Propoxyphene

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe (d)

Belgium: Depronal; Denmark: Abalgin, Doloxene; France: Dextropropoxyphene; Greece: Algaphan, Doloxene, Romidon, Zideron; Italy: Liberen; Luxembourg: Depronal; Netherlands: Depronal; Poland: Algifene; Spain: Deprancol; Sweden: Dexofen, Doloxene.

North America (d)

Canada: 642 Tablet, Darvon; USA: Darvon, Dolene, Propoxyphene.

Latin America

Mexico: Dibagesic; Saludex.

Drug combinations

Propoxyphene and Acetaminophen

Propoxyphene and Dipyrone

Chemistry

Propoxyphene Hydrochloride: C~22~H~29~NO~2~ HCl. Mw: 375.93. (1) Benzeneethanol, α-[2-(dimethylamino)-1-methylethyl]-α-phenyl-, propanoate (ester), hydrochloride, [S-(R*,S*)]-; (2)(2S,3R)-(+)-4-(Dimethylamino)-3-methyl-1,2-diphenyl-2-butanol propionate (ester) hydrochloride. CAS-1639-60-7; CAS-469-62-5 (propoxyphene)(1964).

Propoxyphene Napsylate: C~22~H~29~NO~2~ C~10~H~8~O~3~S H~2~O. Mw: 565.72. (1) Benzeneethanol, α-[2-(dimethylamino)-1-methylethyl]-α-phenyl-, propanoate (ester), [S-(R*,S*)]-, compd. with 2-naphthalenesulfonic acid (1:1), monohydrate; (2)(αS,1R)-α-[2-(Dimethylamino)-1-methylethyl]-α-phenylphenethyl propionate compound with 2-naphthalenesulfonic acid (1:1) monohydrate. CAS-26570-10-5; CAS-17140-78-2 (anhydrous)(1969).

Pharmacologic Category

Analgesics and Antipyretics; Opiate Agonists. (ATC-Code: N02AC).

Mechanism of action

Propoxyphene, as with other narcotic (opiate) analgesics, blocks pain perception in cerebral cortex by binding to specific receptor molecules (opiate receptors) within neuronal membranes of synapses.

Therapeutic use

Management of mild-to-moderate pain.

Pregnancy and lactiation implications

Withdrawal symptoms reported in neonate following propoxyphene use during pregnancy. Teratogenic effects also noted in case reports. Propoxyphene and norpropoxyphene excreted in breast milk.

Unlabeled use

Contraindications

Hypersensitivity to propoxyphene or any component of the formulation.

Warnings and precautions

May cause CNS depression. Propoxyphene is major cause of drug-related deaths when given in excessive doses, either alone or in combination with other CNS depressants (including alcohol). May cause hypotension (use with caution in hypovolemia, cardiovascular disease (including acute myocardial infarction), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics)). May obscure diagnosis or clinical course of acute abdominal conditions. Use with caution in adrenal insufficiency (including Addison’s disease), in biliary tract dysfunction (acute pancreatitis may cause constriction of sphincter of Oddi), and in CNS depression or coma. Should not be prescribed in severely depressed or suicidal patients. Use with caution in history of drug abuse or acute alcoholism (potential for drug dependency exists). Tolerance, psychological and physical dependence may occur with prolonged use. Use with extreme caution in head injury, intracranial lesions, or elevated intracranial pressure (exaggerated elevation of intracranial pressure may occur). Use with caution in hepatic impairment, in morbidly obese patients, in prostatic hyperplasia and/or urinary stricture, in renal impairment (avoid use in CrCl <10 mL/minute), and in thyroid dysfunction. Effects may be potentiated when used with other sedative drugs or ethanol. Use with caution in debilitated patients (greater potential for critical respiratory depression), and in the elderly (may be more sensitive to adverse effects). Optimal analgesic dose varies widely among patients. Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with μ-opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms.

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