Peringatan Keamanan

Symptoms of overdose include lethargy, sinus tachycardia, and transient hypotension. Significant lethality was observed in mice given oral doses of over 200 mg/kg and rabbits given about 50 mg/kg of isradipine. Rats tolerated doses of over 2000 mg/kg without effects on survival.

Isradipine

DB00270

small molecule approved investigational

Deskripsi

Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. It is structurally related to felodipine, nifedipine, and nimodipine and is the most potent calcium-channel blocking agent of the DHP class. Isradipine binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and arterial smooth muscle cells. It exhibits greater selectivity towards arterial smooth muscle cells owing to alternative splicing of the alpha-1 subunit of the channel and increased prevalence of inactive channels in smooth muscle cells. Isradipine may be used to treat mild to moderate essential hypertension.

Struktur Molekul 2D

Berat 371.3871
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 8 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Isradipine is 90%-95% absorbed and is subject to extensive first-pass metabolism, resulting in a bioavailability of about 15%-24%.

Metabolisme

Hepatic. Completely metabolized prior to excretion and no unchanged drug is detected in the urine.

Rute Eliminasi

Approximately 60% to 65% of an administered dose is excreted in the urine and 25% to 30% in the feces.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

2036 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Isradipine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Isradipine is combined with Levodopa.
Risperidone Isradipine may increase the hypotensive activities of Risperidone.
Troglitazone Troglitazone may decrease the excretion rate of Isradipine which could result in a higher serum level.
Reserpine Reserpine may decrease the excretion rate of Isradipine which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Isradipine which could result in a higher serum level.
Chlorpromazine Chlorpromazine may decrease the excretion rate of Isradipine which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Isradipine which could result in a higher serum level.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Isradipine which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Isradipine which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Isradipine which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Isradipine which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Isradipine which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Isradipine which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Isradipine which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Isradipine which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Isradipine which could result in a higher serum level.
Pralsetinib The serum concentration of Pralsetinib can be increased when it is combined with Isradipine.
Ceritinib Isradipine may increase the bradycardic activities of Ceritinib.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Isradipine.
Amifostine Isradipine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Isradipine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Isradipine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Isradipine.
Obinutuzumab Isradipine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Isradipine.
Rituximab Isradipine may increase the hypotensive activities of Rituximab.
Isoetharine Isoetharine may decrease the antihypertensive activities of Isradipine.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Isradipine.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Isradipine.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Isradipine.
Doxapram Doxapram may decrease the antihypertensive activities of Isradipine.
Metaraminol Metaraminol may decrease the antihypertensive activities of Isradipine.
Methoxamine Methoxamine may decrease the antihypertensive activities of Isradipine.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Isradipine.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Isradipine.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Isradipine.
Ritodrine Ritodrine may decrease the antihypertensive activities of Isradipine.
Bitolterol Bitolterol may decrease the antihypertensive activities of Isradipine.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Isradipine.
Naratriptan Naratriptan may decrease the antihypertensive activities of Isradipine.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Isradipine.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Isradipine.
Arbutamine Arbutamine may decrease the antihypertensive activities of Isradipine.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Isradipine.
Fenoterol Fenoterol may decrease the antihypertensive activities of Isradipine.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Isradipine.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Isradipine.
Ephedrine Ephedrine may decrease the antihypertensive activities of Isradipine.
Mephentermine Mephentermine may decrease the antihypertensive activities of Isradipine.
Procaterol Procaterol may decrease the antihypertensive activities of Isradipine.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Isradipine.
Bambuterol Bambuterol may decrease the antihypertensive activities of Isradipine.
MMDA MMDA may decrease the antihypertensive activities of Isradipine.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Isradipine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Isradipine.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Isradipine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Isradipine.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Isradipine.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Isradipine.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Isradipine.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Isradipine.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Isradipine.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Isradipine.
Amineptine Amineptine may decrease the antihypertensive activities of Isradipine.
Amibegron Amibegron may decrease the antihypertensive activities of Isradipine.
Naluzotan Naluzotan may decrease the antihypertensive activities of Isradipine.
Solabegron Solabegron may decrease the antihypertensive activities of Isradipine.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Isradipine.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Isradipine.
Isometheptene Isometheptene may decrease the antihypertensive activities of Isradipine.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Isradipine.
Naphazoline Naphazoline may decrease the antihypertensive activities of Isradipine.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Isradipine.
Cinitapride Cinitapride may decrease the antihypertensive activities of Isradipine.
Tyramine Tyramine may decrease the antihypertensive activities of Isradipine.
Adrafinil Adrafinil may decrease the antihypertensive activities of Isradipine.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Isradipine.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Isradipine.
Etilefrine Etilefrine may decrease the antihypertensive activities of Isradipine.
Cirazoline Cirazoline may decrease the antihypertensive activities of Isradipine.
Synephrine Synephrine may decrease the antihypertensive activities of Isradipine.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Isradipine.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Isradipine.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Isradipine.
Amitraz Amitraz may decrease the antihypertensive activities of Isradipine.
Medetomidine Medetomidine may decrease the antihypertensive activities of Isradipine.
Xylazine Xylazine may decrease the antihypertensive activities of Isradipine.
Atipamezole Atipamezole may decrease the antihypertensive activities of Isradipine.
Ractopamine Ractopamine may decrease the antihypertensive activities of Isradipine.
Romifidine Romifidine may decrease the antihypertensive activities of Isradipine.
Detomidine Detomidine may decrease the antihypertensive activities of Isradipine.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Isradipine.
PF-00610355 PF-00610355 may decrease the antihypertensive activities of Isradipine.
Ritobegron Ritobegron may decrease the antihypertensive activities of Isradipine.
Abediterol Abediterol may decrease the antihypertensive activities of Isradipine.
Tulobuterol Tulobuterol may decrease the antihypertensive activities of Isradipine.
Dopexamine Dopexamine may decrease the antihypertensive activities of Isradipine.
Piclozotan Piclozotan may decrease the antihypertensive activities of Isradipine.
Idazoxan Idazoxan may decrease the antihypertensive activities of Isradipine.

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 T-type calcium channel subunit alpha-1H CACNA1H
Voltage-dependent calcium channel subunit alpha-2/delta-2 CACNA2D2
Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D
Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15512286
    Fletcher H, Roberts G, Mullings A, Forrester T: An open trial comparing isradipine with hydralazine and methyl dopa in the treatment of patients with severe pre-eclampsia. J Obstet Gynaecol. 1999 May;19(3):235-8.
  • PMID: 15858400
    Ganz M, Mokabberi R, Sica DA: Comparison of blood pressure control with amlodipine and controlled-release isradipine: an open-label, drug substitution study. J Clin Hypertens (Greenwich). 2005 Apr;7(4 Suppl 1):27-31.
  • PMID: 16751108
    Hattori T, Wang PL: Calcium antagonist isradipine-induced calcium influx through nonselective cation channels in human gingival fibroblasts. Eur J Med Res. 2006 Mar 27;11(3):93-6.
  • PMID: 15850499
    Johnson BA, Roache JD, Ait-Daoud N, Wallace C, Wells L, Dawes M, Wang Y: Effects of isradipine, a dihydropyridine-class calcium-channel antagonist, on d-methamphetamine's subjective and reinforcing effects. Int J Neuropsychopharmacol. 2005 Jun;8(2):203-13.

Contoh Produk & Brand

Produk: 25 • International brands: 4
Produk
  • DynaCirc
    Tablet, film coated, extended release • 5 mg/1 • Oral • US • Approved
  • DynaCirc
    Tablet, film coated, extended release • 10 mg/1 • Oral • US • Approved
  • DynaCirc
    Capsule • 2.5 mg/1 • Oral • US • Approved
  • DynaCirc
    Capsule • 5 mg/1 • Oral • US • Approved
  • DynaCirc
    Capsule • 2.5 mg/1 • Oral • US • Approved
  • DynaCirc
    Capsule • 5 mg/1 • Oral • US • Approved
  • Dynacirc CR
    Tablet, film coated, extended release • 5 mg/1 • Oral • US • Approved
  • Dynacirc CR
    Tablet, film coated, extended release • 5 mg/1 • Oral • US • Approved
Menampilkan 8 dari 25 produk.
International Brands
  • Clivoten — Italfarmaco (Italy)
  • Esradin — Sigma-Tau (Italy)
  • Lomir — Novartis (Austria, Brazil, Czech Republic, Denmark, Finland, Germany, Greece, Hungary, Netherlands, Norway, Poland, Russia, Sweden), Sankyo (Belgium, Italy), Daiichi Sankyo (Portugal, Switzerland), Mizar (Spain)
  • Prescal — Novartis (United Kingdom)

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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