Imatinib Mesylate

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Overview

What is Imatinib Mesylate?

Imatinib is a small molecule kinase inhibitor. Imatinib mesylate tablets are film-coated and contain imatinib mesylate equivalent to 100 mg or 400 mg of imatinib free base. Imatinib mesylate is designated chemically as 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate. The structural formula is:

CHNO•CHSO M.W. 589.7 (mesylate); 493.6 (free base)

Imatinib mesylate is a white to off-white to brownish or yellowish powder. Imatinib mesylate is very soluble in water and soluble in aqueous buffers less than or equal to pH 5.5, but is very slightly soluble to insoluble in neutral/alkaline aqueous buffers. It is soluble in polar solvents, but only slightly soluble to insoluble in low polar solvents. Imatinib mesylate is freely soluble to very slightly soluble in dimethyl sulfoxide, methanol and ethanol, but is insoluble in n-octanol, acetone and acetonitrile. The free base has very low solubility in water (0.001 g/100 mL) and in aqueous solutions that are slightly alkaline.

Inactive Ingredients: colloidal silicon dioxide, croscarmellose sodium, crospovidone, FD&C Yellow #6 Sunset Yellow FCF aluminum lake, hydroxypropyl cellulose, hypromellose, iron oxide yellow, lactose monohydrate, magnesium stearate, microcrystalline cellulose, sodium stearyl fumarate, talc, and titanium dioxide.

What does Imatinib Mesylate look like?

What are the available doses of Imatinib Mesylate?

Tablets (scored): 100 mg and 400 mg ()

What should I talk to my health care provider before I take Imatinib Mesylate?

How should I use Imatinib Mesylate?

Newly diagnosed adult and pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase.

The prescribed dose should be administered orally, with a meal and a large glass of water. Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day.

For patients unable to swallow the film-coated tablets, the tablets may be dispersed in a glass of water or apple juice. The required number of tablets should be placed in the appropriate volume of beverage (approximately 50 mL for a 100 mg tablet, and 200 mL for a 400 mg tablet) and stirred with a spoon. The suspension should be administered immediately after complete disintegration of the tablet(s).

For daily dosing of 800 mg and above, dosing should be accomplished using the 400 mg tablet to reduce exposure to iron.

Treatment may be continued as long as there is no evidence of progressive disease or unacceptable toxicity.

What interacts with Imatinib Mesylate?

Sorry No Records found

What are the warnings of Imatinib Mesylate?

Sorry No Records found

What are the precautions of Imatinib Mesylate?

Sorry No Records found

What are the side effects of Imatinib Mesylate?

Sorry No records found

What should I look out for while using Imatinib Mesylate?

None.

What might happen if I take too much Imatinib Mesylate?

Experience with doses greater than 800 mg is limited. Isolated cases of imatinib mesylate overdose have been reported. In the event of overdosage, observe the patient and give appropriate supportive treatment.

Adult Overdose

1,200 to 1,600 mg (duration varying between 1 to 10 days):

1,800 to 3,200 mg (as high as 3,200 mg daily for 6 days):

6,400 mg (single dose)

8 to 10 g (single dose):

A patient with myeloid blast crisis experienced Grade 1 elevations of serum creatinine, Grade 2 ascites and elevated liver transaminase levels, and Grade 3 elevations of bilirubin after inadvertently taking 1,200 mg of imatinib mesylate daily for 6 days. Therapy was temporarily interrupted and complete reversal of all abnormalities occurred within 1 week. Treatment was resumed at a dose of 400 mg daily without recurrence of adverse reactions. Another patient developed severe muscle cramps after taking 1,600 mg of imatinib mesylate daily for 6 days. Complete resolution of muscle cramps occurred following interruption of therapy and treatment was subsequently resumed. Another patient that was prescribed 400 mg daily, took 800 mg of imatinib mesylate on Day 1 and 1,200 mg on Day 2. Therapy was interrupted, no adverse reactions occurred and the patient resumed therapy.

Pediatric Overdose

One 3-year-old male exposed to a single dose of 400 mg experienced vomiting, diarrhea and anorexia and another 3-year-old male exposed to a single dose of 980 mg experienced decreased white blood cell count and diarrhea.

How should I store and handle Imatinib Mesylate?

Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. The USP defines controlled room temperature as a temperature maintained thermostatically that encompasses the usual and customary working environment of 20° to 25°C (68° to 77°F); that results in a mean kinetic temperature calculated to be not more than 25°C; and that allows for excursions between 15° and 30°C (59° and 86°F) that are experienced in pharmacies, hospitals, and warehouses.Each film-coated tablet contains 100 mg or 400 mg of imatinib free base.Imatinib mesylate tablets are available as follows:100 mg - orange to brown, film-coated, round-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7629" on the other side of the tablet, in bottles of 90 (NDC 60429-925-90).400 mg - orange to brown, film-coated, modified capsule-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7630" on the other side of the tablet, in bottles of 30 (NDC 60429-926-30).Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Do not crush imatinib mesylate tablets. Avoid direct contact of crushed tablets with the skin or mucous membranes. If such contact occurs, wash thoroughly as outlined in the references. Avoid exposure to crushed tablets Each film-coated tablet contains 100 mg or 400 mg of imatinib free base.Imatinib mesylate tablets are available as follows:100 mg - orange to brown, film-coated, round-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7629" on the other side of the tablet, in bottles of 90 (NDC 60429-925-90).400 mg - orange to brown, film-coated, modified capsule-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7630" on the other side of the tablet, in bottles of 30 (NDC 60429-926-30).Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Do not crush imatinib mesylate tablets. Avoid direct contact of crushed tablets with the skin or mucous membranes. If such contact occurs, wash thoroughly as outlined in the references. Avoid exposure to crushed tablets Each film-coated tablet contains 100 mg or 400 mg of imatinib free base.Imatinib mesylate tablets are available as follows:100 mg - orange to brown, film-coated, round-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7629" on the other side of the tablet, in bottles of 90 (NDC 60429-925-90).400 mg - orange to brown, film-coated, modified capsule-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7630" on the other side of the tablet, in bottles of 30 (NDC 60429-926-30).Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Do not crush imatinib mesylate tablets. Avoid direct contact of crushed tablets with the skin or mucous membranes. If such contact occurs, wash thoroughly as outlined in the references. Avoid exposure to crushed tablets Each film-coated tablet contains 100 mg or 400 mg of imatinib free base.Imatinib mesylate tablets are available as follows:100 mg - orange to brown, film-coated, round-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7629" on the other side of the tablet, in bottles of 90 (NDC 60429-925-90).400 mg - orange to brown, film-coated, modified capsule-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7630" on the other side of the tablet, in bottles of 30 (NDC 60429-926-30).Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Do not crush imatinib mesylate tablets. Avoid direct contact of crushed tablets with the skin or mucous membranes. If such contact occurs, wash thoroughly as outlined in the references. Avoid exposure to crushed tablets Each film-coated tablet contains 100 mg or 400 mg of imatinib free base.Imatinib mesylate tablets are available as follows:100 mg - orange to brown, film-coated, round-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7629" on the other side of the tablet, in bottles of 90 (NDC 60429-925-90).400 mg - orange to brown, film-coated, modified capsule-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7630" on the other side of the tablet, in bottles of 30 (NDC 60429-926-30).Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Do not crush imatinib mesylate tablets. Avoid direct contact of crushed tablets with the skin or mucous membranes. If such contact occurs, wash thoroughly as outlined in the references. Avoid exposure to crushed tablets Each film-coated tablet contains 100 mg or 400 mg of imatinib free base.Imatinib mesylate tablets are available as follows:100 mg - orange to brown, film-coated, round-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7629" on the other side of the tablet, in bottles of 90 (NDC 60429-925-90).400 mg - orange to brown, film-coated, modified capsule-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7630" on the other side of the tablet, in bottles of 30 (NDC 60429-926-30).Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Do not crush imatinib mesylate tablets. Avoid direct contact of crushed tablets with the skin or mucous membranes. If such contact occurs, wash thoroughly as outlined in the references. Avoid exposure to crushed tablets Each film-coated tablet contains 100 mg or 400 mg of imatinib free base.Imatinib mesylate tablets are available as follows:100 mg - orange to brown, film-coated, round-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7629" on the other side of the tablet, in bottles of 90 (NDC 60429-925-90).400 mg - orange to brown, film-coated, modified capsule-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7630" on the other side of the tablet, in bottles of 30 (NDC 60429-926-30).Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Do not crush imatinib mesylate tablets. Avoid direct contact of crushed tablets with the skin or mucous membranes. If such contact occurs, wash thoroughly as outlined in the references. Avoid exposure to crushed tablets Each film-coated tablet contains 100 mg or 400 mg of imatinib free base.Imatinib mesylate tablets are available as follows:100 mg - orange to brown, film-coated, round-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7629" on the other side of the tablet, in bottles of 90 (NDC 60429-925-90).400 mg - orange to brown, film-coated, modified capsule-shaped tablet, scored on one side and debossed with "TE" on the left side of the score and with "VA" on the right side of the score and debossed with "7630" on the other side of the tablet, in bottles of 30 (NDC 60429-926-30).Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Do not crush imatinib mesylate tablets. Avoid direct contact of crushed tablets with the skin or mucous membranes. If such contact occurs, wash thoroughly as outlined in the references. Avoid exposure to crushed tablets

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Clinical Information

Chemical Structure

No Image found

Clinical Pharmacology

Imatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the BCR-ABL tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in CML. Imatinib inhibits proliferation and induces apoptosis in BCR-ABL positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia. Imatinib inhibits colony formation in assays using peripheral blood and bone marrow samples from CML patients.

In vivo

Imatinib is also an inhibitor of the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-kit, and inhibits PDGF- and SCF-mediated cellular events.

Non-Clinical Toxicology

None.

Imatinib mesylate is often associated with edema and occasionally serious fluid retention []. Weigh and monitor patients regularly for signs and symptoms of fluid retention. Investigate unexpected rapid weight gain carefully and provide appropriate treatment. The probability of edema was increased with higher imatinib mesylate dose and age greater than 65 years in the CML studies. Severe superficial edema was reported in 1.5% of newly diagnosed CML patients taking imatinib mesylate, and in 2% to 6% of other adult CML patients taking imatinib mesylate. In addition, other severe fluid retention (e.g., pleural effusion, pericardial effusion, pulmonary edema, and ascites) reactions were reported in 1.3% of newly diagnosed CML patients taking imatinib mesylate, and in 2% to 6% of other adult CML patients taking imatinib mesylate. In a randomized trial in patients with newly diagnosed Ph+ CML in chronic phase comparing imatinib mesylate and nilotinib, severe (Grade 3 or 4) fluid retention occurred in 2.5% of patients receiving imatinib mesylate and in 3.9% of patients receiving nilotinib 300 mg twice daily. Effusions (including pleural effusion, pericardial effusion, ascites) or pulmonary edema were observed in 2.1% (none were Grade 3 or 4) of patients in the imatinib mesylate arm and 2.2% (0.7% Grade 3 or 4) of patients in the nilotinib 300 mg twice daily arm.

The following serious adverse reactions are described elsewhere in the labeling:

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Review

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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Interactions

A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).

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