Aprocan

Aprocan (Flutamide) is a drug that belongs to a class of drugs called antiandrogens. It is used to treat prostate cancer, especially when combined with other drugs or treatments such as surgical removal of the testicles or radiation therapy.

Flutamide works by blocking the action of the male sex hormone testosterone in the body. Prostate cancer often depends on testosterone to grow. By blocking the action of testosterone, flutamide can help slow or stop tumor growth.

The drug is usually taken as a pill, often in combination with other medications or treatments. It is important to use it under the guidance of a doctor, as it can cause side effects and interact with other medications.

Indications Aprocana

Aprocan (flutamide) is used to treat prostate cancer. This drug is used as part of combination therapy, usually with other drugs or treatments such as surgical removal of the testicles (orchidectomy) or radiation therapy.

Prostate cancer often depends on male sex hormones, such as testosterone, to grow. Flutamide is an antiandrogen drug that blocks the action of testosterone in the body. This helps slow or stop tumor growth and may be effective in controlling prostate cancer.

Aprocan is typically used in patients with prostate cancer that has metastasized (spread to other organs) or in cases where it does not respond to other medications or treatments.

Release form

Aprokan (flutamide) is usually available in tablet form for oral administration. The tablets contain the active substance, flutamide, in a specific dosage.

These tablets are available in different dosages depending on the doctor's recommendations and the individual needs of the patient.

Typically, the drug is provided in packages containing a certain number of tablets, with instructions for use and storage.

Pharmacodynamics

Flutamide, the active ingredient in Aprokan, is an antiandrogen, meaning it blocks the action of male sex hormones, particularly testosterone. Prostate cancer often depends on testosterone to grow, and flutamide helps slow or stop this process.

Flutamide works by competing with testosterone for binding to androgen receptors in prostate tissue. Since testosterone cannot bind to androgen receptors, androgen-stimulated processes, such as prostate tumor growth, are slowed or stopped.

Flutamide has a weaker androgenic effect than testosterone, so its blockade does not cause prostate cancer progression. However, it can cause undesirable effects associated with decreased androgenic effect, such as gynecomastia (enlargement of the mammary glands in men), decreased libido, hypertension and, rarely, hepatic toxicity.

Overall, the pharmacodynamics of flutamide lies in its ability to suppress androgenic effects, which makes it effective in the treatment of prostate cancer.

Pharmacokinetics

• Absorption: Flutamide is well absorbed from the gastrointestinal tract after oral administration. Peak plasma concentrations are usually reached 2-5 hours after administration.
• Bioavailability: The bioavailability of flutamide is approximately 90%.
• Distribution: Flutamide has a high volume of distribution, meaning that it is distributed into various tissues and organs of the body, including the prostate. It is 94-96% bound to plasma proteins.
• Metabolism: Flutamide undergoes intensive metabolism in the liver to form an active metabolite, 2-hydroxyflutamide, which is biologically active and has an antiandrogenic effect.
• Excretion: The major route of elimination of flutamide from the body is the metabolic pathway via the liver. About 4-6% of the dose is excreted unchanged via the kidneys.
• Elimination half-life: The elimination half-life of flutamide in the body is approximately 6 hours.

Dosing and administration

• Dosage: The usual recommended starting dose for adults is 250 mg (one tablet) taken three times daily. However, the dosage may be adjusted by your doctor depending on your condition and response to treatment.
• Directions for use: Flutamide tablets are usually taken orally with water. They are best taken after meals.
• Duration of treatment: The duration of treatment and dosage regimen will be determined by your doctor according to the nature and severity of your disease.

Contraindications

• Hypersensitivity: Any known hypersensitivity to flutamide or other components of the drug is a contraindication to its use.
• Hepatitis or liver dysfunction: The drug should be used with caution or avoided in patients with liver dysfunction or previous cases of hepatitis.
• Hyperbilirubinemia: The drug should also be used with caution in patients with hyperbilirubinemia.
• Pregnancy and lactation: Flutamide is contraindicated in pregnant women because it may cause birth defects in the fetus. It is also contraindicated in nursing mothers because it may be excreted in breast milk.
• Symptomatic hypotension: The drug should be used with caution in patients with symptomatic hypotension, as it may cause a decrease in blood pressure.
• Patients with neurological or psychiatric disorders: In these patients, the use of flutamide also requires caution due to its potential effects on the nervous system.

Side effects Aprocana

• Gastrointestinal disorders: Includes nausea, vomiting, diarrhea, appetite disturbances and dyspepsia.
• Gynecomastia: Enlargement of the mammary glands in men can be one of the side effects of flutamide due to its antiandrogenic action.
• Decreased libido: Flutamide may cause decreased sexual desire in some patients.
• Hypertension: Some patients may experience increased blood pressure.
• Hyperprolactinemia: Increased levels of prolactin in the blood can lead to menstrual irregularities or hyperprolactinemic hypogonadism.
• Hepatotoxicity: In rare cases, flutamide may cause liver damage or hepatitis.
• Neurological effects: Include drowsiness, dizziness, asthenia, headache and sensory disturbances.
• Increased blood urea and creatinine: May be noted in some patients.
• Skin reactions: Include skin rash, itching and rarely hives.
• Weight Gain: Some patients may experience weight gain.

Overdose

• Drowsiness and general weakness: This may be one of the first signs of an overdose.
• Gastrointestinal disorders: Including nausea, vomiting and diarrhea.
• Dizziness and headache: Increased intensity of these symptoms may indicate overdose.
• Low blood pressure: This may lead to dizziness or even fainting.
• Increased levels of toxic metabolites: In case of overdose, concentrations of active metabolites of flutamide in the body may increase, which may lead to additional toxic effects.

Interactions with other drugs

• Warfarin (antiplatelet agents): Flutamide may enhance the anticoagulant effect of warfarin, which may increase the risk of bleeding. Frequent monitoring of prothrombin time is necessary.
• Cyclosporine (immunosuppressants): Flutamide may increase the concentration of cyclosporine in the blood, which may lead to toxic effects.
• Theophylline (bronchodilators): Flutamide may increase the blood concentration of theophylline, which may increase its toxic effects.
• Clarithromycin and erythromycin (macrolide antibiotics): These antibiotics may increase the concentration of flutamide in the blood, which may increase its toxic effects.
• Methylphenidate (medications used to treat attention deficit hyperactivity disorder): Flutamide may increase the blood levels of methylphenidate, which may result in increased effects or side effects.