Bisoprolol fumarate

Bezeichnung:Bisoprolol fumarate

CAS-Nr104344-23-2

Englisch Name:Bisoprolol fumarate

CBNumberCB8371980

SummenformelC22H35NO8

Molgewicht441.52

MOL-Datei104344-23-2.mol

Bisoprolol fumarate physikalisch-chemischer Eigenschaften

Schmelzpunkt	100°C
storage temp.	2-8°C
Löslichkeit	DMSO: >20 mg/mL
Aggregatzustand	solid
Farbe	white
Merck	14,1295
InChIKey	RZPZLFIUFMNCLY-WLHGVMLRSA-N
SMILES	C1(OCC(O)CNC(C)C)C=CC(COCCOC(C)C)=CC=1.C(/C(=O)O)=C\C(=O)O
CAS Datenbank	104344-23-2(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xn,Xi
R-Sätze:	22
WGK Germany	3
RTECS-Nr.	UB8390000
HazardClass	IRRITANT
HS Code	2922190900
Toxizität	dog,LDLo,oral,40mg/kg (40mg/kg),BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)SENSE ORGANS AND SPECIAL SENSES: MYDRIASIS (PUPILLARY DILATION): EYELUNGS, THORAX, OR RESPIRATION: OTHER CHANGES,Kiso to Rinsho. Clinical Report. Vol. 23, Pg. 2321, 1989.

Gefahreninformationscode (GHS)

Bisoprolol fumarate Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
Beschreibung
Bisoprolol fumarate is a β1-selective adrenergic blocker useful in the treatment of essential hypertension.
Chemische Eigenschaften
White Solid
Originator
E. Merck (W. Germany)
Verwenden
Labeled Bisoprolol, intended for use as an internal standard for the quantification of Bisoprolol by GC- or LC-mass spectrometry.
Verwenden
semi-synthetic kanamycin-derived aminoglycoside antibiotic
Verwenden
antiinflammatory
Verwenden
A selective β-adrenergic blocker. Used as an antihypertensive.
Verwenden
A selective α-adrenergic blocker. Used as an antihypertensive.
Verwenden
A selective a-adrenergic blocker. Used as an antihypertensive
Manufacturing Process
A solution of 10 g of 1-(p-2-isopropoxyethoxymethylphenoxy)-3-isopropylideneamino-propan-2-ol [obtainable by reacting 1-(p-2- isopropoxyethoxymethylphenoxy)-2,3-epoxy propane with ammonia to give 1- (p-2-isopropoxyethoxymethylphenoxy)-3-amino-propan-2-ol and subsequently reacting this with acetone] in 250 ml of ethanol was hydrogenated on 0.5 g of Raney nickel at 25°C under 1 atmosphere of pressure until 1 equivalent of H2 had been absorbed. The mixture was filtered and the filtrate evaporated to give 1-(p-2-iso-propoxyethoxymethyl-phenoxy)-3-isopropylamino-propan-2-ol, fumarate, m.p. 100°C (after addition of equimolecular quantity of fumaric acid).
Trademarks
Zebeta (Duramed);CONCOR.
Therapeutic Function
Beta-adrenergic blocker
Biologische Aktivität
A selective β 1 -adrenergic antagonist. Has a K d of 2-3 nM at the β 1 receptor and a β 1 / β 2 selectivity of approximately 100-fold.
Biochem/physiol Actions
Bisoprolol hemifumarate is useful in oral formulations due to its high bioavailability. It also shows long elimination half-life.
Clinical Use
Beta-1 adrenoceptor blocker:

Hypertension

Angina

Adjunctive treatment for heart failure
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect. Analgesics: NSAIDs antagonise hypotensive effect. Anti-arrhythmics: increased risk of myocardial depression and bradycardia; increased risk of bradycardia, myocardial depression and AV block with amiodarone; increased risk of myocardial depression and bradycardia with flecainide. Antibacterials: concentration reduced by rifampicin. Antidepressants: enhanced hypotensive effect with MAOIs.
Antihypertensives; enhanced hypotensive effect; increased risk of withdrawal hypertension with clonidine; increased risk of first dose hypotensive effect with post-synaptic alpha-blockers such as prazosin.
Antimalarials: increased risk of bradycardia with mefloquine.
Antipsychotics enhanced hypotensive effect with phenothiazines.
Calcium-channel blockers: increased risk of bradycardia and AV block with diltiazem; hypotension and heart failure possible with nifedipine and nisoldipine; asystole, severe hypotension and heart failure with verapamil.
Cytotoxics: possible increased risk of bradycardia with crizotinib.
Diuretics: enhanced hypotensive effect.
Fingolimod: possibly increased risk of bradycardia.
Moxisylyte: possible severe postural hypotension.
Sympathomimetics: severe hypertension with adrenaline and noradrenaline, and possibly with dobutamine.
Stoffwechsel
Bisoprolol is excreted from the body by two routes. 50% is metabolised by the liver to inactive metabolites which are then excreted by the kidneys. The remaining 50% is excreted by the kidneys in an unmetabolised form.

Bisoprolol fumarate Upstream-Materialien And Downstream Produkte

Bisoprolol fumarate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

104344-23-2, Bisoprolol fumarate Verwandte Suche:

Send Inquriy