Peringatan Keamanan

In preclinical studies, the LD50 of benidipine ranged from 87-384 mg/kg which is more than 100 times the needed dose to achieve anti-hypertensive action. There were no significant changes in histopathological heart examination. Benidipine showed no carcinogenic, antigenicity, teratogenic or mutagenic properties.^A31950

Benidipine

DB09231

small molecule experimental

Deskripsi

Benidipine has the formula 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridine-dicarboxylic acid methyl 1-(phenylmethyl)-3-piperidinyl ester hydrochloride. It is a synthetic dihydropyridine derivative that has anti-hypertensive and anti-anginal actions.^A31948 It was originated in Japan by Kyowa Hakko, it is submitted for FDA approval and it is currently available in some Asian countries like India and Japan.L1385, L1386

Struktur Molekul 2D

Berat 505.571

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

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

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of benidipine is registered to be of approximate 1 hour.[A31950]

Volume Distribusi Benidipine is highly distributed to the tissues mainly in the liver and kidneys and plasma. It does not present a high accumulation following repeated oral administrations.[A31950]

Klirens (Clearance) -

Absorpsi

Benidipine is rapidly absorbed after oral administration reaching a maximum concentration within 2 hours. The short period of time needed for maximum concentration to get reached is a particular characteristic of benidipine when compared with other calcium channel blockers. The registered maximum concentration and AUC are dose-dependent and it can go from 0.55-3.89 ng/ml and 1.04-6.7 ng.h/ml respectively when administered in a dose of 2-8 mg.^A31950

Metabolisme

Benidipine is almost completely metabolized in the liver. From different reports, it is thought that benidipine is mainly metabolized by CYP3A.^A31950 Some of the formed metabolites are N-desbenzylbenidipine and dehydrobenidipine. Analysis on the formation of metabolites has indicated that the metabolism is mainly performed by CYP3A4 and CYP3A5.^A31959

Rute Eliminasi

The percentage of urinary excretion after oral administration is of approximate 36% of the administered dose. Most of the remaining dose is excreted in feces, making bile excretion the major elimination pathway of benidipine. From the eliminated drug, none of it is expressed in the form of the unchanged drug.^A31950

Interaksi Obat

1466 Data

Ceritinib	Benidipine may increase the bradycardic activities of Ceritinib.
Ruxolitinib	Ruxolitinib may increase the bradycardic activities of Benidipine.
Brexpiprazole	The metabolism of Brexpiprazole can be decreased when combined with Benidipine.
Eliglustat	The metabolism of Eliglustat can be decreased when combined with Benidipine.
Everolimus	The metabolism of Everolimus can be decreased when combined with Benidipine.
Flibanserin	The metabolism of Flibanserin can be decreased when combined with Benidipine.
Ibrutinib	The metabolism of Ibrutinib can be decreased when combined with Benidipine.
Ivabradine	The metabolism of Ivabradine can be decreased when combined with Benidipine.
Ivacaftor	The metabolism of Ivacaftor can be decreased when combined with Benidipine.
Lurasidone	The metabolism of Lurasidone can be decreased when combined with Benidipine.
Naloxegol	The metabolism of Naloxegol can be decreased when combined with Benidipine.
Olaparib	The metabolism of Olaparib can be decreased when combined with Benidipine.
Ranolazine	The metabolism of Ranolazine can be decreased when combined with Benidipine.
Sonidegib	The metabolism of Sonidegib can be decreased when combined with Benidipine.
Avanafil	The metabolism of Avanafil can be decreased when combined with Benidipine.
Eplerenone	The metabolism of Eplerenone can be decreased when combined with Benidipine.
Cilostazol	The metabolism of Cilostazol can be decreased when combined with Benidipine.
Colchicine	The metabolism of Colchicine can be decreased when combined with Benidipine.
Fentanyl	The metabolism of Fentanyl can be decreased when combined with Benidipine.
Iloperidone	The metabolism of Iloperidone can be decreased when combined with Benidipine.
Retapamulin	The metabolism of Retapamulin can be decreased when combined with Benidipine.
Tofacitinib	The metabolism of Tofacitinib can be decreased when combined with Benidipine.
Vardenafil	The metabolism of Vardenafil can be decreased when combined with Benidipine.
Eszopiclone	The metabolism of Eszopiclone can be decreased when combined with Benidipine.
Zopiclone	The metabolism of Zopiclone can be decreased when combined with Benidipine.
Lovastatin	The metabolism of Lovastatin can be decreased when combined with Benidipine.
Cimetidine	The serum concentration of Benidipine can be increased when it is combined with Cimetidine.
Clopidogrel	The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Benidipine.
Efavirenz	The serum concentration of Benidipine can be decreased when it is combined with Efavirenz.
Melatonin	The therapeutic efficacy of Benidipine can be decreased when used in combination with Melatonin.
Nafcillin	The therapeutic efficacy of Benidipine can be decreased when used in combination with Nafcillin.
Nitroprusside	Benidipine may increase the hypotensive activities of Nitroprusside.
Dantrolene	The risk or severity of hyperkalemia can be increased when Dantrolene is combined with Benidipine.
Lithium citrate	The risk or severity of adverse effects can be increased when Benidipine is combined with Lithium citrate.
Lithium carbonate	The risk or severity of adverse effects can be increased when Benidipine is combined with Lithium carbonate.
Lithium hydroxide	The risk or severity of adverse effects can be increased when Benidipine is combined with Lithium hydroxide.
Alfuzosin	The metabolism of Alfuzosin can be decreased when combined with Benidipine.
Alprazolam	The metabolism of Alprazolam can be decreased when combined with Benidipine.
Warfarin	The serum concentration of Warfarin can be increased when it is combined with Benidipine.
Acenocoumarol	The serum concentration of Acenocoumarol can be increased when it is combined with Benidipine.
(R)-warfarin	The serum concentration of (R)-warfarin can be increased when it is combined with Benidipine.
R,S-Warfarin alcohol	The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Benidipine.
S,R-Warfarin alcohol	The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Benidipine.
(S)-Warfarin	The serum concentration of (S)-Warfarin can be increased when it is combined with Benidipine.
Midazolam	The serum concentration of Midazolam can be increased when it is combined with Benidipine.
Tacrolimus	The serum concentration of Tacrolimus can be increased when it is combined with Benidipine.
Atorvastatin	The metabolism of Atorvastatin can be decreased when combined with Benidipine.
Boceprevir	The serum concentration of Benidipine can be increased when it is combined with Boceprevir.
Tocainide	Tocainide may increase the arrhythmogenic activities of Benidipine.
Aprindine	Aprindine may increase the arrhythmogenic activities of Benidipine.
Xylometazoline	Xylometazoline may increase the arrhythmogenic activities of Benidipine.
Sparteine	Sparteine may increase the arrhythmogenic activities of Benidipine.
Fasudil	Fasudil may increase the arrhythmogenic activities of Benidipine.
Carteolol	Benidipine may increase the arrhythmogenic activities of Carteolol.
Metipranolol	Benidipine may increase the arrhythmogenic activities of Metipranolol.
Tropisetron	Benidipine may increase the arrhythmogenic activities of Tropisetron.
Spiradoline	Benidipine may increase the arrhythmogenic activities of Spiradoline.
Tiracizine	Benidipine may increase the arrhythmogenic activities of Tiracizine.
Ethacizine	Benidipine may increase the arrhythmogenic activities of Ethacizine.
Hydroquinine	Benidipine may increase the arrhythmogenic activities of Hydroquinine.
Bioallethrin	Benidipine may increase the arrhythmogenic activities of Bioallethrin.
Fosfructose	Benidipine may increase the arrhythmogenic activities of Fosfructose.
Hydroquinidine	Benidipine may increase the arrhythmogenic activities of Hydroquinidine.
SOR-C13	Benidipine may increase the arrhythmogenic activities of SOR-C13.
Digoxin	Digoxin may increase the arrhythmogenic activities of Benidipine.
Acetyldigitoxin	Acetyldigitoxin may increase the arrhythmogenic activities of Benidipine.
Deslanoside	Deslanoside may increase the arrhythmogenic activities of Benidipine.
Cymarin	Benidipine may increase the arrhythmogenic activities of Cymarin.
Metildigoxin	Benidipine may increase the arrhythmogenic activities of Metildigoxin.
Acetyldigoxin	Benidipine may increase the arrhythmogenic activities of Acetyldigoxin.
Disopyramide	Disopyramide may increase the arrhythmogenic activities of Benidipine.
Ibutilide	Ibutilide may increase the arrhythmogenic activities of Benidipine.
Procainamide	Procainamide may increase the arrhythmogenic activities of Benidipine.
Bepridil	Bepridil may increase the arrhythmogenic activities of Benidipine.
Terodiline	Benidipine may increase the arrhythmogenic activities of Terodiline.
Diltiazem	Diltiazem may increase the arrhythmogenic activities of Benidipine.
Nimodipine	Nimodipine may increase the arrhythmogenic activities of Benidipine.
Cinnarizine	Cinnarizine may increase the arrhythmogenic activities of Benidipine.
Atropine	Atropine may increase the arrhythmogenic activities of Benidipine.
Adenosine	Adenosine may increase the arrhythmogenic activities of Benidipine.
Levosimendan	Levosimendan may increase the arrhythmogenic activities of Benidipine.
Flecainide	Flecainide may increase the arrhythmogenic activities of Benidipine.
Prenylamine	Prenylamine may increase the arrhythmogenic activities of Benidipine.
Fluspirilene	Fluspirilene may increase the arrhythmogenic activities of Benidipine.
Azimilide	Azimilide may increase the arrhythmogenic activities of Benidipine.
Tedisamil	Tedisamil may increase the arrhythmogenic activities of Benidipine.
Nilvadipine	Nilvadipine may increase the arrhythmogenic activities of Benidipine.
Fendiline	Fendiline may increase the arrhythmogenic activities of Benidipine.
Eperisone	Eperisone may increase the arrhythmogenic activities of Benidipine.
Melperone	Melperone may increase the arrhythmogenic activities of Benidipine.
Simendan	Benidipine may increase the arrhythmogenic activities of Simendan.
Otilonium	Benidipine may increase the arrhythmogenic activities of Otilonium.
Nizofenone	Benidipine may increase the arrhythmogenic activities of Nizofenone.
Bunaftine	Benidipine may increase the arrhythmogenic activities of Bunaftine.
Lorcainide	Benidipine may increase the arrhythmogenic activities of Lorcainide.
Penfluridol	Benidipine may increase the arrhythmogenic activities of Penfluridol.
Dexverapamil	Benidipine may increase the arrhythmogenic activities of Dexverapamil.
Isradipine	Isradipine may increase the arrhythmogenic activities of Benidipine.
Trimethadione	Trimethadione may increase the arrhythmogenic activities of Benidipine.
Amlodipine	Amlodipine may increase the arrhythmogenic activities of Benidipine.

Target Protein

Voltage-dependent L-type calcium channel CACNA1C

Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B

Voltage-dependent T-type calcium channel CACNA1G

Referensi & Sumber

Artikel (PubMed)

PMID: 3427272
Terada K, Nakao K, Okabe K, Kitamura K, Kuriyama H: Action of the 1,4-dihydropyridine derivative, KW-3049, on the smooth muscle membrane of the rabbit mesenteric artery. Br J Pharmacol. 1987 Nov;92(3):615-25.
PMID: 16565579
Yao K, Nagashima K, Miki H: Pharmacological, pharmacokinetic, and clinical properties of benidipine hydrochloride, a novel, long-acting calcium channel blocker. J Pharmacol Sci. 2006 Apr;100(4):243-61. Epub 2006 Mar 25.
PMID: 17537876
Yoon YJ, Kim KB, Kim H, Seo KA, Kim HS, Cha IJ, Kim EY, Liu KH, Shin JG: Characterization of benidipine and its enantiomers' metabolism by human liver cytochrome P450 enzymes. Drug Metab Dispos. 2007 Sep;35(9):1518-24. doi: 10.1124/dmd.106.013607. Epub 2007 May 30.

Link

Contoh Produk & Brand

Produk: 0 • International brands: 1

International Brands

Coniel — Kyowa Hakko Kogyo

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.