propoxyphene

Adult Dosing

Mild to moderate pain

Propoxyphene napsylate: 100 mg PO q4 hrs PRN. Max: 600 mg/24 hrs
Propoxyphene hydrochloride: 65 mg PO q4 hrs PRN. Max: 390 mg/24 hrs

Pediatric Dosing

Safety and effectiveness in pediatric patients have not been established

[Outline]

Adult Dosing
Pediatric Dosing

Indications ⬆ ⬇

Mild to moderate pain

Contraindications ⬆ ⬇

Hypersensitivity
Hx of drug abuse
Significant respiratory depression (unmonitored settings or absence of resuscitative equipment)
Patients with acute/severe asthma or hypercarbia
Suicidal ideation
Paralytic ileus

Black Box Warnings ⬆ ⬇

Numerous cases of accidental and intentional overdose with propoxyphene products either alone or in combination with alcohol, other CNS depressants have been reported. Fatalities within 1st hr of overdosage are not uncommon; many deaths have occurred in patients with prior emotional disturbances or suicidal ideation/attempts and/or concomitant administration of sedatives, tranquilizers, muscle relaxants, antidepressants, or other CNS-depressant drugs
Do not prescribe for patients with history of suicidal ideation
Concomitant administration of moderate or strong CYP3A4 inhibitors may increase propoxyphene levels. Monitor patients receiving propoxyphene and any CYP3A4 inhibitor carefully for an extended period, adjust dose if warranted

Dosing Adjustment ⬆ ⬇

Renal Dose Adjustment

Mild to moderate impairment: Consider dose reduction; dose adjustments not defined
Severe impairment: Avoid use

Hepatic Dose Adjustment

Hepatic impairment: Consider dose reduction; dose adjustments not defined

Warnings/Precautions ⬆ ⬇

Propoxyphene napsylate 100 mg is equivalent to propoxyphene hydrochloride 65 mg. It is most commonly given in combination with aspirin or acetaminophen
Respiratory depression is the chief hazard of all opioids. Elderly or debilitated patients, non-tolerant patients, or patients taking opioids in conjunction with other agents that depress respiration, are at an increased risk. Use with extreme caution in patients with significant chronic obstructive pulmonary disease or cor pulmonale, and in patients having substantially decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression
Propoxyphene may cause severe hypotension in patients with volume depletion. Patients taking phenothiazines or other agents which compromise vasomotor tone are at increased risk
Do not exceed recommended dose. Numerous cases of accidental and intentional overdose with propoxyphene products have occurred. Propoxyphene products in excessive doses or in drug interactions with CNS depressants (including alcohol) are major causes of drug-related deaths
Taper dose gradually to discontinue if at risk for physical dependence (abrupt cessation of opioids may cause a withdrawal syndrome)

Cautions: Use cautiously in

Hepatic impairment
Renal impairment
Chronic alcohol use
CNS depressant use
Head injury
Increased ICP
Seizure disorder
Depression
Hypovolemia
Hypotension
GI/GU obstruction
Biliary disease
Undiagnosed abdominal pain
Prostatic hypertrophy
Impaired pulmonary function
Adrenal insufficiency
Avoid prolonged use
Elderly patients

Interactions ⬆ ⬇

Darvon, Darvon-N, Dolene interacts with :

Pregnancy/Breast Feeding ⬆ ⬇

Pregnancy Category:C

Breastfeeding: Excreted in breast milk in low levels. However, infant sedation, apnea, bradycardia, and cyanosis have been reported with the maternal use of oral opioids in the first week of life. Monitor the infant for drowsiness, adequate weight gain, and developmental milestones. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 8 July 2010). Manufacturer advises caution

Adverse Reactions ⬆ ⬇

CV: Hypotension, arrhythmia, bradycardia, cardiac/respiratory arrest, congestive arrest, CHF, tachycardia, myocardial infarction
CNS: Dizziness, sedation, lightheadedness, weakness, convulsions, coma, disorientation, incoordination, , somnolence, insomnia
PSYCHIATRIC: Suicidal ideation, confusional state, paradoxical excitement, hallucinations, euphoria, dysphoria
GI: Nausea, vomiting, constipation, abdominal pain, GI bleed, acute pancreatitis
HEPA: Hepatic steatosis, hepatomegaly, hepatocellular injury
RESP: Respiratory depression
DERM: Rashes
EENT: Visual disturbance
MISC: Hypersensitivity, drug tolerance, drug toxicity, withdrawal syndrome, metabolic acidosis

Clinical Pharmacology ⬆ ⬇

Mechanism of action: Binds to opiate receptors; alters the perception of pain; produces generalized CNS depression
Metabolized by liver to active metabolite, norpropoxyphene; CYP450: 3A4 substrate; 2D6, 3A4 inhibitor
Excreted in urine (20-25%)
Half-life: 6-12 hrs (propoxyphene); 30-36 hrs (norpropoxyphene)

Brands and Availability ⬆ ⬇

US Trade Name(s)

Darvon
Darvon-N
Dolene

US Availability

propoxyphene hydrochloride (generic)

CAPS: 65 mg

Darvon (propoxyphene hydrochloride)

CAPS: 65 mg

Darvon-N (propoxyphene napsylate)

TABS: 100 mg

Dolene (propoxyphene hydrochloride)

CAPS: 65 mg

Canadian Trade Name(s)

Darvon-N

Canadian Availability

Darvon-N (dextropropoxyphene napsylate)

CAPS: 100 mg

UK Trade Name(s)

UK Availability

Australian Trade Name(s)

Doloxene

Australian Availability

Doloxene (dextropropoxyphene napsylate)

CAPS: 100 mg