nilutamide


androgen

 [an´dro-jen] any steroid hormone that promotes male secondary sex characters. The two main androgens are androsterone and testosterone. Called also androgenic hormone. adj., adj androgen´ic. 
The androgenic hormones are internal endocrine secretions circulating in the bloodstream and manufactured mainly by the testes under stimulation from the pituitary gland. To a lesser extent, androgens are produced by the adrenal glands in both sexes, as well as by the ovaries in women. Thus women normally have a small percentage of male hormones, in the same way that men's bodies contain some female sex hormones, the estrogens. Male secondary sex characters include growth of the beard and deepening of the voice at puberty. Androgens also stimulate the growth of muscle and bones throughout the body and thus account in part for the greater strength and size of men as compared to women.
androgen insensitivity syndrome complete resistance" >androgen resistance.

nilutamide

Anandron, Nilandron

Pharmacologic class: Antiandrogen

Therapeutic class: Antineoplastic

Pregnancy risk category C

FDA Box Warning

Drug may cause interstitial pneumonitis. Though rare, interstitial changes have led to hospitalization and death postmarketing. Most cases occurred within first 3 months of therapy and reversed after drug was stopped. Obtain routine chest X-ray before starting treatment, and be prepared to obtain baseline pulmonary function tests if ordered. Instruct patient to report new or worsening shortness of breath; this symptom warrants immediate drug withdrawal pending evaluation.

Action

Inhibits testosterone uptake in target tissue, preventing normal androgenic response and arresting tumor growth in androgen-sensitive tissue

Availability

Tablets: 50 mg, 150 mg

Indications and dosages

Metastatic prostate cancer (used with surgical castration)

Adults: 300 mg/day P.O. for 30 days, starting on day of or day after surgery; then 150 mg/day P.O.

Contraindications

• Hypersensitivity to drug or its components

• Severe hepatic or respiratory insufficiency

Precautions

Use cautiously in:

• renal impairment.

Administration

• Give with or without food.

• Start therapy on same day as or day after surgical castration.

Adverse reactions

CNS: dizziness, depression, hyperes-thesia, insomnia

CV: hypertension, peripheral edema, heart failure

EENT: abnormal vision, impaired dark and light adaptation, chromatopsia

GI: nausea, vomiting, constipation, dyspepsia, anorexia

GU: hematuria, nocturia, urinary tract infection, gynecomastia, testicular atrophy, decreased libido, erectile dysfunction

Hematologic: anemia, aplastic anemia

Hepatic: hepatitis

Respiratory: dyspnea, upper respiratory infection, interstitial pneumonia

Other: flulike symptoms, pain, fever, hot flushes, alcohol intolerance

Interactions

Drug-drug. Phenytoin, theophylline, vitamin K: increased risk of toxicity from these drugs

Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase: increased levels

Drug-behaviors. Alcohol use: disulfiram-like reaction

Patient monitoring

• Check for signs and symptoms of hepatitis. Monitor liver function tests.

• Monitor CBC.

• Assess fluid intake and output and weight. Watch for signs and symptoms of heart failure.

• Monitor respiratory status, including chest X-rays.

Patient teaching

• Advise patient he may take with or without food.

• Tell patient therapy will start on day of or day after surgical castration.

• Caution patient not to stop taking drug without consulting prescriber.

• Instruct patient to weigh himself daily and report sudden increases.

Advise patient to report new onset or worsening of dyspnea as well as signs and symptoms of hepatotoxicity, such as nausea, vomiting, abdominal pain, unusual tiredness, or yellowing of skin or eyes.

• Advise patient to avoid alcohol during therapy, because serious adverse reactions may occur.

• Tell patient drug may impair his adaptation to darkness and light, which may cause difficulty driving at night or through tunnels.

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

nilutamide

RU 23908 Oncology A nonsteroidal antiandrogen that binds irreversibly to androgen receptors Indications Metastatic androgen-responsive prostate CA; when combined with LHRH analogues, achieves a relatively complete androgen blockade, preventing fatal flare-up reactions seen in early treatment of metastatic prostate CA; it may be superior to flutamide. See Disease flare-up. Cf Flutamide.