Monograph number:
1336
Title
Bisoprolol Fumarate
Specification
BP/EP
Category
Antihypertensive
DMF Status
TP (Technical Package)
CAS Registry number
[66722-44-9]
CAS name(s)
1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol
Additional name(s)
(plus or minus)-1-[[alpha-(2-isopropoxyethoxy)- p- tolyl]oxy]-3-(isoprop yl amino)-2-propanol; (plus or minus)-1-[ p- (2-isopropoxyethoxymeth yl) phenoxy]-3-(isopropylamino)-2-propanol
Drug code(s)
EMD- 33512
Molecular formula
C 18 H 31 NO 4
Molecular weight
325.45
Percent Composition
C 66.43%, H 9.60%, N 4.30%, O 19.66%
.
Literature references
Cardioselective beta 1 -adrenergic blocker. Prepn: Belg. pat. 859,425; R. Jonas et al., U.S. pat. 4,258,062 (1978, 1981 both to E. Merck). Clinical pharmacology: A. E. Tatters field et al., Brit. J. Clin. Pharmacol. 18, 343 (1984); P. Dorow, U. Toumlnnes mann, Eur. J. Clin. Pharmacol. 27, 135 (1984). Binding study of (minus)-form: A. J. Kaumann, H. Lemoine, Arch. Pharmacol. 331, 27 (1985). HPLC determn of enantiomers in plasma and urine: T. Suzuki et al. , J. Chromatog. 619, 267 (1993). Clinical evaluation in angina: R. S. Kohli et al., Eur. Heart J. 6, 845 (1985); in hypertension: F. R. Bühler et al., J. Cardiovasc. Pharmacol. 8, Suppl. 11, S122 (1986). Review of pharmacokinetics: J. Grevel et al., Clin. Pharmacokinet. 17, 53-63 (1989); of clinical effi cacy in combination with hydrochlorothiazide: P. K. Zachariah et al., Clin. Ther. 15, 779-787 (1993)
Derivative
Hemifumarate
Molecular Formula
C 18 H 31 NO 4 .halfC 4 H 4 O 4
CAS Registry
[104344-23-2]
Trade name(s)
Concor (Merck KGaA) , Detensiel (Merck-Cleacutevenot) , Emconcor (Merck KGaA) , Emcor (Merck KGaA) , Euradal (Lacer) , Isoten (Lederle) , Monocor (Am. Cyanamid) , Soprol (Lederle) , Zebeta (Lederle)
Properties
Crystals, Sol in ethanol
Melting Point
100 degrees
Derivative
Mixture with hydrochlorothiazide
Trade name(s)
Ziac (Am. Cyanamid)