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1 tablet of drug includes 250 mg of a gefitinib.
Additional substances: macrogoal 300, monohydrate of lactose, sodium lauryl sulfate, iron oxide, magnesium stearate, microcrystallic cellulose, gipromelloza, croscarmellose sodium, povidone, titanium dioxide.
Biconvex brown tablets of a round form with texts "250" and "IRESSA" on one surface, on a section is visible a white kernel. 10 tablets in the blister, 3 blisters in packaging from aluminum foil, 1 packaging in a paper pack.
The antineoplastic, suppressing a proteintirozinkinaza action.
Pharmacodynamics and pharmacokinetics
Iress's drug being a selective blocker of a tyrosinekinase of receptors of an epidermal growth factor (EGFR), slows down growth of a tumor, its angiogenesis and innidiation, and also accelerates death of cancer cells.
Slows down development of various lines of cancer cells and stimulates antineoplastic action of chemotherapeutic drugs, hormonal and radiation therapy.
Drug it is proved increases term before progressing of a tumor at persons with metastatic or locally-spread types of not small-celled cancer of lung.
After oral administration it is soaked up slowly. Extreme concentration in blood is reached 4-6 hours later. Bioavailability makes about 58%. Reception of food does not change bioavailability indicators. At rn a gastric juice more 5th bioavailability of drug decreases by 47%.
Reaction with blood proteins reaches 90%. Gefitinib it is metabolized by CYP3A4 isoenzyme by transformation of N-propilmorfolinovoy of group, demethylation and oxidizing dephosphorylation. The main metabolite – O-desmetilgefitinib, its activity in a growth ratio of cells is 14 times weaker than activity of the gefitinib.
Time of semi-removal is on average equal to 41 hour. It is evacuated from an organism mainly with a stake, the insignificant part (about 4%) is removed by kidneys.
Indications to use
Metastatic or locally-spread type of not small-celled cancer of lung with presence of mutations of a tyrosinekinase at structure of a receptor responsible for reaction with an epidermal growth factor in primary line of therapy.
Metastatic or locally-spread type of not small-celled cancer of lung, unreceptive to chemotherapy platinum drugs.
- pregnancy and lactation;
- age less than 18 years;
- allergy to drug components.
Iress's drug with care is used at intersticial pneumonia, a cryptogenic pneumosclerosis, post-beam pneumonia, a pneumoconiosis, medicinal pneumonia, even slight increase of content of bilirubin and transaminases of a liver.
Most often treatment by Iressa is followed by skin rash, diarrhea, an itch and a xeroderma which are observed approximately in 20% of cases. Usually side reactions are shown in the 1st month of use of medicine and are in most cases reversible. At 10% of patients heavy reactions were registered, but only at 3-4% of patients treatment was stopped because of side reactions.
- Reactions from coagulation: hypocoagulation, a hamaturia, increase in quantity of bleedings against treatment by Warfarin, nasal bleeding.
- Reactions from digestion: moderate nausea, diarrhea, anorexia, stomatitis, increase of maintenance of ALT and ACT, dryness in a mouth, vomiting, dehydration, hepatitis, increase of content of bilirubin, a liver failure, pancreatitis, the lethal outcome is possible.
- Reactions from sight: conjunctivitis, cornea erosion, xerophthalmia, loss of eyelashes, blepharitis.
- Reactions from breath: intersticial pneumonia.
- From secretory system: increase of content of creatinine in plasma, a proteinuria.
- Allergic reactions: Quincke's edema, small tortoiseshell.
- Dermatological reactions: xeroderma, itch, pustular rash, alopecia, changes of nails, epidermal toxic necrolysis, violent damage of skin, Stephens-Johnson's syndrome, vasculitis.
- Other reactions: weak adynamy, hyperthermia.
Iressa, application instruction (Way and dosage)
Iress's tablets are appointed to accept orally on 1 piece of times a day.
In case of the admission the patient of reception of the next tablet, it is necessary to accept it immediately if before reception of the subsequent tablet there were more than 12 hours. It is forbidden to take 2 pill for time for compensation of accidentally passed dose.
The tablet before reception is allowed to be dissolved in 100 ml of boiled (not gassy) water. Other liquids for dissolution are forbidden to be used. The tablet needs to be lowered in water and to stir before full dissolution (about 15 minutes), then to immediately drink the formed suspension. The following step it is necessary to pour still a half-glass of water, to wash it vascular walls and to drink the remained suspension. Dissolved by the described way of a tablet it is authorized to enter also by means of a nazogastralny probe.
Iressa at a cancer therapy of lungs in special cases
At persons there is a lot of or a lack of weight, at advanced age, depending on national or a sex, at the liver failure caused by metastatic defeat) dose adjustment is not made.
At persons with the diarrhea which is badly giving in to treatment or at by-effects from skin the field of the expiration of the specified term in a former dosage is authorized to take a break in reception till 14 days with resuming of drug intake.
Overdose signs: increase of weight and frequency of side reactions, generally diarrheas and rashes on skin.
Overdose treatment: symptomatic. The specific antidote is not known.
Joint reception purpose of a gefitinib and Rifampicin causes reduction of concentration of the first by 83%.
Gefitinib (Iressa) and Itrakonazol at joint reception cause increase of contents of the first for 80% that can cause increase in frequency and expressiveness of the undesirable phenomena.
At simultaneous use with Vinorelbin stimulation of neytropenichesky action of the last is not excluded.
The drugs activating CYP3A4 isoenzyme stimulate a metabolism and reduce the maintenance of a gefitinib in blood. Co-administration of the described means with CYP3A4 isoenzyme activators (Carbamazepine, Phenytoinum, St. John's Wort tincture, barbiturates) can weaken its action.
Terms of sale
Only according to recipe.
To store in an original packing at a temperature up to 30 °C. To protect from children
Period of validity
Before purpose of drug in primary line of treatment of the specified types of not small-celled cancer of lung it is necessary to define existence of a mutation of EGFR at all patients as Iressa cannot be used in primary line of therapy at persons without existence of a mutation of EGFR (instead of chemotherapy).
In some cases against Iressa's reception intersticial damage of lungs developed, it is rare with a lethal outcome. When strengthening such symptoms as cough, short wind, fever administration of drug needs to be stopped and to immediately inspect the patient. If existence of an intersticial pulmonary disease is confirmed, drug intake is stopped and appoint to the patient necessary treatment. Factors, increasing probability of emergence of an intersticial pulmonary disease: smoking, normal tissue of lungs <50% according to KT, intersticial pneumonia in the past, duration of an illness is less than half a year, a serious condition, advanced age, cardiological diseases.
Against use of the described means increase of content of transaminases of a liver and bilirubin which proceeded asymptomatically was noted, and also hepatitis infrequently came to light. There were data on isolated cases of insufficiency of work of a liver, up to a lethal outcome. Because of a possibility of emergence of above-mentioned frustration it is recommended to estimate function of a liver regularly. At the expressed increase in concentration of transaminases and bilirubin use of drug needs to be stopped.
At the persons which are at the same time accepting Warfarin it is recommended to exercise control of a prothrombin time regularly.
At identification of any reactions from sight or at development of the expressed diarrhea, vomitings, nausea or anorexias of the patient has to see the attending physician urgently.
Patients with a lack of lactase, a lactose intolerance or a sprue should take drug with caution because of presence at composition of lactose.
As during treatment by Iressa development of vomiting, nausea, an adynamy is not excluded, it is necessary to be careful at management of motor transport.
Drug is not used at persons 18 years are younger.
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