Timolol detailed information: Difference between revisions

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Redirected page to Timolol#Pharmacology
 
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{{drugbox |
#REDIRECT [[Timolol#Pharmacology]]
| IUPAC_name = (''S'')-1-(''tert''-butylamino)-<br />3-(4-morpholino-1,2,5-thiadiazol-3-yloxy)propan-2-ol
| CAS_number = 26839-75-8
| ATC_prefix=C07
| ATC_suffix=AA06
| PubChem=5478
| DrugBank=APRD00229
| C=13 | H=24 | N=4 | O=3 | S=1
| molecular_weight = 316.421 g/mol
| bioavailability = 60%
| metabolism = [[Liver|Hepatic]]: 80%
| elimination_half-life = 2.5-5 hours
| excretion = [[Kidney|Renal]]
| pregnancy_AU = C
| pregnancy_US = C
| pregnancy_category =
| legal_status = Rx-only
| routes_of_administration = oral, [[Eye|Ophthalmic]]
}}
{{CMG}}
 
 
 
'''Timolol maleate'''  is a non-selective [[beta blocker|beta-adrenergic receptor blocker]]. In its oral form ('''Blocadren'''), it is used to treat [[hypertension|high blood pressure]] and prevent [[myocardial infarction|heart attack]]s, and occasionally to prevent [[migraine]] headaches.  In its [[eye|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 blockade of the beta receptors on the ciliary epithelium.
 
==Side effects==
The most serious possible side effects include cardiac [[arrhythmia]]s and severe [[bronchospasm]]s. Timolol can also lead to [[syncope|fainting]], [[congestive heart failure]], [[clinical depression|depression]], [[confusion]], and [[impotence]].
 
==Usual dosage==
*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 1 drop twice daily of 0.5% solution Adults: Oral:
*Hypertension: Initial: 10 mg twice daily, increase gradually every 7 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 1-4 weeks after infarction
*Migraine headache: Initial: 10 mg twice daily, increase to maximum of 30 mg/day
 
==Formulations==
*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 opthalmic use, timolol is also available combined with other medications:
*[[Cosopt]] - timolol maleate and [[Dorzolamide|dorzolamide hydrochloride]]
*[[Alcon#Glaucoma|DuoTrav]] - timolol and [[travoprost]]
 
==Brand names==
*In Canada: Apo-Timol, Apo-Timop, Gen-Timolol, Nu-Timolol, Phoxal-timolol, PMS-Timolol, Tim-AK, Timoptic, Timoptic-XE.
*In United States: Betimol, Blocadren, Istalol, Timoptic, Timoptic-XE, Timoptic OcuDose.
 
{{beta blockers}}
{{Antiglaucoma preparations and miotics}}
 
[[Category:Beta blockers]]
[[Category:Morpholines]]
[[Category:Drugs]]
 
[[de:Timolol]]
[[ru:Тимолол]]
 
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Latest revision as of 00:02, 22 July 2014