Kalumid pills coated 50mg N30
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Active ingredients
Bicalutamide
Release form
Pills
Composition
Bicalutamide 50 mg; Excipients: colloidal silicon dioxide, magnesium stearate, povidone K30, sodium carboxymethyl starch (type A), lactose monohydrate .; The composition of the shell: opadry II33G28707 white (triacetin, macrogol 3000, lactose monohydrate, titanium dioxide, hypromellose).
Pharmacological effect
Antiandrogenic nonsteroid drug. It is a racemic mixture, with predominantly (R) -enantiomer having antiandrogenic activity. Does not possess other types of endocrine activity .; It binds to androgen receptors and, without activating gene expression, inhibits the stimulating effect of androgens. The result is a regression of malignant tumors of the prostate gland .; In some patients, discontinuation of bicalutamide may lead to the development of a clinical "antiandrogen withdrawal syndrome".
Pharmacokinetics
Absorption; After taking the drug inside, bicalutamide is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect absorption .; Distribution; Plasma protein binding is high (for the racemic mixture 96%, for the (R) -enantiomer 99.6%). It is extensively metabolized in the liver by oxidation and the formation of conjugates with glucuronic acid .; With daily intake of the drug Kalumid; the concentration of (R) -enantiomer in plasma increases by about 10 times due to prolonged T1 / 2, which makes it possible to take the drug 1 time / day; With daily intake of the drug Kalumid; in a dose of 50 mg Css (R) -enantiomer in plasma is about 9 μg / ml, and when taking 150 mg of the drug Kalumid; - 22 mcg / ml. At equilibrium, about 99% of all enantiomers circulating in the blood are active (R) -enantiomer .; Metabolism; Intensively metabolized in the liver (by oxidation and the formation of conjugates with glucuronic acid) .; Withdrawal; Metabolites are excreted by the kidneys and through the intestines in approximately equal proportions .; (S) -enantiomer is eliminated from the body much faster (R) -enantiomer, T1 / 2 of the last about 7 days .; Pharmacokinetics in special clinical situations; Pharmacokinetics of (R) -enantiomer does not depend on age, renal dysfunction, as well as mild or moderate liver dysfunction .; There is evidence that in patients with moderate or severely impaired liver function, elimination of the (R) -enantiomer from plasma slows down and cumulation of bicalutamide may be observed.
Indications
- common prostate cancer in combination therapy with the GnRH analogue (gonadotropin releasing hormone) or in combination with surgical castration (for 50 mg pills); - locally advanced prostate cancer (T3-T4, any N, M0; T1-T2, N +, M0) as monotherapy or adjuvant therapy in combination with radical prostatectomy or radiotherapy; - locally advanced non-metastatic prostate cancer in cases where surgical castration or other medical interventions are not applicable or unacceptable.
Contraindications
- simultaneous administration with terfenadine, astemizole, cisapride; - hypersensitivity to the components of the drug .; Kalumid; not prescribed for women and children .; With caution, you should prescribe the drug in violation of liver function, lactase deficiency, lactose intolerance, glucose / galactose malabsorption (in the medicinal form of the drug contains lactose).
Use during pregnancy and lactation
Bicalutamide is contraindicated in women and should not be given to pregnant and lactating mothers.
Dosage and administration
Adult men (including the elderly) with advanced prostate cancer in combination with a GnRH analogue or surgical castration, the drug is prescribed in a dose of 50 mg 1 time / day. Treatment with Kalumid; must begin simultaneously with the start of reception of GnRH analogue or surgical castration .; For locally advanced prostate cancer, 150 mg is prescribed 1 time per day. Kalumid; should be taken for a long time, at least for 2 years. If there is evidence of disease progression, the drug should be discontinued .; In case of impaired renal function, dose adjustment is not required .; In case of abnormal liver function, a mild dose adjustment is not required. In patients with moderate to severely impaired liver function, an increased cumulation of the drug may be observed.
Side effects
The pharmacological action of bicalutamide can cause the following side effects: Very often (≥10%): gynecomastia (it may persist even after stopping the therapy, especially when taking the drug for a long time), pain in the breasts, hot flashes .; Often (≥1% and <10%): diarrhea, nausea,transient increase in liver transaminases, cholestasis and jaundice (the described changes in liver function were rarely evaluated as serious, were transient, completely disappeared or decreased with continued therapy or after discontinuation of the drug), itching, asthenia; with the use of the drug in a daily dose of 150 mg - alopecia or restoration of hair growth, decreased sexual desire, sexual dysfunction, weight gain .; Rare (≥0.1% and <1%): hypersensitivity reactions, including angioedema and urticaria, interstitial pulmonary diseases; with the use of the drug in a daily dose of 150 mg - abdominal pain, depression, dyspepsia, hematuria .; Very rarely (≥0.01% and <0.1%): vomiting, dry skin (when using the drug in a daily dose of 150 mg, dry skin is often observed), hepatic failure (causal relationship with bicalutamide is not reliably established) .; With the simultaneous use of bicalutamide and gonadotropin-releasing hormone analogues (GnRH), the following side effects may occur with a frequency of> 1% (a causal relationship with the administration of the drug has not been established, some of the noted side effects have occurred in elderly patients) .; Since the cardiovascular system: heart failure .; On the part of the digestive system: anorexia, dry mouth, dyspepsia, constipation, flatulence .; Of the nervous system: dizziness, headache, insomnia, increased sleepiness .; On the part of the respiratory system: shortness of breath .; From the genitourinary system: sexual dysfunction, nocturia .; From the hematopoietic system: anemia .; From the skin and its appendages: alopecia, rash, excessive sweating, hirsutism .; Other: diabetes, hyperglycemia, increase or decrease in body weight, abdominal pain, chest pain, pain in the pelvic region, chills.
Overdose
Cases of overdose in humans are not described. The specific antidote is not known. Symptomatic treatment. Dialysis is not effective because bicalutamide binds strongly to proteins and is not excreted in the urine unchanged. General supportive treatment and strict control of vital body functions are recommended.
Interaction with other drugs
There are no data on pharmacokinetic or pharmacodynamic interactions between bicalutamide and GnRH analogues; In vitro studies have shown that (R) -enantiomer of bicalutamide inhibits CYP3A4, affecting CYP2C9, 2C19 and 2D6 activity to a lesser extent; The potential ability of bicalutamide to interact with other drugs was not found, but when using bicalutamide for 28 days while taking midazolam, the area under the AUC curve of midazolam is increased by 80% .; Incompatible with terfenadine, astemizole, cisapride .; Care should be taken when prescribing bicalutamide simultaneously with cyclosporine or calcium channel blockers. It may be necessary to reduce the dose of these drugs, especially in the case of potentiation or the development of side effects. After the use or withdrawal of bicalutamide has begun, careful monitoring of plasma cyclosporine concentration and the patient’s clinical status is recommended; The simultaneous use of bicalutamide and drugs that inhibit microsomal drug oxidation, for example, with cimetidine or ketoconazole, can lead to an increase in plasma bicalutamide concentration and, possibly, to an increase in the incidence of side effects .; Enhances the effect of coumarin anticoagulants, warfarin (competition for communication with proteins).
special instructions
Considering the possibility of slowing down the excretion of bicalutamide and its cumulation in patients with impaired liver function, it is advisable to periodically evaluate the function of the liver. Most changes in liver function occur during the first six months of treatment with Kalumid .; In the case of the development of pronounced changes in liver function, the intake of Kalumid must be stopped .; In patients with progression of the disease while increasing the level of the prostate-specific antigen (PSA), it is necessary to consider stopping treatment with Kalumid .; When Kalumid is prescribed, patients receiving coumarin anticoagulants are advised to regularly monitor their prothrombin time .; Considering the possibility of inhibition of cytochrome P450 (CYP3A4) activity by Kalumid, caution should be exercised with the simultaneous administration of Kalumid with drugs,predominantly metabolized by CYP3A4 .; Patients with lactose intolerance need to be informed that 1 tablet 50 mg contains 63.875 mg of lactose monohydrate, 1 tablet 150 mg contains 191.625 mg of lactose monohydrate .; Influence on ability to drive motor transport and control mechanisms; Kalumid; does not affect the ability of patients to drive vehicles or engage in other potentially dangerous activities that require increased concentration of attention and psychomotor speed.