Evertor

Discount 355.00 USD
BRAND :  EVERTOR PRICE :  1200$ STRENGTH : 10MG ACTIVE :  EVERTOR-EVEROLIMUS-10MG COMPANY NAME :  BIOCON TABLETS :  10 TABLETS read more

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Drug profile;

Evertor containing an active ingredient known as Everolimus which is intercedes with cancer cell growth and slows down its process.

Evertor tablets are not used as curable medicine, which is used to slow their spreading in to the body.

 

Trade name: Evertor

Active component: Everolimus

Strength: 10MG

Mfg: Biocon

Pack: 10 tablets in a strip

Category: Anti-neoplastic drug

 

Evertor prescribing information;

Evertor tablets are mainly indicated in;

Renal carcinoma

Breast carcinoma

Brain carcinoma

Everolimus is also used in various advanced stage cancer in stomach, intestines or pancreas.

 

Evertor mechanism;

Everolimus is an mTOR prohibitor, binds at high compatibility to FK506 binding protein 12, through producing drug complex that prohibits the effective of mTOR.

This prohibition decrease the activity of effectors downstream, which may causes blockage of cell progression from G1 into S phase, subsequently causes cell growth arrest and apoptosis

 

Absorption

The peak plasma concentration time of Everolimus reaches within 1 to 2 hours.

The effect of food with Evertor is given below;

With heavy meal: Reduction of systemic exposure to Evertor 10mg, and the peak blood plasma concentration by 54%.

 

Distribution

The blood plasma ratio of Evertor with the range of 5 to 5000ng/ml is 17% to 73%.

Evertor 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 terminal half life period of Everolimus is relatively 30 hours

The major route of elimination;

5% in urine; the parent compound has been detected in urine or feces.

 

When to take the drug Evertor;

Evertor tablets should be administered with or without food.

 

Dosage regimen of Evertor;

In breast cancer, renal cell cancer, pancreatic cancer, Neuro endocrine cancer:

The recommended dosage is 10mg should be taken as a single dose.

In Brain or intracranial cancer:

The recommended 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 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

 

Drug – Drug interaction;

Evertor is metabolized hepatically, a substrate of CYP3A4.

Evertor combined with strong inhibitor of CYP3A4, or P-gp, leads to cause decreasing the efflux of Everolimus and increase the plasma concentration of Everolimus.

Evertor with strong CYP3A4 inducers, causes increasing the exposure of Everolimus.

Co administration of Evertor with cyclosporine causes increasing the AUC level of Everolimus frequently.

Evertor tablet is combined with ketaconazole or other CYP3A4 inhibitors causes increasing the plasma concentration and AUC of Everolimus.

Concomitant of Evertor with erythromycin causes increasing in AUC of Everolimus.

Co administration of Evertor with verapamil leads to increasing the plasma concentration of Everolimus.

Co administration of Evertor with Atorvastatin or pravastatin causes rhabdomyolysis, due ti increasing concentration of lipid lowering agents.

Evertor with rifampicin causes decreasing the AUC of Everolimus

Moderate inhibitors of CYP3A4 & P-gp coadminstered with Evertor leads to cause increasing the plasma concentration of Everolimus.

Octreotide is co administered with Evertor causes increasing the Cmin value of Octreotide.

 

Food drug interaction;

Grape fruit juice may elevate the blood levels and effect of Everolimus.

Patients, who are receiving Evertor therapy, should not intake the grape fruit or grape fruit juice.

Orange fruit is not conventionally to interact.

 

Possible contraindication

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

 

Safety measures;

Lymphomas

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

Serious infections

Patients receiving Evertor 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 therapy should not be recommended.

Nephrotoxicity

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

Angioedema

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

Hyperlipidaemia

Patient getting Evertor with lipid lowering drugs causes increasing in plasma concentration of these drugs causes hyperlipidaemia

Interstitial lung disease: Occurred in Evertor therapy

Thrombocytopenia: Using Evertor with cyclosporine causes thrombocytopenia

Outbreak of diabetes: Blood glucose level should be monitored

Embryo fetal toxicity: Causes fetal damage using Evertor in pregnancy condition

Immunization: Using live vaccines in Evertor therapy

Hereditary disorders: In the conditions like galactose intolerance, glucose-galactose malabsorption, Evertor should not be used may results in diarrhea & malabsorption.

Interact with grape juice: Causes increasing blood levels of Everolimus; avoid these concomitant.

 

Pregnancy and lactation;

Pregnancy category of Everolimus C

Evertor is used only by the patients after knowing the benefits to the mother outweighs the risk to fetus.

Breast feeding should not be suggested

 

Storage and handling;

Evertor tablet should be kept at 25oC

Keep the tablet away from moisture, heat and light

 

Missed dose;

In case of missed dose, patients must consult with medical practitioner and follow the instructions given by them.

On the other hand the missed dose should be avoid and follow the regular dosing schedule.

 

Over dosage;

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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