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Nilutamide

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Overview

What is Nilandron?

NILANDRON tablets contain nilutamide, a nonsteroidal, orally active antiandrogen having the chemical name 5,5-dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]-2,4-imidazolidinedione with the following structural formula:

Nilutamide is a microcrystalline, white to practically white powder with a molecular weight of 317.25.

Its molecular formula is CHFNO.

It is freely soluble in ethyl acetate, acetone, chloroform, ethyl alcohol, dichloromethane, and methanol. It is slightly soluble in water [
Each NILANDRON tablet contains 150 mg of nilutamide. Other ingredients in NILANDRON tablets are corn starch, lactose, povidone, docusate sodium, magnesium stearate, and talc.



What does Nilandron look like?



What are the available doses of Nilandron?

Sorry No records found.

What should I talk to my health care provider before I take Nilandron?

Sorry No records found

How should I use Nilandron?

The recommended dosage is 300 mg once a day for 30 days, followed thereafter by 150 mg once a day. NILANDRON tablets can be taken with or without food.


What interacts with Nilandron?


  • NILANDRON tablets are contraindicated:

    • in patients with severe hepatic impairment (baseline hepatic enzymes should be evaluated prior to treatment)
    • in patients with severe respiratory insufficiency
    • in patients with hypersensitivity to nilutamide or any component of this preparation.



What are the warnings of Nilandron?

Interstitial Pneumonitis

Interstitial pneumonitis has been reported in 2% of patients in controlled clinical trials in patients exposed to nilutamide. A small study in Japanese subjects showed that 8 of 47 patients (17%) developed interstitial pneumonitis. Reports of interstitial changes including pulmonary fibrosis that led to hospitalization and death have been reported rarely post-marketing. Symptoms included exertional dyspnea, cough, chest pain, and fever. X-rays showed interstitial or alveolo-interstitial changes, and pulmonary function tests revealed a restrictive pattern with decreased DLco. Most cases occurred within the first 3 months of treatment with NILANDRON, and most reversed with discontinuation of therapy. A routine chest X-ray should be performed prior to initiating treatment with NILANDRON. Baseline pulmonary function tests may be considered. Patients should be instructed to report any new or worsening shortness of breath that they experience while on NILANDRON.

Hepatitis

Rare cases of death or hospitalization due to severe liver injury have been reported post-marketing in association with the use of NILANDRON. Hepatotoxicity in these reports generally occurred within the first 3 to 4 months of treatment. Hepatitis or marked increases in liver enzymes leading to drug discontinuation occurred in 1% of NILANDRON patients in controlled clinical trials.

Serum transaminase levels should be measured prior to starting treatment with NILANDRON, at regular intervals for the first 4 months of treatment, and periodically thereafter. Liver function tests should also be obtained at the first sign or symptom suggestive of liver dysfunction, e.g. nausea, vomiting, abdominal pain, fatigue, anorexia, "flu-like" symptoms, dark urine, jaundice, or right upper quadrant tenderness. If at any time, a patient has jaundice, or their ALT rises above 2 times the upper limit of normal, NILANDRON should be immediately discontinued with close followup of liver function tests until resolution.

Use in Women

NILANDRON has no indication for women, and should not be used in this population, particularly for non-serious or non-life threatening conditions.

Other

Foreign postmarketing surveillance has revealed isolated cases of aplastic anemia in which a causal relationship with NILANDRON could not be ascertained.


What are the precautions of Nilandron?

General

Patients whose disease progresses while being treated with an antiandrogen may experience clinical improvement with discontinuation of the antiandrogen.

Information For Patients

Patients should be informed that NILANDRON tablets should be started on the day of, or on the day after, surgical castration. They should also be informed that they should not interrupt their dosing of NILANDRON or stop taking this medication without consulting their physician.

Because of the possibility of interstitial pneumonitis, patients should also be told to report immediately any dyspnea or aggravation of pre-existing dyspnea.

Because of the possibility of hepatitis, patients should be told to consult with their physician should nausea, vomiting, abdominal pain, or jaundice occur.

Because of the possibility of an intolerance to alcohol (facial flushes, malaise, hypotension) following ingestion of NILANDRON, it is recommended that intake of alcoholic beverages be avoided by patients who experience this reaction. This effect has been reported in about 5% of patients treated with NILANDRON.

In clinical trials, 13% to 57% of patients receiving NILANDRON reported a delay in adaptation to dark, ranging from seconds to a few minutes, when passing from a lighted area to a dark area. This effect sometimes does not abate as drug treatment is continued. Patients who experience this effect should be cautioned about driving at night or through tunnels. This effect can be alleviated by the wearing of tinted glasses.

Drug Interactions

In vitro, nilutamide has been shown to inhibit the activity of liver cytochrome P-450 isoenzymes and, therefore, may reduce the metabolism of compounds requiring these systems.

Consequently, drugs with a low therapeutic margin, such as vitamin K antagonists, phenytoin, and theophylline, could have a delayed elimination and increases in their serum half-life leading to a toxic level. The dosage of these drugs or others with a similar metabolism may need to be modified if they are administered concomitantly with nilutamide. For example, when vitamin K antagonists are administered concomitantly with nilutamide, prothrombin time should be carefully monitored and, if necessary, the dosage of vitamin K antagonists should be reduced.

Carcinogenesis, Mutagenesis, Impairment Of Fertility

Administration of nilutamide to rats for 18 months at doses of 0, 5, 15, or 45 mg/kg/day produced benign Leydig cell tumors in 35% of the high-dose male rats (AUC exposures in high-dose rats were approximately 1–2 times human AUC exposures with therapeutic doses). The increased incidence of Leydig cell tumors is secondary to elevated luteinizing hormone (LH) concentrations resulting from loss of feedback inhibition at the pituitary. Elevated LH and testosterone concentrations are not observed in castrated men receiving NILANDRON. Nilutamide had no effect on the incidence, size, or time of onset of any spontaneous tumor in rats.

Nilutamide displayed no mutagenic effects in a variety of in vitro and in vivo tests (Ames test, mouse micronucleus test, and two chromosomal aberration tests).

In reproduction studies in rats, nilutamide had no effect on the reproductive function of males and females, and no lethal, teratogenic, or growth-suppressive effects on fetuses were found. The maximal dose at which nilutamide did not affect reproductive function in either sex or have an effect on fetuses was estimated to be 45 mg/kg orally (AUC exposures in rats approximately 1–2 times human therapeutic AUC exposures).

Pregnancy

Pregnancy Category C; Animal reproduction studies have not been conducted with nilutamide. It is also not known whether nilutamide can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. Nilutamide should be given to a pregnant woman only if clearly needed.

Pediatric Use

Safety and effectiveness in pediatric patients have not been determined.

Animal Pharmacology and Toxicology

Administration of NILANDRON to beagle dogs resulted in drug-related deaths at dose levels that produce AUC exposures in dogs much lower than the AUC exposures of men receiving the therapeutic doses of 150 and 300 mg/day. Nilutamide-induced toxicity in dogs was cumulative with progressively lower doses producing death when given for longer durations. Nilutamide given to dogs at 60 mg/kg/day (1–2 times human AUC exposure) for 1 month produced 100% mortality. Administration of 20 and 30 mg/kg/day nilutamide (1/2–1 times human AUC exposure) for 6 months resulted in 20% and 70% mortality in treated dogs. Administration to dogs of 3, 6, and 12 mg/kg/day nilutamide (1/10–1/2 human AUC exposure) for 1 year resulted in 8%, 33%, and 50% mortality, respectively. Pathology data from the one-year oral toxicity study suggest that the deaths in dogs were secondary to liver toxicity. Marked-to-massive hepatocellular swelling and vacuolization were observed in affected dogs. Liver toxicity in dogs was not consistently associated with elevations of liver enzymes.

Administration of nilutamide to rats at a dose level of 45 mg/kg/day (AUC exposure in rats 1–2 times human therapeutic AUC exposures) for 18 months increased the incidence of lung pathology (granulomatous inflammation and chronic alveolitis).

The hepatic and pulmonary adverse effects observed in nilutamide-treated animals and men are similar to effects observed with another nitroaromatic compound, nitrofurantoin. Nilutamide and nitrofurantoin are both metabolized in vitro to nitroanion free-radicals by microsomal NADPH-cytochrome P450 reductase in the lungs and liver of rats and humans.


What are the side effects of Nilandron?

The following adverse experiences were reported during a multicenter clinical trial comparing NILANDRON + surgical castration versus placebo + surgical castration. The most frequently reported (greater than 5%) adverse experiences during treatment with NILANDRON tablets in combination with surgical castration are listed below. For comparison, adverse experiences seen with surgical castration and placebo are also listed.

The overall incidence of adverse experiences was 86% (194/225) for the NILANDRON group and 81% (188/232) for the placebo group.

The following adverse experiences were reported during a multicenter clinical trial comparing NILANDRON + leuprolide versus placebo + leuprolide. The most frequently reported (greater than 5%) adverse experiences during treatment with NILANDRON tablets in combination with leuprolide are listed below. For comparison, adverse experiences seen with leuprolide and placebo are also listed.

The overall incidence of adverse experiences is 99.5% (208/209) for the NILANDRON group and 98.5% (199/202) for the placebo group.

Some frequently occurring adverse experiences, for example hot flushes, impotence, and decreased libido, are known to be associated with low serum androgen levels and known to occur with medical or surgical castration alone. Notable was the higher incidence of visual disturbances (variously described as impaired adaptation to darkness, abnormal vision, and colored vision), which led to treatment discontinuation in 1% to 2% of patients.

Interstitial pneumonitis occurred in one (
In addition, the following adverse experiences were reported in 2 to 5% of patients treated with NILANDRON in combination with leuprolide or orchiectomy.

Body as a Whole:

Cardiovascular System:

Digestive System:

Metabolic and Nutritional System:

Musculoskeletal System:

Nervous System:

Respiratory System:

Skin and Appendages:

Special Senses:

Laboratory Values:

Adverse ExperienceNILANDRON +surgical castration (N=225)% AllPlacebo+surgical castration (N=232)% All
Cardiovascular System
  Hypertension5.32.6
Digestive System
  Nausea9.86.0
  Constipation7.13.9
Endocrine System
  Hot flushes28.422.4
Metabolic and Nutritional System
  Increased AST8.03.9
  Increased ALT7.64.3
Nervous System
  Dizziness7.13.4
Respiratory System
  Dyspnea6.27.3
Special Senses
  Impaired adaptation to dark12.91.3
  Abnormal vision6.71.7
Urogenital System
  Urinary tract infection8.09.1
Adverse ExperienceNILANDRON +leuprolide (N=209) % AllPlacebo + leuprolide (N=202) % All
Body as a Whole
  Pain26.827.7
  Headache13.910.4
  Asthenia19.120.8
  Back pain11.516.8
  Abdominal pain10.05.4
  Chest pain7.24.5
  Flu syndrome7.23.0
  Fever5.36.4
Cardiovascular System
  Hypertension9.19.9
Digestive System
  Nausea23.98.4
  Constipation19.616.8
  Anorexia11.06.4
  Dyspepsia6.74.5
  Vomiting5.74.0
Endocrine System
  Hot flushes66.559.4
  Impotence11.012.9
  Libido decreased11.04.5
Hemic and Lymphatic System
  Anemia7.26.4
Metabolic and Nutritional System
  Increased AST12.913.9
  Peripheral edema12.417.3
  Increased ALT9.18.9
Musculoskeletal System
  Bone Pain6.25.0
Nervous System
  Insomnia16.315.8
  Dizziness10.011.4
  Depression8.67.4
  Hypesthesia5.32.0
Respiratory System
  Dyspnea10.57.4
  Upper respiratory infection8.110.9
  Pneumonia5.33.5
Skin and Appendages
  Sweating6.23.0
  Body hair loss5.70.5
  Dry skin5.32.5
  Rash5.34.0
Special Senses
  Impaired adaptation to dark56.95.4
  Chromatopsia8.60.0
  Impaired adaptation to light7.71.0
  Abnormal vision6.24.5
Urogenital System
  Testicular atrophy16.312.4
  Gynecomastia10.511.9
  Urinary tract infection8.621.3
  Hematuria8.17.9
  Urinary tract disorder7.210.4
  Nocturia6.76.4



What should I look out for while using Nilandron?

NILANDRON tablets are contraindicated:


What might happen if I take too much Nilandron?

One case of massive overdosage has been published. A 79-year-old man attempted suicide by ingesting 13 g of nilutamide (i.e., 43 times the maximum recommended dose). Despite immediate gastric lavage and oral administration of activated charcoal, plasma nilutamide levels peaked at 6 times the normal range 2 hours after ingestion. There were no clinical signs or symptoms or changes in parameters such as transaminases or chest X-ray. Maintenance treatment (150 mg/day) was resumed 30 days later.

In repeated-dose tolerance studies, doses of 600 mg/day and 900 mg/day were administered to 9 and 4 patients, respectively. The ingestion of these doses was associated with gastrointestinal disorders, including nausea and vomiting, malaise, headache, and dizziness. In addition, a transient elevation in hepatic enzyme levels was noted in one patient.

Since nilutamide is protein bound, dialysis may not be useful as treatment for overdose. As in the management of overdosage with any drug, it should be borne in mind that multiple agents may have been taken. If vomiting does not occur spontaneously, it should be induced if the patient is alert. General supportive care, including frequent monitoring of the vital signs and close observation of the patient, is indicated.


How should I store and handle Nilandron?

Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP] .NILANDRON 150 mg tablets are supplied in boxes of 30 tablets. Each box contains 3 child-resistant, PVC, aluminum foil-backed blisters of 10 tablets (NDC 0088-1111-14). Each white, biconvex, cylindrical (10 mm in diameter) tablet has a triangular logo on one side and an internal reference number (168D) on the other. Store at 25°C (77°F); excursions permitted between 15–30°C (59–86°F) [see USP Controlled Room Temperature]. Protect from light.NILANDRON 150 mg tablets are supplied in boxes of 30 tablets. Each box contains 3 child-resistant, PVC, aluminum foil-backed blisters of 10 tablets (NDC 0088-1111-14). Each white, biconvex, cylindrical (10 mm in diameter) tablet has a triangular logo on one side and an internal reference number (168D) on the other. Store at 25°C (77°F); excursions permitted between 15–30°C (59–86°F) [see USP Controlled Room Temperature]. Protect from light.


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Clinical Information

Chemical Structure

No Image found
Clinical Pharmacology

Prostate cancer is known to be androgen sensitive and responds to androgen ablation. In animal studies, nilutamide has demonstrated antiandrogenic activity without other hormonal (estrogen, progesterone, mineralocorticoid, and glucocorticoid) effects. In vitro, nilutamide blocks the effects of testosterone at the androgen receptor level. In vivo, nilutamide interacts with the androgen receptor and prevents the normal androgenic response.

Non-Clinical Toxicology
NILANDRON tablets are contraindicated:

In vitro, nilutamide has been shown to inhibit the activity of liver cytochrome P-450 isoenzymes and, therefore, may reduce the metabolism of compounds requiring these systems.

Consequently, drugs with a low therapeutic margin, such as vitamin K antagonists, phenytoin, and theophylline, could have a delayed elimination and increases in their serum half-life leading to a toxic level. The dosage of these drugs or others with a similar metabolism may need to be modified if they are administered concomitantly with nilutamide. For example, when vitamin K antagonists are administered concomitantly with nilutamide, prothrombin time should be carefully monitored and, if necessary, the dosage of vitamin K antagonists should be reduced.

The following adverse experiences were reported during a multicenter clinical trial comparing NILANDRON + surgical castration versus placebo + surgical castration. The most frequently reported (greater than 5%) adverse experiences during treatment with NILANDRON tablets in combination with surgical castration are listed below. For comparison, adverse experiences seen with surgical castration and placebo are also listed.

The overall incidence of adverse experiences was 86% (194/225) for the NILANDRON group and 81% (188/232) for the placebo group.

The following adverse experiences were reported during a multicenter clinical trial comparing NILANDRON + leuprolide versus placebo + leuprolide. The most frequently reported (greater than 5%) adverse experiences during treatment with NILANDRON tablets in combination with leuprolide are listed below. For comparison, adverse experiences seen with leuprolide and placebo are also listed.

The overall incidence of adverse experiences is 99.5% (208/209) for the NILANDRON group and 98.5% (199/202) for the placebo group.

Some frequently occurring adverse experiences, for example hot flushes, impotence, and decreased libido, are known to be associated with low serum androgen levels and known to occur with medical or surgical castration alone. Notable was the higher incidence of visual disturbances (variously described as impaired adaptation to darkness, abnormal vision, and colored vision), which led to treatment discontinuation in 1% to 2% of patients.

Interstitial pneumonitis occurred in one (
In addition, the following adverse experiences were reported in 2 to 5% of patients treated with NILANDRON in combination with leuprolide or orchiectomy.

Body as a Whole:

Cardiovascular System:

Digestive System:

Metabolic and Nutritional System:

Musculoskeletal System:

Nervous System:

Respiratory System:

Skin and Appendages:

Special Senses:

Laboratory Values:

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72
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Tips

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Interactions

Interactions

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