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Brand Name :
Darvon, PP-Cap 
Synonyms :
D-propoxyphene, Dextropropoxyphene, Dextropropoxyphene-M, Dextroproxifeno, propoxyphene HCl 
Class :
Neuropsychiatric agent, Opioid analgesics, Opioid receptor agonist, mu-Opioid receptor agonist 
Brand Name :
Darvon, PP-Cap 
Synonyms :
D-propoxyphene, Dextropropoxyphene, Dextropropoxyphene-M, Dextroproxifeno, propoxyphene HCl 
Class :
Neuropsychiatric agent, Opioid analgesics, Opioid receptor agonist, mu-Opioid receptor agonist 
Dosage forms& StrengthsÂ
Tablets/ CapsulesÂ
65 mg Â
100 mg Â
Safety and efficacy studies are not establishedÂ
combining CNS depressants with propoxyphene may result in an additive CNS depression
combining CNS depressants with propoxyphene may result in an additive CNS depression
combining CNS depressants with propoxyphene may result in an additive CNS depression
combining CNS depressants with propoxyphene may result in an additive CNS depression
combining CNS depressants with propoxyphene may result in an additive CNS depression
may enhance the severity of adverse effects when combined
may enhance the severity of adverse effects when combined
may enhance the severity of adverse effects when combined
may enhance the severity of adverse effects when combined
may enhance the severity of adverse effects when combined
may reduce the therapeutic effect
may reduce the therapeutic effect
may reduce the therapeutic effect
acetaminophen/dextromethorphan/pseudoephedrine/guaifenesin
it may diminish the excretion rate when combined with analgesics, resulting in an enhanced serum level
acetaminophen, pheniramine, and phenylephrine
it may diminish the excretion rate when combined with analgesics, resulting in an enhanced serum level
diltiazem has the potential to modify the metabolism of propoxyphene, resulting in increased levels of propoxyphene in the bloodstream
itraconazole has the potential to modify the metabolism of propoxyphene, resulting in increased levels of propoxyphene in the bloodstream
nelfinavir has the potential to modify the metabolism of propoxyphene, resulting in increased levels of propoxyphene in the bloodstream
ketoconazole has the potential to modify the metabolism of propoxyphene, resulting in increased levels of propoxyphene in the bloodstream
nefazadone has the potential to modify the metabolism of propoxyphene, resulting in increased levels of propoxyphene in the bloodstream
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
verapamil has the potential to modify the metabolism of propoxyphene, resulting in increased levels of propoxyphene in the bloodstream
amprenavir has the potential to modify the metabolism of propoxyphene, resulting in increased levels of propoxyphene in the bloodstream
Actions and spectrum:Â
Although the exact mechanism of action of the drug is not known, it may stimulate the opioid receptors in the brain. In vitro studies suggest that the drug and its metabolite norpropoxyphene might inhibit the sodium channels with the metabolite being twice potent than the parent drug and ten-folds more active than lidocaine. Â
Black box warningÂ
Do not discontinue the medication without the suggestion of the doctor. Â
Do not operate heavy machinery or drive vehiclesÂ
Contraindications/CautionÂ
ContraindicationsÂ
HypersensitivityÂ
CautionsÂ
Renal impairment Â
Biliary tract/pancreatic disease Â
Hepatic impairment Â
Drug interactions Â
Tolerance Â
Geriatrics Â
Physical dependence Â
Pregnancy  Â
BreastfeedingÂ
Pregnancy & breastfeeding:Â
Pregnancy consideration:Â
USFDA pregnancy category: Not assignedÂ
Breastfeeding warnings:Â
It is known to be compatible with lactating mothers. Small amounts of the drug and its active metabolite is known to be excreted into breast milk.Â
Pregnancy category:Â
Pharmacology:Â
Propoxyphene is a narcotic analgesic which is centrally acting. It is also known as dextropropoxyphene and a synthetic weak opioid that is similar to methadone structurally.Â
Pharmacodynamics:Â
Propoxyphene, a synthetic opioid agonist, is a compound that has the same elemental features as methadone and acts generally like opiates. Its painkilling activity is due to dextropropoxyphene, the d-isomer which supplies opiate receptors and hence decreases the perception of the pain stimuli. Propoxyphene has almost no antitussive action and does not reduce fevers.Â
Pharmacokinetics:Â
Absorption:Â
Peak effects can be achieved in 2 to 2.5 hoursÂ
Distribution:Â
The volume of distribution is 16L/kg and 80% of the drug is known to be bound to proteins.Â
Metabolism:Â
It undergoes first-pass metabolism in the liver. It undergoes N-demethylation by CYP3A4 to produce norpropoxyphene, an active metabolite of the drug.Â
Elimination:Â
Its major and active metabolite is excreted via kidneys. Approximately 20%- 25% of the drug is excreted in urine.Â
Half-life:Â
6-12 hoursÂ
Administration:Â
This medication should be administered orally with food.Â
Patient information leafletÂ
Generic Name: propoxyphene Â
Pronounced: pro-POX-ih-feen Â
Why do we use propoxyphene?Â
This is an opioid analgesic used in treating mild to moderate pain. Along with analgesic activity, it also possesses local anesthetic and anti-tussive properties. Due to potential side effects like cardiovascular events that may lead to death, it was withdrawn from the market.Â
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