IMATINIB 400MG


Glivec 400mg Description


Glivec 400mg tablet is an anti neoplastic medicine which is used in the treatment of;Advanced myelogenous leukemia (CML),Gastrointestinal stromal tumors (GISTs) and a number of malignancies Glivec 400mg is used as monotherapy, or it may combine with some other medicine in the conditions of certain types of cancer or bone marrow disorders. Glivec 400mg is a tyrosine kinase inhibitor that prohibits BCR-ABL kinase produced by chromosomal rearrangement in chronic myeloid leukemia and acute lymphoblastic leukemia


Glivec 400mg tablet prescribed for


Glivec 400mg tablets are mainly indicated for the treatment of;
Aggressive systemic mastocytosis
Chronic esinophillic leukemia
Dermatofibrosarcoma protuberans
Gastrointestinal stromal tumors
Hyperesinophillic syndrome
Myelodysplastic syndrome
Myeloproliferative disease
Philadelphia chromosome positive acute lymphoblastic leukemia
Philadelphia chromosome positive chronic myeloid leukemia





Glivec 400mg tablet


The usual dose of tablet Glivec 400mg is 400mg or 600mg as a single dose. Whereas 800mg which is administered as 400mg twice daily.Glivec 400mg tablets should be taken with food


Glivec 400mg tablet


The recommended dose for following conditions;
Acute lymphoblastic leukemia:
In adults, the prescribed dose is 600mg should be taken orally as a single dose.
Myelodysplastic/Myeloproliferative diseases:
The usual dose is 400mg PO qDay
Hyperesinophillic syndrome:
In this condition, recommended dose is 400mg PO qDay
Chronic myeloid leukemia:
Chronic phase: In newly diagnosed patients, the dose of Glivec 400mg tablet is 400mg should be orally taken as a single dose. If the failure of chronic phase of the treatment with interferon alpha therapy; dose is raised to 600mg per day. Quick phase: 600mg PO qDay; dose variation to 400mg PO as twice in a day if there is no serious adverse drug reaction or non leukemia associated neutropenia or thrombocytopenia.
Dermatofibrosarcoma protuberans:
Recommended dose is 400mg PO q12hr
Gastrointestinal stromal tumors
The prescribed dose of the tablet Glivec 400mg is 400mg should be taken orally as a twice daily

Pharmacokinetics


Absorption :
Glivec 400mg tablets after oral administration, it is absorbed within 2-4 hours. The bioavailability of Glivec 400mg tablets is about 98%.
Distribution:
Human plasma protein bound almost range of 95%. Glivec 400mg tablet is mostly bound to albumin and α1-acid glycoprotein.
Metabolism:
The enzyme which is responsible for metabolism of Glivec 400mg tablet is CYP3A4. Active metabolite of Glivec 400mg tablet is N-demethylated piperizine derivative
Excretion:
The elimination of Imatinib through feces 81% of the total drug excreted through feces and 13% of drug through urine with 7 days The half life time of Imatinib and active metabolite N-demethyl derivative are around 18 and 40 hours respectively


Mechanism of action


Glivec 400mg contains an active component known as Imatinib mesylate; it is an inhibitor of certain tyrosine kinase enzymes. Glivec 400mg prohibits BCR-ABL tyrosine Glivec 400mg obstruct the multiplication and promote the apoptosis in BCR-ABL positive cells in addition to fresh leukemia cells from Philadelphia chromosome positive CML Glivec 400mg also inhibits tumor growth of BCR-ABL transacted murine myeloid cells along other BCR-ABL positive leukemia CML in blast crisis Glivec 400mg inhibits receptor tyrosine kinase for platelet-derived growth factor (PDGF), stem cell factor (SCF) and PDGF and SCF mediated cellular events get prohibited. 1. Glivec 400mg a 2-phenylaminopyrimidine analog, it acts as a prohibitor of tyrosine kinase enzyme. 2. In malignancy conditions, Philadelphia chromosome leads to fusing of protein with BCR (breakpoint cluster region). Glivec 400mg used to reduced Bcr-Abl activity


Drug interaction


Glivec 400mg tablet is contraindicated to some medicines like; Cobimetinib, conivaptan, dihydroergotamine, eliglustat, aspirin, vitamin D, rosuvastatin, duloxetine, dasatinib, grapefruit, ibuprofen, Atorvastatin, pregabalin

In pediatric


Chronic myeloid leukemia:
<1 year: the safety and efficacy of the drug has not been established ≥1 year: 340mg/m2/day PO; should not be exceed 600mg/day
Acute lymphoblastic leukemia:
<1 year: the safety and efficacy of the drug has not been established ≥1 year: 340mg/m2/day PO; should not be exceed 600mg/day

Pregnancy and lactation


Pregnancy category: D Glivec 400mg should not recommended to pregnant and breast feeding mothers, it can able to cause fetal malformations and cause fetal harm The metabolites excreted in human milk

Storage condition


Glivec 400mg tablet container should be stored in cool and dry place It should be keep away from moisture, heat and light

Side Effects


Vascular disorders:
Flushing, hemorrhage, hypertension, peripheral coldness, Reynaud’s phenomenon, elevated LDH levels
Skin disorders:
Dry skin, alopecia, face edema, Erythema, photosensitivity reactions, nail disorder, purpura, psoriasis, rashes, vascular rash, Stevens Johnson syndrome, acute febrile neutrophillic dermatosis.
Eye, ear and labyrinth disorders:
Conjunctivitis, vision blurred, orbital edema, conjuctival hemorrhage, dry eye, vertigo, tinnitus, eye irritation, eye pain, scleral hemorrhage, retinal hemorrhage, papilla edema, glaucoma
Renal and urinary disorders:
Renal failure, frequency of urine will increased, Hematuria, renal pain
Cardiac disorders:
Palpitations, pericardial effusion, congestive cardiac failure, tachycardia, pulmonary edema, arrhythmia, atrial fibrillation, cardiac arrest, myocardial infarction, angina pectoris
General disorders:
Weakness, anasarca, chills, malaise
Blood and lymphatic system:
Pancytopenia, febrile neutropenia, Lymphopenia, esinophillia, thrombocythemia, bone marrow depression, lymphadenopathy, hemolytic anemia, Aplastic anemia
Hepatobiliary:
Hepatitis, jaundice, hepatic failure, hepatic necrosis
Immune system:
Angioedema
Infection and infestation:
Herpes simplex, herpes zoster, cellulitis, urinary tract infection (UTI), gastroenteritis, sepsis
Metabolism and nutrition:
Weight decreased, loss of appetite, dehydration, gout, hyperuricemia, hypocalcaemia, hyperglycemia, hyponatremia, hyperkelamia, hypomagnesemia
Gastrointestinal disorders:
Abdominal distension, gastro esophageal reflux, dry mouth, gastritis, gastric ulcer, stomatitis, mouth ulcer, eructation, esophagitis, dysphasia, and pancreatitis
Musculoskeletal:
Joint swelling, muscle stiffness, muscular weakness, arthritis
Nerve system:
Paresthesia, hypesthesia, syncope, peripheral neuropathy, somnolence, tremor
Reproductive system:
Breast enlargement, menorrhagia, sexual dysfunction, gynecomastia, erectile dysfunction, menstruation irregular, nipple pain, scrotal edema
Respiratory:
Epistaxis, pleural effusion, interstitial pneumonitis, pulmonary fibrosis, pulmonary hypertension, pulmonary hemorrhage



Precaution


Caution with use in hepatic impairment patients. Avoid combination with strong CYP3A4 inducers. Risk of severe CHF or ventricular dysfunction. Hemorrhage occurs. Growth retardation occurs in children.


Missed Dose


If patient fail to take Glivec 400mg tablet, patient should administered within a time. Otherwise, tablet should be discontinued and follow the next drug schedule.


Contraindication


Hypersensitive reaction to Imatinib mesylate and other excipients present in Glivec 400mg tablets


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