1 tablet of the drug includes 250 mg gefitinib.
Additional substances: macrogol 300, lactose monohydrate, sodium lauryl sulfate, iron oxide, magnesium stearate, microcrystalline cellulose, hypromellose, croscarmellose sodium, povidone, titanium dioxide.
Biconvex brown round tablets with the inscription "250"And"IRESSA»On one surface, on a section the white core is visible. 10 tablets in a blister, 3 blisters in a package of aluminum foil, 1 package in a paper bundle.
Antitumor, inhibitory protein tyrosine kinase effect.
Pharmacodynamics and pharmacokinetics
Iressa's drug being epidermal growth factor receptor selective tyrosine kinase blocker (EGFR)slows the growth of the tumor, her angiogenesisand metastasis, and also accelerates the death of cancer cells.
It inhibits the development of a variety of cancer cell lines and stimulates the antitumor effect of chemotherapeutic drugs, hormonal and radiation therapy.
The drug has been proven to increase the period until tumor progression in individuals with metastatic or locally common types of non-small cell lung cancer.
After oral administration, it is absorbed slowly. The maximum concentration in the blood is reached after 4-6 hours. Bioavailability is approximately 58%. Eating does not change bioavailability. When the pH of gastric juice is more than 5, the bioavailability of the drug is reduced by 47%.
The reaction with blood proteins reaches 90%. Gefitinibmetabolized isoenzyme CYP3A4 by transformation of the N-propylmorpholine group, demethylation and oxidative dephosphorylation. The main metabolite is O-desmethylgefitinib, its activity in relation to cell growth is 14 times weaker than the activity of gefitinib.
The elimination half-life is on average 41 hours. It is evacuated from the body mainly with feces, a small part (about 4%) is excreted by the kidneys.
Indications for use
Metastatic or locally advanced type of non-small cell lung cancer with the presence of mutations tyrosine kinases in the structure of the receptor responsible for responding with epidermal growth factor in the primary line of therapy.
Metastatic or locally advanced type of non-small cell lung cancerchemotherapy resistant platinum preparations.
- pregnancy and lactation;
- age less than 18 years;
- allergy on the components of the drug.
The drug Iressa is used with caution with interstitial pneumonia, cryptogenic pulmonary fibrosis, postradiation pneumonia, pneumoconiosis, drug pneumonia, even a slight increase in content bilirubin and transaminase the liver.
The most common treatment for Iressa is a skin rash, diarrhea, itching and dry skin, which are observed in about 20% of cases. Adverse reactions usually occur in the 1st month of the drug and in most cases are reversible. Severe reactions were recorded in 10% of patients, but only 3-4% of patients stopped treatment due to adverse reactions.
- Reactions from coagulation: hypocoagulation, hematuriaan increase in bleeding during treatment Warfarin, nose bleed.
- Reactions from digestion: moderate nausea diarea, anorexia, stomatitisincreasing content ALT and ACTdry mouth, vomiting, dehydration, hepatitis, increase in content bilirubin, liver failure, pancreatitisfatal outcome is possible.
- Reactions from of view: conjunctivitiscorneal erosion xerophthalmiaeyelash loss blepharitis.
- Reactions from breathing: interstitial pneumonia.
- By excretory system: increase in content creatininein plasma proteinuria.
- Allergic reactions: Quincke's edema, hives.
- Dermatological reactions: dry skin, itching, pustular rash, alopecianail changes epidermal toxic necrolysis, bullous lesion skin Stevens-Johnson syndrome, vasculitis.
- Other reactions: weak asthenia, hyperthermia.
Iressa, instructions for use (Method and dosage)
Iressa tablets are prescribed to be taken orally, 1 piece once a day.
If patients miss the next pill, it should be taken immediately if more than 12 hours are left before taking the next pill. It is forbidden to take 2 tablets at a time to compensate for an accidentally missed dose.
The tablet before administration is allowed to be dissolved in 100 ml of boiled (still) water. It is forbidden to use other liquids for dissolution. The tablet must be immersed in water and stirred until completely dissolved (about 15 minutes), then immediately drink the resulting suspension. The next step is to pour another half a glass of water, wash the walls of the vessel with it and drink the remaining suspension. The tablets dissolved in the described manner can also be administered by means of a nasogastric tube.
Iressa in the treatment of lung cancer in special cases
In persons with excess or underweight, in old age, depending on national or gender, with liver failure caused by metastatic lesion) dose adjustment is not performed.
In persons with diarrhea that is difficult to treat, or with side effects from the skin, it is allowed to take an interval of up to 14 days with the resumption of medication, the expiry of the indicated period at the previous dosage.
Signs of an overdose: increased severity and frequency of adverse reactions, mainly diarrhea and skin rashes.
Overdose treatment: symptomatic. The specific antidote is not known.
Joint appointment appointment gefitiniband Rifampicin causes a decrease in the concentration of the first by 83%.
Gefitinib(Iressa) and Itraconazolewhen taken together, they cause an increase in the content of the former by 80%, which can cause an increase in the frequency and severity of adverse events.
With simultaneous use with Vinorelbinestimulation of the neutropenic effect of the latter is not excluded.
Preparations that activate the CYP3A4 isoenzyme stimulate metabolism and reduce the content of gefitinibin blood. The simultaneous appointment of the described means with CYP3A4 isoenzyme activators (Carbamazepine, Phenytoin, hypericum tincture, barbiturates) may weaken its effect.
Terms of sale
Store in original packaging at temperatures up to 30 ° C. Keep out of the reach of children.
Before prescribing the drug in the primary line of treatment for these species non-small cell lung cancer it is necessary to determine the presence of a mutation Egfr in all patients, since Iressa cannot be used in the primary line of therapy in individuals without a mutation Egfr(instead of chemotherapy).
In some cases, against the background of taking Iressa, it developed interstitial lung lesionrarely fatal. When symptoms such as cough, shortness of breath, fever taking the drug must be stopped and the patient should be examined immediately. If availability interstitial lung disease it is confirmed that the medication is stopped and the necessary treatment is prescribed to the patient. Factors that increase the likelihood of interstitial lung disease: smoking, normal lung tissue <50% according to CT, interstitial pneumoniain the past, the duration of the disease is less than six months, serious condition, old age, cardiac diseases.
Against the background of the use of the described means, an increase in the content was noted transaminase liver and bilirubinwhich was asymptomatic, and was also rarely detected hepatitis. There was evidence of isolated cases of liver failure, including death. Due to the possibility of the aforementioned disorders, it is recommended to regularly evaluate liver function. With a pronounced increase in concentration transaminaseand bilirubin the use of the drug must be stopped.
In persons taking at the same time Warfarinit is recommended to regularly monitor prothrombin time.
In identifying any reactions from the side of vision or with the development of severe diarrheavomiting, or nausea or anorexia the patient should immediately consult a doctor.
Disabled Patients lactasesintolerance lactose or malabsorption syndromethe drug should be taken with caution due to the presence in the composition lactose.
Since during the treatment of Iressa the development of vomiting, nausea is not excluded, asthenia, you need to be careful when driving.
The drug is not used in people under 18 years of age.
During pregnancy and lactation
The use of the described agent is contraindicated in pregnancy and lactation.
Persons of childbearing age while taking the drug and for at least 3 months after therapy should use reliable methods of contraception.
Reviews about the drug Iressa
Due to the high price of the drug and its narrow therapeutic effect, reviews about it are quite rare. However, the few posts that can still be found on the forums indicate a good therapeutic effect of the drug.
Side effects occur very often, sometimes they require the abolition of treatment. As a result, a gray market appears for trading unused, expensive pills, and you can often find messages on the Internet "selling to Iress" or "buy Iressa".
Price, where to buy
The price of the medicine of Iress No. 30 in Russia is 75,000-102,000 rubles.
In Ukraine, the price of a standard package can reach 30,000 hryvnias.