Arpimune Mechanism of Action

Pharmacotherapeutic Group: Antineoplastic/immunosuppressant.
Pharmacology: Pharmacodynamics/Pharmacokinetics: Ciclosporin (Arpimune) is widely distributed throughout the body. Distribution in the blood is concentration-dependent with between 41 and 58% in erythrocytes and 10 to 20% in leucocytes; the remainder is found in plasma, about 90% protein-bound, mostly to lipoproteins. Because of the wide distribution, into blood cells whole blood concentrations are higher than and not compatible with plasma concentrations; where peak plasma concentrations are reported to be approximately 1 nanogram/mL for each mg of oral ciclosporin (Arpimune) whole blood concentrations for each mg range from about 1.4 to 2.7 nanograms/mL. Ciclosporin (Arpimune) is reported to cross the placenta and to be distributed into breast milk.
Clearance from the blood is biphasic. The terminal elimination half-life of an oral dose is reported to range from about 5 to 20 hours. Clearance in children is more rapid.
Ciclosporin (Arpimune) is extensively metabolized in the liver and primarily excreted in feces via the bile. About 6% of a dose is reported to be excreted in urine, less than 0.1% unchanged.
Used in immunosuppression for prophylactic treatment of organ transplants, ciclosporin (Arpimune) exerts specific and reversible inhibition of immunocompetent lymphocytes in the G0- or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited. The T1-helper cell is the main target, although the T1-suppressor cell may also be suppressed. It also inhibits lymphokine production and release including interleukin-2.