TIMOLOL MALEATE tablet

Land: Verenigde Staten

Taal: Engels

Bron: NLM (National Library of Medicine)

Werkstoffen:

TIMOLOL MALEATE (UNII: P8Y54F701R) (TIMOLOL ANHYDROUS - UNII:5JKY92S7BR)

Beschikbaar vanaf:

Athem LLC

Toedieningsweg:

ORAL

Prescription-type:

PRESCRIPTION DRUG

therapeutische indicaties:

Hypertension Timolol maleate tablets are indicated for the treatment of hypertension. They may be used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics. Myocardial Infarction Timolol is indicated in patients who have survived the acute phase of myocardial infarction, and are clinically stable, to reduce cardiovascular mortality and the risk of reinfarction. Migraine Timolol is indicated for the prophylaxis of migraine headache. Timolol maleate is contraindicated in patients with bronchial asthma or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease (see WARNINGS); sinus bradycardia; second- and third-degree atrioventricular block; overt cardiac failure (see WARNINGS); cardiogenic shock; hypersensitivity to this product.

Product samenvatting:

Timolol Maleate Tablets, USP are available containing 5 mg, 10 mg and 20 mg of timolol maleate, USP. The 5 mg tablets are white to off-white, round tablets, engraved IT70 on one side, and the other side is plain. They are available as follows: NDC 73152-029-01 bottles of 100 tablets The 10 mg tablets are white to off-white, round tablets, engraved IT above bisect and 71 below bisect on one side, other side is plain. They are available as follows: NDC 73152-030-01 bottles of 100 tablets The 20 mg tablets are white to off-white, capsule shaped tablets, engraved IT bisect 72 on one side and other side is plain. They are available as follows: NDC 73152-031-01 bottles of 100 tablets Store at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.] Protect from light. Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure. Keep container tightly closed. Athem, LLC East Brunswick, NJ 08816 Rev. 05/2021

Autorisatie-status:

Abbreviated New Drug Application

Productkenmerken

TIMOLOL MALEATE- TIMOLOL MALEATE TABLET
ATHEM LLC
----------
TIMOLOL MALEATE
DESCRIPTION
Timolol maleate is a nonselective beta-adrenergic receptor blocking
agent. The chemical
name for timolol maleate is
(S)-1-[(1,1-dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-
thiadiazol-3-yl]oxy]-2-propanol (Z)-2-butenedioate (1:1) salt. It
possesses an
asymmetric carbon atom in its structure and is provided as the levo
isomer. Its
molecular formula is C13H24N4O3S•C4H4O4and its structural formula
is:
Timolol maleate has a molecular weight of 432.50. It is a white,
odorless, crystalline
powder which is soluble in water, methanol, and alcohol.
Timolol maleate is supplied as tablets containing 5 mg, 10 mg and 20
mg timolol maleate
for oral administration. Inactive ingredients are: colloidal silicon
dioxide, croscarmellose
sodium, magnesium stearate, microcrystalline cellulose, pregelatinized
maize starch,
sodium lauryl sulfate.
CLINICAL PHARMACOLOGY
Timolol maleate is a beta1 and beta2 (nonselective) adrenergic
receptor blocking agent
that does not have significant intrinsic sympathomimetic, direct
myocardial depressant,
or local anesthetic activity.
PHARMACODYNAMICS
Clinical pharmacology studies have confirmed the beta-adrenergic
blocking activity as
shown by (1) changes in resting heart rate and response of heart rate
to changes in
posture; (2) inhibition of isoproterenol-induced tachycardia; (3)
alteration of the
response to the Valsalva maneuver and amyl nitrite administration; and
(4) reduction of
heart rate and blood pressure changes on exercise.
Timolol decreases the positive chronotropic, positive inotropic,
bronchodilator, and
vasodilator responses caused by beta-adrenergic receptor agonists. The
magnitude of
this decreased response is proportional to the existing sympathetic
tone and the
concentration of timolol at receptor sites.
In normal volunteers, the reduction in heart rate response to a
standard exercise was
dose dependent over the test range of 0.5 to 20 mg, with a peak
reduction at 2 hours
of approximatel