TIMOLOL MALEATE tablet

Land: USA

Sprog: engelsk

Kilde: NLM (National Library of Medicine)

Aktiv bestanddel:

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

Tilgængelig fra:

TRIGEN LABORATORIES, LLC

Indgivelsesvej:

ORAL

Recept type:

PRESCRIPTION DRUG

Terapeutiske indikationer:

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.

Produkt oversigt:

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 13811-618-10 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 13811-619-10 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 13811-620-10 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. Trigen Laboratories, LLC Bridgewater, NJ 08807 Rev. 10/2018

Autorisation status:

Abbreviated New Drug Application

Produktets egenskaber

TIMOLOL MALEATE- TIMOLOL MALEATE TABLET
TRIGEN LABORATORIES, LLC
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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