Calumide

Kalumid is an effective medicine intended for the treatment of tumors.

Indications Calumide

Kalumid 50 mg is prescribed for the treatment of prostate cancer in the late stages. It is part of a complex treatment with therapy using luteinizing hormone releasing factor analogues or with surgical castration.

Kalumid with a volume of 150 mg is intended for monotherapy or as an additional agent during prostate removal or radiotherapy for patients with locally advanced prostate cancer with an increased risk of progression of the pathology.

Kalumid 150 mg is used in the treatment of non-metastatic locally advanced prostate cancer, in which surgical castration or other treatment methods cannot be used.

Release form

It is produced in the form of tablets, with a volume of 50 mg. One blister contains 15 tablets. One package contains 2 or 6 blister plates. Tablets with a volume of 150 mg are also produced. One blister plate contains 10 tablets, and the package contains 3 blisters.

Pharmacodynamics

Kalumid is an antiandrogen that has no other effect on the endocrine system. By binding to androgenic conductors, it weakens the effect of androgenic stimuli without activating gene expression. As a result of such suppression, the tumor that has developed in the prostate begins to regress. After discontinuing the drug, some patients may experience the so-called withdrawal syndrome.

Calumid is a racemic mixture with antiandrogenic properties. The drug is represented almost exclusively by the (R)-enantiomer.

Pharmacokinetics

Bicalutamide is rapidly absorbed after oral administration. Food has not been shown to have a clinically significant effect on the bioavailability of the drug.

The (S)-enantiomer is eliminated from the body quite quickly, compared to the (R)-enantiomer. The half-life of the latter from blood plasma is about 1 week.

In case of daily administration of the drug, the (R)-enantiomer, due to its long half-life, accumulates in the blood plasma in a 10-fold concentration.

The equilibrium concentration of the (R)-enantiomer is about 9 μg/ml when taking a daily dose of 50 mg of the drug, and about 22 μg/ml when taking a daily dose of 150 mg. In the stable phase, 99% of the total number of active enantiomers is the active (R)-enantiomer.

The pharmacokinetic properties of the active component are not affected by mild or moderate liver or kidney dysfunction, nor by the patient's age. There is evidence that in patients with severe liver dysfunction, the elimination of the (R)-enantiomer from the blood plasma occurs more slowly.

The drug has high plasma protein binding rates (96% for the racemate and over 99% for the (R)-enantiomer), it is effectively metabolized (through glucuronidation and oxidation), and its breakdown products are equally excreted in bile and urine.

There is evidence that the average level of (R)-bicalutamide in the semen of patients taking Calumid at a dosage of 150 mg is 4.9 mcg/ml. During intercourse, about 0.3 mcg/ml of bicalutamide can potentially enter the woman's body. This level is lower than the values at which changes in the offspring occurred in laboratory animals.

Dosing and administration

Oral medication for adult men. In the complex treatment of widespread prostate cancer in combination with surgical castration or taking GnRH analogues, the dosage is 50 mg 1 time per day. It should be taken into account that the use of Kalumid should be started simultaneously with the above treatment methods.

For locally advanced prostate cancer, you need to take 150 mg of the drug 1 time per day. The course of treatment should be long - at least 2 years.

If symptoms of pathology progression occur, the use of the drug should be stopped.

In case of kidney disorders, dosage adjustment is not necessary. In case of mild liver dysfunction, adjustment is also not necessary, but in case of severe or moderate forms, increased drug accumulation is possible.

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Contraindications

The medicine is contraindicated for children and women. In addition, it is prohibited for patients with individual intolerance to the active components or additional substances contained in the medicine.

Should not be used in combination with astemizole, cisapride or terfenadine.

Side effects Calumide

Side effects of the drug Calumid include:

• Lymphatic system and blood circulation – development of anemia;
• Immune system: Quincke's edema, hypersensitivity, and urticaria;
• Nutrition and metabolic processes: loss of appetite;
• Mental reactions: depression, decreased libido;
• NS: drowsiness, as well as dizziness;
• Heart: development of heart failure, as well as myocardial infarction;
• Vessels: the appearance of hot flashes;
• Chest, mediastinum, airways: interstitial lung disease;
• Digestive system: nausea, constipation and abdominal pain, as well as bloating and dyspepsia;
• Hepatobiliary system: jaundice, hepatotoxicity is observed, and in addition, liver failure, liver transaminases may be activated;
• Subcutaneous tissue and skin: baldness, rashes and itching, dry skin, hirsutism;
• Urinary organs and kidneys: development of hematuria;
• Mammary glands and reproductive system: pain in the mammary glands, gynecomastia, erectile problems;
• General disorders: swelling, chest pain, asthenia;
• Other: weight gain.

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Interactions with other drugs

Bicalutamide does not interact with GnRH analogues.

In vitro testing has shown that the (R)-enantiomer of the active substance inhibits CYP 3A4, but has little effect on the functioning of CYP 2C9, 2C19, and 2D6.

The potential ability of the active component of Calumid to interact with other drugs has not been identified, but in the case of using bicalutamide for 28 days in combination with midazolam, the AUC levels of this drug increase by 80%.

It is necessary to combine Kalumid with caution with such substances as cyclosporine, as well as with calcium antagonist drugs. It may be necessary to reduce the dosage of such drugs if potentiation has begun or side effects have appeared.

After starting or stopping the use of Calumid, it is recommended to carefully monitor the level of concentration in the blood plasma of cyclosporine, as well as monitor the clinical condition of the patient.

When combining Kalumid with drugs that suppress monooxygenase oxidation of drugs (such as ketoconazole and cimetidine), its concentration in the blood plasma may increase, and the occurrence of side effects may also increase.

The drug enhances the properties of coumarin anticoagulants, such as warfarin (competition occurs for binding to plasma proteins).

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Storage conditions

The medicine must be kept in a place out of reach of children. Temperature conditions – within 15-30°C.

Shelf life

Kalumid can be used for 5 years (if these are 50 mg tablets) or 2 years (if these are 150 mg tablets).