Some of the brands for nifedipine might be better known than nifedipine itself. It has a molecular weight of 346.3. The currents through voltage-activated calcium channels in heart cell membranes are suppressed by dihydropyridine calcium antagonists such as nifedipine. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Read more about the prescription drug NIFEDIPINE SUSTAINED-ACTION - ORAL. [medical citation needed] It is also used for the small subset of people with pulmonary hypertension. It was once frequently prescribed on an as-needed basis to patients taking MAOIs for real or perceived hypertensive crises. Back to top. The thumbs didn't receive any cream and served as a control group. It controls chest pain by increasing the supply of blood and oxygen to the heart. Biochem Pharmacol. Classification Nifedipine. J Geriatr Cardiol. Trade name: Procardia, Adalat. 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. It works by relaxing the muscles of your heart and blood vessels. 1983 Jul-Aug;5(4 Pt 2):II18-24. The effects of varying the duration of drug treatment were also examined. There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. (2004). 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. 2015;8(2):110-22. [2] There is tentative evidence that its use in pregnancy is safe; however, it is not recommended during breastfeeding. Download PDF (1 MB) Abstract. The absence of an interaction does not necessarily mean no interactions exist. Antianginal, antihypertensive, calcium channel blocker. By continuing to browse the site you are agreeing to our policy on the use of cookies. Epub 2016 Apr 22. World Health Organization's List of Essential Medicines, "Nifedipine Pregnancy and Breastfeeding Warnings", National Institute for Health and Clinical Excellence, "Nifedipine for MAOI Hypertension? Procardia® (nifedipine) is an antianginal drug belonging to a class of pharmacological agents, the calcium channel blockers. [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. The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral vascular resistance. Epub 2006 May 4. [, 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. Nifedipine's mechanism of action is through smooth-muscle relaxation secondary to blockage of the slow calcium channels into the cells. [, Lee SJ, Bell DA, Coulter SJ, Ghanayem B, Goldstein JA: Recombinant CYP3A4*17 is defective in metabolizing the hypertensive drug nifedipine, and the CYP3A4*17 allele may occur on the same chromosome as CYP3A5*3, representing a new putative defective CYP3A haplotype. Mechanism of Action. Multiple studies in women have demonstrated the effectiveness and safety of nifedipine as an antihypertensive. Extended description of the mechanism of action and particular properties of each drug interaction. Mechanism Of Action Nifedipine is a peripheral arterial vasodilator which acts directly on vascular smooth muscle. C. The mechanism by which nifedipine reduces arterial blood press… Generic name: Nifedipine. Therapeutic doses range from 10-30 mg orally every 6-8 hours. Nifedipine is a dihydropyridine calcium channel blocking agent. SmPC; Patient Leaflet; Adanif XL 30mg Tablets nifedipine ADVANZ Pharma. 3. [2] Nifedipine is taken by mouth and comes in fast- and slow-release formulations. There are several possible mechanisms, including the inhibition of CYP3A4-mediated metabolism. 2015 Oct;3(5):e00161. Interestingly, however, many of the listed effects (see Table 1) can also be caused by adenosine. Epub 2013 Sep 6. [, 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. [, Chung M, Reitberg DP, Gaffney M, Singleton W: Clinical pharmacokinetics of nifedipine gastrointestinal therapeutic system. Search for more papers by this author. [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. Mechanism : Nifedipine is a calcium channel blocker and inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle. [, 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. Contraindications & Blackbox Warnings data. 2011 Feb 3;12:5. doi: 10.1186/1471-2091-12-5. Photoinduced Removal of Nifedipine Reveals Mechanisms of Calcium Antagonist Action on Single Heart Cells . 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Xenobiotica. eCollection 2017. [, 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. [, Whitebloom D, Fitzharris J: Nifedipine overdose. [, Takara K, Sakaeda T, Tanigawara Y, Nishiguchi K, Ohmoto N, Horinouchi M, Komada F, Ohnishi N, Yokoyama T, Okumura K: Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression. Nicardipine was approved by the FDA in December 1988. Abacavir may decrease the excretion rate of Nifedipine which could result in a higher serum level. Drug Metab Dispos. A unique ID assigned by the FDA when a product is submitted for approval by the labeller. Talk to your doctor before using this form of nifedipine if you have galactose intolerance, or severe problems with lactose (milk sugar). Grapefruit down-regulates post-translational expression of CYP3A4, the major metabolizing enzyme of nifedipine. 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. Dilates coronary arteries and arterioles in normal and ischemic tissue, prevents coronary artery spasm 2006;78(1):11-20. [25] 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. Consultant (Obstetrics) McMaster University, Hamilton, Ontario, Canada. A) Angina . Nifedipine, as we mentioned above, belongs to the calcium antagonist medications. Nifedipine Mechanism of action inhibits movement of calcium ions across cell membranes; calcium channel blocker; arterial and venous vasodilator; reduces preload and afterload; prevents coronary artery spasm and decreases total peripheral resistance; reduces myocardial oxygen demands; does not prolong AV nodal conduction. doi: 10.1002/prp2.161. Papaverine produced a relaxation of La3+-contracture as well as K+-contracture, in both types of smooth muscles. Epub 2015 Aug 10. It may be used to treat severe high blood pressure in pregnancy. Mol Pharmacol. Nicardipine also has a longer half-life than nifedipine. Drug Metab Rev. [, 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. NIFEDIPINE AND ADENOSINE: BASIC SCIENCE We feel nifedipine exerts part of its action via an interaction with endogenously produced adenosine. 2003 Jul;31(7):938-44. 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. 1986 May;38(5):399-400. doi: 10.1111/j.2042-7158.1986.tb04598.x. 1985 Nov 1;34(21):3837-43. Nifedipine is a calcium ion influx inhibitor (slow-channel blocker or calcium ion antagonist) and inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle. Br J Clin Pharmacol. The medicine is only available on prescription. 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. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. 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. [1], Nifedipine was patented in 1967, and approved for use in the United States in 1981. Analogous to the use of NTG intra-anal ointment, nifedipine ointment is also available for use in clinical trials. [13], Raynaud's phenomenon is often treated with nifedipine. 1998 Nov;125(5):1005-12. The adverse effects include lethargy, bradycardia, marked hypotension and loss of consciousness. Analogous to the use of NTG intra-anal ointment, nifedipine ointment is also available for use in clinical trials. The increased peripheral vascular resistance that is an underlying cause of hypertension results from an increase in active tension in the vascular smooth muscle. [, Patki KC, Von Moltke LL, Greenblatt DJ: In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. 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. It has a molecular weight of 346.3. Concomitant administration with strong CYP3A4 inducers (eg, rifampin, rifabutin, phenobarbital, phenytoin, carbamazepine, St John's wort) significantly reduces nifedipine efficacy. [, Morel N, Buryi V, Feron O, Gomez JP, Christen MO, Godfraind T: The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits. In vivo, there is minimal effect on the cardiac conducting system. Grapefruit, in all forms (e.g. 2002 Jan 1;30(1):412-5. Nifedipine dilates the main coronary arteries and coronary arterioles, both in normal and Calcium-channel blocker; inhibits transmembrane influx of extracellular calcium ions across myocardial and vascular smooth muscle cell membranes without changing serum calcium concentrations; this results in inhibition of cardiac and vascular smooth muscle contraction, thereby dilating main coronary and systemic arteries 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,