Depressants and Inhalants
Depressants include alcohol, prescription drugs, sedatives to reduce
anxiety (low dose) and hypnotics for sleep (higher dose). The most
widely used depressant is alcohol. The most widely prescribed of the
sedative-hypnotics are benzodiazepines. These have replaced barbiturates.
Inhalants (glues, paints, solvents, and gas fumes) produce a similar
depressant effect.
Barbiturates are grouped by duration of effectiveness.
Short-acting (Pentobarbital- Nembutal, Secobarbital- Seconal) Onset
in 15 min., lasts 2-3 hours) Most lipid-soluble, so faster acting.
Intermediate-acting (Amytal, Butisol) onset in 30 min., lasts 5-6
hrs.)
Long-acting (Phenobarbital) onset in 1 hr., lasts 6 – 10 hrs.)
Rate of onset and effectiveness makes a difference in usage. A rapid onset
drug that is designed to make you sleep (hypnotic) will also need to last a
shorter time but can use a higher dose. (Secobarbital). But for function
during the daytime, simply to calm a person (sedative) you want a low dose
of a long-acting drug- Phenobarbital.
Because this drug is processed in the liver, tolerance builds up due to liver
enzyme action. Downside is they depress respiration and in combination
with alcohol, can completely stop breathing. Commonly used for suicide, but
also produced accidental overdoses when used after a drinking party for
sleep (Marilyn Monroe). Due to concerns over addiction and overdose:
Newer drugs were developed: antianxiety agents developed from a muscle
relaxant, mephenesin. Miltown, Equalnil (Meprobate) began the drug
revolution in the 1950s. It did produce both psychological and physical
dependence, however, when used at higher doses. At lower doses, which it
was designed for, it only produced a calming, sedative effect.
Methaqualone (Qualude, Sopor) was produced as a safer hypnotic, sleeping
agent. It was seriously misused on the street, however. It became the drug of
choice for suicide, and resulting in many overdoses. It was finally seen as a
serious drug of abuse and put on Schedule II in 1973. Now it’s a Schedule I
and no longer available, even by prescription.
Benzodiazepines were developed in response to problems with the
barbiturates.
Librium (chlordiazepoxide) First marketed in 1960, it was presented
as an antianxiety agent with less drowsiness than barbiturates and a greater
safety margin before overdose and death occurred.
Diazepam (Valium) largely replaced Librium in the early 1970s.
There were reports of dependence and overdose deaths associated with
Valium, but most often in combination with alcohol or other depressants.
Xanax (alprazolam) is the best seller in this class of drugs today.
Psychological dependence is most related to drugs that hit the brain
quickly (crack is more addictive than chewing coca leaves, IV heroin is
more addictive than oral use). So a drug with rapid onset will more likely
produce psychological dependence than a slower acting drug.
Physical dependence occurs when the drug leaves the system more
rapidly than the body can adapt. Drugs with a shorter duration of
effectiveness leave the system quickly and are more likely to produce
withdrawal symptoms than longer-acting drugs.
(Fig. 9.1) shows that Secobarbital is a short-acting barbiturate, with
rapid onset, producing psychological dependence, and with rapid
termination of effects, more likely to produce serious withdrawal symptoms.
It was prescribed as a sleeping pill, so large doses were prescribed. There
was a lot of ODing and physical and psychological dependence.
Phenobarbital is a long acting barbiturate has a slower onset,
producing less psychological dependence. Drug clearance and termination is
slower, so withdrawal symptoms are less. It was prescribed in lower sedative
doses, so was rarely a cause of OD.
Chlordiazepoxide (Librium) the first benzodiazepine, was sold in
low doses as a sedative for daytime use, has a slow onset and longer duration
of effectiveness. It has few problems with addictive use or withdrawal
symptoms and there are few OD with it.
Diazepam (Valium) has a more rapid onset then Librium, but also a
longer duration of action. It produces more psychological dependence, but
rarely withdrawal symptoms.
Rohypnol (roofies) is a benzodiazepine, sold as a hypnotic in other
countries except the US. It is known as a date rape drug, since the
combination in an alcoholic drink produces such a profound intoxication that
women were being drugged and raped by acquaintances, with little or no
memory of the experience after the drink. In 1997 the manufacturer changed
the formula so that when it dissolves in a drink it turns the drink blue.
The way the benzodiazepines seem to work is by enhancing the
inhibitory effects of GABA (an inhibitory neurotransmitter). The newest
research is designed to separate the subtypes of the GABA receptors, to
produce more accurate antianxiety drugs or hypnotic, sleeping drugs.
Purposes of the depressants:
Sedatives- to obliterate our awareness of our condition. The
antianxiety drugs (anxiolytics) are some of the best selling drugs in the
country. These drugs can treat phobias, panic attacks, OCD, psychosomatic
problems, serious anxiety disorders, such as PTSD. The problem with
relying too heavily on a pharmaceutical remedy for these problems, is that
many people don’t ever learn to deal with the sources of their stress and
change their situations or their responses or attitudes. Is it justified to put
someone on Ativan or Buspar because they are shy- have social anxiety? Do
some patients just resist feeling anything negative in life?
Sleeping pills -larger doses will result in sleep for those with
problems sleeping (1/3 adults in US). The problem with hypnotics for sleep
is tolerance, rebound insomnia, dependence, hangover effects. Halcion is the
most commonly prescribed benzodiazepam for sleep, since it has a shorteracting effect. Tolerance doesn’t build up as quickly as the barbiturates
(which put people at risk for OD since they take more of the drug to get the
same hypnotic effect). Doctors do not prescribe these drugs readily anymore,
and they limit the length of time. Halcion has had some adverse psychiatric
effects, such as paranoia, so it is more carefully prescribed today. Ambien is
the newest benzodiazepine hypnotic. It has a rapid onset and shorter duration
of action. It is the leading sleeping agent bought today.
Anticonvulsants are designed to control seizure disorders. Since they
are required for chronic use, they have some problems with drowsiness and
tolerance.
Concerns
Psychological dependence occurs most often with the short-acting
barbiturates. But as more people use Valium, Xanax more reports of
dependence are surfacing.
Physical dependence is displayed differently than narcotic
withdrawal (heroin). At first the patient seems better, then s/he displays
anxiety, insomnia, shakiness, weakness, anorexia, nausea & vomiting. There
may even be gran mal seizures on the 2nd or 3rd day of withdrawal from
barbiturates. After the seizure there may be a psychosis showing confusion,
disorientation in time and place, agitation, insomnia, delusions, and
hallucinations. It resembles DTs coming off alcohol. Terminates in a deep
sleep. This withdrawal lasts longer than narcotic withdrawal and seems even
more unpleasant than narcotic withdrawal. It is also life-threatening. Death
occurs for 5% of those who withdraw abruptly after having been on large
doses of barbiturates. Benzodiazepines can produce a withdrawal syndrome
if there has been higher dosages. In hospitals, they often use another
depressant (benzodiazepines, usually) to moderate the effects of withdrawal
from a chronic depressant drug. These are longer-acting drugs given in
divided doses to control the withdrawal symptoms.
Toxicity relates to how the drug can produce damage in the body
(acute toxicity) or uninhibited behaviors that put the user and others at risk.
Depressants are so often used in combination with alcohol, which
unwittingly puts the user at great risk of respiration interruption & death.
The other people at risk for depressant abuse are older adults who originally
get a legal prescription for the meds, but need higher dosages, so go to
multiple doctors for several Rxs until they put themselves at risk for OD.
Younger people who take the drugs in large doses to get high. They often
mix them with alcohol or other drugs, putting themselves at great risk.
Inhalants produce similar effects to depressants, and most of the materials
are readily available. Several types of materials can be inhaled.
Gaseous anesthetics are used in surgery to block pain. So medical
professionals may abuse these drugs. (Nitrous oxide- laughing gas is a safe
anesthetic, but it only works effectively if the person almost exclusively
inhales it- leading to high risk of suffocation without oxygen. It is also used
as a propellant in whipping-cream containers and is sold in small bottleswhippets, for home dispensers.)
Nitrites are amyl nitrite or butyl nitrite and they cause rapid dilation
of the arteries and drop blood pressure to the brain- producing faintness or
unconsciousness. They seem to be popular with some homosexual males
who use “poppers” during sex to enhance orgasm. They have a strong odor
and are sold under the names “Locker Room” or “Aroma of Men.”
Volatile solvents – glue sniffing was first publicized in the Denver
Post in 1959- after which incidents went from no reported cases to 50 in 6
months. Publicity seemed to increase use. Some “huffers” are adults, but
most are young people who can’t easily get alcohol. Middle schoolers are
more likely to use. It’s also seen more often within poorer Hispanic youth
and Native American youth. These solvents have been linked to kidney
damage, brain damage, peripheral nerve damage, irritation of the respiratory
tract, severe headaches, and some die of suffocation. (Cider House Rules)
Aerosols, propellants, gases include spray paint , hari spray, lighters,
gasoline, and whippets.