SandboxAlonso: Difference between revisions

Jump to navigation Jump to search
VisualWikitext
No edit summary
No edit summary
Line 1: Line 1:
{{Timolol}}
{{Drugbox
| verifiedrevid = 457286138
| IUPAC_name = (''S'')-1-(''tert''-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
| image = Timol01.jpg
| image2 =Timolol02.png
<!--Clinical data-->
| tradename = Timoptic
| Drugs.com = {{drugs.com|monograph|timolol-eent}}
| MedlinePlus = a602022
| pregnancy_AU = C
| pregnancy_US = C
| legal_status = Rx-only
| routes_of_administration = oral, [[human eye|Ophthalmic]]
<!--Pharmacokinetic data-->
| bioavailability = 60%
| metabolism = [[Liver|Hepatic]]: 80%
| elimination_half-life = 2.5-5 hours
| excretion = [[Kidney|Renal]]
<!--Identifiers-->
| CASNo_Ref = {{cascite|correct|CAS}}
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 26839-75-8
| ATC_prefix = C07
| ATC_suffix = AA06
| ATC_supplemental = {{ATC|S01|ED01}}
| PubChem = 33624
| IUPHAR_ligand = 565
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00373
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 31013
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 5JKY92S7BR
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D08600
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 9599
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 499
<!--Chemical data-->
| C=13 | H=24 | N=4 | O=3 | S=1
| molecular_weight = 316.421 g/mol
| smiles = O[C@H](COc1nsnc1N2CCOCC2)CNC(C)(C)C
| InChI = 1/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
| InChIKey = BLJRIMJGRPQVNF-JTQLQIEIBV
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = BLJRIMJGRPQVNF-JTQLQIEISA-N
}}
__NOTOC__
__NOTOC__
{{Penbutolol}}
{{CMG}}
{{CMG}}; {{AE}} {{SS}}


'''''For patient information about Penbutolol, click [[Penbutolol (patient information)|here]]'''''
'''''For patient information about Timolol Tablet, click [[Timolol Oral (patient information)|here]].'''''


{{SB}} LEVATOL<sup>®</sup>
'''''For patient information about Timolol Drop/Solution, click [[Timolol Ophthalmic (patient information)|here]].'''''
 
{{SB}} Betimol, Blocadren, Istalol, Timoptic, Timoptic-XE, Timoptic OcuDose


==Overview==
==Overview==


'''Penbutolol''' ('''Levatol''', '''Levatolol''', '''Lobeta''', '''Paginol''', '''Hostabloc''', '''Betapressin''') is a [[medication]] in the class of [[beta blocker]]s, used in the treatment of [[hypertension|high blood pressure]]. Penbutolol is able to bind to both beta-1 adrenergic receptors and [[beta-2 adrenergic receptors]] (the two subtypes), thus making it a non-selective β blocker [1]. Penbutolol is a [[sympathomimetic drug]] with properties allowing it to act as a partial agonist at β adrenergic receptors [2]. Penbutolol has also been found to be one of very few compounds that are 5-HT1A antagonists. 5-HT1A receptors are activated by [[serotonin]], which have many different actions in different species. This makes it difficult to create generalizations about serotonin and its effects [1].
'''Timolol maleate''' is a non-selective [[beta blocker|beta-adrenergic receptor antagonist]] indicated for treating [[glaucoma]], [[myocardial infarction|heart attacks]] and [[hypertension]].


==Category==
==Category==
Cardiovascular Drugs:Beta blockers
 
Beta-blockers


==FDA Package Insert==
==FDA Package Insert==


'''| [[Penbutolol indications and usage|Indications and Usage]]'''
====TIMOLOL MALEATE tablet====
'''| [[Penbutolol dosage and administration|Dosage and Administration]]'''
 
'''| [[Penbutolol contraindications|Contraindications]]'''
''' [[Timolol tablet indications and usage|Indications and Usage]]'''
'''| [[Penbutolol warnings and precautions|Warnings and Precautions]]'''
'''| [[Timolol tablet dosage and administration|Dosage and Administration]]'''
'''| [[Penbutolol adverse reactions|Adverse Reactions]]'''
'''| [[Timolol tablet contraindications|Contraindications]]'''
'''| [[Penbutolol drug interactions|Drug Interactions]]'''
'''| [[Timolol tablet warnings and precautions|Warnings and Precautions]]'''
'''| [[Penbutolol use in specific populations|Use in Specific Populations]]'''
'''| [[Timolol tablet adverse reactions|Adverse Reactions]]'''
'''| [[Penbutolol overdosage|Overdosage]]'''
'''| [[Timolol tablet drug interactions|Drug Interactions]]'''
'''| [[Penbutolol description|Description]]'''
'''| [[Timolol tablet use in specific populations|Use in Specific Populations]]'''
'''| [[Penbutolol clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Timolol tablet overdosage|Overdosage]]'''
'''| [[Penbutolol nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Timolol tablet description|Description]]'''
'''| [[Penbutolol how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Timolol tablet clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Penbutolol patient counseling information|Patient Counseling Information]]'''
'''| [[Timolol tablet how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Penbutolol labels and packages|Labels and Packages]]'''
'''| [[Timolol tablet labels and packages|Labels and Packages]]'''
 
{|
| [[File:Ti01.png|800px|thumb]]
|}
 
==Uses==
 
In its oral form ('''Blocadren'''), it is used:
* to treat [[hypertension|high blood pressure]]
* to prevent [[myocardial infarction|heart attack]]s
* to prevent [[migraine]] headaches<ref name="MarcusBain2009">{{cite book|author1=Dawn A. Marcus|author2=Philip A. Bain|title=Effective Migraine Treatment in Pregnant and Lactating Women: A Practical Guide|url=http://books.google.com/books?id=Z5YWpjj89NEC&pg=PA141|accessdate=14 November 2010|date=27 February 2009|publisher=シュプリンガー・ジャパン株式会社|isbn=978-1-60327-438-8|pages=141–}}</ref>
 
In its [[human 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 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 [[Intraocular pressure|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 [[arrhythmia]]s and severe [[bronchospasm]]s. Timolol can also lead to [[Syncope (medicine)|fainting]], [[congestive heart failure]], [[clinical depression|depression]], [[confusion]], worsening of [[Raynaud's syndrome]] 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 2 drops twice daily of 0.5% solution Adults: Oral:
*Hypertension: Initial: 10&nbsp;mg twice daily, increase gradually every 14 days, usual dosage: 20–40&nbsp;mg/day in 2 divided doses; maximum: 60&nbsp;mg/day
*Prevention of myocardial infarction: 10&nbsp;mg twice daily initiated within 1–6 weeks after infarction
*Migraine headache: Initial: 10&nbsp;mg twice daily, increase to maximum of 30&nbsp;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&nbsp;mg, 10&nbsp;mg, 20&nbsp;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|dorzolamide hydrochloride]]
*[[Alcon#Glaucoma|DuoTrav]] - timolol and [[travoprost]]
*XOalacom (Pfizer) - timolol and latanoprost
 
==Brand names==
 
* 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.
* IOTIM is No. 1 prescribed brand in INDIA from FDC LIMITED.
 
==Chemical synthesis==
 
{|
| [[File:Timolol03.png|800px|thumb]]
|}


==Mechanism of Action==
==Mechanism of Action==
Penbutolol decreases plasma renin activity in normal subjects and in patients with essential and renovascular hypertension. The mechanisms of the antihypertensive actions of ß-receptor antagonists have not been established. However, factors that may be involved are: (1) competitive antagonism of [[catecholamine]]s at peripheral adrenergic receptor sites (especially cardiac) that leads to decreased cardiac output; (2) a central nervous system (CNS) action that results in a decrease in tonic sympathetic neural outflow to the periphery; and (3) a reduction of renin secretion through blockade of ß-receptors involved in release of renin from the kidneys.
 
Timolol maleate is a beta1 and beta2 (nonselective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic activity.


==References==
==References==
{{Reflist|2}}


{{Reflist|2}}
{{Beta blockers}}
{{Antiglaucoma preparations and miotics}}


[[Category:Beta blockers]]
[[Category:Morpholines]]
[[Category:Cardiovascular Drugs]]
[[Category:Cardiovascular Drugs]]
[[Category:Antimigraine drugs]]
[[Category:Drugs]]
[[Category:Drugs]]

Revision as of 13:03, 14 July 2014

Timolol
TIMOLOL MALEATE® FDA Package Insert
Indications and Usage
Dosage and Administration
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
How Supplied/Storage and Handling
Labels and Packages
Clinical Trials on Timolol
ClinicalTrials.gov
SandboxAlonso
Clinical data
Trade namesTimoptic
AHFS/Drugs.comMonograph
MedlinePlusa602022
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Routes of
administration		oral, Ophthalmic
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability60%
MetabolismHepatic: 80%
Elimination half-life2.5-5 hours
ExcretionRenal
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC13H24N4O3S
Molar mass316.421 g/mol
3D model (JSmol)
  (verify)

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

For patient information about Timolol Tablet, click here.

For patient information about Timolol Drop/Solution, click here.

Synonyms / Brand Names: Betimol, Blocadren, Istalol, Timoptic, Timoptic-XE, Timoptic OcuDose

Overview

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

Category

Beta-blockers

FDA Package Insert

TIMOLOL MALEATE tablet

Indications and Usage | Dosage and Administration | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | How Supplied/Storage and Handling | Labels and Packages

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

  • 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

  • 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:

Brand names

  • 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.
  • IOTIM is No. 1 prescribed brand in INDIA from FDC LIMITED.

Chemical synthesis

Mechanism of Action

Timolol maleate is a beta1 and beta2 (nonselective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic activity.

References

  1. ↑ 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.

Template:Antiglaucoma preparations and miotics

Retrieved from "https://www.wikidoc.org/index.php?title=SandboxAlonso&oldid=993433"