AlternativeCiclosporin: Neoral · Tacrolimus: Prograf, Adoport
Ciclosporin / Tacrolimus
Calcineurin inhibitors
Compatible — useful steroid-sparing option; monitor BP and renal function.
OralIV
First-line for
- Lupus nephritis or transplant-related autoimmune disease when azathioprine/HCQ insufficient
Mechanism
Inhibit calcineurin → block IL-2 transcription → suppress T-lymphocyte activation.
Calcineurin inhibitors in pregnancy
- Compatible — continue if needed for disease control
- Tacrolimus dose often needs increasing in pregnancy (↑ clearance)
- Monitor BP + renal function every trimester
Dosing
- Ciclosporin
- 2.5–5 mg/kg/day PO in 2 divided doses, trough-level guided
- Tacrolimus
- 0.1–0.2 mg/kg/day PO in 2 divided doses, trough-level guided — often needs uptitration in pregnancy
Contraindications
- CautionUncontrolled hypertension
- CautionRenal impairment
- AbsoluteVoclosporin specifically avoided in pregnancy/lactation — alcohol-containing formulation (distinct from ciclosporin/tacrolimus)
Side effects
- Hypertension
- Nephrotoxicity
- Tremor, headache
- Gum hyperplasia / hirsutism (ciclosporin)
Fetal & maternal notes
- • Compatible in pregnancy; possible association with preterm birth/low birth weight, though hard to separate from underlying maternal disease.
- • Low transfer into breast milk — compatible with breastfeeding.
Key interactions
Grapefruit juice
Caution↑ levels via CYP3A4 inhibition
NSAIDs
Caution↑ nephrotoxicity risk
Clinical pearls
- 💡 A useful steroid- and MMF-sparing option that can safely bridge a woman through pregnancy when disease needs more than azathioprine/HCQ alone.
Content last reviewed: REPLACE_ME (e.g. 2026-07) · Sources: Rheumatology Secrets 5th ed. Table 78.2
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