Flutamide, pills 250 mg, 84 pcs.

Composition

1 tablet contains:

Active ingredients:

flutamide 250 mg

. Pharmacological action

Flutamide is a non-steroidal drug with an antiandrogenic, antitumor effect.

Pharmacodynamics

Competitively blocks androgen receptors of target tissue cells and prevents androgen binding to them. Prevents the manifestation of biological effects of androgens in androgen-sensitive organs (including the prostate gland and seminal vesicles). After taking flutamide, there is an increase in plasma levels of testosterone and estradiol. The ability of flutamide to inhibit the action of testosterone at the cellular level serves as a supplement to the drug castration caused by gonadotropin-releasing hormone (GnRH) analogues.

Pharmacokinetics

When taken orally, it is rapidly and completely absorbed from the gastrointestinal tract. It is metabolized in the liver. At least 6 metabolites have been identified. The main metabolite found in blood plasma is the alpha-hydroxylated derivative (2-hydroxyflutamide) – it is biologically active. Binding to plasma proteins is 94-96% (flutamide) and 92-94% (2-oxyflutamide). _{Cmax of} 2-oxiflutamide — 2 h. T_1/2 of 2-oxiflutamide — 6 h (in elderly patients-8 h after a single dose and 9.6 h when a stable concentration is reached). It is mainly excreted by the kidneys in the form of metabolites,4.2% – in feces for 72 hours.

Indications

• Treatment of patients with advanced prostate cancer who have been shown to inhibit the action of testosterone
• Initial therapy in combination with an analog of LH/RH or in combination with orchiectomy (complex androgen blockade)
• Treatment of patients undergoing LH/RH analog therapy or undergoing surgical Ablatio testis
• Treatment of patients who have not been treated with endocrine forms of therapy or for whom such therapy is not tolerated, but who, if necessary, are indicated for them

Use during pregnancy and lactation

Not applicable.

Contraindications

Hypersensitivity, severe diseases of the liver, kidneys, and thyroid gland.

With caution: patients with reduced liver function, patients with a tendency to thrombosis and cardiovascular diseases.

Side effects

Endocrine disorders: gynecomastia and / or galactorrhea.

From the digestive system: nausea, vomiting, jaundice, diarrhea, increased activity of hepatic transaminases.

From the side of water-electrolyte metabolism: fluid retention.

Other: rarely-headache, thromboembolism, impaired renal function, sleep disorders, subcutaneous hemorrhage, lupus-like syndrome.

Interaction

It is believed that drug interaction is possible with the simultaneous use of flutamide with paracetamol, opioid analgesics, NSAIDs.

How to take, course of administration and dosage

of Flutamide is prescribed 1 tablet 3 times a 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 LHRH agonists, both drugs can be prescribed simultaneously or flutamide is started three days before the first administration of an LHRH agonist.

Overdose

Treatment: if the patient is conscious and without spontaneous vomiting, induce vomiting.

Monitoring of vital functions and symptomatic therapy are necessary.

Hemodialysis and peritoneal dialysis are ineffective (due to the high degree of binding to plasma proteins).

Special instructions

In the treatment of prostate cancer, liver function should be monitored (laboratory tests should be performed once a month for the first four months and then regularly).

If the level of liver enzymes increases by 2-3 times compared to the upper limit of normal values and/or jaundice occurs in the absence of liver metastases, the use of flutamide should be discontinued. If the first symptoms of liver dysfunction appear, such as pruritus, dark urine, nausea, vomiting, persistent loss of appetite, yellowing of the skin or whites of the eyes, pain in the right hypochondrium, or flu-like symptoms of unclear origin, you should immediately consult a doctor.

When evaluating the results of differential diagnosis of male hypogonadism, it is necessary to focus on the following indicators: in healthy people with normal basal gonadotropin excretion after administration of the drug, there is an increase in their excretion by 1.5 times or more; in primary hypogonadism, the initial gonadotropin excretion is significantly increased, less often – normal, the use of the drug leads to a further increase in their excretion by 1.5-2 times or more; in secondary hypogonadism, the initial gonadotropin excretion is reduced, less often – normal, a significant increase in their excretion after administration the drug is not observed.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature of 15-30 °C.

Shelf

life is 3 years.

Active ingredient

Flutamide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults by doctor’s prescription, For men

Weight

Weight: 88 gr.