Peringatan Keamanan

Ld50: >5 g/kg in rats, orally L1441, L1459.
Some common adverse effects include hot flashes, flushing of the face, and headache. Elevation in serum total cholesterol, ALT (SGPT), AST (SGOT) and BUN may also occur. Frequent urination, pedal edema, increased triglycerides have been found to occur in less than 0.1% of patients L1460, L1459.

Efonidipine

DB09235

small molecule experimental

Deskripsi

Efonidipine is a calcium channel blocker of the dihydropyridine class, commercialized by Shionogi & Co. (Japan). Initially, it was marketed in 1995 under the trade name, Landel. The drug has been shown to block T-type in addition to L-type calcium channels A7844, A32001. It has also been studied in atherosclerosis and acute renal failure A32001. This drug is also known as NZ-105, and several studies have been done on its pharmacokinetics in animals L1456.

Struktur Molekul 2D

Berat 631.666
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The peak plasma concentration is attained at approximately 1.5 to 3.67 hours after ingestion. The half-life is measured to be about 4 hours [L1450].
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The metabolism of efonidipine was studied in rats. The absorption ratio of radioactivity estimated from the sum of biliary and urinary excretions was found to be approximately 62% L1457. The radioactivity was high in the gastrointestinal tract and liver, followed by the adrenal glands L1457, suggesting high rates of metabolism in these regions. The unchanged drug in the plasma accounted for 47.7% of radioactivity at 2hr after ingestion, demonstrating a lower first-pass effect in comparison with other drugs in the same class. In plasma, major metabolites of NZ-105 were: N-debenzylated compound (DBZ), N-dephenylated compound (DPH), oxidative deaminated compound (AL), AL-corresponding pyridine compound (ALP), unknown metabolite M-1 and M-25. NZ-105 was metabolized by N-debenzylation, N-dephenylation, oxidative deamination, ester hydrolysis and oxidation of 1, 4-dihydropyridine ring to its corresponding pyridine L1457.

Metabolisme

It has been suggested that efonidipine is less likely to be subject to the first-pass than other members of its drug class, and and that its dihydropyridine ring is oxidized primarily after metabolism of the side chain L1443. Efonidipine is highly lipophilic and this allows for its entry into the phospholipid-rich cell membrane and reach the dihydropyridine binding site of the calcium channel targets L1446. Efonidipine is mainly metabolized in the liver. Its metabolites are N-dephenylated Efonidipine (DPH), deaminated efonidipine (AL) and N-debenzylated Efonidipine (DBZ). Both metabolites behave as calcium antagonists. In one study, the vasodilating capabilities of DBZ and DPH were about two-thirds and one-third respectively than that of the unmetabolized drug. Research suggests that the majority of the pharmacological effect after oral dosing of efonidipine hydrochloride is due to unchanged drug and its metabolites play little role in its therapeutic effect. In a study of six healthy volunteers, no significant amount of unchanged drug was excreted in urine. The urine samples collected for 24?h after oral efonidipine administration, 1.1% of the dose was excreted as deaminated-efonidipine, and 0.5% as a pyridine analogue of deaminated-efonidipine L1457.

Rute Eliminasi

Efonidipine is also referred to as NZ-105 L1456 and has been found to be mainly eliminated by the biliary system L1457.

Interaksi Obat

1728 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Efonidipine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Efonidipine is combined with Levodopa.
Risperidone Efonidipine may increase the hypotensive activities of Risperidone.
Ceritinib Efonidipine may increase the bradycardic activities of Ceritinib.
Ivabradine Efonidipine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Efonidipine.
Amifostine Efonidipine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Efonidipine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Efonidipine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Efonidipine.
Obinutuzumab Efonidipine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Efonidipine.
Rituximab Efonidipine may increase the hypotensive activities of Rituximab.
Isoetharine Isoetharine may decrease the antihypertensive activities of Efonidipine.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Efonidipine.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Efonidipine.
Doxapram Doxapram may decrease the antihypertensive activities of Efonidipine.
Metaraminol Metaraminol may decrease the antihypertensive activities of Efonidipine.
Methoxamine Methoxamine may decrease the antihypertensive activities of Efonidipine.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Efonidipine.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Efonidipine.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Efonidipine.
Ritodrine Ritodrine may decrease the antihypertensive activities of Efonidipine.
Bitolterol Bitolterol may decrease the antihypertensive activities of Efonidipine.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Efonidipine.
Naratriptan Naratriptan may decrease the antihypertensive activities of Efonidipine.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Efonidipine.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Efonidipine.
Arbutamine Arbutamine may decrease the antihypertensive activities of Efonidipine.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Efonidipine.
Fenoterol Fenoterol may decrease the antihypertensive activities of Efonidipine.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Efonidipine.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Efonidipine.
Mephentermine Mephentermine may decrease the antihypertensive activities of Efonidipine.
Procaterol Procaterol may decrease the antihypertensive activities of Efonidipine.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Efonidipine.
Bambuterol Bambuterol may decrease the antihypertensive activities of Efonidipine.
MMDA MMDA may decrease the antihypertensive activities of Efonidipine.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Efonidipine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Efonidipine.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Efonidipine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Efonidipine.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Efonidipine.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Efonidipine.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Efonidipine.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Efonidipine.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Efonidipine.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Efonidipine.
Amineptine Amineptine may decrease the antihypertensive activities of Efonidipine.
Amibegron Amibegron may decrease the antihypertensive activities of Efonidipine.
Naluzotan Naluzotan may decrease the antihypertensive activities of Efonidipine.
Solabegron Solabegron may decrease the antihypertensive activities of Efonidipine.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Efonidipine.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Efonidipine.
Isometheptene Isometheptene may decrease the antihypertensive activities of Efonidipine.
Naphazoline Naphazoline may decrease the antihypertensive activities of Efonidipine.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Efonidipine.
Cinitapride Cinitapride may decrease the antihypertensive activities of Efonidipine.
Tyramine Tyramine may decrease the antihypertensive activities of Efonidipine.
Adrafinil Adrafinil may decrease the antihypertensive activities of Efonidipine.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Efonidipine.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Efonidipine.
Etilefrine Etilefrine may decrease the antihypertensive activities of Efonidipine.
Cirazoline Cirazoline may decrease the antihypertensive activities of Efonidipine.
Synephrine Synephrine may decrease the antihypertensive activities of Efonidipine.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Efonidipine.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Efonidipine.
Amitraz Amitraz may decrease the antihypertensive activities of Efonidipine.
Medetomidine Medetomidine may decrease the antihypertensive activities of Efonidipine.
Xylazine Xylazine may decrease the antihypertensive activities of Efonidipine.
Atipamezole Atipamezole may decrease the antihypertensive activities of Efonidipine.
Ractopamine Ractopamine may decrease the antihypertensive activities of Efonidipine.
Romifidine Romifidine may decrease the antihypertensive activities of Efonidipine.
Detomidine Detomidine may decrease the antihypertensive activities of Efonidipine.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Efonidipine.
PF-00610355 PF-00610355 may decrease the antihypertensive activities of Efonidipine.
Ritobegron Ritobegron may decrease the antihypertensive activities of Efonidipine.
Abediterol Abediterol may decrease the antihypertensive activities of Efonidipine.
Tulobuterol Tulobuterol may decrease the antihypertensive activities of Efonidipine.
Dopexamine Dopexamine may decrease the antihypertensive activities of Efonidipine.
Piclozotan Piclozotan may decrease the antihypertensive activities of Efonidipine.
Idazoxan Idazoxan may decrease the antihypertensive activities of Efonidipine.
Higenamine Higenamine may decrease the antihypertensive activities of Efonidipine.
Reproterol Reproterol may decrease the antihypertensive activities of Efonidipine.
Opipramol Opipramol may decrease the antihypertensive activities of Efonidipine.
Tramazoline Tramazoline may decrease the antihypertensive activities of Efonidipine.
Mephedrone Mephedrone may decrease the antihypertensive activities of Efonidipine.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Efonidipine.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Efonidipine.
Quinupramine Quinupramine may decrease the antihypertensive activities of Efonidipine.
Octopamine Octopamine may decrease the antihypertensive activities of Efonidipine.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Efonidipine.
Fenozolone Fenozolone may decrease the antihypertensive activities of Efonidipine.
Norfenefrine Norfenefrine may decrease the antihypertensive activities of Efonidipine.
Melitracen Melitracen may decrease the antihypertensive activities of Efonidipine.
Oxyfedrine Oxyfedrine may decrease the antihypertensive activities of Efonidipine.
Lofepramine Lofepramine may decrease the antihypertensive activities of Efonidipine.
Xenon Xenon may decrease the antihypertensive activities of Efonidipine.
Iprindole Iprindole may decrease the antihypertensive activities of Efonidipine.
Buflomedil Buflomedil may decrease the antihypertensive activities of Efonidipine.

Target Protein

Voltage gated L-type calcium channel CACNA1C
Voltage-dependent calcium channel CACNG1
Voltage-dependent T-type calcium channel CACNA1G
Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G
Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H
Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I
Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12070536
    Tanaka H, Shigenobu K: Efonidipine hydrochloride: a dual blocker of L- and T-type ca(2+) channels. Cardiovasc Drug Rev. 2002 Winter;20(1):81-92.
  • PMID: 20558909
    Nakano N, Ishimitsu T, Takahashi T, Inada H, Okamura A, Ohba S, Matsuoka H: Effects of efonidipine, an L- and T-type calcium channel blocker, on the renin-angiotensin-aldosterone system in chronic hemodialysis patients. Int Heart J. 2010 May;51(3):188-92.
  • PMID: 16306803
    Hasegawa K, Wakino S, Kanda T, Yoshioka K, Tatematsu S, Homma K, Takamatsu I, Sugano N, Hayashi K: Divergent action of calcium channel blockers on ATP-binding cassette protein expression. J Cardiovasc Pharmacol. 2005 Dec;46(6):787-93.
  • PMID: 20881449
    Hayashi K, Homma K, Wakino S, Tokuyama H, Sugano N, Saruta T, Itoh H: T-type Ca channel blockade as a determinant of kidney protection. Keio J Med. 2010;59(3):84-95.
Link

Contoh Produk & Brand

Produk: 0 • International brands: 3
International Brands
  • Landel — Shionogi & Co.
  • NZ-105
  • Selefodipine

Sekuens Gen/Protein (FASTA)

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