| 词条 | Nifedipine |
| 释义 |
| verifiedrevid = 462260435 | IUPAC_name = 3,5-dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate | image = Nifedipine.svg | width = 165 | image2 = Nifedipine-from-xtal-3D-balls.png | tradename = Adalat, Procardia, others | Drugs.com = {{drugs.com|monograph|nifedipine}} | MedlinePlus = a684028 | pregnancy_category = C: (USA) | legal_status = | routes_of_administration = by mouth, topical | bioavailability = 45-56% | protein_bound = 92-98% | metabolism = Gastrointestinal, Liver | elimination_half-life = 2 hours | excretion = Kidneys: >50%, Biliary: 5-15% | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 21829-25-4 | ATC_prefix = C08 | ATC_suffix = CA05 | ATC_supplemental = | PubChem = 4485 | IUPHAR_ligand = 2514 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB01115 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4330 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = I9ZF7L6G2L | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D00437 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 7565 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 193 | C=17 | H=18 | N=2 | O=6 | molecular_weight = 346.335 g/mol | smiles = O=C(OC)\\C1=C(\/C(=C(/C(=O)OC)C1c2ccccc2[N+]([O-])=O)C)C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C17H18N2O6/c1-9-13(16(20)24-3)15(14(10(2)18-9)17(21)25-4)11-7-5-6-8-12(11)19(22)23/h5-8,15,18H,1-4H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = HYIMSNHJOBLJNT-UHFFFAOYSA-N | melting_point = 173 }}Nifedipine, sold under the brand name Adalat among others, is a medication used to manage angina, high blood pressure, Raynaud's phenomenon, and premature labor.[1] It is one of the treatments of choice for Prinzmetal angina.[1] It may be used to treat severe high blood pressure in pregnancy.[1] Its use in preterm labor may allow more time for steroids to improve the baby's lung function and provide time for transfer of the mother to a well qualified medical facility before delivery.[1] Nifedipine is taken by mouth and comes in fast and slow release formulations.[1] Common side effects include lightheadedness, headache, feeling tired, leg swelling, cough, and shortness of breath.[1] Serious side effects may include low blood pressure and heart failure.[1] There is tentative evidence that its use in pregnancy is safe; however, it is not recommended during breastfeeding.[2] It is a calcium channel blocker of the dihydropyridine type.[1] Nifedipine was patented in 1967 and approved for use in the United States in 1981.[1][3][4] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[5] It is available as a generic medication.[1] The wholesale price in the developing world for the slow-release form is approximately US$1.90–3.80 per month.[6] In the United States, it costs approximately $40–60 per month, depending on the dose.[1] In 2016 it was the 154th most prescribed medication in the United States with more than 4 million prescriptions.[7] Medical usesHigh blood pressureThe approved uses are for the long-term treatment of hypertension and angina pectoris. In hypertension, recent clinical guidelines generally favour diuretics and ACE inhibitors, although calcium channel antagonists, along with thiazide diuretics, are still favoured as primary treatment for patients over 55 and African American patients.[8] Nifedipine given as sublingual administration has previously been used in hypertensive emergencies. It was once frequently prescribed on an as-needed basis to patients taking MAOIs for real or perceived hypertensive crises.[9] This was found to be dangerous, and has been abandoned. Sublingual administration of nifedipine promotes a hypotensive effect via peripheral vasodilation. It can cause an uncontrollable decrease in blood pressure, reflex tachycardia, and a steal phenomenon in certain vascular beds. There have been multiple reports in the medical literature of serious adverse effects with sublingual nifedipine, including cerebral ischemia/infarction, myocardial infarction, complete heart block, and death. As a result of this, in 1985 the FDA reviewed all data regarding the safety and effectiveness of sublingual nifedipine for the management of hypertensive emergencies, and concluded that the practice should be abandoned because it was neither safe nor effective.[10][11] An exception to the avoidance of this practice is in the use of nifedipine for the treatment of hypertension associated with autonomic dysreflexia in spinal cord injury.[12] Early laborNifedipine has been used frequently as a tocolytic (agent that delays premature labor). A Cochrane review has concluded that it has benefits over placebo or no treatment for prolongation of pregnancy. It also has benefits over beta-agonists and may also have some benefits over atosiban and magnesium sulfate, although atosiban results in fewer maternal adverse effects. No difference was found in the rate of deaths among babies around the time of birth, while data on longer-term outcomes is lacking.[13] OtherRaynaud'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.[14]Topical nifedipine has been shown to be as effective as topical nitrates for anal fissures.[15]Nifedipine is also used in high-altitude medicine to treat high altitude pulmonary edema.[16] Other uses include painful spasms of the esophagus such as from cancer or tetanus. It is also used for the small subset of people with pulmonary hypertension. Side effectsNifedipine 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. 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 inhibition of CYP3A4-mediated metabolism.[17] OverdoseA number of persons have developed toxicity due to acute overdosage with nifedipine, either accidentally or intentionally, and via either oral or parenteral administration. The adverse effects include lethargy, bradycardia, marked hypotension and loss of consciousness. The drug may be quantified in blood or plasma to confirm a diagnosis of poisoning, or to assist in a medicolegal investigation following death. Analytical methods usually involve gas or liquid chromatography and specimen concentrations are usually in the 100-1000 μg/L range.[18][19] Mechanism of actionNifedipine is a calcium channel blocker. Although nifedipine and other dihydropyridines are commonly regarded as specific to the L-type calcium channel, they also possess nonspecific activity towards other voltage-dependent calcium channels.[20][21] Nifedipine has additionally been found to act as an antagonist of the mineralocorticoid receptor, or as an antimineralocorticoid.[22] HistoryNifedipine (initially BAY a1040) was developed by the German pharmaceutical company Bayer, with most initial studies being performed in the early 1970s.[23] The use of nifedipine and related calcium channel antagonists was much reduced in response to 1995 trials that mortality was increased in patients with coronary artery disease who took nifedipine.[24] 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.[25] See also
References1. ^1 2 3 4 5 6 7 8 9 10 {{cite web|title=Nifedipine|url=https://www.drugs.com/monograph/nifedipine.html|publisher=The American Society of Health-System Pharmacists|accessdate=Dec 19, 2015|deadurl=no|archiveurl=https://web.archive.org/web/20151225224837/http://www.drugs.com/monograph/nifedipine.html|archivedate=2015-12-25|df=}} 2. ^{{cite web|title=Nifedipine Pregnancy and Breastfeeding Warnings|url=https://www.drugs.com/pregnancy/nifedipine.html|accessdate=25 December 2015|deadurl=no|archiveurl=https://web.archive.org/web/20151221122156/http://www.drugs.com/pregnancy/nifedipine.html|archivedate=21 December 2015|df=}} 3. ^{{cite book|last1=Corey|first1=E.J.|title=Drug discovery practices, processes, and perspectives|date=2013|publisher=John Wiley & Sons|location=Hoboken, N.J.|isbn=9781118354469|page=172|url=https://books.google.ca/books?id=mIyxO5cLEAcC&pg=PA172|deadurl=no|archiveurl=https://web.archive.org/web/20170901032155/https://books.google.ca/books?id=mIyxO5cLEAcC&pg=PA172|archivedate=2017-09-01|df=}} 4. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. 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Clinical guideline CG34. National Institute for Health and Clinical Excellence (NICE), June 2006. Fulltext index {{webarchive|url=https://web.archive.org/web/20070617040043/http://www.nice.org.uk/CG034 |date=2007-06-17 }}. {{ISBN|1-86016-285-1}}. 9. ^{{Cite web|url = http://www.dr-bob.org/tips/split/Nifed-MAOI-hypertension.html|title = Nifedipine for MAOI Hypertension? Reversing a Previous Recommendation|date = March 1997|accessdate = 22 Jan 2015|website = |publisher = Biological Therapies in Psychiatry|deadurl = yes|archiveurl = https://web.archive.org/web/20150910023142/http://www.dr-bob.org/tips/split/Nifed-MAOI-hypertension.html|archivedate = 2015-09-10|df = }} 10. ^{{cite journal |vauthors=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=10.1001/jama.276.16.1328}} 11. ^{{cite journal |vauthors=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 |pmc=270718}} 12. ^{{cite web|last=Campagnolo|first=DI|title=Autonomic Dysreflexia in Spinal Cord Injury|url=http://emedicine.medscape.com/article/322809-medication|publisher=eMedicine|accessdate=2011-07-14}} 13. ^{{Cite journal|last=Flenady|first=Vicki|last2=Wojcieszek|first2=Aleena M.|last3=Papatsonis|first3=Dimitri N. M.|last4=Stock|first4=Owen M.|last5=Murray|first5=Linda|last6=Jardine|first6=Luke A.|last7=Carbonne|first7=Bruno|date=2014-06-05|title=Calcium channel blockers for inhibiting preterm labour and birth|journal=The Cochrane Database of Systematic Reviews|issue=6|pages=CD002255|doi=10.1002/14651858.CD002255.pub2|issn=1469-493X|pmid=24901312}} 14. ^{{cite journal |vauthors=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}} 15. ^{{cite journal |vauthors=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=10.1007/s10350-004-6660-8}} 16. ^{{cite web| url= http://www.emedicine.com/med/topic1956.htm| title= Pulmonary Edema, High-Altitude| author1= Ali, Mir Omar| author2= Qazi, Samia| lastauthoramp= yes| date= 2007-09-19| publisher= eMedicine| accessdate= 2007-11-25| deadurl= no| archiveurl= https://web.archive.org/web/20071116141543/http://www.emedicine.com/med/topic1956.htm| archivedate= 2007-11-16| df= }} 17. ^{{cite journal |vauthors=Odou P, Ferrari N, Barthélémy C, etal |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}} 18. ^Nifediac package insert, TEVA Pharmaceuticals, Sellersville, Pennsylvania, August, 2009. 19. ^{{cite book |author=Baselt, Randall C. |title=Disposition of Toxic Drugs and Chemicals in Man |publisher=Biomedical Publications |location=Foster City, CA |year=2008 |pages=1108–1110|isbn=0-9626523-7-7}} 20. ^{{cite journal|last1=Curtis|first1=Tim M.|last2=Scholfield|first2=C. Norman|title=Nifedipine blocks Ca2+ store refilling through a pathway not involving L-type Ca2+ channels in rabbit arteriolar smooth muscle store refilling through a pathway not involving L-type Ca2+ channels in rabbit arteriolar smooth muscle|journal=The Journal of Physiology|date=May 2001|volume=532|issue=3|pages=609–623|doi=10.1111/j.1469-7793.2001.0609e.x|pmc=2278590|pmid=11313433}} 21. ^{{cite journal|last1=McDonald|first1=TF|last2=Pelzer|first2=S|last3=Trautwein|first3=W|last4=Pelzer|first4=DJ|title=Regulation and modulation of calcium channels in cardiac, skeletal, and smooth muscle cells.|journal=Physiological Reviews|date=April 1994|volume=74|issue=2|pages=365–507|pmid=8171118}} 22. ^{{cite journal|last1=Luther|first1=James M.|title=Is there a new dawn for selective mineralocorticoid receptor antagonism?|journal=Current Opinion in Nephrology and Hypertension|volume=23|issue=5|year=2014|pages=456–461|issn=1062-4821|doi=10.1097/MNH.0000000000000051|pmc=4248353}} 23. ^{{cite journal |vauthors=Vater W, Kroneberg G, Hoffmeister F, etal |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=}} 24. ^{{cite journal |vauthors=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=10.1161/01.cir.92.5.1326}} 25. ^{{cite journal |vauthors=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=10.1161/01.cir.92.5.1068}} External links
| title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Glycine receptor modulators}}{{Ion channel modulators}}{{Mineralocorticoid receptor modulators}}{{Xenobiotic-sensing receptor modulators}} }}{{portal bar|Pharmacy and pharmacology|Medicine}} 9 : Antimineralocorticoids|Calcium channel blockers|Carboxylate esters|Dihydropyridines|Glycine receptor antagonists|Nitrobenzenes|RTT|Tocolytics|World Health Organization essential medicines |
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