Rapact 10mg
Rapact 10mg belongs to anti-neoplastic agent; it comes under mTOR kinase inhibitor (single transduction inhibitor). Rapact 10mg is an immunosuppressive macrolide.
Everolimus
Rapact
10mg
Natco Pharma
Used for
Breast cancer
patient who fail to respond the tablet letrozole or anastrozole therapy, would be treated with Rapact. Rapact 10mg is used in advanced stage of breast cancer.
Neuroendocrine tumors
Rapact 10mg involved in the treatment of some neuroendocrine tumors like pancreatic, gastrointestinal or lung cancer.
Renal cell cancer
patient treating with Rapact 10mg after the failure of treatment with Sunitinib or Sorafenib.
Rapact 10mg also used in the condition of;
Heart, liver, kidney transplantation
Waldenström macroglobulinemia
Other carcinoid tumors.
Mechanism of action
Rapact is prohibitor of mammalian target of rapamycin (mTOR), a serine threonine kinase.
Rapact bind with intercellular protein (FKBP-12), leads to inhibitory complex formation with mTOR complex 1 (mTORC1) this leads to inhibition of mTOR kinase activity.
Rapact 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 Rapact lead to reduce cell multiplication and angiogenesis.
Pharmacokinetics
The peak plasma concentration of Rapact reached within 1 to 2 hours after administration.
The blood plasma ratio of Rapact occurs over the range of 5 to 5000ng/ml.
On oral administration, Rapact is metabolized into six main metabolites;
Three monohydroxylated
Two hydrolytic ring opened product
Phosphatidylcholine conjugate of Rapact.
Rapact is a substrate of CYP3A4 and PgP.
Rapact is mixed inhibitor of CYP2D6 substrate dextromethorphan
Rapact inhibits the metabolism of CYP3A4.
The 80% of the drug eliminated through feces. The half-life time of drug Rapact is approximately 30 hours.
Dosage and administration
The recommended dose of the Tablet Rapact 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.
Rapact is in tablet form. It should be administered orally at same time every day.
Rapact should be taken with or without food.
Rapact tablets should not crush or broken.
Over dosage
The over dosage of Rapact 10mg 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 Rapact 10mg tablets are predicted by the terms of their onset, duration, and severity
Side effects of Rapact 10mg 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 Rapact 10mg 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 Rapact, they will interact with Rapact 10mg to produce serious ill:
Angiotensin converting enzyme inhibitors: Rapact 10mg increases the adverse effect of ACE inhibitors.
Anti-diabetic agents
Anti-hepaciviral increase the serum concentration of Rapact 10mg
Amphetamine/dextroamphetamine
Aspirin
Lorazepam
Amoxicillin/clavulanate
Sulfamethoxazole/trimethaprim
Vitamin D
Fish oil
Fluconazole
Atorvastatin
Paracetamol
Clopidogrel
Pantoprazole
Sorafenib
Sunitinib.
