BISOPROLOL FUMARATE tablet

País: Estats Units

Idioma: anglès

Font: NLM (National Library of Medicine)

ingredients actius:

BISOPROLOL FUMARATE (UNII: UR59KN573L) (BISOPROLOL - UNII:Y41JS2NL6U)

Disponible des:

DIRECTRX

Vía de administración:

ORAL

tipo de receta:

PRESCRIPTION DRUG

indicaciones terapéuticas:

BISOPROLOL FUMARATE is indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents. BISOPROLOL FUMARATE is contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, and marked sinus bradycardia.

Resumen del producto:

BISOPROLOL FUMARATE is supplied as 5 mg and 10 mg tablets. The 5 mg tablet is pink colored, biconvex, round, film coated tablet debossed with UL on one side and scored on the other side with 5 debossed on either side of the score. Bottles of 30: NDC 29300-126-13 Bottles of 100: NDC 29300-126-01 Bottles of 500: NDC 29300-126-05 The 10 mg tablet is white colored, biconvex, round, film coated tablet debossed with UL on one side and 10 on the other side. Bottles of 30: NDC 29300-127-13 Bottles of 100: NDC 29300-127-01 Bottles of 500: NDC 29300-127-05 Store at 20° to 25°C (68° to 77°F). [see USP Controlled Room Temperature]. Protect from moisture. Dispense in tight, light-resistant containers. Please address medical inquiries to Unichem's toll free # 1-866-562-4616.

Estat d'Autorització:

Abbreviated New Drug Application

Fitxa tècnica

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET
DIRECTRX
----------
BISOPROLOL FUMARATE
Rx Only
BISOPROLOL FUMARATE is a beta1-selective (cardioselective)
adrenoceptor blocking agent
without significant membrane stabilizing activity or intrinsic
sympathomimetic activity in its therapeutic
dosage range. Cardioselectivity is not absolute, however, and at
higher doses (≥ 20 mg) bisoprolol
fumarate also inhibits beta2-adrenoceptors, chiefly located in the
bronchial and vascular musculature; to
retain selectivity it is therefore important to use the lowest
effective dose.
Pharmacokinetics and Metabolism
The absolute bioavailability after a 10 mg oral dose of bisoprolol
fumarate is about 80%. Absorption is
not affected by the presence of food. The first pass metabolism of
bisoprolol fumarate is about 20%.
Binding to serum proteins is approximately 30%. Peak plasma
concentrations occur within 2-4 hours of
dosing with 5 to 20 mg, and mean peak values range from 16 ng/mL at 5
mg to 70 ng/mL at 20 mg. Once
daily dosing with bisoprolol fumarate results in less than twofold
intersubject variation in peak plasma
levels. The plasma elimination half-life is 9-12 hours and is slightly
longer in elderly patients, in part
because of decreased renal function in that population. Steady state
is attained within 5 days of once
daily dosing. In both young and elderly populations, plasma
accumulation is low; the accumulation
factor ranges from 1.1 to 1.3, and is what would be expected from the
first order kinetics and once daily
dosing. Plasma concentrations are proportional to the administered
dose in the range of 5 to 20 mg.
Pharmacokinetic characteristics of the two enantiomers are similar.
Bisoprolol fumarate is eliminated equally by renal and non-renal
pathways with about 50% of the dose
appearing unchanged in the urine and the remainder appearing in the
form of inactive metabolites. In
humans, the known metabolites are labile or have no known
pharmacologic activity. Less than 2% of the
dose is excreted in the feces. Bisoprolol f