Dextropropoxyphene


Generic Medicine Info
Indications and Dosage
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.
Administration
May be taken with or without food.
Contraindications
Hypersensitivity, chronic resp diseases, porphyria, pregnancy. Patients on MAOI treatment or within 2 wk of stopping treatment.
Special 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.
Overdosage
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).
Food Interaction
Absorption decreased.
Action
Description:
Mechanism of Action: 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.
Pharmacokinetics:
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).
Storage
Store at 15-30°C.
MIMS Class
Analgesics (Opioid)
Disclaimer: This information is independently developed by MIMS based on Dextropropoxyphene from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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