Chemical formula: C₁₄H₂₀N₂O₂ Molecular mass: 248.321 g/mol PubChem compound: 4828
Pindolol is a potent beta-adrenoceptor antagonist (beta-blocker) with uses similar to those of propranolol. It is classified as non cardioselective. It blocks both B1- and B2-adrenoceptors for more than 24 hours after administration. It has negligible membrane-stabilising activity. Pindolol exhibits low cardiodepressant activity at therapeutic dose. As a beta-blocker, pindolol protects the heart from beta-adrenoceptor stimulation by acetecholamines during physical exercise and mental stress, prevents excessive sympathetic drive to the heart, resulting in a fall in heart rate and a decrease in cardiac work and myocardial oxygen consumption and also reduces the sympathetic drive to the heart at rest. Its intrinsic sympathomimetic activity (ISA) even at low dosage, provides the heart with basal stimulation similar to that elicited by normal resting sympathetic activity, with the result that heart rate and contractility at rest and intracardiac conduction are not unduly depressed. The risk of bradycardia is therefore small and normal cardiac output is not reduced.
Pindolol is a beta-blocker with clinically relevant vasodilator activity. This results from the ISA exerted on B2-adrenoceptors in blood vessels. The high vascular resistance of established hypertension is lowered by pindolol; tissue and organ perfusion is not impaired, and may even be improved.
The rapid, nearly complete absorption (>95%) and the negligible hepatic first-pass effect (13%) of pindolol result in a high bioavailability (87%). Maximum plasma concentration is reached within one hour after oral administration.
Pindolol has a plasma protein binding of 40%, a volume of distribution of 2-3 l/Kg and a total clearance of 500 ml/min.
The elimination half-life of pindolol is 3-4 hours. 30-40% is excreted unchanged in the urine, while 60-70% is excreted via kidney and liver as inactive metabolites. Pindolol crosses the placental barrier and passes in small quantities into breast milk.
Patients with impaired kidney or liver function may usually be treated with normal doses. Only in severe cases may a reduction of the daily dose be necessary.
There are no additional preclinical data.
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