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{{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__
{{CMG}}
{{Amlodipine}}
{{CMG}}; {{AE}}


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


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


==Overview==
==Overview==
 
'''Amlodipine''' ('''Norvasc''' (Pfizer) and generics)  (as [[besylate]], [[mesylate]] or [[maleate]]) is a long-acting [[dihydropyridine]]-type (DHP) [[calcium channel blocker]] used [[antihypertensive|to lower blood pressure]] and to treat [[angina pectoris|anginal chest pain]]. Like other calcium channel blockers, amlodipine lowers blood pressure by relaxing [[Artery|arterial]] [[smooth muscle]]s, which decreases [[total peripheral resistance]] and therefore reduces [[blood pressure]]. In angina, amlodipine increases blood flow to the [[Cardiac muscle|heart muscle]] (although DHP-class calcium channel blockers are more selective for arteries than the muscular tissue of the heart (myocardium), as the calcium ion channels of the heart are not of the dihydropyridine-type).
'''Timolol maleate''' is a non-selective [[beta blocker|beta-adrenergic receptor antagonist]] indicated for treating [[glaucoma]], [[myocardial infarction|heart attacks]] and [[hypertension]].
 
==Category==
==Category==
 
[[Dihydropyridine]] [[calium channel blocker]].
Beta-blockers
 
==FDA Package Insert==
==FDA Package Insert==


====TIMOLOL MALEATE tablet====
===Norvasc<sup>®</sup>===


'''  [[Timolol tablet indications and usage|Indications and Usage]]'''
'''| [[Timolol tablet dosage and administration|Dosage and Administration]]'''
'''| [[Timolol tablet contraindications|Contraindications]]'''
'''| [[Timolol tablet warnings and precautions|Warnings and Precautions]]'''
'''| [[Timolol tablet adverse reactions|Adverse Reactions]]'''
'''| [[Timolol tablet drug interactions|Drug Interactions]]'''
'''| [[Timolol tablet use in specific populations|Use in Specific Populations]]'''
'''| [[Timolol tablet overdosage|Overdosage]]'''
'''| [[Timolol tablet description|Description]]'''
'''| [[Timolol tablet clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Timolol tablet how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Timolol tablet labels and packages|Labels and Packages]]'''


{|
'''  [[Amlodipine indications and usage|Indications and Usage]]'''
| [[File:Ti01.png|800px|thumb]]
'''| [[Amlodipine dosage and administration|Dosage and Administration]]'''
|}
'''| [[Amlodipine dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[Amlodipine contraindications|Contraindications]]'''
'''| [[Amlodipine warnings and precautions|Warnings and Precautions]]'''
'''| [[Amlodipine adverse reactions|Adverse Reactions]]'''
'''| [[Amlodipine drug interactions|Drug Interactions]]'''
'''| [[Amlodipine use in specific populations|Use in Specific Populations]]'''
'''| [[Amlodipine overdosage|Overdosage]]'''
'''| [[Amlodipine description|Description]]'''
'''| [[Amlodipine clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Amlodipine nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Amlodipine clinical studies|Clinical Studies]]'''
'''| [[Amlodipine how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Amlodipine patient counseling information|Patient Counseling Information]]'''
'''| [[Amlodipine labels and packages|Labels and Packages]]'''


==Uses==
===Pill Images===
{{TempDrugImages}}
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{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_07812272.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=07812272|drugAuthor=Sandoz Inc|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=S;SANDOZ;572|dosageValue=10|dosageUnit=mg|pillColor=Brown|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_07812273.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=07812273|drugAuthor=Sandoz Inc|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=S;SANDOZ;573|dosageValue=5|dosageUnit=mg|pillColor=Pink|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_07812273.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=07812273|drugAuthor=Sandoz Inc|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=S;SANDOZ;573|dosageValue=20|dosageUnit=mg|pillColor=Pink|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_07812274.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=07812274|drugAuthor=Sandoz Inc|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=S;SANDOZ;574|dosageValue=10|dosageUnit=mg|pillColor=Purple|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_07812274.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=07812274|drugAuthor=Sandoz Inc|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=S;SANDOZ;574|dosageValue=20|dosageUnit=mg|pillColor=Purple|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_551110339.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=551110339|drugAuthor=Dr.Reddy's Laboratories Limited|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=RDY;339|dosageValue=5|dosageUnit=mg|pillColor=Grey;Yellow|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_551110339.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=551110339|drugAuthor=Dr.Reddy's Laboratories Limited|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=RDY;339|dosageValue=10|dosageUnit=mg|pillColor=Grey;Yellow|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_551110340.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=551110340|drugAuthor=Dr.Reddy's Laboratories Limited|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=RDY;340|dosageValue=5|dosageUnit=mg|pillColor=Grey;Orange|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_and_Benazepril_Hydrochloride_NDC_551110340.jpg|drugName=Amlodipine Besylate and Benazepril Hydrochloride|NDC=551110340|drugAuthor=Dr.Reddy's Laboratories Limited|ingredients=AMLODIPINE BESYLATE[AMLODIPINE];BENAZEPRIL HYDROCHLORIDE[BENAZEPRILAT]|pillImprint=RDY;340|dosageValue=20|dosageUnit=mg|pillColor=Grey;Orange|pillShape=Capsule|pillSize=19|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_00930083.jpg|drugName=Amlodipine Besylate|NDC=00930083|drugAuthor=Teva Pharmaceuticals USA Inc|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=93;83|dosageValue=2.5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=7|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_00937167.jpg|drugName=Amlodipine Besylate|NDC=00937167|drugAuthor=Teva Pharmaceuticals USA Inc|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=93;7167|dosageValue=5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=8|pillScore=1}}
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{{PillImage|fileName=Amlodipine_Besylate_NDC_03785208.jpg|drugName=Amlodipine Besylate|NDC=03785208|drugAuthor=Mylan Pharmaceuticals Inc.|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=M;A8|dosageValue=2.5|dosageUnit=mg|pillColor=Blue|pillShape=Round|pillSize=6|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_03785209.jpg|drugName=Amlodipine Besylate|NDC=03785209|drugAuthor=Mylan Pharmaceuticals Inc.|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=M;A9|dosageValue=5|dosageUnit=mg|pillColor=Blue|pillShape=Round|pillSize=8|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_03785210.jpg|drugName=Amlodipine Besylate|NDC=03785210|drugAuthor=Mylan Pharmaceuticals Inc.|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=M;A10|dosageValue=10|dosageUnit=mg|pillColor=Blue|pillShape=Round|pillSize=10|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_06032108.jpg|drugName=Amlodipine Besylate|NDC=06032108|drugAuthor=Qualitest Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=2108;V|dosageValue=2.5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=6|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_06032109.jpg|drugName=Amlodipine Besylate|NDC=06032109|drugAuthor=Qualitest Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=2109;V|dosageValue=5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=8|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_06032110.jpg|drugName=Amlodipine Besylate|NDC=06032110|drugAuthor=Qualitest Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=2110;V|dosageValue=10|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=10|pillScore=1}}
{{PillImage|fileName=amlodipine_besylate_NDC_08320043.jpg|drugName=amlodipine besylate|NDC=08320043|drugAuthor=Upsher-Smith Laboratories, Inc.|ingredients=amlodipine besylate[amlodipine]|pillImprint=ALP;5;832|dosageValue=5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=8|pillScore=1}}
{{PillImage|fileName=amlodipine_besylate_NDC_08320044.jpg|drugName=amlodipine besylate|NDC=08320044|drugAuthor=Upsher-Smith Laboratories, Inc.|ingredients=amlodipine besylate[amlodipine]|pillImprint=ALP;10;832|dosageValue=10|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=11|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_09046188.jpg|drugName=Amlodipine Besylate|NDC=09046188|drugAuthor=Major Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=IP;6|dosageValue=2.5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=6|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_317220237.jpg|drugName=Amlodipine Besylate|NDC=317220237|drugAuthor=Camber Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=237;IG|dosageValue=2.5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=6|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_317220238.jpg|drugName=Amlodipine Besylate|NDC=317220238|drugAuthor=Camber Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=238;IG|dosageValue=5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=8|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_317220239.jpg|drugName=Amlodipine Besylate|NDC=317220239|drugAuthor=Camber Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=239;IG|dosageValue=10|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=10|pillScore=1}}
{{PillImage|fileName=amlodipine_besylate_NDC_597621520.jpg|drugName=amlodipine besylate|NDC=597621520|drugAuthor=Greenstone LLC|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=G;1520;2;5|dosageValue=2.5|dosageUnit=mg|pillColor=White|pillShape=Clover|pillSize=7|pillScore=1}}
{{PillImage|fileName=amlodipine_besylate_NDC_597621530.jpg|drugName=amlodipine besylate|NDC=597621530|drugAuthor=Greenstone LLC|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=G;1530;5|dosageValue=5|dosageUnit=mg|pillColor=White|pillShape=Octagon|pillSize=9|pillScore=1}}
{{PillImage|fileName=amlodipine_besylate_NDC_597621540.jpg|drugName=amlodipine besylate|NDC=597621540|drugAuthor=Greenstone LLC|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=G;1540;10|dosageValue=10|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=10|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_605050194.jpg|drugName=Amlodipine Besylate|NDC=605050194|drugAuthor=Apotex Corp.|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=APO;AML;5|dosageValue=5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=6|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_605050195.jpg|drugName=Amlodipine Besylate|NDC=605050195|drugAuthor=Apotex Corp.|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=APO;AML;10|dosageValue=10|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=8|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_651620006.jpg|drugName=Amlodipine Besylate|NDC=651620006|drugAuthor=Amneal Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=IP;6|dosageValue=2.5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=6|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_651620008.jpg|drugName=Amlodipine Besylate|NDC=651620008|drugAuthor=Amneal Pharmaceuticals|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=IP;8|dosageValue=10|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=10|pillScore=1}}
{{PillImage|fileName=Amlodipine_Besylate_NDC_683820123.jpg|drugName=Amlodipine Besylate|NDC=683820123|drugAuthor=Zydus Pharmaceuticals (USA) Inc.|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=Z;5|dosageValue=10|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=8|pillScore=1}}
{{PillImage|fileName=Amlodipine_besylate_NDC_762820238.jpg|drugName=Amlodipine besylate|NDC=762820238|drugAuthor=Exelan Pharmaceuticals, Inc.|ingredients=AMLODIPINE BESYLATE[AMLODIPINE]|pillImprint=238;IG|dosageValue=5|dosageUnit=mg|pillColor=White|pillShape=Round|pillSize=6|pillScore=1}}


In its oral form ('''Blocadren'''), it is used:
==Mechanism of Action==
* to treat [[hypertension|high blood pressure]]  
Amlodipine is a [[dihydropyridine]] [[calcium antagonist]] (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that amlodipine binds to both dihydropyridine and [[nondihydropyridine]] binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative [[inotropic]] effects can be detected in vitro but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound (pKa=8.6), and its kinetic interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect.
* 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.
Amlodipine is a peripheral arterial [[vasodilator]] that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.


==Side effects==
The precise mechanisms by which amlodipine relieves [[angina]] have not been fully delineated, but are thought to include the following:


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]].
'''Exertional Angina:''' In patients with exertional [[angina]], NORVASC reduces the total peripheral resistance ([[afterload]]) against which the heart works and reduces the rate pressure product, and thus myocardial oxygen demand, at any given level of exercise.


==Usual dosage==
'''Vasospastic Angina:''' NORVASC has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium [[epinephrine]], [[serotonin]], and [[thromboxane A2]] analog in experimental animal models and in human coronary vessels in vitro. This inhibition of coronary spasm is responsible for the effectiveness of NORVASC in vasospastic ([[Prinzmetal's]] or variant) angina.<ref name="dailymed.nlm.nih.gov">{{Cite web  | last = | first = | title = NORVASC (AMLODIPINE BESYLATE) TABLET [CARDINAL HEALTH] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=44e5ad27-e062-461a-bdf4-192d852fbc49#nlm42230-3 | publisher =  | date =  | accessdate = 6 March 2014 }}</ref>


*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==
==References==


*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==
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==
{{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 17:23, 14 July 2014

Amlodipine
NORVASC®, AMLODIPINE®, AMLODIPINE BESYLATE® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Clinical Trials on Amlodipine
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief:

For patient information about Amlodipine, click here.

Synonyms / Brand Names: Norvasc®, Amlodipine®, Amlodipine Besylate®.

Overview

Amlodipine (Norvasc (Pfizer) and generics) (as besylate, mesylate or maleate) is a long-acting dihydropyridine-type (DHP) calcium channel blocker used to lower blood pressure and to treat anginal chest pain. Like other calcium channel blockers, amlodipine lowers blood pressure by relaxing arterial smooth muscles, which decreases total peripheral resistance and therefore reduces blood pressure. In angina, amlodipine increases blood flow to the heart muscle (although DHP-class calcium channel blockers are more selective for arteries than the muscular tissue of the heart (myocardium), as the calcium ion channels of the heart are not of the dihydropyridine-type).

Category

Dihydropyridine calium channel blocker.

FDA Package Insert

Norvasc®

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

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Mechanism of Action

Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects can be detected in vitro but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound (pKa=8.6), and its kinetic interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect.

Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.

The precise mechanisms by which amlodipine relieves angina have not been fully delineated, but are thought to include the following:

Exertional Angina: In patients with exertional angina, NORVASC reduces the total peripheral resistance (afterload) against which the heart works and reduces the rate pressure product, and thus myocardial oxygen demand, at any given level of exercise.

Vasospastic Angina: NORVASC has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium epinephrine, serotonin, and thromboxane A2 analog in experimental animal models and in human coronary vessels in vitro. This inhibition of coronary spasm is responsible for the effectiveness of NORVASC in vasospastic (Prinzmetal's or variant) angina.[1]


References

  1. ↑ "NORVASC (AMLODIPINE BESYLATE) TABLET [CARDINAL HEALTH]". Retrieved 6 March 2014.
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