Flutamide

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Available since: 2019-09-19

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Clinical Pharmacology

Flutamide is a nonsteroid drug with antiandrogenic effects. The mechanism of action includes inhibition of androgen uptake and / or inhibition of androgen binding in the nuclei of target tissue cells. Its ability to inhibit the action of testosterone at the cellular level complements drug castration caused by gonadotropin releasing hormone agonists (GnRH).
The target organs of pharmacological action of flutamide are the prostate gland and seminal vesicles. Flutamide does not possess estrogenic, antiestrogenic, progestogenic and anti-progestogenic activity.
Pharmacokinetics
The drug is completely and rapidly absorbed after oral administration, undergoing biotransformation in the liver. The main metabolite found in plasma, the Cmax of which is reached after 2 hours, is a biologically active α-hydroxylated derivative (2-hydroxyflutamide). 94-96% of flutamide and 92-94% of the α-hydroxylated metabolite binds to proteins. The drug is mainly excreted from the body by the kidneys, approximately 4.2% is excreted through the intestine within 72 hours. T1 / 2 of the active metabolite from plasma is about 6 hours (in elderly patients - 8 hours after a single dose and 9.6 hours at a stable concentration). After ingestion of flutamide 250 mg 3 times / day, a stable concentration of the drug and its active metabolite in plasma is reached after the fourth dose of the drug.

Indications

Treatment of metastatic prostate cancer when testosterone suppression is indicated:

at the beginning of treatment in combination with GnRH agonists;
as an additional treatment for patients already receiving treatment with GnRH agonists;
in patients with surgical castration;
treatment of patients in whom other types of hormone therapy were ineffective or with intolerance to such treatment.

Composition

Excipients: lactose monohydrate - 150 mg, microcrystalline cellulose - 50 mg, corn starch - 30 mg, sodium lauryl sulfate - 10 mg, silicon dioxide colloid - 5 mg, magnesium stearate - 5 mg.

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Dosage and Administration

For oral use. 250 mg 3 times / day every 8 hours. If a positive effect is achieved, the drug is used until signs of progression of the tumor disease appear.
In the case of combined therapy with GnRH agonists, both drugs can be administered simultaneously or flutamide is started three days before the first dose of GnRH agonist.

Adverse reactions

The frequency of side effects is described in accordance with the following gradation: most often (10% and above), less often (from 1 to 10%), rarely (less than 1%).
When using the drug in monotherapy:
Most often: gynecomastia and / or pain in the chest glands, sometimes accompanied by galactorrhea. These phenomena disappear after discontinuation of treatment or dose reduction.
Less often: diarrhea, nausea, vomiting, increased appetite, insomnia, fatigue, transient liver dysfunction, hepatitis.
Rarely: hepatitis or jaundice (including cholestatic), hepatic necrosis, hepatic encephalopathy, increased transaminase activity (these side effects are usually reversible after cessation of therapy, however, there were reports of deaths due to severe hepatic insufficiency with flutamide therapy); subcutaneous hemorrhage, shingles, pruritus, lupus-like syndrome; anorexia, heartburn, constipation, dyspepsia; decreased libido, headache, hot flashes (sensation of heat, excessive sweating), increased blood pressure, dizziness, weakness, blurred vision, thirst, chest pain, swelling (fingers, feet, legs), anxiety, depression and thrombocytopenia . With prolonged treatment, spermatogenesis was suppressed. Individual cases of hemolytic anemia, macrocytic anemia, methemoglobinemia, hypersensitivity reactions (including erythema, skin ulceration, bullous rash, epidermal necrolysis) were noted. Sometimes patients have a change in the color of urine from amber to yellow-green.
When treated in combination with GnRH agonists
Most often: "hot flashes" (sensation of heat, excessive sweating), decreased libido, impotence, diarrhea, nausea, vomiting. The incidence of these side effects, with the exception of diarrhea (more pronounced when used in combination with flutamide), is the same as with monotherapy with GnRH agonists.
Less often: gynecomastia, anemia, leukopenia, thrombocytopenia, lack of appetite, edema, symptoms of neuromuscular disorders, difficulty urinating, increased blood pressure and side effects from the central nervous system (drowsiness, depression, confusion, anxiety, neurosis).
Rarely: respiratory failure, hepatic failure, hepatitis, cholestatic jaundice, liver necrosis, hepatic encephalopathy, increased photosensitivity, methemoglobinemia.

Contraindications

With care: in patients with reduced liver function, with a tendency to thrombosis and in cardiovascular diseases, as well as in conditions that predispose to aniline intoxication (one of the metabolites of flutamide, methylaniline derivative): deficiency of glucose-b-phosphate dehydrogenase, smoking, hemoglobinopathy (M-hemoglobin).

Drug interactions

Due to the possible enhancement of the anticoagulant action with simultaneous use of warfarin and Flutamide, the dose of anticoagulant should be selected under the control of prothrombin time.

Special instructions

Flutamide treatment should be carried out under control of the level of liver enzymes in the blood serum (appropriate laboratory tests should be carried out 1 time per month for the first 4 months and more regularly).
If the level of liver enzymes increases by 2-3 times compared with the upper limit of normal values and / or the appearance of jaundice in the absence of metastases in the liver, the use of Flutamide should be discontinued.
Patients should receive a recommendation to immediately consult a doctor when the first symptoms of abnormal liver function appear, such as pruritus, dark urine, nausea, vomiting, persistent loss of appetite, yellowness of the skin or sclera, pain in the right upper quadrant or flu-like symptoms.

Overdosage

In case of overdose, if the patient is conscious and without spontaneous vomiting, induce vomiting. Symptomatic therapy should be used with constant monitoring of the patient and vital functions. Due to the high degree of association with plasma proteins, hemodialysis is practically ineffective.