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| {{drugbox | IUPAC_name = dimethyl2,6-dimethyl-4-(2-nitrophenyl)- 1,4-dihydropyridine-3,5-dicarboxylate | image = Nifedipine.png | image2 = Nifedipine 3D.png | width = 165 | CAS_number = 21829-25-4 | ATC_prefix = C08 | ATC_suffix = CA05 | ATC_supplemental = | PubChem = 4485 | DrugBank = APRD00590 | C=17 | H=18 | N=2 | O=6 | molecular_weight = 346.335 g/mol | smiles = | melting_point = 173 | bioavailability = 45-56% | protein_bound = 92-98% | metabolism = Gastrointestinal, Hepatic | elimination_half-life = 2 hours | pregnancy_category = C: (USA) | legal_status = | routes_of_administration = Oral | excretion = Renal: >50%, Biliary: 5-15% }}
| | #REDIRECT [[Nifedipine#Pharmacology]] |
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| ==[[Nifedipine (patient information)|For patient information, click here]]==
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| ==Overview==
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| '''Nifedipine''' (brand name '''Adalat''', '''Nifedical''', and '''Procardia''') is a [[dihydropyridine]] [[calcium channel blocker]]. Its main uses are as an [[antianginal]] (especially in [[Prinzmetal's angina]]) and [[antihypertensive]], although a large number of other uses have recently been found for this agent, such as [[Raynaud's phenomenon]], [[Premature birth|premature labor]], and painful spasms of the [[esophagus]] in [[cancer]] and [[tetanus]] patients. It is also commonly used for the small subset of [[pulmonary hypertension]] patients whose symptoms respond to [[calcium channel blockers]].
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| ==Dosing==
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| Nifedipine rapidly lowers blood pressure, and patients are commonly warned they may feel dizzy or faint after taking the first few doses. [[Tachycardia]] (fast heart rate) may occur as a reaction. These problems are much less frequent in the sustained-release preparations of nifedipine (such as Adalat OROS). A more novel release system is GITS (Gastro-Intestinal Therapeutic System), which - according to Bayer - provides 24-hour continuous release through an osmotic push system. Recent trials with GITS include INSIGHT (for blood pressure)<ref>{{cite journal |author=Brown MJ, Palmer CR, Castaigne A, ''et al'' |title=Morbidity and mortality in patients randomised to double-blind treatment with a long-acting calcium-channel blocker or diuretic in the International Nifedipine GITS study: Intervention as a Goal in Hypertension Treatment (INSIGHT) |journal=Lancet |volume=356 |issue=9227 |pages=366-72 |year=2000 |pmid=10972368 |doi=}}</ref> and ACTION (for angina).<ref>{{cite journal |author=Poole-Wilson PA, Kirwan BA, Vokó Z, de Brouwer S, van Dalen FJ, Lubsen J |title=Safety of nifedipine GITS in stable angina: the ACTION trial |journal=Cardiovas Drugs Ther|volume=20 |issue=1 |pages=45-54 |year=2006 |pmid=16552473 |doi=10.1007/s10557-006-6312-4}}</ref>
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| Extended release formulations of nifedipine should be taken on an empty stomach, and patients are warned not to consume anything containing grapefruit or grapefruit juice, as they raise blood nifedipine levels. There are several possible mechanisms, including the lowering of [[CYP3A4]] activity.<ref>{{cite journal |author=Odou P, Ferrari N, Barthélémy C, ''et al'' |title=Grapefruit juice-nifedipine interaction: possible involvement of several mechanisms |journal=Journal Clinical Pharm Ther |volume=30 |issue=2 |pages=153-8 |year=2005 |pmid=15811168 |doi=10.1111/j.1365-2710.2004.00618.x}}</ref>
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| ==Uses==
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| ===Approved uses===
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| The approved uses for nifedipine are the long-term treatment of [[hypertension]] (high blood pressure) and [[angina pectoris]]. In hypertension, recent clinical guidelines generally favour [[diuretic]]s and [[ACE inhibitor]]s, although calcium channel antagonists are still favoured as primary treatment for older black patients.<ref>''Hypertension: management of hypertension in adults in primary care''. Clinical guideline CG34. [[National Institute for Health and Clinical Excellence]] (NICE), June 2006. [http://www.nice.org.uk/CG034 Fulltext index]. ISBN 1-86016-285-1.</ref>
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| Sublingual nifedipine has previously been used in [[Hypertensive emergency|hypertensive emergencies]]. This was found to be dangerous, and has been abandoned.<ref name="pmid8861992">{{cite journal |author=Grossman E, Messerli FH, Grodzicki T, Kowey P |title=Should a moratorium be placed on sublingual nifedipine capsules given for hypertensive emergencies and pseudoemergencies? |journal=JAMA |volume=276 |issue=16 |pages=1328-31 |year=1996 |pmid=8861992 |doi=}}</ref><ref name="pmid12974970">{{cite journal |author=Varon J, Marik PE |title=Clinical review: the management of hypertensive crises |journal=Critical care (London, England) |volume=7 |issue=5 |pages=374-84 |year=2003 |pmid=12974970 |doi=10.1186/cc2351}}</ref>
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| ===Off-label uses===
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| Nifedipine has been used frequently as a [[tocolytic]] (agent that delays premature labor). A Cochrane review has concluded that it is comparable with magnesium sulfate and beta-agonists (such as [[ritodrine]]) with fewer side-effects.<ref>{{cite journal |author=King JF, Flenady VJ, Papatsonis DN, Dekker GA, Carbonne B |title=Calcium channel blockers for inhibiting preterm labour |journal=Cochrane database of systematic reviews (Online) |volume= |issue=1 |pages=CD002255 |year=2003 |pmid=12535434 |doi=}}</ref> Its role ''vis à vis'' [[atosiban]] is not established.
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| [[Raynaud's phenomenon]] is often treated with nifedipine. A 2005 meta-analysis showed modest benefits (33% decrease in attack severity, 2.8-5 reduction in absolute number of attacks per week); it does conclude that most included studies used low doses of nifedipine.<ref>{{cite journal |author=Thompson AE, Pope JE |title=Calcium channel blockers for primary Raynaud's phenomenon: a meta-analysis |journal=Rheumatology (Oxford, England) |volume=44 |issue=2 |pages=145-50 |year=2005 |pmid=15546967 |doi=10.1093/rheumatology/keh390}}</ref>
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| [[Topical]] nifedipine has been shown to be as effective as topical nitrates for [[anal fissure]]s.<ref name="pmid12794583">{{cite journal |author=Ezri T, Susmallian S |title=Topical nifedipine vs. topical glyceryl trinitrate for treatment of chronic anal fissure |journal=Dis. Colon Rectum |volume=46 |issue=6 |pages=805-8 |year=2003 |pmid=12794583 |doi=10.1097/01.DCR.0000070044.62336.1D}}</ref>
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| Nifedipine is also used in high-altitude medicine to treat [[high altitude pulmonary edema]].<ref name="eMedicine">{{cite web | url= http://www.emedicine.com/med/topic1956.htm| title= Pulmonary Edema, High-Altitude| author= Ali, Mir Omar and Qazi, Samia| publisher= eMedicine }}</ref>
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| ==History==
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| Nifedipine (initially BAY a1040) was developed by the German [[pharmaceutical company]] [[Bayer]], with most initial studies being performed in the early 1970s.<ref>{{cite journal |author=Vater W, Kroneberg G, Hoffmeister F, ''et al'' |title=[Pharmacology of 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester (Nifedipine, BAY a 1040)] |language=German |journal=Arzneimittel-Forschung |volume=22 |issue=1 |pages=1-14 |year=1972 |pmid=4622472 |doi=}}</ref>
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| The use of nifedipine and related calcium channel antagonists was reduced much in response to 1995 trials that mortality was increased in patients with [[coronary artery disease]] who took nifedipine.<ref>{{cite journal |author=Furberg CD, Psaty BM, Meyer JV |title=Nifedipine. Dose-related increase in mortality in patients with coronary heart disease |journal=Circulation |volume=92 |issue=5 |pages=1326-31 |year=1995 |pmid=7648682 |doi=}}</ref> This study was a meta-analysis, and demonstrated harm mainly in short-acting forms of nifedipine (that could cause large fluctations in blood pressure) and at high doses of 80 mg a day and more.<ref>{{cite journal |author=Opie LH, Messerli FH |title=Nifedipine and mortality. Grave defects in the dossier |journal=Circulation |volume=92 |issue=5 |pages=1068-73 |year=1995 |pmid=7648646 |doi=}}</ref>
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| ==References==
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| {{Reflist|2}}
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| ==External links==
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| * [http://www.adalat.com/ Official site] (Bayer)
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| * {{MedlinePlusDrugInfo|medmaster|a684028}}
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| {{Calcium channel blockers}}
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| [[Category:Calcium channel blockers]]
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| [[Category:Tocolytics]]
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| [[Category:Antianginals]]
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| [[pl:Nifedypina]]
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