Nisoldipine

DB00401

small molecule approved

Deskripsi

Nisoldipine is a 1,4-dihydropyridine calcium channel blocker. 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, nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction. Nisoldipine may be used in alone or in combination with other agents in the management of hypertension.

Struktur Molekul 2D

Berat 388.4144
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 7-12 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Relatively well absorbed into the systemic circulation with 87% of the radiolabeled drug recovered in urine and feces. The absolute bioavailability of nisoldipine is about 5%.

Metabolisme

Pre-systemic metabolism in the gut wall, and this metabolism decreases from the proximal to the distal parts of the intestine. Nisoldipine is highly metabolized; 5 major urinary metabolites have been identified. The major biotransformation pathway appears to be the hydroxylation of the isobutyl ester. A hydroxylated derivative of the side chain, present in plasma at concentrations approximately equal to the parent compound, appears to be the only active metabolite and has about 10% of the activity of the parent compound. Cytochrome P450 enzymes are believed to play a major role in the metabolism of nisoldipine. The particular isoenzyme system responsible for its metabolism has not been identified, but other dihydropyridines are metabolized by cytochrome P450 IIIA4.

Rute Eliminasi

Although 60-80% of an oral dose undergoes urinary excretion, only traces of unchanged nisoldipine are found in urine.

Interaksi Makanan

1 Data
  • 1. Avoid grapefruit products.

Interaksi Obat

1672 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Nisoldipine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Nisoldipine is combined with Levodopa.
Risperidone Nisoldipine may increase the hypotensive activities of Risperidone.
Ceritinib Nisoldipine may increase the bradycardic activities of Ceritinib.
Ivabradine Nisoldipine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Nisoldipine.
Alfuzosin Alfuzosin may increase the hypotensive activities of Nisoldipine.
Amifostine Nisoldipine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Nisoldipine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Nisoldipine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Nisoldipine.
Obinutuzumab Nisoldipine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Nisoldipine.
Rituximab Nisoldipine may increase the hypotensive activities of Rituximab.
Isoetharine Isoetharine may decrease the antihypertensive activities of Nisoldipine.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Nisoldipine.
Protriptyline Protriptyline may decrease the antihypertensive activities of Nisoldipine.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Nisoldipine.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Nisoldipine.
Doxapram Doxapram may decrease the antihypertensive activities of Nisoldipine.
Metaraminol Metaraminol may decrease the antihypertensive activities of Nisoldipine.
Methoxamine Methoxamine may decrease the antihypertensive activities of Nisoldipine.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Nisoldipine.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Nisoldipine.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Nisoldipine.
Ritodrine Ritodrine may decrease the antihypertensive activities of Nisoldipine.
Bitolterol Bitolterol may decrease the antihypertensive activities of Nisoldipine.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Nisoldipine.
Naratriptan Naratriptan may decrease the antihypertensive activities of Nisoldipine.
Formoterol Formoterol may decrease the antihypertensive activities of Nisoldipine.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Nisoldipine.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Nisoldipine.
Arbutamine Arbutamine may decrease the antihypertensive activities of Nisoldipine.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Nisoldipine.
Fenoterol Fenoterol may decrease the antihypertensive activities of Nisoldipine.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Nisoldipine.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Nisoldipine.
Ephedrine Ephedrine may decrease the antihypertensive activities of Nisoldipine.
Mephentermine Mephentermine may decrease the antihypertensive activities of Nisoldipine.
Procaterol Procaterol may decrease the antihypertensive activities of Nisoldipine.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Nisoldipine.
Bambuterol Bambuterol may decrease the antihypertensive activities of Nisoldipine.
MMDA MMDA may decrease the antihypertensive activities of Nisoldipine.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Nisoldipine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Nisoldipine.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Nisoldipine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Nisoldipine.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Nisoldipine.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Nisoldipine.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Nisoldipine.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Nisoldipine.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Nisoldipine.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Nisoldipine.
Amineptine Amineptine may decrease the antihypertensive activities of Nisoldipine.
Amibegron Amibegron may decrease the antihypertensive activities of Nisoldipine.
Naluzotan Naluzotan may decrease the antihypertensive activities of Nisoldipine.
Solabegron Solabegron may decrease the antihypertensive activities of Nisoldipine.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Nisoldipine.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Nisoldipine.
Isometheptene Isometheptene may decrease the antihypertensive activities of Nisoldipine.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Nisoldipine.
Naphazoline Naphazoline may decrease the antihypertensive activities of Nisoldipine.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Nisoldipine.
Cinitapride Cinitapride may decrease the antihypertensive activities of Nisoldipine.
Tyramine Tyramine may decrease the antihypertensive activities of Nisoldipine.
Adrafinil Adrafinil may decrease the antihypertensive activities of Nisoldipine.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Nisoldipine.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Nisoldipine.
Etilefrine Etilefrine may decrease the antihypertensive activities of Nisoldipine.
Butriptyline Butriptyline may decrease the antihypertensive activities of Nisoldipine.
Olodaterol Olodaterol may decrease the antihypertensive activities of Nisoldipine.
Dosulepin Dosulepin may decrease the antihypertensive activities of Nisoldipine.
Cirazoline Cirazoline may decrease the antihypertensive activities of Nisoldipine.
Synephrine Synephrine may decrease the antihypertensive activities of Nisoldipine.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Nisoldipine.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Nisoldipine.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Nisoldipine.
Amitraz Amitraz may decrease the antihypertensive activities of Nisoldipine.
Medetomidine Medetomidine may decrease the antihypertensive activities of Nisoldipine.
Xylazine Xylazine may decrease the antihypertensive activities of Nisoldipine.
Atipamezole Atipamezole may decrease the antihypertensive activities of Nisoldipine.
Ractopamine Ractopamine may decrease the antihypertensive activities of Nisoldipine.
Romifidine Romifidine may decrease the antihypertensive activities of Nisoldipine.
Detomidine Detomidine may decrease the antihypertensive activities of Nisoldipine.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Nisoldipine.
PF-00610355 PF-00610355 may decrease the antihypertensive activities of Nisoldipine.
Ritobegron Ritobegron may decrease the antihypertensive activities of Nisoldipine.
Abediterol Abediterol may decrease the antihypertensive activities of Nisoldipine.
Tulobuterol Tulobuterol may decrease the antihypertensive activities of Nisoldipine.
Dopexamine Dopexamine may decrease the antihypertensive activities of Nisoldipine.
Piclozotan Piclozotan may decrease the antihypertensive activities of Nisoldipine.
Idazoxan Idazoxan may decrease the antihypertensive activities of Nisoldipine.
Higenamine Higenamine may decrease the antihypertensive activities of Nisoldipine.
Reproterol Reproterol may decrease the antihypertensive activities of Nisoldipine.
Theodrenaline Theodrenaline may decrease the antihypertensive activities of Nisoldipine.
Opipramol Opipramol may decrease the antihypertensive activities of Nisoldipine.
Tramazoline Tramazoline may decrease the antihypertensive activities of Nisoldipine.
Mephedrone Mephedrone may decrease the antihypertensive activities of Nisoldipine.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Nisoldipine.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Nisoldipine.

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

Referensi & Sumber

Synthesis reference: Massimo Ferrari, Marcello Ghezzi, Manuel Alberelli, Alberto Ambrosini, "Industrial process for the synthesis of isobutyl methyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridine dicarboxylate (nisoldipine)." U.S. Patent US20050240022, issued October 27, 2005.
Artikel (PubMed)
  • PMID: 15834448
    Mielcarek J, Grobelny P, Szamburska O: The effect of beta-carotene on the photostability of nisoldipine. Methods Find Exp Clin Pharmacol. 2005 Apr;27(3):167-71.
  • PMID: 14530219
    Missan S, Zhabyeyev P, Dyachok O, Jones SE, McDonald TF: Block of cardiac delayed-rectifier and inward-rectifier K+ currents by nisoldipine. Br J Pharmacol. 2003 Nov;140(5):863-70. Epub 2003 Oct 6.
  • PMID: 11720635
    Hamilton SF, Houle LM, Thadani U: Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure. Heart Dis. 1999 Nov-Dec;1(5):279-88.

Contoh Produk & Brand

Produk: 25 • International brands: 10
Produk
  • Nisoldipine
    Tablet, film coated, extended release • 8.5 mg/1 • Oral • US • Generic • Approved
  • Nisoldipine
    Tablet, film coated, extended release • 17 mg/1 • Oral • US • Generic • Approved
  • Nisoldipine
    Tablet, film coated, extended release • 25.5 mg/1 • Oral • US • Generic • Approved
  • Nisoldipine
    Tablet, film coated, extended release • 34 mg/1 • Oral • US • Generic • Approved
  • Nisoldipine
    Tablet, film coated, extended release • 40 mg/1 • Oral • US • Generic • Approved
  • Nisoldipine
    Tablet, film coated, extended release • 8.5 mg/1 • Oral • US • Generic • Approved
  • Nisoldipine
    Tablet, film coated, extended release • 17 mg/1 • Oral • US • Generic • Approved
  • Nisoldipine
    Tablet, film coated, extended release • 25.5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 25 produk.
International Brands
  • Baymycard — Bayer
  • Baymycard RR — Bayer
  • Bo Ping — Rui Yang Pharm
  • Di Yi Xin — Tasly
  • Ji Ni Le Er — Jiankang Pharmaceutical
  • Ninobarucin — Choseido Pharmaceutical
  • Nisomynard — Yoshindo
  • Riohard — Taiyo Pharmaceutical
  • Ruidi — Nanjing Sanrui Pharmaceutical Co.
  • Syscor — Bayer

Sekuens Gen/Protein (FASTA)

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