Trade name : Afinitor
Active component : Everolimus
Strength : 5mg
Manufactured by : Novartis
Pack : 10 tablets in a strip
Afinitor 5mg is belongs to class of anti-cancer drugs.
Afinitor 5mg contains of an active compound known as Everolimus which is interfere with development of cancer cell and process is slows down.
Afinitor 5mg tablets is not a curable medication, which is helps to slow their spreading into the body.
The drug Afinitor 5mg is mainly used for the treatment of following disease
• kidney carcinoma
• Breast carcinoma
• Brain carcinoma
Afinitor 5mg is also used to treat in various advanced stage cancer in stomach, intestines or pancreas.
CLINICAL PHARMACOLOGY OF AFINITOR
Everolimus is an prohibitor of mTOR, links at peak compatibility to FK506 binding protein 12, through producing drug complex which prevents the productive of mTOR. This inhibition reduces the activity of effectors downstream, which may lead to stoppage of cell progression from G1 into S phase, finally causes cell growth arrest and apoptosis.Afinitor also prohibits the expression of hypoxia-inducible factor, causing to a reduces in the expression of vascular endothelial growth factor. The results of everolimus prevention of mTOR is a reduction in cell multiplication, angiogenesis, and glucose uptake.
The time to peak plasma concentration of Afinitor 5mg occurs between 1 to 2 hours.
The drug Afinitor 5mg has Albumin human plasma protein bound of 74%.
In hepatic Afinitor 5mg metabolism is take place, which is a substrate of CYP3A4.
The Afinitor 5mg metabolism will occur through 3 processes;
• Three monohydroxylated metabolite,
• Two hydrolytic rings opened products,
• Phosphatidylcholine conjugate of Everolimus.
The drug excretion primarily through 5% in urine; the parent compound has been detected in urine or feces. The drug half-life period is 30 hours
Afinitor 5mg tablets should be given with or without food.
Dosage regimen of Afinitor:
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 as a single dose. is 4.5mg/m2 given orally
The pediatric dosage of Afinitor as a single dose in brain or intracranial tumor is 4.5mg/m2 should be given orally.
Embryo fetal toxicity:
using Afinitor 5mg in pregnancy condition Causes fetal damage
Developed hazard of skin cancers, patient may protect from UV light
Patients getting Afinitor 5mg have severe risk of achieve various infections related to bacteria, virus, and fungi.
Hepatic artery thrombosis:Afinitor 5mg therapy should not be recommended in in liver transplant patients.
while using Afinitor the conditions occurs like galactose intolerance, glucose-galactose malabsorption, Afinitor 5mg should not be used may results in diarrhea & malabsorption.
avoid these concomitant use with grape juice Causes increasing blood levels of Everolimus
Nephrotoxicity:While using Afinitor 5mg in renal impaired patients Renal function should be monitored frequently; drug use with caution Angioedema:
While patients receiving concomitantly Afinitor 5mg with Angiotensin converting enzyme agents will cause angioedema
Interstitial lung disease:
In Afinitor 5mg therapy interstitial lung disease occur
Blood glucose level should be monitored
Drug – Drug interaction
Interaction of Afinitor 5mg with strong inhibitor of CYP3A4, or P-gp, cause reducing the efflux of Everolimus and high plasma concentration of Everolimus.
Concomitant use of Afinitor 5mg with strong CYP3A4 inducers, will increasing the disclosure of Everolimus.
Interaction of Afinitor 5mg with cyclosporine will increasing the AUC level of Everolimus frequently.
Interaction of ketoconazole with Afinitor 5mg tablet or other CYP3A4 inhibitors will increasing the plasma concentration and AUC of Everolimus.
Combination of Afinitor 5mg with verapamil leads to increasing the plasma concentration of Everolimus.
Interaction of Afinitor 5mg with Atorvastatin or pravastatin leads to rhabdomyolysis, due to increasing concentration of lipid lowering agents.
When Afinitor 5mg combination with rifampicin will reduces the AUC of Everolimus
The over dosage of Everolimus is limited, If over dosage occurs patient must be provide with supportive measures. And monitor evidence of toxicity in Everolimus over dosage
If the patients missed dose, patients must consult with medical practitioner and follow the instructions given by them.
Or missed dose should be avoid and follow the regular dosing schedule.
• Hypersensitivity reactions
• Lymphomas & other malignancy
• Male infertility
• New commencement of diabetes
• Serious infections
• Kidney graft thrombosis
• Hepatic artery thrombosis
• Interstitial lung disease.