Dextropropoxyphene

Indications
Oral
Mild to moderate pain
Adult: As hydrochloride: 65 mg 3-4 times daily. As napsilate: 100 mg 3-4 times daily.
Renal impairment: Dose reduction may be needed.
Hepatic impairment: Dose reduction may be needed.
Contraindications
Hypersensitivity, chronic resp diseases, porphyria, pregnancy. Patients on MAOI treatment or within 2 wk of stopping treatment.
Warnings / Precautions
Suicidal patients, hepatic or renal disease; lactation, elderly.
Adverse Reactions
Dizziness, sedation, weakness; nausea, vomiting, constipation; rash, urticaria; visual disturbances; physiological dependence.
Potentially Fatal: Convulsions in long-term therapy. Cardiac conduction abnormalities and arrhythmias; liver impairment.
Overdose Reactions
Symptoms: Coma, respiratory depression, circulatory collapse, pulmonary oedema, seizures, nephrogenic diabetes insipidus, ECG abnormalities. Death may occur as early within the 1st 15 minutes to 1 hr. Management: Intensive symptomatic and supportive therapy to be instituted immediately. IV naloxone may reverse intoxication. Induction of emesis or gastric lavage followed by activated charcoal helps to reduce absorption. Monitor blood gases, pH, electrolytes and ECG. Dialysis is unlikely to be useful.
Drug Interactions
Inhibits hepatic metabolism of benzodiazepines, β-blockers, carbamazepine, phenytoin and warfarin. Increased risk of toxicity when co-administered with ritonavir. Potentiation of depressant effects when used with alcohol or CNS depressants.
Potentially Fatal: Accidental or intentional overdosage fatal (especially if combined with alcohol, and analgesics e.g. paracetamol and aspirin).
See Below for More dextropropoxyphene Drug Interactions
Food Interactions
Absorption decreased.
Mechanism of Actions
Dextropropoxyphene is a relatively weak opioid analgesic which binds to mu- and kappa-receptors in order to block pain perception in the cerebral cortex. This results in inhibiton of pain sensation flow into high centers.
Absorption: Readily absorbed from the GI tract; napsilate form more slowly absorbed than the HCl (oral); peak plasma concentrations after 1-2 hr.
Distribution: Concentrated in the liver, lungs and brain; crosses the placenta and small amounts enter breast milk. Protein-binding: 80%.
Metabolism: Hepatic, to nordextropropoxyphene (norpropoxyphene); undergoes 1st-pass metabolism.
Excretion: Urine (as metabolites). Elimination half-life: 6-12 hr (dextropropoxyphene), 30-36 hr (norpropoxyphene).
Administration
May be taken with or without food.
Storage Conditions
Oral: Store at 15-30°C.
ATC Classification
N02AC04 - dextropropoxyphene ; Belongs to the class of diphenylpropylamine derivative opioids. Used to relieve pain.
Storage
Oral: Store at 15-30°C.
Available As
  • Dextropropoxyphene 30 mg
  • Dextropropoxyphene 32 mg
  • Dextropropoxyphene 32.5 mg
  • Dextropropoxyphene 32.5mg
  • Dextropropoxyphene 33 mg
  • Dextropropoxyphene 65 mg
  • Dextropropoxyphene 70 mg
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