Pindolol drug data and news

Pindolol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Pindolol
Brand Names/Synonyms Betapindol; Blockin L; Blocklin L; Calvisken; Cardilate; Decreten; Durapindol; Glauco-Visken; LB-46; Pectobloc; Pinbetol; Pindolol; Prinodolol; Pynastin; Visken
Indication For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.
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Description Not Available
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.
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.
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Dosage Forms TABLET
Drug_Category Vasodilator Agents; Antihypertensive Agents; Adrenergic beta-Antagonists; Serotonin Antagonists; ATC:C07AA03; ATC:C07AA14; ATC:C07AA17
Absorption Rapidly and reproducibly absorbed (bioavailability greater than 95%).
Interactions Interactions for Pindolol:

Catecholamine-depleting drugs (e.g., reserpine) may have an additive effect when given with beta-blocking agents. Patients receiving pindolol plus a catecholamine-depleting agent should, therefore, be closely observed for evidence of hypotension and/or marked bradycardia which may produce vertigo, syncope, or postural hypotension.

Pindolol has been used with a variety of antihypertensive agents, including hydrochlorothiazide, hydralazine, and guanethidine without unexpected adverse interactions.

Pindolol has been shown to increase serum thioridazine levels when both drugs are co-administered. Pindolol levels may also be increased with this combination.

Risk of anaphylactic reaction: While taking beta blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reactions.

Toxicity Oral, rat LD50: 263 mg/kg. Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm.
Organisms Affected Humans and other mammals
Chemical IUPAC Name 1-(1H-indol-4-yloxy)-3-(1-methylethylamino)propan-2-ol
Chemical Formula C14H20N2O2
Molecular Weight 248.321 g/mol
Smiles String CC(C)NCC(COC1=CC=CC2=C1C=CN2)O
Melting Point 167-171 °C
Water Solubility 7880 mg/L
State Solid
LogP/Hphobicity 2.525
Isoelectric Point Not Available
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.
Half Life 3 to 4 hours
Protein Binding [%] 40%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Pindolol.html
http://www.rxlist.com/cgi/generic3/pindolol.htm
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/pin1611.shtml
Drug Type Approved Drug
Accession No APRD00678
CAS Registry Number 13523-86-9
KEGG Compound ID C07445
PubChem ID SID:168830
PharmGKB ID PA450966
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 828424

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