Nifedipine, sold under the brand name Procardia among others, is a calcium channel blocker medication used to manage angina, high blood pressure, Raynaud's phenomenon, and premature labor.[3] It is one of the treatments of choice for Prinzmetal angina.[3] It may be used to treat severe high blood pressure in pregnancy.[3] 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.[3] It is a calcium channel blocker of the dihydropyridine type.[3] Nifedipine is taken by mouth and comes in fast- and slow-release formulations.[3]
Common side effects include lightheadedness, headache, feeling tired, leg swelling, cough, and shortness of breath.[3] Serious side effects may include low blood pressure and heart failure.[3] Nifedipine is considered safe in pregnancy and breastfeeding.[4]
Nifedipine was patented in 1967 and approved for use in the United States in 1981.[3][5][6] It is on the World Health Organization's List of Essential Medicines.[7] It is available as a generic medication.[3] In 2023, it was the 120th most commonly prescribed medication in the United States, with more than 5million prescriptions.[8][9]
Medical uses
High blood pressure
The 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 black patients.[10]
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.[11] 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.[12][13] 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.[14]
Early labor
Nifedipine 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.[15]
Other
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.[16]
Topical nifedipine has been shown to be as effective as topical nitrates for anal fissures.[17]
Nifedipine is also used in high-altitude medicine to treat high altitude pulmonary edema.[18]
Nifedipine is one of the main choices for the treatment of Prinzmetal angina due to its vasodilating effects on the coronary arteries.[3]
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.
Finally, nifedipine can be used in the treatment of renal calculi, which are commonly referred to as kidney stones. Studies have indicated that it helps to relieve renal colic. However, alpha blockers (such as tamsulosin) have been described as being significantly better.[19] It has also been reported to bind tubulin, blocking its polymerization.[20]
Side effects
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.
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.[21]
As a calcium channel blocker, nifedipine has a risk of causing gingival hyperplasia.[22]
Overdose
A 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.[23][24]
Mechanism of action
Nifedipine 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.[25][26]
Nifedipine has additionally been found to act as an antagonist of the mineralocorticoid receptor, or as an antimineralocorticoid.[27]
History
Nifedipine (initially BAY a1040, then Adalat) was developed by the German pharmaceutical company Bayer, with most initial studies being performed in the early 1970s.[28]
In 1980, Ahmed Hegazy and Klaus-Dieter Rämsch submitted their invention on extended release formulation that became known as Adalat retard.[29] Marketed as Adalat 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 with coronary 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]
Society and culture
Brand names
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]
References
- Nifedipine Pregnancy and Breastfeeding Warnings retrieved 25 December 2015^
- Product monograph brand safety updates Health Canada, February 2024, retrieved 24 March 2024^
- Nifedipine The American Society of Health-System Pharmacists, retrieved 17 September 2019^
- Nifedipine Drugs and Lactation Database, National Institute of Child Health and Human Development, 15 August 2023, retrieved 14 October 2023^
- Drug Discovery: Practices, Processes, and Perspectives John Wiley & Sons, 2013, retrieved 20 January 2022^
- Analogue-based Drug Discovery John Wiley & Sons, 2006^
- The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023) World Health Organization, 2023^
- Top 300 of 2023 ClinCalc, retrieved 12 August 2025^
- Nifedipine Drug Usage Statistics, United States, 2013 - 2023 ClinCalc, retrieved 18 August 2025^
- Hypertension: management of hypertension in adults in primary care. Clinical guideline CG34 National Institute for Health and Clinical Excellence (NICE), June 2006^
- Nifedipine for MAOI Hypertension? Reversing a Previous Recommendation Biological Therapies in Psychiatry, March 1997, retrieved 22 January 2015^
- Should a moratorium be placed on sublingual nifedipine capsules given for hypertensive emergencies and pseudoemergencies? JAMA, 1996^
- Clinical review: the management of hypertensive crises Critical Care, October 2003^
- Autonomic Dysreflexia in Spinal Cord Injury eMedicine, retrieved 14 July 2011^
- Calcium channel blockers for inhibiting preterm labour and birth The Cochrane Database of Systematic Reviews, June 2014^
- Calcium channel blockers for primary Raynaud's phenomenon: a meta-analysis Rheumatology, February 2005^
- Topical nifedipine vs. topical glyceryl trinitrate for treatment of chronic anal fissure Diseases of the Colon and Rectum, June 2003^
- Pulmonary Edema, High-Altitude eMedicine, 19 September 2007, retrieved 25 November 2007^
- Update on medical expulsive therapy for distal ureteral stones: Beyond alpha-blockers Canadian Urological Association Journal, November 2014^
- NanoDSF Screening for Anti-tubulin Agents Uncovers New Structure–Activity Insights Journal of Medicinal Chemistry, 2025^
- Grapefruit juice-nifedipine interaction: possible involvement of several mechanisms Journal of Clinical Pharmacy and Therapeutics, April 2005^
- Nifedipine NICE, retrieved 1 April 2021^
- Nifediac package insert, TEVA Pharmaceuticals, Sellersville, Pennsylvania, August 2009.^
- Disposition of Toxic Drugs and Chemicals in Man Biomedical Publications, 2008^
- Nifedipine blocks Ca2+ store refilling through a pathway not involving L-type Ca2+ channels in rabbit arteriolar smooth muscle The Journal of Physiology, May 2001^
- Regulation and modulation of calcium channels in cardiac, skeletal, and smooth muscle cells Physiological Reviews, April 1994^
- Is there a new dawn for selective mineralocorticoid receptor antagonism? Current Opinion in Nephrology and Hypertension, September 2014^
- [Pharmacology of 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester (Nifedipine, BAY a 1040)] Arzneimittel-Forschung, January 1972^
- Solid pharmaceutical compositions containing nifedipine, and process for their preparation^
- Pfizer Found Guilty In Adalat CC Case The Pharma Letter, 4 September 1994, retrieved 29 January 2022^
- Solid medicament formulations containing nifedipine, and processes for their preparation^
- Nifedipine. Dose-related increase in mortality in patients with coronary heart disease Circulation, September 1995^
- Nifedipine and mortality. Grave defects in the dossier Circulation, September 1995^
- Nicardia XL Medical Dialogues, retrieved 24 February 2021^
- Compendium retrieved 10 February 2023^