Peringatan Keamanan

Symptoms of overdose include excessive peripheral vasodilation with marked hypotension and possibly bradycardia. Oral rat LD50 is 1050 mg/kg.

Felodipine

DB01023

small molecule approved investigational

Deskripsi

Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker (CCB)b. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, felodipine prevents calcium-dependent myocyte contraction and vasoconstriction. Felodipine is the most potent CCB in use and is unique in that it exhibits fluorescent activity. In addition to binding to L-type calcium channels, felodipine binds to a number of calcium-binding proteins, exhibits competitive antagonism of the mineralcorticoid receptor, inhibits the activity of calmodulin-dependent cyclic nucleotide phosphodiesterase, and blocks calcium influx through voltage-gated T-type calcium channels. Felodipine is used to treat mild to moderate essential hypertension.

Struktur Molekul 2D

Berat 384.254
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 17.5-31.5 hours in hypertensive patients; 19.1-35.9 hours in elderly hypertensive patients; 8.5-19.7 in healthy volunteers.
Volume Distribusi * 10 L/kg
Klirens (Clearance) * 0.8 L/min [Young healthy subjects]

Absorpsi

Is completely absorbed from the gastrointestinal tract; however, extensive first-pass metabolism through the portal circulation results in a low systemic availability of 15%. Bioavailability is unaffected by food.

Metabolisme

Hepatic metabolism primarily via cytochrome P450 3A4. Six metabolites with no appreciable vasodilatory effects have been identified.

Rute Eliminasi

Although higher concentrations of the metabolites are present in the plasma due to decreased urinary excretion, these are inactive. Animal studies have demonstrated that felodipine crosses the blood-brain barrier and the placenta.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1587 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Felodipine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Felodipine is combined with Levodopa.
Risperidone Felodipine may increase the hypotensive activities of Risperidone.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Felodipine which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Felodipine which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Felodipine which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Felodipine which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Felodipine which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Felodipine which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Felodipine which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Felodipine which could result in a higher serum level.
Ceritinib Felodipine may increase the bradycardic activities of Ceritinib.
Ivabradine Felodipine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Felodipine.
Alfuzosin Alfuzosin may increase the hypotensive activities of Felodipine.
Amifostine Felodipine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Felodipine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Felodipine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Felodipine.
Obinutuzumab Felodipine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Felodipine.
Rituximab Felodipine may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Felodipine.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Felodipine.
Doxapram Doxapram may decrease the antihypertensive activities of Felodipine.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Felodipine.
Naratriptan Naratriptan may decrease the antihypertensive activities of Felodipine.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Felodipine.
Dopamine Dopamine may decrease the antihypertensive activities of Felodipine.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Felodipine.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Felodipine.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Felodipine.
Amineptine Amineptine may decrease the antihypertensive activities of Felodipine.
Naluzotan Naluzotan may decrease the antihypertensive activities of Felodipine.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Felodipine.
Cinitapride Cinitapride may decrease the antihypertensive activities of Felodipine.
Tyramine Tyramine may decrease the antihypertensive activities of Felodipine.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Felodipine.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Felodipine.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Felodipine.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Felodipine.
Atipamezole Atipamezole may decrease the antihypertensive activities of Felodipine.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Felodipine.
Piclozotan Piclozotan may decrease the antihypertensive activities of Felodipine.
Idazoxan Idazoxan may decrease the antihypertensive activities of Felodipine.
Tramazoline Tramazoline may decrease the antihypertensive activities of Felodipine.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Felodipine.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Felodipine.
Quinupramine Quinupramine may decrease the antihypertensive activities of Felodipine.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Felodipine.
Fenozolone Fenozolone may decrease the antihypertensive activities of Felodipine.
Melitracen Melitracen may decrease the antihypertensive activities of Felodipine.
Lofepramine Lofepramine may decrease the antihypertensive activities of Felodipine.
Xenon Xenon may decrease the antihypertensive activities of Felodipine.
Iprindole Iprindole may decrease the antihypertensive activities of Felodipine.
Buflomedil Buflomedil may decrease the antihypertensive activities of Felodipine.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Felodipine.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Felodipine.
Mefenorex Mefenorex may decrease the antihypertensive activities of Felodipine.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Felodipine.
Solriamfetol Solriamfetol may decrease the antihypertensive activities of Felodipine.
Midodrine Midodrine may decrease the antihypertensive activities of Felodipine.
Metergoline Metergoline may decrease the antihypertensive activities of Felodipine.
Theodrenaline Theodrenaline may decrease the antihypertensive activities of Felodipine.
Bethanidine Bethanidine may decrease the antihypertensive activities of Felodipine.
Isoetharine Isoetharine may decrease the antihypertensive activities of Felodipine.
Etomidate Etomidate may decrease the antihypertensive activities of Felodipine.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Felodipine.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Felodipine.
Metaraminol Metaraminol may decrease the antihypertensive activities of Felodipine.
Guanabenz Guanabenz may decrease the antihypertensive activities of Felodipine.
Dexmedetomidine Dexmedetomidine may decrease the antihypertensive activities of Felodipine.
Methoxamine Methoxamine may decrease the antihypertensive activities of Felodipine.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Felodipine.
Dobutamine Dobutamine may decrease the antihypertensive activities of Felodipine.
Ritodrine Ritodrine may decrease the antihypertensive activities of Felodipine.
Bitolterol Bitolterol may decrease the antihypertensive activities of Felodipine.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Felodipine.
Arbutamine Arbutamine may decrease the antihypertensive activities of Felodipine.
Fenoterol Fenoterol may decrease the antihypertensive activities of Felodipine.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Felodipine.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Felodipine.
Ephedrine Ephedrine may decrease the antihypertensive activities of Felodipine.
Procaterol Procaterol may decrease the antihypertensive activities of Felodipine.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Felodipine.
Bambuterol Bambuterol may decrease the antihypertensive activities of Felodipine.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Felodipine.
Amibegron Amibegron may decrease the antihypertensive activities of Felodipine.
Solabegron Solabegron may decrease the antihypertensive activities of Felodipine.
Droxidopa Droxidopa may decrease the antihypertensive activities of Felodipine.
Isometheptene Isometheptene may decrease the antihypertensive activities of Felodipine.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Felodipine.
Naphazoline Naphazoline may decrease the antihypertensive activities of Felodipine.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Felodipine.
Adrafinil Adrafinil may decrease the antihypertensive activities of Felodipine.
Isoxsuprine Isoxsuprine may decrease the antihypertensive activities of Felodipine.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Felodipine.
Etilefrine Etilefrine may decrease the antihypertensive activities of Felodipine.
Cirazoline Cirazoline may decrease the antihypertensive activities of Felodipine.
Synephrine Synephrine may decrease the antihypertensive activities of Felodipine.

Target Protein

Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C
Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1
Voltage-dependent L-type calcium channel subunit beta-2 CACNB2
Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D
Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S
Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H
Voltage-dependent calcium channel subunit alpha-2/delta-2 CACNA2D2
Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B
Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A
Mineralocorticoid receptor NR3C2
Troponin C, skeletal muscle TNNC2
Troponin C, slow skeletal and cardiac muscles TNNC1
Calmodulin CALM1

Referensi & Sumber

Synthesis reference: Vinay Sharma, "Preparation of micron-size felodipine particles by microfluidization." U.S. Patent US20020086061, issued July 04, 2002.
Artikel (PubMed)
  • PMID: 1782737
    Dunselman PH, Edgar B: Felodipine clinical pharmacokinetics. Clin Pharmacokinet. 1991 Dec;21(6):418-30.

Contoh Produk & Brand

Produk: 154 • International brands: 7
Produk
  • Altace Plus Felodipine 2.5mg + 2.5mg
    Tablet • - • Oral • Canada • Approved
  • Altace Plus Felodipine 5mg + 5mg
    Tablet • - • Oral • Canada • Approved
  • Apo-felodipine
    Tablet, extended release • 2.5 mg • Oral • Canada • Generic • Approved
  • Apo-felodipine
    Tablet, extended release • 5 mg • Oral • Canada • Generic • Approved
  • Apo-felodipine
    Tablet, extended release • 10 mg • Oral • Canada • Generic • Approved
  • Felodipine
    Tablet, film coated • 2.5 mg/1 • Oral • US • Generic • Approved
  • Felodipine
    Tablet, film coated, extended release • 5 mg/1 • Oral • US • Generic • Approved
  • Felodipine
    Tablet, film coated, extended release • 10 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 154 produk.
International Brands
  • Felodur ER
  • Felogard
  • Penedil
  • Plendil Depottab — AstraZeneca
  • Plendil ER — AstraZeneca
  • Plendil Retard — AstraZeneca
  • Splendil

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul