Peringatan Keamanan

The oral LD50 in rats is 1022mg/kg and in mice is 202mg/kg.L11428

Patients experiencing an overdose may present with hypotension, sinus node dysfunction, atrioventricular node dysfunction, and reflex tachycardia.A190219,A190222 Overdose may be managed by monitoring cardiovascular and respiratory function; elevating extremities; and administering vasopressors, fluids, and calcium infusions.L11383

Nifedipine

DB01115

small molecule approved

Deskripsi

Nifedipine, or BAY a 1040, is a first generation dihydropyridine L-type calcium channel blocker, similar to nicardipine.A190210,A190273,A175390,L11383 Nifedipine was developed by Bayer and first described in the literature, along with other dihydropyridines, in 1972.A175390,A190276 Since nifedipine's development, second and third generation dihydropyridines have been developed with slower onsets and longer durations of action.A190273 The most popular of the third generation dihydropyridines is amlodipine.A190273

Nifedipine was granted FDA approval on 31 December 1981.L11383

Struktur Molekul 2D

Berat 346.3346
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half life of nifedipine is approximately 2 hours.[A190210,A190261]
Volume Distribusi 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.[A190210]
Klirens (Clearance) The total body clearance of nifedipine is 450-700mL/min.[A190210]

Absorpsi

Sublingual dosing leads to a Cmax of 10ng/mL, with a Tmax of 50min, and an AUC of 25ng\*h/mL.A190264 Oral dosing leads to a Cmax of 82ng/mL, with a Tmax of 28min, and an AUC of 152ng\*h/mL.A190264 Nifedipine is a Biopharmaceutics Classification System Class II drug, meaning it has low solubility and high intestinal permeability.A190261 It is almost completely absorbed in the gastrointestinal tract but has a bioavilability of 45-68%, partly due to first pass metabolism.A190210,A190261

Metabolisme

Nifedipine is predominantly metabolized by CYP3A4.A190204,A190261,L11383,L11389,L1245 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.A190228 Nifedipine is also minorly metabolized to dehydronifedipine.A190225

Rute Eliminasi

Nifedipine is 60-80% recovered in the urine as inactive water soluble metabolites, and the rest is eliminated in the feces as metabolites.L11389

Interaksi Makanan

4 Data
  • 1. Avoid excessive or chronic alcohol consumption.
  • 2. Avoid grapefruit products. Grapefruit down-regulates post-translational expression of CYP3A4, the major metabolizing enzyme of nifedipine. Grapefruit, in all forms (e.g. whole fruit, juice and rind), can significantly increase serum levels of nifedipine and may cause toxicity. Avoid grapefruit products while on this medication.
  • 3. Avoid natural licorice.
  • 4. Take with or without food.

Interaksi Obat

1876 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Nifedipine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Nifedipine is combined with Levodopa.
Risperidone Nifedipine may increase the hypotensive activities of Risperidone.
Olmesartan Olmesartan may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Nitrofurantoin Nitrofurantoin may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Ursodeoxycholic acid Nifedipine may decrease the excretion rate of Ursodeoxycholic acid which could result in a higher serum level.
Cholic Acid Nifedipine may decrease the excretion rate of Cholic Acid which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Letermovir The metabolism of Nifedipine can be decreased when combined with Letermovir.
Valinomycin Valinomycin may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Tinidazole Tinidazole may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Flucloxacillin Flucloxacillin may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Glipizide Glipizide may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Sulfinpyrazone Nifedipine may decrease the excretion rate of Sulfinpyrazone which could result in a higher serum level.
Pravastatin Pravastatin may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Ezetimibe Ezetimibe may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Loratadine Loratadine may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Lovastatin The metabolism of Nifedipine can be decreased when combined with Lovastatin.
Atorvastatin Atorvastatin may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Rosuvastatin Rosuvastatin may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Belantamab mafodotin Nifedipine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Ceritinib Nifedipine may increase the bradycardic activities of Ceritinib.
Ivabradine Nifedipine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Nifedipine.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Nifedipine.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Nifedipine.
Deferasirox The serum concentration of Nifedipine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Nifedipine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Nifedipine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Nifedipine can be decreased when it is combined with Teriflunomide.
Esmolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Esmolol.
Betaxolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Betaxolol.
Timolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Timolol.
Sotalol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Sotalol.
Propranolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Propranolol.
Labetalol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Labetalol.
Alprenolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Alprenolol.
Pindolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Pindolol.
Carvedilol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Carvedilol.
Propafenone The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Propafenone.
Acebutolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Acebutolol.
Nadolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Nadolol.
Bevantolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Bevantolol.
Practolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Practolol.
Penbutolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Penbutolol.
Oxprenolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Oxprenolol.
Dexpropranolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Dexpropranolol.
Celiprolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Celiprolol.
Nebivolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Nebivolol.
Bufuralol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Bufuralol.
Bopindolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Bopindolol.
Bupranolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Bupranolol.
Indenolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Indenolol.
Arotinolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Arotinolol.
Levobetaxolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Levobetaxolol.
Talinolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Talinolol.
Anisodamine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Anisodamine.
Bucindolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Bucindolol.
Esatenolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Esatenolol.
Cloranolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Cloranolol.
Mepindolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Mepindolol.
Epanolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Epanolol.
Tertatolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Tertatolol.
Bisoprolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Bisoprolol.
Landiolol The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Landiolol.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Nifedipine.
Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Nifedipine.
Cimetidine The serum concentration of Nifedipine can be increased when it is combined with Cimetidine.
Clopidogrel The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nifedipine.
Efavirenz The serum concentration of Nifedipine can be decreased when it is combined with Efavirenz.
Melatonin The therapeutic efficacy of Nifedipine can be decreased when used in combination with Melatonin.
Nafcillin The therapeutic efficacy of Nifedipine can be decreased when used in combination with Nafcillin.
Nitroprusside Nifedipine may increase the hypotensive activities of Nitroprusside.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Nifedipine.
Dantrolene The risk or severity of hyperkalemia can be increased when Dantrolene is combined with Nifedipine.
Lithium citrate The risk or severity of adverse effects can be increased when Nifedipine is combined with Lithium citrate.
Lithium carbonate The risk or severity of adverse effects can be increased when Nifedipine is combined with Lithium carbonate.
Lithium hydroxide The risk or severity of adverse effects can be increased when Nifedipine is combined with Lithium hydroxide.
Cisapride The serum concentration of Nifedipine can be increased when it is combined with Cisapride.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Nifedipine.
Perampanel The metabolism of Perampanel can be increased when combined with Nifedipine.
Warfarin The metabolism of Warfarin can be increased when combined with Nifedipine.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Nifedipine.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Nifedipine.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Nifedipine.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Nifedipine.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Nifedipine.
Mirabegron The serum concentration of Nifedipine can be increased when it is combined with Mirabegron.
Boceprevir The serum concentration of Nifedipine can be increased when it is combined with Boceprevir.
Abiraterone The serum concentration of Nifedipine can be increased when it is combined with Abiraterone.
Nicorandil Nicorandil may increase the hypotensive activities of Nifedipine.

Target Protein

Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C
Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D
Voltage-dependent L-type calcium channel subunit beta-2 CACNB2
Nuclear receptor subfamily 1 group I member 2 NR1I2
Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S
A-type voltage-gated potassium channel KCND3 KCND3
Voltage-dependent T-type calcium channel CACNA1G
Calmodulin CALM1

Referensi & Sumber

Synthesis reference: Hiroitsu Kawata, Tadayoshi Ohmura, Katsuhiko Yano, Mikio Matsumura, Saburo Higuchi, Yoshiaki Soeishi, "Nifedipine-containing solid preparation composition." U.S. Patent US4412986, issued November, 1976.
Artikel (PubMed)
  • PMID: 30725737
    Khan KM, Patel J, Schaefer TJ: Nifedipine .
  • PMID: 2872322
    Otto J, Lesko LJ: Protein binding of nifedipine. J Pharm Pharmacol. 1986 May;38(5):399-400. doi: 10.1111/j.2042-7158.1986.tb04598.x.
  • PMID: 3503594
    Chung M, Reitberg DP, Gaffney M, Singleton W: Clinical pharmacokinetics of nifedipine gastrointestinal therapeutic system. A controlled-release formulation of nifedipine. Am J Med. 1987 Dec 21;83(6B):10-4. doi: 10.1016/0002-9343(87)90630-9.
  • PMID: 3740090
    Herrington DM, Insley BM, Weinmann GG: Nifedipine overdose. Am J Med. 1986 Aug;81(2):344-6. doi: 10.1016/0002-9343(86)90276-7.
  • PMID: 3416517
    Whitebloom D, Fitzharris J: Nifedipine overdose. Clin Cardiol. 1988 Jul;11(7):505-6. doi: 10.1002/clc.4960110714.
  • PMID: 6862586
    Raemsch KD, Sommer J: Pharmacokinetics and metabolism of nifedipine. Hypertension. 1983 Jul-Aug;5(4 Pt 2):II18-24. doi: 10.1161/01.hyp.5.4pt2.ii18.
  • PMID: 6529535
    Waller DG, Renwick AG, Gruchy BS, George CF: The first pass metabolism of nifedipine in man. Br J Clin Pharmacol. 1984 Dec;18(6):951-4. doi: 10.1111/j.1365-2125.1984.tb02569.x.
  • PMID: 27106837
    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. AAPS J. 2016 Jul;18(4):981-8. doi: 10.1208/s12248-016-9918-x. Epub 2016 Apr 22.
Menampilkan 8 dari 12 artikel.

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