Calumid

Kalumid is an effective drug designed to treat tumors.

Indications Calumid

Calumid with a volume of 50 mg is prescribed for the treatment of prostate cancer in later stages. It is part of a complex treatment with therapy with the help of analogues of the releasing factor of luteinizing hormone or with surgical castration.

Calumid with a volume of 150 mg is intended for monotherapy, or as an additional remedy for prostate removal or radiotherapy - for patients with a locally advanced form of prostate cancer with an increased risk of progression of the pathology.

Calumid with a volume of 150 mg is used in the treatment of non-metastatic form of locally advanced prostate cancer, in which it is impossible to apply surgical castration or other methods of treatment.

Release form

Produced in the form of tablets, 50 mg. In one blister 15 tab. 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 in the package - 3 blisters.

Pharmacodynamics

Kalumid is an antiandrogen that does not have any other effect on the endocrine system. Linking to androgenic conductors, it weakens the effect of androgenic stimuli, without activating gene expression. Due to this suppression, the tumor developing in the prostate begins to regress. After the abolition of the use of the medicine in individual patients, the so-called. Withdrawal syndrome.

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

Pharmacokinetics

Bicalutamide is rapidly absorbed after internal use. It is not proven that eating has a clinically significant effect on the bioavailability of the drug.

(S) -enantiomer is rapidly removed from the body, in comparison with the (R) -enantiomer. The half-life from the blood plasma of the latter is about 1 week.

In the case of a daily medication, the (R) -enantiomer is cumulated in the blood plasma at a 10-fold concentration because of a prolonged half-life.

The equilibrium concentration of the (R) -enantiomer in the range of about 9 μg / ml is noted when a daily dosage of 50 mg of the drug is used, as well as about 22 μg / ml when a daily dosage of 150 mg is administered. In the stable phase, 99% of the total number of enantiomers is active (R) -enantiomer.

The pharmacokinetic properties of the active ingredient are not affected by mild or moderate disorders in the liver, as well as the kidneys, and with it the age of the patient. There is evidence that in patients who have severe disorders in the liver, removing (R) -enantiomer from the blood plasma is slower.

The drug has high plasma protein binding (96% for the racemate, and more than 99% for the (R) -enantiomer), it is efficiently metabolized (through glucuronization as well as oxidation), and the products of its decay are equally deduced together with bile and urine.

There is evidence that the mean (R) -bicalutamide value contained in the semen of patients who consumed Calumid at a dosage of 150 mg is 4.9 μg / ml. In the process of sexual intercourse, about 0.3 μg / ml of bicalutamide can potentially enter the woman's body. This level is lower than the indices at which in laboratory animals the offspring changed.

Dosing and administration

Medication for oral administration, adult men. In the complex treatment of a common form of prostate cancer in conjunction with surgical castration or the admission of GnRH analogues, the dosage is 50 mg 1 r./day. It should be borne in mind that the use of Kalumid should start simultaneously with the above methods of treatment.

With the locally advanced form of prostate cancer, you need to drink 150 mg of medicine 1 p. / Day. The course of treatment should be long - at least 2 years.

In case of symptoms of progression of the pathology, the use of the drug should be discontinued.

In disorders in the work of the kidneys, you do not need to adjust the dosage. With a mild form of liver function disorder, correction is also not needed, but in the case of a severe or moderate form, an increased cumulation of the drug is possible.

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Contraindications

The drug is contraindicated for children, as well as for women. In addition, it is forbidden to use to patients with individual intolerance active ingredients or additional substances contained in drugs.

Do not use in combination with astemizole, as well as cisapride and terfenadine.

Side effects Calumid

Among the adverse reactions to the drug Kalumid:

• Lymphatic system and circulation - development of anemia;
• The immune system: Quincke's edema, hypersensitivity, and urticaria;
• Nutrition and metabolic processes: deterioration 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 tides;
• Thorax, mediastinum, respiratory tract: interstitial pathology of the lungs;
• Digestion system: nausea, constipation and pain in the abdomen, as well as swelling and indigestion;
• Hepatobiliary system: jaundice, hepatotoxicity is observed, and in addition liver failure, hepatic transaminases may become more active;
• Subcutaneous fat and skin: alopecia, rashes and itchy skin, dry skin, hirsutism;
• Urinary organs and kidneys: development of hematuria;
• Mammary glands and reproductive system: pain in the mammary glands, gynecomastia, problems with erection;
• General disorders: swelling, chest pain, and asthenia;
• Other: weight gain.

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Interactions with other drugs

Bicalutamide does not interact with GnRH analogues.

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

No potential potency of the active component of Kalumid was found to interact with other drugs, but in the case of bicalutamide for 28 days. In combination with midazolam, AUC levels of this drug are increased by 80%.

It is necessary to carefully combine Kalumid with substances such as cyclosporine, as well as with calcium antagonist drugs. You may need to reduce the dosage of such drugs if potentiation starts or if side effects appear.

After the beginning of the application or the abolition of the use of Kalumid, it is recommended to closely monitor the level of concentration in the blood plasma of cyclosporine, and also to monitor the clinical condition of the patient.

When Kalumida is combined with drugs that suppress monooxygenase oxidation of drugs (such as ketoconazole, as well as cimetidine), its concentration in the blood plasma can increase, and there may be an increase in the occurrence of adverse reactions.

The drug enhances the properties of coumarin anticoagulants - for example, warfarin (there is competition for binding to plasma proteins).

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Storage conditions

Keep the medicine in a place that is not accessible to children. Temperature conditions - within 15-30 ° C.

Shelf life

Kalumid can be used for 5 years (if it's 50 mg tablets) or 2 years (if it's 150 mg tablets).