ROLIMUS 5MG

ROLIMUS DESCRIPTION

Rolimus 5mg containing an active ingredient known as Everolimus which is intercedes with cancer cell growth and slows down its process.

Rolimus 5mg tablets are not used as curable medicine, which is used to slow their spreading in to the body.

ROLIMUS 5MG PRESCRIBING INFORMATION

Rolimus 5mg 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.

ROLIMUS 5MG 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 decreases the activity of effectors downstream, which may cause blockage of cell progression from G1 into S phase, subsequently causes cell growth arrest and apoptosis

Absorption

The peak plasma concentration time of Everolimus reaches within 1 to 2 hours.

The effect of food with Rolimus 5mg is given below; With heavy meal: Reduction of systemic exposure to Rolimus, and the peak blood plasma concentration by 54%.

Distribution

The blood plasma ratio of Rolimus 5mg with the range of 5 to 5000ng/ml is 17% to 73%. Rolimushuman 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 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 ROLIMUS

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 Rolimus is 4.5mg/m² orally as a single dose.

In pediatric

The usual pediatric dosage of Rolimus in brain or intracranial tumor is 4.5mg/m² should be taken orally as a single dose. 

Rolimus tablets should be administered with or without food.

OVER DOSAGE

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.

ROLIMUS 5MG 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

DRUG – DRUG INTERACTION

• Rolimus 5mg is metabolized hepatically, a substrate of CYP3A4.
• Rolimus 5mg combined with strong inhibitor of CYP3A4, or P-gp, leads to cause decreasing the efflux of Everolimus and increase the plasma concentration of Everolimus.
• Rolimus 5mg with strong CYP3A4 inducers, causes increasing the exposure of Everolimus.
• Co administration of Rolimus 5mg with cyclosporine causes increasing the AUC level of Everolimus frequently.
• Rolimus 5mg tablet is combined with ketaconazole or other CYP3A4 inhibitors causes increasing the plasma concentration and AUC of Everolimus.
• Concomitant of Rolimus 5mg with erythromycin causes increasing in AUC of Everolimus.
• Co administration of Rolimus 5mg with verapamil leads to increasing the plasma concentration of Everolimus.
• Co administration of Rolimus 5mg with Atorvastatin or pravastatin causes rhabdomyolysis, due to increasing concentration of lipid lowering agents.

CONTRAINDICATION

Some anaphylactic reaction occurs, if patients are contraindicated to the components present in the Rolimus 5mg tablets.

SAFETY MEASURES

Lymphomas

Increased exposure of skin cancers, patient may protect from UV light

Serious infections

Patients receiving Rolimus 5mg 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, Rolimus 5mg therapy should not be recommended.

Nephrotoxicity

Renal function should be monitored frequently; caution should be taken while using Rolimus 5mg in renal impaired patients.

Angioedema

This may have occurred in the patients receiving concomitantly Rolimus 5mg with Angiotensin converting enzyme agents

Hyperlipidemia

Patient getting Rolimus 5mg with lipid lowering drugs causes increasing in plasma concentration of these drugs causes hyperlipidemia

Interstitial lung disease: Occurred in Rolimus 5mgtherapy

Thrombocytopenia: Using Rolimus 5mg with cyclosporine causes thrombocytopenia

Outbreak of diabetes: Blood glucose level should be monitored

Embryo fetal toxicity: Causes fetal damage using Rolimus 5mg in pregnancy condition

Immunization: Using live vaccines in Rolimus 5mg therapy

Hereditary disorders: In the conditions like galactose intolerance, glucose-galactose malabsorption, Rolimus 5mg should not be used may results in diarrhea & malabsorption.

Interact with grape juice: Causes increasing blood levels of Everolimus; avoid these concomitants.

PREGNANCY AND LACTATION

Pregnancy category of Everolimus C

Rolimus 5mg is used only by the patients after knowing the benefits to the mother outweighs the risk to fetus.

Breast feeding should not be suggested

STORAGE AND HANDLING

Rolimus 5mg tablet should be kept at 25^oC

Keep the tablet away from moisture, heat and light

MISSED DOSE

In case of missed dose, patients must consult with medical practitioner and follow the instructions given by them.

On the other hand, the missed dose should be avoiding and follow the regular dosing schedule.

OVER DOSAGE

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.