CNS Depressant
Narcotics
Opioids
CNS Depressants
Opioids CNS
Depressants
Non-Opioids
CNS
Depressants
Narcotics
Alcohol,
Barbiturates,
Benzodiazepines ..
Etc.
Opium, Morphine, Codeine,
Thebaine, Heroin,
Oxycodone, Fentanyl .. Etc.
The term “narcotic,” derived from the Greek word for
stupor, originally referred to a variety of substances that
dulled the senses and relieved pain.
Some individuals define narcotics as those substances
that bind at opiate receptors (cellular membrane
proteins activated by substances like heroin or
morphine), while others refer to any illicit substance as
a narcotic.
In a legal context, narcotic refers to opium,
opium derivatives, and their semi-synthetic substitutes.
Narcotics are used therapeutically to treat
pain, suppress cough, alleviate diarrhea, and
induce anesthesia.
Aside from their medical use, narcotics
produce a general sense of well-being by reducing
tension, anxiety, and aggression. These effects are
helpful in a therapeutic setting but contribute to
their abuse.
Opioids
An opioid is a psychoactive chemical that works by binding
to opioid receptors, which are found principally in the
central and peripheral nervous system and the
gastrointestinal tract. The receptors in these organ systems
mediate both the beneficial effects and the side effects of
opioids.
Opioids are among the world's oldest known drugs as
analgesic. The side effects of opioids include sedation,
respiratory depression, constipation, and a strong sense
of euphoria.
Opioid dependence can develop with ongoing
administration, leading to a withdrawal syndrome with
abrupt discontinuation.
Opiate is the usual term used to designate
drugs derived from opium (eig morphine, codeine,
thebaine, noscapine, papaverin and norceine) and
their chemically related derivatives such as the
semisynthetic alkaloids (e.g. dihydrocodeine,
ethylmorphine and heroin), whereas Opioid is a
more general term that comprises natural, semisynthetic and synthetic drugs with morphine-like
actions although the chemical structure may differ
from that of morphine (e.g dextropropoxyphene,
pethidine, tilidine, diphenyoxylate, methadone,
trimeperidine, ketobemidone and fentanyl).
Opium:
It is the dried latex obtained by incision
from the unripe but fully grown capsules of
opium poppy, Papver somniferum
(papaveraceae) it is cultivated illicitly in a
number of countries around the world
however, India has been for several decades
the major producer and sole licit suppliers of
opium to meet world requirements for opiates.
*** The word opium is derived from the Greek opos (juice).
Genus Papaver includes more than 100 species of
which Papaver somniferum, Papaver setigerum and
Papaver decaisnei are the only known to produce
morphine.
Papaver bracteatum produces mainly thebaine
which is used for the production of synthetic opiates for
medicinal need.
Illicit production:
- Opium latex is obtained from the poppy capsules while
they are in the green stage, usually 7-8 days after flowering
and petals fall.
- The latex is harvested by making a series of shallow
incisions, using a three-bladed knife, through pericarp,
containing the latex-producing lactiferous, vessels, which
allow the latex to bleed onto the surface of the capsules as a
white milky exudates.
- Most commonly, the latex is allowed to partially dry on the
capsule surface, and is then removed by scrapping the
capsules with a specially designed hand tool.
Opium is a complex mix of an alkaloid fraction
(10-20%) together with sugars, protein, lipids and
other gummy substances.
The alkaloid fraction consists of about 40 alkaloids
with 5 major ones belonging to two major and
important groups of alkaloids.
The first is phenanthrene group including
morphine, codeine and thebaine.
The second one is isoquinoline group including
papaverine and noscapine (narcotine).
Illicit opium products:
•Raw opium
•Medicinal opium
•Prepared opium
•Opium dross
Raw opium: (Indian opium) is the natural product
obtained by incision of the unripe poppy capsules.
• When fresh it is sticky, has a tar-like consistency, a medium brown
color, and easily molded into different shapes and forms depending
on the method of packing and country of origin.
• It readily dissolves in water yielding a brown colored solution with
liquorices-like odor .
• Banana pulp, rosin, flour, powdered poppy capsules gum, roasted
bread and grinded dates are commonly used as adulterants.
• Raw opium can be distinguished by its characteristic odor the
presence of plant fragments and the presence of meconic acid and
porphyroxine.
Medicinal opium:
It is generally one of the three preparations
1) Granulated or powdered opium: (depending on the final mesh
size of the product), and is an opium which dried at 70°C and
whose morphine content is adjusted to pharmacopeia
requirements of 10-15%w/w, by the addition of lactose,
powdered coca husk or rice starch.
2) Deodorized opium or de-narcotized opium: this material is
prepared by treating opium with petrolium ether, which removes
both narcotine (noscapine) and the characteristic odor of opium.
Morphine concentration also 10-15% w/w.
3) Concentrated opium= Pantopon= Omnopor= papaveretum: it is
a mixture of morphine, codeine, papaverine and noscapine as HCl
salts with the morphine content adjusted to 50% w/w.
Prepared opium (caked opium):
it is an opium extract suitable for smoking.
• It is produced by boiling raw opium in water after filtration to
remove insoluble materials evaporating them till roasted.
• The roasted product is re-extracted with water and evaporated to
a black residue known, in South East Asia as chandoo or chandu that
means opium extract for smoking.
• It contains about 8% morphine.
• Prepared opium, like raw opium give positive color test for
meconic acid but differ from raw opium in the absence or near
absence of plant fragments and porphyroxine.
Opium dross: is the residue that remains in the
opium smoking pipe.
• Dross is both eaten and re-smoked after being added to
prepared opium.
• The presence of dross in prepared opium is generally
obvious as a charred material within the prepared opium,
and a burnt odor is frequently present.
• Dross does not give a positive color test for either
meconic acid or porphyroxine.
Opioids Classification:
a) Natural: alkaloids contained in the resin of the opium poppy,
primarily morphine, codeine, and thebaine, but not papaverine
and noscapine which have a different mechanism of action; The
following could be considered natural opiates.
b) Esters of morphine : slightly chemically altered but
more natural than the semi-synthetics, as most are morphine
prodrugs, diacetylmorphine (morphine diacetate; heroin),
nicomorphine (morphine dinicotinate) ..
c) Semi-synthetic : created from either the natural opiates
or morphine esters, such as hydromorphone, hydrocodone,
oxycodone, oxymorphone, ethylmorphine and buprenorphine.
d) Fully synthetic : such as fentanyl, pethidine, levorphanol,
methadone, tramadol and dextropropoxyphene.
Opium constituents of forensic significance:
Opium Constituents of Forensic Significance
Morphine is the principal constituent of opium
and ranges in concentration from 4 to 21 percent.
Commercial opium is standardized to contain 10 %
morphine. Morphine is one of the most effective
drugs known for the relief of severe pain and
remains the standard against which new analgesics
are measured.
It is the drug of choice for relieving the pain of
myocardial infarction and for its cardiovascular
effects in the treatment of acute pulmonary edema.
Codeine is an alkaloid found in opium in concentrations
ranging from 0.7 to 2.5 %. Codeine is medically prescribed
for the relief of moderate pain and cough suppression.
Compared to morphine, codeine produces less analgesia,
sedation, and respiratory depression, and is usually taken
orally.
Thebaine,
is a minor constituent of opium. Although
chemically similar to both morphine and codeine, thebaine
produces stimulatory rather than depressant effects.
Thebaine is not used therapeutically, but is converted into
a variety of substances including oxycodone, oxymorphone,
naloxone, naltrexone, and buprenorphine.
Heroin (also known as diamorphine,
diacetylmorphine):
It is a semisynthetic analog of morphine, prepared
by acetylation with acetyl chloride or acetic anhydride.
It is more lipid soluble, more rapidly absorbed and
2-3 times more potent as analgesic than morphine.
Heroin is rapidly deacetylated in the body and in
alkaline media to morphine. It belongs to the
internationally controlled narcotic analgesic with
morphine, codeine and some other synthetic drugs.
Medicinal Uses:
Opium and opiates are used as
analgesic, sedatives, and hypnotics,
anticough and in treatment of acute
diarrhea.
Administration:
•Opium is commonly administered by oral route
particularly in the Middle East region, prepared opium by
inhalation through smoking, and morphine HCl, SO4 or
tartarate by oral, subcutaneous, IV or IM.
•Heroin is commonly administered by inhalation through
smoking (usually heroin base) and snorting or snitting
(usually diluted heroin HCl. High quality heroin HCl is
usually abused through subcutaneous and intravenous
injection Heroin HCl, when taken by parenteral route, the
powder is first dissolved in H2O through gentle heating.
Pharmacological Effects:
•Opium and opiates are CNS depressants. They produce general
narcosis, analgesia, sedation, euphoria, constipation, respiratory
depression due to decreased medullary sensitivity to CO2, cough
depression, nausea, vomiting, hypotension and miosis (pin-point
pupil). These effects indicate narcotic intoxication and addiction.
•Heroin like morphine is a CNS depressant. It is 2-3 times more
potent as analgesic than morphine but less safe on respiratory
center. It resembles morphine in control of diarrhea but fewer
tendencies to produce constipation. It is more lipid soluble and then
readily penetrates the BBB (Blood Brain Barrier). It is rapidly
converted into the body to MAM (Mono Acetyl Morphine) and then to
morphine.
Dependence:
opium and opiates are narcotic analgesic. They
produce rapid and severe psychic and physical
dependence.
Heroin intoxication produces like morphine,
general narcosis, analgesia and sedation but it is
characterized by greater Euphoria.
Drug dependence means that a person needs a drug to function
normally. Abruptly stopping the drug leads to withdrawal symptoms.
Withdrawal or Abstinence syndrome:
Opium and opiates are specifically bound to the opiate
receptors in the cell membrane of neuron and smooth
muscle cells.
The organism develops a need for continuous intake of the
drug otherwise a physiological disturbance develops known
as withdrawal syndrome due to autonomic hyperactivity.
The sympathetic effects are manifested by lacrimation,
salivation, sweating, piloerection, dilatation of the pupil,
increase blood pressure, and increase heart rate, while the
parasympathetic effects include, nausea, vomiting,
abdominal pain, diarrhea, anxiety, tremors and convulsion.
In heroin, it appears after 12-14 hours of
abstinence and is characterized by light
perception, lacrimation, and insomnia, dilatation
of the pupil and twitching of various muscle
groups.
The symptoms reach peak intensity 48 hours
after the last dose and remain intense until 72
hours of abstinence then begin to decline.