BETAXOLOL tablet, film coated

País: Estados Unidos

Língua: inglês

Origem: NLM (National Library of Medicine)

Ingredientes ativos:

BETAXOLOL HYDROCHLORIDE (UNII: 6X97D2XT0O) (BETAXOLOL - UNII:O0ZR1R6RZ2)

Disponível em:

Epic Pharma LLC

DCI (Denominação Comum Internacional):

BETAXOLOL HYDROCHLORIDE

Composição:

BETAXOLOL HYDROCHLORIDE 10 mg

Via de administração:

ORAL

Tipo de prescrição:

PRESCRIPTION DRUG

Indicações terapêuticas:

Betaxolol is indicated in the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly thiazide-type diuretics. Betaxolol is contraindicated in patients with known hypersensitivity to the drug. Betaxolol is contraindicated in patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure. (see Warnings).

Resumo do produto:

Betaxolol Tablets USP, 10 mg* contains 10 mg betaxolol hydrochloride (equivalent to 8.94 mg betaxolol) are white, round biconvex, film-coated tablets, debossed “ Є ” above and “38” below bisect on one side and plain on the other side, available in bottles of 100 and 1000. Betaxolol Tablets USP, 20 mg* contains 20 mg betaxolol hydrochloride (equivalent to 17.88 mg betaxolol) are white, round biconvex, film-coated tablets, debossed “ Є ” above “39” on one side and plain on the other side, available in bottles of 100 and 1000. Store at 20°–25°C (68°–77°F) [See USP Controlled Room Temperature]. Manufactured by: Epic Pharma, LLC Laurelton, NY 11413 Manufactured in USA Revised February 2016 MF038REV02/16 OE1091

Status de autorização:

Abbreviated New Drug Application

Características técnicas

BETAXOLOL- BETAXOLOL TABLET, FILM COATED
EPIC PHARMA LLC
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BETAXOLOL TABLETS USP, FILM-COATED
DESCRIPTION
Betaxolol is a β
-selective (cardioselective) adrenergic receptor blocking agent
available as 10-mg
and 20-mg tablets for oral administration. Betaxolol is chemically
described as 2-propanol,1-[4-[2-
(cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-,hydrochloride,(±).
It has the following
chemical structure:
Betaxolol hydrochloride is a water-soluble white crystalline powder
with a molecular formula of C
H
NO
•HCl and a molecular weight of 343.9. It is freely soluble in water,
ethanol, chloroform,
and methanol, and has a pKa of 9.4.
The inactive ingredients are anhydrous lactose, carnauba wax,
hypromellose, microcrystalline
cellulose, polyethylene glycol, polysorbate 80, pregeletanized starch
(corn), sodium starch glycolate,
stearic acid and titanium dioxide.
CLINICAL PHARMACOLOGY
Betaxolol is a β
-selective (cardioselective) adrenergic receptor blocking agent that
has weak
membrane-stabilizing activity and no intrinsic sympathomimetic
(partial agonist) activity. The
preferential effect on β
receptors is not absolute, however, and some inhibitory effects on β
receptors (found chiefly in the bronchial and vascular musculature)
can be expected at higher doses.
PHARMACOKINETICS AND METABOLISM
In man, absorption of an oral dose is complete. There is a small and
consistent first-pass effect resulting
in an absolute bioavailability of 89% ± 5% that is unaffected by the
concomitant ingestion of food or
alcohol. Mean peak blood concentrations of 21.6 ng/ml (range 16.3 to
27.9 ng/ml) are reached between
1.5 and 6 (mean about 3) hours after a single oral dose, in healthy
volunteers, of 10 mg of betaxolol.
Peak concentrations for 20-mg and 40-mg doses are 2 and 4 times that
of a 10-mg dose and have been
shown to be linear over the dose range of 5 to 40 mg. The peak to
trough ratio of plasma concentrations
over 24 hours is 2.7. The mean elimination half-life in various
studies in normal volunt