Adults

For kidney transplant prophylaxis: Initial dose 0.75 mg orally twice daily, adjusted based on therapeutic drug monitoring (TDM). For heart transplant prophylaxis: Initial dose 1.5 mg orally twice daily, adjusted based on TDM. Doses for other indications vary.

Elderly

No specific dose adjustment is required for elderly patients, but careful monitoring is recommended due to potential age-related decline in renal or hepatic function.

Renal_impairment

No dose adjustment is required in patients with renal impairment. However, for patients on dialysis, dosing should be carefully considered.

Onset

Immunosuppressive effects require steady-state concentrations, typically achieved within 2-4 days of consistent dosing.

Excretion

Primarily eliminated via feces (approximately 80%), with a small amount excreted in urine (approximately 5%).

Half life

Approximately 28-35 hours.

Absorption

Rapidly absorbed after oral administration, with peak concentrations (Cmax) achieved within 1-2 hours. Bioavailability is approximately 10-20%.

Metabolism

Extensively metabolized in the liver and intestinal wall by cytochrome P450 3A4 (CYP3A4) and is a substrate for P-glycoprotein (P-gp).

Live vaccines

Avoid during Certican treatment due to risk of disseminated infection.

Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital, St. John's Wort)

Can significantly decrease everolimus blood levels, potentially reducing efficacy. Avoid concomitant use.

Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, grapefruit juice)

Can significantly increase everolimus blood levels, increasing risk of adverse effects. Avoid concomitant use or reduce everolimus dose with careful monitoring.