Imatib 100mg

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BRAND :  IMATIB PRICE :  125$ STRENGTH : 100 MG ACTIVE :  IMATIB-IMATINIB-MESYLATE-100MG COMPANY NAME :  CIPLA TABLETS :  100 TABLETS read more

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Drug profile

Imatib 100mg tablets are containing anti-neoplastic activity which is due to the presence of Imatinib mesylate as an active component.

Imatib 100mg tablet is a cipla product, which is FDA approved product for the treatment of various stages of myelogenous leukemia associated with Philadelphia chromosome.

Imatib 100mg is a prescription medicine, prescribed only by medical oncologist

Imatib 100mg is known to contains 100mg of Imatinib mesylate

Brand: Imatib

Active component: Imatinib mesylate

Strength: 100mg

Mfg: Cipla

Package: 10 tablets in a strip; 10 stripes in a carton

Category: Anti-neoplastic agent

Prescribing information of Imatib 100mg

The prescribing information of Imatib 100mg are given below as follows;

Imatib 100mg is used in both adults and pediatric patients with various dosage conditions depending upon the body weight of the patients.

Conditions like;

Newly diagnosed Philadelphia positive chronic myeloid leukemia

Philadelphia positive chronic myeloid leukemia in

  • Blast crisis, accelerated phase, or
  • Chronic stage while after interferon alfa therapy

Philadelphia positive acute lymphoblastic leukemia

Dermatofibrosarcoma protuberans

cKit positive gastrointestinal stromal tumors (GIST)

Myelodysplastic or Myeloproliferative diseases

Aggressive systemic mastocytosis

Hyperesinophillic syndrome or chronic esinophillic leukemia

Supporting therapy of GIST

Mechanism of Imatib 100mg

Imatib comprises of Imatinib mesylate, which has tyrosine kinase inhibiting activity.

Imatib prohibits the Bcr-Abl tyrosine kinase in in-vivo, invitro and cellular levels. Imatinib mesylate prohibits multiplication and generate apoptosis in Bcr-Abl positive cell line in addition to new leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia and acute lymphoblastic leukemia patients.

Imatinib mesylate prohibits growth of the tumor cells of Bcr-Abl transfected murine myeloid cells along with Bcr-Abl positive lines in chronic myeloid leukemia patients in blast crisis stage.

 Imatinib mesylate prohibits various receptors like;

Stem cell factor receptor coded for by c-Kit proto oncogene

Discoidin domain receptor (DDR1 & DDR2)

Colony stimulating factor receptors (CSF-1R)

Platelet derived growth factor receptors; Alpha & beta (PDGFR-alpha & PDGFR-beta)

Imatinib mesylate is prohibits cellular development which is interceded by stimulating these receptor kinase

Imatinib mesylate is also prohibits multiplication and encourage apoptosis in gastrointestinal stromal tumor in-vitro which precisely activating kit alteration.

Absorption

The absorption of Imatinib is occurring very rapidly. The peak plasma time of Imatinib reaches within 2 to 4 hours after dose administration.

The mean absolute bioavailability of Imatinib is reaches as 98%.

The effect of food is;

While taking with high fat meal, the absorption rate of Imatinib mesylate reduced at least possible correlated to fasted state.

Distribution

Imatinib mesylate has high plasma protein bound capacity, occurs relatively 95%

Metabolism

Imatinib metabolism occurs majorly in liver. The major circulating metabolite of Imatinib mesylate is N-demethylated piperizine derivative has potent activity compared to the parent compound.

Elimination

The major route of elimination occurs through feces usually as metabolites.

Almost 75% of drug undergoes biotransformation, the half life period of Imatinib is 19 hours (14 to 23 hours) and its main circulating metabolite is 40 hours (30 to 50 hours)

When to take the Imatib 100mg tablet

Imatib 100mg tablets should be administered with food with large amount of water.

The dosage of Imatinib is usually taken as a single dose or alternatively.

The usage of Imatinib tablets are usually not recommended under the age of 2 years.

Dosage regimens of Imatib 100mg

Chronic myelogenous leukemia:

In chronic phase: The usual dose of Imatinib is 400mg should be taken as a single dose orally

In accelerated or blast crisis stage: The usual dose of Imatinib is 600mg should be taken as single dose

In disease advancement chronic phase: The recommended dosage of Imatinib is 600mg is taken as once a day.

 In disease advancement accelerated or blast crisis stage: The dosage of Imatinib is 400mg should be administered as two times a day.

Acute lymphoblastic leukemia:

The usual recommended dosage of Imatinib is 600mg should be taken as single dose.

Myeloproliferative disorder:

The suggested dosage of Imatinib is 400mg should be given as a single dose.

Myelodysplastic disease:

The recommended dosage of Imatinib is 400mg should be taken as a single dose.

Systemic mastocytosis:

ASM without D816V c-Kit: 400mg of Imatinib is given orally as a single dose

Patients with ASM related to esinophillia (fusion kinase FIP1L1-PDGFR alpha) initial dose is 100mg per day, dose slightly increased to 400mg.

Hyperesinophillic syndrome:

Patients with HES/CEL: The recommended dose is 400mg given orally as a single dose.

Patients HES /CEL with FIP1L1-PDGFR alpha fusion kinase: The initial dose is 100mg then increased to 400mg.

Chronic esinophillic leukemia:

Patients with HES/CEL: The recommended dose is 400mg given orally as a single dose.

Patients HES /CEL with FIP1L1-PDGFR alpha fusion kinase: The initial dose is 100mg then increased from 100mg to 400mg.

Dermatofibrosarcoma protuberans:

The recommended dosage is 100mg of Imatinib should be given as a single dose.

Gastrointestinal stromal tumor:

In malignant condition: The recommended dose of Imatinib is 400mg orally per day, then the dose is increased up to 800mg (400mg as two times a day).

In pediatrics:

Chronic myelogenous leukemia:

The recommended dosage is 340mg/m2 given orally as a single dose or 170mg/m2 given orally as two times a day.

Maximal dosage of Imatinib is 600mg per day.

Acute lymphoblastic leukemia:

The recommended dosage is 340mg/m2 given orally as a single dose

Maximum dose: 600mg as single dose.

In renal impairment patients:

Mild: CrCl 40 to 59ml/min the dose higher than 600mg, not recommended.

Moderate: CrCl 20 to 39ml/min decreasing the initial dose by 50% and further maintenance dose can be increased if tolerated.

The dose greater than 400mg not suggested.

In chronic or severe: CrCl less than 20ml/min, Imatinib is use with caution and the tolerated dose is 100mg per day.

In hepatic impairment:

Mild to moderate: dosage adjustment is not recommended

In chronic condition: Dose should be decreased to 25% from recommended dose.

 Avoid concomitant use of Imatinib with strong CYP3A4 inducers like phenytoin, carbamazepine, rifampin, rifampicin, Phenobarbital etc. If co administration of Imatinib with strong CYP3A4 inducers is necessary, then the dose of Imatinib is increased to 50%.

Imatib 100mg caused side effects

Fluid retention

Superficial edema

Nausea

Muscle cramps

Musculoskeletal pain

Diarrhea

Rash and related problems

Fatigue

Headache

Joint pain

Abdominal pain

Nasopharyngitis

Hemorrhage (GI & CNS)

Myalgia

Dyspepsia

Respiratory tract infections

Dizziness

Weight gain

Depression

Influenza like symptoms

Bone pain

Constipation

Sinusitis

Hematological toxicity like;

Neutropenia

Thrombocytopenia

Anemia

Creatinine levels increased

Elevation of bilirubin

Elevation of alkaline phosphatase

Elevation of SGOT & SGPT

Anorexia

Eye edema

Lacrimation elevation

Dyspnea

Rhinitis

Drug – drug interaction

While concomitant use of Imatinib with strong inducers of CYP3A4, the dose of Imatinib increased to 50%. If used with CYP3A4 strong inducers the AUC of Imatinib decreases to 73%.

Co administration of st. Johns wort with Imatinib causes decreasing AUC of Imatinib to 30%. To avoid this problem, the dosage of Imatinib increases up to 1200mg /day (600mg as two times a day).

Concomitant use of Imatinib with strong CYP3A4 inhibitors; increase the risk of Imatinib. Avoid these co administrations like Imatinib with ketaconazole, itraconazole, clarithromycin, atazanavir, indinavir, ritonavir, voriconazole etc.

If concurrent usage of Imatinib with grapefruit juice causes, increasing the plasma concentration of Imatinib.

Drug which inhibits the CYP3A4 activity may have chance to reduce metabolism and elevates the plasma concentration of Imatinib frequently.

Co administering Imatinib with CYP3A4 substrates like alfentanil, cyclosporine, ergotamine, fentanyl, sirolimus or Tacrolimus causes low therapeutic effects. Imatinib elevates the plasma concentration of CYP3A4 metabolized drugs like lipid lowering, calcium channel blockers etc.

Warfarin is metabolized by CYP2C9 & CYP2A4, so patients who are taking anticoagulation therapy with Imatinib, should take low molecular weight or standard heparin in reverse of warfarin.

Imatinib has low inhibitory effect on CYP2D6 mediated metabolism, if co administration of Imatinib with CYP2D6 metabolized drugs like metoprolol causes increasing the AUC and Cmax of metoprolol.

Imatinib prohibits the acetaminophen O glucuronidate pathway; co administration of Imatinib with acetaminophen causes no changes in pharmacokinetic of acetaminophen.

Food drug interaction

Avoid to take grapefruit juice during Imatinib therapy, because to elevate the blood levels and effect of Imatinib.

Possible contraindication

An anaphylactic reaction occurs due to the component present in the Imatib tablets.

Safety measures

Fluid retention and edema: The major disadvantage of Imatinib is fluid accumulation which may causes edema majorly superficial edema has been reported. To overcome these problem patients may frequently monitor for manifestation of fluid retention.

Hematological toxicity: Neutropenia, thrombocytopenia, anemia are the major blood related problems. To avoid these conditions, monitor the patients periodically with counting blood cell counts weekly for one month, two weeks for two months.

Serious congestive heart failure and left ventricular dysfunction: Patients who have cardiac problems should be monitored frequently.

Hepatotoxicity: Liver function test should be taken periodically to overcome these problems.

Hemorrhage

Gastrointestinal disorders: To avoid this problem, Imatinib should be taken with food and large glass of water.

Hyperesinophillic cardiac toxicity

Dermatological toxicities

Hypothyroidism: Levothyroxine replacement therapy recommended; TSH level of the patients should be monitored periodically.   

Pregnancy and lactation

Pregnancy category of Imatinib: D

Imatinib tablets should not be recommended in pregnancy condition. Teratogenecity occurs in patients who are receiving Imatinib

Breast feeding should not be recommended

Children & adolescents: Growth retardation occurs in children who are receiving Imatinib.

Storage and handling

Imatib tablets container should be kept at 25oC (77oF); excursion allowed between 15oC to 30oC.

Container should be keep away from heat, moisture and light

The shelf life of Imatinib is 2 years

Missed dose

Imatib 100mg tablet is a chemo medicine; it should not be used as self medication.

Imatib 100mg tablet is used under the guidance of medical practitioner.

If patients fail to take Imatib tablet, must consult with oncologist and take the dose within the time as soon as possible. On the other hand the missed dose should be avoid and follow the regular dosing schedule.

Over dosage

The maximum dose of Imatinib is 800mg/day.

In adult:

Imatinib dose of 1200 to 1600mg causes nausea, vomiting, diarrhea, rash Erythema, edema, fatigue, muscle spasm, thrombocytopenia, and loss of appetite.

Imatinib dose of 1800mg to 3200mg causes weakness, Myalgia, elevation of bilirubin, gastrointestinal pain, elevating CPK.

Imatinib dose of 6400mg causes nausea, abdominal pain, pyrexia, facial swelling, neutrophils counts depletes and elevation of transaminase.

Imatinib dose of 8 to 10gm causes gastrointestinal pain

In pediatric:

Pediatric patient exposed to 400mg of Imatinib have vomiting, diarrhea and anorexia in adverse.

If patient exposed to 980mg causes depletion in white blood cell count and diarrhea.

Patient suffered with myeloid blast crisis stage occurs;

Grade 1: Increased serum creatinine

Grade 2: Ascites, increased transaminase level

Grade 3: Bilirubin levels get elevated after rashly administering 1200mg of Imatinib daily for 6 days.

The treatment with Imatinib is postponed for short period of time until complete reversal of all deformities which is occurred within one week.

Again therapy is continue with the dose of 400mg of Imatinib without reappearance of adverse effects

If patient with muscle cramps after getting 1600mg of Imatinib for 6 days, complete reoccurrence from muscle cramps occur and follow the therapy.

 

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