Dasatinib

Indications
 Oral
Chronic myeloid leukaemia
Adult: For chronic phase CML: Initially, 100 mg once daily, may increase up to 140 mg once daily. For accelerated, myeloid or lymphoid blast phase CML or Philadelphia chromosome-positive ALL: Initially, 70 mg bid, may increase up to 100 mg bid.
Contraindications
 Pregnancy.
Warnings / Precautions
 Caution in patients with hypokalaemia, hypomagnesaemia, or those on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines due to possible QT interval prolongation. Antacids should be given 2 hr apart from the admin of dasatinib. Monitor CBC and signs of haemorrhage regularly. Lactation.
Adverse Reactions
 Fluid retention, Gl disturbances and bleeding. Severe CNS haemorrhages. GI haemorrhaging may require interruption of therapy, and transfusions. Myelosuppression, headache, pyrexia, musculoskeletal pain, fatigue, skin rashes, dyspnoea, cough, dizziness, chest pain, neuropathy, chills and pruritus.
Overdose Reactions
 Overdose may lead to severe myelosuppression and bleeding.
Drug Interactions
 Azole antifungals, macrolide antibacterials, HIV-protease inhibitors and nefazodone may increase plasma concentrations of dasatinib. Carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampicin, antacids and PPIs may reduce blood concentrations of dasatinib.
See Below for More dasatinib Drug Interactions
Food Interactions
 St John's wort may decrease dasatinib concentrations.
Mechanism of Actions
 Dasatinib is used for the treatment of all phases of chronic myeloid leukaemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukaemia (ALL) in adults who have resistance or intolerance to previous therapy, including imatinib.
Absorption: Cmax is achieved 0.5-6 hr after oral admin.
Distribution: Extensively distributed into the extravascular space. Apparent volume of distribution is 2505 L.
Metabolism: Primarily metabolised by CYP3A4.
Excretion: Primarily via faeces.
Administration
 May be taken with or without food. (Swallow whole, do not break/crush/cut.)
Storage Conditions
 Oral: Store between 15-30°C.
ATC Classification
 L01XE06 - dasatinib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
Storage
 Oral: Store between 15-30°C.
Available As
  • Dasatinib 50 mg

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