Zimilast Mechanism of Action

Pharmacology: Adults: Intravenous infusion of Zimilast over 20 min results in peak plasma levels of imipenem antimicrobial activity that range from 14-24 mcg/mL for the 250-mg dose, from 21-58 mcg/mL for the 500-mg dose and from 41-83 mcg/mL for the 1000-mg dose. At these doses, plasma levels of imipenem antimicrobial activity decline to ≤1 mcg/mL in 4-6 hrs. Peak plasma levels of cilastatin following a 20-min IV infusion of Zimilast. Range from 15-25 mcg/mL for the 250-mg dose, from 31-49 mcg/mL for the 500-mg dose and from 56-88 mcg/mL for the 1000-mg dose.
The plasma half-life of each component is approximately 1 hr. The binding of imipenem to human serum proteins is approximately 20% and that of cilastatin is approximately 40%. Approximately 70% of the administered imipenem is recovered in the urine within 10 hrs after which no further urinary excretion is detectable. Urine concentrations of imipenem in excess of 10 mcg/mL can be maintained for up to 8 hrs with Zimilast at the 500-mg dose. Approximately 70% of the cilastatin sodium dose is recovered in the urine within 10 hrs of administration of Zimilast.