Temsirolimus (Temsirolimusum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antineoplastic agents - inhibitors of protein kinases

Included in the formulation
  • Torizel®
    concentrate d / infusion 
    Pfizer Inc.     USA
    • АТХ:

    L.01.X.E.09   Temsirolimus

    Pharmacodynamics:

    Selectively inhibits mTOR-kinase (TOR - mammalian target of rapamycin), due to which the growth of tumor cells in the G1 phase ceases, as a result, the processes of protein translation that regulate the cell cycle are disrupted. At the same time blockade mTOR-kinase leads to a disruption in the production of angiogenic vascular endothelial growth factor, as a result of which the development of blood vessels slows down.

    Pharmacokinetics:

    After intravenous administration of 25 mg, the maximum plasma concentration is 585 ng / ml. The connection with plasma proteins is 50%.

    Metabolism in the liver, with the formation of an active metabolite of sirolimus.

    The half-life of tessirolimus is 17.7 hours, sirolimus 73.3 hours. Elimination by the kidneys.

    Indications:

    It is used in the therapy of the 1st line of advanced renal cell carcinoma.

    ICD-10

    II.C64-C68.C64   Malignant neoplasm of kidney, except for renal pelvis

    Contraindications:

    Individual intolerance, children under 18 years of age (no data on safety and efficacy).

    Carefully:

    Violations of liver function of medium or severe degree.

    Pregnancy and lactation:

    Recommendations for FDA - category D. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Intravenously drip for 60 minutes to 25 mg once a week. 30 minutes before infusion intravenously Antihistamine is administered diphenhydramine, in an amount of 25-50 mg.

    The highest daily dose: 25 mg.

    The highest single dose: 25 mg.

    Side effects:

    Central and peripheral nervous system: asthenia, rarely - intracranial hemorrhage.

    Respiratory system: pneumonitis (interstitial pulmonary process).

    Hemopoietic system: anemia, neutropenia, thrombocytopenia, leukopenia, febrile neutropenia, rarely - lymphopenia, coagulopathy.

    The cardiovascular system: thromboembolism, arterial hypertension, rarely pericardial effusion.

    Digestive system: stomatitis, abdominal pain, vomiting, anorexia, diarrhea, constipation, nausea, gastroesophageal reflux disease, esophagitis, colitis, intestinal obstruction, evacuation of stomach contents, dysphagia, gastrointestinal bleeding, gastritis, rarely intestinal perforation.

    Musculoskeletal system: back pain, myalgia, arthralgia, muscle weakness.

    Dermatological reactions: Alopecia, skin rash, syndrome eritrodizestezii fingers and toes, hyperpigmentation of the skin, itching, peeling skin, nail infections, rarely - erythema multiforme.

    Sense organs: Distortion or lack of taste, conjunctivitis, blurred vision, cataract, lacrimation, tinnitus.

    Urinary system: renal failure.

    Reproductive system: decreased potency.

    Allergic reactions.

    Overdose:

    Increased side effects.

    Treatment is symptomatic.

    Interaction:

    Inhibitors of the isoenzyme CYP3A4 temsirolimus slow metabolism and increase its concentration in plasma.

    Preparations that induce the isoenzyme CYP3A4 (dexamethasone, carbamazepine, rifabutin, phenytoin, phenobarbital, rifampicin, Preparations of Hypericum perforatum), temsirolimus accelerate metabolism and reduce its concentration in the blood plasma.

    Special instructions:

    The duration of treatment takes a long time - until the clinical efficacy is confirmed or toxicity is absent.

    Persons of reproductive age are recommended to use reliable methods of contraception during taking temsirolimus and within 3 months aftertreatment.

    Patients receiving treatment with tamsirolimus are prohibited from driving and working with moving mechanisms.
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