PINDAC

Clinical safety rating: caution

Comprehensive clinical and safety monograph for PINDAC (PINDAC).

How it works

Vasodilator (arteriolar dilator) reducing afterload; also inhibits platelet aggregation through inhibition of phosphodiesterase III.

What the body does with it

Metabolism	Hepatic via N-acetylation (polymorphic) and conjugation; active metabolite (hydralazine).
Excretion	Pindac (pindolol) is eliminated predominantly via hepatic metabolism (60-65%) with renal excretion of unchanged drug (35-40%). Less than 1% is excreted in feces via biliary elimination.
Half-life	Terminal elimination half-life is 3-4 hours in healthy individuals, prolonged to 7-15 hours in renal impairment and in elderly patients. Clinical context: dosing interval adjustment recommended for CrCl <30 mL/min.
Protein binding	40-50% bound to plasma proteins, primarily to albumin.
Volume of Distribution	2-3 L/kg (range 1.2-3.2 L/kg); high Vd indicates extensive tissue distribution, including crossing blood-brain barrier and placenta.
Bioavailability	Oral: 50-95% (mean ~85% with high first-pass metabolism; significant interindividual variation due to hepatic extraction). No data for other routes (IV is 100% by definition).
Onset of Action	Oral: 30-60 minutes for beta-blockade (reduction in heart rate); peak effect at 1-2 hours. Intravenous: within 1-5 minutes for acute effects.
Duration of Action	Oral: 12-24 hours (once-daily dosing for hypertension, but shorter for angina may require twice-daily). Clinical notes: intrinsic sympathomimetic activity may cause less bradycardia; duration of antihypertensive effect may last up to 24 hours with sustained-release formulation.

Classification & Brands

Dosing & administration

Oral: 2.5-5 mg twice daily; maximum 20 mg daily.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	GFR 30-50 mL/min: reduce dose by 50%; GFR <30 mL/min: use every 24 hours;, not recommended if GFR <15 mL/min.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use.
Pediatric use	Not approved for pediatric use; safety and efficacy not established.
Geriatric use	Start at 2.5 mg twice daily; increase cautiously due to age-related renal impairment.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for PINDAC (PINDAC).

Breastfeeding

Pindolol is excreted into human breast milk with a milk-to-plasma (M/P) ratio of approximately 1.0. The relative infant dose is estimated to be less than 5% of the maternal weight-adjusted dose, which is generally considered safe. However, monitor infant for bradycardia, hypotension, and hypoglycemia.

Teratogenic Risk

Pindolol (PINDAC) is a beta-blocker with FDA Pregnancy Category B. In the first trimester, data are limited but no consistent pattern of major malformations has been observed. However, beta-blockers may cause fetal bradycardia, hypoglycemia, and growth restriction, particularly in the second and third trimesters. Use should be limited to situations where benefit outweighs risk, with careful fetal monitoring.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity, coronary artery disease (relative), mitral valve rheumatic heart disease, high-output heart failure, dissecting aortic aneurysm, acute myocardial infarction.

Clinical Precautions

Precautions

Drug-induced lupus (dose-related, more common in slow acetylators), peripheral neuritis (pyridoxine deficiency), hypotension, tachycardia, myocardial ischemia (in CAD), hepatotoxicity, hemolytic anemia (rare).

Clinical Tips & Counseling

Drug interactions

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PINDAC

Clinical safety rating: caution

Comprehensive clinical and safety monograph for PINDAC (PINDAC).

How it works

Vasodilator (arteriolar dilator) reducing afterload; also inhibits platelet aggregation through inhibition of phosphodiesterase III.

What the body does with it

Metabolism	Hepatic via N-acetylation (polymorphic) and conjugation; active metabolite (hydralazine).
Excretion	Pindac (pindolol) is eliminated predominantly via hepatic metabolism (60-65%) with renal excretion of unchanged drug (35-40%). Less than 1% is excreted in feces via biliary elimination.
Half-life	Terminal elimination half-life is 3-4 hours in healthy individuals, prolonged to 7-15 hours in renal impairment and in elderly patients. Clinical context: dosing interval adjustment recommended for CrCl <30 mL/min.
Protein binding	40-50% bound to plasma proteins, primarily to albumin.
Volume of Distribution	2-3 L/kg (range 1.2-3.2 L/kg); high Vd indicates extensive tissue distribution, including crossing blood-brain barrier and placenta.
Bioavailability	Oral: 50-95% (mean ~85% with high first-pass metabolism; significant interindividual variation due to hepatic extraction). No data for other routes (IV is 100% by definition).
Onset of Action	Oral: 30-60 minutes for beta-blockade (reduction in heart rate); peak effect at 1-2 hours. Intravenous: within 1-5 minutes for acute effects.
Duration of Action	Oral: 12-24 hours (once-daily dosing for hypertension, but shorter for angina may require twice-daily). Clinical notes: intrinsic sympathomimetic activity may cause less bradycardia; duration of antihypertensive effect may last up to 24 hours with sustained-release formulation.

Classification & Brands

Dosing & administration

Oral: 2.5-5 mg twice daily; maximum 20 mg daily.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	GFR 30-50 mL/min: reduce dose by 50%; GFR <30 mL/min: use every 24 hours;, not recommended if GFR <15 mL/min.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use.
Pediatric use	Not approved for pediatric use; safety and efficacy not established.
Geriatric use	Start at 2.5 mg twice daily; increase cautiously due to age-related renal impairment.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for PINDAC (PINDAC).

Breastfeeding

Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity, coronary artery disease (relative), mitral valve rheumatic heart disease, high-output heart failure, dissecting aortic aneurysm, acute myocardial infarction.