QuickView for Pindolol (compound)

Summary
General Info

PubChem

PubChem Compound 155030

Name:	Pindolol
PubChem Compound ID:	155030
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)
Molecular formula:	C₁₄H₂₀N₂O₂
Molecular weight:	248.321 g/mol
Synonyms:	NCGC00024925-01; Tocris-0994; Lopac-P-0778; CAS-13523-86-9; Lopac-P-152-Batch2; 2-Propanol, 1-(1H-indol-4-yloxy)-3-((1-methylethyl)amino)-, (R)-; 68374-35-6; Lopac-P-152; NCGC00015786-03; NCGC00016700-01. show more » NCGC00024925-01; Tocris-0994; Lopac-P-0778; CAS-13523-86-9; Lopac-P-152-Batch2; 2-Propanol, 1-(1H-indol-4-yloxy)-3-((1-methylethyl)amino)-, (R)-; 68374-35-6; Lopac-P-152; NCGC00015786-03; NCGC00016700-01; NCGC00015786-02; NCGC00015786-01 show less «

DrugBank

Identification

Name:	Pindolol
Name (isomeric):	DB00960
Drug Type:	small molecule
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)
Synonyms:	Betapindol; Prinodolol
Brand:	Visken, Durapindol, Decreten, Pectobloc, Pinbetol, Calvisken, Blocklin L, Cardilate, Blockin L, Pynastin, Glauco-Visken
Brand name mixture:	Viskazide 10/50tab(Hydrochlorothiazide + Pindolol), Viskazide 10/25tab(Hydrochlorothiazide + Pindolol)
Category:	Serotonin Antagonists, Vasodilator Agents, Adrenergic beta-Antagonists, Antihypertensive Agents
CAS number:	13523-86-9

Pharmacology

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-choles... show more » 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. show less «
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... show more » 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. show less «
Absorption:	Rapidly and reproducibly absorbed (bioavailability greater than 95%).
Protein binding:	40%
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.
Route of 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.
Half Life:	3 to 4 hours
Clearance:	50-300 mL/min [cirrhotic patients]
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

Interactions

Food interaction:

Take without regard to meals. Avoid alcohol.

Magnesium, potassium and zinc needs increased.

Drug interaction:

Methyldopa	Possible hypertensive crisis
Ibuprofen	Risk of inhibition of renal prostaglandins
Ergonovine	Ischemia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Tolazamide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.

Methyldopa	Possible hypertensive crisis
Ibuprofen	Risk of inhibition of renal prostaglandins
Ergonovine	Ischemia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Tolazamide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Procaterol	Antagonism
Epinephrine	Hypertension, then bradycardia
Glipizide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Oxtriphylline	Antagonism of action and increased effect of theophylline
Terazosin	Increased risk of hypotension. Initiate concomitant therapy cautiously.
Clonidine	Increased hypertension when clonidine stopped
Insulin	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Salmeterol	Antagonism
Acetohexamide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Lidocaine	The beta-blocker increases the effect and toxicity of lidocaine
Dyphylline	Antagonism of action and increased effect of theophylline
Terbutaline	Antagonism
Methysergide	Ischemia with risk of gangrene
Chlorpromazine	Increased effect of both drugs
Tolbutamide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Mesoridazine	Increased risk of cardiotoxicity and arrhythmias
Salbutamol	Antagonism
Disopyramide	The beta-blocker, pindolol, may increase the toxicity of disopyramide.
Fenoterol	Antagonism
Glyburide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Pipobroman	Antagonism
Thioridazine	Increased risk of cardiotoxicity and arrhythmias
Orciprenaline	Antagonism
Dihydroergotamine	Ischemia with risk of gangrene
Formoterol	Antagonism
Glisoxepide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Diltiazem	Increased risk of bradycardia
Dihydroergotoxine	Ischemia with risk of gangrene
Repaglinide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Isoproterenol	Antagonism
Verapamil	Increased effect of both drugs
Aminophylline	Antagonism of action and increased effect of theophylline
Pirbuterol	Antagonism
Theophylline	Antagonism of action and increased effect of theophylline
Chlorpropamide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Glycodiazine	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Prazosin	Risk of hypotension at the beginning of therapy
Insulin Glargine	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Piroxicam	Risk of inhibition of renal prostaglandins
Gliclazide	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Indomethacin	Risk of inhibition of renal prostaglandins

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Targets

Beta-1 adrenergic receptor

Beta-2 adrenergic receptor

5-hydroxytryptamine 1A receptor

5-hydroxytryptamine 1B receptor

Enzymes

Cytochrome P450 2D6