Flutamide
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(British Approved Name, US Adopted Name, rINN)
Drug Nomenclature
International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):
Pharmacopoeias. In Europe and US.
European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Flutamide). A pale yellow, crystalline powder. Practically insoluble in water; freely soluble in alcohol and in acetone. Protect from light.
The United States Pharmacopeia 31, 2008 (Flutamide). A pale yellow, crystalline powder. Practically insoluble in water, in liquid paraffin, and in petroleum spirit; freely soluble in acetone, in ethyl acetate, and in methyl alcohol; soluble in chloroform and in ether. Store in airtight containers. Protect from light.
Adverse Effects and Precautions
The most frequently reported adverse effects with flutamide are hot flushes and reversible gynaecomastia or breast tenderness, sometimes accompanied by galactorrhoea. Nausea, vomiting, diarrhoea, increased appetite, anorexia, and sleep disturbances may occur. There have been reports of skin reactions, including epidermal necrolysis, and of liver damage, sometimes fatal. Other adverse effects reported in patients receiving flutamide include anaemias, haemolysis, headache, dizziness, malaise, blurred vision, anxiety, depression, decreased libido, impotence, and hypertension. Abdominal pain, chest pain, dyspnoea, and cough have been reported rarely. Discoloration of the urine to amber or yellow-green can be caused by the presence of flutamide and/or its metabolites.
Flutamide should be used with care in patients with cardiovascular disease because of the possibility of fluid retention. It should also be used with caution in patients with hepatic impairment and is contra-indicated in those with severe impairment. Regular liver function testing is recommended in all patients: therapy should be stopped or dosage reduced if there is evidence of hepatotoxicity.
Effects on the blood. A report of methaemoglobinaemia in an elderly man was attributed to flutamide. A study of 45 patients given flutamide found no cases of methaemoglobinaemia, but the authors noted a further 3 published case reports.
Effects on the liver. Hepatitis occurred in a 79-year-old man taking flutamide 750 mg daily as sole therapy after a prostatectomy, but a subsequent study in 1091 patients given flutamide 250 mg three times daily as part of a regimen for prostate cancer found marked signs of liver damage only in 4, of whom only 2 had clinical evidence of hepatotoxicity. In the USA, the FDA had 46 reports of patients with hepatotoxicity associated with flutamide up to December 1994. Of these patients, 20 died from progressive liver disease. Further cases have continued to be reported. Early tapering of the dose, stopping therapy, or switching to another anti-androgen may resolve hepatotoxic effects. Patients with chronic viral hepatitis may be at higher risk of developing hepatotoxicity with anti-androgen therapy.
Effects on the lungs. In a review of 78 cases of pneumonitis reported to the FDA between 1998 and 2000 that were associated with bicalutamide, flutamide, or nilutamide, it was found that 14 patients had died of respiratory failure. It was estimated that the incidence of pneumonitis was highest for nilutamide (0.77%), but lower for flutamide (0.04%) and brcalutamrde (0.01%).
Effects on the skin. Photosensitivity reactions have been reported in patients receiving flutamide. Some consider it to be an early manifestation of SLE.
Gynaecomastia. Gynaecomastia and breast pain are frequent adverse effects of nonsteroidal anti-androgens used to treat prostate cancer. Nearly 90% of patients treated with bicalutamide in the Early Prostate Cancer programme experienced breast pain, gynaecomastia, or both. Some patients who develop gynaecomastia will accept it as a tolerable adverse effect of therapy but others will require specifrc treatment, and a number of different measures have been tried for both prevention and treatment. The risk of breast changes can be reduced by the use of prophylactic low-dose irradiation of the breast area before nonsteroidal anti-androgen therapy is started. However, skin irritation can occur, and the long-term risk for development of breast cancer is unknown. Irradiation is unlikely to be effective once breast enlargement has occurred but it can help to reduce pain. Empirical use of oral analgesics or topical local anaesthetics may be considered for breast pain. Specifrc surgical treatment to reduce breast tissue includes liposuction and breast tissue excision.
Hormonal therapy using tamoxifen or anastrozole has been suggested, largely based on reports of benefit in various patient groups with gynaecomastia. Two randomised controlled studies of men who were treated with bicalutamide for prostate cancer found that prophylactic tamoxifen was effective for the prevention of gynaecomastia and breast pain, but that anastrozole was no better than placebo. One of these studies also assessed the use of these drugs as treatment and found that gynaecomastia and breast pain resolved in at least 65% of patients treated with tamoxifen, but only in about 18% of those treated with anastrozole. Tamoxifen is considered to be more effective than radiotherapy for prevention of gynaecomastia.
Interactions
Flutamide may increase the effect of warfarin, see Antineoplastics.
Pharmacokinetics
Flutamide is reported to be rapidly and completely absorbed from the gastrointestinal tract with peak plasma concentrations occurring 1 hour after a dose. It is rapidly and extensively metabolised; the major metabolite (2-hydroxyflutamide) possesses anti-androgenic properties. The half-life of the metabolite is about 6 hours. Both flutamide and 2-hydroxyflutamide are more than 90% bound to plasma proteins. Excretion is mainly in the urine with only minor amounts appearing in the faeces.
Uses and Administration
Flutamide is a nonsteroidal compound with anti-androgenic properties which appears to act by inhibiting the uptake and/or binding of androgens in target tissues. It is used, usually with gonadorelin analogues, in the palliative treatment of prostatic carcinoma. The usual oral dose is 250 mg three times daily. When used in combination therapy UK licensed product information recommends that flutamide treatment should be started at least 3 days before the gonadorelin analogue to suppress any ‘flare’ reaction; however, in some other countries it is recommended that treatment with both agents be begun simultaneously for optimum effect.
Congenital adrenal hyperplasia. For mention of the use of flutamide with testolactone to block androgenic effects in congenital adrenal hyperplasia.
Hirsutism. Anti-androgens (usually cyproterone or spironolac-tone) are widely used for the drug treatment of hirsutism. Flutamide has no particular advantage in this context; one study has found flutamide to be more effective than spironolactone in inhibiting hirsutism, but others found them to be of similar efficacy, and the risk of hepatotoxicity with flutamide is a problem. Nonetheless, flutamide has continued to be investigated.
Malignant neoplasms. Androgen blockade, which may include the use of flutamide, is used in the management of meta-static hormone-responsive prostate cancer; once the cancer begins to progress despite such therapy, stopping flutamide occasionally produces paradoxical disease regression. Promising preliminary results have also followed the use of flutamide in patients with adenocarcinoma of the pancreas.
Polycystic ovary syndrome. Flutamide has been used, usually with metformin, in the management of polycystic ovary syndrome; additive effects have been reported with this combination.
Preparations
The United States Pharmacopeia 31, 2008: Flutamide Capsules.
Single-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed
Argentina: Asoflut; Dedile; Eulexin¤; Flutaplex; Flutax¤; Flutepan; Flutrax; FTDA¤; Olter¤; Australia: Eulexin; Flutamin; Fugerel; Austria: Afluta; Androbloc; Flutabene; Flutahexal; Flutastad; Fugerel; Belgium: Eulexin; Flutaplex¤; Brazil: Biomida; Eulexin; Tecnoflut; Teflut; Canada: Euflex; Chile: Androdor¤; Drogenil; Etaconil; Flulem; Czech Republic: Andraxan; Flucinom; Flutacan; Prostandril; Xadaren; Denmark: Eulexin; Fluprosin; Flutacan¤; Flutaplex¤; Profamid; Finland: Eulexin; Profamid; France: Eulexine; Prostadirex; Germany: Apimid; Flumid; Fluta; Flutamex¤; Flutexin; Fugerel; Prostica; Prostogenat¤; Testac¤; Testotard; Greece: Adiprost; Elbat; Flucinom; Flutaplex; Palistop; Prostamide; Tremexal; Hong Kong: Flutan¤; Fugerel; Hungary: Cytamid; Flutam; Fugerel; India: Cytomid; Prostamid; Ireland: Androstat; Drogenil; Israel: Eulexin; Italy: Drogenil; Eulexin; Fluprost; Virflutam¤; Malaysia: Flutan; Flutaplex; Fugerel¤; Mexico: Eulexin; Fluken; Flulem; Tafenil; Netherlands: Drogenil; Eulexin; Norway: Eulexin; New Zealand: Eulexin; Flutamin; Flutol¤; Portugal: Draxon¤; Eulexin; Russia: Flutamid (Флутамид); Flutaplex (Флутаплекс); South Africa: Eulexin; Flutahexal; Flutaplex; Singapore: Fugerel¤; Spain: Eulexin; Flutandrona; Flutaplex; Grisetin; Oncosal; Prostacur; Sweden: Eulexin; Flutacan¤; Switzerland: Flucinome; Thailand: Flutan; Fugerel; United Kingdom: Chimax; Drogenil; United States: Eulexin¤; Venezuela: Eulexin
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