AFINITOR 5MG |

EVEROLIMUS | MHP

Million Health Pharmaceuticals

DESCRIPTION
 Afinitor 5mg is a derivative of Rapamycin
(sirolimus) and works similarly to
Rapamycin as an mTOR (mammalian
target of rapamycin) inhibitor.
 It is normally used as an
immunosuppressant to prevent rejection
of organ transplants.
In a similar fashion to other mTOR
inhibitors
 AFINITOR 5MG |
EVEROLIMUS | MHP

Million Health Pharmaceuticals

PRESCRIBING INFORMATION

 Afinitor 5mg tablet are mainly indicated

for the treatment of Renal carcinoma.
 Afinitor 5mg tablet are mainly indicated
for the treatment of Breast carcinoma.
Afinitor 5mg tablet are mainly indicated
for the treatment of Brain carcinoma.
Afinitor 5mg is also used in various
advanced stage cancer in stomach,
intestines or pancreas.
MECHANISM OF ACTION

 Everolimus is an mTOR prohibitor, joints

at high compatibility to FK506 binding
protein 12, via producing drug complex
whichinhibits the specific of mTOR.
This inhibitiondecreases the activity of
effectors downstream, that may cause
blockage of cell progression from G1 into
S phase, subsequently causes cell growth
arrest and apoptosis
AFINITOR 5MG
PRODUCT DETAILS:

 Brand : Afinitor
Ingredients : Everolimus
Strength : 5mg
Manufactured : Novartis
Package : 10 tablets
 PHARMACOKINETICS
 ABSORPTION
The high plasma concentration time of
Everolimus is 1 to 2 hours.
The effect of food with Afinitor 5mg that with
heavy meal
 DISTRIBUTION
Afinitor 5mg 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 major route of elimination;

5% in urine; the parent compound has
been detected in urine or feces.
The half-life period of Everolimus is
relatively 30 hours
Brain carcinoma
DOSAGE MANAGEMENT

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

 In pediatric:
The usual pediatric dosage of Afinitor 5mg in brain or
intracranial tumor is 4.5mg/m2 should be taken orally
as a single dose.
PRECAUTIONS

 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
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

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

• Afinitor 5mg tablet interaction with strong

inhibitor of CYP3A4, or P-gp, leads to cause
decreasing the efflux of Everolimus and increase the
plasma concentration of Everolimus.
• Combination of Afinitor 5mg with verapamil leads
to increasing the plasma concentration of
Everolimus.
• Combination of Afinitor 5mg with Atorvastatin or
pravastatin causes rhabdomyolysis, due to increasing
concentration of lipid lowering agents.
• Afinitor 5mg tablet combination with strong
CYP3A4 inducers, causes increasing the exposure of
Everolimus.
CONTRAINDICATIONS

 Some anaphylactic reaction occurs, if

patients are contraindicated to the
components present in the Afinitor 5mg
tablet
CONTRAINDICATIONS

 PREGNANCY:
 Pregnancy category C Afinitor 5mg is
needed only by the patients after knowing
the benefits to the mother outweighs the
risk to fetus.
LACTATION:
 Breast feeding should not be suggested
STORAGE :
 Afinitor 5mg tablet should be kept at
25°C
CONTACT US:

 MOBILE NO:+91-9940472902
 EMAIL: millionhealthpharmaceuticals@gmail.
cOm
 WEBSITE
URL:https://millionpharma.com/afinitor-5-
mg.php