Peringatan Keamanan

Oral LD50 is 800 mg/kg in rats.L32393

In clinical trials, postural hypotension was the most common dose-limiting adverse event. In case of drug overdose leading to hypotension, the patient should be placed in a supine position to restore blood pressure and normalize heart rate. Further measures, such as administration of intravenous fluids, may be initiated. In case of the use of vasopressors, renal function should be monitored and supported as needed. Since silodosin is highly bound to plasma proteins, dialysis is unlikely to be beneficial.L32368

Silodosin

DB06207

small molecule approved

Deskripsi

Silodosin is a selective antagonist of alpha(?)-1 adrenergic receptors that binds to the ?1A subtype with the highest affinity. ?1-adrenergic receptors regulate smooth muscle tone in the bladder neck, prostate, and prostatic urethra: the ?1A subtype accounts for approximately 75% of ?1-adrenoceptors in the prostate.A231159

Silodosin was first approved by the FDA in October 2008 A231159 and it is also approved in Europe and Canada. Silodosin is available as oral capsules with common trade names Rapaflo and Urorec. It is indicated for the symptomatic treatment of benign prostatic hyperplasia in adults.L32368 Most commonly affecting males over the age of 40 years, benign prostatic hyperplasia is the non-malignant enlargement of the prostate gland, associated with lower urinary tract symptoms that have a negative impact on the quality of life of patients.A231159 Silodosin works by binding to ?1A-adrenoceptors with high affinity and relaxing the lower urinary tract, thereby improving urinary symptoms and alleviating bladder outlet obstruction.A231229

Struktur Molekul 2D

Berat 495.5345
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of silodosin is 13.3 ± 8.07 hours. KMD-3213G, the main metabolite of silodosin, has an extended half-life of approximately 24 hours.[L32368]
Volume Distribusi Silodosin has an apparent volume of distribution of 49.5 L.[L32368]
Klirens (Clearance) After intravenous administration, the plasma clearance of silodosin was approximately 10 L/hour. [L32368]

Absorpsi

The absolute bioavailability is approximately 32%. Following oral administration of silodosin 8 mg once daily in healthy male subjects, Cmax was 61.6 ± 27.54 ng/mL and AUC was 373.4 ± 164.94 ng x hr/mL. The Tmax was 2.6 ± 0.90 hours.L32368 Silodosin glucuronide or KMD-3213G, the main metabolite of silodosin, has an AUC three- or four fold higher than for the parent compound.A231159 A moderate fat or calorie meal reduces Cmax by 18% to 43% and AUC by 4% to 49%, as well as Tmax by about one hour. However, the US prescribing information recommends drug intake with meals to avoid the potential adverse effects associated with high plasma drug concentrations.L32368

Metabolisme

The main metabolite of silodosin is silodosin glucuronide (KMD-3213G), which is a pharmacologically active metabolite formed by direct glucuronide conjugation mediated by UDP-glucuronosyltransferase 2B7 (UGT2B7). Silodosin glucuronide reaches plasma exposure (AUC) approximately four times greater than that of silodosin. The second major metabolite, KMD-3293, is formed from dehydrogenation catalyzed by alcohol and aldehyde dehydrogenases. KMD-3293 has negligible pharmacological activity and reaches plasma exposures similar to that of silodosin. Silodosin is also metabolized by CYP3A4, which catalyzes the oxidation reaction.L32368 Other than glucuronidation, dehydrogenation, and oxidation as its main metabolic pathways, silodosin can also undergo dealkylation (KMD-3289), N-dealkylation, hydroxylation, glucosylation, and sulfate conjugation. Metabolites of silodosin can undergo a series of further metabolic pathways.A231179

Rute Eliminasi

At 10 days following oral administration of radiolabelled silodosin, about 33.5% of the dose was recovered in urine and 54.9% was recovered in feces.L32368

Interaksi Makanan

1 Data
  • 1. Take with food. A moderate fat or calorie meal decreases drug exposure as well as the risk of adverse effects.

Interaksi Obat

669 Data
Fluconazole The excretion of Silodosin can be decreased when combined with Fluconazole.
Erythromycin The excretion of Silodosin can be decreased when combined with Erythromycin.
Sildenafil The excretion of Silodosin can be decreased when combined with Sildenafil.
Reserpine The excretion of Silodosin can be decreased when combined with Reserpine.
Sorafenib The excretion of Silodosin can be decreased when combined with Sorafenib.
Loxapine The excretion of Silodosin can be decreased when combined with Loxapine.
Quinine The excretion of Silodosin can be decreased when combined with Quinine.
Ritonavir The excretion of Silodosin can be decreased when combined with Ritonavir.
Toremifene The excretion of Silodosin can be decreased when combined with Toremifene.
Simvastatin The excretion of Silodosin can be decreased when combined with Simvastatin.
Verapamil The excretion of Silodosin can be decreased when combined with Verapamil.
Tamoxifen The excretion of Silodosin can be decreased when combined with Tamoxifen.
Mifepristone The excretion of Silodosin can be decreased when combined with Mifepristone.
Vardenafil The excretion of Silodosin can be decreased when combined with Vardenafil.
Tacrolimus The excretion of Silodosin can be decreased when combined with Tacrolimus.
Conivaptan The excretion of Silodosin can be decreased when combined with Conivaptan.
Quinidine The excretion of Silodosin can be decreased when combined with Quinidine.
Zonisamide The excretion of Silodosin can be decreased when combined with Zonisamide.
Tipranavir The excretion of Silodosin can be decreased when combined with Tipranavir.
Ketoconazole The excretion of Silodosin can be decreased when combined with Ketoconazole.
Amiodarone The excretion of Silodosin can be decreased when combined with Amiodarone.
Carvedilol The excretion of Silodosin can be decreased when combined with Carvedilol.
Itraconazole The excretion of Silodosin can be decreased when combined with Itraconazole.
Propafenone The excretion of Silodosin can be decreased when combined with Propafenone.
Clarithromycin The excretion of Silodosin can be decreased when combined with Clarithromycin.
Saquinavir The excretion of Silodosin can be decreased when combined with Saquinavir.
Lapatinib The excretion of Silodosin can be decreased when combined with Lapatinib.
Paliperidone The excretion of Silodosin can be decreased when combined with Paliperidone.
Mibefradil The excretion of Silodosin can be decreased when combined with Mibefradil.
Lopinavir The excretion of Silodosin can be decreased when combined with Lopinavir.
Biricodar The excretion of Silodosin can be decreased when combined with Biricodar.
Dronedarone The excretion of Silodosin can be decreased when combined with Dronedarone.
Nilotinib The excretion of Silodosin can be decreased when combined with Nilotinib.
Elacridar The excretion of Silodosin can be decreased when combined with Elacridar.
Flibanserin The excretion of Silodosin can be decreased when combined with Flibanserin.
Vandetanib The excretion of Silodosin can be decreased when combined with Vandetanib.
Telaprevir The excretion of Silodosin can be decreased when combined with Telaprevir.
Zosuquidar The excretion of Silodosin can be decreased when combined with Zosuquidar.
Tariquidar The excretion of Silodosin can be decreased when combined with Tariquidar.
Temsirolimus The excretion of Silodosin can be decreased when combined with Temsirolimus.
Simeprevir The excretion of Silodosin can be decreased when combined with Simeprevir.
Isavuconazonium The excretion of Silodosin can be decreased when combined with Isavuconazonium.
Brefeldin A The excretion of Silodosin can be decreased when combined with Brefeldin A.
Ticagrelor The excretion of Silodosin can be decreased when combined with Ticagrelor.
Ivacaftor The excretion of Silodosin can be decreased when combined with Ivacaftor.
Lomitapide The excretion of Silodosin can be decreased when combined with Lomitapide.
Crizotinib The excretion of Silodosin can be decreased when combined with Crizotinib.
Vemurafenib The excretion of Silodosin can be decreased when combined with Vemurafenib.
Linagliptin The excretion of Silodosin can be decreased when combined with Linagliptin.
Mirabegron The excretion of Silodosin can be decreased when combined with Mirabegron.
Regorafenib The excretion of Silodosin can be decreased when combined with Regorafenib.
Enzalutamide The serum concentration of Silodosin can be decreased when it is combined with Enzalutamide.
Ponatinib The excretion of Silodosin can be decreased when combined with Ponatinib.
Canagliflozin The excretion of Silodosin can be decreased when combined with Canagliflozin.
Afatinib The excretion of Silodosin can be decreased when combined with Afatinib.
Ledipasvir The excretion of Silodosin can be decreased when combined with Ledipasvir.
Vorapaxar The excretion of Silodosin can be decreased when combined with Vorapaxar.
Suvorexant The excretion of Silodosin can be decreased when combined with Suvorexant.
Netupitant The excretion of Silodosin can be decreased when combined with Netupitant.
Cobicistat The excretion of Silodosin can be decreased when combined with Cobicistat.
Palbociclib The excretion of Silodosin can be decreased when combined with Palbociclib.
Daclatasvir The excretion of Silodosin can be decreased when combined with Daclatasvir.
Niguldipine The excretion of Silodosin can be decreased when combined with Niguldipine.
Lumacaftor The excretion of Silodosin can be decreased when combined with Lumacaftor.
Rolapitant The excretion of Silodosin can be decreased when combined with Rolapitant.
Venetoclax The excretion of Silodosin can be decreased when combined with Venetoclax.
Asunaprevir The excretion of Silodosin can be decreased when combined with Asunaprevir.
Velpatasvir The excretion of Silodosin can be decreased when combined with Velpatasvir.
Isavuconazole The excretion of Silodosin can be decreased when combined with Isavuconazole.
Neratinib The excretion of Silodosin can be decreased when combined with Neratinib.
Valspodar The excretion of Silodosin can be decreased when combined with Valspodar.
Dacomitinib The excretion of Silodosin can be decreased when combined with Dacomitinib.
Glasdegib The excretion of Silodosin can be decreased when combined with Glasdegib.
Voxilaprevir The excretion of Silodosin can be decreased when combined with Voxilaprevir.
Sarecycline The excretion of Silodosin can be decreased when combined with Sarecycline.
Erdafitinib The excretion of Silodosin can be decreased when combined with Erdafitinib.
Laniquidar The excretion of Silodosin can be decreased when combined with Laniquidar.
Enasidenib The excretion of Silodosin can be decreased when combined with Enasidenib.
Pibrentasvir The excretion of Silodosin can be decreased when combined with Pibrentasvir.
Glecaprevir The excretion of Silodosin can be decreased when combined with Glecaprevir.
Dexniguldipine The excretion of Silodosin can be decreased when combined with Dexniguldipine.
ONT-093 The excretion of Silodosin can be decreased when combined with ONT-093.
Ivosidenib The metabolism of Silodosin can be increased when combined with Ivosidenib.
Ranolazine The excretion of Silodosin can be decreased when combined with Ranolazine.
Elagolix The excretion of Silodosin can be decreased when combined with Elagolix.
Entrectinib The excretion of Silodosin can be decreased when combined with Entrectinib.
Fedratinib The excretion of Silodosin can be decreased when combined with Fedratinib.
Istradefylline The excretion of Silodosin can be decreased when combined with Istradefylline.
Lasmiditan The excretion of Silodosin can be decreased when combined with Lasmiditan.
Cyclosporine The excretion of Silodosin can be decreased when combined with Cyclosporine.
Norgestimate The excretion of Silodosin can be decreased when combined with Norgestimate.
Carfilzomib The excretion of Silodosin can be decreased when combined with Carfilzomib.
Everolimus The excretion of Silodosin can be decreased when combined with Everolimus.
Favipiravir The excretion of Silodosin can be decreased when combined with Favipiravir.
Methylene blue The excretion of Silodosin can be decreased when combined with Methylene blue.
Ripretinib The excretion of Silodosin can be decreased when combined with Ripretinib.
Pralsetinib The excretion of Silodosin can be decreased when combined with Pralsetinib.
Lonafarnib The excretion of Silodosin can be decreased when combined with Lonafarnib.
Clofazimine The excretion of Silodosin can be decreased when combined with Clofazimine.
Arsenic trioxide The excretion of Silodosin can be decreased when combined with Arsenic trioxide.

Target Protein

Alpha-1A adrenergic receptor ADRA1A
Alpha-1D adrenergic receptor ADRA1D
Alpha-1B adrenergic receptor ADRA1B
HERG human cardiac K+ channel KCNH2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18042003
    Yoshida M, Homma Y, Kawabe K: Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia. Expert Opin Investig Drugs. 2007 Dec;16(12):1955-65.
  • PMID: 21116335
    Rossi M, Roumeguere T: Silodosin in the treatment of benign prostatic hyperplasia. Drug Des Devel Ther. 2010 Oct 27;4:291-7. doi: 10.2147/DDDT.S10428.
  • PMID: 25575983
    Keating GM: Silodosin: a review of its use in the treatment of the signs and symptoms of benign prostatic hyperplasia. Drugs. 2015 Feb;75(2):207-17. doi: 10.1007/s40265-014-0344-z.
  • PMID: 27747994
    Vishnuvardhan C, Baikadi S, Borkar RM, Srinivas R, Satheeshkumar N: In vivo metabolic investigation of silodosin using UHPLC-QTOF-MS/MS and in silico toxicological screening of its metabolites. J Mass Spectrom. 2016 Oct;51(10):867-882. doi: 10.1002/jms.3795.
  • PMID: 17225563
    Tatemichi S, Kiguchi S, Kobayashi M, Yamazaki Y, Shibata N, Uruno T: Cardiovascular effects of the selective alphalA-adrenoceptor antagonist silodosin (KMD-3213), a drug for the treatment of voiding dysfunction. Arzneimittelforschung. 2006;56(10):682-7. doi: 10.1055/s-0031-1296773.
  • PMID: 24198606
    Yamanishi T, Mizuno T, Kamai T, Yoshida K, Sakakibara R, Uchiyama T: Management of benign prostatic hyperplasia with silodosin. Open Access J Urol. 2009 Aug 20;1:1-7. doi: 10.2147/rru.s5004.

Contoh Produk & Brand

Produk: 91 • International brands: 2
Produk
  • Ag-silodosin
    Capsule • 4 mg • Oral • Canada • Generic • Approved
  • Ag-silodosin
    Capsule • 8 mg • Oral • Canada • Generic • Approved
  • Apo-silodosin
    Capsule • 4 mg • Oral • Canada • Generic • Approved
  • Auro-silodosin
    Capsule • 8 mg • Oral • Canada • Generic • Approved
  • Auro-silodosin
    Capsule • 4 mg • Oral • Canada • Generic • Approved
  • Jamp Silodosin
    Capsule • 4 mg • Oral • Canada • Generic • Approved
  • Jamp Silodosin
    Capsule • 8 mg • Oral • Canada • Generic • Approved
  • PMS-silodosin
    Capsule • 4 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 91 produk.
International Brands
  • Rapilif — Ipca Urosciences
  • Urief — Watson Pharmaceuticals Inc.

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