Semisynthetic derivative of camptothecin, a specific inhibitor of the cellular enzyme topoisomerase I. In tissues the drug is metabolized to the active metabolite which is superior to the activity of Irinotecan. And Irinotecan metabolite complex is stabilized with a side effects of trenbolone enanthate DNA topoisomerase I, which prevents its replication. The pharmacokinetic profile of irinotecan not dose-dependent. Metabolized mainly in the liver by an enzyme karboksiesterazy to the active metabolite. The distribution of the drug in the plasma or di- three-phase. The average half-life of the drug in the first phase of 12 minutes, the second phase – 2.5 hours in the last phase – 14.2 hours. Maximum plasma concentrations of irinotecan and was achieved by the end of intravenous infusion at the recommended dose of ;. With the urine within 24 hours on average, of unchanged drug and as a metabolite . Since bile displayed about of the drug is in an unmodified form, or as a metabolite glucuronide. Contact of blood plasma proteins for irinotecan is approximately , to its active metabolite and calcium folinate does not affect the pharmacokinetics of irinotecan.
Indications for Use
Locally advanced or metastatic cancer of the colon and rectum:
- Increased sensitivity to irinotecan or other ingredients.
- Chronic inflammatory bowel disease and / or disorder of the intestinal permeability.
- Severe depression of medullary hematopoiesis.
- The level of serum bilirubin, exceeding by more than 1.5 times the upper limit of normal (ULN).
- The general condition of the patients, as measured by the scale of the WHO> 2.
- Pregnancy and lactation.
- Children’s age (safety and efficacy data in children side effects of trenbolone enanthate are not available).Precautions : radiotherapy (in history) on the area of the abdomen or pelvis; leukocytosis; female patients (increased risk of diarrhea).
Dosing and Administration
The drug is intended for adults only.
Iritis administered as an intravenous infusion lasting at least 30 minutes and no more than 90 minutes.
When choosing the dose and mode of administration in each individual case should be referred to the literature.
In monotherapy: Irit used in . a dose of 350 mg / m² every 3 weeks
in a dose of combination chemotherapy iritis is:
- with 5-fluorouracil and folinic acid with the weekly administration – 80 mg / m²,
- when administered by continuous infusion of 1 times a week ² – 180 mg / m²;
- in combination with a bolus of 5-fluorouracil and calcium folinate -. 125 mg / m weekly
Dose and mode of administration of 5-fluorouracil and calcium folinate described in detail in the literature.
Introduction iritis should not be performed as long as the number of side effects of trenbolone enanthate neutrophils in the peripheral blood exceeds 1500 cells / ml, and until they are fully cropped complications such as nausea, vomiting and especially diarrhea. The introduction of the drug to the resolution of all side effects can be delayed for 1-2 weeks.
With the development during treatment pronounced inhibition of bone marrow hematopoiesis (neutrophil count less than 500 / ml, and / or white blood cell count less than 1000 / mm, and / or platelet count of less than 100,000 / microliter), febrile neutropenia (neutrophil count 1000 / ml of blood or less, combined with an increase in body temperature over 38 ° C), infectious complications, severe diarrhea, or other hematological toxicity grade 3-4, subsequent doses of iritis, and if necessary 5 -ftoruratsila should be reduced by 15-20%. Patients with impaired liver function. When the bilirubin level in blood serum higher than the upper normal limit of no more than 1.5 times, due to the increased risk of severe neutropenia should be carefully monitored blood parameters of the patient . When the bilirubin level more than 1.5 times – Iritenom treatment should be discontinued. Patients with impaired renal function. Is not recommended for treatment Iritenom as data on the use of irinotecan in this category there are no patients.Patients with advanced age. There are no special instructions Usage irinotecan absent in older people. Dose in each case should be selected with care. Instructions for preparation of a solution for infusion . The required amount of formulation diluted with 250 ml of 0.5% dextrose or 0.9% sodium chloride solution and stir the resulting solution by rotating the vial. Before the introduction of the solution should be visually inspected for clarity. In the case of sludge, the drug must be discarded. The solution should be used immediately after dilution. If dilution performed under aseptic conditions (for example, to install the laminar air flow), iritis solution can be used in the case of storage at room temperature, within 12 hours (including the time of infusion) and, in the case of storage at 2-8 ° C for 24 hours after opening the vial with the concentrate.Side effect On the part of hematopoiesis: neutropenia is observed on average 80% of patients, including half of them there is a decrease of neutrophils less than 1,000 cells in 1 mm. Recovery of neutrophils usually occurs 7-20 days after the start of treatment. Anemia varying severity occurs on average 60% ??of patients, and thrombocytopenia – 7% of patients. We describe a case of thrombocytopenia with the formation of anti-platelet antibodies. On the part of the digestive system: Late diarrhea occurring more than 24 hours (on average 5 days) after administration of the drug is a dose-limiting toxicities observed in approximately 87% of patients with severe – at 38%. Nausea and vomiting is usually occurs on the first day of administration or after 24 hours in 85% of patients. It reported the development of dewatering on the background of vomiting and diarrhea, rarely with the development of renal insufficiency, hypotension and cardiac insufficiency. There may be abdominal pain, anorexia, mucositis, constipation. Acute cholinergic syndrome observed in 9% of patients during the first 24 hours after administration of the drug and is manifested by diarrhea, abdominal pain, sweating, cramps, disorder of vision, lacrimation, salivation, decrease in blood pressure , dizziness, fever and general malaise. On the part of the central nervous system: involuntary muscle twitching or convulsions, paraesthesia, asthenia. Allergic reactions: seldom – skin rash, very rarely – anaphylactic shock. Other: dyspnea, alopecia, fever, local reaction.
main expected manifestations of overdose – neutropenia and diarrhea. A specific antidote is not known to irinotecan. Treatment is symptomatic. In the case of an overdose the patient should be hospitalized and carefully monitor the function of vital organs.
Interaction with other drugs
Since irinotecan has anticholinesterase activity may increase the duration of neuromuscular blockade when combined with suxamethonium and antagonism of neuromuscular blockade with regard to the combination of a non-depolarizing muscle relaxants. Iritis should not be mixed with other medications in the same bottle.
Iritenom Treatment should be carried out in specialized chemotherapy wards under the supervision of a physician who has experience with anticancer drugs.
Patients receiving iritis, it is necessary to make weekly detailed clinical analysis of blood and monitor liver function.
Diarrhea that arises as a consequence of the cytotoxic action of the side effects of trenbolone enanthate , usually It celebrated not earlier than 24 hours after administration of iritis (the majority of patients at a mean of 5 days). When the first episode of loose stools assignment must abundant drink containing electrolytes and the immediate holding antidiarrheal therapy comprising loperamide receiving high doses (4 mg and the first reception then 2 mg every 2 hours). This therapy is continued for at least 12 hours after the last episode of loose stools, no more than 48 hours because of the possibility of intestinal paresis. If diarrhea is regarded as severe (more than 6 episodes of loose stools within a day or severe tenesmus), and if it is accompanied by vomiting or fever, the patient should be urgently hospitalized in the intensive care unit for the comprehensive treatment, including the introduction of broad-spectrum antibiotics. In moderate or mild diarrhea (less than 6 episodes of loose stools during the day and moderate tenesmus), which is not stopped during the first 48 hours you need to start taking broad-spectrum antibiotics in.
With the simultaneous occurrence of diarrhea and neutropenia (white blood cell count less than 500 cells / mm ) in addition to the antidiarrheal therapy prophylactically inside appointed broad-spectrum antibiotics.
Loperamide should not be given prophylactically, including patients who have diarrhea was observed during previous administrations iritis.
The patient should be forewarned about the possibility of his delayed diarrhea. Patients should immediately inform your doctor of the occurrence of diarrhea and immediately begin the appropriate treatment.
With inadequate treatment of diarrhea condition may develop, threatening the patient’s life, especially if diarrhea developed against the backdrop of neutropenia.
Patients with febrile neutropenia (body temperature> 38 ° C and neutrophil count <1000 / mm) must be immediately initiated the introduction of broad-spectrum antibiotics in the hospital.
Acute cholinergic syndrome usually occurs during administration of the drug trenbolone enanthate uk or in the first 24 hours after administration to quickly and effectively stopped by subcutaneous administration of 0.25 mg of atropine (caution in patients bronchial asthma).
a dosage form as a drug adjuvant comprises sorbitol, and therefore can not be used iritis patients with hereditary fructose intolerance. During treatment Iritenom and, at least for three months after discontinuation of therapy should be applied reliable contraceptive measures.
If you get a solution iritis or infusion solution to the skin or mucous membranes of the skin, immediately wash with soap and water, mucous membranes just water.
Patients necessary to prevent the possibility of occurrence during treatment Iritenom dizziness and visual disorders that develop within 24 hours after dosing. If you have these symptoms, patients are advised to refrain from driving and other activities potentially hazardous activities that require high concentration and psychomotor speed reactions.
Concentrate for solution for infusion 100 mg / 5 mL and 40 mg / 2 ml vials of dark glass. 1 bottle with the attached instructions for use in a carton box. In 5 or 10 vials with instructions for use in a carton box with partitions or special jacks.
By 50. 85 or 100 vials with instructions for use, one for 10 bottles in a box made ??of cardboard (for hospitals).
List B. The temperature side effects of trenbolone enanthate is not above 25 ° C, protected from light and the reach of children.
Do not use after expiry date stated on the package.
Conditions of supply of pharmacies