Finasteride (Tablet, Film Coated)

Finasteride (Tablet, Film Coated)

Pharmacokinetics:<br/>Absorption: In a study of 15 healthy young subjects, the mean bioavailability of finasteride 5 mg tablets was 63% (range 34 to 108%), based on the ratio of area under the curve (AUC) relative to an intravenous (IV) reference dose. Maximum finasteride plasma concentration averaged 37 ng/mL (range, 27 to 49 ng/mL) and was reached 1 to 2 hours postdose. Bioavailability of finasteride was not affected by food.<br/>Distribution:<br/>Metabolism: Finasteride is extensively metabolized in the liver, primarily via the cytochrome P450 3A4 enzyme subfamily. Two metabolites, the t-butyl side chain monohydroxylated and monocarboxylic acid metabolites, have been identified that possess no more than 20% of the 5��-reductase inhibitory activity of finasteride.<br/>Excretion:<br/>Special Populations:<br/>Pediatric: Finasteride pharmacokinetics have not been investigated in patients<18 years of age.<br/>Gender: Finasteride pharmacokinetics in women are not available.<br/>Geriatric: No dosage adjustment is necessary in the elderly. Although the elimination rate of finasteride is decreased in the elderly, these findings are of no clinical significance. See also Pharmacokinetics, Excretion, PRECAUTIONS, Geriatric Use and DOSAGE AND ADMINISTRATION.<br/>Race:<br/>Renal Insufficiency: No dosage adjustment is necessary in patients with renal insufficiency. In patients with chronic renal impairment, with creatinine clearances ranging from 9 to 55 mL/min, AUC, maximum plasma concentration, half-life, and protein binding after a single dose ofC-finasteride were similar to values obtained in healthy volunteers. Urinary excretion of metabolites was decreased in patients with renal impairment. This decrease was associated with an increase in fecal excretion of metabolites. Plasma concentrations of metabolites were significantly higher in patients with renal impairment (based on a 60% increase in total radioactivity AUC). However, finasteride has been well tolerated in BPH patients with normal renal function receiving up to 80 mg/day for 12 weeks, where exposure of these patients to metabolites would presumably be much greater.<br/>Hepatic Insufficiency: The effect of hepatic insufficiency on finasteride pharmacokinetics has not been studied. Caution should be used in the administration of finasteride in those patients with liver function abnormalities, as finasteride is metabolized extensively in the liver.<br/>Drug Interactions: No drug interactions of clinical importance have been identified. Finasteride does not appear to affect the cytochrome P450-linked drug metabolism enzyme system. Compounds that have been tested in man have included antipyrine, digoxin, propranolol, theophylline, and warfarin, and no clinically meaningful interactions were found.<br/>Clinical Studies:<br/>Effect on Symptom Score:<br/>Effect on the Need for Surgery: In a long-term efficacy and safety study, efficacy was also assessed by evaluating the treatment failures. Treatment failure was prospectively defined as BPH-related urological events or clinical deterioration, lack of improvement and/or the need for alternative therapy. BPH-related urological events were defined as urological surgical intervention. Complete event information was available for 92% of the patients. The following table (Table 1) summarizes the results<br/>Effect on Maximum Urinary Flow Rate:<br/>Effect on Prostate Volume:<br/>Prostate Volume as a Predictor of Therapeutic Response: A meta-analysis combining 1-year data from seven double-blind, placebo-controlled studies of similar design, including 4491 patients with symptomatic BPH, demonstrated that, in patients treated with finasteride, the magnitude of symptom response and degree of improvement in maximum urinary flow rate were greater in patients with an enlarged prostate at baseline.<br/>Summary of Clinical Studies: The data from these studies, showing improvement in BPH-related symptoms, reduction in treatment failure (BPH-related urological events), increased maximum urinary flow rates, and decreasing prostate volume, suggest that finasteride arrests the disease process of BPH in men with an enlarged prostate.

http://www4.wiwiss.fu-berlin.de/drugbank/resource/drugs/DB01216

dailymed-ingredient:Docusate_Sodium, dailymed-ingredient:FD&C_Blue#2_Aluminum_Lake, dailymed-ingredient:Hydroxypropyl_Cellulose, dailymed-ingredient:Hypromellose, dailymed-ingredient:Iron_Oxide_Yellow, dailymed-ingredient:Lactose_Monohydrate, dailymed-ingredient:Magnesium_Stearate, dailymed-ingredient:Microcrystalline_Cellulose, dailymed-ingredient:Pregelatinised_Starch, dailymed-ingredient:Sodium_Starch_Glycolate, dailymed-ingredient:Talc, dailymed-ingredient:Titanium_Dioxide

General:<br/>Effects on PSA and Prostate Cancer Detection:<br/>Information for Patients:<br/>Drug Interactions:<br/>Drug/Laboratory Test Interactions: In patients with BPH, finasteride has no effect on circulating levels of cortisol, estradiol, prolactin, thyroid-stimulating hormone, or thyroxine. No clinically meaningful effect was observed on the plasma lipid profile (i.e., total cholesterol, low density lipoproteins, high density lipoproteins and triglycerides) or bone mineral density. Increases of about 10% were observed in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in patients receiving finasteride, but levels remained within the normal range. In healthy volunteers, treatment with finasteride did not alter the response of LH and FSH to gonadotropin-releasing hormone indicating that the hypothalamic-pituitary-testicular axis was not affected.<br/>Carcinogenesis, Mutagenesis, Impairment of Fertility:<br/>Pregnancy:<br/>Nursing Mothers:<br/>Pediatric Use:<br/>Geriatric Use:

Finasteride (Tablet, Film Coated)

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http://www4.wiwiss.fu-berlin.de/dailymed/resource/routeOfAdministration/Oral