Finasteride
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Drug Approvals
(British Approved Name, US Adopted Name, rINN)
International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish): Finasterid; Finasterida; Finasteridas; Finasteride; Finasteridi; Finastendum; Finasztend; MK-906; MK-0906; YM-152.
Pharmacopoeias. In Europe and US.
European Pharmacopoeia, 6th ed. (Finasteride). A white or almost white crystalline powder. It exhibits polymorphism. Practically insoluble in water freely soluble in dehydrated alcohol and in dichloromethane. Protect from light.
The United States Pharmacopeia 31, 2008 (Finasteride). A white to off-white crystalline solid. Very slightly soluble in water freely soluble in alcohol and in chloroform. Store in airtight containers.
Adverse Effects
The most commonly reported adverse effects of finasteride are decreased libido, erectile dysfunction, ejaculation disorders, and reduced volume of ejaculate. Breast tenderness and enlargement (gynaecomastia) may occur, and there have been reports of hypersensi-tivity reactions such as swelling of the lips and face, pruritus, urticaria, and rashes. Testicular pain has also been reported.
Incidence of adverse effects. In a study using prescription event monitoring data, the most commonly reported adverse effects of finasteride in 14 772 patients were impotence or ejacula-tory failure (2.1% of patients), reduced libido (1%), and breast disorders such as gynaecomastia (0.4%). Adverse effects reported in a single patient each, and verified on rechallenge, were ex-foliative dermatitis, perioral numbness, and swollen glands. Finasteride appeared to be associated with ataxia in 1 patient and wheeziness in another.
Effects on the breast. Gynaecomastia was the adverse effect of finasteride most frequently reported to the FDA between June 1992 and February 1995 (a total of 214 reports). The onset after therapy ranged from 14 days to 2.5 years, and the condition could be unilateral or bilateral. Mastectomy was performed in 12 men. Of the 86 men for whom follow-up information was available, partial or complete remission of gynaecomastia occurred in 80%, and no change occurred in 20%. In 2 of the cases, primary intra-ductal breast carcinoma was subsequently found, although 1 probably had breast cancer before finasteride therapy. Continued surveillance of the relationship between finasteride and breast cancer is required.
Effects on mental function. Depression has been reported in 20 patients given finasteride for the treatment of alopecia. In most cases the depression began about 3 to 4 months after starting finasteride, and resolved within a few weeks of stopping it. In 2 patients rechallenged with finasteride, depression recurred within 2 weeks of restarting the drug.
Precautions
Finasteride should be used with caution in hepatic impairment. When used for benign prostatic hyperplasia, finasteride should be used with caution in men at risk of obstructive uropathy. Patients should be evaluated for prostatic carcinoma before and during therapy. Use of finasteride decreases concentrations of serum markers of prostate cancer such as prostate specific antigen (PSA) by up to 50% even when cancer is present, and reference values should be adjusted accordingly the ratio of free to total PSA (percent free PSA) remains constant.
Studies in animals suggest finasteride could produce feminisation (hypospadia) of a male fetus if used in pregnant women therefore, its use is contra-indicated in women who are or may become pregnant. In addition, it is recommended that women in this category should not handle crushed or broken finasteride tablets. Finasteride has been detected in semen, therefore use of a condom is recommended if the patient’s sexual partner is, or may become, pregnant.
Pharmacokinetics
Finasteride is absorbed after oral doses, and peak plasma concentrations are achieved in 1 to 2 hours. The mean bioavailability has variously been reported as 63% and 80%. It is about 90% bound to plasma protein. Finasteride crosses the blood-brain barrier, and is distributed into semen. It is metabolised in the liver, primarily by the cytochrome P450 isoenzyme CYP3 A4, and excreted in urine and faeces as metabolites. The mean terminal half-life is about 6 hours in patients under 60 years of age but may be prolonged to about 8 hours in those 70 years of age or older.
Uses and Administration
Finasteride is an azasteroid that inhibits the type-2 iso-form of 5α-reductase, the enzyme responsible for conversion of testosterone to the more active dihydrotestos-terone, and therefore has anti-androgenic properties. It is given orally in a dose of 5 mg daily in the management of benign prostatic hyperplasia to cause regression of the enlarged prostate and to improve symptoms it may reduce the incidence of acute urinary retention and the need for surgery. Response may be delayed and treatment may be required for 6 months or more to assess whether benefit has been achieved.
In the treatment of male-pattern baldness (alopecia androgenetica) in men, finasteride is given orally in a dose of 1 mg daily. In general, use for 3 months or more is required before benefit is seen, and effects are reversed within 12 months of ceasing therapy.
Alopecia. In men with male-pattern baldness (alopecia), treatment with oral finasteride for 12 months resulted in an 11 % increase in vertex hair count, which was maintained in those who continued therapy. Extension of this study to 5 years found that long-term treatment with finasteride maintained beneficial effects, or at least slowed hair loss. The use of oral finasteride for this purpose has been reviewed. Some efficacy has also been found with topical finasteride.
Although finasteride is contra-indicated in women who are or may become pregnant (see Precautions, above), it has been investigated in the treatment of male-pattern baldness in postmeno-pausal women. However, a 1-year placebo-controlled study found no benefit from finasteride. There has been a report of benefit from finasteride in 4 women with hair loss due to hyper-androgenism.
Benign prostatic hyperplasia. Finasteride is used in the management of benign prostatic hyperplasia. It produces moderate reductions in prostate volume, although this takes a number of months and is not always associated with much symptomatic improvement therapy must be continued indefinitely for benefit to be maintained. A 4-year study found that finasteride reduced the probability of surgery and acute urinary retention in men with symptomatic benign prostate hyperplasia with prostatic enlargement. Although the need for prostatectomy was reduced by 55% it was pointed out that only 6% extra patients would benefit from treatment with finasteride. For every 100 men treated, 7 finasteride and 13 placebo recipients required surgery. A 2-year, open-label follow-up of this study reported that the reductions in probability of surgery and acute urinary retention were maintained. It was also found that in patients who switched from placebo to finasteride, these measures decreased to become similar to those recorded in men already receiving finasteride. A comparative 12-month study found the alpha blocker terazosin to be more effective than finasteride in relieving symptoms and improving peak urine flow rates the combination of finasteride plus terazosin was no more effective than terazosin alone. Moreover, although finasteride reduced prostatic volume, it was no more effective than placebo, a finding that is at odds with previous placebo-controlled studies. It has been suggested that the smaller median prostate size in this study may explain the negative findings, and that men with larger prostates do benefit from finasteride. Similar results were reported in a 12-month study using doxazosin. Later results from a large study showed that over a longer period of 4 or more years the combination of doxazosin and finasteride reduced the risk of clinical progression more than either drug alone. The combination of an alpha blocker and 5a-reductase inhibitor is therefore considered to be a suitable option for patients with urinary symptoms and demonstrable prostatic enlargement, and who are at significant risk of progression.
Hirsutism. Finasteride is reported to be effective for the treatment of hirsutism in women. It should be noted that finasteride should not be used in women who are or may become pregnant (see Precautions, above).
Malignant neoplasms of the prostate. Finasteride appears to have little effect in established prostate cancer,’ but is under investigation for its prevention. The results of 1 small study of its effects on the prostate found little evidence to support its use for prevention of malignancy in patients at high risk. In healthy men, a large controlled study, the Prostate Cancer Prevention Trial (PCPT), found that 7 years of finasteride prophylaxis reduced the incidence of prostate cancer by about 25% compared with placebo, but this benefit was offset by an increased risk of high-grade tumours associated with finasteride. The risk-benefit implications of these results have been debated, although some commentaries” suggest that preventive use would be justified, at least in selected patients. Further analysis of the PCPT data found that finasteride had introduced a detection bias for both prostate cancer and for high-grade prostate cancer. Finasteride increased the sensitivity of prostate specific antigen (PSA) testing, implying that the PCPT primary findings of increased risk of high-grade tumours were due, at least in part, to improved detection. The reported 25% decrease in prostate cancer incidence was also likely to be an underestimate. The European Association of Urology has endorsed a recommendation that prostate cancer management guidelines be updated to reflect these findings.
Preparations
British Pharmacopoeia 2008: Finasteride Tablets
The United States Pharmacopeia 31, 2008: Finasteride Tablets.
Proprietary Preparations
Argentina: Anatine † Andropel Avertex Conef † Daric Eutiz † Finasterin Fin-prostat Flutiamik Folcres HPB Nasteril Pelicrep † Propecia Proscar Pros-min Prostanil Prostanovag Prostene Renacidin Sutrico Tealep Tricofarma Urofin Urototal Vetiprost
Austral.: Propecia Proscar
Austria: Propecia Proscar
Belgium: Proscar
Brazil: Alfasin Capyla Finalop Finastec Finastil Flaxin Nasterid Nasterid A Pracap Prohair † Pronasteron Propecia Proscar Prostide Reduscarf
Canada: Propecia Proscar
Chile: Apeplus † Prohair Proscar Saniprostol Vastus
Czech Republic: Androfin Apo-Finas Duromeran Edufil Finajel † Finanorm Finard Finex Finpros Gefin Ibition Lekoprost Mostrafin Penester Propecia Proscar Radicut
Denmark: Propecia Proscar
Finland: Gefina Propecia Proscar
France: Chibro-Proscar Propecia
Germany: Propecia Proscar
Greece: Pervil Poruxin Propecia Proscar
Hong Kong: Propecia Proscar
Hungary: Finpros Proscar Prosterid
India: Fincar Finpecia Ultrafinaf
Indonesia: Finaxal Finpro Proscar Prostacom Reprostom
Ireland: Proscar
Israel: Pro-Cure Propecia
Italy: Finastid Genaprost Propecia Proscar Prostide
Malaysia: Propecia Proscar
Mexico: Propeshia Proscar
The Netherlands: Finaburg Propecia Proscar
Norway: Proscar
New Zealand: Propecia Proscar
Philippines: Propecia Proscar
Poland: Ambulase Finaride Finaster Lifin Penester Propecia Proscar Zasterid
Portugal: Propecia Proscar Prostacide Prostafin Zidoril Zylfina
Russia: Finast Penester Proscar Prosterid
South Africa: Propecia Proscar
Singapore Propecia Proscar
Spain: Eucoprost Propecia Proscar
Sweden: Propecia Proscar
Switzerland: Propecia Proscar
Thailand: Firide Harifin Propecia Proscar
Turkey: Dilaprost Finarid Propecia Proscar Prosterit
UK: Propecia Proscar
USA: Propecia Proscar
Venezuela: Finast † Nasterol Propecia Proscar Prosdina †
Multi-ingredient
Argentina: Tricoplus Conef †
India: Urimax F
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