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Timolol maleate is a non-selective beta-adrenergic receptor antagonist indicated for treating glaucoma, heart attacks and hypertension.

Uses[edit]

In its oral form (Blocadren), it is used:

to treat high blood pressure
to prevent heart attacks
to prevent migraine headaches^[1]

In its ophthalmic form (brand names Timoptol in Italy; Timoptic), it is used to treat open-angle and occasionally secondary glaucoma by reducing aqueous humour production through blockage of the beta receptors on the ciliary epithelium. The pharmacological mechanism by which it actually does this is still unknown. First beta-blocker approved for topical use in treatment of glaucoma in the USA (1978). With monotherapy, depresses IOP 18-34% below baseline within first few treatments. However, there are short-term escape and long-term drift effects in some patients. That is, tolerance develops. May reduce extent of diurnal IOP curve up to 50%. IOP higher during sleep. 5-10x more potent beta-blocker than propranolol. Light sensitive; preserved with 0.01% benzalkonium Cl (and also comes BAC free). Can also be used in adjunctive therapy with pilocarpine or CAIs.

Side effects[edit]

The most serious possible side effects include cardiac arrhythmias and severe bronchospasms. Timolol can also lead to fainting, congestive heart failure, depression, confusion, worsening of Raynaud's syndrome and impotence.

Usual dosage[edit]

Children and Adults: Ophthalmic: Initial: 0.25% solution, instill 1 drop twice daily; increase to 0.5% solution if response not adequate; decrease to 1 drop/day if *controlled; do not exceed 2 drops twice daily of 0.5% solution Adults: Oral:
Hypertension: Initial: 10 mg twice daily, increase gradually every 14 days, usual dosage: 20–40 mg/day in 2 divided doses; maximum: 60 mg/day
Prevention of myocardial infarction: 10 mg twice daily initiated within 1–6 weeks after infarction
Migraine headache: Initial: 10 mg twice daily, increase to maximum of 30 mg/day

Formulations[edit]

Gel-forming solution, ophthalmic, as maleate (Timoptic-XE): 0.25% (2.5 mL, 5 mL); 0.5% (2.5 mL, 5 mL)
Solution, ophthalmic, as hemihydrate (Betimol): 0.25% (5 mL, 10 mL, 15 mL); 0.5% (5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]
Solution, ophthalmic, as maleate: 0.25% (5 mL, 10 mL, 15 mL); 0.5% (5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]
Timoptic: 0.25% (5 mL, 10 mL); 0.5% (5 mL, 10 mL) [contains benzalkonium chloride]
Solution, ophthalmic, as maleate [preservative free] (Timoptic OcuDose): 0.25% (0.2 mL);0.5% (0.2 mL) [single use]
Tablet, as maleate (Blocadren): 5 mg, 10 mg, 20 mg

For ophthalmic use, timolol is also available combined with other medications:

Combigan - timolol and brimonidine
IOTIM-B - timolol and brimonidine
Cosopt - timolol maleate and dorzolamide hydrochloride
DuoTrav - timolol and travoprost
XOalacom (Pfizer) - timolol and latanoprost

Brand names[edit]

In Canada: Apo-Timol, Apo-Timop, Gen-Timolol, Nu-Timolol, Phoxal-timolol, PMS-Timolol, Tim-AK, Timoptic, Timoptic-XE.
In the United States: Betimol, Blocadren, Istalol, Timoptic, Timoptic-XE, Timoptic OcuDose.
In Jordan:Apimol ( By API )^[2]
IOTIM is No. 1 prescribed brand in INDIA from FDC LIMITED .

Chemical synthesis[edit]

References[edit]

^ Dawn A. Marcus; Philip A. Bain (27 February 2009). Effective Migraine Treatment in Pregnant and Lactating Women: A Practical Guide. シュプリンガー・ジャパン株式会社. pp. 141–. ISBN 978-1-60327-438-8. Retrieved 14 November 2010.
^ http://www.jfda.jo/

External links[edit]

http://dx.doi.org/10.1021/jo00881a011

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 幼児血管腫のマネージメント management of infantile hemangiomas
2. 閉塞隅角緑内障 angle closure glaucoma
3. 開放隅角緑内障：治療 open angle glaucoma treatment
4. 成人における片頭痛の予防的治療 preventive treatment of migraine in adults
5. 慢性片頭痛 chronic migraine

English Journal

Evaluation of aqueous humor concentrations of Istalol and Betimol following a single ocular instillation in rabbit eyes.

Baklayan GA, Collins EC, Thetford T, Soriano A, Song CK, Han J.SourceISTA Pharmaceuticals, Inc., Irvine, CA, USA. gbaklayan@istavision.com
Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics.J Ocul Pharmacol Ther.2008 Oct;24(5):507-12. doi: 10.1089/jop.2007.0131.
PURPOSE: The aim of this study was to evaluate the pharmacokinetic absorption profiles of two commercially available ophthalmic solutions following a single instillation into each eye of New Zealand white rabbit eyes.METHODS: A single dose of either timolol maleate with potassium sorbate (TLA) or ti
PMID 18800867

Medical therapy cost considerations for glaucoma.

Fiscella RG, Green A, Patuszynski DH, Wilensky J.SourceDepartment of Pharmacy Practice, University of Illinois at Chicago, Illinois 60612, USA. Fisc@UIC.EDU
American journal of ophthalmology.Am J Ophthalmol.2003 Jul;136(1):18-25.
PURPOSE: To determine the calculated daily patient cost (cost minimization) of medical glaucoma therapy and review cost trends.DESIGN: Experimental, controlled, prospective study.METHODS: The actual volume of various glaucoma medications or glaucoma medications with redesigned bottles was determined
PMID 12834665

Efficacy and safety of timolol solution once daily vs timolol gel added to latanoprost.

Stewart WC, Day DG, Sharpe ED, Dubiner HB, Holmes KT, Stewart JA.SourcePharmaceutical Research Corporation, Charleston, South Carolina 29412-2464, USA. pharm@quik.com
American journal of ophthalmology.Am J Ophthalmol.1999 Dec;128(6):692-6.
PURPOSE: To compare the efficacy and safety of timolol hemihydrate 0.5% (Betimol, Ciba Vision Ophthalmics, Duluth, Georgia) vs timolol maleate gel-forming solution 0.5% (Timoptic-XE, Merck, Blue Bell, Pennsylvania), both given every morning added to latanoprost 0.005% given every evening.METHODS: A
PMID 10612504

Related Pictures

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★リンクテーブル★

リンク元

「チモロール」

Timolol
Systematic (IUPAC) name
	(S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
Clinical data
Trade names	Timoptic
AHFS/Drugs.com	monograph
MedlinePlus	a602022
Pregnancy cat.	C (AU) C (US)
Legal status	℞ Prescription only
Routes	oral, Ophthalmic
Pharmacokinetic data
Bioavailability	60%
Metabolism	Hepatic: 80%
Half-life	2.5-5 hours
Excretion	Renal
Identifiers
CAS number	26839-75-8
ATC code	C07AA06 S01ED01
PubChem	CID 33624
IUPHAR ligand	565
DrugBank	DB00373
ChemSpider	31013
UNII	5JKY92S7BR
KEGG	D08600
ChEBI	CHEBI:9599
ChEMBL	CHEMBL499
Chemical data
Formula	C13H24N4O3S
Mol. mass	316.421 g/mol
	SMILES O[C@H](COc1nsnc1N2CCOCC2)CNC(C)(C)C;
	InChI InChI=1S/C13H24N4O3S/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17/h10,14,18H,4-9H2,1-3H3/t10-/m0/s1 ; Key:BLJRIMJGRPQVNF-JTQLQIEISA-N ;
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　　[★]

英: timolol
化: マレイン酸チモロール timolol maleate
商: ブロカドレン BLOCARDEN、チマバック、Timoptic、Betimol; コソプト、ザラカム、チアブート、チモプトール、チモレート、デュオトラバ、ファルチモ、リズモン
関: 眼科用剤

β受容体遮断薬(競合阻害)

薬効薬理

チマバック点眼液0.5％

眼圧下降作用：チマバック点眼液0.5％は，家兎の正常眼圧を用いた試験系において，眼圧下降効果が認められた1）．また，家兎の実験的高眼圧モデルに対しても，眼圧上昇抑制及び下降効果が認められた1）．

チモプトールＸＥ点眼液０．２５％／チモプトールＸＥ点眼液０．５％

1. 眼圧下降作用

ウサギにおけるα-キモトリプシン惹起高眼圧及び水負荷による眼圧上昇試験において、チモロールマレイン酸塩の点眼は有意に眼圧上昇を抑制することが認められている。9)

2. β-受容体遮断作用

ラット、イヌ、ネコにチモロールマレイン酸塩を全身投与した場合、イソプレナリンにより惹起された心拍数、心筋収縮力及び心拍出量の増加は著明に抑制され、本剤のβ-受容体遮断作用はピンドロールと同程度、プロプラノロールより数倍強力である。10)、11) また、チモロールマレイン酸塩は有意の内因性交感神経刺激作用、直接心筋抑制作用、局所麻酔作用を示さない。10)、11)

作用機序