Codeine addiction

The opium narcotics used in the U.S. are, particularly, morphine and heroin, especially the former but juveniles definitely prefer heroin. Heroin has greater addiction liability than other narcotics, produces more euphoria and stimulation, requires smaller doses, and is easier to traffic in illicitly. Codeine addiction is rare because the drug produces relatively little euphoria, and is thus less desirable to the potential addict, and because it is quite expensive and bulky in effective amounts. Codeine addicts are usually persons who originally received the drug for clinical purposes. Many narcotic addicts also use cocaine, usually in combination with heroin, and resort to whisky or barbiturate when their supply of narcotic is low. Every conceivable method and route are used to get the narcotic into the body. Morphine and heroin, however, are ordinarily taken hypodermically or intravenously cocaine and heroin are employed by snuffing. The use of galenical preparations of opium is rare in the U.S. Occasionally, however, a paregoric addict is discovered. 

Serious addiction to codeine is not as common as it once was, possibly due to the availability of greater numbers of competing, more potent opioids. The perception by some that addiction to a weak opioid like codeine is not serious results in fewer individuals seeking treatment for their codeine addiction. However, in those cases where treatment is needed, codeine addiction should be approached in the same manner as addiction to other opioids, such as heroin or morphine. 

Sectional analysis of a hair sample of a codeine addict. The proximal hair section was natural hair, the distal 3 sections were bleached. 

Most of us are aware of the big Codeine cough-syrup scare of the early 60 s. All of a sudden, with a history going back to the Civil War, we "discover" a few milder Codeine addicts are still around, and set out to stomp them out via the media. As a result, some heavy anti-cough syrup legislation was created, and millions of people became aware that Codeine existed. Abuse rate shot way up, and to this date we still have... 

By 1930 codeine addiction was still an infrequent reality, but the medical use of codeine was increasing. A study of the narcotic prescriptions showed that for a number of patients a first prescription had been w ritten for codeine in therapeutic amounts next came orders for larger amounts at shorter intervals and finally for addiction-sustaining amounts of morphine, heroin, or opium. 

Codeine, mol wt 299.3, is a significantly less potent analgesic than morphine, requiring 60 mg (0.20 mmol) to equal the effectiveness of 10 mg (0.04 mmol) of morphine. However, codeine is orally effective, and it is less addictive and associated with less nausea than morphine. Codeine is used as an antitussive agent, although newer, nonaddictive agents are preferred (see Expectorants, antitussives, and related agents). 

Codeine, like morphine, is isolated from the opium poppy. However, the low yield of 0.7—2.5% does not provide sufficient material to meet commercial demands. The majority of marketed codeine is prepared by methylating the phenolic hydroxyl group of morphine. Morphine yields from opium poppy are 4—21%. When prescribed for cough, the usual oral dose is 10—20 mg, three to four times daily. At these doses, adverse side effects are very few. Although the abuse potential for codeine is relatively low, the compound can substitute for morphine in addicts (47). 

Hydromorphone [466-99-9] (31) and hydrocodone [125-29-1] (32) are isomers of morphine and codeine, respectively. Hydromorphone can be prepared by catalytic rearrangement of morphine (49) or by oxidation of the aliphatic hydroxyl group of dihydromorphine (50). Hydrocodone can be similarly prepared. As an antitussive, hydromorphone is several times more active than morphine and hydrocodone is slightly more active than codeine. Hydromorphone has a much higher addiction potential than hydrocodone. 

Dihydrocodeine [125-28-0] (33), introduced in Germany before 1930, and dihydrocodeinone enol acetate [466-90-0] (34) both have clinical activity and addiction potential comparable to codeine. 

Nonnarcotic Antitussives. The most centrally active, noimarcotic antitussive is dextromethorphan [125-71-3] (39). It is similar to codeine in terms of potency and mechanism of action, ie, it is a direct depressant of the cough center. It is unique in that even though it is stmcturaHy related to codeine, it is not addictive. 

Levopropoxyphene [2338-37-6] (42), the optical antipode of the dextrorotatory analgetic propoxyphene, is an antitussive without analgetic activity. The 2-naphthalenesulfonate salt has a less unpleasant taste than the hydrochloride salt, and is widely used. Clinical effectiveness has been demonstrated against pathological and artificially induced cough, but the potency is somewhat less than codeine. The compound is reported not to cause addiction. Levopropoxyphene can be prepared (62) by first resolving [ -dimethylamino-CX-methylpropiophenone with dibenzoyl-(+)-tartaric acid. The resolved... 

Codeine (morphine methyl ether) resembles morphine in its general effect, but is less toxic and its depressant action less marked and less prolonged, whilst its stimulating action involves not only the spinal cord, but also the lower parts of the brain. In small doses in man it induces sleep, which is not so deep as that caused by morphine, and in large doses it causes restlessness and increased reflex excitability rather than sleep. The respiration is slowed less than by morphine (cf. table, p. 261). Cases of addiction for codeine can occur but according to Wolff they are rare. The best known ethers of morphine are ethylmorphine and benzyl-morphine [cf., table, p. 261), both used to replace morphine or codeine for special purposes. 

Codeine (Cod), a powerful and addictive painkiller, is a weak base. 

Tramadol is a pain reliever (analgesic). Its action is similar to opioid narcotics such as codeine and morphine, but it does not depress breathing the way the others can, and less often leads to abuse and addiction. 

Morphine and related opiates are known to suppress the cough reflex these compounds have thus been used extensively in antitussive preparations. Since this activity is not directly related to the analgesic potency, the ideal agent is one that has much reduced analgesic activity and thus, presumably, lower addiction potential. The weak analgesic codeine (4) is... 

The answer is c. (Hardman, pp 528-537.) Morphine is a pure agonist opioid drug with agonist activity toward all the opioid subtype receptor sites. In high doses, deaths associated with morphine are related to the depression of the respiratory center in the medulla. Morphine has a high addiction potential related to the activity of heroin or dihydromorphine. Codeine has a significantly lower addiction potential. 

Dihydromorphinone is 3-4 times more powerful than morphine and dihydrocodeinone is just a little less than morphine in potency. Their pitfall is an addiction liability, as great if not greater than morphine. To produce Hydrogenate morphine or codeine in a warm, strongly acidic solution, in a large excess of palladium or platinum catalyst, as per instructed in the reductions chapter. 

Codeine. Is a narcotic derived from morphine and is addictive. It can be purchased over the counter, but you will have to sign for it. Sometimes you will have to show identification. It creates feelings of euphoria and weightlessness with doses of about 50 to 150 mg. It can also be made much more potent by hydrogenating to dihydrocodeinone as instructed in the analgesic chapter in this book. 

Codeine is similar to morphine in terms of properties, but its pain-relieving ability is significantly less and it causes addiction to some degree. This drug is very effective in oral use and is used for average to moderate pain. It is often used as an antitussive drug. Synonyms for codeine are codyl, acutus, and others. 

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