TIMOLOL MALEATE solution/ drops

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

FDC Limited

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Timolol Maleate Ophthalmic Solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Timolol Maleate Ophthalmic Solution 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.

Product summary:

Sterile ophthalmic solution of timolol maleate is a clear, colorless solution. Timolol maleate ophthalmic solution USP, 0.25% timolol equivalent, is supplied in a labeled translucent LDPE bottle with insert cap assembly comprising of a yellow colored HDPE screw cap over a LDPE nozzle with tamper-evident LDPE dust- cover sealing the bottle cap. NDC 55545-1000-1,  5 mL in a 5 mL bottle NDC 55545-1000-2,  10 mL in a 10 mL bottle NDC 55545-1000-3,  15 mL in a 15 mL bottle Timolol maleate ophthalmic solution USP, 0.5% timolol equivalent, is supplied in a labeled translucent LDPE bottle with insert cap assembly comprising of a yellow colored HDPE screw cap over a LDPE nozzle with tamper-evident LDPE dust- cover sealing the bottle cap. NDC 55545-1001-1,  5 mL in a 5 mL bottle NDC 55545-1001-2,  10 mL in a 10 mL bottle NDC 55545-1001-3,  15 mL in a 15 mL bottle Storage Store at 25°C (77°F); excursions permitted 15°C to 30°C (59°F to 86°F)[See USP controlled room temperature] Protect from freezing. Protect from light.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TIMOLOL MALEATE- TIMOLOL MALEATE SOLUTION/ DROPS
FDC LIMITED
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STERILE OPHTHALMIC SOLUTION
TIMOLOL MALEATE
OPHTHALMIC SOLUTION
USP 0.25% AND 0.5%
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:
Its molecular formula is C
H N O S•C H O and its structural formula is:
IMAG E
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 stable at
room temperature. Timolol
Maleate Ophthalmic Solution is supplied as a sterile, isotonic,
buffered, aqueous solution of Timolol
maleate in two dosage strengths: Each mL of Timolol Maleate Ophthalmic
Solution 0.25% contains 2.5
mg of timolol (3.4 mg of Timolol Maleate). The pH of the solution is
approximately 7.0, and the
osmolarity is 274-328 mOsm. Each mL of Timolol Maleate Ophthalmic
Solution 0.5% contains 5 mg of
timolol (6.8 mg of timolol maleate).
Inactive ingredients: monobasic and dibasic sodium phosphate, sodium
chloride, sodium hydroxide to
adjust pH, and water for injection. Benzalkonium chloride 0.01% is
added as preservative.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Timolol maleate is a beta and beta (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
adequate cardiac function.
Beta-adrenergic r