AHFS/Drugs.com Monograph Routes of
administration oral, iv Molar mass 248.321 g/mol | MedlinePlus a684032 ATC code C07AA03 (WHO) CAS ID 13523-86-9 | |
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Trade names Visken (originator), many generic brands Pregnancy
category AU: C
US: B (No risk in non-human studies) | ||
Pindolol (originally marketed as Visken, now marketed under many brands as a generic drug) is a beta blocker.
Contents
Medical use
Pindolol is used for hypertension in the US, Canada, and Europe, and also for angina pectoris outside the US. When used alone for hypertension, pindolol can significantly lower blood pressure and heart rate, but the evidence base for its use is weak, as the number of subjects in published studies is small.
In some countries pindolol is also used for arrhythmias and prophylaxis of acute stress reactions.
Contraindications
Similar to propranolol with an extra contraindication for hyperthyroidism. In patients with thyrotoxicosis, possible deleterious effects from long-term use of pindolol have not been adequately appraised. Beta-blockade may mask the clinical signs of continuing hyperthyroidism or complications, and give a false impression of improvement. Therefore, abrupt withdrawal of pindolol may be followed by an exacerbation of the symptoms of hyperthyroidism, including thyroid storm.
Pindolol has modest beta-adrenergic agonist activity and is therefore used with caution in angina pectoris.
Pharmacology
Pindolol is a nonselective beta blocker with partial beta-adrenergic receptor agonist activity and also possesses intrinsic sympathomimetic activity. This means that pindolol, particularly in high doses, exerts effects like epinephrine or isoprenaline (increased pulse rate, increased blood pressure, bronchodilation), but these effects are limited. Pindolol also shows membrane stabilizing effects like quinidine, possibly accounting for its antiarrhythmic effects. It also functions as a 5-HT1A receptor weak partial agonist / antagonist (Ki=33nM).
Pharmacokinetics
Pindolol is rapidly and well absorbed from the GI tract. It undergoes some first-pass-metabolization leading to an oral bioavailability of 50 to 95%. Patients with uremia may have a reduced bioavailability. Food does not alter the bioavailability, but may increase the resorption. Following an oral single dose of 20 mg peak plasma concentrations are reached within 1 to 2 hours. The effect of pindolol on pulse rate (lowering) is evident after 3 hours. Despite the rather short halflife of 3 to 4 hours, hemodynamic effects persist for 24 hours after administration. Plasma halflives are increased to 3 - 11.5 hours in patients with renal impairment, to 7 – 15 hours in elderly patients, and from 2.5 to 30 hours in patients with liver cirrhosis. Approximately 2/3 of pindolol are metabolized in the liver giving hydroxylates, which are found in the urine as gluconurides and ethereal sulfates. The remaining 1/3 of pindolol is excreted in urine in unchanged form.
History
Pindolol was patented by Sandoz in 1966 and was launched in the US in 1977.