| Indication |
For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation. |
| Pharmacodynamics |
Pindolol is a non-selective beta-adrenergic antagonist
(beta-blocker) which possesses intrinsic sympathomimetic activity (ISA)
in therapeutic dosage ranges but does not possess quinidine-like
membrane stabilizing activity. Pindolol impairs AV node conduction and
decreases sinus rate and may also increase plasma triglycerides and
decrease HDL-cholesterol levels. Pindolol is nonpolar and hydrophobic,
with low to moderate lipid solubility. Pindolol has little to no
intrinsic sympathomimetic activity and, unlike some other
beta-adrenergic blocking agents, pindolol has little direct myocardial
depressant activity and does not have an anesthetic-like
membrane-stabilizing action. |
| Mechanism of action |
Pindolol non-selectively blocks beta-1 adrenergic receptors mainly
in the heart, inhibiting the effects of epinephrine and norepinephrine
resulting in a decrease in heart rate and blood pressure. By binding
beta-2 receptors in the juxtaglomerular apparatus, Pindolol inhibits the
production of renin, thereby inhibiting angiotensin II and aldosterone
production and therefore inhibits the vasoconstriction and water
retention due to angiotensin II and aldosterone, respectively. |
| Absorption |
Rapidly and reproducibly absorbed (bioavailability greater than 95%). |
| Volume of distribution |
|
| Protein binding |
40% |
| Metabolism |
Hepatic. In man, 35% to 40% is excreted unchanged in the urine
and 60% to 65% is metabolized primarily to hydroxy-metabolites which are
excreted as glucuronides and ethereal sulfates. |
| Route of elimination |
Pindolol undergoes extensive metabolism in animals and man. In
man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is
metabolized primarily to hydroxy-metabolites which are excreted as
glucuronides and ethereal sulfates. About 6% to 9% of an administered
intravenous dose is excreted by the bile into the feces. |
| Half life |
3 to 4 hours |
| Clearance |
- 50-300 mL/min [cirrhotic patients]
|
| Toxicity |
LD50=263 mg/kg (orally in rats). Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm. |
