Cyclosporine

Administration

• Type: immunosuppressant
• Dosage Forms: 25,100; 100/mL
• Routes of Administration: PO, injection
• Common Trade Names: Sandimmune

Adult Dosing

Organ transplant rejection prophylaxis

• Dosing protocols vary
• Start: 7-9mg/kg/day PO divided BID; give 1st dose 4-12 hr pre-transplant or postop
• For heart, kidney, or liver transplant, adjust dose based on target levels, rejection status, adverse effects

Rheumatoid arthritis, severe

• Start: 2.5 mg/kg/day PO divided BID, increase 0.5-0.75 mg/kg/day after 8 wk and after 12 wk; Max: 4mg/kg/day
• Use alone or with methotrexate; decreased 25-50% PRN adverse effects, discontinue if no benefit by 16 wks

Psoriasis, severe recalcitrant plaque

• Start: 2.5 mg/kg/day PO divided BID, increase 0.5 mg/kg/day q 2 wk after 4 wk; Max: 4mg/kg/day
• Decrease 25-50% PRN adverse effects, discontinue if inadequate response after 6 weeks on max tolerated dose

Pediatric Dosing

Organ transplant rejection prophylaxis

• Dosing protocols vary
• Start 7-9mg/kg/day PO divided BID, give 1st dose 4-12 hr pre-transplant or post op
• For heart, kidney, or liver transplant, adjust dose based on target levels, rejection status, adverse effects

Special Populations

• Pregnancy Rating: Pregnancy Category C
• Lactation risk: safety unknown

Renal Dosing

• Adult:
  • transplant: no adjustment
  • rheumatoid arthritis or psoriasis: contraindicated in renal impairment
• Pediatric:
  • transplant: no adjustment

Hepatic Dosing

• Adult: not defined, caution advised
• Pediatric: not defined, caution advised

Contraindications

• Allergy to class/drug
• uncontrolled hypertension (RA or psoriasis use)
• renal impairment (RA or psoriasis use)
• malignancy (RA or psoriasis use)
• PUVA/UVB treatment (psoriasis use)
• concurrent immunosuppressants (psoriasis use)
• coal tar treatment (psoriasis use)
• concomitant XRT (psoriasis use)

Adverse Reactions

Serious

• HTN, severe
• immunosuppression
• infection, severe
• opportunistic infection
• BK virus-associated nephropathy
• hyperkalemia, severe
• nephrotoxicity
• hepatotoxicity
• glomerular capillary thrombosis
• diabetes mellitus
• leukopenia
• thrombocytopenia
• hemolytic anemia
• malignancy
• malignancy
• seizures
• encephalopathy
• posterior reversible encephalopathy syndrome
• neurotoxicity
• intracranial hypertension
• optic disc edema
• MI
• depression
• pancreatitis
• GI bleeding

Common

• BUN, Cr elevated
• HTN
• hirsutism
• infection
• tremor
• gingival overgrowth
• headache
• hypertriglyceridemia
• nausea/vomiting
• diarrhea
• leg cramps
• paresthesia
• influenza-like symptoms
• edema
• dizziness
• rash
• acne
• chest pain
• stomatitis
• hypomagnesemia
• arthralgia
• flushing
• bronchospasm
• hyperkalemia
• hyperglycemia
• hyperuricemia

Pharmacology

• Half-life: 8.4h
• Metabolism: liver extensively, GI tract, kidney; CYP450
• Excretion: bile primarily, urine 6%

Mechanism of Action

exact mechanism of action unknown; inhibits T-lymphocytes

References

epocrates