Betaxolol

Bezeichnung:Betaxolol

CAS-Nr63659-18-7

Englisch Name:Betaxolol

CBNumberCB1134548

SummenformelC18H29NO3

Molgewicht307.43

MOL-Datei63659-18-7.mol

Betaxolol physikalisch-chemischer Eigenschaften

Schmelzpunkt	61-63°C
Siedepunkt	448.0±40.0 °C(Predicted)
Dichte	1.067±0.06 g/cm3(Predicted)
storage temp.	-20°C Freezer
Löslichkeit	Chloroform (Slightly), Methanol (Slightly)
pka	pKa 9.21 (Uncertain)
Aggregatzustand	Solid
Farbe	White
CAS Datenbank	63659-18-7(CAS DataBase Reference)

Sicherheit

HS Code

29225090

Gefahreninformationscode (GHS)

Betaxolol Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
White Crystalline Solid
Originator
Kerlone,Carriere,France,1983
Verwenden
Cardioselective β1-adrenergic blocker. An antihypertensive; antiglaucoma.
Verwenden
Cardioselective 1-adrenergic blocker. An antihypertensive; antiglaucoma
Definition
ChEBI: A propanolamine that is 3-aminopropane-1,2-diol in which the hydrogen of the primary hydoxy is substituted by a 4-[2-(cyclopropylmethoxy)ethyl]phenyl group and one of the hydrogens attached to the amino group is substituted by isopropyl. It is a selective beta1-receptor blocker and is used in the treatment of glaucoma as well as hypertension, arrhythmias, and coronary heart disease. It is also used to reduce non-fatal cardiac events in patients with heart failure.
Manufacturing Process
(1) 1 g of sodium hydroxide pellets (0.025 mol) is added to a suspension of 3.8 g of 4-[2-(cyclopropylmethoxy)-ethyl]-phenol in 30 ml of water. When the solution becomes homogenous, 2.3 ml of epichlorohydrin are added and the mixture is stirred for 8 hours. It is then extracted with ether and the extract is washed with water, dried over sodium sulfate and evaporated to dryness. The compound is purified by passing it over a silica column. 2.4 g of 1-[4-[2- (cyclopropylmethoxy)ethyl]-phenoxy]-2,3-epoxy-propane are thus obtained.
(2) 4.9 g of the preceding compound (0.02 mol) are condensed with 25 ml of isopropylamine by contact for 8 hours at ambient temperature and then by heating for 48 hours at the reflux temperature. After evaporation to dryness, the compound obtained is crystallized from petroleum ether. 5 g (yield 80%) of 2-[[4-(2-cyclopropylmethoxy)-ethyl]-phenoxy]-3-isopropylaminopropan-2-ol are thus obtained, melting point 70° to 72°C.
The hydrochloride is prepared by dissolving the base in the minimum amount of acetone and adding a solution of hydrochloric acid in ether until the pH is acid. The hydrochloride which has precipitated is filtered off and is recrystallized twice from acetone, melting point 116°C.
Trademarks
Betoptic (Alcon); Kerlone (Sanofi Aventis).
Therapeutic Function
Beta-adrenergic blocker
Biologische Aktivität
betaxolol is a cardioselective beta-adrenergic receptor blocking agent. betaxolol (5 mg/kg via i.p. injection) was administered at 24 and then 44 h following the final chronic cocaine administration. animals treated with betaxolol during cocaine withdrawal
Veterinary Drugs and Treatments
Betaxolol HCl is a specific Beta1 adrenergic blocking agent which reduces aqueous humor production by decreasing cyclic-AMP synthesis in the ciliary body. This drug is a suitable substitute for timolol and because of its specific Beta1 activity, might be a first choice Beta blocking agent for patients with concurrent respiratory disease. Either levobunolol HCl or betaxolol HCl would be the first choice Beta blocking agent in a feline patient with glaucoma and asthma, although a topical carbonic anhydrates inhibitor should be considered before a Beta blocking agent in this situation. Betaxolol and the other Beta blockers should be used with caution in patients with cardiac disease.
Stoffwechsel
Absorption of an oral dose of betaxolol (Kerlone, Betoptic) is almost complete. The drug is subject to a slight first-pass effect such that the absolute bioavailability of the drug is about 90%.Approximately 50% of administered betaxolol binds to plasma proteins, and its plasma half-life is about 20 hours; it is suitable for dosing once per day.The primary route of elimination is by liver metabolism, with only 15% of unchanged drug being excreted.

Betaxolol Upstream-Materialien And Downstream Produkte

Betaxolol Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

63659-18-7, Betaxolol Verwandte Suche:

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