Drugs of Abuse

Drugs of Abuse

by Richard E. Long and Richard P. Penna ince World War II, increasing attention has been devoted to drugs, particulal'ly drugs that affect the mind, ...

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by Richard E. Long and Richard P. Penna

ince World War II, increasing attention has been devoted to drugs, particulal'ly drugs that affect the mind, as either an intended or a side effect. While we are concerned with abuse of drugs which are taken intentionally to produce an altered state of mind, other types of drug abuse cannot be overlooked. The busy executive who takes tranquilizers four to five times daily to relax, amphetamines to curb his appetite, three or four martinis before lunch and dinner and barbiturates to go to sleep is guilty of abusing drugs. Where the blame lies and how extensive his "sickness" is can be a matter of debate. That people, other than addicts and hippies, are drug abusers is, however, a fact. Habitual smokers also may be placed in this classification. These brief monographs are intended to provide a background and insight into the general classes of drugs being abused and information about specific agents. The number of drugs dictates the necessity of brevity.

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Journal of the AMERICAN PHARMACEUTICAL ASSOCIATION

Should the reader wish additional information, journal and textbook references have been provided. To avoid confusion, certain terms must be defined. These definitions are not held by all experts in the field but they merely serve as a reference point for mutual understanding. 1- 2 Tolerance-A state in which the body's tissue cells become ac· climatized to the presence of a drug and fail to respond to ordinarily effective concentrations. Increased quantities of a drug are required to produce the desired effect. Physical dependence-A state created by the constant administration of a drug in which the presence of the drug in the body is necessary for normal functioning of the body. If the drug is withdrawn, violent physical and psychic reactions occur. Withdrawal symptoms or abstinence syndrome-The reaction occurring in the body when a drug on which the body has acquired dependence is withdrawn .

Habituation-A situation in which one desires and becomes accus· tomed to a drug but is not physi· cally dependent upon it. Addiction-A combination of toler· ance, habituation and physical de· pendence.

the narcotics

The problem of narcotic addiction and abuse dates r from ancient times and its seriousne~s has increased with the years (see History of Drug Abuse, page 16). The popularity of the narcotics among those who want to escape lies in the effect of the drug on the mind. A feeling of being "high," similar to the feeling obtained with amphetamines, is desirable among addicts. In addition euphoria (a feeling of well-being), tranquillity and somnolence are desirable features also. Another effect is the "thrill" or turning in the stomach, a feeling of warmth and a tingling sensation in the abdomen similar to orgasm. Following the initia,l effects of the narcotic, the subject "goes on the nod," a dreamy state of imperturbability. Sleep comes easy but the subject can be aroused with little difficulty. Continued use of narcotics leads to physical dependence, tolerance, habituation and addiction. Symptoms of withdrawal from narcotics depend on the severity of the addiction and the degree of tolerance achieved. Involved also with the severity of withdrawal is the nature of the narcotic used. Symptoms range from mildsuch as yawning, lacrimation and perspiration-to moderate-such as tremors, loss of appetite and insomnia-to severe-such as diarrhea, vomiting, muscle pain and weight loss. Withdrawal symptoms may be brought on by withdrawing the drug from the addict or by injecting a narcotic antagonist such as Nalline. This has become the basis of the Nalline test for narcotic addiction which is used in many parts of the country. A small dose of Nalline will cause a mild withdrawal reaction such as a dilation of the pupil in the eyes of subjects who have taken narcotics recently. Once 'a n addict has experienced withdrawal ("cold turkey") and "kicked the habit," he has lost his tolerance and may get his kicks again on lower doses of narcotics which are less expensive. Addicts live under the perpetual threat of overdosage. This may come about through several means. An individual who has kicked the habit may miscalculate on how li-ttle his new dose should be. An addict, while under the influence of narcotics, alcohol or other drugs, may miscalculate his dose or the drug which is usually 'c ut with an excipient may be stronger than the "pusher" bas represented it to be.

Death from narcotic overdosage is caused by respiratory depression. Narcotics selectively depress the respiratory center in the brain. heroin Diacetylmorphine, "H," boy, horse, white stuff, Harry, hairy, joy powder, scot, doojee.

Heroin is from two to ten times as potent as morphine depending on measuring technics. The intense euphoria produced by the drug has made heroin the most popular narcotic among 'addicts. Similar to all narcotic agents, tolerance rapidly develops to the euphodc effects of the drug so that the user must ingest larger quantities to get his "kicks." An individual may begin with a dose of two to eight mg but addicts may use as much as 450 mg per day as tolerance is acquired. The drug is commonly administered intravenously ("mainline"). Other methods of administration are oral and inhalational. "Mainlining" gives the most pronounced and rapid effecthence its popuIar-ity. Heroin is synthesized from morphine. A process of acetylation using acetic anhydride with simple and inexpensive equipment will produce a high qua'l,i ty product with a good yield. Since heroin is more potent than morphine and the yield is high, it is economicaHy desirable to convert morphine to heroin. Opium, grown in Turkey, lis shipped to Lebanon where morphine is extracted. The morphine is then sent to France where it is converted to heroin. From France to Italy to New York, the circuit for heroin is completed. 3 morphine "M," white stuff, hard stuff, hocus, morpho, morphie, emsel, unkie, Miss Emma.

Morphine, the drug of choice in relief of pain, has taken second place to heroin as a drug of abuse. Nevertheless morphine is widely used by addicts, particularly when heroin is difficult to obtain. 'Morphine is capable of sustaining a heroin addict and inducing physical dependence in its own right. Euphoria can be produced with as little as 10 to 15 mg. Doses increase as tolerance is built up. other narcotic agents codeine

More commonly abused in the form of the exempt narcotic cough preparations, codeine is less addictive than morphine or heroin and less potent in terms of inducing euphoria. Withdrawal symptoms when they occur are less severe than with more potent drugs.

hydrocodone Hycodan, dihydrocodeinone

Before its change from an exempt narcotic to a class B narcotic, hydrocodone was fairly popular among the exempt narcotic abusers slince it is more addictive than codeine. Since its change in status, little effort has been expended in obtaining the drug in any great quantity. hydromorphone Dilaudid, dihydromorphinone

Hydromorphone, like morphine, is the next choice after heroin. Although about as potent as heroin as an analgesic, the compound does not appear to have the "thriU" -associated with "mainlining" possessed by heroin. Hydromorphone in doses of one to two mg intravenously the first time used will provide all the desired effects. meperidine Demerol

When first marketed, this agent was claimed to be devoid of addicting potential. Experience, however, proved otherwise. Addiction is slower to develop and is less vicious than with morphine. 4 oxycodone Percodan, dihydrohydroxycodeinone

This agent has recently been transferred from olass B to class A status because of its addicting potential. AIthougheffecvive oraUy, addicts dissolve tablets in water, filter out the insoluble binders and "mainline" the active drug. Transferring the drug to class A status has cut down significantly on its improper use. exempt narcotics

Exempt narcotics have for years been the target of drug abusers. Although not responsible for hard addiction, their easy availability has made them ideal for thrill-seeking youngsters and certain elements of the adu1t population. Many an addict has admitted that his road to addiction began with the exempt narcotic cough preparations or marihuana. Of the many exempt narcot-ic preparations 'available, the most popular are the codeine-containing cough mixtures and paregoric (P.G., P.C.). The cough preparations contain approximately one grain of codeine per fluid ounce and they are usually available in four-ounce containers. Paregoric, when ,available as an exempt preparation, is packaged in one- or two-ounce containers depending on state law. The usual five ml dose of paregoric contains two mg of morphine. Consuming two or three bottles of elixir of terpin hydrate and codeine or paregoric can supply eight to twelve grains of codeine and 24 to 36 mg of morphine. With the alcoholic content Vol. NS8, No. I, January 1968

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of 80 and 90 proof liquor the appeal of these compounds is obvious. These preparations usually are administered orally although paregoric addicts have been known to inject the product intravenously; the jugular vein in the neck and the antecubital and femoral veins are the locations of choice. A recent "epidemic" of paregoric addiction in Detroit turned up many addicts ("Gee Heads") with ulcerating sores of the neck, arms and legs from the attempted injection of paregoric. Irritation of the vein and surrounding tissue by the anise oil, camphor and benzoic acid contained in paregoric plus the unsanitary method of injection takes its toll. A common method of preparing paregoric is to boil the product until it takes on a cloudy appearance (precipitation of camphor). The camphor is removed with cotton and the remaining material injected. Amphetamine, barbiturates, glutethimide or tripelennamine have been used as additives to increase the effect. A favorite mixture among users of these preparations is a combination of elixir terpin hydrate and codeine and tablets of tripelennamine (Pyribenzamine) called "blue velvet." The high dose of antihistamine and codeine have combined depressant effects desired by some individuals. The combination antihistaminecodeine cough preparation has gained in popularity recently. Robitussin AC, a mixture of codeine, pheniramine maleate and glyceryl guaiacolate, particularly has been in demand by drug abusers. One may speculate on the effect of high doses of codeine, antihistamine and glyceryl guaiacol ate (a derivative of the muscle relaxant methocarbamol) . depressants

Barbiturates and other central nervous system depressants are used therapeutically to induce sleep and act as mild sedatives or "tranquilizers." These agents ,are not only habit-forming but also addicting. The extensive use of "tranquilizers" and "non-barbiturate" sedatives is responsible for much of today's drug abuse. On the basis of clinical impressions, barbiturate abuse, like alcohol abuse, is more socially acceptable than opiate abuse. 5 High doses of the sedatives create a feeling of elation, tranquility and well-being. Addicts have shown that 150 mg pentobarbital given intramuscularly is equivalent to 32 mg morphine. This fact strongly indicates that the barbiturates have the capacity to produce a type of euphoria. During chronic intoxication, the subject exhibits symptoms of ~ncoordination, ataxia, confusion and emotional instability. Motor incoordination is the 14

most serious effect and is responsible for personal injmies and automobile accidents. In this respect, chronic intoxication with barbiturates is not unlike that of alcohol. Partial, low-grade tolerance develops with the use of sedatives. The upper range of .barbiturate administration ranges from one to two and a half gm per day. Physical dependence develops with all sedativehypnotics. Withdrawal symptoms do not appear until 12 to 24 hours after the drug has been removed and the patient "sobers up." This delayed reaction often gives the patient a false indication of recovery without abstinence symptoms. The syndrome begins with anxiety, weakness, loss of appetite, and tremors and sleeplessness. The symptoms become more intense with time and include vomiting, hypotension, fever, uncontrolled tremors and grand mal convulsions. Convulsions have been noted as late as seven days after withdrawal of a drug. The most serious symptoms are convulsions, delirium and hypothermia which can endanger life, The probability of grand mal seizures occurring during withdrawa,l increases in direct ratio to the dose of the drug being abused. Daily doses of pentobarbital or secobarbital in excess of 0.4 gm have been claimed to produce a "clinically significant" degree of dependence. 5 Death from overdose of sedativehypnotics is usually caused by respiratory depression, similar to that from the narcotics. A common form of accidental death from these agents is the "suicide" where the subject while intoxicated continues to consume the depressant oblivious of his actions. All sedative-hypnotic agents are capable of causing intoxication, habituation and physical dependence and withdrawal symptoms occur when the drug is discontinued. These sedative agents are listed in the DACA list of controlled drugs (see JAPhA, August 1967). Chlordiazepoxide, diazepam and oxazepam, although not yet covered by DACA, are capable of causing physical dependence. pentobarbital sodium

Nembutal, yel/ow nimbie, nimby.

jackets,

yellows,

Four hundred mg per day is sufficient to produce a physical dependence, The route of administration is oral, but given the opportunity the addict will "mainline" the drug. amobarbital sodium

Amyta,l, blues, blue heaven, bluebirds, blue devils.

Dosage, route of administration and dependence appear to be similar to pentobarbita,l.

Journal of the AMERICAN PHARMACEUTICAL ASSOCIATION

secobarbital sodium

Seconal, reds, redbirds, saggy, seccy, pinks.

red

devils,

As in the case of pentobarbital, 400 mg daily is sufficient to produce physical dependence. Similar also to pentobarbital and amobarbital, secobarbital is a short-acting baI1biturate with a rapid onset of action. These shortacting barbiturates seem to be preferred over the longer-acting products such as phenobarbital. amobarbital and secobarbital Tuinal, rainbows, double trouble (See individual barbiturates for specific comments .) alcohol

Alcohol, as a depressant, is perhaps the most frequently abused of the sedatives. It causes acute and chronic intoxication, habituation, physical dependence and addiction. Withdrawal symptoms (delirium tremens) result when alcohol is discontinued. In chemistry and pharmacology, alcohol resembles chloral hydrate and paraldehyde_ bromides

Therapeutic use of bromides has decreased markedly over the last several years_ Likewise its abuse and misuse have decreased. The availability of sedative and headache products without prescription provides easy access to ,the drug and there are suU a few individuals who are suffering from chronic toxicity due to bromides (bromism). Bromism affects the skin in the form of acneform lesions. Constipation, loss of appetite and gastric distress are symptoms referable to the gastrointestinal tract. Psychic disturbances are most severe, however, with ''bromide psychosis" a frequent complication. chloral hydrate Mickey Finn, Mickey, Peter

Like the barbiturates, alcohol and other sedative-hypnotics, chloral hydrate causes habituation, tolerance and addiction. Addiction to chloral hydrate is less frequent than addiction to barbiturates, however. Due to its irritant effect on the gastrointestinal tract, addicts suffer from gastric symptoms_ This forces them to Iook elsewhere for their ''kicks.'' As wIth alcohol, large doses of the drug are necessary to susra
There is no evidence that ingesting in therapeutic doses will 'lead to physical dependence. Large doses in the range of 300 to (continued on page 22) chlordiazepo~ide

drugs of abuse on stamps 2

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These postage stamps picture various drugs of abuse, including (1-2) the opium poppy on UN and Hungary; (3) the growing of hemp or cannabis on Italy; (4) myristica on Grenada; (5) morning glory on Switzerland; (6) fly agaric (Amanita muscar;a) mushroom on Czechoslovakia; (7) peyote-like cactus on Kenya, Uganda and Tanganyika; (8) stramonium on Yugoslavia; (9) tobacco on Cuba; (10) vapors such as benzene on Germany; (11) alcohol on Japan _

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Vol. NS8, No_ 1, January 1968

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