Timolol

• Antihypertensive Agents
• Anti-Arrhythmia Agents
• Adrenergic beta-Antagonists
• ATC:C07AA06
• ATC:S01ED01

• Apo-Timol
• Apo-Timop
• Aquanil
• Betim
• Betimol
• Blocadren
• Istalol
• Novo-Timol
• Proflax
• Temserin
• Tenopt
• Tim-AK
• Timacar
• Timacor
• Timololum [INN-Latin]
• Timopic
• Timoptic
• Timoptic in Ocudose
• Timoptic-XE
• Timoptol

• Combigan (Brimonidine Tartrate + Timolol Maleate)
• Cosopt -(2%/0.5% Oph Dps) (Dorzolamide Hydrochloride + Timolol Maleate)
• Timolide Tab (Hydrochlorothiazide + Timolol Maleate)
• Timpilo 2 (Pilocarpine Hydrochloride + Timolol Maleate)
• Timpilo 4 (Pilocarpine Hydrochloride + Timolol Maleate)
• Xalacom (Latanoprost + Timolol Maleate)

C₁₃H₂₄N₄O₃S

http://www.rxlist.com/cgi/generic3/timololgfs.htm

Timolol FDA

Timolol MSDS

Wasson et al., J. Med. Chem. 15, 615 (1972)

316.421 g/mol

201.5-202.5 ^oC

2.74 mg/mL

Solid

1.761

Drops; Liquid; Solution; Solution (long-acting); Tablet

In its oral form it is used to treat high blood pressure and prevent heart attacks, and occasionally to prevent migraine headaches. In its opthalmic form it is used to treat open-angle and occasionally secondary glaucoma.

Similar to propranolol and nadolol, timolol is a non-selective, beta-adrenergic receptor antagonist. Timolol does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity, but does possess a relatively high degree of lipid solubility. Timolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage.

Bioavailability is about 60%

LD₅₀=1190 mg/kg (oral, mice), LD₅₀=900 mg/kg (oral, rat). Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.

Patients should be instructed to avoid allowing the tip of the dispensing container to contact the eye or surrounding structures. Patients should also be instructed that ocular solutions, if handled improperly, could become contaminated by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions.

Patients should also be advised that if they have ocular surgery or develop an intercurrent ocular condition (e.g.,trauma or infection), they should immediately seek their physicianís advice concerning the continued use of the present multidose container. Patients should be instructed to invert the closed container and shake once before each use. It is not necessary to shake the container more than once. Patients requiring concomitant topical ophthalmic medications should be instructed to administer these at least 10 minutes before instilling Timolol GFS. Patients with bronchial asthma, a history of bronchial asthma, severe chronic obstructive pulmonary disease, sinus bradycardia, second or third degree atrioventricular block, or cardiac failure should be advised not to take this product. Transient blurred vision or visual disturbance, generally lasting from 30 seconds to 5 minutes, following instillation may impair the ability to perform hazardous tasks such as operating machinery or driving a motor vehicle.

Humans and other mammals