Imatinib Pharmacology


About Imatinib
Anticancer, Tyrosine- kinase inhibitor, First generation.
Mechanism of Action of Imatinib
Imatinib is an inhibitor of multiple tyrosine kinases including Kit, abl, and PDGFR( platelet-derived growth factor receptor) and inhibit phosphorelation.
Pharmacokinets of Imatinib
Absorption: Absorbed after oral administration
Distribution: Protein binding 95%
Metabolism: Metabolised in the liver
Excretion: Excretion via fecal(68%), and renal(13%)
Onset of Action for Imatinib
Hours to day
Duration of Action for Imatinib
Half Life of Imatinib
18 hrs and 40 hrs(active metabolite)
Side Effects of Imatinib
1.Weight gain
8.Musculoskeletal pain.
Contra-indications of Imatinib
1.Hypersensitivity to drug
2.Cardiac problem
Special Precautions while taking Imatinib
1.Cardiac disease
2.Liver disease
3.Kidney disease
5.Fluid retention
Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
Use with caution
Neonates :Contraindicated
Indications for Imatinib
1.Chronic myelogenous leukemia
2.Lymphoblastic leukemia (PH+ALL)
3.Gastrointestinal stromal tumors
4.Systemic mastocytosis
5.Hypereosinophilic syndrome
6.Dermatofibrosarcoma protuberans.
7.Plexiform neurofibromas
Interactions for Imatinib
CYP3A4 inhibitors e.g. ketoconazole, erythromycin, clarithromycin, itraconazole, grapefruit juice)---- decrease metabolism---- increase Imatinib exposure (40%)

CYP3A4 inducers (dexamethasone, phenytoin, carbamazepine, rifampicin, phenobarbital or St. John?s Wort)----- increase metabolism---- decrease Imatinib exposure (74%)

CYP2D6 inhibitors (e.g. doxorubicin, quinidine, vinca alkaloids, dextropropoxyphene)---- decrease metabolism---- increased Imatinib concentrations.

CYP 2C9 substrates (e.g. Warfarin)---- Imatinib inhibits CYP2C9 at high doses---- increase anticoagulant effect.
Typical Dosage for Imatinib
Adult: 400 mg to 600 mg once dialy for Chronic Myeloid Leukemia (Ph+ CML)
600 mg to 800 mg (given as 400 mg twice daily) ( in accelerated phase or blast crisis Ph+CML)

Children:340 mg/m?/day (not to exceed 600 mg) in Ph+ CML

Schedule of Imatinib
Storage Requirements for Imatinib
Store at room temperature at 77 degrees F (25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is permitted. Do not store in the bathroom. Keep all medications away from children and pets.
Effects of Missed Dosage of Imatinib
Effects of Overdose of Imatinib

Home Delivery for Imatinib in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including imatinib.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for imatinib and other medicines and health products. Home delivery services for imatinib may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take imatinib only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for imatinib before they complete the sale. You can get this information while placing the order for imatinib with the pharmacy.

Imatinib is a generic medicine name and there are several brands available for it. Some of the brands for imatinib might be better known than imatinib itself. If the pharmacy that's willing to deliver medicines to your home doesn't have imatinib in stock, you can ask for one of the branded alternatives for imatinib.