NILOTINIB

COMMON BRAND NAME(S): Tasigna

GENERIC NAME(S): NILOTINIB HCL

 

Description: Nilotinib is a potent inhibitor of BCR-ABL tyrosine kinase which can slow down or stop the growth of cancer cells.

Pharmacokinetics:

Absorption: Food increases its bioavailability by approx 2-fold. Bioavailability: Approx 30%. Time to peak plasma concentration: Approx 3 hr.

Distribution: Plasma protein binding: Approx 98%.

Metabolism: Undergoes hepatic oxidation and hydroxylation via CYP3A4 isoenzyme.

Excretion: Via faeces (approx 93% as unchanged drug). Elimination half-life: Approx 17 hr.

  • Used for
    • Treatment of chronic myelogenous leukemia-CML by slowing or stopping the growth of cancer cells.

 

How to use nilotinib

  • Always refer to your doctors instructions before taking this medication. Duration and dosage will be determined by your medical condition and its response to the medication. Make sure to take this mediciation in the prescribed amount and time period even after symptoms disappear. Discontinuing the medication before completion of treatment may cause incomplete treatment of condition. If Symptoms persist, consult your doctor

 

  • Taken by mouth; on an empty stomach; Do not eat any food for at least 2 hours before or for 1 hour after; usually twice a day or as directed by your physician; Swallow the capsule whole with water. Do not open, break, or chew the capsules. If unable to swallow the capsules, the capsules may be opened and the contents sprinkled in 1 teaspoon of applesauce. This mixture should be swallowed right away (within 15 minutes). Use only 1 teaspoon of applesauce. Do not sprinkle the contents onto other types of food.

 

  • Avoid eating grapefruit or drinking grapefruit juice while being treated with this medication unless your doctor instructs you otherwise. Grapefruit can increase the amount of certain medications in your bloodstream. Consult your doctor or pharmacist for more details.

 

If you are also taking an antacid, take it 2 hours before or after nilotinib. If you are also taking an H2 blocker (such as cimetidine, famotidine), take it 10 hours before or 2 hours after nilotinib.

  • Can infrequently cause serious (possibly fatal) irregular heartbeats (QT prolongation). Nilotinib should not be used in people with low blood levels of certain minerals (potassium, magnesium) or a certain heart problem (long QT syndrome).
    • Minor side effects (if these symptoms persist or worsen, inform your doctor)
      • Nausea, vomiting, headache, tiredness, constipation, and diarrhea

     

    • Serious side effects (inform your doctor immediately)
      • severe tiredness, pale skin, signs of infection (such as fever, chills, persistent sore throat), easy bruising/bleeding (such as bloody/black stool, bloody/pink urine), severe stomach/abdominal pain, toe/joint pain, painful urination, change in the amount of urine, swelling hands/ankles/feet, unusual/rapid weight gain, symptoms of high blood sugar (such as increased thirst/urination), signs of liver disease (such as persistent nausea/vomiting, stomach/abdominal pain, yellowing eyes/skin, dark urine), fast/pounding/irregular heartbeat, severe dizziness, fainting, seizures, signs of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating), signs of a stroke (such as weakness on one side of the body, slurred speech, sudden vision changes, confusion), signs of bleeding in the brain (such as sudden severe headache, sudden vision changes, confusion, loss of consciousness), signs of blood circulation disease (such as numbness/pain in the legs, leg pain with physical activity, decrease in walking distance).

     

    • Severe allergic reactions are rare. Get immediate medical help if you notice the following:

    Rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing

    • Precautions:
      • Inform your doctor
        • Allergy to the medication or to lactose/galactose or any allergies
        • Medical History of liver disease, pancreatitis, heart disease (such as coronary artery disease, chest pain, heart attack), high blood pressure, high cholesterol, diabetes, stroke (including “mini-strokes” or transient ischemic attacks), blood circulation disease (peripheral arterial disease), blood vessel disease (hardening of the arteries/atherosclerosis).

       

      • May make you more likely to get infections or may worsen any current infections. Therefore, wash your hands well to prevent the spread of infection. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.

       

      • Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).

       

       

      • Not recommended for use during pregnancy as it may harm an unborn baby. If you are planning to be pregnant or think you may be pregnant, discuss the risks and benefits of use with your doctor.

       

      • It is uknown if this drug passes into breast milk. Before breast-feeding, consult your physician.

       

      Interactions:

       

      Taking multiple drugs may affect how medications work and/or cause unwanted side effects. List down all the medications you are taking and inform your physician and pharmacist. Do not take, discontinue, or alter any dose of medications without prior approval of your physician.

       

      • Products that may interact with this medication include:

      antacids, H2 blockers (such as cimetidine/famotidine), proton pump inhibitors (such as omeprazole), azole antifungals (such as itraconazole, ketoconazole), HIV protease inhibitors (such as ritonavir), macrolide antibiotics (such as clarithromycin), rifamycins (such as rifabutin), St. John’s wort, drugs used to treat seizures (such as carbamazepine, phenytoin), amiodarone, dofetilide, pimozide, procainamide, quinidine, sotalol, macrolide antibiotics (such as erythromycin), among others.

    • Overdose: If overdose is suspected, contact a poison control center or emergency room immediately.

       

      Missed Dose

      If you miss a dose, take it as soon as you remember but do not take if it is less than 2 hours before or 1 hour after a meal. If it is near the time of the next dose, skip the missed dose and As soon as you remember, take a regular dose or if the time of the next dose is near, wait for it before taking another dose and resume your usual schedule. Do not increase the dose to compensate for the missed dose.

       

      Storage

      • Room temperature
      • Do not expose to light and moisture
      • Do not store in the bathroom
      • Keep all medications away from pets and children

       

      Brands:

       

      Available Brands:

      Tasigna [ Novartis Healthcare ]

Related Articles

LESINURAD

Lesinurad suppresses the enzymes uric acid transporter 1 (URAT1) and organic anion carrier 4 (OAT4), which increases uric acid outflow [...]

LEMBOREXANT

Lemborexant is an orexin potent inhibitor that's competitive. It is considered to prevent the attachment of wake-promoting neurotrophins orexin A [...]

INSULIN LISPRO + INSULIN LISPRO PROTAMINE

Insulin lispro is a fast-acting human insulin alternative, whereas insulin lispro protamine is a slow-acting human insulin alternative. They both [...]