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Pharmacology: Pharmacodynamics: Silodosin is a selective antagonist of post-synaptic alpha-1 adrenoreceptors, which are found in the human prostate, bladder neck, prostatic capsule, and prostatic urethra. As a result of blockage of these alpha-1 adrenoreceptors, smooth muscle in these tissue relaxes, resulting in an improvement in urine flow and reduction in benign prostatic hyperplasia symptoms.
Pharmacokinetics: Absorption: Tmax: 2.6 hours.
Bioavailability: 32%.
Effect of food: Cmax decreased by approximately 18% to 43% and AUC decreased by 4% to 49%.
Protein binding: 97%.
Distribution: Vd: 49.5 L.
Metabolism: Hepatic: extensive via glucuronidation, alcohol and aldehyde dehydrogenase, and CYP3A4 pathways.
Active metabolite is glucuronide conjugate (KMD-3213G).
Excretion: Renal: Approximately 33.5%, Fecal: Approximate by 54.9%.
Total body clearance: 10 L/hr.
Elimination half life: Silodosin: 13.3 hours.
Glucuronide conjugate: 24 hours.
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