Imat 100mg (Imatinib)

DESCRIPTION

Imat 100mg tablet belongs to class of anti cancer medicine which is useful for treating; Advanced myelogenous leukemia (CML), and gastrointestinal stromal tumors (GISTs) and a number of malignancies. Imat 100mg is a class of tyrosine kinase inhibitor which inhibits BCR-ABL kinase produced by chromosomal rearrangement in chronic myeloid leukemia and acute lymphoblastic leukemia.

The PDG-derived tyrosine kinase which are expressed in gastrointestinal stromal tumor. Imat 100mg is used as alone treatment, or combine with some other medicine in the conditions of certain types of cancer or bone marrow disorders.

INDICATION

The drug Imat 100mg is mostly indicated for the treatment of patient having following disease 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

ADME

ABSORPTION

It is highly absorbed peak plasma concentration of 2-4 hours. The bioavailability is 98%.

DISTRIBUTION

Imat 100mg is highly bound to the human plasma protein is 95%.

METABOLISM

Primary enzyme that is specific for metabolism of Imat 100mg tablet is CYP3A4. The Imat 100mg Active metabolite is N-demethylated piperizine derivative

ELIMINATION

The excretion of Imat 100mg is broadly occurred in feces. Nearly drug eliminated within 7 days via feces 81% and of drug through urine 13%. The half life time of Imatinib around 18 and 40 hours respectively

DOSAGE MANAGEMENT

DOSAGE AND ADMINISTRATION

The usual dose of tablet Imat 100mg or 600mg as a single dose. Whereas 800mg which is administered as 400mg twice daily. Imat 100mg tablets should be taken with food 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 Imat 100mg 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 Imat 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

PRECAUTIONS

in hepatic impairment patients use with caution Avoid concomitant use with strong CYP3A4 inducers Risk of serious ventricular dysfunction (CHF) Bleeding occurs In children Growth retardation occurs

SIDE EFFECTS

GENERAL DISORDERS

Weakness, anasarca, chills, malaise

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.

CARDIAC DISORDERS

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

GASTROINTESTINAL DISORDERS

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

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

Sepsis, herpes simplex, herpes zoster, cellulitis, urinary tract infection, gastroenteritis

METABOLISM AND NUTRITION

Weight decreased, loss of appetite, dehydration, gout, hyperuricemia, hypocalcaemia, hyperglycemia, hyponatremia, hyperkelamia, hypomagnesemia

MUSCULOSKELETAL

Joint swelling, muscle stiffness, muscular weakness, arthritis

NERVE SYSTEM

Paresthesia, hypesthesia, syncope, peripheral neuropathy, somnolence, tremor

RENAL AND URINARY DISORDERS

Renal failure, frequency of urine will increased, Hematuria, renal pain

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

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

DRUG INTERACTION

Imat 100mg tablet is contraindicated to some medicines like; Interaction with these drugs Cobimetinib, conivaptan, dihydroergotamine, eliglustat, aspirin, vitamin D, rosuvastatin, duloxetine, dasatinib, grapefruit, ibuprofen, Atorvastatin, pregabalin will reduce effectiveness of the drug.

CONTRAINDICATION

The Imat 100mg tablet is contraindicated to the hypersensitivity reaction and the products of its expicients

PREGNANCY & LACTATION

Pregnancy category: D Imat 100mg should not administrated for pregnant women and breast feeding mothers, it will cause fetal malformations and cause harm to the fetus. The metabolites excreted into human milk

STORAGE 

Stored in cool and dry place The drug should keep away from moisture, heat and light.

MISSED DOSE

If the patient missed to take the drug, he/ she should administered within a time. Or the ,tablet should be discontinued and follow the next drug schedule. Please consult the doctor.