Yes: Capsule

Analgesic, Narcotic

Management of mild to moderate pain

C-IV

C/D (if used for prolonged periods)

Hypersensitivity to propoxyphene or any component

Administer with caution in patients dependent on opiates, substitution may result in acute opiate withdrawal symptoms, use with caution in patients with severe renal or hepatic dysfunction; when given in excessive doses, either alone or in combination with other CNS depressants or propoxyphene products, propoxyphene is a major cause of drug-related deaths; do not exceed recommended dosage; tolerance or drug dependence may result from extended use

Percentage unknown: Increased liver enzymes, may increase LFTs; may decrease glucose, urinary 17-OHCS

>10%:

Cardiovascular: Hypotension

Central nervous system: Dizziness, lightheadedness, sedation, paradoxical excitement and insomnia, fatigue, drowsiness

Gastrointestinal: Nausea, vomiting, constipation

Neuromuscular & skeletal: Weakness

1% to 10%:

Central nervous system: Nervousness, headache, restlessness, malaise, confusion

Gastrointestinal: Anorexia, stomach cramps, xerostomia, biliary spasm

Genitourinary: Decreased urination, ureteral spasms

Respiratory: Dyspnea, shortness of breath

<1%: Mental depression hallucinations, paradoxical CNS stimulation, increased intracranial pressure, rash, urticaria, paralytic ileus, psychologic and physical dependence with prolonged use, histamine release

Symptoms of overdose include CNS, respiratory depression, hypotension, pulmonary edema, seizures

Treatment of an overdose includes support of the patient's airway; establishment of an I.V. line and administration of naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg; emesis is not indicated as overdose may cause seizures; charcoal is very effective (>95%) at binding propoxyphene

CYP3A3/4 enzyme inhibitor

Increased toxicity: CNS depressants may potentiate pharmacologic effects; propoxyphene may inhibit the metabolism and increase the serum concentrations of carbamazepine, phenobarbital, MAO inhibitors, tricyclic antidepressants, and warfarin

Binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression

Onset of effect: Oral: Within 0.5-1 hour

Duration: 4-6 hours

Metabolism: First-pass effect; metabolized in the liver to an active metabolite (norpropoxyphene) and inactive metabolites

Bioavailability: Oral: 30% to 70%

Half-life: Adults: Parent drug: 8-24 hours (mean: ~15 hours); Norpropoxyphene: 34 hours

Elimination: 20% to 25% excreted in urine

Oral:

Adults:

Hydrochloride: 65 mg every 3-4 hours as needed for pain; maximum: 390 mg/day

Napsylate: 100 mg every 4 hours as needed for pain; maximum: 600 mg/day

Dosing comments in renal impairment: Cl_cr <10 mL/minute: Avoid use

Hemodialysis: Not dialyzable (0% to 5%)

Dosing adjustment in hepatic impairment: Reduced doses should be used

Alcohol: Additive CNS effects, avoid or limit alcohol; watch for sedation

Food: May decrease rate of absorption, but may slightly increase bioavailability

Glucose may cause hyperglycemia; monitor blood glucose concentrations

Pain relief, respiratory and mental status, blood pressure

Therapeutic: Ranges published vary between laboratories and may not correlate with clinical effect

Therapeutic concentration: 0.1-0.4 mg/mL (SI: 0.3-1.2 mmol/L)

Toxic: >0.5 mg/mL (SI: >1.5 mmol/L)

False-positive methadone test

Dizziness, drowsiness, insomnia, and paradoxical excitement are common; may cause nervousness, restlessness, confusion; may rarely cause depression or hallucinations

Concurrent use with psychotropics may produce additive sedation as well as increase their serum levels; monitor for altered clinical response or preferably, use a different analgesic

No information available to require special precautions

No effects or complications reported

Take as directed; do not take a larger dose or more often than prescribed. Do not use alcohol, other prescription or OTC sedatives, tranquilizers, antihistamines, or pain medications without consulting prescriber. May cause dizziness, drowsiness, or impaired judgment; avoid driving or engaging in tasks requiring alertness until response to drug is known. If you experience vomiting or loss of appetite, frequent mouth care, small frequent meals, chewing gum, or sucking lozenges may help. Increased fluid intake, exercise, fiber in diet may help with constipation (if unresolved consult prescriber). Report unresolved nausea or vomiting, difficulty breathing or shortness of breath, or unusual weakness. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding women should take this drug 4-5 hours before nursing.

Monitor pain relief, respiratory and mental status, blood pressure, excessive sedation

Capsule, as hydrochloride: 65 mg

Tablet, as napsylate: 100 mg

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Hasday JD and Weintraub M, "Propoxyphene in Children With Iatrogenic Morphine Dependence," Am J Dis Child, 1983, 137(8):745-8.

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Proudfoot AT, "Clinical Features and Management of Distalgesic Overdose," Hum Toxicol, 1984, 3(Suppl):85S-94S.

Stork CM, Redd JT, Fine K, et al, "Propoxyphene-Induced Wide QRS Complex Dysrhythmia Responsive to Sodium Bicarbonate - A Case Report," J Toxicol Clin Toxicol, 1995, 33(2):179-83.

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Wetli CV and Bednarczyk LR, "Deaths Related to Propoxyphene Overdose: A Ten Year Assessment," South Med J, 1980, 73(9):1205-9.