Chemical Abstracts Service Registry Number: 469-62-5. (Hydrochloride form 1639-60-7)
Formal Names: Algaphan, Algodex, Antalvic, Darvocet, Darvon, Depronal, Develin, Dexofen, Distalgesic, Dolene, Dolocap, Doloxene, Doraphen, Erantin, Mardon, Novopropoxyn, Pro-65, Proxagesic, Wygesic Informal Names: Pink Ladies, Pumpkin Seeds Type: Depressant (opioid class). See page 24
Federal Schedule Listing: Schedule II and Schedule IV controlled substance, depending on amount (large quantities are Schedule II, DEA no. 9273; individual doses are Schedule IV, DEA no. 9278) USA Availability: Prescription Pregnancy Category: C
Uses. Propoxyphene has two isomers that are mentioned in drug control matters. Isomers are varieties of a chemical having the same components but different appearances; we might say that a person's right hand is an isomer of the left hand. The levopropoxyphene isomer of propoxyphene may work as a cough suppressant and is not a scheduled substance. The dextropropox-yphene isomer is the controlled substance and for convenience is simply called propoxyphene in this book.
Propoxyphene is a relatively mild pain reliever introduced in the 1950s. As the 1970s began, it was the most commonly prescribed pain reliever in America. One authority describes codeine as three times stronger than propoxyphene; another says the two drugs are about equal. Either way, propoxyphene is one of the less potent opioids. A typical use is for easing chronic moderate pain, as in osteoarthritis, rheumatoid arthritis, or other afflictions of the joints. The drug is also given to control early stages discomfort in cancer and has had experimental success in treating headache. In addition to pain reduction, propoxyphene has shown occasional usefulness for treating "restless leg syndrome," a condition in which people have difficulty sleeping and feel a need to frequently move their limbs day and night. Little or no improvement was seen, however, when an experiment used the drug against Tourette's syndrome, an affliction involving tics.
The substance has cross-tolerance with other opiates/opioids and can com bat their withdrawal symptoms. Propoxyphene is related to methadone so closely that propoxyphene can cause a false positive for methadone in drug screens.
Drawbacks. Normal medical doses of propoxyphene seldom produce unwanted effects, but those can include nausea, vomiting, constipation, sleepiness, and dizziness. Occasional cases of liver damage have been attributed to the drug. Extended use of propoxyphene suppositories can cause ulcerations. Injecting the drug can cause muscle damage at the injection site, and injecting the oral format can cause lung damage. Blood sugar levels can drop when taking propoxyphene, a condition that is easy to treat but that can become serious if ignored (as when an abuser is unconscious). A study of medical records found seizures to be common among abusers who had taken high doses daily for years, but those records did not demonstrate cause and effect. Case reports have attributed deafness and blindness to propoxyphene abuse. Examination of thousands of medical records determined that old people who use propoxyphene are more likely to become unsteady and break their hips in a fall, and this risk increases if the old persons are also taking drugs intended to alter their mental state. Propoxyphene may cause euphoria. That effect is noted in horses as well; the substance also makes them more physically active, perhaps tempting unscrupulous individuals to dose horses before races.
One human experiment found that the substance slowed reaction times and interfered with recognizing pictures, results that may be relevant to driving skills. Another study using the same dosage, however, found the drug to have no significant impact on decision making, picture recognition, or reaction time. Investigators running still another experiment concluded that the normal doses of the drug do not impair driving. Nonetheless, people are supposed to be warned against operating dangerous machinery while using the drug.
Propoxyphene overdose deaths became so common in the 1970s that the U.S. Food and Drug Administration warned that the dangers of this mild drug needed more respect from prescribers and users. Similar concerns were expressed in Great Britain during the 1980s, in Denmark during the 1990s, and in Sweden as the twenty-first century began.
Abuse factors. Despite propoxyphene's relative mildness, tolerance and dependence can occur if a person takes large doses long enough. Case reports tell of individuals who became so addicted that switching the persons to meth-adone became necessary. Other case reports relate instances of propoxyphene dependence so strong that psychosis developed during withdrawal. Propox-yphene itself has been used as a maintenance drug for addicts being switched from some other opiate/opioid. One study found propoxyphene to be about 80 times weaker than methadone when used for this purpose.
A study noted that a group of adolescents being treated for illicit propox-yphene use had multiproblem lifestyles, and analysis of propoxyphene overdose deaths in Los Angeles revealed that all the persons had led troubled lives involving different drug overdoses, arrests, strife with other persons, mental afflictions, and suicide attempts. That analysis prompted the investigator to ask whether availability of this drug and other opiates/opioids posed a risk to normal persons or just to abnormal people. Other research presented find ings relevant to that question: In a group of 37 rheumatic patients using a combination pharmaceutical containing propoxyphene, none were abusing the drug. When a group of 135 hospitalized psychiatric patients received unlimited access to the drug, the level of use roughly correlated with the level of personality disturbance, but all used it for proper medical purposes. Compared to a general population, hospitalized psychiatric patients should be more prone to drug abuse, so their lack of interest in propoxyphene is noteworthy.
Drug interactions. Propoxyphene's actions can be impeded if a person smokes tobacco cigarettes. Propoxyphene can lengthen the time span of effects produced by alprazolam and diazepam. Studies have found that blood levels from a dose of the epilepsy medicine carbamazepine will be higher if a person also takes propoxyphene, possibly high enough to cause harm. Propoxyphene should be used with particular caution if a person is also using alcohol, antidepressants, antihistamines, or tranquilizers. Conceivably the alcohol-propoxyphene combination could seriously impair driving skills, although scientists testing various mental and physical performance effects of the combination found that alcohol had more impact than propoxyphene.
Cancer. The drug has been suspected of promoting a form of cancer called multiple myeloma, but analysis of several hundred sets of medical records failed to link propoxyphene with the disease.
Pregnancy. Rats with prenatal exposure to propoxyphene have seemed physically normal but show some abnormal behavior. Studies with hamsters led an investigator to warn that the drug may cause congenital malformations. A case report discusses birth defects in a child born to a woman who routinely used propoxyphene during pregnancy, but we do not know if those malformations were caused by the drug. Such reports about propoxyphene are rare. A small survey of medical records found no association between propoxy-phene and birth defects. The drug passes into a human fetus, and infants born to pregnant women taking propoxyphene can be dependent on the drug. The drug passes into human milk but apparently causes no harm to nursing infants.
Additional information. Propoxyphene napsylate (CAS RN 17140-78-2 or monohydrate form 26570-10-5) is another variety of this drug. Differences between the hydrochloride version and the napsylate version may lead a medical practitioner to choose one over the other for a particular patient, but they are used for the same purposes and have about the same actions. Rat studies found no evidence that the napsylate form caused birth defects.
Additional scientific information may be found in:
"Dangers of Dextropropoxyphene." British Medical Journal 1 (1977): 668. Jonasson, U., B. Jonasson, and T. Saldeen. "Middle-Aged Men—A Risk Category Regarding Fatal Poisoning Due to Dextropropoxyphene and Alcohol in Combination." Preventive Medicine 31 (2000): 103-6. Miller, R.R., A. Feingold, and J. Paxinos. "Propoxyphene Hydrochloride: A Critical
Review." Journal of the American Medical Association 213 (1970): 996-1006. Ng, B., and M. Alvear. "Dextropropoxyphene Addiction—A Drug of Primary Abuse." American Journal of Drug and Alcohol Abuse 19 (1993): 153-58.
Rosenberg, W.M., et al. "Dextropropoxyphene Induced Hepatotoxicity: A Report of Nine Cases." Journal of Hepatology 19 (1993): 470-74.
Saarialho-Kere, U., et al. "Psychomotor Performance of Patients with Rheumatoid Arthritis: Cross-Over Comparison of Dextropropoxyphene, Dextropropoxyphene plus Amitriptyline, Indomethacin, and Placebo." Pharmacology and Toxicology 63 (1988): 286-92.
Salter, F.J. "Propoxyphene: Dependence, Abuse and Treatment of Overdosage." American Journal of Hospital Pharmacy 28 (1971): 208-10.
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