Pindolol

Pindolol

Clinical data
Trade names	Visken (originator), many generic brands
AHFS/Drugs.com	Monograph
MedlinePlus	a684032
Pregnancy category	AU: C US: B (No risk in non-human studies)
Routes of administration	oral, iv
ATC code	C07AA03 (WHO)
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Bioavailability	50% to 95%
Metabolism	Hepatic
Biological half-life	3–4 hours
Excretion	Renal
Identifiers
IUPAC name (RS)-1-(1H-indol-4-yloxy)-3-(isopropylamino)propan-2-ol
CAS Number	13523-86-9 Y
PubChem (CID)	4828
IUPHAR/BPS	91
DrugBank	DB00960 N
ChemSpider	4662 N
UNII	BJ4HF6IU1D N
KEGG	D00513 Y
ChEBI	CHEBI:8214 N
ChEMBL	CHEMBL500 N
ECHA InfoCard	100.033.501
Chemical and physical data
Formula	C14H20N2O2
Molar mass	248.321 g/mol
3D model (Jmol)	Interactive image
Chirality	Racemic mixture
SMILES CC(C)NCC(O)COc2cccc1nccc12
InChI InChI=1S/C14H20N2O2/c1-10(2)16-8-11(17)9-18-14-5-3-4-13-12(14)6-7-15-13/h3-7,10-11,15-17H,8-9H2,1-2H3 N Key:JZQKKSLKJUAGIC-UHFFFAOYSA-N N
NY (what is this?)

Pindolol (originally marketed as Visken, now marketed under many brands as a generic drug) is a beta blocker.

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.

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.

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-HT_1A receptor weak partial agonist / antagonist (K_i=33nM).

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.