Evertor 5mg tablets | Everolimus | MHP
EVERTOR 5MG
DESCRIPITION:
Evertor 5mg is a derivative of Rapamycin (sirolimus) and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor.It is normally used as an immunosuppressant to prevent rejection of organ transplants.
In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein.
PRESCRIBING INFORMATION
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
MECHANISM OF ACTION
Everolimus is an mTOR prohibitor, joints at high compatibility to FK506 binding protein 12, via producing drug complex whichinhibits 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
PRODUCT DETAILS
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| EVERTOR 5Mg |
Ingredients : Everolimus
Strength : 5MG
Manufactured : Biocon Pharma
Package : 10 tablets
PHARMACOKINETICS
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 5mg10mg, and the high blood plasma concentration by 54%.
DISTRIBUTION
Evertor 5mg human plasma protein bound with the range of 74%.80 ml/kgMETABOLISM
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
DOSAGE MANAGEMENT
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.
PRECAUTIONS
Lymphomas: Increased exposure of skin cancers, patient may protect from UV lightSerious 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.
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.
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.
CONTRAINDICATIONS
Some anaphylactic reaction occurs, if patients are contraindicated to the components present in the Evertor 5mg tablets.PREGNANCY:
Pregnancy category C Evertor 5mg is needed only by the patients after knowing the benefits to the mother outweighs the risk to fetus.
LACTATION:
Breast feeding should not be suggested
STORAGE :
Evertor 5mg tablet should be kept at 25°C
Keep the tablet away from moisture, heat and light
Dispense only in original container
Dispense only in original container
MISSED DOSE:
If patient failed to take a single dose, patients must consult with medical practitioner and follow the instructions given by them.
Or the missed dose should be avoiding and follow the regular dosing schedule.
OVERDOSAGE:
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.
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