IMATINIB 100MG

Glivec is a small molecule kinase inhibitor. Glivec film -coated tablets contain Imatinib mesylate. STI-571 is another name for Glivec andis a targeted therapy. Glivec is classified as a signal transduction inhibitor - protein-tyrosine kinase inhibitor

Imatinib

100mg

28 tablets




Glivec 100mg indicated for

Glivec 100mg tablet is belongs to anti-neoplastic medicine which is indicated in the treatment of Advanced myelogenous leukemia (CML) and Gastrointestinal stromal tumors (GISTs) and several malignancies.

Glivec 100mg is indicated as single treatment, or it may have consolidated with some other drug in the conditions of some types of cancer or bone marrow disorders.

Glivec 100mg is a type of tyrosine kinase inhibitor which inhibits BCR-ABL kinase produced by chromosomal rearrangement in chronic myeloid leukemia and acute lymphoblastic leukemia

Glivec 100mg tablet prescribed for

Glivec 100mg 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


How Glivec 100mg tablets work

Glivec 100mg is an inhibitor of certain tyrosine kinase enzymes. Glivec 100mg inhibits BCR-ABL tyrosine. Glivec 100mg obstruct the multiplication and promote the apoptosis in BCR-ABL positive cells in addition to fresh leukemia cells from Philadelphia chromosome positive CML Glivec 100mg also inhibits tumor growth of BCR-ABL transacted murine myeloid cells along other BCR-ABL positive leukemia CML in blast crisis

Glivec 100mg inhibits receptor tyrosine kinase for platelet-derived growth factor (PDGF), stem cell factor (SCF) and PDGF and SCF mediated cellular events get prohibited. Glivec 100mg a 2-phenylaminopyrimidine analog, it acts as a prohibitor of tyrosine kinase enzyme.In malignancy conditions, Philadelphia chromosome leads to fusing of protein with BCR (breakpoint cluster region). Glivec 100mg used to reduced Bcr-Abl activity



ADME PROPERTIES

It is absorbed within 2-4 hours and bioavailability of Glivec 100mg tablets is about 98%.

Glivec 100mg tablet has Human plasma protein bound almost range of 95%.

Glivec 100mg tablet Active metabolite is N-demethylated piperizine derivative.The enzyme which is responsible for metabolism of Glivec 100mg tablet is CYP3A4.

The elimination of Glivec through feces The total drug excreted through feces 81% and drug through urine 13% with 7 days The half life time of Glivec and active metabolite N-demethyl derivative are around 18 and 40 hours respectively




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imatinib-100mg

Ingredients Imatinib
Strength 100mg
Pack 28 tablets
Rating

Dosage and administration

given by dividing the dose into two as 400mg twice daily. Glivec 100mg tablets should be taken with food The usual dose for following conditions;

Hyperesinophillic syndrome

In this condition, recommended dose is 400mg PO qDay

Acute lymphoblastic leukemia

In adults, the prescribed dose is 600mg should be taken orally as a single dose.

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.

Myelodysplastic / Myeloproliferative diseases

The usual dose is 400mg PO qDay

Dermatofibrosarcoma protuberans

Recommended dose is 400mg PO q12hr

Gastrointestinal stromal tumors

The prescribed dose of the tablet Glivec 100mg is 400mg should be taken orally as a twice daily.

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

Glivec 100mg tablet causes some side effects

Blood and lymphatic system

Pancytopenia, febrile neutropenia, Lymphopenia, eosinophilia, thrombocythemia, bone marrow depression, lymphadenopathy, hemolytic anemia, Aplastic anemia

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 neutrophilic dermatosis.

Eye, ear and labyrinth disorders

Conjunctivitis, vision blurred, orbital edema, conjunctival 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 have increased, Hematuria, renal pain

Cardiac disorders

Palpitations, pericardial effusion, congestive cardiac failure, tachycardia, pulmonary edema, arrhythmia, atrial fibrillation, cardiac arrest, myocardial infarction, angina pectoris

Respiratory

Epistaxis, pleural effusion, interstitial pneumonitis, pulmonary fibrosis, pulmonary hypertension, pulmonary hemorrhage

General disorders

Weakness, anasarca, chills, malaise

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, hypocalcemia, hyperglycemia, hyponatremia, hyperkalemia, hypomagnesemia

Gastrointestinal disorders

Abdominal distension, gastro esophageal reflux, dry mouth, gastritis, gastric ulcer, stomatitis, mouth ulcer, eructation, esophagitis, dysphasia, and pancreatitis

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

Fluid retention and edema

The major disadvantage of Glivec is fluid accumulation which may causes edema majorly superficial edema has been reported. To overcome these problem patients may frequently monitor for manifestation of fluid retention.

Hematological toxicity

Neutropenia, thrombocytopenia, anemia are the major blood related problems. To avoid these conditions, monitor the patients periodically with counting blood cell counts weekly for one month, two weeks for two months.

Serious congestive heart failure and left ventricular dysfunction

Patients who have cardiac problems should be monitored frequently.

Hepatotoxicity

Liver function test should be taken periodically to overcome these problems. Hemorrhage

Gastrointestinal disorders

To avoid this problem, Glivec should be taken with food and large glass of water. Hyperesinophillic cardiac toxicity Dermatological toxicities

Hypothyroidism

Levothyroxine replacement therapy recommended; TSH level of the patients should be monitored periodically.

Drug – drug interaction

  • Drug which inhibits the CYP3A4 activity may have chance to reduce metabolism and elevates the plasma concentration of Glivec frequently.
  • Co administration of St. John’s wort with Glivec causes decreasing AUC of Glivec to 30%. To avoid this problem, the dosage of Glivec increases up to 1200mg /day (600mg as two times a day).
  • While concomitant use of Glivec with strong inducers of CYP3A4, the dose of Glivec increased to 50%. If used with CYP3A4 strong inducers the AUC of Glivec decreases to 73%.
  • Concomitant use of Glivec with strong CYP3A4 inhibitors; increase the risk of Glivec. Avoid these co administrations like Glivec with ketaconazole, itraconazole, clarithromycin, atazanavir, indinavir, ritonavir, voriconazole etc.
  • If concurrent usage of Glivec with grapefruit juice causes, increasing the plasma concentration of Glivec.
  • Co administering Glivec with CYP3A4 substrates like alfentanil, cyclosporine, ergotamine, fentanyl, sirolimus or Tacrolimus causes low therapeutic effects. Glivec elevates the plasma concentration of CYP3A4 metabolized drugs like lipid lowering, calcium channel blockers etc.
  • Warfarin is metabolized by CYP2C9 & CYP2A4, so patients who are taking anticoagulation therapy with Glivec , should take low molecular weight or standard heparin in reverse of warfarin.


Glivec 100mg tablet Contraindication


Hypersensitive reaction to Glivec mesylate and other excipients present in Glivec 100mg tablets.




Pregnancy category: D Glivec 100mg 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.

Glivec 100mg tablet container should be stored in cool and dry place It should be keep away from moisture, heat and light

If patient fail to take Glivec 100mg tablet, patient should have administered within a time. Otherwise, tablet should be discontinued and follow the next drug schedule.

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