Timolol
- Atc Codes:C07AA06#S01ED01
- CAS Codes:91524-16-2#26921-17-5
- PHARMGKB ID:91524-16-2#26921-17-5
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Betimol; Belgium: Geltim, Nyogel, Nyolol, Timabak, Timolol, Timo-Pos, Timoptol; Bulgaria: Arutimol, Cusimolol, Nyolol, Timolol, Unitimolol; Cyprus: Nyolol, Timolol; Czech Republic: Arutimol, Timo-Comod, Timohexal, Timolol, Timoptol; Denmark: Optimol, Timacar, Timosan; Estonia: Arutimol, Nyolol, Timolol, Timosan; Finland: Blocanol, Timolol, Timosan; France: Digaol, Gaoptol, Geltim, Nyogel, Nyolol, Ophtim, Timabak, Timacor, Timocomod, Timoptol; Germany: Arutimol, Chibro-Timoptol, Dispatim, Glautim, Nyogel, Timo EDO, Timo-COMOD, Timogel, Timohexal, Timolol, Timomann, Tim-Ophtal, Timo-Stulln; Greece: Lithimole, Matorane, Noval, Nyogel, Nyolol, Temserin, Timolol, Waucosin, Yesan; Hungary: Arutimol, Cusimolol, Timolol; Ireland: Nyogel, Timolol, Timoptol; Italy: Blocadren, Cusimolol, Droptimol, Ialutim, Nyogel, Oftimolo, Timod, Timololo, Timoptol; Latvia: Arutimol, Nyolol, Timolol, Timosan, Unitimolol; Lithuania: Arutimol, Nyolol, Tim-Alcon, Timolol, Timosan; Netherlands: Nyogel, Timo-Comod, Timogel, Timolol, Timoptol; Poland: Cusimolol, Nyolol, Oftensin, Timo-Comod, Timohexal, Timolol, Timoptic; Portugal: Nyogel, Nyolol, Timabak, Timogel, Timoglau, Timolen, Timoptol; Romania: Nyolol, Timabak, Timo-Comod, Timo-Gal, Timolol, Timoptic, Unitimolol; Slovakia: Nyolol, Timolol, Unitimolol; Slovenia: Nyolol, Timoptic; Spain: Cusimolol, Timabak, Timoftol, Timogel, Timolol; Sweden: Blocadren, Optimol, Timolol, Timosan, Xalcom; UK: Betim, Nyogel, Timoptol.
North America
Canada: Apo-Timol, Apo-Timop, Tim-AK, Timolol, Timoptic; USA: Betimol, Istalol, Timolol, Timoptic.
Latin America
Argentina: Atiglauc, Glatim, Klonalol, Ofal, Plostim, Poentimol, Proflax, Protevis, Timed, Timolol, Timolpres, Timoptic, Zopirol; Brazil: Glaucotrat, Glautimol, Nyolol, Tenoftal, Timabak, Timolol, Timoptol; Mexico: Blocadren, Horex, Imot Ofteno, Jertz, Nyolol, Shemol, Tenglamol, Timoptol, Timozzard.
Asia
Japan: Phartimo, Rysmon, Thiaboot, Timaback, Timoleate, Timolol, Timoptol.
Drug combinations
Timolol and Bendroflumethiazide
Timolol and Bimatoprost
Timolol and Brimonidine
Timolol and Brinzolamide
Timolol and Dorzolamide
Timolol and Latanoprost
Timolol and Pilocarpine
Timolol and Travoprost
Timolol, Amiloride, and Hydrochlorothiazide
Chemistry
Timolol: C~13~H~24~N~4~O~3~S ½H~2~O. Mw: 325.43. (1) 2-Propanol, 1-[(1,1-dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-, hemihydrate, (S)-; (2)(S)-1-(tert-Butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy]-2-propanol hemihydrate. CAS-91524-16-2 (1985).
Timolol Maleate: C~13~H~24~N~4~O~3~S C~4~H~4~O~4~. Mw: 432.49. (1) 2-Propanol, 1-[(1,1-dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-, (S)-, (Z)-2-butenedioate (1:1); (2)(-)-1-(tert-Butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy]-2-propanol maleate (1:1). CAS-26921-17-5 (1973).
Pharmacologic Category
Antiglaucoma Agents; β-Adrenergic Blocking Agents. Cardiovascular Drugs; β-Adrenergic Blocking Agents. (ATC-Code: C07AA06; S01ED01).
Mechanism of action
Blocks both β~1~- and β~2~-adrenergic receptors, reduces intraocular pressure by reducing aqueous humor production or possibly outflow. Reduces blood pressure by blocking adrenergic receptors and decreasing sympathetic outflow, produces negative chronotropic and inotropic activity through unknown mechanism.
Therapeutic use
Treatment of elevated intraocular pressure such as glaucoma or ocular hypertension. Treatment of hypertension and angina, to reduce mortality following myocardial infarction. Prophylaxis of migraine.
Pregnancy and lactiation implications
β-Blockers associated with bradycardia, hypotension, hypoglycemia, intrauterine growth rate. Available evidence suggests β-blockers generally safe during pregnancy. Cases of neonatal hypoglycemia reported following maternal use of β-blockers at parturition or during breast-feeding. Bradycardia and arrhythmia reported in an infant following ophthalmic administration of timolol during pregnancy. Enters breast milk (use with caution in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to timolol or any component of the formulation. Sinus bradycardia. Sinus node dysfunction. Heart block greater than first-degree (except in patients with functioning artificial pacemaker). Cardiogenic shock. Uncompensated cardiac failure. Bronchospastic disease. Pregnancy (2^nd^ and 3^rd^ trimesters).
Warnings and precautions
Use caution with history of severe anaphylaxis to allergens (patients taking β-blockers may become more sensitive to repeated challenges). Treatment of anaphylaxis (e.g. epinephrine) in patients taking β-blockers may be ineffective or promote undesirable effects. In general, patients with bronchospastic disease should not receive β-blockers. Consider pre-existing conditions such as sick sinus syndrome before initiating. Use with caution in diabetes mellitus (may potentiate hypoglycemia and/or mask signs and symptoms), in compensated heart failure, in myasthenia gravis (can worsen), in PVD (including Raynaud’s), and in pheochromocytoma (untreated). Use with caution in history of psychiatric illness (may cause or exacerbate CNS depression), in severe renal impairment (marked hypotension can occur in patients maintained on hemodialysis), in patients receiving anesthetic agents which decrease myocardial function, in patients on concurrent verapamil or diltiazem (bradycardia or heart block can occur). Some products contain benzalkonium chloride (may be absorbed by soft contact lenses). Systemic absorption and adverse effects may occur in ophthalmic administration, including bradycardia and/or hypotension. Should not be used alone in angle-closure glaucoma (has no effect on pupillary constriction). Multidose vials associated with development of bacterial keratitis. β-Blocker therapy should not be withdrawn abruptly (particularly in CAD).