EVEROLIMUS 10MG[AFFINITOR 10MG
DESCRIPTION
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| Affinitor 10mg |
Afinitor 10mg 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.
PRESCRIBE INFORMATION
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| Affinitor 10mg |
Afinitor 10mg tablets are mainly indicated for the treatment of Renal carcinoma.
Afinitor 10mg tablets are mainly indicated for the treatment of Breast carcinoma.
Afinitor 10mg tablets are mainly indicated for the treatment of Brain carcinoma.
Afinitor 10mg tablet is also used in various advanced stage cancer in stomach, intestines or pancreas.
MECHANISM OF ACTION
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| Affinitor 10mg |
Everolimus is an mTOR prohibitor, joints at high compatibility to FK506 binding protein 12, via producing drug complex whichinhibits the specific of mTOR.
This inhibitiondecreases the activity of effectors downstream, that may cause blockage of cell progression from G1 into S phase, subsequently causes cell growth arrest and apoptosis
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| Affinitor 10mg |
PROPERTIES
Ingredients : Everolimus
Strength : 10mg
Package : 10 tablets
The high plasma concentration time of Everolimus is 1 to 2 hours.
The effect of food with Afinitor 10mg that with heavy meal: Reduction of systemic exposure to Afinitor 5mg 10mg, and the high blood plasma concentration by 54%.
Afinitor 10mg human plasma protein bound with the range of 74%.
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.
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
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 Afinitor is 4.5mg/m2 orally as a single dose.
In pediatric:
The usual pediatric dosage of Afinitor in brain or intracranial tumor is 4.5mg/m2 should be taken orally as a single dose.
Afinitor 10mg tablet should be administered with or without food.
Increased exposure of skin cancers, patient may protect from UV light
In liver transplant patients, Afinitor 10mg therapy should not be recommended.
Patient getting Afinitor 10mg tablet with lipid lowering drugs causes increasing in plasma concentration of these drugs causes hyperlipidemia
• 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 .
Pregnancy category C Afinitor 10mg is needed only by the patients after knowing the benefits to the mother outweighs the risk to fetus.
Keep the tablet away from moisture, heat and light
Dispense only in original container
Or the missed dose should be avoiding and follow the regular dosing schedule.
EMAIL : millionhealthpharmaceuticals@gmail.com
WEBSITE : https://millionpharma.com/everolimus-10mg.php
PHARMACOKINETICS
ABSORPTION
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| Affinitor 10mg |
The effect of food with Afinitor 10mg that with heavy meal: Reduction of systemic exposure to Afinitor 5mg 10mg, and the high blood plasma concentration by 54%.
DISTRIBUTION
Afinitor 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 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
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| Affinitor 10mg |
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 Afinitor is 4.5mg/m2 orally as a single dose.
In pediatric:
The usual pediatric dosage of Afinitor in brain or intracranial tumor is 4.5mg/m2 should be taken orally as a single dose.
Afinitor 10mg tablet should be administered with or without food.
PRECAUTIONS
Lymphomas:
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| Affinitor 10mg |
Serious infections:
Patients receiving Afinitor 10mg 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:
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| Affinitor 10mg |
Nephrotoxicity:
Renal function should be monitored frequently; caution should be taken while using Afinitor 10mg in renal impaired patients.Angioedema:
This may have occurred in the patients receiving concomitantly Afinitor 10mg with Angiotensin converting enzyme agentsHyperlipidemia:
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| Affinitor 10mg |
Interstitial lung disease:
Occurred in Afinitor 10mg therapyInteract 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 .
PREGNANCY:
Pregnancy category C Afinitor 10mg is needed only by the patients after knowing the benefits to the mother outweighs the risk to fetus.
LACTATION:
Breast feeding should not be suggestedSTORAGE :
Afinitor 10mg tablet should be kept at 25°CKeep the tablet away from moisture, heat and light
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.CONTACT US
PHONE NO : +91-9940472902EMAIL : millionhealthpharmaceuticals@gmail.com
WEBSITE : https://millionpharma.com/everolimus-10mg.php
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