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Codeine

(prescription opioids)

Summary of Opioids

Opioids are commonly prescribed because of their effective analgesic, or pain relieving, properties. Studies have shown that properly managed medical use of opioid analgesic compounds is safe and rarely causes addiction. Taken exactly as prescribed, opioids can be used to manage pain effectively.

Among the compounds that fall within this class—sometimes referred to as narcotics—are morphine, codeine, and related medications. Morphine is often used before or after surgery to alleviate severe pain. Codeine is used for milder pain. Other examples of opioids that can be prescribed to alleviate pain include oxycodone (OxyContin—an oral, controlled release form of the drug); propoxyphene (Darvon); hydrocodone (Vicodin); hydromorphone (Dilaudid); and meperidine (Demerol), which is used less often because of its side effects. In addition to their effective pain relieving properties, some of these medications can be used to relieve severe diarrhea (Lomotil, for example, which is diphenoxylate) or severe coughs (codeine).

Opioids act by attaching to specific proteins called opioid receptors, which are found in the brain, spinal cord, and gastrointestinal tract. When these compounds attach to certain opioid receptors in the brain and spinal cord, they can effectively change the way a person experiences pain.

In addition, opioid medications can affect regions of the brain that mediate what we perceive as pleasure, resulting in the initial euphoria that many opioids produce. They can also produce drowsiness, cause constipation, and, depending upon the amount taken, depress breathing. Taking a large single dose could cause severe respiratory depression or death.

Opioids may interact with other medications and are only safe to use with other medications under a physician's supervision. Typically, they should not be used with substances such as alcohol, antihistamines, barbiturates, or benzodiazepines. Since these substances slow breathing, their combined effects could lead to life-threatening respiratory depression.

Codeine

Codeine is sometimes marketed in combination preparations with paracetamol (acetaminophen) as co-codamol or paracod (best known in North America as Tylenol 3), with aspirin as co-codaprin or with ibuprofen. These combinations provide greater pain relief than either agent alone (drug synergy; see synergy). Codeine is also commonly compounded with other pain killers or muscle relaxers such as Fioricet with Codeine, Soma Compound/Codeine, etc. Codeine-only products can be obtained with a prescription as a time release tablet (eg. Codeine Contin(r) 100mg).

In the United States, codeine is regulated by the Controlled Substances Act. It is a Schedule II controlled substance for pain-relief products containing codeine alone or more than 90 mg per dosage unit. In combination with aspirin or acetaminophen (paracetamol/Tylenol) it is listed as Schedule III or V, depending on formula. Preparations for cough or diarrhoea containing small amounts of codeine in combination with two or more other active ingredients are Schedule V in the US, and may be dispensed in amounts up to 4 fl. oz. per 48 hours without a prescription.

Common adverse drug reactions associated with the use of codeine include euphoria, itching, nausea, vomiting, drowsiness, dry mouth, miosis, orthostatic hypotension, urinary retention and constipation.

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.

Another side effect commonly noticed is the lack of sexual drive.

* page last updated 5/18/2008

 

Source: National Institute on Drug Abuse (NIDA), various other sources

 

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