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Flutamide

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Indications: This product is suitable for patients with advanced prostate cancer who have not previously been treated, or who have failed or failed in hormone control therapy. It can be used alone (testectomy or not) or stimulated with luteinizing hormone releasing hormone (LHRH)剂 合 合。 Combination of agents. As part of the treatment of localized B2-C2 (T2b-T4) type prostate cancer, this product can also reduce tumor volume and strengthen tumor control and extend disease-free survival.

Approval date: January 05, 2007

Date of revision: August 04, 2011 December 01, 2013 June 19, 2014 December 01, 2015

Please read the instructions carefully and use under the guidance of a physician

Disable allergic to this product

【Drug Name】

Common name: Flutamide tablets

English name: Flutamide Tablets

Phonetic script (Hanyu Pinyin): Futa'an Pian

[Ingredients]

The main ingredients of this product are: Flutamide

Chemical name: N- [4-nitro-3- (trifluoromethyl) phenyl] -2-propanamide

Molecular formula: C 11 H 11 F 3 N 2 O 3

Molecular weight: 276.21

[Character]

This product is a light yellow tablet.

[Specifications] 0.25g

[Dosage and Administration] Oral

The recommended dose for a single medication or a combination with an LHRH agonist is 250 mg three times daily at 8-hour intervals. When combined with LHRH agonist, both can be started at the same time, or use this product 24 hours before starting to use LHRH agonist.

The recommended dose for the treatment of localized prostate cancer is 250 mg three times daily with an interval of 8 hours. If an LHRH agonist is also used, this product should be taken at the same time as the LHRH agonist or 24 hours in advance. This product must be used 8 weeks before radiotherapy, and continuous use during radiotherapy.

【Adverse reactions】

Treatment alone:

The most common reports of adverse reactions to this product are men's breast development and / or breast tenderness, sometimes with galactorrhea. These adverse reactions will disappear with the reduction or withdrawal of medication.

The potential effect of this product on cardiovascular is small, compared with diethylstilbestrol, this effect appears smaller.

Rare side effects include nausea, vomiting, increased appetite, insomnia and fatigue, transient liver dysfunction and hepatitis (see "Other adverse reactions" and "Precautions" for the adverse reactions of the hepatobiliary system).

Rare adverse reactions are: decreased libido, upset stomach, anorexia, ulcer pain, heartburn, constipation, edema, ecchymosis, shingles, pruritus, lupus-like syndrome, headache, dizziness, fatigue, discomfort, blurred vision, Thirst, chest pain, anxiety, depression, lymphedema. Sperm count reduction is rarely reported.

Combination therapy:

When this product is combined with an LHRH agonist, the most common adverse reactions are hot flushes, decreased libido, impotence, diarrhea, nausea, and vomiting. In addition to diarrhea, these adverse reactions are also very common when the LHRH agonist is used alone.

The feminization of men's breasts is more frequent when flutamide is used alone, but it is greatly reduced during combination therapy. In controlled clinical trials, there was no significant difference in the incidence of feminization of male breasts between the placebo group and the combination of flutamide and LHRH agonists.

Rare side effects include anemia, leukocytopenia, non-specific gastrointestinal disorders, pruritus and rashes at the injection site, edema, neuromuscular symptoms, jaundice, urinary symptoms, hypertension, central nervous system adverse reactions (sleepiness, depression, coma, anxiety , Neuroticism), and thrombocytopenia.

Very rare interstitial lung disease, hepatitis, and light sensitivity.

Other adverse reactions:

In the worldwide sales and use of this product, the following adverse reactions have been reported: hemolytic anemia, giant cell anemia, methemoglobinemia, photoallergic reactions-including erythema, ulcers, herpes and epidermal necrosis-and amber or yellow Green urine, which may be caused by flutamide and / or its metabolites. Adverse reactions such as jaundice, hepatic encephalopathy, and liver necrosis have also been observed. Liver damage is usually reversible after discontinuation, however, serious liver damage and death have been reported with flutamide.

Rare hyperglycemia and diabetes worsening

Two reports of malignant male breast tumors caused by this product have been reported. One patient had hypertrophy of the prostate, and a breast nodule was found to increase after 3-4 months of treatment, and was diagnosed as poorly differentiated breast cancer after resection. Another case was a patient with advanced prostate cancer. Male breast feminization occurred 2 months after the treatment with this product, breast nodules were found 6 months, and nodules were removed and diagnosed as moderate differentiation infiltration 9 months after treatment. Sexual breast cancer T4NOMO, G3, no distant metastases.

Abnormal laboratory indicators include liver dysfunction, elevated serum urea nitrogen (BUN), and very few people have elevated serum creatinine.

[Contraindications] Those who are allergic to this product are prohibited.

[Caution] This product may cause liver damage. Patients with transaminase 2-3 times higher than normal should not take this product. All patients must undergo liver function tests on a regular basis. Regular laboratory tests should be performed monthly after the first four months, when symptoms / signs of abnormal liver function appear (for example: itching, deep urine, nausea, vomiting, persistent anorexia, jaundice, upper right Those who have abdominal tenderness or have unexplained flu-like symptoms) should take appropriate laboratory tests. In the case of laboratory examination results showing liver damage or jaundice in patients, but no liver metastasis has been confirmed, if patients have increased jaundice or transaminase is 2-3 times higher than the usual value, this product should be discontinued even without clinical symptoms .

When this product is treated with LHRH agonist in combination with Sichuan medicine, it is necessary to understand the possible adverse reactions of each medicine. Without guidance, patients cannot stop the medicine or change the dosage scheme at will.

Patient precautions

Before treatment, all patients should be informed that the drug may cause liver damage, and patients should be consulted immediately if symptoms of liver damage occur. These symptoms include itchy skin, dark urine (excluding light yellow or yellow-green Urine), nausea, vomiting, persistent loss of appetite, yellow sclera or skin jaundice, upper abdominal tenderness or "flu" -like symptoms.

[Medication for pregnant women and lactating women] This product is only suitable for male patients. There has been no research on the use of pregnant women and lactating women. However, the possibility of pregnant women taking this product to harm the fetus and the possibility of the drug in breast milk must be considered.

[Children's medication] This experiment has not been performed and there are no reliable references.

[Medicine for the elderly] See [Contraindications] [Precautions]

【medicine interactions】

In some patients receiving neodicoumarin combined with this product, prolonged prothrombin time was seen. Therefore, the prothrombin time must be measured to determine the first dose and the amount of maintenance anticoagulant.

There have been reports of increased theophylline plasma concentrations when this product is combined with theophylline. CYP 1A2 is the main metabolizing enzyme of theophylline, and it is also the main training enzyme for converting flutamide to its sexual substance 2-hydroxyflutamide.

[Drug overdose]

In animal tests using flutamide alone, signs of overdose are reduced activity, hair growth, slow breathing, ataxia and / or tearing, anorexia, quietness, vomiting, and methemoglobinemia.

A single dose of flutamide that causes overdose symptoms or is fatal has not yet been determined.

Due to the high protein binding capacity of flutamide, dialysis is not effective for overdose. As with any overdose, the effects of any medications you have ever taken should be considered. If there is no spontaneous vomiting, induce vomiting when the patient is awake, systemic supportive care, including frequent monitoring of various vital signs and close observation of the patient.

[Pharmacology and Toxicology]

Pharmacological effect: Flutamide tablet is a non-steroidal acetanilide oral anti-androgen, which can prevent the absorption of androgens in target cells and / or prevent the binding of androgens to the nucleus. Shows potent anti-androgenic effects.

Toxicology research: This product has not been confirmed to have a tendency to cause mutations by Ames test, DNA repair experiment, sister chromosomal swap in vivo, or dominant lethal factor analysis. Long-term dosing experiments on rats have found that this product can produce interstitial cell carcinoma and breast cancer.

【Pharmacokinetics】

This product is absorbed from the gastrointestinal tract after oral administration. Human pharmacokinetic studies show that most of this product is rapidly metabolized in the body, and the main active metabolite is α-hydroxyflutamide. With a single oral dose of 250mg, the metabolite reached its peak blood concentration in about 2 hours, the plasma protein binding rate was above 90%, and the elimination phase half-life was about 6 hours. The original drug and active metabolites are mainly distributed in the prostate, most of which are excreted in the body through urine and a small amount through feces.

[Storage] shading, sealed, and stored in a dry place.

[Packaging] Aluminum plastic, 12 pieces / board, 1 plate / box; plastic bottle, 50 pieces / bottle;

[Validity] 36 months

[Executive Standards] 2015 Chinese Pharmacopoeia

[Approval number] National Medicine Standard H19990144

【manufacturer】