Afinitor 5mg
Afinitor 5mg belongs to anti-neoplastic agent; it comes under mTOR kinase inhibitor (single transduction inhibitor). Afinitor 5mg is an immunosuppressive macrolide.
Everolimus
Afinitor
5mg
Novartis
Used for
Breast cancer
patient who fail to respond the tablet letrozole or anastrozole therapy, would be treated with Afinitor. Afinitor 5mg is used in advanced stage of breast cancer.
Neuroendocrine tumors
Afinitor 5mg involved in the treatment of some neuroendocrine tumors like pancreatic, gastrointestinal or lung cancer.
Renal cell cancer
patient treating with Afinitor 5mg after the failure of treatment with Sunitinib or Sorafenib.
Afinitor 5mg also used in the condition of;
Heart, liver, kidney transplantation
Waldenström macroglobulinemia
Other carcinoid tumors.
Mechanism of action
Afinitor is prohibitor of mammalian target of rapamycin (mTOR), a serine threonine kinase.
Afinitor bind with intercellular protein (FKBP-12), leads to inhibitory complex formation with mTOR complex 1 (mTORC1) this leads to inhibition of mTOR kinase activity.
Afinitor decreased the effect of S6 ribosomal protein kinase (S6K1) and eukaryotic elongation factor 4E binding protein (4E-BP1) which are essential for protein synthesis.
mTOR inhibited by Afinitor lead to reduce cell multiplication and angiogenesis.
Pharmacokinetics
The peak plasma concentration of Afinitor reached within 1 to 2 hours after administration.
The blood plasma ratio of Afinitor occurs over the range of 5 to 5000ng/ml.
On oral administration, Afinitor is metabolized into six main metabolites;
Three monohydroxylated
Two hydrolytic ring opened product
Phosphatidylcholine conjugate of Afinitor.
Afinitor is a substrate of CYP3A4 and PgP.
Afinitor is mixed inhibitor of CYP2D6 substrate dextromethorphan
Afinitor inhibits the metabolism of CYP3A4.
The 80% of the drug eliminated through feces. The half-life time of drug Afinitor is approximately 30 hours.
Dosage and administration
The recommended dose of the Tablet Afinitor is 10mg should be taken as a single dose in all carcinogenic condition, except organ transplantation.
Organ transplant: 0.75mg orally twice daily.
Brain/intracranial tumor: 4.5mg/m2 orally once a day (for both pediatric and adult dose)
Hepatic impairment: dose reduced to 7.5mg once daily followed by 5mg as a single dose.
Afinitor is in tablet form. It should be administered orally at same time every day.
Afinitor should be taken with or without food.
Afinitor tablets should not crush or broken.
Over dosage
The over dosage of Afinitor 5mg 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.
SIDE EFFECTS
The side effects of Afinitor 5mg tablets are predicted by the terms of their onset, duration, and severity
Side effects of Afinitor 5mg is preventable and it is minimized:
Mouth sores,
Mucositis,
Stomatitis or esophagitis,
Infection,
Rash, itching or dry skin,
Fatigue,
Diarrhea,
Edema,
Stomach pain,
Nausea, vomiting,
Fever,
Weakness or asthenia,
Headache.
Blood test abnormalities
Hypercholesterolemia, High triglycerides, High blood sugar level, Low calcium, Low phosphate, Low blood counts, Liver problems, Kidney problems.
Less common
Cough, Loss appetite, Shortness of breath, Hypertension, Bleeding problems, Joint pain, Muscle pain, Loss of fertility.
Precautions
Before going to start the Afinitor 5mg therapy, doctor should consult with patient whether they are taking any medicines like:
Aspirin
Any kind of immunization or vaccine
Care should be taken in pregnancy condition.
Drug interaction
Some list of medications should not be taken with Tablet Afinitor, they will interact with Afinitor 5mgto produce serious ill:
Angiotensin converting enzyme inhibitors: Afinitor 5mg increases the adverse effect of ACE inhibitors.
Anti-diabetic agents
Anti-hepaciviral increase the serum concentration of Afinitor 5mg
Amphetamine/dextroamphetamine
Aspirin
Lorazepam
Amoxicillin/clavulanate
Sulfamethoxazole/trimethaprim
Vitamin D
Fish oil
Fluconazole
Atorvastatin
Paracetamol
Clopidogrel
Pantoprazole
Sorafenib
Sunitinib.
