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Opiates

Opium, codeine, morphine, heroin

The opioids include both natural opiates - that is, drugs from the opium poppy - and opiate-related synthetic drugs, such as meperidine and methadone.

The opiates are found in a gummy substance extracted from the seed pod of the Asian poppy, Papaver somniferum. Opium is produced from this substance, and codeine and morphine are derived from opium. Other drugs, such as heroin, are processed from morphine or codeine.

Opiates have been used both medically and non-medically for centuries. A tincture of opium called laudanum has been widely used since the 16th century as a remedy for "nerves" or to stop coughing and diarrhea.

By the early 19th century, morphine had been extracted in a pure form suitable for solution. With the introduction of the hypodermic needle in the mid-19th century, injection of the solution became the common method of administration.

Heroin (diacetylmorphine) was introduced in 1898 and was heralded as a remedy for morphine addiction. Although heroin proved to be a more potent painkiller (analgesic) and cough suppressant than morphine, it was also more likely to produce dependence.

Of the 20 alkaloids contained in opium, only codeine and morphine are still in widespread clinical use today. In this century, many synthetic drugs have been developed with essentially the same effects as the natural opium alkaloids.

Opiate-related synthetic drugs, such as meperidine (Demerol) and methadone, were first developed to provide an analgesic that would not produce drug dependence. Unfortunately, all opioids (including naturally occurring opiate derivatives and synthetic opiate-related drugs), while effective as analgesics, can also produce dependence. (Note that where a drug name is capitalized, it is a registered trade name of the manufacturer.)

Modern research has led, however, to the development of other families of drugs. The narcotic antagonists (e.g. naloxone hydrochloride) - one of these groups - are used not as painkillers but to reverse the effects of opiate overdose.

Another group of drugs possesses both morphine-like and naloxone-like properties (e.g. pentazocine, or Talwin) and are sometimes used for pain relief because they are less likely to be abused and to cause addiction. Nevertheless, abuse of pentazocine in combination with the antihistamine tripelennamine (Pyribenzamine) was widely reported in the 1980s, particularly in several large cities in the United States. This combination became known on the street as "Ts and blues." The reformulation of Talwin, however, with the narcotic antagonist naloxone has reportedly reduced the incidence of Ts and blues use.

Appearance

Opium appears either as dark brown chunks or in powder form, and is generally eaten or smoked. Heroin usually appears as a white or brownish powder, which is dissolved in water for injection. Most street preparations of heroin contain only a small percentage of the drug, as they are diluted with sugar, quinine, or other drugs and substances. Other opiate analgesics appear in a variety of forms, such as capsules, tablets, syrups, elixirs, solutions, and suppositories. Street users usually inject opiate solutions under the skin ("skin popping") or directly into a vein or muscle, but the drugs may also be "snorted" into the nose or taken orally or rectally.

Effects

The effects of any drug depend on several factors: Short-term effects appear soon after a single dose and disappear in a few hours or days. Opioids briefly stimulate the higher centres of the brain but then depress activity of the central nervous system. Immediately after injection of an opioid into a vein, the user feels a surge of pleasure or a "rush." This gives way to a state of gratification; hunger, pain, and sexual urges rarely intrude.

The dose required to produce this effect may at first cause restlessness, nausea, and vomiting. With moderately high doses, however, the body feels warm, the extremities heavy, and the mouth dry. Soon, the user goes "on the nod," an alternately wakeful and drowsy state during which the world is forgotten.

As the dose is increased, breathing becomes gradually slower. With very large doses, the user cannot be roused; the pupils contract to pinpoints; the skin is cold, moist, and bluish; and profound respiratory depression resulting in death may occur.

Overdose is a particular risk on the street, where the amount of drug contained in a "hit" cannot be accurately gauged. In a treatment setting, the effects of a usual dose of morphine last three to four hours. Although pain may still be felt, the reaction to it is reduced, and the patient feels content because of the emotional detachment induced by the drug.

Long-term effects appear after repeated use over a long period. Chronic opiate users may develop endocarditis, an infection of the heart lining and valves as a result of unsterile injection techniques.

Drug users who share needles are also at a high risk of acquiring AIDS (acquired immune deficiency syndrome) and HIV infection (human immunodeficiency virus). Unsterile injection techniques can also cause abscesses, cellulitis, liver disease, and even brain damage. Among users with a long history of subcutaneous injection, tetanus is common. Pulmonary complications, including various types of pneumonia, may also result from the unhealthy lifestyle of the user, as well as from the depressant effect of opiates on respiration.

Tolerance and Dependence

With regular use, tolerance develops to many of the desired effects of the opioids. This means the user must use more of the drug to achieve the same intensity of effect.

Chronic users may also become psychologically and physically dependent on opioids.

Psychological dependence exists when a drug is so central to a person's thoughts, emotions, and activities that the need to continue its use becomes a craving or compulsion.

With physical dependence, the body has adapted to the presence of the drug, and withdrawal symptoms occur if use of the drug is reduced or stopped abruptly. Some users take heroin on an occasional basis, thus avoiding physical dependence.

Withdrawal from opioids, which in regular users may occur as early as a few hours after the last administration, produces uneasiness, yawning, tears, diarrhea, abdominal cramps, goose bumps, and runny nose. These symptoms are accompanied by a craving for the drug.

Major withdrawal symptoms peak between 48 and 72 hours after the last dose and subside after a week. Some bodily functions, however, do not return to normal levels for as long as six months. Sudden withdrawal by heavily dependent users who are in poor health has occasionally been fatal. Opioid withdrawal, however, is much less dangerous to life than alcohol and barbiturate withdrawal

Opioids and pregnancy

Opioid-dependent women are likely to experience complications during pregnancy and childbirth. Among their most common medical problems are anemia, cardiac disease, diabetes, pneumonia, and hepatitis. They also have an abnormally high rate of spontaneous abortion, breech delivery, caesarian section, and premature birth. Opioid withdrawal has also been linked to a high incidence of stillbirths.

Infants born to heroin-dependent mothers are smaller than average and frequently show evidence of acute infection. Most exhibit withdrawal symptoms of varying degrees and duration. The mortality rate among these infants is higher than normal.

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Copyright (c) 1970 Revised January 1991 Alcoholism and Drug Addiction Research Foundation, Toronto Canada
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