PROPRANOLOL HYDROCHLORIDE INTENSOL

Clinical safety rating: caution

Other drugs that lower heart rate or blood pressure can have additive effects Abrupt withdrawal may exacerbate angina pectoris or cause myocardial infarction.

How it works

Nonselective beta-adrenergic receptor antagonist; competitively blocks beta-1 and beta-2 receptors, decreasing heart rate, myocardial contractility, and blood pressure; also suppresses renin release and reduces CNS sympathetic outflow.

What the body does with it

Metabolism	Extensively hepatic via CYP2D6 and glucuronidation; active metabolite 4-hydroxypropranolol; highly protein bound; elimination half-life 3-6 hours.
Excretion	Primarily hepatic metabolism (>99%) with <1% excreted unchanged in urine. Metabolites are excreted renally. Fecal elimination is minimal.
Half-life	Terminal elimination half-life is 3–6 hours, but clinical effects (e.g., beta-blockade) persist longer due to prolonged receptor occupancy. Half-life may increase in hepatic impairment.
Protein binding	Approximately 90% bound, primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	3–4 L/kg, indicating extensive extravascular distribution, including into the central nervous system.
Bioavailability	Oral bioavailability is 25–30% due to extensive first-pass hepatic metabolism; INTENSOL formulation has similar bioavailability as tablets.
Onset of Action	Oral: 30–60 minutes (with INTENSOL concentrated solution). IV: 2–5 minutes.
Duration of Action	Oral: 6–12 hours (beta-blockade persists up to 24 hours for some effects). IV: 2–4 hours post-infusion.

Classification & Brands

Dosing & administration

Initial: 40 mg orally twice daily; maintenance: 120-240 mg/day in 2-3 divided doses. Maximum: 640 mg/day. For hypertension, start 40 mg twice daily, increase gradually.

Dosage form	CONCENTRATE
Renal impairment	No dose adjustment required for renal impairment. Consider reduced dosing in severe renal failure due to accumulation of metabolites.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Use with caution; consider 75% dose reduction or alternative therapy.
Pediatric use	Hypertension: Initial 0.5-1 mg/kg/day orally in 2-3 divided doses; increase gradually every 5-7 days; usual range 1-5 mg/kg/day. Maximum 16 mg/kg/day or 640 mg/day. Arrhythmias: 0.5-1 mg/kg/dose every 6-8 hours; maximum 16 mg/kg/day. Migraine prophylaxis (≥6 years): 10-20 mg orally 2-3 times daily; increase to 20-40 mg 3 times daily.
Geriatric use	Initiate at low end of dosing range (20-40 mg twice daily) and titrate slowly due to increased risk of bradycardia and hypotension. Monitor renal and hepatic function.

Use during pregnancy

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

Clinical note

Other drugs that lower heart rate or blood pressure can have additive effects Abrupt withdrawal may exacerbate angina pectoris or cause myocardial infarction.

FDA category	Animal
Breastfeeding	Propranolol is excreted into breast milk with an M/P ratio of approximately 0.5. The relative infant dose is about 0.1% of the maternal weight-adjusted dose, likely safe but monitor infant for bradycardia and hypotension.
Teratogenic Risk	First trimester: Not associated with major congenital malformations in human studies. Second and third trimesters: Fetal bradycardia, growth restriction, and hypoglycemia reported. Avoid near term due to possible fetal or neonatal bradycardia, hypotension, and hypoglycemia.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning.

Side Effect Profile

Common Effects	angina
Serious Effects

Absolute Contraindications

["Cardiogenic shock","Sinus bradycardia","Heart block greater than first degree","Bronchial asthma","Decompensated heart failure","Known hypersensitivity to propranolol"]

Clinical Precautions

Precautions

["May precipitate heart failure in patients with poor cardiac reserve","Avoid abrupt discontinuation (risk of myocardial ischemia)","May mask signs of hypoglycemia in diabetic patients","May exacerbate peripheral vascular disease","Use caution in hepatic impairment","May worsen bronchospastic disease (e.g., asthma)"]

Clinical Tips & Counseling

Drug interactions

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PROPRANOLOL HYDROCHLORIDE INTENSOL

Clinical safety rating: caution

Other drugs that lower heart rate or blood pressure can have additive effects Abrupt withdrawal may exacerbate angina pectoris or cause myocardial infarction.

How it works

What the body does with it

Metabolism	Extensively hepatic via CYP2D6 and glucuronidation; active metabolite 4-hydroxypropranolol; highly protein bound; elimination half-life 3-6 hours.
Excretion	Primarily hepatic metabolism (>99%) with <1% excreted unchanged in urine. Metabolites are excreted renally. Fecal elimination is minimal.
Half-life	Terminal elimination half-life is 3–6 hours, but clinical effects (e.g., beta-blockade) persist longer due to prolonged receptor occupancy. Half-life may increase in hepatic impairment.
Protein binding	Approximately 90% bound, primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	3–4 L/kg, indicating extensive extravascular distribution, including into the central nervous system.
Bioavailability	Oral bioavailability is 25–30% due to extensive first-pass hepatic metabolism; INTENSOL formulation has similar bioavailability as tablets.
Onset of Action	Oral: 30–60 minutes (with INTENSOL concentrated solution). IV: 2–5 minutes.
Duration of Action	Oral: 6–12 hours (beta-blockade persists up to 24 hours for some effects). IV: 2–4 hours post-infusion.

Classification & Brands

Dosing & administration

Initial: 40 mg orally twice daily; maintenance: 120-240 mg/day in 2-3 divided doses. Maximum: 640 mg/day. For hypertension, start 40 mg twice daily, increase gradually.

Dosage form	CONCENTRATE
Renal impairment	No dose adjustment required for renal impairment. Consider reduced dosing in severe renal failure due to accumulation of metabolites.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Use with caution; consider 75% dose reduction or alternative therapy.
Pediatric use	Hypertension: Initial 0.5-1 mg/kg/day orally in 2-3 divided doses; increase gradually every 5-7 days; usual range 1-5 mg/kg/day. Maximum 16 mg/kg/day or 640 mg/day. Arrhythmias: 0.5-1 mg/kg/dose every 6-8 hours; maximum 16 mg/kg/day. Migraine prophylaxis (≥6 years): 10-20 mg orally 2-3 times daily; increase to 20-40 mg 3 times daily.
Geriatric use	Initiate at low end of dosing range (20-40 mg twice daily) and titrate slowly due to increased risk of bradycardia and hypotension. Monitor renal and hepatic function.

Use during pregnancy

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

Clinical note

Other drugs that lower heart rate or blood pressure can have additive effects Abrupt withdrawal may exacerbate angina pectoris or cause myocardial infarction.

FDA category	Animal
Breastfeeding	Propranolol is excreted into breast milk with an M/P ratio of approximately 0.5. The relative infant dose is about 0.1% of the maternal weight-adjusted dose, likely safe but monitor infant for bradycardia and hypotension.
Teratogenic Risk	First trimester: Not associated with major congenital malformations in human studies. Second and third trimesters: Fetal bradycardia, growth restriction, and hypoglycemia reported. Avoid near term due to possible fetal or neonatal bradycardia, hypotension, and hypoglycemia.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning.

Side Effect Profile

Common Effects	angina
Serious Effects

Absolute Contraindications

["Cardiogenic shock","Sinus bradycardia","Heart block greater than first degree","Bronchial asthma","Decompensated heart failure","Known hypersensitivity to propranolol"]