Working hours:
Mon-Fri: 9 a.m.- 6 p.m.
Call me back

Afinitor 5mg (Everolimus)

Rating:
Availability:
In stock
Quantity:
+
0,00 $
Shipping methods

New Post

Other transport services

Courier in Kiev

Pickup

Payment methods

Cash

Non-cash transfer

Privat 24

WebMoney

AFINITOR 5MG

AFINITOR DESCRIPTION

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

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

AFINITOR 5MG PRESCRIBING INFORMATION

Afinitor 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.

AFINITOR 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 Afinitor is given below; With heavy meal: Reduction of systemic exposure to Afinitor, and the peak blood plasma concentration by 54%.

Distribution

The blood plasma ratio of Afinitor with the range of 5 to 5000ng/ml is 17% to 73%. Afinitor human 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 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.

In pediatric:

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.

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.

AFINITOR 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

  • Afinitor 5mg is metabolized hepatically, a substrate of CYP3A4.
  • Afinitor 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.
  • Afinitor 5mg with strong CYP3A4 inducers, causes increasing the exposure of Everolimus.
  • Co administration of Afinitor 5mg with cyclosporine causes increasing the AUC level of Everolimus frequently.
  • Afinitor 5mg tablet is combined with ketaconazole or other CYP3A4 inhibitors causes increasing the plasma concentration and AUC of Everolimus.
  • Concomitant of Afinitor 5mg with erythromycin causes increasing in AUC of Everolimus.
  • Co administration of Afinitor 5mg with verapamil leads to increasing the plasma concentration of Everolimus.
  • Co administration of Afinitor 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 Afinitor 5mg tablets.

SAFETY MEASURES

Lymphomas

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

Serious infections

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

Nephrotoxicity

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

Angioedema

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

Hyperlipidemia

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

Interstitial lung disease

Occurred in Afinitor 5mg therapy

Thrombocytopenia

Using Afinitor 5mg with cyclosporine causes thrombocytopenia

Outbreak of diabetes

Blood glucose level should be monitored

Embryo fetal toxicity

Causes fetal damage using Afinitor 5mg in pregnancy condition

Immunization

Using live vaccines in Afinitor 5mg therapy

Hereditary disorders

In the conditions like galactose intolerance, glucose-galactose malabsorption, Afinitor 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

Afinitor 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

Afinitor 5mg tablet should be kept at 25oC

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.

  • Trade name Afinitor 5mg
  • Substance Everolimus
  • Manufacturer Novartis India Ltd
  • Packaging 10 tablets
  • Country of origin India
No comments yet
Write a comment
Name*
Email
Enter your comment*
35 + ? = 38
Enter Captcha*
Recommend