Geftinat 250mg Tablet

What is Geftinat 250 mg?

IMATIB is a chemotherapy drug that works by slowing or stopping the growth of cancer cells. Imatib tablets 100mg contain imatinib, a tyrosine kinase (TK) inhibitor that is used to treat several cancers characterised by an abnormal TK that results in loss of control of cell growth, without affecting normal cells.

Imatib containing the active ingredient imatinib mesylate is an anticancer type of medicine called a kinase inhibitor. It works by interfering with the action of certain proteins to help prevent cancer cells from multiplying and stop the spread of cancer cells.

It can be utilized to treat certain types of cancer such as leukemia, gastrointestinal stromal tumors, and dermamtofibrosarcoma protuberans when the tumor cannot be removed surgically, has spread to other parts of the body or has come back after surgery.

Geftinat 250 mg Uses

Imatib is usually taken once or twice per day or as directed by a doctor. The tablets should be taken with a meal along with a full glass of water. For patients who cannot swallow the tablet whole, it may be dissolved in a glass of water or apple juice to be taken as a liquid. Contact a physician for the correct dosage as it will depend on the sick person situation, weight and response to the medication.

How does Geftinat 250 mg work?

Imatib tablets 100mg contain imatinib, a tyrosine kinase (TK) inhibitor that blocks the activity of several different TKs.  These TKs are cell surface receptors for many cellular messengers including growth factors.  Tyrosine kinase is an enzyme that phosphorylates a protein inside a cell, which is the way many cell processes are regulated and is the first step in a complex cell signalling pathway involved in cell proliferation and survival. 

Normally activation of these TK receptors is regulated and therefore, cell proliferation is controlled and programmed cell death (apoptosis) takes place.  However, over production or over stimulation of this enzyme receptor causes loss of control of cell growth resulting in enhanced cell proliferation, arrest in cell differentiation (when a simple cell becomes specialised for a particular function) and resistance to cell death.  This is a common mechanism found in several cancers. 

These abnormal enzymes are usually a product of a genetic mutation resulting in the formation of an oncogene, which is a gene that has the potential to cause cancer.

The abnormality can result from overproduction or constitutive activation of the respective TK involved.  The Philadelphia chromosome is a chromosome abnormality caused by exchange of genetic material between chromosomes 9 and 22 resulting in a truncated chromosome 22 containing the proto- oncogene Bcr-Abl11.

A proto-oncogene is a gene that can cause normal cells to become tumour cells when mutated to become an oncogene.  They usually code for proteins that stimulate cell division, inhibit cell differentiation and halt cell death, such as TK.  The Bcr-Abl1 proto-oncogene results in constantly activated or turned on (constitutively activated) TK.  It can be expressed in a single leukemic stem cell in the bone marrow, which results in enhanced activity of TK and clonal expansion of the abnormal cell that develops into leukaemia. 

Imatib tablets 100mg inhibits the activity of this abnormal Bcr-Abl1 protein TK in both CML and ALL, thereby preventing growth of the cancer cells without affecting growth of normal cells2.  Imatinib in Imatib tablets 100mg also inhibit TKs for other growth factors that cause cancers. These include the abnormal TK receptor for platelet-derived growth factor A and B (PDGFRA and PDGFRB) that are caused by gene rearrangements and are found in systemic mastocytosis (SM), chronic eosinophilic leukaemia (CEL), dermatofibrosarcoma protuberans (DFSP) and some cases of chronic myeloid leukaemia (CML)3, 4, 5. 

Another abnormal TK that Imatinib in Imatib tablets 100mg targets is the receptor for mast cell growth factor (KIT) caused by c-kit an oncogene found in gastrointestinal stromal tumour (GIST) and most cases of aggressive systemic mastocytosis (SM)6, 7.  Imatinib in Imatib tablets 100mg inhibits the action of these various abnormal TKs that are known to be involved in the development of several cancers, thereby blocking uncontrolled cell proliferation, restoring normal cell differentiation and apoptosis. 

This action of Imatinib in Imatib 100 is effective in reducing the growth of susceptible cancers, while having no effect on the growth of normal cells.

How to take Geftinat 250 mg?

use this drug in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Imatib 100mg Capsule is to be taken with food.

Geftinat 250 mg Contraindications

Hypersensitivity to Imatib Tablet is a contraindication. In addition, Imatib Tablet should not be used if you have the following conditions:

• Breastfeeding
• Hypersensitivity
• Levothyroxine
• Liver, kidney or heart problems
• Weight gain

Geftinat 250 mg Dosage

• Missed Dose:

Use the missed dose as soon as you remember. If it is almost time for the next scheduled dose, then the missed dose can be skipped. Contact your physician for further instructions if you miss more than one scheduled dose of this medicine.

• Overdose:

Contact your physician immediately if an overdose with this medicine is suspected. Symptoms may include nausea, vomiting, diarrhea, skin allergies, tiredness, fever, etc.

Geftinat 250 mg Side effects

• Chills
• Fever
• Swelling due to fluid retention
• Headache
• Blurred vision
• Sore throat
• Vomiting
• Nausea
• Lack of sleep
• Bone pain

Warnings:

instantly proceed to your nearest emergency division if you suffer an allergic reaction. Symptoms usually associated with such a reaction include difficulty breathing or swallowing, chest tightness, swelling, skin rashes, and hives.

Imatib is not always suitable for all patients. Always consult your health care provider prior to using this medication if you are pregnant, breastfeeding, trying to conceive, utilized any other medicine (prescription or non-prescription), using any herbal products or supplements, or if you have any allergies or other health problems.

The correct dosage and prescription commonly depend on the patient and the condition being treated. Do not adjust your dosage without the approval of your health care provider. This product is only for use as prescribed and instructed.

References:

Imatinib: MedlinePlus Drug Information [Internet]. Medlineplus.gov. 2017 [cited 13 September 2017]. Available from: https://medlineplus.gov/druginfo/meds/a606018.html

DailyMed: Imatinib Mesylate tablet, film coated [Internet]. Dailymed.nlm.nih.gov. 2017 [cited 13 September 2017]. Available from: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0291eca5-7a1d-4a79-30be-252224d96509

Imatinib mesylate [Internet]. Pubchem.ncbi.nlm.nih.gov. 2017 [cited 13 September 2017]. Available from: https://pubchem.ncbi.nlm.nih.gov/compound/123596