TIMOLOL MALEATE solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Physicians Total Care, Inc.

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Timolol maleate ophthalmic solution USP is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Timolol maleate is contraindicated in patients with (1) bronchial asthma; (2) a history of bronchial asthma; (3) severe chronic obstructive pulmonary disease (see WARNINGS ); (4) sinus bradycardia; (5) second or third degree atrioventricular block; (6) overt cardiac failure (see WARNINGS ); (7) cardiogenic shock; or (8) hypersensitivity to any component of this product. The DROP-TAINER® bottle is designed to assure the delivery of a precise dose of medication. Before using your DROP-TAINER bottle, read the complete instructions carefully. 1. If you use other topically applied ophthalmic medications, they should be administered at least 10 minutes before or after Timolol Maleate Ophthalmic Solution. 2. Wash hands before each use. 3. Before using the medication for the first time, be sure the Safety Seal on the bottle is unbroken. 4. Tear off th

Product summary:

Sterile timolol maleate ophthalmic solution USP is a clear, colorless to light yellow solution. Timolol maleate ophthalmic solution, 0.25% timolol equivalent, is supplied in a white, opaque, plastic ophthalmic dispenser with a controlled drop tip as follows: NDC 54868-3713-0 10 mL Timolol maleate ophthalmic solution, 0.5% timolol equivalent, is supplied in a white, opaque, plastic ophthalmic dispenser with a controlled drop tip as follows: NDC 54868-3714-2 5 mL NDC 54868-3714-1 10 mL Storage : Store at room temperature 15° - 30°C (59° - 86°F). Protect from freezing. Protect from light. * BLOCADREN is a registered trademark of Merck & Co., Inc. Rx Only 340048-0604 Revised: June 2004          

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TIMOLOL MALEATE - TIMOLOL MALEATE SOLUTION
PHYSICIANS TOTAL CARE, INC.
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TIMOLOL MALEATE
OPHTHALMIC SOLUTION USP
STERILE
DESCRIPTION
Timolol maleate ophthalmic solution is a non-selective beta-adrenergic
receptor blocking agent. Its
chemical name is
(-)-1-(_tert-_butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy]-2-propanol
maleate (1:1) (salt). Timolol maleate possesses an asymmetric carbon
atom in its structure and is
provided as the levo-isomer. The optical rotation of timolol maleate
is:
[α] 25° in 1.0N HCl (C = 5%) = -12.2° ( -11.7° to -12.5°).
405 nm
Its molecular formula is C
H N O S•C H O and 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 ophthalmic
solution USP is stable at room
temperature.
Timolol maleate ophthalmic solution is supplied as a sterile,
isotonic, buffered, aqueous solution of
timolol maleate in two do sage strengths: Each mL of timolol maleate
ophthalmic solution 0.25%
contains 2.5 mg of timolol (3.4 mg of timolol maleate). Each mL of
timolol maleate ophthalmic solution
0.5% contains 5.0 mg of timolol (6.8 mg of timolol maleate). Inactive
ingredients: monobasic and
dibasic sodium phosphate, sodium hydroxide to adjust pH (6.5 to 7.5),
and purified water. Benzalkonium
chloride 0.01% is added as preservative.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Timolol maleate is a beta1 and beta2 (non-selective) adrenergic
receptor blocking agent that does not
have significant intrinsic sympathomimetic, direct myocardial
depressant, or local anesthetic
(membrane-stabilizing) activity.
Beta-adrenergic receptor blockade reduces cardiac output in both
healthy subjects and patients with
heart disease. In patients with severe impairment of myocardial
function beta-adrenergic receptor
blockade may inhibit the stimulatory effect of the sympathetic nervous
system necessary to maintain
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4
3
4
4
4
adequate cardiac function.
Beta-adrenergic receptor