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Finasteride: profile and news
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Feb 6, 2006 Stay in the Shade Of Jade Feb 10, 2006 PLETCHER TODD A Feb 3, 2006 Kelly Clarkson gets the Grammy party started Feb 9, 2006 ROAD TO THE TRIPLE CROWN Feb 14, 2006 OAKLAWN GLANCE Feb 5, 2006 IDEAL SOCIETY SERIES FINAL FRIDAY Feb 2, 2006 Other information Indication For the treatment of symptomatic benign prostatic hyperplasia (BPH) in men with an enlarged prostate to: Improve symptoms, reduce the risk of acute urinary retention, reduce the risk of the need for surgery including transurethral resection of the prostat Pharmacology Finasteride is indicated for the treatment of male pattern hair loss (androgenetic alopecia) in men only. Finasteride is a competitive and specific inhibitor of Type II 5a-reductase, an intracellular enzyme that converts the androgen testosterone into DHT. Two distinct isozymes are found in mice, rats, monkeys, and humans: Type I and II. Each of these isozymes is differentially expressed in tissues and developmental stages. In humans, Type I 5a-reductase is predominant in the sebaceous glands of most regions of skin, including scalp, and liver. Type I 5a-reductase is responsible for approximately one-third of circulating DHT. The Type II 5a-reductase isozyme is primarily found in prostate, seminal vesicles, epididymides, and hair follicles as well as liver, and is responsible for two-thirds of circulating DHT. Mechanism Of Action The mechanism of action of Finasteride is based on its preferential inhibition of Type II 5a-reductase, an intracellular enzyme that converts the androgen testosterone into DHT. Inhibition of Type II 5a-reductase blocks the peripheral conversion of testosterone to DHT, resulting in significant decreases in serum and tissue DHT concentrations. Drug Category Anti-baldness Agents; Antihyperplasia Agents; Skin and Mucous Membrane Agents (84:92.00); ATC:D11AX10; ATC:G04CB01 Brand Names/Synonyms CCRIS 7438; Chibro-Proscar; Finasterida [Inn-Spanish]; Finasteride; Finasteride [Usan:Ban:Inn]; Finasteride and Its Intermediates; Finasteridum [Inn-Latin]; Finastid; Finpecia; HSDB 6793; MK-0906; MK-906; Propecia; Proscar; Prostide Dosage Forms TABLET Absorption Not Available Interactions -->Interactions for Finasteride: No drug interactions of clinical importance have been identified. Finasteride does not appear to affect the cytochrome P450-linked drug-metabolizing enzyme system. Compounds that have been tested in man include antipyrine, digoxin, propranolol, theophylline, and warfarin and no clinically meaningful interactions were found. Other concomitant therapy Although specific interaction studies were not performed, finasteride doses of 1 mg or more were concomitantly used in clinical studies with acetaminophen, acetylsalicylic acid, a-blockers, analgesics, angiotensin-converting enzyme (ACE) inhibitors, anticonvulsants, benzodiazepines, beta blockers, calcium-channel blockers, cardiac nitrates, diuretics, H2 antagonists, HMG-CoA reductase inhibitors, prostaglandin synthetase inhibitors (also referred to as NSAIDs), and quinolone anti-infectives without evidence of clinically significant adverse interactions. Drug/Laboratory Test Interactions Finasteride had no effect on circulating levels of cortisol, thyroid-stimulating hormone, or thyroxine, nor did it affect the plasma lipid profile (e.g., total cholesterol, low-density lipoproteins, high-density lipoproteins and triglycerides) or bone mineral density. In studies with finasteride, no clinically meaningful changes in luteinizing hormone (LH), follicle-stimulating hormone (FSH) or prolactin were detected. 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. In clinical studies with PROPECIA (finasteride, 1 mg) in men 18-41 years of age, the mean value of serum prostate-specific antigen (PSA) decreased from 0.7 ng/mL at baseline to 0.5 ng/mL at Month 12. Further, in clinical studies with PROSCAR (finasteride, 5 mg) when used in older men who have benign prostatic hyperplasia (BPH), PSA levels are decreased by approximately 50%. These findings should be taken into account for proper interpretation of serum PSA when evaluating men treated with finasteride. Chemical IUPAC Name Not Available Chemical Formula C23H36N2O2 Half Life 4.5 hours (range 3.3-13.4 hours) Drug Type Approved Drug # Accession No APRD00632 CAS Registry Number 98319-26-7 |
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