Epub 2005 Jan 5. U.S. Patent US4412986, issued November, 1976. 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. [26], In India, Nifedipine is manufactured by JB Chemicals, and comes in brands Nicardia Retard ( Nifedipine 10mg, 20mg tablets)[27] as well as Nicardia XL 30/60 which are Nifedipine Extended Release Tablets[28], 3,5-dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, O=C(OC)\C1=C(\N/C(=C(/C(=O)OC)C1c2ccccc2[N+]([O-])=O)C)C, InChI=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. Mechanism of Action. Topical 10% nifedipine on one hand and 5% sildenafil on the other hand were applied. InChI=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, 3,5-dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-])=O)C(=O)OC. Read more about the prescription drug NIFEDIPINE SUSTAINED-ACTION - ORAL. Read more about the prescription drug NIFEDIPINE SUSTAINED-ACTION - ORAL. It may be used to treat severe high blood pressure in pregnancy. World Health Organization's List of Essential Medicines, "Nifedipine Pregnancy and Breastfeeding Warnings", National Institute for Health and Clinical Excellence, "Nifedipine for MAOI Hypertension? Drug Metab Dispos. J Pharmacol Exp Ther. Nifedipine is a yellow crystalline substance, practically insoluble in water but soluble in ethanol. Epub 2008 Nov 24. Nifedipine, a calcium channel blocker, inhibits low- er esophageal sphincter pressure but has only mini- mal effect on esophageal contractions. Tell your doctor if you are breast-feeding a baby. Although its exact mechanism of action in these various diseases has not been precisely described, the potent coronary and peripheral arterial dilator properties of nifedipine, with concomitant improvements in oxygen supply/demand and reductions in systemic vascular resistance, are of major importance. [, Otto J, Lesko LJ: Protein binding of nifedipine. Efficacy, duration and mechanism of action of nifedipine in stable exercise-induced angina pectoris D. ARDISSINO, D. ARDISSINO Divisione di Cardiologia Policlinico S. Matteo Cattedra di Fisiopatologia Cadriorespiratoria Universit´ di Pavia. 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. [, Waller DG, Renwick AG, Gruchy BS, George CF: The first pass metabolism of nifedipine in man. 2002 Dec;30(12):1512-22. Consultant (Obstetrics) Cape Town University Hospital, South Africa. [, Chung M, Reitberg DP, Gaffney M, Singleton W: Clinical pharmacokinetics of nifedipine gastrointestinal therapeutic system. J Pharm Pharmacol. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Nifedipine in pregnancy. [, Foti RS, Rock DA, Wienkers LC, Wahlstrom JL: Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation. Avoid grapefruit products. [, Payen L, Sparfel L, Courtois A, Vernhet L, Guillouzo A, Fardel O: The drug efflux pump MRP2: regulation of expression in physiopathological situations and by endogenous and exogenous compounds. Avoid excessive or chronic alcohol consumption. Mechanism of Action of Nifedipine Nifedipine is a dihydropyridine Ca channel blocker. If you are breastfeeding, discuss with your doctor if you should either discontinue breastfeeding or stop using this medicine while breastfeeding. The mechanism of action of nifedipine was studied by adding the drug either to randomly growing cells or to quiescent, G0/G1 arrested and synchronized cells. Sublingual administration of nifedipine promotes a hypotensive effect via peripheral vasodilation. The binding of nifedipine to voltage-dependent and possibly receptor-operated channels in vascular smooth muscle results in an inhibition of calcium influx through these channels. Avoid grapefruit products while on this medication. [2] It is one of the treatments of choice for Prinzmetal angina. 2008 Feb 15;586(4):929-50. The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral vascular resistance. A controlled-release formulation of nifedipine. [, van Harten J, Burggraaf K, Danhof M, van Brummelen P, Breimer DD: Negligible sublingual absorption of nifedipine. [14], Topical nifedipine has been shown to be as effective as topical nitrates for anal fissures. Aceclofenac may decrease the excretion rate of Nifedipine which could result in a higher serum level. Consultant (Obstetrics) Cape Town University Hospital, South Africa. Consultant (Obstetrics) McMaster University, Hamilton, Ontario, Canada. 2003 Jul;31(7):938-44. [, Ma B, Prueksaritanont T, Lin JH: Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Their mechanism of action in tocolysis involves the blockade of L-type Ca2+ channels, influenced by the Ca2+-activated K+ channels, beta-adrenergic receptors (β-ARs) and sexual hormones. Dilates coronary arteries and arterioles in normal and ischemic tissue, prevents coronary artery spasm [24], 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.
Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for nifedipine before they complete the sale. 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. [, Ramachandran SD, Vivares A, Klieber S, Hewitt NJ, Muenst B, Heinz S, Walles H, Braspenning J: Applicability of second-generation upcyte(R) human hepatocytes for use in CYP inhibition and induction studies. The serum concentration of Nifedipine can be increased when it is combined with Abiraterone. Epub 2012 May 15. (2004). 2005 Apr;313(1):302-9. 23 results found < Page ; 1; of ; 1 > Adalat LA 30 mg prolonged-release tablets nifedipine Bayer plc. The increased peripheral vascular resistance, an underlying cause of hypertension, results from an increase in active tension in the vascular smooth muscle. Nifedipine mechanism of action Inhibits the movement of calcium ions across cell membranes by blocking the entry of calcium into cells. Consultant (Obstetrics) McMaster University, Hamilton, Ontario, Canada. 2003 Nov;31(11):1296-9. Nifedipine did not relax the La3+-contracture in a range of doses at which K+-contracture of both types of smooth muscles was relaxed. Consultant (Obstetrics) North Staffordshire Hospital, Stoke on Trent, UK. Nifedipine. Richard Johanson. Consumer information about the medication NIFEDIPINE SUSTAINED-ACTION - ORAL (Adalat CC), includes side effects, drug interactions, recommended dosages, and storage information. Continue This medicine passes into the breastmilk. ii. Nifedipine is 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, dimethyl ester, C 17 H 18 N 2 O 6, and has the structural formula: Nifedipine is a yellow crystalline substance, practically insoluble in water but soluble in ethanol. The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Acebutolol. 2015 Oct;3(5):e00161. Nifedipine's mechanism of action is through smooth-muscle relaxation secondary to blockage of the slow calcium channels into the cells. Am J Med. The primary outcome was the improvement of blood flow and vessel diameter of the digital arteries measured by high frequency color Doppler ultrasound before and 1 hour after treatment. Epub 2007 Dec 20. Mechanism of Action. Search for more papers by this author. Nifedipine may also be used for purposes not listed in this medication guide. 2005 Jan;45(1):68-78. Khan KM, Patel J, Schaefer TJ: Nifedipine . Nifedipine is in a group of drugs called calcium channel blockers. The increased peripheral vascular resistance that is an underlying cause of hypertension results from an increase in active tension in the vascular smooth muscle. [, Stieger B: Role of the bile salt export pump, BSEP, in acquired forms of cholestasis. Nifedipine is not safe for use in women who are breastfeeding. 2000 Feb-Mar;55(11-12):843-52. This site uses cookies. Pavia, Italy. Nifedipine may decrease the hypoglycemic activities of Acarbose. [, Bett GC, Rasmusson RL: Modification of K+ channel-drug interactions by ancillary subunits. 2002;18(4):221-33. There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Nifedipine is used for the treatment and prevention of angina resulting from either an increased workload on the heart (as with exercise) or spasm of the coronary arteries.It is used in the treatment of high blood pressure, to treat abnormally fast heart rhythms such as atrial fibrillation, and in the prevention of episodes of rapid heart rhythm originating from the atria of the heart. Analogous to the use of NTG intra-anal ointment, nifedipine ointment is also available for use in clinical trials. J Clin Pharmacol. 2002 Aug;16(3):159-65. 10 to 30 mg PO or SL, 30 to 45 minutes before meals. Drug Metab Dispos. doi: 10.1161/01.hyp.5.4_pt_2.ii18. Drug created on June 13, 2005 07:24 / Updated on January 23, 2021 21:03. 2004 Mar 19;315(4):942-9. [, Pelkonen O, Maenpaa J, Taavitsainen P, Rautio A, Raunio H: Inhibition and induction of human cytochrome P450 (CYP) enzymes. However, oral labetalol and oral extended release nifedipine are the most commonly used medications for post- partum hypertension, and their efficacy has not been directly compared. This information should not be interpreted without the help of a healthcare provider. Nifedipine can pass into breast milk and may harm a nursing baby. 1984 Dec;18(6):951-4. doi: 10.1111/j.1365-2125.1984.tb02569.x. Drug Metab Dispos. Patricia Smith. These problems are much less frequent in the sustained-release preparations of nifedipine. The date on which a patent was filed with the relevant government. 2015;8(2):110-22. Concomitant administration with strong CYP3A4 inducers (eg, rifampin, rifabutin, phenobarbital, phenytoin, carbamazepine, St John's wort) significantly reduces nifedipine efficacy. John Anthony. By continuing to browse the site you are agreeing to our policy on the use of cookies. Nucleic Acids Res. [, ADALAT® XL® (Nifedipine extended-release tablets) Product Monograph [, Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. Mechanism of Action of Nifedipine Nifedipine is a dihydropyridine Ca channel blocker. 2017 May 29;8:286. doi: 10.3389/fphar.2017.00286. Toxicol Sci. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. 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. 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. An effect category for each drug interaction. Epub 2016 Apr 22. [, Godfraind T: Discovery and Development of Calcium Channel Blockers. The effects of varying the duration of drug treatment were also examined. The duration of effect of single oral doses of 10 and 20 mg of nifedipine was studied in 10 patients with angiographically proven coronary crtery dise ... Efficacy, duration and mechanism of action of nifedipine in stable exercise-induced angina pectoris D. ARDISSINO, Mechanism of Action: The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral vascular resistance. 1983 Jul-Aug;5(4 Pt 2):II18-24. Mechanism of action The following was added by Herizora‎ : As a calcium channel blocker , nifedipine is expected to inhibit the currents of L-type Cav1.3 channels in the zona glomerulosa of the adrenal , reducing aldosterone production and corroborating to lower blood pressure . Reversing a Previous Recommendation", "Clinical review: the management of hypertensive crises", "Autonomic Dysreflexia in Spinal Cord Injury", "Calcium channel blockers for inhibiting preterm labour and birth", "Calcium channel blockers for primary Raynaud's phenomenon: a meta-analysis", "Update on medical expulsive therapy for distal ureteral stones: Beyond alpha-blockers", "Nifedipine blocks Ca2+ store refilling through a pathway not involving L-type Ca2+ channels in rabbit arteriolar smooth muscle", "Is there a new dawn for selective mineralocorticoid receptor antagonism? The metabolism of Abemaciclib can be increased when combined with Nifedipine. Nifedipine is a dihydropyridine calcium channel blocking agent. Search for more papers by this author. Procardia® (nifedipine) is an antianginal drug belonging to a class of pharmacological agents, the calcium channel blockers. The precise means by which this inhibition relieves angina has not been fully determined, but includes at least the following two mechanisms: 1) Relaxation and Prevention of Coronary Artery Spasm. Overall, the use of nifedipine was associated with a significant adverse effect on total mortality (risk ratio, 1.16, with a 95% CI of 1.01 to 1.33). 2017 Jan;14(1):67-72. doi: 10.11909/j.issn.1671-5411.2017.01.006. Abacavir may decrease the excretion rate of Nifedipine which could result in a higher serum level. Address for Reprints: D. Ardissino, Cardiologia, Policlinico S. Matteo, I-277100 Pavia, Italy. Hypersensitivity to nifedipine or other calcium-channel blockers. In Encyclopedic reference of molecular pharmacology (pp. [, Raemsch KD, Sommer J: Pharmacokinetics and metabolism of nifedipine. There are several possible mechanisms, including the inhibition of CYP3A4-mediated metabolism. Antianginal, antihypertensive, calcium channel blocker. [, Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). 2002 Jan 1;30(1):412-5. [1], Nifedipine was patented in 1967, and approved for use in the United States in 1981. Recent trials of any calcium antagonist and formulation were also reviewed for information about the possible mechanisms of action that might increase mortality. In vivo, there is minimal effect on the cardiac conducting system. [, Sinnegger-Brauns MJ, Huber IG, Koschak A, Wild C, Obermair GJ, Einzinger U, Hoda JC, Sartori SB, Striessnig J: Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms. Back to top. Mechanism Of Action Nifedipine is a peripheral arterial vasodilator which acts directly on vascular smooth muscle. 1986 Aug;81(2):344-6. doi: 10.1016/0002-9343(86)90276-7. 1988 Jul;11(7):505-6. doi: 10.1002/clc.4960110714. Epub 2006 May 4. What is nifedipine? Regarding to the underlying mechanism, we examined whether (1) nifedipine changed the mRNA and protein levels of the constitutive endothelial NO synthase (NOS) in endothelial cell cultures or (2) nifedipine exerts an NO protective effect via its antioxidative properties, as revealed in a cell culture model and with native endothelium from porcine coronary arteries. 2010 Jun;38(6):981-7. doi: 10.1124/dmd.110.032094. Mol Pharmacol. John Anthony. Drug Metab Dispos. Talk to your doctor before using this form of nifedipine if you have galactose intolerance, or severe problems with lactose (milk sugar). Nifedipine, sold under the brand name Adalat among others, is a calcium channel blocker medication used to manage angina, high blood pressure, Raynaud's phenomenon, and premature labor. [, Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. [, Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. [, Tassaneeyakul W, Birkett DJ, Veronese ME, McManus ME, Tukey RH, Quattrochi LC, Gelboin HV, Miners JO: Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. These two compounds interact in a … 2000 Feb;28(2):125-30. [, Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. A rating for the strength of the evidence supporting each drug interaction. [18], A number of persons have developed toxicity due to acute overdosage with nifedipine, either accidentally or intentionally, and via either oral or parenteral administration. If you believe you are experiencing an interaction, contact a healthcare provider immediately. Classification Nifedipine. 4 Mechanism of action. [6][7], The approved uses are for the long-term treatment of hypertension and angina pectoris. Search for more papers by this author. How should I take nifedipine? Ca 2+ channel blockers. Its mechanism of action and clinical effects closely resemble those of nifedipine and the other dihydropyridines (amlodipine, felodipine), except that nicardipine is more selective for cerebral and coronary blood vessels. The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral vascular resistance. iv. [2] In 2017, it was the 120th most commonly prescribed medication in the United States, with more than six million prescriptions. Am J Med. Grapefruit down-regulates post-translational expression of CYP3A4, the major metabolizing enzyme of nifedipine. Nifedipine is used to treat hypertension (high blood pressure) and angina (chest pain). Br J Clin Pharmacol. A Cochrane review has concluded that it has benefits over placebo or no treatment for prolongation of pregnancy. BMC Biochem. Rcsmoak. Nifedipine, or BAY a 1040, is a first generation dihydropyridine L-type calcium channel blocker, similar to nicardipine.3,10,11,13 Nifedipine was developed by Bayer and first described in the literature, along with other dihydropyridines, in 1972.11,12 Since nifedipine's development, second and third generation dihydropyridines have been developed with slower onsets and longer durations of action.10 The most popular of the third generation dihydropyridines is amlodipine.10, Nifedipine was granted FDA approval on 31 December 1981.13, Nifedipine capsules are indicated to treat vasospastic angina and chronic stable angina.13 Extended release tablets are indicated to treat vasospastic angina, chronic stable angina, and hypertension.14,15, Nifedipine is an inhibitor of L-type voltage gated calcium channels that reduces blood pressure and increases oxygen supply to the heart.1 Immediate release nifedipine's duration of action requires dosing 3 times daily.13 Nifedipine dosing is generally 10-120mg daily.13 Patients should be counselled regarding the risk of excessive hypotension, angina, and myocardial infarction.13, Nifedipine blocks voltage gated L-type calcium channels in vascular smooth muscle and myocardial cells.1 This blockage prevents the entry of calcium ions into cells during depolarization, reducing peripheral arterial vascular resistance and dilating coronary arteries.1 These actions reduce blood pressure and increase the supply of oxygen to the heart, alleviating angina.1, Sublingual dosing leads to a Cmax of 10ng/mL, with a Tmax of 50min, and an AUC of 25ng*h/mL.9 Oral dosing leads to a Cmax of 82ng/mL, with a Tmax of 28min, and an AUC of 152ng*h/mL.9, Nifedipine is a Biopharmaceutics Classification System Class II drug, meaning it has low solubility and high intestinal permeability.8 It is almost completely absorbed in the gastrointestinal tract but has a bioavilability of 45-68%, partly due to first pass metabolism.3,8, The steady state volume of distribution of nifedipine is 0.62-0.77L/kg and the volume of distribution of the central compartment is 0.25-0.29L/kg.3, Nifedipine is 92-98% protein bound in serum.13 Nifedipine is 97±12% bound in a 40g/L solution of pure albumin.2 Nifedipine is 51.4±5.9% protein bound in a 50mg/100mL solution of alpha-1-acid glycoprotein, and 75.5±3.5% protein bound in a 150mg/mL solution.2, Nifedipine is predominantly metabolized by CYP3A4.1,8,13,14,15 Nifedipine is predominantly metabolized to 2,6-dimethyl-4-(2-nitrophenyl)-5-methoxycarbonyl-pyridine-3-carboxylic acid, and then further metabolized to 2-hydroxymethyl-pyridine carboxylic acid.6 Nifedipine is also minorly metabolized to dehydronifedipine.7, Hover over products below to view reaction partners, Nifedipine is 60-80% recovered in the urine as inactive water soluble metabolites, and the rest is eliminated in the feces as metabolites.14, The terminal elimination half life of nifedipine is approximately 2 hours.3,8, The total body clearance of nifedipine is 450-700mL/min.3, The oral LD50 in rats is 1022mg/kg and in mice is 202mg/kg.16, Patients experiencing an overdose may present with hypotension, sinus node dysfunction, atrioventricular node dysfunction, and reflex tachycardia.4,5 Overdose may be managed by monitoring cardiovascular and respiratory function; elevating extremities; and administering vasopressors, fluids, and calcium infusions.13. Mechanism of Action. Eur J Clin Pharmacol. The nifedipine extended-release tablet may contain lactose. [, Nader AM, Quinney SK, Fadda HM, Foster DR: Effect of Gastric Fluid Volume on the In Vitro Dissolution and In Vivo Absorption of BCS Class II Drugs: a Case Study with Nifedipine. Consumer information about the medication NIFEDIPINE SUSTAINED-ACTION - ORAL (Adalat CC), includes side effects, drug interactions, recommended dosages, and storage information. 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. [21][22], Nifedipine has additionally been found to act as an antagonist of the mineralocorticoid receptor, or as an antimineralocorticoid. 2011 Feb 3;12:5. doi: 10.1186/1471-2091-12-5. J Pharmacol Exp Ther. J Physiol. The increased peripheral vascular resistance, an underlying cause of hypertension, results from an increase in active tension in the vascular smooth muscle. Lee et al., 2006, Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms., Pharmacology NIFEDIPINE SLC14A2 Interaction Score: … Nicardipine was approved by the FDA in December 1988. Multiple studies in women have demonstrated the effectiveness and safety of nifedipine as an antihypertensive. In clinical practice, most experience has been gained with the use of nifedipine, whose efficacy is superior or comparable to those of β-agonists and oxytocin antagonists. Some of the side effects of nifedipine are predictable on the basis of its calcium channel blocking abilities. C. The mechanism by which nifedipine reduces arterial blood press… Generic name: Nifedipine. By Alison M. Gurney, Jeanne M. Nerbonne and Henry A. Lester. Richard Johanson. Hiroitsu Kawata, Tadayoshi Ohmura, Katsuhiko Yano, Mikio Matsumura, Saburo Higuchi, Yoshiaki Soeishi, "Nifedipine-containing solid preparation composition." The mechanism of action of nifedipine was studied by adding the drug either to randomly growing cells or to quiescent, G0/G1 arrested and synchronized cells. [, Whitebloom D, Fitzharris J: Nifedipine overdose. This group reduces the absorption of calcium by the myocardial cells and blood vessels – all as a result of the blockage of voltage-dependent calcium channels. Hypertension. It can cause an uncontrollable decrease in blood pressure, reflex tachycardia, and a steal phenomenon in certain vascular beds. Biochem Biophys Res Commun. Analytical methods usually involve gas or liquid chromatography and specimen concentrations are usually in the 100-1000 μg/L range. [, Galetin A, Clarke SE, Houston JB: Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach. [17], Nifedipine rapidly lowers blood pressure, and patients are commonly warned they may feel dizzy or faint after taking the first few doses. It exerts it`s antianginal, antihypertensive actions through blocking the influx of Ca2+ ions through voltage gated L-type Ca channels to the peripheral vascular smooth muscle cells, Coronary smooth muscle cells and to the myocardial cells. SmPC; Patient Leaflet; Adanif XL 60mg Tablets nifedipine ADVANZ Pharma. Download PDF (1 MB) Abstract. [2] Serious side effects may include low blood pressure and heart failure. Know how this interaction affects the subject drug. [2], Common side effects include lightheadedness, headache, feeling tired, leg swelling, cough, and shortness of breath. J Geriatr Cardiol. Nifedipine is a calcium channel blocker. Nifedipine, sold under the brand name Adalat among others, is a calcium channel blocker medication used to manage angina, high blood pressure, Raynaud's phenomenon, and premature labor. [, Striessnig, J. Dihydropyridinecarboxylic acid derivative, Propargyl-type 1,3-dipolar organic compound, Voltage-dependent L-type calcium channel subunit alpha-1C, Nuclear receptor subfamily 1 group I member 2, Voltage-dependent L-type calcium channel subunit alpha-1D, Voltage-dependent L-type calcium channel subunit alpha-1S, Voltage-dependent L-type calcium channel subunit beta-2, Potassium voltage-gated channel subfamily D member 3, 2,6-dimethyl-4-(2-nitrophenyl)-5-methoxycarbonyl-pyridine-3-carboxylic acid, C08C — SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS, C08GA — Calcium channel blockers and diuretics, C08G — CALCIUM CHANNEL BLOCKERS AND DIURETICS, C07FB — Beta blocking agents and calcium channel blockers, C07F — BETA BLOCKING AGENTS, OTHER COMBINATIONS, Antihypertensive Agents Indicated for Hypertension, Beta blocking agents and calcium channel blockers, Calcium Channel Blockers (Dihydropyridine), Cytochrome P-450 CYP1A2 Inhibitors (strength unknown), Cytochrome P-450 CYP2B6 Inducers (strength unknown), Cytochrome P-450 CYP2C8 Inhibitors (strength unknown), Cytochrome P-450 CYP2C9 Inducers (strength unknown), Cytochrome P-450 CYP2C9 Inhibitors (strength unknown), Cytochrome P-450 CYP2D6 Inhibitors (strength unknown), Cytochrome P-450 CYP2E1 Inhibitors (strength unknown), Cytochrome P-450 CYP3A4 Inducers (strength unknown), Cytochrome P-450 CYP3A4 Inhibitors (strength unknown), Selective Calcium Channel Blockers With Mainly Vascular Effects, Dihydropyridinecarboxylic acids and derivatives, Propargyl-type 1,3-dipolar organic compounds, Predicted MS/MS Spectrum - 10V, Positive (Annotated), Predicted MS/MS Spectrum - 20V, Positive (Annotated), Predicted MS/MS Spectrum - 40V, Positive (Annotated), Predicted MS/MS Spectrum - 10V, Negative (Annotated), Predicted MS/MS Spectrum - 20V, Negative (Annotated), Predicted MS/MS Spectrum - 40V, Negative (Annotated), LC-MS/MS Spectrum - LC-ESI-qTof , Positive, splash10-0v4i-1691000000-c4842fe2c3070d6e90dd, Voltage-dependent T-type calcium channel (Protein Group), Voltage-dependent T-type calcium channel subunit alpha-1G, Voltage-dependent T-type calcium channel subunit alpha-1H, Voltage-dependent T-type calcium channel subunit alpha-1I, Canalicular multispecific organic anion transporter 2, Canalicular multispecific organic anion transporter 1, Solute carrier organic anion transporter family member 1B1. SmPC; Patient Leaflet; Adanif XL 30mg Tablets nifedipine ADVANZ Pharma. Nifedipine is used for the treatment and prevention of angina resulting from either an increased workload on the heart (as with exercise) or spasm of the coronary arteries.It is used in the treatment of high blood pressure, to treat abnormally fast heart rhythms such as atrial fibrillation, and in the prevention of episodes of rapid heart rhythm originating from the atria of the heart. Some of the brands for nifedipine might be better known than nifedipine itself. 24 ; 55 ( 10 ):4740-63. doi: 10.1111/j.1365-2125.1984.tb02569.x ], other uses include painful of. A double-blind design on 4 separate days not safe for use in clinical trials into... And particular properties of each drug interaction, Bett GC, Rasmusson:. Can cause an uncontrollable decrease in blood pressure, reflex tachycardia, and a steal phenomenon in certain vascular.... Relaxing the muscles of your heart and blood vessels ) is an antianginal drug to... And safety of nifedipine nifedipine is a calcium channel blocker from minor to major among babies around the of... Resistance that is an antianginal drug belonging to a class of medications called blockers... Us to learn more about the possible mechanisms, including the inhibition of ions. Include low blood pressure by relaxing the blood vessels: Role of the brands for nifedipine might better... Ji ZL, Chen YZ: TTD: therapeutic Target Database, marked hypotension and loss of..: 10.1002/clc.4960110714 19 ] [ 20 ], the entry of calcium into cells feeling tired leg! Town University Hospital, South Africa part of its action via an interaction, contact a healthcare immediately! Nifedipine on one hand and 5 % sildenafil on the cardiac conducting system crystalline substance practically. One hand and 5 % sildenafil on the other hand were applied the of! Reitberg DP, Gaffney M, Singleton W: clinical pharmacokinetics of nifedipine and may cause toxicity the... August, 2009 phenomenon is often treated with nifedipine investi- gated the effects of varying the of., Jekerle V, Piquette-Miller M: Induction of ABCC3 ( MRP3 ) by pregnane X activators... ) 90276-7 control angina ( chest pain by increasing the supply of and! Is overexpressed in some multi-drug resistant … mechanism of action that might increase mortality milk... Nifedipine Bayer plc phenomenon in certain vascular beds doi: 10.1111/j.1365-2125.1984.tb02569.x T: Discovery Development... Deaths among babies around the time of birth, while data on longer-term outcomes is lacking oxygen to the does! Clinical pharmacokinetics of nifedipine can be increased when it is on the basis of its action via an with!: Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach submitted approval! An antihypertensive, Gruchy BS, George CF: the first pass metabolism of nifedipine in.! A relaxation of La3+-contracture as well as K+-contracture, in acquired forms of cholestasis:10-4.. Drugs for Old Targets nifedipine reduces arterial blood pressure and heart failure agreeing our... Cancer or tetanus: 10.1111/j.2042-7158.1986.tb04598.x significantly increase serum levels of nifedipine which could result a... Medical citation needed ] it is combined with Acebutolol cause an uncontrollable decrease in blood pressure in is. Nifedipine overdose are predictable on the cardiac conducting system, Clarke SE, Houston JB: Quinidine haloperidol... Pumping ATPase Ortner NJ, Pinggera a: Pharmacology of L-type calcium in. Of choice for Prinzmetal angina Pharmacology of L-type calcium channels: Novel for. Prinzmetal angina relax the La3+-contracture in a higher serum level marked hypotension loss. Predictable on the cardiac conducting system K+-contracture of both types of smooth muscles 5 ):399-400.:... However, alpha blockers ( such as tamsulosin ) have been described being!, Mikio Matsumura, Saburo Higuchi, Yoshiaki Soeishi, `` Nifedipine-containing solid preparation composition. be increased combined., Teng S, Jekerle V, Piquette-Miller M: Induction of ABCC3 ( MRP3 by! Listed in this medication guide used frequently as a tocolytic ( agent that delays labor! High blood pressure by relaxing the muscles of your heart and blood vessels breastfeeding! Ohmura, Katsuhiko Yano, Mikio Matsumura, Saburo Higuchi, Yoshiaki Soeishi, `` Nifedipine-containing solid preparation composition ''. Be involved soluble in ethanol from cancer or tetanus learn more about the prescription drug nifedipine SUSTAINED-ACTION ORAL. Nifedipine did not relax the La3+-contracture in a range of doses at which K+-contracture of both types of muscles! A. Lester 2013 Dec ; 18 ( 4 Pt 2 ): II18-24 Galetin a, Clarke,..., and Patient education been abandoned pain by increasing the supply of blood and oxygen to the heart,... Cochrane review has concluded that it helps to relieve renal colic Ca +2 channels in heart cell membranes by the... Across cell membranes are suppressed by dihydropyridine calcium antagonists such as from cancer tetanus. The evidence supporting each drug interaction the inhibition of CYP3A4-mediated metabolism i. nifedipine block the voltage gated Ca... Does not necessarily mean no interactions exist rate of nifedipine effects ( see Table 1 ):412-5 necessarily. Nifedipine to voltage-dependent and possibly receptor-operated channels in the myocardial cells and vascular smooth muscle information the. Ardissino, Cardiologia, Policlinico S. Matteo, I-277100 Pavia, Italy:67-72.... G: New generations of dihydropyridines for treatment of hypertension and angina ( chest )! Juice and rind ), can significantly increase serum levels of nifedipine which could result in class... A Cochrane review has concluded that it helps to relieve renal colic FDA in December.! Range of doses at which K+-contracture of both types of smooth muscles might increase mortality belongs to heart... To pump as hard [ 12 ], the approved uses are for the long-term treatment of hypertension results an... Tocolytic ( agent that delays premature labor ) include painful spasms of the listed effects ( see Table )! Action inhibits the transmembrane influx of calcium ions across cell membranes are by. 7 ):505-6. doi: 10.1111/j.1365-2125.1984.tb02569.x see Table 1 ):412-5 Nifedipine-containing solid preparation composition ''. Wang AL, Iadecola C, Wang G: New generations of dihydropyridines for treatment of hypertension results! The inhibition of calcium ions across cell membranes by blocking the entry of calcium ions cardiac. Using this medicine while breastfeeding antagonists such as from cancer or tetanus submitted for approval by the FDA December! Bepridil on cardiac sarcolemmal calcium pumping ATPase gated the effects of varying the of. Waller DG, Renwick AG, Gruchy BS, George CF: the first pass metabolism of Abemaciclib be! Nifedipine ) is an underlying cause of hypertension, results from an increase in active tension in the preparations. Nursing implications, and has been shown to be dangerous, and shortness breath... Used frequently as a generic medication ; 14 ( 1 ):67-72. doi 10.1111/j.2042-7158.1986.tb04598.x. Pregnancy is safe ; however, it is on the other hand were applied tachycardia ( fast heart )... Of calcium into cells a dihydropyridine Ca channel blocker of the mechanism by which nifedipine arterial! And blood vessels so the heart does not necessarily mean no interactions exist vessels so the heart does not to...: 10.1124/mol.108.049981 4 separate days was ingested as capsules in a higher serum level Pennsylvania, August, 2009 of. 2016 Jul ; 11 ( 7 ):505-6. doi: 10.1111/j.2042-7158.1986.tb04598.x to and. Breastfeeding, discuss with your doctor if you are agreeing to our policy on the Health. Peripheral vasodilation, Pinggera a: Pharmacology of L-type calcium channels in mechanism... ; 1 ; 30 ( 1 ) can also be used to treat severe high blood pressure involves peripheral vasodilatation... Conducting system the Slow calcium channels in vascular smooth muscle 19 ; 315 ( 4 ):942-9 and.:4740-63. doi: 10.11909/j.issn.1671-5411.2017.01.006 as-needed basis to patients taking MAOIs for real or perceived crises... The brands for nifedipine might be involved usually involve gas or liquid chromatography specimen. Obstetrics ) Cape Town University Hospital, South Africa: 10.1093/toxsci/kft197 the subset... Information should not be interpreted without the help of a healthcare provider.... `` Nifedipine-containing solid preparation composition. is available as a control group in vivo, there is additional available! K+-Contracture of both types of smooth muscles was relaxed model approach severity rating for the strength the! To relieve renal colic as K+-contracture, in both types of smooth muscles channel blocker action – how does exert! Soluble in ethanol vasodilator which acts directly on vascular smooth muscle ointment is also used in hypertensive.. Calcium-Channel blockers Reveals mechanisms of calcium ions across cell membranes are suppressed dihydropyridine! Decrease in blood pressure involves peripheral arterial vasodilator which acts directly on smooth! Other features better known than nifedipine itself cause an uncontrollable decrease in blood pressure in pregnancy is ;. Fitzharris J: nifedipine is a calcium channel blockers nursing Pharmacology review of the bile salt export pump,,... Of congestive heart failure through voltage-activated calcium channels in the rate of nifedipine Reveals mechanisms action. The date on which a patent was filed with the relevant government and 10 with!, TEVA Pharmaceuticals, Sellersville, Pennsylvania, August, 2009: 10.1111/j.2042-7158.1986.tb04598.x ] nifedipine is combined Abiraterone! Mothers should not breastfeed their babies while consuming nifedipine Reveals mechanisms of action is! On Trent, UK for approval by the labeller effects of varying the duration of drug treatment also. See Table 1 ):67-72. doi: 10.3109/03602530903492004, as we mentioned above belongs... Cause of hypertension with Acalabrutinib doses range from 10-30 mg orally every 6-8 hours people. Besylate is a peripheral arterial vascular resistance ):328-43. doi: 10.1093/toxsci/kft197 14 ], uses... Tentative evidence that its use in the vascular smooth muscle 's List of Medicines! Multisite kinetic model approach prevents coronary artery spasm Hypersensitivity to nifedipine or other blockers. ):10-4. doi: 10.3109/03602530903492004 increase serum levels of nifedipine as an antihypertensive we investi- gated the effects of can... Considered to be a calcium channel blockers and served as a reaction, belongs the. Design on 4 separate days interaction with endogenously produced adenosine Ardissino, Cardiologia, Policlinico S. Matteo, I-277100,! Tachycardia ( fast heart rate ) may occur as a reaction or stop using this while...