Ciclosporin

Ciclosporin - is a cyclic peptide molecule derived from a soil fungus. It is a potent nephrotoxin, producing interstitial renal fibrosis with tubular atrophy. Monitoring of ciclosporin blood level is essential.
Normal range: 100–300 μg/l
For renal transplants: lower end of range
For heart/lung/liver: upper end of range
For stem cell transplant: 200–600 μg/l – dependent upon donor, conditioning
regimen and T-depletion of graft

Uses:
Prevention of organ rejection after transplantation

Administration:
• IV dose: 1–5 mg/kg/day
To be diluted 1 in 20 to 1 in 100 with 0.9% sodium chloride or 5% glucose
To be given over 2–6 h
Infusion should be completed within 12 h if using PVC lines
Switch to oral for long-term therapy

• Oral: 1.5 times IV dose given 12 hourly
Monitor: Hepatic function
         Renal function
         Ciclosporin blood level (pre-dose sample)

How not to use ciclosporin:
Must not be given as IV bolus
Do not infuse at >12 h if using PVC lines – leaching of phthalates from the PVC

Adverse effects:
Enhanced renal sensitivity to insults
↑ Plasma urea and serum creatinine secondary to glomerulosclerosis
Hypertension – responds to conventional antihypertensives
Hepatocellular damage (↑ transaminases)
Hyperuricaemia
Gingival hypertrophy
Hirsutism
Tremors or seizures at high serum levels

Cautions:
↑ Susceptibility to infections and lymphoma
↑ Nephrotoxic effects with concurrent use of other nephrotoxic drugs