CNS DepressantNarcotics

Opioids

CNS Depressants

Opioids CNS Depressants

Narcotics Opium, Morphine, Codeine,

Thebaine, Heroin, Oxycodone, Fentanyl .. Etc.

Non-Opioids CNS

Depressants

Alcohol, Barbiturates,

Benzodiazepines .. 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, semi-synthetic 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.

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.

Opioids Classification:

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.