BETAXOLOL tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Physicians Total Care, Inc.

INN (International Name):

BETAXOLOL HYDROCHLORIDE

Composition:

BETAXOLOL HYDROCHLORIDE 10 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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).

Product summary:

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 Store at 20°–25°C (68°–77°F) [See USP Controlled Room Temperature]. Manufactured by: Epic Pharma, LLC Laurelton, NY 11413 Issued 05/10 MF038ISS05/10 OE1091 Relabeling and Repackaging by: Physicians Total Care, Inc. Tulsa, Oklahoma        74146

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BETAXOLOL - BETAXOLOL TABLET, FILM COATED
PHYSICIANS TOTAL CARE, INC.
----------
BETAXOLOL TABLETS USP, FILM-COATED
RX ONLY
DESCRIPTION
Betaxolol is a β1-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:
FIG URE 1 - STRUCTURAL FORMULA
Betaxolol hydrochloride is a water-soluble white crystalline powder
with a molecular formula of
C18H29NO3•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 β1-selective (cardioselective) adrenergic receptor
blocking agent that has weak
membrane-stabilizing activity and no intrinsic sympathomimetic
(partial agonist) activity. The
preferential effect on β1 receptors is not absolute, however, and
some inhibitory effects on β2
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 me