Afinitor 10mg containing an active ingredient known as Everolimus which is intercedes with cancer cell growth and slows down its process. Afinitor 10mg tablets are not used as curable medicine, which is used to slow their spreading in to the body.
Afinitor 10mg PRESCRIBING INFORMATION
Afinitor 10mg 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.
Afinitor 10mg 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
The peak plasma concentration time of Everolimus reaches within 1 to 2 hours. The effect of food with Afinitor 10mg is given below; With heavy meal: Reduction of systemic exposure to Afinitor 10mg 10mg, and the peak blood plasma concentration by 54%.
The blood plasma ratio of Afinitor 10mg with the range of 5 to 5000mg/ml is 17% to 73%.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 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.
DOSAGE REGIMEN AND ADMINISTRATION OF AFINITOR
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 Afinitor is 4.5mg/m2 orally as a single dose.
The usual pediatric dosage of Afinitor in brain or intracranial tumor is 4.5mg/m2 should be taken orally as a single dose. Afinitor tablets should be administered with or without food.
Afinitor 10mg 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
Increased exposure of skin cancers, patient may protect from UV light
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:
In liver transplant patients, Afinitor 10mg therapy should not be recommended.
Renal function should be monitored frequently; caution should be taken while using Afinitor 10mg in renal impaired patients.
This may have occurred in the patients receiving concomitantly Afinitor 10mg with Angiotensin converting enzyme agents
Patient getting Afinitor 10mg with lipid lowering drugs causes increasing in plasma concentration of these drugs causes hyperlipidaemia
Interstitial lung disease:
Occurred in Afinitor 10mg therapy
Using Afinitor 10mg with cyclosporine causes thrombocytopenia
Outbreak of diabetes:
Blood glucose level should be monitored
Embryo fetal toxicity:
Causes fetal damage using Afinitor 10mg in pregnancy condition
Using live vaccines in Afinitor 10mg therapy
In the conditions like galactose intolerance, glucose-galactose malabsorption, Afinitor 10mg should not be used may results in diarrhea & malabsorption.
Interact with grape juice:
Causes increasing blood levels of Everolimus; avoid these concomitants.