Nilutamide (Ainedex) is an antiandrogen that inhibits the effects of testosterone. It is used in the treatment of metastatic prostatic cancer.

Nilutamide Uses:

• Metastatic Prostate cancer:

  • Metastatic prostate cancer treatment   (in combination with surgical castration)

Nilutamide (Ainedex) Dose in Adults

Nilutamide (Ainedex) Dose in the treatment of Metastatic prostate cancer:

• P/O:
• 300 milligram once everyday (starting the same day or day after surgical castration) for 30 days, followed by 150 milligram once everyday.
• In patients with evidence of disease progression, consider therapy discontinuation.

Nilutamide (Ainedex) Dose in Childrens

Not indicated for use in children.

Nilutamide Pregnancy Risk Category: C

• Studies on animal reproduction have not been conducted. Nilutamide should not be used in women.

Nilutamide use during breastfeeding:

• Nilutamide should not be used in women.

Nilutamide Dose in Kidney Disease:

• In the manufacturer’s labeling, there are no dosage adjustments provided.

Nilutamide Dose in Liver disease:

• Hepatic impairment at treatment initiation:

  • Mild or moderate impairment:

    • In the manufacturer’s labeling, there are no dosage adjustments provided.

  • Severe impairment:

    • Use is contraindicated.

• Hepatotoxicity during treatment:

  • ALT >2 times ULN or jaundice:

    • Treatment is discontinued.

• From monotherapy and combination therapy, reactions are reported.

Common Side Effects of Nilutamide (Ainedex):

• Endocrine & metabolic:

  • Hot flash

• Ophthalmic:

  • Nocturnal amblyopia

Less Common Side Effects of Nilutamide (Ainedex):

• Cardiovascular:

  • Hypertension
  • Cardiac Failure
  • Angina Pectoris
  • Edema
  • Syncope

• Central Nervous System:

  • Dizziness
  • Paresthesia
  • Malaise
  • Nervousness

• Dermatologic:

  • Pruritus

• Endocrine & Metabolic:

  • Hyperglycemia
  • Increased Haptoglobin
  • Weight Loss

• Gastrointestinal:

  • Nausea
  • Constipation
  • Diarrhea
  • Gastrointestinal Hemorrhage
  • Melena
  • Xerostomia

• Hematologic & Oncologic:

  • Leukopenia

• Hepatic:

  • Increased Serum ALT
  • Increased Serum AST
  • Increased Serum Alkaline Phosphatase

• Neuromuscular & Skeletal:

  • Arthritis

• Ophthalmic:

  • Visual Disturbance
  • Cataract
  • Photophobia

• Renal:

  • Increased Blood Urea Nitrogen
  • Increased Serum Creatinine

• Respiratory:

  • Dyspnea
  • Cough
  • Interstitial Pneumonitis
  • Rhinitis

• Miscellaneous:

  • Alcohol Intolerance

Contraindications to Nilutamide (Ainedex):

• Hypersensitivity to nilutamide and any component of the formulation
• Severe hepatic impairment.
• Grave respiratory insufficiency

Canadian labeling:

• Additional contraindications not listed in the US labeling:
  • Use for women and children

Warnings and precautions

• Hematologic:

  • Anemia can occur when testosterone is suppressed.
  • As mentioned, you should check the CBC regularly.
  • Postmarketing case reports have reported an increase in the incidence of anemia.

• Hepatotoxicity:

  • One percent of patients who received nilutamide were found to have Hepatitis, or significant increases in liver enzymes that led to drug discontinuation.
  • Rare cases of death or hospitalization due to severe liver injury were reported.
  • Hepatotoxicity is most commonly diagnosed within the first three to four months of treatment.
  • Examine transaminases.
  • These Signs/Symptoms of Hepatic Dysfunction (nausea/vomiting and abdominal pain, anorexia. fatigue. flu-like symptoms. dark urine, jaundice and/or right Upper Quadrant pain) should prompt liver function testing.
  • Stop immediately any treatment for jaundice, ALT >2x the upper limit of normal (ULN)

• Interstitial pneumonitis: [US Boxed Warning]:

  • Interstitial pneumonitis was reported in controlled studies. It has been shown that nilutamide exposure caused 2 percent of patients to develop interstitial pneumonia.
  • A small study with Japanese patients has shown an increase in incidence.
  • You may experience symptoms such as exertional dyspnea and chest pains, fever, and cough.
  • Interstitial changes, including pulmonary fibrosis, that can lead to fatalities and hospitalization have been reported (rarely).
  • Most cases resolved within the first three months. Interstitial and alveolointerstitial changes were seen on X-rays.
  • Pulmonary function tests reveal a restrictive pattern with a decreased DLco.
  • Before starting treatment, consider baseline pulmonary function testing. Patients should be instructed to report any dyspnea that is new or worsening.
  • Interstitial pneumonitis symptoms can be detected. You should immediately stop using nilutamide until you are able to rule out a causal cause.

• Vision effects:

  • A delay was reported in adaptation to the darkness.
  • In clinical studies, this was reported by between 13 and 57 percent patients.
  • The delay between passing from a bright area to dark areas was from seconds to several minutes.
  • Wearing tinted sunglasses can help, but it is not a cure.
  • Patients who are experiencing adaptation delays in driving through tunnels or at night should be cautious.

• Cardiovascular disease

  • Androgen-deprivation therapy may increase the risk of cardiovascular disease (Levine 2010, 2010).
  • The QT/QTc interval has been lengthened by anti-androgen therapy that includes androgen deprivation therapy.
  • Patients with congenital long QT syndrome and heart failure should be evaluated for risk and benefit.
  • Patients at high risk of QT prolongation should have their electrolytes checked before initiation.

• Reduced bone mineral density

  • Antiandrogen therapy can lead to decreased bone mineral density and increased fracture risk.
  • The risk may be increased by alcohol abuse, familial history of osteoporosis, & chronic use of drugs capable of decreasing bone mass (eg, corticosteroids).
  • Be sure to carefully assess the risk before you begin therapy.

• Diabetes:

  • It has been proven that hyperglycemia can be treated.
  • Use caution in diabetic patients. Check for possible loss of glucose control.

Nilutamide: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

• CBC (periodic), liver function tests (transaminases at baseline, regularly during the first 4 months of treatment, & then periodically thereafter; more frequently if clinically indicated),
• electrolytes,
• serum testosterone,
• PSA,
• blood glucose & glycosylated hemoglobin (HbA1c) in patients with diabetes.
• Chest x-ray (baseline).
• Consider pulmonary function testing (baseline).
• Bone-mineral density (as clinically indicated in patients at risk of osteoporosis).
• ECG
• Signs & symptoms of liver dysfunction.
• Vision changes.
• Closely monitor prothrombin time, if initiating nilutamide in patients who are on warfarin.

How to administer Nilutamide (Ainedex)?

• Administer Without regard to meals.

Mechanism of action of Nilutamide (Ainedex):

• Nilutamide, a nonsteroidal anti-androgen, prevents androgen response. It blocks testosterone effects at androgen receptor levels.

Absorption:

• Rapid & complete

Metabolism:

• Hepatic (extensive)
• Forms active metabolites

Half-life elimination:

• Terminal:
  • 38-59 hours.
• Metabolites:
  • 59-126 hours

Excretion:

• Urine (62 percent; <2 percent as unchanged drug)
• Feces (1 percent to 7 percent)

International Brands of Nilutamide:

• Nilandron
• Anandron
• Ainedix

Nilutamide Brand Names in Pakistan:

No Brands Available in Pakistan.