Drug/Small Molecule:
pindolol

2D structure

Overview

Generic Names: Betapindol; Prinodolol
Trade Names: Blockin L; Blocklin L; Calvisken; Cardilate; Decreten; Durapindol; Glauco-Visken; Pectobloc; Pinbetol; Pynastin; Visken
Brand Mixtures: Viskazide 10/25tab (Hydrochlorothiazide + Pindolol); Viskazide 10/50tab (Hydrochlorothiazide + Pindolol)
PharmGKB Accession Id: PA450966

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) (source: Drug Bank)

Indication

For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation. (source: Drug Bank)

ATC Therapeutic Category

  • C07AA:Beta blocking agents, non-selective

Pharmacology, Interactions, and Contraindications

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. (source: Drug Bank)

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. (source: Drug Bank)

Food Interactions

Magnesium, potassium and zinc needs increased.
Take without regard to meals. Avoid alcohol. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

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. (source: Drug Bank)

Protein Binding

40% (source: Drug Bank)

Absorption

Rapidly and reproducibly absorbed (bioavailability greater than 95%). (source: Drug Bank)

Toxicity

LD<sub>50</sub>=263 mg/kg (orally in rats). Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm. (source: Drug Bank)

Isomeric SMILES Code:

CC(C)NCC(COc1cccc2c1cc[nH]2)O (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data Genotype Data Available Literature annotations available Not annotated
GRK5
  • CO
  •   
  •   
  •   
  • GN
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
HTR1A Uncurated Annotation (source: Drug Bank)
HTR1B Uncurated Annotation (source: Drug Bank)
ADRB1 Uncurated Annotation (source: Drug Bank)
ADRB2 Uncurated Annotation (source: Drug Bank)
ADRB3 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
Methyldopa Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
acetohexamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
aminophylline Uncurated Annotation Antagonism of action and increased effect of theophylline (source: Drug Bank)
chlorpromazine Uncurated Annotation Increased effect of both drugs (source: Drug Bank)
chlorpropamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
clonidine Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
dihydroergotamine Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
dihydroergotoxine Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
diltiazem Uncurated Annotation Increased risk of bradycardia (source: Drug Bank)
disopyramide Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
dyphylline Uncurated Annotation Antagonism of action and increased effect of theophylline (source: Drug Bank)
epinephrine Uncurated Annotation Hypertension, then bradycardia (source: Drug Bank)
ergonovine Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
ergotamine Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
fenoterol Uncurated Annotation Antagonism (source: Drug Bank)
formoterol Uncurated Annotation Antagonism (source: Drug Bank)
glibenclamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
gliclazide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glipizide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glisoxepide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glycodiazine Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
ibuprofen Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
indomethacin Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
isoproterenol Uncurated Annotation Antagonism (source: Drug Bank)
l-methyldopa Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
lidocaine Uncurated Annotation The beta-blocker increases the effect and toxicity of lidocaine (source: Drug Bank)
mesoridazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
methysergide Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
orciprenaline Uncurated Annotation Antagonism (source: Drug Bank)
oxtriphylline Uncurated Annotation Antagonism of action and increased effect of theophylline (source: Drug Bank)
pirbuterol Uncurated Annotation Antagonism (source: Drug Bank)
piroxicam Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
prazosin Uncurated Annotation Risk of hypotension at the beginning of therapy (source: Drug Bank)
procaterol Uncurated Annotation Antagonism (source: Drug Bank)
repaglinide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
salbutamol Uncurated Annotation Antagonism (source: Drug Bank)
salmeterol Uncurated Annotation Antagonism (source: Drug Bank)
terbutaline Uncurated Annotation Antagonism (source: Drug Bank)
theophylline Uncurated Annotation Antagonism of action and increased effect of theophylline (source: Drug Bank)
thioridazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
tolazamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
tolbutamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
verapamil Uncurated Annotation Increased effect of both drugs (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Cardiomyopathy, Dilated
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Cardiomyopathy, Hypertrophic
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Heart Failure
  • CO
  •   
  •   
  •   
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00960
KEGG Compound ID:
C07445
KEGG Drug ID:
D00513
PubChem Compound ID:
4828
PubChem Substance ID:
168830
IUPHAR Ligand ID:
127
91

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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