Immunosuppressants Flashcards
(12 cards)
What is the mechanism of action of cyclosporine?
Binds to cyclophilin, inhibiting calcineurin → ↓ IL-2 transcription → ↓ T-cell activation.
What is the mechanism of action of tacrolimus?
Binds to FKBP-12, inhibiting calcineurin → ↓ IL-2 transcription → ↓ T-cell activation.
What are the main indications for cyclosporine?
Organ transplantation, RA, psoriasis, uveitis, dry eye (Restasis®).
What are the main indications for tacrolimus?
Organ transplantation (especially liver), atopic dermatitis (Protopic®), rescue therapy.
Which calcineurin inhibitor causes hirsutism and gingival hyperplasia?
Cyclosporine.
Which calcineurin inhibitor is more diabetogenic and neurotoxic?
Tacrolimus.
Which calcineurin inhibitor causes more hyperlipidemia?
Cyclosporine.
Which one has a higher risk of tremor and seizures?
Tacrolimus.
What are key contraindications for tacrolimus and cyclosporine?
Hypersensitivity, concurrent calcineurin inhibitor use, active infections, pregnancy (relative), renal failure.
Which drug is preferred in liver transplantation?
Tacrolimus.
Which drug is more potent and used in lower doses?
Tacrolimus.
Which calcineurin inhibitor is better avoided in patients with cosmetic concerns?
Cyclosporine.
