To date, in the treatment of cancer, the most effective drugs that destroy cancer are the inhibitors of protein kinases( enzymes that cause tumor growth).To this group of drugs belongs Iressa, intended for the treatment of lung cancer.
Form release, formulation and packaging
The tablets are round, convex on both sides of the form. Covered with a film coating of a brown hue, on a break - white. On one side of each tablet there is an engraving "IRESSA" and "250", the second side without marking.
1 tablet contains:
- Gefitinib( 250 mg).
- Lactose monohydrate( disaccharide, to which a water molecule is attached).It is necessary for effective compression of tablets( 163.5 mg).
- Microcrystalline cellulose( modification of cotton cellulose), which is used as emulsifier and stabilizer( 50 mg).
- Sodium croscarmellose( sodium cellulose), which helps the tablet to dissolve completely after its use. Reduces the loss of the amount of active substance before it enters the circulatory system( 20 mg).
- Povidone, low molecular weight polyvinylpyrrolidone, which is used as a binder for other components of the substance. Improves the dissolution and bioavailability of the drug( 10 mg).
- Sodium lauryl sulfate( sodium salt of lauryl sulfonic acid).It is an emulsifier( surfactant), which stabilizes a mixture of the components of the preparation( 1.5 mg).
- Magnesium stearate is a stabilizing agent that is used to improve the viscosity and maintain the consistency of the preparation( 5 mg).
The sheath consists of:
- Hypromellose is an odorless and tasteless partially methylated and hydroxypropylated cellulose, the solution of which is used to produce solid film coatings( 7.65 mg).
- Macrogol 300( ethylene glycol polymer), which regulates the dissolution rate of the tablet shell in gastric juice( 1.5 mg).
- Iron oxide red and yellow E172 - chemical compounds of iron and oxygen, which are used to color the shell( 0.9 mg).
- Titanium dioxide E171 - food color( 0.5 mg).
Three blisters are packed in a cardboard box. Each blister pack contains 10 tablets.
Manufacturer
British-registered Anglo-Swedish pharmaceutical company AstraZeneca.
Indications for use
- Locally spread( not affecting other organs and lymph nodes) lung cancer;
- metastatic non-small cell lung cancer( squamous cell carcinoma, adenocarcinoma, large cell carcinoma), immune to chemotherapy, which is performed using platinum derivatives.
Contraindications
- Presence of an individual intolerance to any component.
- Breastfeeding, pregnancy.
Not used for therapy in children and adolescents.
The drug with caution( the application requires a doctor's supervision and, possibly, dose adjustment) is prescribed for:
- pneumonia, post-radiation, drug, interstitial;
- idiopathic pulmonary fibrosis;
- pneumoconiosis.
Mechanism of action
Gefitinib selectively suppresses the tumor growth promoting enzyme receptor tyrosine kinase epidermal growth factor.
Under the influence of gefitinib inhibited:
- tumor growth;
- appearance of metastases;
- neoplasm of the network of blood vessels in the tumor( angiogenesis).
In addition, gefitinib:
- accelerates the death of tumor cells( apoptosis);
- increases the activity of antitumor chemotherapeutic drugs and the effectiveness of other therapies.
Absorption of the drug is not very fast, therefore in the blood plasma the constant concentration of the drug is established after the use of 7-10 doses. The maximum concentration occurs 3-7 hours after the use of the drug.
On average, the absolute bioavailability of the drug( the amount of active substance that has reached its place of action) is 59%.Food intake for the bioavailability of gefitinib is not affected, but if the pH of the gastric juice exceeds 5, bioavailability is reduced.
Gefitinib is distributed in tissues extensively( not into the depths, but in the breadth).
Studies outside the living body demonstrated that gefitinib slightly suppresses the enzyme CYP2D6( a hepatic enzyme responsible for the metabolism of about ¼ of all drugs).
The total rate of plasma clearance( plasma clearance) with gefitinib is about 500 ml / min, and the half-life is an average of 41 hours. The drug is excreted mainly with feces( the kidney accounts for less than 4% of the dose).
Gefitinib is significantly metabolized in the body - 5 metabolites( intermediate products of metabolism) and 8 - in the blood plasma were detected in the secretions.
In patients with hepatitis or cirrhosis, the effects of the drug have not been studied.
Instructions for the use of Iressa: dosage
The drug( 250 mg) should be taken 1 time per day.
Application features:
- Other liquids for solution preparation are not used.
- Do not take a double dose( the interval should be more than 12 hours).
- Reception of Iressa solution can also be administered through a nasogastric tube.
- Indication for changing the dose is poorly-resistant diarrhea.
- The treatment can be interrupted for 2 weeks, after which Iressa's treatment is continued.
Side effects of
With what frequency were observed side effects: very often( & gt; 10%);often( & gt; 1 - & lt; 10%);infrequently( & gt; 0.1 - & lt; 1%);rarely( & gt; 0.01 - & lt; 0.1%);very rarely( & lt; 0.01%).
Disorders from:
- of the digestive system: very often observe nausea, diarrhea, vomiting, stomatitis;often - anorexia, dehydration, dryness in the oral cavity;rarely - perforation of the gastrointestinal tract, pancreatitis.
- of the vascular system: often - the presence of blood in the urine, nosebleeds;infrequently - delayed blood coagulability, increased frequency of bleeding when taking warfarin.
- of the eye: often - blepharitis, conjunctivitis, dry eyes;infrequently - characterized by a reversible form of corneal erosion, which can be combined with abnormal eyelash growth, keratitis.
- Respiratory: infrequently observed interstitial pneumonia, a possible fatal outcome.
- skin and skin: very often there are manifestations of pustular rash, dry skin, itching;often observe alopecia, change of nails;infrequently observe hives and angioedema;very rarely observed manifestations of multiforme exudative erythema and epidermal toxic necrolysis.
- of the urinary system: often reveal an asymptomatic laboratory increase in the level of creatinine, cystitis, proteinuria;rarely - hemorrhagic cystitis.
- of the hepatobiliary system: very often asymptomatic, usually minimal increase in the level of activity of "liver" transaminases or the level of total bilirubin, rarely hepatitis
Other disorders - very often there is asthenia( usually expressed in insignificant degree), often pyrexia.
Usually, the side effects are reversible( manifested most often during the first month).
In 8% of patients, adverse reactions were present, expressed to a large extent.
In 1% of cases, therapy due to adverse reactions had to be discontinued.
Overdose
No specific therapy, treatment is only possible symptomatic.
Specific instructions
Because interstitial lung involvement has been identified among the side effects of the drug, with increased dyspnoea, cough, fever, the drug should be discontinued before the examination. With the confirmation of IPL, the application of Iressa is canceled and appropriate treatment is performed.
The factors that contribute to the development of IPL include smoking, elderly age, the presence of cardiovascular diseases, the presence in the history of interstitial pneumonia, a severe general condition, the duration of the disease is less than 6 months.
As with the reception of Iressa, the enhanced activity of "liver" transaminases is possible, it is desirable to periodically check the hepatic function.
Any unwanted reactions are a reason to contact your doctor in the near future.
Drug Interaction
The application of Iresses simultaneously with preparations that activate the production of the isoenzyme CYP3A4( St. John's wort in the form of tinctures, barbiturates, carbamazepine, etc.), significantly reduces the effectiveness of gefitinib.
Suppressing isoenzyme CYP3A4 preparations( itraconazole) enhance the effect of Iressa.
With the use of vinorelbine concurrently with Iresse, the possibility of developing neutropenia increases.
The effectiveness of Iressa decreases with the use of drugs that increase the pH of the stomach.
Combination of anticoagulants and gefitinib requires control of blood coagulability( increased risk of bleeding).
Reviews
After a month of use, analgesics were not needed, cough decreased, life quality improved significantly after 3 months, there were no serious side effects, but there was an intestinal disorder and a skin rash( they can be controlled).
With the reception of Iressa, the tumor decreased 2-fold, the drug is tolerated easily.
Analogues of Iress medication
Tarceva, Giotrf, Tarlenib, Erlotinib.
Price In Moscow
From 61200 to 84812 руб.
Synonyms for
Gefitinib.
Conditions for dispensing from pharmacies
Prescription.
Storage Conditions and Shelf Life
Conditions: factory packing, the temperature in the storage place does not exceed 30 ° C.
It is usable for 4 years from the date of manufacture.