Description

Everolimus Tablets 0.25 mg

Everolimus Tablets 0.25 mg is an immunosuppressive and anti-cancer medication used primarily for preventing organ transplant rejection and in the treatment of various types of cancer, depending on the indication and strength. The 0.25 mg dose is primarily used to maintain organ transplant health, especially in kidney and liver transplant patients, and is usually taken in combination with other immunosuppressants such as tacrolimus or cyclosporine.

Everolimus is classified as an mTOR inhibitor (mammalian target of rapamycin inhibitor). It works by blocking signals essential for T-cell activation and proliferation, thereby preventing the immune system from attacking transplanted organs. It also has anti-angiogenic effects that make it useful in select cancers by limiting blood supply to tumors.

Brand Reference: Certican (for immunosuppressive therapy), also known as Afinitor (for oncology)
Generic name: Everolimus
Strength: 0.25 mg
Form: Oral tablet
Schedule: Prescription-only

Indications

Everolimus 0.25 mg is used for:

• Prevention of organ transplant rejection (especially kidney or liver)
• Used in kidney transplant patients at low-to-moderate immunological risk in combination with basiliximab induction, cyclosporine, and corticosteroids
• May be used in liver transplant patients with appropriate dose adjustment
• NOT typically used for cancer at this strength (higher strengths like 5 mg or 10 mg are used in oncology)

Mechanism of Action

Everolimus inhibits the mTOR (mammalian target of rapamycin) pathway, which is critical in regulating cell growth, proliferation, and survival:

• Suppression of T-cell activation and proliferation
• Prevention of antibody-mediated immune responses
• Inhibition of smooth muscle cell proliferation
• Reduction in the risk of chronic allograft nephropathy

Dosage and Administration

• Strength: 0.25 mg
• Route: Oral
• Dosage: Varies depending on patient weight, transplant type (kidney or liver), and whether it’s used in combination with cyclosporine or tacrolimus
• Often combined with calcineurin inhibitors (CNIs) and steroids in transplant protocols
• Frequency: Usually taken twice daily
• Instructions:
  • Take consistently either with food or without food
  • Swallow tablet whole with water
  • Ensure timing of dose is 12 hours apart for consistency in blood levels

Blood concentration of Everolimus should be monitored regularly, especially after dose changes.

Composition

• Active Ingredient: Everolimus 0.25 mg
• Excipients: Lactose monohydrate, magnesium stearate, hypromellose, crospovidone, etc. (may vary by manufacturer)
• Packaging: Typically available in blister packs or bottles – 10, 30, or 60 tablets

Common Side Effects

• Mouth ulcers (stomatitis)
• High blood pressure (hypertension)
• Elevated blood sugar (hyperglycemia)
• Increased cholesterol or triglycerides
• Delayed wound healing
• Risk of infections due to immune suppression
• Anemia or low white blood cell counts

Serious Adverse Effects

• Renal dysfunction (especially with concomitant cyclosporine)
• Non-infectious pneumonitis
• Severe infections (bacterial, viral, fungal)
• Liver enzyme elevations
• Hypersensitivity reactions
• Increased susceptibility to malignancies as with other immunosuppressants

Warnings and Precautions

• Pregnancy: Not recommended; use effective contraceptive measures
• Breastfeeding: Not recommended during treatment
• Requires regular blood monitoring for drug levels, renal and liver function
• Risk of bone marrow suppression
• Ensure appropriate vaccination history before starting therapy
• Avoid grapefruit juice, it may interfere with metabolism of the drug

Drug Interactions

• Drugs that affect the CYP3A4 enzyme pathway (like ketoconazole, erythromycin, or rifampin)
• NSAIDs may increase risk of kidney dysfunction when used with CNI + Everolimus
• Avoid concurrent use with strong immunosuppressants unless indicated

Storage and Handling

• Store at room temperature: between 15°C and 30°C
• Protect from light and humidity
• Keep in the original packaging
• Keep out of reach of children and pets

Frequently Asked Questions (FAQs)

1. What is Everolimus 0.25 mg used for?
It is used to prevent organ transplant rejection, especially in kidney and liver transplant patients.

2. Is Everolimus a chemotherapy drug?
Not at this strength. Higher doses are used in oncology. The 0.25 mg dose is strictly for immunosuppression.

3. Can I take Everolimus with food?
Yes, but it should be taken consistently with or without food. Avoid switching between fed and fasted states.

4. How often should Everolimus be taken?
Doses are usually taken twice daily, approximately 12 hours apart.

5. How is the dose of Everolimus determined?
The dose is based on body weight, transplant type, co-administered drugs, and therapeutic drug monitoring levels.

6. Can Everolimus cause kidney problems?
Yes, especially when used with cyclosporine. Renal function should be monitored regularly.

7. What precautions should women of childbearing age take?
They should use effective contraception during treatment and for at least 8 weeks after the last dose.

8. Can Everolimus be used in children?
Yes, but only in pediatric transplant settings under medical supervision.

9. Should alcohol be avoided?
Alcohol may exacerbate liver issues, so discuss alcohol use with your doctor.

10. Is Everolimus a steroid?
No, it is not a steroid. It is an mTOR inhibitor used for immune system suppression.