Common side effects includelightheadedness,headache, feeling tired, leg swelling, cough, and shortness of breath.[2] Serious side effects may includelow blood pressure andheart failure.[2] Nifedipine is considered safe in pregnancy and breastfeeding.[5]
The approved uses are for the long-term treatment ofhypertension andangina pectoris. In hypertension, recent clinical guidelines generally favourdiuretics andACE inhibitors, although calcium channel antagonists, along withthiazide diuretics, are still favoured as primary treatment for patients over 55 and black patients.[11]
Nifedipine given assublingual administration has previously been used inhypertensive emergencies. It was once frequently prescribed on an as-needed basis to patients takingMAOIs for real or perceived hypertensive crises.[12] 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 asteal phenomenon in certain vascular beds. There have been multiple reports in the medical literature of serious adverse effects with sublingual nifedipine, includingcerebral ischemia/infarction,myocardial infarction, completeheart block, and death. As a result of this, in 1985 theFDA 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.[13][14] An exception to the avoidance of this practice is in the use of nifedipine for the treatment of hypertension associated withautonomic dysreflexia inspinal cord injury.[15]
Nifedipine has been used frequently as atocolytic (agent that delays premature labor). ACochrane review has concluded that it has benefits over placebo or no treatment for prolongation of pregnancy. It also has benefits overbeta-agonists and may also have some benefits overatosiban andmagnesium sulfate, althoughatosiban 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.[16]
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.[17]
Finally, nifedipine can be used in the treatment of renal calculi, which are commonly referred to askidney stones. Studies have indicated that it helps to relieve renal colic. However, alpha blockers (such astamsulosin) have been described as being significantly better.[20]
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.[medical citation needed]
Extended release formulations of nifedipine should be taken on an empty stomach, and patients are warned not to consume anything containinggrapefruit or grapefruit juice, as they raise blood nifedipine levels. There are several possible mechanisms, including the inhibition ofCYP3A4-mediated metabolism.[21]
A number of persons have developed toxicity due to acute overdosage with nifedipine, either accidentally or intentionally, and via either oral orparenteral administration. The adverse effects include lethargy, bradycardia, marked hypotension andloss 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 liquidchromatography and specimen concentrations are usually in the 100-1000 μg/L range.[23][24]
Nifedipine (initially BAY a1040, then Adalat) was developed by the German pharmaceutical companyBayer, with most initial studies being performed in the early 1970s.[28]
In 1980,Ahmed Hegazy and Klaus-Dieter Rämsch submitted their invention onextended release formulation that became known asAdalat retard.[29] Marketed asAdalat CC in US, a 1995 US lawsuit found that Pfizer's Procardia XL was also based on Bayer's Adalat European and US patents.[30][31]
The use of nifedipine and related calcium channel antagonists was much reduced in response to 1995 trials that mortality was increased in patients withcoronary artery disease who took nifedipine.[32] This study was a meta-analysis, and demonstrated harm mainly in short-acting forms of nifedipine (that could cause large fluctuations in blood pressure) and at high doses of 80 mg a day and more.[33]
In India, nifedipine is manufactured by JB Chemicals, and comes in brands Nicardia Retard (Nifedipine 10 mg, 20 mg tablets) and Nicardia XL 30/60, which are Nifedipine Extended Release tablets.[34]
In Switzerland, nifedipine is sold only as a generic version of extended release formulation, under the names Nifedipin Mepha and Nifedipin Spirig.[35]
^"Nifedipine".Drugs and Lactation Database. Bethesda (MD): National Institute of Child Health and Human Development. 15 August 2023.PMID30000106. Retrieved14 October 2023.
^Sliskovic DR (2013)."Cardiovascular Drugs". InLi JJ,Corey EJ (eds.).Drug Discovery: Practices, Processes, and Perspectives. Hoboken, NJ: John Wiley & Sons. pp. 141–204.ISBN9781118354469.Archived from the original on 1 September 2017. Retrieved20 January 2022. p. 172:nifedipine...1,4-dihydropyrine originally approved in 1981.
^World Health Organization (2023).The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization.hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
^Grossman E, Messerli FH, Grodzicki T, Kowey P (1996). "Should a moratorium be placed on sublingual nifedipine capsules given for hypertensive emergencies and pseudoemergencies?".JAMA.276 (16):1328–1331.doi:10.1001/jama.1996.03540160050032.PMID8861992.
^Ezri T, Susmallian S (June 2003). "Topical nifedipine vs. topical glyceryl trinitrate for treatment of chronic anal fissure".Diseases of the Colon and Rectum.46 (6):805–808.doi:10.1007/s10350-004-6660-8.PMID12794583.S2CID24717470.
^McDonald TF, Pelzer S, Trautwein W, Pelzer DJ (April 1994). "Regulation and modulation of calcium channels in cardiac, skeletal, and smooth muscle cells".Physiological Reviews.74 (2):365–507.doi:10.1152/physrev.1994.74.2.365.PMID8171118.
^Vater W, Kroneberg G, Hoffmeister F, Saller H, Meng K, Oberdorf A, et al. (January 1972). "[Pharmacology of 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester (Nifedipine, BAY a 1040)]".Arzneimittel-Forschung (in German).22 (1):1–14.PMID4622472.
^EP 0047899B2, Hegasy A, Rämsch KD, "Solid pharmaceutical compositions containing nifedipine, and process for their preparation", issued 28 February 1996, assigned to Bayer AG
^US US5264446A, Hegasy A, Ramsch KD, "Solid medicament formulations containing nifedipine, and processes for their preparation", issued November 23, 1993, assigned to Bayer AG
^Furberg CD, Psaty BM, Meyer JV (September 1995). "Nifedipine. Dose-related increase in mortality in patients with coronary heart disease".Circulation.92 (5):1326–1331.doi:10.1161/01.cir.92.5.1326.PMID7648682.S2CID32044931.
^Opie LH, Messerli FH (September 1995). "Nifedipine and mortality. Grave defects in the dossier".Circulation.92 (5):1068–1073.doi:10.1161/01.cir.92.5.1068.PMID7648646.
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