flutamide


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flutamide

 [floo´tah-mīd]
a nonsteroidal antiandrogen administered orally in the treatment of advanced or metastatic prostatic carcinoma.

flutamide

APO-Flutamide (CA), Drogenil (UK), Euflex (CA), Novo-Flutamide (CA), PMS-Flutamide (CA)

Pharmacologic class: Antiandrogen

Therapeutic class: Antineoplastic

Pregnancy risk category D

Action

Exerts potent antiandrogenic activity at cellular level by inhibiting androgen uptake or nuclear binding of androgen

Availability

Capsules: 125 mg

Indications and dosages

Metastatic prostate cancer

Adults: 250 mg P.O. t.i.d. q 8 hours, given with luteinizing hormone-releasing hormone (LHRH) analog. Total daily dosage is 750 mg.

Off-label uses

• Benign prostatic hypertrophy

Contraindications

• Hypersensitivity to drug

• Severe hepatic impairment

• Sleep apnea

• Women

Precautions

None

Administration

• Be aware that leuprolide acetate is the most common LHRH analog given with flutamide.

Adverse reactions

CNS: drowsiness, confusion, depression, anxiety, nervousness, paresthesia

CV: peripheral edema, hypertension

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, anorexia, dry mouth

GU: erectile dysfunction, loss of libido, gynecomastia, hot flashes

Hematologic: anemia, leukopenia, thrombocytopenia

Hepatic: hepatitis

Skin: rash, photosensitivity

Interactions

Drug-drug. Warfarin: increased prothrombin time

Drug-diagnostic tests. Alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, blood urea nitrogen, creatine kinase: increased levels

Hemoglobin, platelets, white blood cells: decreased levels

Drug-herbs. Chaparral, comfrey, eucalyptus, germander, pennyroyal, skullcap, valerian: increased risk of hepatotoxicity

Drug-behaviors. Sun exposure: increased risk of photosensitivity

Patient monitoring

• Monitor CBC and liver function tests.

Watch for bleeding tendency and signs and symptoms of hepatic damage (jaundice, vomiting, dark yellow or brown urine).

• Monitor blood pressure.

Patient teaching

Instruct patient to immediately report unusual bleeding or bruising.

• Tell patient to avoid activities that can cause injury. Advise him to use soft toothbrush and electric razor to avoid gum and skin injury.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• Instruct patient to minimize GI upset by eating frequent, small servings of healthy food.

• Tell patient he'll undergo regular blood testing during therapy.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

flutamide

(flo͞o′tə-mīd′)
n.
A nonsteroidal antiandrogen that inhibits the binding of testosterone and dihydrotestosterone to androgen receptors, used in the treatment of prostate cancer.

flutamide

Endocrinology A nonsteroidal antiandrogen which, unlike steroidal antiandrogens, lacks androgenic, estrogenic, antiestrogenic, progestational, adrenocortical, and antigonadotropic activity; flutamide has been used for metastatic androgen-responsive prostate CA and, when combined with LHRH analogues, achieves a relatively complete androgen blockade; flutamide has been used to treat acne and hirsutism Adverse effects GI tract–diarrhea, nausea, dizziness, gynecomastia, hepatic dysfunction or toxicity. Cf Nilutamide.

flutamide

A drug that opposes male sex hormones (androgens) and is used to treat advances cancer of the prostate gland. Brand names are Chimax and Drogenil.

flu·ta·mide

(flūtă-mīd)
A nonsteroidal antiinflammatory drug used to treat arthritis.
References in periodicals archive ?
It was found that exposure to flutamide during intrauterine life resulted in a chronic apoptotic germ cell death in the adult rat testicular tissue correlated with an increase in the expression and activation in germ cells of caspases-3 and -6 which are two important components in the apoptotic machinery (Omezzine et al., 2003).
Because the initial injection of the series can cause a transient increase in testosterone (prior to its sustained decline), flutamide, a testosterone receptor blocking agent, is ordinarily prescribed for the first 14 days only, following initiation of treatment with depot leuprolide.
Drugs causing methaemoglobinaemia are acetanilide, alloxan, aniline, arsine, benzene derivatives, bivalent copper, bismuth, bupivacaine, chorates, chloroquine, chromates, dapsone, dimethyl sulfoxide, dinitrophenol, exhaust fumes, ferricyanide, flutamide, hydroxylamine, lidocaine, metoclopramide, naphthalene, nitrates, nitrofuran, nitroglycerin, sodium nitroprusside, paraquet, phenacetin, phenol, phenytoin, rifampin, sulphasalazine and sulphonamides
--Steroidal olmayan veya saf, ornegin; nilutamide, flutamide ve bicalutamide.
Antihypertensive effects of flutamide in rats that are exposed to a low-protein diet in utero.
we determine that Petitioner has shown by a preponderance of the evidence that all claims of the '438 patent for which trial was instituted, namely, claims 1-20, are unpatentable." The '438 patent describes administration of a therapeutically effective amount of a CYP17 inhibitor, such as abiraterone acetate, with a therapeutically effective amount of at least one additional therapeutic agent including, but not limited to, an anti-cancer agent, such as mitoxantrone, paclitaxel, docetaxel, leuprolide, goserelin, triptorelin, seocalcitol, bicalutamide, or flutamide, or a steroid, such as hydrocortisone, prednisone, or dexamethasone, the ruling states.
Topical flutamide: In a randomized parallel study, comparative mexameter measurements showed that melasma 4% HQ with 1% flutamide cream were found to be as effective as HQ.
de Zegher, "High neutrophil count in girls and women with hyperinsulinaemic hyperandrogenism: Normalization with metformin and flutamide overcomes the aggravation by oral contraception," Human Reproduction, vol.
Relevantly, neonatal treatment with flutamide, a nonsteroidal antagonist of the androgen receptor, induced a decrease in the peripheral levels of leptin [35].
The newly established method was then applied to benzo(a) pyrene (BaP) and flutamide. BaP and other polycyclic aromatic hydrocarbons are widespread environmental contaminants formed during incomplete combustion or pyrolysis of organic material with estrogenic and class 1 carcinogenic properties (IARC, 2012).