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Evertor 5mg tablets are mainly indicated for the treatment of Renal carcinoma. Evertor 5mg tablets are mainly indicated for the treatment of Breast carcinoma. Evertor 5mg tablets are mainly indicated for the treatment of Brain carcinoma. Evertor 5mg is also used in various advanced stage cancer in stomach, intestines or pancreas.

Everolimus is an mTOR prohibitor, joints at high compatibility to FK506 binding protein 12, via producing drug complex which inhibits the specific of mTOR. This inhibition decreases the activity of effectors downstream, that may cause blockage of cell progression from G1 into S phase, subsequently causes cell growth arrest and apoptosis



ADME properties

Absorption

The high plasma concentration time of Everolimus is 1 to 2 hours. The effect of food with Evertor 5mg that with heavy meal: Reduction of systemic exposure to Evertor 5mg 10mg, and the high blood plasma concentration by 54%.

Distribution

Evertor 5mg human plasma protein bound with the range of 74%.

Metabolism

The metabolism of Everolimus is occurred in liver, which is a substrate of CYP3A4. The metabolites of Everolimus; Three monohydroxylated metabolite, Two hydrolytic rings opened products, & Phosphatidylcholine conjugate of Everolimus.

Excretion

The major route of elimination; 5% in urine; the parent compound has been detected in urine or feces. The half-life period of Everolimus is relatively 30 hours

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Brand : Evertor
Ingredients : Everolimus
Strength : 5mg
Manufactured : Biocon
Package : 10 tablets in 1 strips

DOSAGE REGIMEN AND ADMINISTRATION OF Evertor

In breast cancer, renal cell cancer, pancreatic cancer, Neuro endocrine cancer: The prescribed dosage is 10mg should be taken as a single dose. In Brain or intracranial cancer: The prescribed dosage of Evertor is 4.5mg/m2 orally as a single dose. In pediatric: The usual pediatric dosage of Evertor in brain or intracranial tumor is 4.5mg/m2 should be taken orally as a single dose. Evertor tablets should be administered with or without food.

OVERDOSE

The over dosage of Everolimus is rarely occur, in case of over dosage patient must be provide with supportive measures. The acute toxicity of Everolimus over dosage should be monitored.

Evertor 5MG CAUSED SIDE EFFECTS

Hypersensitivity reactions, Lymphomas & other malignancy, Serious infections, Kidney graft thrombosis, Hepatic artery thrombosis, Nephrotoxicity, Hyperlipemia, Angioedema, Interstitial lung disease, Thrombocytopenia, Male infertility, Proteinuria, New commencement of diabetes

SAFETY MEASURES
Lymphomas

Increased exposure of skin cancers, patient may protect from UV light

Serious infections

Patients receiving Evertor 5mg have high risk of acquiring various infections related to bacteria, virus, and fungi. Anti-microbial agents are preferred for the suspected patients.

Hepatic artery thrombosis

In liver transplant patients, Evertor 5mg therapy should not be recommended.

Nephrotoxicity

Renal function should be monitored frequently; caution should be taken while using Evertor 5mg in renal impaired patients.

Angioedema

This may have occurred in the patients receiving concomitantly Evertor 5mg with Angiotensin converting enzyme agents

Hyperlipidemia

Patient getting Evertor 5mg with lipid lowering drugs causes increasing in plasma concentration of these drugs causes hyperlipidemia

Interstitial lung disease

Occurred in Evertor 5mg therapy

Interact with grape juice

Causes increasing blood levels of Everolimus; avoid these concomitants.



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DRUG – DRUG INTERACTION

Evertor 5mg interaction with strong inhibitor of CYP3A4, or P-gp, leads to cause decreasing the efflux of Everolimus and increase the plasma concentration of Everolimus. Combination of Evertor 5mg with verapamil leads to increasing the plasma concentration of Everolimus.

Combination of Evertor 5mg with Atorvastatin or pravastatin causes rhabdomyolysis, due to increasing concentration of lipid lowering agents. Evertor 5mg combination with strong CYP3A4 inducers, causes increasing the exposure of Everolimus.

Concomitant use of Evertor 5mg with cyclosporine causes increasing the AUC level of Everolimus frequently. Evertor 5mg tablet is interaction with ketoconazole or other CYP3A4 inhibitors causes increasing the plasma concentration and AUC of Everolimus. Concomitant use with erythromycin causes increasing in AUC of Everolimus.

Contraindication

Some anaphylactic reaction occurs, if patients are contraindicated to the components present in the Evertor 5mg tablets.


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