Peringatan Keamanan

The LD₅₀ of Solifenacin has yet to be determined.^L7520

Signs of overdose include severe anticholinergic effects, mental status changes, and decreased consciousness.^L7511 In case of overdose, treat patients with gastric lavage and supportive measures.^L7511 Monitor patients with an ECG.^L7511

Solifenacin

DB01591

small molecule approved

Deskripsi

Solifenacin is a competitive muscarinic receptor antagonist indicated to treat an overactive bladder with urinary incontinence, urgency, and frequency.^L7511 It has a long duration of action as it is usually taken once daily.^L7511

Solifenacin was granted FDA approval on 19 November 2004.^L7511

Struktur Molekul 2D

Berat 362.473

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 solifenacin ranges from 33-85 hours.[A181247]

Volume Distribusi The volume of distribution of solifenacin is 600L.[A181247]

Klirens (Clearance) The clearance of solifenacin is 7-14L/h and a renal clearance of 0.67-1.51L/h.[A181247]

Absorpsi

Solifenacin is well absorbed in the duodenum, jejunum, and ileum but not the stomach.^A181247 Absorption occurs via passive diffusion and so no transporters are involved.^A181247 The mean oral bioavailability of solifenacin is 88%.^A181247 The T_max of solifenacin is 3-8 hours with a C_ss of 32.3ng/mL for a 5mg oral dose and 62.9ng/mL for a 10mg oral dose.^L7511

Metabolisme

Solifenacin undergoes N-oxidation at the quinuclidin ring by cytochrome P450, though the exact enzymes are not revealed in the literature.^A181247 The tetrahydroisoquinolone ring is 4R-hydroxylated by CYP3A4, CYP1A1, and CYP2D6.^A181247 A 4R-hydroxy N-oxide metabolite is also formed by CYP3A4.^A181247 Finally, solifenacin can undergo direct glucuronidation.^A181247 Only solifenacin and the 4R-hydroxy metabolite are pharmacologically active.^A181247

Rute Eliminasi

69.2±7.8% of a radiolabelled dose is recovered in the urine, 22.5±3.3% was recovered in feces, and 0.4±7.8% was recovered in exhaled air.^A181247 18% of solifenacin is eliminated as the N-oxide metabolite, 9% is eliminated as the 4R-hydroxy N-oxide metabolite, and 8% is eliminated as the 4R-hydroxy metabolite.^A181247

Interaksi Makanan

1 Data

1. Take with or without food.

Interaksi Obat

1323 Data

Valsartan	Solifenacin may decrease the antihypertensive activities of Valsartan.
Remikiren	Solifenacin may decrease the antihypertensive activities of Remikiren.
Torasemide	Solifenacin may decrease the antihypertensive activities of Torasemide.
Guanadrel	Solifenacin may decrease the antihypertensive activities of Guanadrel.
Olmesartan	Solifenacin may decrease the antihypertensive activities of Olmesartan.
Nitroprusside	Solifenacin may decrease the antihypertensive activities of Nitroprusside.
Atenolol	Solifenacin may decrease the antihypertensive activities of Atenolol.
Minoxidil	Solifenacin may decrease the antihypertensive activities of Minoxidil.
Prazosin	Solifenacin may decrease the antihypertensive activities of Prazosin.
Fosinopril	Solifenacin may decrease the antihypertensive activities of Fosinopril.
Trandolapril	Solifenacin may decrease the antihypertensive activities of Trandolapril.
Benazepril	Solifenacin may decrease the antihypertensive activities of Benazepril.
Cyclothiazide	Solifenacin may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril	Solifenacin may decrease the antihypertensive activities of Candoxatril.
Mecamylamine	Solifenacin may decrease the antihypertensive activities of Mecamylamine.
Lisinopril	Solifenacin may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin	Solifenacin may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine	Solifenacin may decrease the antihypertensive activities of Metyrosine.
Cryptenamine	Solifenacin may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil	Solifenacin may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam	Solifenacin may decrease the antihypertensive activities of Fenoldopam.
Eprosartan	Solifenacin may decrease the antihypertensive activities of Eprosartan.
Quinapril	Solifenacin may decrease the antihypertensive activities of Quinapril.
Telmisartan	Solifenacin may decrease the antihypertensive activities of Telmisartan.
Methyldopa	Solifenacin may decrease the antihypertensive activities of Methyldopa.
Deserpidine	Solifenacin may decrease the antihypertensive activities of Deserpidine.
Pentolinium	Solifenacin may decrease the antihypertensive activities of Pentolinium.
Trimethaphan	Solifenacin may decrease the antihypertensive activities of Trimethaphan.
Diazoxide	Solifenacin may decrease the antihypertensive activities of Diazoxide.
Terazosin	Solifenacin may decrease the antihypertensive activities of Terazosin.
Captopril	Solifenacin may decrease the antihypertensive activities of Captopril.
Nadolol	Solifenacin may decrease the antihypertensive activities of Nadolol.
Epoprostenol	Solifenacin may decrease the antihypertensive activities of Epoprostenol.
Bevantolol	Solifenacin may decrease the antihypertensive activities of Bevantolol.
Practolol	Solifenacin may decrease the antihypertensive activities of Practolol.
Cilazapril	Solifenacin may decrease the antihypertensive activities of Cilazapril.
Saprisartan	Solifenacin may decrease the antihypertensive activities of Saprisartan.
Spirapril	Solifenacin may decrease the antihypertensive activities of Spirapril.
Dexpropranolol	Solifenacin may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid	Solifenacin may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine	Solifenacin may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine	Solifenacin may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril	Solifenacin may decrease the antihypertensive activities of Temocapril.
Trimazosin	Solifenacin may decrease the antihypertensive activities of Trimazosin.
Nicorandil	Solifenacin may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root	Solifenacin may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat	Solifenacin may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7	Solifenacin may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril	Solifenacin may decrease the antihypertensive activities of Imidapril.
BQ-123	Solifenacin may decrease the antihypertensive activities of BQ-123.
Landiolol	Solifenacin may decrease the antihypertensive activities of Landiolol.
Dihydralazine	Solifenacin may decrease the antihypertensive activities of Dihydralazine.
Zofenopril	Solifenacin may decrease the antihypertensive activities of Zofenopril.
Guanoxan	Solifenacin may decrease the antihypertensive activities of Guanoxan.
Delapril	Solifenacin may decrease the antihypertensive activities of Delapril.
Vincamine	Solifenacin may decrease the antihypertensive activities of Vincamine.
Linsidomine	Solifenacin may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz	Solifenacin may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine	Solifenacin may decrease the antihypertensive activities of Tolonidine.
Endralazine	Solifenacin may decrease the antihypertensive activities of Endralazine.
Esatenolol	Solifenacin may decrease the antihypertensive activities of Esatenolol.
Cadralazine	Solifenacin may decrease the antihypertensive activities of Cadralazine.
Cloranolol	Solifenacin may decrease the antihypertensive activities of Cloranolol.
Bietaserpine	Solifenacin may decrease the antihypertensive activities of Bietaserpine.
Guanazodine	Solifenacin may decrease the antihypertensive activities of Guanazodine.
Methoserpidine	Solifenacin may decrease the antihypertensive activities of Methoserpidine.
Epanolol	Solifenacin may decrease the antihypertensive activities of Epanolol.
Guanoclor	Solifenacin may decrease the antihypertensive activities of Guanoclor.
Muzolimine	Solifenacin may decrease the antihypertensive activities of Muzolimine.
Xipamide	Solifenacin may decrease the antihypertensive activities of Xipamide.
Candesartan	Solifenacin may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone	Solifenacin may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat	Solifenacin may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat	Solifenacin may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat	Solifenacin may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat	Solifenacin may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat	Solifenacin may decrease the antihypertensive activities of Quinaprilat.
Furosemide	Solifenacin may decrease the antihypertensive activities of Furosemide.
Enalapril	Solifenacin may decrease the antihypertensive activities of Enalapril.
Nisoldipine	Solifenacin may decrease the antihypertensive activities of Nisoldipine.
Bosentan	Solifenacin may decrease the antihypertensive activities of Bosentan.
Doxazosin	Solifenacin may decrease the antihypertensive activities of Doxazosin.
Bisoprolol	Solifenacin may decrease the antihypertensive activities of Bisoprolol.
Eplerenone	Solifenacin may decrease the antihypertensive activities of Eplerenone.
Tadalafil	Solifenacin may decrease the antihypertensive activities of Tadalafil.
Irbesartan	Solifenacin may decrease the antihypertensive activities of Irbesartan.
Carvedilol	Solifenacin may decrease the antihypertensive activities of Carvedilol.
Guanethidine	Solifenacin may decrease the antihypertensive activities of Guanethidine.
Hydralazine	Solifenacin may decrease the antihypertensive activities of Hydralazine.
Nebivolol	Solifenacin may decrease the antihypertensive activities of Nebivolol.
Sitaxentan	Solifenacin may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan	Solifenacin may decrease the antihypertensive activities of Ambrisentan.
Pinacidil	Solifenacin may decrease the antihypertensive activities of Pinacidil.
Riociguat	Solifenacin may decrease the antihypertensive activities of Riociguat.
Macitentan	Solifenacin may decrease the antihypertensive activities of Macitentan.
Aliskiren	Solifenacin may decrease the antihypertensive activities of Aliskiren.
Selexipag	Solifenacin may decrease the antihypertensive activities of Selexipag.
Naftopidil	Solifenacin may decrease the antihypertensive activities of Naftopidil.
Dexniguldipine	Solifenacin may decrease the antihypertensive activities of Dexniguldipine.
Amlodipine	Solifenacin may decrease the antihypertensive activities of Amlodipine.

Target Protein

Muscarinic acetylcholine receptor M3 CHRM3

Muscarinic acetylcholine receptor M2 CHRM2

Muscarinic acetylcholine receptor M4 CHRM4

Muscarinic acetylcholine receptor M5 CHRM5

Muscarinic acetylcholine receptor M1 CHRM1

Referensi & Sumber

Synthesis reference: Katsumi Saito, Masataka Katsuma, "Solifenacin transdermal preparation and method for enhancing transdermal permeation thereof." U.S. Patent US20050181031, issued August 18, 2005.

Artikel (PubMed)

PMID: 19566112
Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001.
PMID: 17011384
Kreder KJ: Solifenacin. Urol Clin North Am. 2006 Nov;33(4):483-90, ix. doi: 10.1016/j.ucl.2006.06.008.

Link

Contoh Produk & Brand

Produk: 146 • International brands: 1

Produk

Ach-solifenacin Succinate

Tablet • 5 mg • Oral • Canada • Generic • Approved
Ach-solifenacin Succinate

Tablet • 10 mg • Oral • Canada • Generic • Approved
Act Solifenacin

Tablet • 5 mg • Oral • Canada • Approved
Act Solifenacin

Tablet • 10 mg • Oral • Canada • Approved
Apo-solifenacin

Tablet • 5 mg • Oral • Canada • Generic • Approved
Apo-solifenacin

Tablet • 10 mg • Oral • Canada • Generic • Approved
Auro-solifenacin

Tablet • 5 mg • Oral • Canada • Generic • Approved
Auro-solifenacin

Tablet • 10 mg • Oral • Canada • Generic • Approved

Menampilkan 8 dari 146 produk.

International Brands

Vesikur

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.