TIMOLOL MALEATE- timolol solution/ drops

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Timolol (UNII: 817W3C6175) (Timolol Anhydrous - UNII:5JKY92S7BR)

Available from:

Akorn

INN (International Name):

Timolol

Composition:

Timolol Anhydrous 2.5 mg in 1 mL

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Timolol is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Timolol is contraindicated in patients with overt heart failure, cardiogenic shock, sinus bradycardia, second- or third-degree atrioventricular block, bronchial asthma or history of bronchial asthma, or severe chronic obstructive pulmonary disease, or hypersensitivity to any component of this product.

Product summary:

Timolol Ophthalmic Solution is a clear, colorless solution. Timolol Ophthalmic Solution 0.25% is supplied in a white, opaque, plastic, ophthalmic dispenser bottle with a controlled drop tip as follows: STORAGE: Store at 20º to 25°C (68º to 77°F) [see USP Controlled Room Temperature]. Do not freeze. Protect from light. AKORN Manufactured by: Akorn, Inc. Lake Forest, IL 60045 TML00N       Rev. 07/15

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TIMOLOL MALEATE- TIMOLOL SOLUTION/ DROPS
AKORN
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TIMOLOL OPHTHLAMIC SOLUTION, 0.25% AND 0.5%
DESCRIPTION
Timolol ophthalmic solution, 0.25% and 0.5%, is a non-selective
beta-adrenergic
antagonist for ophthalmic use. The chemical name of the active
ingredient is (S)-1-[(1,1-
dimethylethyl)amino]-3-[(4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-
propanol. Timolol
hemihydrate is the levo isomer. Specific rotation is [α]
405nm= -16° (C=10% as the
hemihydrate form in 1N HCl).
The molecular formula of timolol is Formula C
H
N O S and its structural formula is:
Timolol (as the hemihydrate) is a white, odorless, crystalline powder
which is slightly
soluble in water and freely soluble in ethanol. Timolol hemihydrate is
stable at room
temperature.
Timolol ophthalmic solution is a clear, colorless, isotonic, sterile,
microbiologically
preserved phosphate buffered aqueous solution. It is supplied in two
dosage strengths,
0.25% and 0.5%.
Each mL of Timolol 0.25% contains 2.56 mg of timolol hemihydrate
equivalent to 2.5 mg
Timolol. Each mL of Timolol 0.5% contains 5.12 mg of timolol
hemihydrate equivalent to
5 mg timolol.
Inactive ingredients: monosodium and disodium phosphate dihydrate to
adjust pH (6.5
to 7.5) and water for injection, benzalkonium chloride 0.01% added as
preservative.
The osmolality of timolol ophthalmic solution is 260 to 320 mOsmol/kg.
CLINICAL PHARMACOLOGY
Timolol is a non-selective beta-adrenergic antagonist.
It blocks both beta1- and beta2-adrenergic receptors. Timolol does not
have significant
intrinsic sympathomimetic activity, local anesthetic
(membrane-stabilizing) or direct
myocardial depressant activity.
Timolol, when applied topically in the eye, reduces normal and
elevated intraocular
pressure (IOP) whether or not accompanied by glaucoma. Elevated
intraocular pressure
is a major risk factor in the pathogenesis of glaucomatous visual
field loss. The higher
25
13
24
4
3
the level of IOP, the greater the likelihood of glaucomatous visual
field loss and optic
nerve damage. The predomina