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: 2.5mg/kg/day PO divided BID, increase 0.5-0.75mg/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: 2.5mg/kg/day PO divided BID, increase 0.5mg/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

  • hypertension, 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, creatinine elevated
  • hypertension
  • 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

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