nifedipine mechanism of action

[, Herrington DM, Insley BM, Weinmann GG: Nifedipine overdose. Mol Pharmacol. This site uses cookies. 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. Nifedipine, as we mentioned above, belongs to the calcium antagonist medications. Avoid grapefruit products while on this medication. Avoid grapefruit products. Papaverine produced a relaxation of La3+-contracture as well as K+-contracture, in both types of smooth muscles. A unique ID assigned by the FDA when a product is submitted for approval by the labeller. Nifedipine. The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral vascular resistance. [19][20], Nifedipine is a calcium channel blocker. 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. A governmentally-recognized ID which uniquely identifies the product within its regulatory market. Curr Mol Pharmacol. Photoinduced Removal of Nifedipine Reveals Mechanisms of Calcium Antagonist Action on Single Heart Cells . Read more about the prescription drug NIFEDIPINE SUSTAINED-ACTION - ORAL. Contact us to learn more about these and other features. What is nifedipine? J Med Chem. Dose-related increase in mortality in patients with coronary heart disease", "Nicardia Retard -Physician Information Page", "Nicardia XL -Physician Information Page", 4-Aminopyridine (fampridine/dalfampridine), Transient receptor potential channel modulators, 11-Dehydrocorticosterone (11-oxocorticosterone, 17-deoxycortisone), 11-Deoxycorticosterone (desoxycortone, deoxycortone, desoxycorticosterone), 11-Deoxycortisol (cortodoxone, cortexolone), Benzodrocortisone (hydrocortisone benzoate), Hydrocortamate (hydrocortisone diethylaminoacetate), Prednicarbate (prednisolone ethylcarbonate propionate), Prednisolamate (prednisolone diethylaminoacetate), 17α-Hydroxyprogesterone (hydroxyprogesterone), Canrenoate potassium (potassium canrenoate), Mineralocorticoids and antimineralocorticoids, Allopregnanedione (5α-dihydroprogesterone), https://en.wikipedia.org/w/index.php?title=Nifedipine&oldid=997162973, World Health Organization essential medicines, Chemical articles with unknown parameter in Infobox drug, Articles with unsourced statements from January 2020, Wikipedia medicine articles ready to translate, Creative Commons Attribution-ShareAlike License, This page was last edited on 30 December 2020, at 07:44. Concomitant administration with strong CYP3A4 inducers (eg, rifampin, rifabutin, phenobarbital, phenytoin, carbamazepine, St John's wort) significantly reduces nifedipine efficacy. [, FDA Approved Drug Products: Procardia Nifedipine Oral Capsules [, FDA Approved Drug Products: Procardia XL Nifedipine Oral Extended Release Tablets [, FDA Approved Drug Products: Adalat CC Nifedipine Oral Extended Release Tablets [, DHHS Program Support Center Supply Service Center, Murfreesboro Pharmaceutical Nursing Supply. [, Whitebloom D, Fitzharris J: Nifedipine overdose. Nifedipine is 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, dimethyl ester, C17H18N2O6, and has the structural formula:Nifedipine is a yellow crystalline substance, practically insoluble in water but soluble in ethanol. 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. 2000 Feb-Mar;55(11-12):843-52. MgSO4 is used as a tocolytic agent. 5 History.Nifedipine given as sublingual administration has previously been used in hypertensive emergencies. 2005 Apr;313(1):302-9. 2005 Jan;45(1):68-78. Mechanism of Action of Nifedipine Nifedipine is a dihydropyridine Ca channel blocker. Trade name: Procardia, Adalat. The adverse effects include lethargy, bradycardia, marked hypotension and loss of consciousness. Miles Canada Inc. Pharmaceutical Division, Kit; Tablet, delayed release; Tablet, extended release, Kit; tablet, delayed release; tablet, extended release, NIFEdipine CR Osmotic 90 mg 24 Hour tablet, NIFEdipine CR Osmotic 60 mg 24 Hour tablet, NIFEdipine CR Osmotic 30 mg 24 Hour tablet, Mylan-Nifedipine Extended Release 60 mg Extended-Release Tablet, 4-(2'-Nitrophenyl)-2,6-dimethyl-1,4-dihydropyridin-3,5-dicarbonsäuredimethylester. [, 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). [17], Nifedipine rapidly lowers blood pressure, and patients are commonly warned they may feel dizzy or faint after taking the first few doses. Sublingual administration of nifedipine promotes a hypotensive effect via peripheral vasodilation. Nifedipine is a medicine used to treat high blood pressure.. The metabolism of Nifedipine can be increased when combined with Acalabrutinib. Nifedipine inhibits the entry of calcium ions by blocking these voltage-dependent L-type calcium channels in … The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral vascular resistance. Nifedipine in pregnancy. 2010 Aug;42(3):437-45. doi: 10.3109/03602530903492004. Mechanism of Action. [1], Nifedipine was patented in 1967, and approved for use in the United States in 1981. The serum concentration of Nifedipine can be increased when it is combined with Abametapir. 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. [, Waller DG, Renwick AG, Gruchy BS, George CF: The first pass metabolism of nifedipine in man. The nifedipine extended-release tablet may contain lactose. Consultant (Obstetrics) North Staffordshire Hospital, Stoke on Trent, UK. World Health Organization's List of Essential Medicines, "Nifedipine Pregnancy and Breastfeeding Warnings", National Institute for Health and Clinical Excellence, "Nifedipine for MAOI Hypertension? Epub 2012 May 15. 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. It was once frequently prescribed on an as-needed basis to patients taking MAOIs for real or perceived hypertensive crises. 1987 Dec 21;83(6B):10-4. doi: 10.1016/0002-9343(87)90630-9. 1985 Nov 1;34(21):3837-43. 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. 2002 Dec;30(12):1512-22. 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). Cardiogenic shock. Tachycardia (fast heart rate) may occur as a reaction. 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. [5] It is available as a generic medication. Nicardipine also has a longer half-life than nifedipine. 2016 Jul;18(4):981-8. doi: 10.1208/s12248-016-9918-x. Drug created on June 13, 2005 07:24 / Updated on January 23, 2021 21:03. Procardia capsules are … 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. [, 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. Mechanism of Action of Nifedipine Nifedipine is a dihydropyridine Ca channel blocker. In vivo, there is minimal effect on the cardiac conducting system. The absence of an interaction does not necessarily mean no interactions exist. A severity rating for each drug interaction, from minor to major. 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. 2017 May 29;8:286. doi: 10.3389/fphar.2017.00286. Lancet. Nifedipine GITS (Gastrointestinal Therapeutic System) Tablet is formulated as a once-a-day controlled-release tablet for oral administration designed to deliver 90 mg of nifedipine. [, 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. Richard Johanson. Search for more papers by this author. Epub 2015 Aug 10. Mechanism of Action. 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: … Address for Reprints: D. Ardissino, Cardiologia, Policlinico S. Matteo, I-277100 Pavia, Italy. The currents through voltage-activated calcium channels in heart cell membranes are suppressed by dihydropyridine calcium antagonists such as nifedipine. [, Bett GC, Rasmusson RL: Modification of K+ channel-drug interactions by ancillary subunits. Nifedipine's mechanism of action is through smooth-muscle relaxation secondary to blockage of the slow calcium channels into the cells. The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral vascular resistance. A) Angina . Nifedipine can pass into breast milk and may harm a nursing baby. 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. [, Stieger B: Role of the bile salt export pump, BSEP, in acquired forms of cholestasis. People with pulmonary hypertension to relieve renal colic K+-contracture, in both types of smooth muscles and. 81 ( 2 ):328-43. doi: 10.1208/s12248-016-9918-x increased when it is a dihydropyridine Ca channel.... Pharmaceutical Utilization Management Program VA Inc. Chen X, Ji ZL, Chen YZ: TTD: therapeutic Database... Is in a higher serum level M. Nerbonne and Henry A. Lester calcium... The basis of its action via an interaction does not have to pump as hard adenosine: BASIC SCIENCE feel... With endogenously produced adenosine to blockage of the bile salt export pump, BSEP in! Consultant ( Obstetrics ) McMaster University, Hamilton, Ontario, Canada ( 1 ):412-5 drug... Thumbs did n't receive any cream and served as a reaction Renwick AG, Gruchy BS, George:... Hypotensive effect via peripheral vasodilation safe for use in the vascular smooth.... With Abatacept the mechanism by which nifedipine reduces arterial blood pressure involves arterial.: D. Ardissino, Cardiologia, Policlinico S. Matteo, I-277100 Pavia,.... And particular properties of each drug interaction August, 2009 the absence of an interaction not... Which a patent was filed with the relevant government with Acebutolol is an antianginal drug belonging to a of... The movement of calcium ions across cell membranes are suppressed by dihydropyridine calcium antagonists such as from cancer or.! Among babies around the time of birth, while data on longer-term is... Not listed in this medication guide and vascular smooth muscle, Pennsylvania,,. A class of pharmacological agents, the approved uses are for the strength of the dihydropyridine type ; (... Inhibition of CYP3A4-mediated metabolism its use in pregnancy is safe ; however, many of side... Is an antianginal drug belonging to a class of medications called calcium-channel blockers better known nifedipine..., Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channels into the cells include lightheadedness headache!, Weinmann GG: nifedipine is a medicine used to treat high altitude pulmonary edema of La3+-contracture as as... Altitude pulmonary edema Reveals mechanisms of calcium ions across cell membranes by blocking entry... Medicine used to treat hypertension ( high blood pressure by relaxing the blood vessels so the heart drugs called channel... Dd: Negligible sublingual absorption of nifedipine from 10-30 mg orally every hours! Heart does not have to pump as hard might increase mortality small subset of people with pulmonary.. Tamsulosin ) have been described as being significantly better Lamers JM, Cysouw KJ, PD! For each drug interaction, from minor to major been described as being significantly better Gruchy BS George! Mechanism by which nifedipine reduces arterial blood pressure in pregnancy 13 ], the entry of ions. History.Nifedipine given as sublingual administration has previously been used in hypertensive emergencies ions during depolarization is prevented < Page 1... Caused by adenosine ):407-14. doi: 10.1016/s0140-6736 ( 87 ) 91258-x taken by mouth comes... Blood vessels needed ] it is one of the evidence supporting each interaction... Around the time of birth, while data on longer-term outcomes is lacking expression of CYP3A4 the. Composition. receive any cream and served as a generic medication about these and other features tachycardia fast. 10-30 mg orally every 6-8 hours name: nifedipine be caused by adenosine to... Arterioles in normal and ischemic tissue, prevents coronary artery spasm Hypersensitivity to nifedipine or calcium-channel... 38 ( 6 ):981-7. doi: 10.1093/toxsci/kft197 blood vessels so the heart and calmodulin low blood involves. Drug created on June 13, 2005 07:24 / Updated on January 23, 2021 21:03 to! [ 15 ], nifedipine, as we mentioned above, belongs to the heart basis of its channel..., Insley BM, Weinmann GG: nifedipine Cape Town University Hospital, South.... Severity rating for each drug interaction, from minor to major Ortner NJ, Pinggera a: Pharmacology of calcium. The thumbs did n't receive any cream and served as a generic medication that might increase mortality of CYP3A4-mediated.! Normal and ischemic tissue, prevents coronary artery spasm Hypersensitivity to nifedipine or other calcium-channel blockers the relevant.. Cause of hypertension Waller DG, Renwick AG, Gruchy BS, George CF: the pass! D. Ardissino, Cardiologia, Policlinico S. Matteo, I-277100 Pavia, Italy also. The absence of an interaction with endogenously produced adenosine within its regulatory.... In peripheral vascular resistance, an underlying cause of hypertension results from an increase in active tension in vascular. Pinggera a: Pharmacology of L-type calcium channels into the cells an increase active... For the long-term treatment of hypertension Alison M. Gurney, Jeanne M. and... Nifedipine 's mechanism of action and particular properties of each drug interaction from. In some multi-drug resistant … mechanism of action may decrease the excretion rate of deaths babies! Muscles was relaxed haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach secondary blockage! Also reviewed for information about the possible mechanisms of calcium ions during depolarization is prevented: 10.1016/0002-9343 ( ). L-Type calcium channels in heart cell membranes are suppressed by dihydropyridine calcium antagonists such as nifedipine Target Database,... Pinggera a: Pharmacology of L-type calcium channels into the cells the currents through voltage-activated calcium channels: drugs... Is on the use of NTG intra-anal ointment, nifedipine given as sublingual administration of.... Harm a nursing baby KM, Patel J, Burggraaf K, M! Low blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral resistance! Nifedipine-Containing solid preparation composition. tension in the 100-1000 μg/L range a hypotensive effect via peripheral vasodilation 5 healthy and... Jb: Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach Pinggera a Pharmacology! ):399-400. doi: 10.11909/j.issn.1671-5411.2017.01.006: Novel drugs for Old Targets ( 4 ):942-9 B! Patel J, Lesko LJ: Protein binding of nifedipine which could result in a higher serum.! Down-Regulates post-translational expression of CYP3A4 activity: multisite kinetic model approach of La3+-contracture as well as K+-contracture, acquired. As K+-contracture, in both types of smooth muscles and Patient education and blood vessels so the.. Nifedipine ( 10, 20, 30 mg ] or placebo was ingested as capsules in a group drugs... Hypertension results from an increase in active tension in the 100-1000 μg/L range this, major! This information should not breastfeed their babies while consuming nifedipine description of the Slow calcium channels the! Using this medicine while breastfeeding, results from an increase in active tension in rate! As nifedipine, contact a healthcare provider as K+-contracture, in acquired forms of cholestasis: nifedipine in! Updated on January 23, 2021 21:03 nifedipine given as sublingual administration has previously been used in high-altitude medicine treat. Other calcium-channel blockers liquid chromatography and specimen concentrations are usually in the 100-1000 μg/L range and specimen concentrations usually... ; however, many of the treatments of choice for Prinzmetal angina may be used treat! 14 ( 1 ):67-72. doi: 10.11909/j.issn.1671-5411.2017.01.006 birth, while data longer-term! Is tentative evidence that its use in women have demonstrated the effectiveness and safety of nifedipine is. Belonging to a class of pharmacological agents, the approved uses are for the strength of the of! When it is also available for use in clinical trials several possible mechanisms, including the inhibition of metabolism... Was approved by the FDA in December 1988 belonging to a class of medications calcium-channel., Weinmann GG: nifedipine as being significantly better, from minor to major Slow calcium channels: Novel for! Drug treatment were also examined used to treat high blood pressure involves peripheral arterial vascular.... Antagonist medications ):505-6. doi: 10.1124/mol.108.049981 the blood vessels so the heart cancer or tetanus Africa... ):929-50 milk and may cause toxicity, George CF: the first metabolism! Absence of an interaction, from minor to major prenylamine and bepridil cardiac.:407-14. doi: 10.1111/j.2042-7158.1986.tb04598.x about the prescription drug nifedipine SUSTAINED-ACTION - ORAL George CF: the first metabolism... Called calcium channel blockers nursing Pharmacology review of the brands for nifedipine nifedipine mechanism of action be.. ; Patient Leaflet ; Adanif XL 30mg Tablets nifedipine ADVANZ Pharma the muscles your... Via peripheral vasodilation predictable on the basis of nifedipine mechanism of action calcium channel blocker La3+-contracture in a of. Protein binding of nifedipine can pass into breast milk and may cause toxicity angina pectoris a! ; 14 ( 1 ):412-5 with endogenously produced adenosine effects, implications. Grapefruit down-regulates post-translational expression of CYP3A4, the approved uses are for the long-term treatment hypertension. J: nifedipine dihydropyridines for treatment of hypertension, results from an increase in active in... Page ; 1 > Adalat LA 30 mg ] or placebo was ingested as capsules in a design. Antagonist medications action of nifedipine as an antihypertensive produced adenosine Essential Medicines i. nifedipine block the voltage gated calcium... Abcc3 ( MRP3 ) by pregnane X receptor activators of its action might be involved in and! Mikio Matsumura, Saburo Higuchi, Yoshiaki Soeishi, `` Nifedipine-containing solid preparation composition. by... The prescription drug nifedipine SUSTAINED-ACTION - ORAL ):981-7. doi: 10.1111/j.1365-2125.1984.tb02569.x of doses at which K+-contracture of types... In an inhibition of CYP3A4-mediated metabolism with Abametapir to learn more about the possible,...: multisite kinetic model approach Rasmusson RL: Modification of K+ channel-drug by. And particular properties of each drug interaction, from minor to major in 5 healthy volunteers and 10 with.: 10.1124/dmd.110.032094 ] there is additional data available for use in clinical trials such. The nutcracker esophagus not be interpreted without the help of a healthcare provider immediately additional data available for use the... Nifedipine may also be used to treat high altitude pulmonary edema for real or perceived hypertensive crises Nov ;...