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Propoxyphene (Darvon)

(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.

Propoxyphene

Dextropropoxyphene is an analgesic in the opioid category. It is used to treat mild to moderate pain and as an antitussive. It can be used to ease pain before, during and after an operation. It is often combined with paracetamol (Acetaminophen) in the preparation co-proxamol, however, there is no evidence that this combination is any more effective than paracetamol alone (This combination is known as Darvocet in the US and Capadex or Di-Gesic in Australia). It is manufactured and marketed by Eli Lilly and Company.

Dextropropoxyphene, like codeine, is a "weak" opioid. Codeine is more commonly used; however, some individuals (approximately 10-20% of the Caucasian population) are unable to metabolize it, due to poor functioning of the enzyme CYP2D6. It is in these people that dextropropoxyphene is particularly useful, as its metabolism does not require CYP2D6.

In the United States, dextropropoxyphene HCl is available as a prescription formulation with acetaminophen in ratio anywhere from 30mg / 600mg to 100mg / 650mg, respectively. These are usually named "Darvocet." On the other hand, "Darvon" is a pure Propoxyphene preparation available in the U.S. that does not contain acetaminophen.

Darvon, a dextropropxyphene made by Eli Lilly, which had been on the market for 25 years, came under heavy fire in 1978 by consumer groups that said it was associated with suicide. Darvon was never withdrawn from the market, but Lilly has waged a sweeping, and largely successful, campaign among doctors, pharmacists and Darvon users to defend the drug as safe when it is used in proper doses and not mixed with alcohol.

* page last updated 5/21/2008

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

 

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