Betaxolol

ZB-5 · C06849 · βxolol · BETAXOLOL · Betaxolols · Betoptic S · Betaprolol · Betaxolol Base

Identifikatoren & physikalische Daten

CAS No.	63659-18-7
Summenformel	C18H29NO3
Durchschnittliche Molmasse	307,4 g/mol
Monoisotopische Masse	307,21474379 g/mol
SMILES	CC(C)NCC(O)COc1ccc(CCOCC2CC2)cc1
InChIKey	NWIUTZDMDHAVTP-UHFFFAOYSA-N
PubChem CID	2369
ChEMBL	CHEMBL423
ChEBI	CHEBI:3082
EC No.	613-310-1
DTXSID	DTXSID2022674

Chemische & physikalische Eigenschaften

XLogP	2,8
Polarare Oberfläche (TPSA)	50,7
H-Brücken-Donoren	2
H-Brücken-Akzeptoren	4
Frei drehbare Bindungen	11
Schwere Atome	22
Formalladung	0
Komplexität	286
Arzneimittel	Pharmaceuticals
LogP (Verteilungskoeffizient)	2.42.81
Löslichkeit	2.98e-02 g/LChloroform (Slightly), Methanol (Slightly)
Human Drugs	Breast FeedingLactationMilk, HumanAntihypertensive AgentsAdrenergic Beta-AntagonistsAntiglaucoma AgentsAntiarrhythmicsPharmaceuticals
Schmelzpunkt	70-72 °C70 - 72 °C61-63°C
Physical Description	Solid
Dissociation Constants	9.219.4
Siedepunkt	448.0±40.0 °C(Predicted)
Dichte	1.067±0.06 g/cm3(Predicted)
Lagerbedingungen	-20°C Freezer
pKa (Säurekonstante)	pKa 9.21 (Uncertain)
Aggregatzustand	Solid
Farbe	White
CAS Datenbank	63659-18-7(CAS DataBase Reference)

Sicherheit & Vorschriften

GHS-Einstufung	WarningH302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]P203, P264, P270, P273, P280, P301+P317, P318, P330, P405, and P501 (click each P-code to see the statement)The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.
Hazard Classes and Categories	Acute Tox. 4 (100%)
Hepatotoxicity	Betaxolol therapy has been associated with a low rate of mild-to-moderate elevations of serum aminotransferase levels which are usually asymptomatic and transient and resolve even with continuation of therapy. There have been no well documented cases of clinically apparent, acute liver injury attributable to betaxolol. Thus, hepatotoxicity due to betaxolol must be very rare, if it occurs at all. Most commonly used beta-blockers have been linked to rare instances of clinically apparent liver injury, typically with onset within 2 to 12 weeks, a hepatocellular pattern of liver enzyme elevations, rapid recovery on withdrawal, and little evidence of hypersensitivity (rash, fever, eosinophilia) or autoantibody formation.
Unerwünschte Wirkungen	Betaxolol has both local and systemic adverse effects. The ocular adverse drug reactions include transient irritation (25% to 40%), burning, pruritus, punctate keratitis, and blurry vision. Compared to topical timolol (a nonselective β-blocker), betaxolol showed a higher incidence of ocular adverse effects. Compared to nonselective topical β-adrenergic receptor blockers, betaxolol is less likely to cause adverse effects on pulmonary function. However, betaxolol use still requires caution in patients with underlying pulmonary disease. Symptomatic pulmonary obstruction due to betaxolol has been reported in patients with underlying asthma or chronic obstructive pulmonary disease. A post-marketing study in the United States identified 56 spontaneous adverse effect reports, with 8 cases requiring hospitalization due to asthma exacerbation.
Toxizitätsübersicht	Signs and Symptoms of Overdose
Drug Induced Liver Injury	Drug-Induced Liver Injury Severity and Toxicity (DILIst)betaxololDILI NegativeOralDOI:10.1016/j.drudis.2019.09.022
Effects During Pregnancy and Lactation	◉ Summary of Use during Lactation
Zollcode	29225090

Anwendungen & Verwendung

Verwenden

Cardioselective 1-adrenergic blocker. An antihypertensive; antiglaucoma