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QuickView for Betaxolol (compound)

Name: Betaxolol
PubChem Compound ID: 107952
Description: A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.
Molecular formula: C18H30ClNO3
Molecular weight: 343.888 g/mol
Betoptima; SL-75212; 1-(Isopropylamino)-3-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)propan-2-ol hydrochloride; MLS000028464; 2-Propanol, 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-, hydrochloride, (+-)-; EINECS 264-384-3; EU-0100193; Betoptic S; Kerlon; D00598.
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Name: Betaxolol
Name (isomeric): DB00195
Drug Type: small molecule
Description: A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.
Betaxolol HCL; Betaxololum [INN-Latin]; Betazolol
Brand: Betoptic, Kerlone, Betoptic S, Betaxon
Category: Sympatholytics, Adrenergic beta-Antagonists, Antihypertensive Agents, EENT Drugs
CAS number: 63659-18-7
Indication: For the management of hypertension.
Betaxolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Betaxolol is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. Activation of beta(1)-receptors (located mainly in the heart) by epinephrine increases the ...
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Mechanism of Action:
Betaxolol selectively blocks catecholamine stimulation of beta(1)-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Betaxolol can also competitively block beta(2)-adrenergic responses in the bron...
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Absorption: Absorption of an oral dose is complete. There is a small and consistent first-pass effect resulting in an absolute bioavailability of 89% ± 5% that is unaffected by the concomitant ingestion of food or alcohol.
Protein binding: 50%
Biotransformation: Primarily hepatic. Approximately 15% of the dose administered is excreted as unchanged drug, the remainder being metabolites whose contribution to the clinical effect is negligible.
Half Life: 14-22 hours
Toxicity: Oral LD50s are 350 to 400 mg betaxolol/kg in mice and 860 to 980 mg/kg in rats. Predicted symptoms of overdose include bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia.
Affected organisms: Humans and other mammals
Drug interaction:
ErgotamineIschemia with risk of gangrene
ChlorpropamideThe beta-blocker, betaxolol, may decrease symptoms of hypoglycemia.
ThiabendazoleThe strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Betaxolol by decreasing Betaxolol metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Betaxolol if Thiabendazole is initiated, discontinued or dose changed
FenoterolBeta-Blockers (Beta-1 Selective) like betaxolol may diminish the bronchodilatory effect of Beta2-Agonists like fenoterol. Therapy should be monitored.
ClonidineIncreased hypertension when clonidine stopped
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