DOLENE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DOLENE (DOLENE).

How it works

Opioid agonist, primarily mu-opioid receptor activation, leading to analgesic and euphoric effects.

What the body does with it

Metabolism	Hepatic via CYP2D6 and CYP3A4; active metabolite morphine-6-glucuronide.
Excretion	Renal: 70-80% as conjugated metabolites (mostly glucuronides), 5-10% as unchanged drug; Fecal: 5-10%; Biliary: minor.
Half-life	2.5-3.5 hours; prolonged in hepatic impairment (up to 6-8 hours) and in neonates.
Protein binding	20-30% bound to albumin.
Volume of Distribution	1-2 L/kg; indicates extensive tissue distribution.
Bioavailability	Oral: 50-60% (first-pass metabolism); Rectal: ~50%.
Onset of Action	Oral: 30-60 minutes; Intravenous: 5-10 minutes.
Duration of Action	Oral: 4-6 hours; Intravenous: 2-4 hours. Analgesic effect lasts 3-5 hours.

Classification & Brands

Dosing & administration

50 mg orally every 4-6 hours as needed for pain; maximum 400 mg per day.

Dosage form	CAPSULE
Renal impairment	GFR 30-50 mL/min: 50 mg every 6 hours; GFR 10-29 mL/min: 50 mg every 8 hours; GFR <10 mL/min: 50 mg every 12 hours.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: 50 mg every 8 hours; Child-Pugh C: not recommended.
Pediatric use	1-2 mg/kg orally every 4-6 hours as needed; maximum 5 mg/kg per day or 200 mg per day, whichever is less.
Geriatric use	Initiate at 25 mg every 6 hours; increase cautiously to 50 mg every 6 hours if needed; maximum 300 mg per day.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DOLENE (DOLENE).

Breastfeeding	Propoxyphene is excreted into breast milk; M/P ratio not well established; estimated infant dose is 1-2% of maternal weight-adjusted dose; potential for neonatal respiratory depression and sedation; use with caution; monitor infant for drowsiness and feeding difficulties.
Teratogenic Risk	DOLENE (propoxyphene) is pregnancy category C; first trimester: no adequate human studies; potential risk of teratogenicity cannot be excluded; second and third trimesters: associated with neonatal respiratory depression, withdrawal syndrome, and fetal growth restriction with chronic use; avoid use during pregnancy unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Risk of addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; interaction with alcohol or CNS depressants; risk of opioid-induced hyperalgesia.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to morphine; severe respiratory depression; acute or severe bronchial asthma; gastrointestinal obstruction; concurrent MAOIs or within 14 days.

Clinical Precautions

Precautions

Respiratory depression, particularly in elderly or debilitated; increased intracranial pressure; severe hypotension; adrenal insufficiency; serotonin syndrome; risk of seizures; severe hypotension; use in renal or hepatic impairment.

Clinical Tips & Counseling

Drug interactions

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DOLENE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DOLENE (DOLENE).

How it works

Opioid agonist, primarily mu-opioid receptor activation, leading to analgesic and euphoric effects.

What the body does with it

Metabolism	Hepatic via CYP2D6 and CYP3A4; active metabolite morphine-6-glucuronide.
Excretion	Renal: 70-80% as conjugated metabolites (mostly glucuronides), 5-10% as unchanged drug; Fecal: 5-10%; Biliary: minor.
Half-life	2.5-3.5 hours; prolonged in hepatic impairment (up to 6-8 hours) and in neonates.
Protein binding	20-30% bound to albumin.
Volume of Distribution	1-2 L/kg; indicates extensive tissue distribution.
Bioavailability	Oral: 50-60% (first-pass metabolism); Rectal: ~50%.
Onset of Action	Oral: 30-60 minutes; Intravenous: 5-10 minutes.
Duration of Action	Oral: 4-6 hours; Intravenous: 2-4 hours. Analgesic effect lasts 3-5 hours.

Classification & Brands

Dosing & administration

50 mg orally every 4-6 hours as needed for pain; maximum 400 mg per day.

Dosage form	CAPSULE
Renal impairment	GFR 30-50 mL/min: 50 mg every 6 hours; GFR 10-29 mL/min: 50 mg every 8 hours; GFR <10 mL/min: 50 mg every 12 hours.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: 50 mg every 8 hours; Child-Pugh C: not recommended.
Pediatric use	1-2 mg/kg orally every 4-6 hours as needed; maximum 5 mg/kg per day or 200 mg per day, whichever is less.
Geriatric use	Initiate at 25 mg every 6 hours; increase cautiously to 50 mg every 6 hours if needed; maximum 300 mg per day.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DOLENE (DOLENE).

Breastfeeding	Propoxyphene is excreted into breast milk; M/P ratio not well established; estimated infant dose is 1-2% of maternal weight-adjusted dose; potential for neonatal respiratory depression and sedation; use with caution; monitor infant for drowsiness and feeding difficulties.
Teratogenic Risk	DOLENE (propoxyphene) is pregnancy category C; first trimester: no adequate human studies; potential risk of teratogenicity cannot be excluded; second and third trimesters: associated with neonatal respiratory depression, withdrawal syndrome, and fetal growth restriction with chronic use; avoid use during pregnancy unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to morphine; severe respiratory depression; acute or severe bronchial asthma; gastrointestinal obstruction; concurrent MAOIs or within 14 days.