Timolol
 | |
|---|---|
| Systematic (IUPAC) name | |
| (S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol | |
| Identifiers | |
| CAS number | 26839-75-8 |
| ATC code | C07AA06 |
| PubChem | CID 33624 |
| IUPHAR ligand | 565 |
| DrugBank | APRD00229 |
| ChemSpider | 31013 |
| UNII | 5JKY92S7BR |
| KEGG | D08600 |
| ChEMBL | CHEMBL499 |
| Chemical data | |
| Formula | C13H24N4O3S |
| Mol. mass | 316.421 g/mol |
| SMILES | eMolecules & PubChem |
| Pharmacokinetic data | |
| Bioavailability | 60% |
| Metabolism | Hepatic: 80% |
| Half-life | 2.5-5 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | C(AU) C(US) |
| Legal status | ℞ Prescription only |
| Routes | oral, Ophthalmic |
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Timolol maleate is a non-selective beta-adrenergic receptor blocker.
Uses
In its oral form (Blocadren), it is used:
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
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
Formulations
For ophthalmic use, timolol is also available combined with other medications:
Brand names
Chemical synthesis
References
External links
Retrieved from : http://en.wikipedia.org/wiki/Timolol
