation, alterations to subunit
configuration of GABAA receptors, uncoupling andinternalisation of the benzodiazepine binding
site from the GABAA receptor complex as well as changes in gene expression.
Interactions
Lorazepam is not usually fatal in overdose, but may cause fatal respiratory depression if taken
in overdose with alcohol. The combination also causes synergistic enhancement of
the disinhibitoryand amnesic effects of both drugs, with potentially embarrassing or criminal
consequences. Some experts advise that patients should be warned against drinking alcohol
while on lorazepam treatment, but such clear warnings are not universal. Synergistic adverse
effects may also occur when lorazepam is administered with other drugs, such as opioids or
other hypnotics. Lorazepam may also interact with rifabutin. Valproate inhibits the metabolism of
lorazepam, whereas carbamazepine, lamotrigine, phenobarbital, phenytoin,
and rifampin increase its rate of metabolism. Some antidepressants, antiepileptic drugs such as
phenobarbital, phenytoin and carbamazepine, sedative antihistamines, opiates, antipsychotics
and alcohol, when taken with lorazepam may result in enhanced sedative effects.
Overdose
In cases of a suspected lorazepam overdose, it is important to establish whether the patient is a
regular user of lorazepam or other benzodiazepines, since regular use causes tolerance to
develop. Also, one must ascertain whether other drugs were also ingested.
1. Signs of overdose range through mental confusion, dysarthria, paradoxical
reactions, drowsiness, hypotonia, ataxia, hypotension, hypnotic state, coma,
cardiovascular depression, respiratory depression, and death.
2. Early management of alert patients includes emetics, gastric lavage, and activated
charcoal. Otherwise, management is by observation, including of vital signs, support
and, only if necessary, considering the hazards of doing so,
giving intravenous flumazenil.
3. Patients are ideally nursed in a kind, nonfrustrating environment, since, when given or
taken in high doses, benzodiazepines are more likely to cause paradoxical reactions. If
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Drug abuse and their effect
shown sympathy, even quite crudely feigned, patients may respond solicitously, but they
may
respond
with
disproportionate
aggression
to
frustrating
cues. Opportunistic counseling has limited value here, as the patient is unlikely to recall
this later, owing to drug-induced anterograde amnesia.
Pharmacology
Lorazepam has anxiolytic, sedative, hypnotic, amnesic, anticonvulsant, and muscle
relaxant properties. It is a high-potency and an intermediate-acting benzodiazepine, and its
uniqueness, advantages, and disadvantages are largely explained by its pharmacokinetic
properties (poor water and lipid solubility, high protein binding and anoxidative metabolism to a
pharmacologically inactive glucuronide form) and by its high relative potency (lorazepam 1-2 mg
is equal in effect to diazepam 10 to 20 mg). The half-life of lorazepam is 10–20 hours.
Pharmacokinetics(ADME)
Lorazepam is highly protein bound and is extensively metabolised into pharmacologically
inactive metabolites. Due to its poor lipid solubility, lorazepam is absorbed relatively slowly by
mouth and is unsuitable for rectal administration. However, its poor lipid solubility and high
degree of protein binding (85-90%) mean its volume of distribution is mainly
the vascular compartment, causing relatively prolonged peak effects. This contrasts with the
highly lipid-soluble diazepam, which, although rapidly absorbed orally or rectally, soon
redistributes from the serum to other parts of the body, in particular body fat. This explains why
one lorazepam dose, despite its shorter serum half-life, has more prolonged peak effects than
an equivalent diazepam dose. On regular administration, diazepam will, however, accumulate
more, since it has a longer half-life and active metabolites with even longer half-lives.
Pharmacodynamics
Relative to other benzodiazepines, lorazepam is thought to have high affinity for GABA
receptors, which may also explain its marked amnesic effects. Its main pharmacological effects
are the enhancement of the effects of GABA at the GABAA receptor.[4] Benzodiazepines, such
as lorazepam, enhance the effects of GABA at the GABAA receptor via increasing the frequency
of opening of the chloride ion channel on the GABAA receptors; which results in the therapeutic
actions of benzodiazepines. They, however, do not on their own enhance the GABAA receptors,
but require the neurotransmitter GABA to be present. Thus, the effect of benzodiazepines is to
enhance the effects of the neurotransmitter GABA.
The magnitude and duration of lorazepam effects are dose-related, meaning larger doses have
stronger and longer-lasting effects, because the brain has spare benzodiazepine drug receptor
capacity, with single, clinical doses leading only to an occupancy of some 3% of the available
receptors.
The anticonvulsant properties of lorazepam and other benzodiazepines may be, in part or
entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine
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Drug abuse and their effect
receptors. Sustained repetitive firing seems to get limited, by the benzodiazepine effect of
slowing recovery of sodium channels from inactivation in mouse spinal cord cell cultures.
Chemistry
Lorazepam is synthesized according to a scheme containing some of the same elements for the
synthesis of chlordiazepoxide and oxazepam.
1. 2-amino-2′,5-dichlorobenzophenone is reacted with hydroxylamine.
2. The intermediate oxime is then reacted with chloracetyl chloride, and upon
heterocyclization, 6-chloro-2-chlormethyl-4-(2′-chlorophenyl)quinazolin-3-oxide is
formed.
3. The above product is reacted with methylamine, as in the case of chlordiazepoxide, this
leads to rearrangement and a ring expansion, forming 7-chloro-2-methylamino-5-(2′chlorphenyl)-3H-1,4-benzodiazepin-4-oxide.
4. The resulting benzodiazepin-4-oxide undergoes acetylation by acetic anhydride at the
secondary nitrogen atom, and is further hydrolyzed by hydrochloric acid into 7-chloro-5(2′-chlorophenyl)-1,2- dihydro-3H-1,4-benzodiazepin-2-on-4-oxide.
5. Reaction of the above product with acetic anhydride leads to a Polonovski-type
rearrangement reaction, giving a 3-acetoxylated benzodiazepine, 7-chloro-1,3-dihydro3-acetoxy-5-(2′-chlorphenyl)-2H-benzodiazepin-2-one.
6. Hydrolysis of the above product forms the desired product lorazepam.
(5) Pentazocine (30mg/1ml solution for injection ampoules)
Pentazocine lactate (pen-taz-oh-seen lak-tate) is a medicine which is used in relieving moderate
to severe pain. The information in this Medicine Guide for Pentazocine lactatevaries according
to the condition being treated and the particular preparation used. There are 2 preparations of
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Drug abuse and their effect
Pentazocine lactate available. If Pentazocine 30mg/1ml solution for injection ampoules is not
the preparation you are looking for, please select from the drop down list below.
Pentazocine 30mg/1ml solution for injection ampoules
Information specific to Pentazocine 30mg/1ml solution for injection ampoules when used in
relieving moderate to severe pain
medicine
Pentazocine lactate is a type of strong pain killer. It is used to help relieve moderate to
severe pain. It works by affecting chemicals in the brain and nervous system which are involved
in the sensation of pain. Pentazocine lactate can cause tolerance and dependence in some
people. Pentazocine lactate is usually given to you by a healthcare professional. The person
responsible for giving you your medicinewill make sure that you get the right dose. If you feel
that the medicine is making you unwell or you do not think it is working, then talk to
your prescriber or someone involved in your medical care.
When to take your medicine
The person with responsibility for giving you your medicine will make sure that you have
your medicine at the prescribed times.
How to take your medicine
This medicine will be given to you as an injection. If you have any concerns about
this medicine or how this will be given to you, talk to someone who is involved in your medical
care.
Taking too much of your medicine
Having extra doses of some medicines can be harmful. In some cases even one extra dose can
cause you problems.
In the case of Pentazocine lactate, the person who is responsible for giving you
your medicine will make sure that you are given the correct dose.
Stopping your medicine
Some people experience withdrawal symptoms when they stop having this medicine. The
person in charge of your medical care will decide when to stop giving you this medicine and how
best to minimise any withdrawal symptoms.
If you have any concerns about this, talk to someone who is involved in your care.
Whether this medicine is suitable for you
Pentazocine lactate is not suitable for everyone and some people should never use it. Other
people should only use it with special care. It is important that the person prescribing
this medicine knows your full medical history.
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Your prescriber may only prescribe this medicine with special care or may not prescribe it at all
if you:
1. are allergic or sensitive to or have had a reaction to any of the ingredients in the medicine
2. are dependent on opioids
3. are elderly
4. are having an asthma attack
5. are intoxicated with alcohol
6. are prone to seizures
7. have a low level of oxygen in the blood
8. have a medical condition where raised blood pressure may be dangerous
9. have abdominal pain
10. have adrenal gland problems
11. have biliary problems
12. have bowel problems
13. have breathing problems
14. have excessive bronchial secretions
15. have had monoamine oxidase inhibitors in the last 14 days
16. have head injuries
17. have heart problems
18. have high intracranial pressure
19. have hypothyroidism
20. have kidney problems
21. have liver problems
22. have lung problems
23. have misused drugs in the past
24. have pancreatitis
25. have phaeochromocytoma
26. have porphyria
27. have prostate problems
28. have recently had a heart attack
29. have respiratory depression
Furthermore the prescriber may only prescribe this medicine with special care or may not
prescribe it at all for a child under the age of one year.
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Drug abuse and their effect
Side-effects
A medicine is only made available to the public if the clinical trials have shown that
the benefits of taking the medicineoutweigh the risks.
Once a medicine has been licensed, information on the medicine's effects, both intended and
unintended, is continuously recorded and updated.
Some side-effects may be serious while others may only be a mild inconvenience
1. allergic reactions
2. anaphylactic shock
3. biliary problems
4. blood problems
5. changes in uterine contractions during labour
6. chills
7. circulation problems
8. confusion
9. constipation
10. constriction of the pupil of the eye
11. convulsions
12. dependence
13. dermatitis
14. difficulty sleeping
15. dry mouth
16. erythema multiforme
17. euphoria
18. eye or eyesight problems
19. fainting or brief loss of consciousness
20. faster heart rate
21. feeling dizzy
22. feeling light-headed
23. feelings of disorientation
24. flushing
25. hallucinations
26. headaches
27. injection site problems such as hardening of the skin or tissues, indentation of the
formation of lumps, ulceration and stinging
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28. itching
29. lowered blood pressure
30. mood changes
31. muscle problems
32. nausea
33. nightmares
34. oedema of the face
35. paraesthesiae
36. raised blood pressure
37. raised intracranial pressure
38. respiratory depression
39. sleepiness
40. stomach pain
41. sweating
42. toxic epidermal necrolysis
43. tremors
44. urinary retention
45. vomiting
46. withdrawal symptoms if Pentazocine lactate is stopped suddenly after using it for a long time
such as: stomach cramps, nausea, vomiting, feeling nervous or restless, dizziness, fever, chills,
runny nose and increased tear production
Taking other medicines
If you are taking more than one medicine they may interact with each other. At times
your prescriber may decide to usemedicines that interact, in other cases this may not be
appropriate.
The decision to use medicines that interact depends on your specific circumstances.
Your prescriber may decide to usemedicines that interact, if it is believed that the benefits of
taking the medicines together outweigh the risks. In such cases, it may be necessary to alter
your dose or monitor you more closely.
The following medicines may interact with Pentazocine lactate:
1. diamorphine
2. morphine
3. naloxone
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Drug abuse and their effect
The following types of medicine may interact with Pentazocine lactate:
1. medicines that cause sedation
2. monoamine oxidase inhibitors
3. narcotics
4. opioids
5. phenothiazines
6. tricyclic antidepressants
7. tobacco
8. alcohol.
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REFERENCES
1. Introduction

.Oxford University Press – Oxford Specialist Handbook: Addiction, 2009.
o
National Institute on Drug Abuse (NIDA) The Science of Addiction, 2010
http://www.nida.nih.gov/scienceofaddiction
o
Diagnostic and Statistical Manual of Mental Disorders (DSM) IV, 1994.
http://en.wikipedia.org/wiki/Substance_abuse#DSM



National Health Service (NHS), UK
Centers for Disease Control and Prevention (CDC), USA
National Institutes of Health (NIH), USA

Wikipedia
2. Harmful effect


MayoClinic.com: Drug Addiction
National Institute on Drug Abuse: Understanding Drug Abuse and Addiction

Medline Plus: Drug Abuse

National Institute of Drug Abuse

Facts for Teens on Inhalants

Adolscnt


Choose Help: Teen Drug Use Statistics
Drug-Addiction.com: Adolescent Substance Abuse
3. Descriptn



Altman J, Everitt BJ, Glautier S, et al. The biological, social
and clinical bases of drug addiction: commentary and debate.
Psychopharmacology (Berl) 1996;125:285–345.
Rungta college of pharmaceutical science and research, bhilai (c.g)
Page 51
Drug abuse and their effect



Di Chiara G, Imperato A. Drugs abused by humans preferentially
increase synaptic dopamine concentrations in the mesolimbic
system of freely moving rats. Proc Natl Acad Sci USA 1988;85:



Wise RA, Mendrek A, Carlezon WA Jr. MK-801 (dizocilpine):
synergist and conditioned stimulus in bromocriptine-induced
psychomotor sensitization. Synapse 1996;22:362–368.



Rudnick G, Clark J. From synapse to vesicle: the reuptake and
storage of biogenic amine neurotransmitters. Biochim Biophys
Acta 1993;1144:249–263.
4. CHEMICAL
Alprazolam

First DataBank (July 2008). "Xanax (Alprazolam) Clinical Pharmacology – Prescription
Drugs and Medications at RxList". RxList.

First DataBank (July 2008). "Xanax XR (Alprazolam) Clinical Pharmacology –
Prescription Drugs and Medications at RxList". RxList.

Work Group on Panic Disorder (January 2009). "APA Practice Guideline for the
Treatment of Patients With Panic Disorder, Second Edition". Retrieved 2009-12-07.

FDA (2011-08-23). "FDA approved labeling for Xanax revision 08/23/2011" (pdf).
Federal Drug Administration. p. 4. Retrieved 2011-09-14. "Anxiety Disorders – XANAX
Tablets (alprazolam) are indicated for the management of anxiety disorder (a condition
corresponding most closely to the APA Diagnostic and Statistical Manual [DSMIII-R]
diagnosis of generalized anxiety disorder) or the short-term relief of symptoms of
anxiety. ^ a b Mandrioli, R.; Mercolini, L.; Raggi, M. A. (2008). "Benzodiazepine
Metabolism:
An
Analytical
Perspective".Current
Drug
Metabolism 9 (8):
827–
844.doi:10.2174/138920008786049258.PMID 18855614. edit

Sheehan, D. V.; Sheehan, K. H.; Raj, B. A. (2007). "The Speed of Onset of Action of
Alprazolam-XR Compared to Alprazolam-CT in Panic Disorder". Psychopharmacology
Bulletin 40 (2): 63–81. PMID 17514187. edit

Smith, R. B.; Kroboth, P. D.; Vanderlugt, J. T.; Phillips, J. P.; Juhl, R. P. (1984).
"Pharmacokinetics
and
Pharmacodynamics
of
Alprazolam
after
Oral
and
IV
Administration". Psychopharmacology 84 (4): 452–456.PMID 6152055. edit

Verster J. C.; Volkerts E. R. (2004). "Clinical Pharmacology, Clinical Efficacy, and
Behavioral Toxicity of Alprazolam: A Review of the Literature" (pdf). CNS Drug
Reviews 10 (1): 45–76. doi:10.1111/j.1527-3458.2004.tb00003.x. PMID 14978513.
Rungta college of pharmaceutical science and research, bhilai (c.g)
Page 52
Drug abuse and their effect

Tampi, R. R.; Muralee, S.; Weder, N. D. et al., eds. (2008).Comprehensive Review of
Psychiatry. Philadelphia, PA: Wolters Kluwer / Lippincott Williams & Wilkins Health.
pp. 226. ISBN 978-0-7817-7176-4.

Pavuluri, M. N.; Janicak, P. G.; Marder, S. R. (2010).Principles and Practice of
Psychopharmacotherapy (5th ed.). Philadelphia, PA: Wolters Kluwer Health / Lippincott
Williams & Wilkins. pp. 535. ISBN 978-1-60547-565-3.

Galanter, M. (2008). The American Psychiatric Publishing Textbook of Substance
Abuse Treatment (4th ed.). American Psychiatric Publishing. p. 222. ISBN 978-1-58562276-4.
Lorazepam

Greenblatt DJ, Shader RI, Franke K, Maclaughlin DS, Harmatz JS, Allen MD, Werner A,
Woo E (1991). "Pharmacokinetics and bioavailability of intravenous, intramuscular, and
oral
lorazepam
in
humans". Journal
of
Pharmaceutical
Sciences 68 (1):
57–
63.doi:10.1002/jps.2600680119. PMID 31453.

Greenblatt DJ, von Moltke LL, Ehrenberg BL, Harmatz JS, Corbett KE, Wallace DW,
Shader RI (2000). "Kinetics and dynamics of lorazepam during and after continuous
intravenous infusion".Critical Care Medicine 28 (8): 2750–2757. doi:10.1097/00003246200008000-00011.PMID 10966246.

Papini O, da Cunha SP, da Silva Mathes Ado C, Bertucci C, Moisés EC, de Barros
Duarte L, de Carvalho Cavalli R, Lanchote VL (2006). "Kinetic disposition of lorazepam
with a focus on the glucuronidation capacity, transplacental transfer in parturients and
racemization in biological samples". Journal of Pharmaceutical and Biomedical
Analysis 40 (2): 397–403.doi:10.1016/j.jpba.2005.07.021. PMID 16143486.

Riss J, Cloyd J, Gates J, Collins S (2008). "Benzodiazepines in epilepsy: pharmacology
and
pharmacokinetics". Acta
Neurologica
Scandinavica 118 (2):
69–
86.doi:10.1111/j.1600-0404.2008.01004.x. PMID 18384456.

Hindmarch I (January 30, 1997). "Benzodiazepines and their effects". benzo.org.uk.
Retrieved 2007-05-13.

Cox CE, Reed SD, Govert JA, Rodgers JE, Campbell-Bright S, Kress JP, Carson SS
(2008). "An Economic Evaluation of Propofol and Lorazepam for Critically Ill Patients
Undergoing
Mechanical
Ventilation". Critical
Care
Medicine 36 (3):
706–
714.doi:10.1097/CCM.0B013E3181544248. PMC 2763279. PMID 18176312.
Rungta college of pharmaceutical science and research, bhilai (c.g)
Page 53
Drug abuse and their effect

Walker M (2005). "Status epilepticus: an evidence based guide". BMJ 331 (7518): 673–
677. doi:10.1136/bmj.331.7518.673. PMC 1226249. PMID 16179702.

Battaglia J (2005). "Pharmacological management of acute agitation". Drugs 65 (9):
1207–1222. doi:10.2165/00003495-200565090-00003. PMID 15916448.

^ Kemper N, Poser W, Poser S (1980). "[Benzodiazepine dependence: addiction
potential of the benzodiazepines is greater than previously assumed]" (in
German). Deutsche Medizinische Wochenschrift 105 (49): 1707–1712. doi:10.1055/s2008-1070941. PMID 7439058.

Griffiths RR, Johnson MW (2005). "Relative abuse liability of hypnotic drugs: a
conceptual framework and algorithm for differentiating among compounds". Journal of
Clinical Psychiatry66 (Suppl 9): 31–41. PMID 16336040.

Michel L, Lang JP (2003). "[Benzodiazepines and forensic aspects]" (in
French).L'Encéphale 29 (6): 479–485. PMID 15029082.

Kintz P (2007). "Bioanalytical procedures for detection of chemical agents in hair in the
case of drug-facilitated crimes" (pdf). Analytical and Bioanalytical Chemistry 388 (7):
1467–1474. doi:10.1007/s00216-007-1209-z. PMID 17340077
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