Propoxyphene is a synthetic opioid analgesic and antitussive drug that is widely used in the treatment of pain and cough. It has been used since the early 1960s and is still widely used in many developing countries today. This article will discuss the pharmacology, pharmacokinetics, clinical uses, and safety of propoxyphene.
Pharmacology:
Propoxyphene is a centrally-acting analgesic and antitussive drug. It produces its effects by binding to the μ-opioid receptor, as well as the κ-opioid receptor. It has a relatively weak opioid agonist effect, with a potency of approximately one-sixth that of morphine. It also produces additive effects when combined with other opioid agonists, such as morphine and codeine. Propoxyphene has a high safety margin and is not associated with significant respiratory depression or other serious side effects.
Pharmacokinetics:
Propoxyphene is rapidly absorbed from the gastrointestinal tract following oral administration. Its bioavailability is approximately 70-80%. The drug is metabolized primarily by the liver, with metabolites being excreted primarily in the urine. Its elimination half-life is approximately 3-4 hours.
Clinical Uses:
Propoxyphene is primarily used as an analgesic for the treatment of mild to moderate pain. It is also used as an antitussive to relieve cough. The drug is well-tolerated and has a relatively low risk of serious side effects.
Safety:
Propoxyphene has a high safety margin and is not associated with significant respiratory depression or other serious side effects. However, the drug has been associated with a number of adverse effects, including dizziness, drowsiness, nausea, vomiting, constipation, and headaches. It is important to use caution when administering propoxyphene in patients with a history of substance abuse or addiction, as it can be habit-forming.
Conclusion:
Propoxyphene is a centrally-acting analgesic and antitussive drug that is widely used in the treatment of pain and cough. It has a relatively low risk of serious side effects, but should be used with caution in patients with a history of substance abuse or addiction.
References
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Papaleontiou, M., & Fudin, J. (2016). Opioid pharmacology. In J. Fudin (Ed.), Opioid Pharmacology (pp. 1-17). Boca Raton, FL: CRC Press.