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Propoxyphene
Propoxyphene is a weak opioid analgesic and depressant1 of the diphenylpropylamine class2. It is used to treat mild pain3 and also has cough suppressant and local anaesthetic effects. Its pain-relieving activity is lower than that of codeine. It is habit-forming3 and carries risks of fatal overdose3 and heart arrhythmias.3
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Threshold~30 mg
Light30-65 mg
Moderate65-100 mg
Strong100-200 mg
Heavy200+ mg
Duration
Onset20-30 minutes
After Effects2-6 hours
Total1-3 hours
Subjective Effects
Subjective Effects not written up yet
Pharmacology
Pharmacodynamics
Propoxyphene acts as a μ-opioid receptor agonist.4 It also potently blocks α3β4 neuronal nicotinic acetylcholine receptors through a noncompetitive mechanism and weakly inhibits serotonin reuptake. It blocks cardiac sodium channels5 and has local anesthetic activity at concentrations approximately ten times those needed for opioid effects.6
Pharmacokinetics
Propoxyphene napsylate is very slightly soluble in water.7 Propoxyphene can remain detectable for up to nine days after the last dose, with trace amounts potentially persisting longer.
Interactions
Interactions not written up yet
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Tolerance not written up yet
Harm Potential
Addiction & Dependence
Psychological
Propoxyphene is habit-forming and has recognized addiction potential.8
Toxicity
Small increases above the therapeutic dose can cause severe toxicity and fatal overdose. Fatalities have also occurred when patients with depression or suicidal tendencies misused propoxyphene.
Propoxyphene can cause cardiac arrhythmias at typical doses, while poisoning can decrease heart rate, contractility, and cardiac electrical conduction; severe cardiotoxicity can occur with small increases above the therapeutic dose.
Propoxyphene poisoning causes central nervous system depression.9
Propoxyphene poisoning can cause respiratory depression,10 aspiration pneumonia, and pulmonary edema.
Seizure Risk
Seizures can occur in propoxyphene poisoning10 and may arise from opioid or local anesthetic effects.
History & Culture
Legality
International
European and U.S. markets removed propoxyphene because of fatal-overdose and heart-arrhythmia concerns.
By Country
Illegal1
United StatesIllegalUnder 21 C.F.R. § 1308.12(c)(5), bulk non-dosage dextropropoxyphene has been listed in Schedule II since September 22, 1980; under that paragraph's opiate scope, the listing includes chemically possible isomers, esters, ethers, salts, and salts of isomers, esters, and ethers, but excludes levopropoxyphene and applies unless specifically excepted or placed in another schedule. Section 1308.14(b)(2) separately places in Schedule IV, unless specifically excepted or listed in another schedule, any material, compound, mixture, or preparation containing dextropropoxyphene, specifically alpha-(+)-4-dimethylamino-1,2-diphenyl-3-methyl-2-propionoxybutane, or its salts. The Drug Enforcement Administration identifies propoxyphene as another name for dextropropoxyphene and assigns code 9273 to bulk non-dosage forms and code 9278 to dosage forms. Federal law prohibits manufacture, distribution, dispensing, and possession with intent to manufacture, distribute, or dispense except as authorized; it prohibits knowing or intentional possession unless obtained directly or through a valid prescription or order from a practitioner acting in professional practice, or otherwise authorized.
References
Citations
Article Status
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