ZEBETA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ZEBETA (ZEBETA).

How it works

Selective beta-1 adrenergic receptor antagonist (cardioselective beta-blocker). Reduces heart rate, myocardial contractility, and blood pressure by blocking catecholamine effects at beta-1 receptors.

What the body does with it

Metabolism	Hepatic metabolism via CYP2D6 to active metabolite (N-dealkylated product).
Excretion	Approximately 50% of an oral dose is excreted unchanged in urine; the remainder is hepatically metabolized with biliary excretion of metabolites contributing to fecal elimination.
Half-life	Terminal elimination half-life is 12–15 hours in patients with normal renal function, allowing once-daily dosing.
Protein binding	Approximately 50% bound to serum albumin.
Volume of Distribution	Volume of distribution is about 8–10 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is approximately 50–60% due to first-pass metabolism.
Onset of Action	Oral: Antihypertensive effect begins within 1–2 hours.
Duration of Action	Duration of antihypertensive effect is approximately 24 hours, supporting once-daily administration.

Classification & Brands

Dosing & administration

Initial dose 5 mg orally twice daily; may increase to 10 mg twice daily after 2 weeks; maximum 20 mg twice daily.

Dosage form	TABLET
Renal impairment	GFR 30-59 mL/min: reduce dose by 50%. GFR <30 mL/min: use with caution; not recommended.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated.
Pediatric use	Not approved for pediatric use.
Geriatric use	Start at 5 mg once daily; increase cautiously; monitor heart rate and blood pressure closely.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for ZEBETA (ZEBETA).

Breastfeeding	Excreted in breast milk in low amounts. M/P ratio approximately 1.0. Monitor infant for bradycardia and hypotension. Consider alternative agents with lower milk transfer if available.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: Limited human data; animal studies show embryotoxicity and fetotoxicity at high doses. Second/third trimesters: Risk of fetal bradycardia, hypotension, hypoglycemia, and intrauterine growth restriction due to β-blockade. Use only if potential benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Abrupt discontinuation may exacerbate angina or precipitate myocardial infarction in patients with coronary artery disease.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Sinus bradycardia","Heart block greater than first degree","Cardiogenic shock","Uncompensated cardiac failure","Hypersensitivity to any component","Bronchial asthma (relative contraindication)"]

Clinical Precautions

Precautions

["Do not abruptly discontinue; taper over 1-2 weeks.","Use with caution in patients with bronchospastic diseases (e.g., asthma) due to relative beta-2 blockade.","May mask symptoms of hypoglycemia and thyrotoxicosis.","Use with caution in patients with peripheral vascular disease.","May cause bradycardia and hypotension."]

Clinical Tips & Counseling

Drug interactions

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ZEBETA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ZEBETA (ZEBETA).

How it works

Selective beta-1 adrenergic receptor antagonist (cardioselective beta-blocker). Reduces heart rate, myocardial contractility, and blood pressure by blocking catecholamine effects at beta-1 receptors.

What the body does with it

Metabolism	Hepatic metabolism via CYP2D6 to active metabolite (N-dealkylated product).
Excretion	Approximately 50% of an oral dose is excreted unchanged in urine; the remainder is hepatically metabolized with biliary excretion of metabolites contributing to fecal elimination.
Half-life	Terminal elimination half-life is 12–15 hours in patients with normal renal function, allowing once-daily dosing.
Protein binding	Approximately 50% bound to serum albumin.
Volume of Distribution	Volume of distribution is about 8–10 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is approximately 50–60% due to first-pass metabolism.
Onset of Action	Oral: Antihypertensive effect begins within 1–2 hours.
Duration of Action	Duration of antihypertensive effect is approximately 24 hours, supporting once-daily administration.

Classification & Brands

Dosing & administration

Initial dose 5 mg orally twice daily; may increase to 10 mg twice daily after 2 weeks; maximum 20 mg twice daily.

Dosage form	TABLET
Renal impairment	GFR 30-59 mL/min: reduce dose by 50%. GFR <30 mL/min: use with caution; not recommended.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated.
Pediatric use	Not approved for pediatric use.
Geriatric use	Start at 5 mg once daily; increase cautiously; monitor heart rate and blood pressure closely.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for ZEBETA (ZEBETA).

Breastfeeding	Excreted in breast milk in low amounts. M/P ratio approximately 1.0. Monitor infant for bradycardia and hypotension. Consider alternative agents with lower milk transfer if available.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: Limited human data; animal studies show embryotoxicity and fetotoxicity at high doses. Second/third trimesters: Risk of fetal bradycardia, hypotension, hypoglycemia, and intrauterine growth restriction due to β-blockade. Use only if potential benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Abrupt discontinuation may exacerbate angina or precipitate myocardial infarction in patients with coronary artery disease.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Sinus bradycardia","Heart block greater than first degree","Cardiogenic shock","Uncompensated cardiac failure","Hypersensitivity to any component","Bronchial asthma (relative contraindication)"]