Nilotinib

Also known as: AMN 107, Nilotinibum

Drug #2289

Nilotinib is an antineoplastic agent and shows its activity through tyrosine kinase inhibitor that is used for the treatment of chronic myeloid leukaemia.chemically it is Nilotinibum. 4-Methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]- amino}benzamide

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Primary Characteristics

Nilotinib is also known as AMN 107, Nilotinibum.

It is of Synthetic origin and belongs to n-phenylbenzamides.

It belongs to Tyrosine kinase inhibitor pharmacological group on the basis of mechanism of action.

Molecular Weight: 529.51 · Non-proprietary name: Nilotinib.

Pharmacokinetics

Absorption: Nilotinib has an oral bioavailability is 30%.

Distribution: Nilotinib has a volume of distribution is 0.71. plasma protein binding is about 98%.

Elimination: it is metabolised via liver, plasma half-life is 17hrs, renal excretion is 94% by feces.

Indications

Nilotinib is primarily indicated in conditions like Myeloid leukaemia.

Contraindications

None recorded.

Dosage

Nilotinib's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
400 mg	400 mg	Every 2h	PO	No food should be consumed for at least 2 hours before the dose is taken and no food should be consumed for at least one hour after the dose is taken
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

4 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Nilotinib in overdosage may give rise to further complications which include Thrombocytopenia , Neutropenia , Pneumonia, Leukopenia, febrile neutropenia, intracranial hemorrhage, pyrexia, febrile neutropenia, intracranial hemorrhage, eleated lipase.

Nilotinib is known to cause more or less tolerable side effects which are usually transient. These include Diarrhea, Fatigue, Headache, Nausea, Pruritis, Rash, Vomiting .

Warnings / Precautions

Myelosuppression: Associated with neutropenia, thrombocytopenia and anemia. CBC should be done every 2 weeks for the first 2 months, then monthly. Reversible by withholding dose. Dose reduction may be required. nilotinib prolongs the QT interval. Correct hypokalemia or hypomagnesemia prior to administration and monitor periodically.Caution is recommended in patients with history of pancreatitis. Check serum lipase periodically. nilotinib may result in elevations in bilirubin, AST/ALT, and alkaline phosphatase. Check hepatic function tests periodically. nilotinib can cause hypophosphatemia, hypokalemia, hyperkalemia, hypocalcemia, and hyponatremia. Correct electrolyte abnormalities prior to initiating Tasigna and monitor periodically during therapy. Food increases blood levels of nilotinib . Avoid food 2 hours before and 1 hour after a dose.Fetal harm can occur when administered to a pregnant woman.

Interference in Pathology

Nilotinib may interfere in the diagnosis of elevated blood glucose, elevated lipids.

Available Brands

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Single Ingredient

Caps

150 mg 200 mg

Storage Conditions

Nilotinib should be stored capsule.

Drug Classification

1.8.2 — Cytotoxic (anti-neoplastic) drugs

Manufacturers

Manufacturers of Nilotinib in Pakistan:

Novartis