Drug Guide


By Anthony McDaniel, M.D.

Codeine or 3-methylmorphine (a natural isomer of methylated morphine, the other being the semi-synthetic 6-methylmorphine) is an opiate used for its analgesic, antitussive, and antidiarrheal properties. Codeine is the second-most predominant alkaloid in opium, at up to 3 percent; it is much more prevalent in the Iranian poppy (Papaver bractreatum), and codeine is extracted from this species in some places although the below-mentioned morphine methylation process is still much more common. It is considered the prototype of the weak to midrange opioids. Common effects other than analgesia associated with the use of codeine include euphoria, itching, nausea, vomiting, drowsiness, dry mouth, miosis, orthostatic hypotension, urinary retention, depression and constipation. Another side effect commonly noticed is the lack of sexual drive and increased complications in erectile dysfunction. Some people may also have an allergic reaction to codeine, such as the swelling of skin and rashes. Erectile dysfunction and diminished libido can be a longer-term effect (years to decades) of many narcotic analgesics due to development of central hypogonadism; this appears to be an especially common effect of methadone. The observation that acute effects of codeine, dihydrocodeine, oxycodone, hydrocodone, morphine, and include an increase in libido in women and a plurality of men has been made ab initio for the aforementioned and for 2500 years or longer with opium -- presumably anxiolysis, euphoria, effects of co-administered substances like caffeine, and environmental factors are involved.

Codeine and morphine as well as opium were used for control of diabetes until relatively recently, and still in rare cases in some countries, and the hypoglycaemic effect of codeine, although usually weaker than that of morphine, diamorphine, or hydromorphone, can lead to cravings for sugar. Tolerance to many of the effects of codeine develops with prolonged use, including therapeutic effects. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance. A potentially serious adverse drug reaction, as with other opioids, is respiratory depression. This depression is dose-related and is the mechanism for the potentially fatal consequences of overdose. As codeine is metabolized to morphine, morphine can be passed through breast milk in potentially lethal amounts, fatally depressing the respiration of a breastfed baby.

As with other opiate-based pain killers, chronic use of codeine can cause physical dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops the medication. Withdrawal symptoms include: drug craving, runny nose, yawning, sweating, insomnia, weakness, stomach cramps, nausea, vomiting, diarrhea, muscle spasms, chills, irritability, and pain. To minimize withdrawal symptoms, long-term users should gradually reduce their codeine medication under the supervision of a healthcare professional. A support group called Codeine Free exists to help people who have found themselves dependent on codeine.

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