Uploaded on Jul 24, 2019
Evertor 10mg
Evertor 10mg
Evertor 10mg - Everolimus Biocon Tablets
Uses, Dose, Side Effects, Price india
MILLION HEALTH
PHARMACEUTICALS
Drug profile
• Evertor 10mg containing an active ingredient
known as Everolimus which is intercedes with
cancer cell growth and slows down its process.
Evertor 10mg 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
PRODUCT DETAILS
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 10mg tablet
with the range of 5 to 5000ng/ml is 17% to 73%.
Evertor 10mg 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 10mg
Evertor 10mg 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 10mg is 4.5mg/m2 orally as a
single dose.
In pediatric:
The usual pediatric dosage of Evertor 10mg tablet 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 10mg 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 10mg tablet 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.
Drug – Drug interaction
• 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 10mg 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 10mg tablet 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 10mg
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 10mg 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 10mg tablet 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 10mg therapy
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 10mg 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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