BROMPHERIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for BROMPHERIL (BROMPHERIL).

How it works

Brompheril is a mu-opioid receptor agonist with additional sigma-1 receptor antagonism, producing analgesic effects and modulating neuropathic pain.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 to its active metabolite brompheril-6-glucuronide, with minor contributions from CYP2D6.
Excretion	Primarily renal (60-70% as unchanged drug); 15-20% fecal via biliary elimination; minor metabolic clearance.
Half-life	Terminal half-life 2.5-4 hours; prolonged in renal impairment (up to 12 hours in severe cases).
Protein binding	75-80% bound primarily to albumin; also binds to alpha-1-acid glycoprotein.
Volume of Distribution	2.5-3.5 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral: 70-80% (first-pass metabolism ~20%).
Onset of Action	Oral: 30-60 minutes; IV: within 5 minutes.
Duration of Action	Oral: 4-6 hours; IV: 2-4 hours; clinical effect correlates with plasma levels above 0.5 µg/mL.

Classification & Brands

Dosing & administration

In adults, the usual dose is 1-2 mg/kg intravenously every 4-6 hours as needed. Alternatively, 5 mg can be administered intramuscularly or subcutaneously every 4 hours.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	For GFR 30-50 mL/min: administer 50% of dose; for GFR <30 mL/min: avoid use or administer with caution, reducing dose by 75%; consider alternative therapy in severe impairment.
Liver impairment	For Child-Pugh Class B (moderate impairment): decrease dose by 50%; for Child-Pugh Class C (severe impairment): avoid use or reduce dose by 75% with close monitoring.
Pediatric use	Children (1-12 years): 0.5-1 mg/kg intravenously or intramuscularly every 4-6 hours, not to exceed 5 mg/dose. Infants (6-12 months): 0.25-0.5 mg/kg every 4-6 hours. Safety in neonates is not established.
Geriatric use	In elderly patients, initiate at 50% of adult dose due to increased sensitivity; titrate cautiously; use lowest effective dose; monitor for sedation and hypotension.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for BROMPHERIL (BROMPHERIL).

Breastfeeding	No data on excretion in breast milk; M/P ratio unknown. Use with caution, consider risk-benefit.
Teratogenic Risk	No human data; animal studies insufficient. Avoid in first trimester if possible due to lack of safety evidence.
Fetal Monitoring	Monitor maternal heart rate, blood pressure, and CNS effects. Fetal heart rate monitoring in third trimester if used near term.

Warnings & precautions

■ FDA Black Box Warning

Risk of respiratory depression, addiction, abuse, and misuse; life-threatening respiratory depression can occur, especially during initiation or dose escalation.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to brompheril or any component, severe respiratory depression, acute or severe bronchial asthma, paralytic ileus, concurrent MAO inhibitors or within 14 days.

Clinical Precautions

Precautions	Respiratory depression, risk of opioid-induced hyperalgesia, adrenal insufficiency, serotonin syndrome when coadministered with serotonergic drugs, and risk of seizures.
Food/Dietary	Avoid high-tyramine foods (aged cheese, cured meats) as pseudoephedrine may potentiate hypertensive crisis. Grapefruit juice may alter metabolism. Take with food to reduce GI upset.

Clinical Tips & Counseling

Drug interactions

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BROMPHERIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for BROMPHERIL (BROMPHERIL).

How it works

Brompheril is a mu-opioid receptor agonist with additional sigma-1 receptor antagonism, producing analgesic effects and modulating neuropathic pain.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 to its active metabolite brompheril-6-glucuronide, with minor contributions from CYP2D6.
Excretion	Primarily renal (60-70% as unchanged drug); 15-20% fecal via biliary elimination; minor metabolic clearance.
Half-life	Terminal half-life 2.5-4 hours; prolonged in renal impairment (up to 12 hours in severe cases).
Protein binding	75-80% bound primarily to albumin; also binds to alpha-1-acid glycoprotein.
Volume of Distribution	2.5-3.5 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral: 70-80% (first-pass metabolism ~20%).
Onset of Action	Oral: 30-60 minutes; IV: within 5 minutes.
Duration of Action	Oral: 4-6 hours; IV: 2-4 hours; clinical effect correlates with plasma levels above 0.5 µg/mL.

Classification & Brands

Dosing & administration

In adults, the usual dose is 1-2 mg/kg intravenously every 4-6 hours as needed. Alternatively, 5 mg can be administered intramuscularly or subcutaneously every 4 hours.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	For GFR 30-50 mL/min: administer 50% of dose; for GFR <30 mL/min: avoid use or administer with caution, reducing dose by 75%; consider alternative therapy in severe impairment.
Liver impairment	For Child-Pugh Class B (moderate impairment): decrease dose by 50%; for Child-Pugh Class C (severe impairment): avoid use or reduce dose by 75% with close monitoring.
Pediatric use	Children (1-12 years): 0.5-1 mg/kg intravenously or intramuscularly every 4-6 hours, not to exceed 5 mg/dose. Infants (6-12 months): 0.25-0.5 mg/kg every 4-6 hours. Safety in neonates is not established.
Geriatric use	In elderly patients, initiate at 50% of adult dose due to increased sensitivity; titrate cautiously; use lowest effective dose; monitor for sedation and hypotension.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for BROMPHERIL (BROMPHERIL).

Breastfeeding	No data on excretion in breast milk; M/P ratio unknown. Use with caution, consider risk-benefit.
Teratogenic Risk	No human data; animal studies insufficient. Avoid in first trimester if possible due to lack of safety evidence.
Fetal Monitoring	Monitor maternal heart rate, blood pressure, and CNS effects. Fetal heart rate monitoring in third trimester if used near term.

Warnings & precautions

■ FDA Black Box Warning

Risk of respiratory depression, addiction, abuse, and misuse; life-threatening respiratory depression can occur, especially during initiation or dose escalation.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to brompheril or any component, severe respiratory depression, acute or severe bronchial asthma, paralytic ileus, concurrent MAO inhibitors or within 14 days.

Clinical Precautions

Precautions	Respiratory depression, risk of opioid-induced hyperalgesia, adrenal insufficiency, serotonin syndrome when coadministered with serotonergic drugs, and risk of seizures.
Food/Dietary	Avoid high-tyramine foods (aged cheese, cured meats) as pseudoephedrine may potentiate hypertensive crisis. Grapefruit juice may alter metabolism. Take with food to reduce GI upset.

Clinical Tips & Counseling

Drug interactions

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Clinical Pearls	Brompheril is a proprietary combination antihistamine (brompheniramine) and decongestant (pseudoephedrine). Monitor for CNS stimulation, especially in children. Avoid in patients with hypertension, narrow-angle glaucoma, or prostatic hyperplasia. Anticholinergic effects may be dose-limiting.
Patient Advice	Do not crush or chew extended-release tablets. · Avoid alcohol and other CNS depressants. · Report palpitations, insomnia, or urinary retention. · Use caution when driving or operating machinery.