Afinitor Tablets
Everolimus
5mg
Novartis Pharma AG
| Pack size | 30's (10's Blister x 3) |
|---|---|
| Dispensing mode | POM |
| Source | SWITZERLAND |
| Agent | CITY MEDICAL STORE |
| Retail Price | 16083.50 AED |
Available as:
Indications
Afinitor Tablets is used for:
Breast cancer, Kidney cancer, Renal transplant, Liver transplant, Neuroendocrine tumors, Renal cell carcinoma, Astrocytoma, Renal angiomyolipoma,Tuberous sclerosis
Adult Dose
Oral
Breast Cancer, Renal Cell Carcinoma, Renal Angiomyolipomas with TSC, Advanced Neuroendocrine Tumors
10 mg once daily with or without food
Child Dose
Renal Dose
Administration
May be taken with or without food. Administer consistently with food or consistently without food.
Contra Indications
Patients with hypersensitivity to the active substance, to other rapamycin derivatives, or to any of the excipients. Hypersensitivity reactions manifested by symptoms including, but not limited to, anaphylaxis, dyspnea, flushing, chest pain, or angioedema (e.g., swelling of the airways or tongue, with or without respiratory impairment) have been observed with everolimus and other rapamycin derivatives
Precautions
Patients taking concomitant ACE inhibitor therapy may be at increased risk for angioedema
Interstitial lung disease/noninfectious pneumonitis; monitor for clinical symptoms or radiological changes; fatal cases have occurred; manage by dose reduction or discontinuation until symptoms resolve, and consider use of corticosteroids; pulmonary hypertension (including pulmonary arterial hypertension) as a secondary event reported
Elicits immunosuppressive effects and may increase risk for infections; some infections have been severe or fatal; monitor for signs and symptoms and treat promptly
Pneumocystis jiroveci pneumonia, some with a fatal outcome, reported; this may be associated with concomitant use of corticosteroids or other immunosuppressive agents
Mouth ulcers, stomatitis, and oral mucositis are common; management includes mouthwashes (without alcohol or peroxide) and topical treatments
May delay wound healing and increase wound-related complications (eg, dehiscence, wound infection, incisional hernia, lymphocele, and seroma)
Cases of renal failure (including acute renal failure), some fatal, have been observed
May cause angioedema and fluid accumulation
Decreases Hgb, lymphocytes, ANC, platelets; increases cholesterol, TG, glucose, creatinine
Elevations of serum creatinine, urinary protein, blood glucose, and lipids may occur; decreases in hemoglobin, neutrophils, and platelets may also occur; monitor renal function, blood glucose, lipids, and hematologic parameters prior to treatment and periodically thereafter
May impair male fertility
Child-Pugh Class C hepatic impairment
Avoid use of live vaccines during treatment and close contact with live vaccine recipients
Can cause fetal harm when administered to a pregnant woman; advise female patients of reproductive potential to use highly effective contraception while receiving everolimus and for up to 8 weeks after ending treatment.
Lactation: distribution into breast milk unknown; not recommended
Pregnancy-Lactation
Pregnancy
Based on animal studies and mechanism of action therapy can cause fetal harm when administered to pregnant woman; there are limited case reports of use in pregnant women; however, these reports are not sufficient to inform about risks of birth defects or miscarriage; advise pregnant women of potential risk to fetus
Contraception
Females
Advise female patients of reproductive potential to use effective contraception during treatment and for 8 weeks after last dose
Verify the pregnancy status of females of reproductive potential prior to starting treatment
Males
Based on findings in animal reproduction studies, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 4 weeks after last dose
Infertility
Females
Menstrual irregularities, secondary amenorrhea, and increases in luteinizing hormone (LH) and follicle stimulating hormone (FSH) occurred in female patients receiving therapy; based on these clinical findings and findings in animals, female fertility may be compromised by treatment with drug
Males
Based on clinical findings and findings in animals, treatment may impair fertility in male patients; cases of reversible azoospermia reported in male patients receiving therapy; in male rats, sperm motility, sperm count, plasma testosterone levels and fertility were diminished at exposures (AUC) similar to those in patients receiving a dose of 10 mg daily; the fertility index in rats increased when everolimus administration was stopped for a 10-13 week recovery
Lactation
There are no data on presence of everolimus in human milk, effects on breastfed infant or on milk production; drug and/or its metabolites passed into milk of lactating rats at a concentration 3.5 times higher than in maternal serum; because of potential for serious adverse reactions in breastfed infants from everolimus, advise lactating women not to breastfeed during treatment and for 2 weeks after last dose
Interactions
CYP3A4 inhibitors &/or inducers, CYP2D6 substrates w/ narrow therapeutic index, PgP inhibitors, rifampicin, ACE inhibitors, grapefruit juice & live vaccines.
Adverse Effects
Side effects of Everolimus :
>10%
Stomatitis (44%), Constipation (38%), Infections (37%), Asthenia (33%), Fatigue (31%), Cough (30%), Diarrhea (30%), Rash (29%), Anemia (26%), Nausea (26%), Anorexia (25%), Edema, peripheral (25-45%), Dyspnea (24%), Pyrexia (20%), Vomiting (20%), Headache (19%), Epistaxis (18%), Decreased lymphocytes, Grade 3 (16%), Increased glucose, Grade 3 (15%), Pneumonitis (14%), Pruritus (14%), Dry skin (13%), Decreased Hgb, Grade 3 (12%), Menstrual irregularities (11%)
1-10% (selected)
Dysgeusia (10%), Hypertension (4%), Hemorrhage (3%), Tachycardia (3%), CHF (1%)
Mechanism of Action
Everolimus, a proliferation signal inhibitor, prevents allograft rejection in rodent and nonhuman primate models of allotransplantation. It exerts its immunosuppressive effect by inhibiting the proliferation and thus, clonal expansion, of antigen-activated T cells which is driven by T cell-specific interleukins eg, interleukin-2 and interleukin-15. Everolimus inhibits an intracellular signaling pathway that normally leads to cell proliferation when triggered by the binding of these T cell growth factors to their receptors. The blockage of this signal by everolimus causes cells to be arrested at the G1 stage of the cell cycle.
At the molecular level, everolimus forms a complex with the cytoplasmic protein FKBP-12. In the presence of everolimus, the growth factor-stimulated phosphorylation of the p70 S6 kinase is inhibited. Since p70 S6 kinase phosphorylation is under the control of FRAP (also called m-TOR), this finding suggests that the everolimus-FKBP-12 complex binds to and thus, interferes with the function of FRAP. FRAP is a key regulatory protein which governs cell metabolism, growth and proliferation; disabling FRAP function thus explains the cell cycle arrest caused by everolimus.
Note
Afinitor 5mg Tablets manufactured by Novartis Pharma AG. Its generic name is Everolimus. Afinitor is availble in United Arab Emirates.
Farmaco UAE drug index information on Afinitor Tablets is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.