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Pindolol

Catalog No. DB00960 Name DrugBank
CAS Number 13523-86-9 Website http://www.ualberta.ca/
M. F. C14H20N2O2 Telephone (780) 492-3111
M. W. 248.3208 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 836

SYNONYMS

IUPAC name
[2-hydroxy-3-(1H-indol-4-yloxy)propyl](propan-2-yl)amine
IUPAC Traditional name
pindolol
Brand Name
Calvisken
Visken
Pectobloc
Blockin L
Blocklin L
Cardilate
Decreten
Durapindol
Glauco-Visken
Pinbetol
Pynastin
Synonyms
Betapindol
Prinodolol

DATABASE IDS

PubChem SID 46508362
PubChem CID 4828
CAS Number 13523-86-9

PROPERTIES

Hydrophobicity(logP) 1.9
Solubility 7880 mg/L

DETAILS

Description (English)
Item Information
Drug Groups approved
Description A moderately lipophilic beta blocker (adrenergic beta-antagonists). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
Indication For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.
Pharmacology 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.
Toxicity LD50=263 mg/kg (orally in rats). Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm.
Affected Organisms
Humans and other mammals
Biotransformation 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.
Absorption Rapidly and reproducibly absorbed (bioavailability greater than 95%).
Half Life 3 to 4 hours
Protein Binding 40%
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.
Distribution * 2 L/kg
Clearance * 50-300 mL/min [cirrhotic patients]
External Links
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REFERENCES