Universal reference book for medicines
Name of the drug: IMAGLIV (IMAGLIV)

Active substance: imatinib

Type: Antitumor drug.
Protein tyrosine kinase inhibitor
Manufacturer: SANDOZ (Slovenia) manufactured by NOVARTIS PHARMA STEIN (Switzerland)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
Protein tyrosine kinase inhibitor.
Inhibits the enzyme Bcr-Abl-tyrosine kinase at the cellular level, in vitro and in vivo. Selectively suppresses proliferation and induces apoptosis of Bcr-Abl positive cell lines, as well as of young leukemic cells in chronic myeloid leukemia with a positive Philadelphia chromosome and in acute lymphoblastic leukemia.
In studies on the transformation of colonies performed on samples of peripheral blood and bone marrow, it was shown that imatinib selectively inhibits Bcr-Abl-positive colonies obtained from patients with chronic myelogenous leukemia.

In studies conducted in vivo in animal models using Bcr-Abl-positive tumor cells, it has been shown that the drug has antitumor activity in monotherapy.

In addition, imatinib is an inhibitor of tyrosine kinase receptors for platelet growth factor and stem cell factor, and also suppresses cellular reactions mediated by the above factors.

In vitro imatinib inhibits proliferation and induces apoptosis of cells of gastrointestinal stromal tumors expressing kit mutations.

PHARMACOKINETICS
After oral administration, bioavailability is an average of 98%.
The variation coefficient for AUC is 40-60%. When taken with a high-fat diet, compared to fasting, there is a slight decrease in the degree of absorption (a decrease in C max by 11%, AUC by 7.4%) and a slowing of the absorption rate (T max extension by 1.5 h).
At clinically significant concentrations of imatinib, its binding to plasma proteins is about 95% (mainly with albumin and acid alpha-glycoprotein, to a small extent - with lipoprotein).

The main metabolite of imatinib circulating in the bloodstream is the N-demethylated piperazine derivative, which in vitro has pharmacological activity similar to that of the unchanged active substance.
The AUC value for the metabolite is 16% of the Imatinib AUC.
After ingestion of 14 C-labeled imatinib for 7 days, 68% of the administered dose was excreted with feces and with a 13% dose of urine.
In an unchanged form, about 25% of the dose is excreted (20% with feces and 5% with urine). The rest of the imatinib is excreted as metabolites.
T 1/2 imatinib in healthy volunteers was about 18 h.

If the liver function is impaired, an increase in the concentration of imatinib in the blood plasma is possible.

INDICATIONS
Chronic myelogenous leukemia in the phase of acceleration, blast crisis, and also in the chronic phase;
treatment of inoperable and / or metastatic malignant gastrointestinal stromal tumors (in adult patients).
DOSING MODE
Individual, depending on the indications and treatment regimen.

SIDE EFFECT
From the hemopoietic system: often - neutropenia, thrombocytopenia, anemia, febrile neutropenia;
possible pancytopenia, oppression of bone marrow hematopoiesis.
On the part of the digestive system: often - anorexia, nausea, vomiting, diarrhea, dyspepsia, abdominal pain, bloating, flatulence, constipation, reflux esophagitis, ulceration of the oral cavity, increased activity of liver enzymes;
possible hyperbilirubinemia, jaundice, hepatitis; rarely - gastrointestinal bleeding, melena, ascites, gastric ulcer, gastritis, gastroesophageal reflux, dry mouth, hepatic insufficiency, colitis, intestinal obstruction, pancreatitis, increased appetite.
There are some reports of the development of cytolytic or cholestatic hepatitis and liver failure, in some cases, resulting in death;
gastroenteritis.
On the part of metabolism: rarely - dehydration, hyperuricemia, hypokalemia, hyperkalemia, hyponatremia, increased uric acid concentration in the blood, gout), hypophosphatemia, hyperkalemia, hyponatremia.

From the side of the central nervous system and peripheral nervous system: often - headache, dizziness, taste disorder, paresthesia, insomnia;
possible hemorrhagic stroke, syncope, peripheral neuropathy, hypoesthesia, drowsiness, migraine, depression, memory impairment, anxiety, decreased libido; rarely - confusion, cerebral edema, increased intracranial pressure, convulsions.
From the side of the organ of vision: often - conjunctivitis, increased teardrop, blurred vision;
possible irritation of the eyes, hemorrhage in the conjunctiva, dryness of the conjunctiva, puffiness of the eyelids; rarely - macular edema, papillary edema, retinal hemorrhages, hemorrhages in the vitreous, glaucoma.
Auditory and vestibular disorders: dizziness, tinnitus are possible.

From the cardiovascular system: possible heart failure, pulmonary edema, tachycardia, hematomas, arterial hypertension, arterial hypotension, flushes to the face, cold extremities;
rarely - hydropericarditis, pericarditis, thrombosis / embolism.
From the respiratory system: often - dyspnea;
possible pleural effusion, pain in the pharynx or larynx, cough; rarely pulmonary fibrosis, interstitial pneumonia.
Dermatological reactions: often - periorbital edema, dermatitis, eczema, rash, swelling of the face, puffiness of the eyelids, itching, erythema, dry skin, alopecia, night sweats;
possible petechiae, increased sweating, urticaria, nail damage, photosensitivity reactions, purpura, hypotrichosis, cheilitis, hyperpigmentation of the skin, hypopigmentation of the skin, psoriasis, exfoliative dermatitis, bullous rash; rarely - angioedema, vesicular rash, Stevens-Johnson syndrome.
From the musculoskeletal system: often - muscle spasms and cramps, musculoskeletal pain and arthralgia, swelling of the joints;
possible ischialgia, stiffness of muscles and joints.
From the side of the urinary system: kidney failure, kidney pain, frequent urination, hematuria are possible.

On the part of the reproductive system: gynecomastia, breast enlargement, swelling of the scrotum, pain in the nipples, a decrease in potency are possible.

On the part of the body as a whole: often - fluid retention, swelling;
often - fever, weakness, chills; sometimes - severe malaise, hemorrhages; rarely - anasarca, hemorrhages in the tumor, tumor necrosis.
Other: often - weight gain, nosebleeds;
sometimes - increased AF, creatinine, CK, LDH, weight loss.
Possible sepsis, herpes simple, herpes zoster, upper respiratory tract infections.

CONTRAINDICATIONS
Hypersensitivity to imatinib.

APPLICATION FOR FUNCTIONS OF THE LIVER
Recommendations for the use of imatinib in patients with impaired renal function are currently not available.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution in patients with impaired hepatic function, since it is possible to increase the effect of imatinib.

SPECIAL INSTRUCTIONS
Use with caution in patients with impaired hepatic function, since it is possible to increase the effect of imatinib.

Recommendations for the use of imatinib in patients with impaired renal function are currently not available.

During the treatment period, the patient's body weight should be monitored in order to detect fluid retention in the body in a timely manner;
systematically carry out a complete clinical analysis of peripheral blood; regularly monitor liver function.
In case of neutropenia and thrombocytopenia, as well as in case of increased activity of hepatic transaminases, alkaline phosphatase and bilirubin content, it is recommended to temporarily cancel imatinib or reduce the dose.

Impact on the ability to drive vehicles and manage mechanisms

Given that imatinib can cause dizziness and blurred vision, caution should be exercised when driving a car or working with machinery.

DRUG INTERACTION
When used simultaneously with drugs that inhibit the isoenzyme CYP3A4 (including ketoconazole), an increase in the concentration of imatinib in the blood plasma is possible.

In contrast, the simultaneous use of drugs that are inducers of the CYP3A4 isoenzyme (eg, dexamethasone) can lead to an increase in the metabolism of imatinib and a decrease in its plasma concentration.

With simultaneous application with simvastatin, there is an increase in C max and AUC of simvastatin by 2 and 3.5 times, respectively, which is a consequence of inhibition of the isoenzyme CYP3A4 under the influence of imatinib.

It is advisable to use imatinib concomitantly with preparations that are substrates of CYP3A4 and have a narrow range of therapeutic concentration, as well as with preparations containing paracetamol.

In vitro studies, it has been shown that imatinib inhibits the CYP2D6 isoenzyme at the same concentrations in which it inhibits CYP3A4.
In this connection, the possibility of enhancing the effects of preparations that are substrates of the isoenzyme CYP2D6 should be taken into account when combined with imatinib.
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