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HY points about each drug followed by a quiz at the end
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Cyclosporin
MOA of cyclosporine? –> inhibits cyclophilin (intracellular protein) –> decreases intracellular calcineurin –> decreases IL-2 transcription.
Important toxicities of cyclosporine? –> answer = nephrotoxicity (hyperkalemia), hypertension, hypertrichosis (↑ hair growth), gingival hyperplasia. USMLE wants you to know all of these. This isn’t just some random list of arbitrary yieldness.
- USMLE vignette will tell you someone is on an immunosuppressant and that the creatinine has increased –> answer = cyclosporine.
- Cyclosporine, verapamil (non-dihydropyridine CCB), and phenytoin (anti-convulsant that blocks Na channels) all are HY for causing gingival hyperplasia.
- Random context: On my peds rotation years ago, I sat in on a consult with a family where the kid was on cyclosporine. I remember the pediatrician looked at the gums, checked the blood pressure, and asked the mom if she noticed any changes in hair growth. I was like, “What do you know? The stuff we study actually does sometimes apply to real life.”
Tacrolimus
MOA of tacrolimus? –> answer = inhibits FK506 –> decreases intracellular calcineurin –> decreases IL-2 transcription.
Important side-effects of tacrolimus? –> answer = type II diabetes, nephrotoxicity (hyperkalemia).
- USMLE likes dysglycemia for tacrolimus.
- Random context: met two people in real life who were on tacrolimus. Both had type II diabetes because of it.
Sirolimus
MOA of sirolimus? –> answer = blocks mTOR –> does not decrease intracellular calcineurin –> decreases responsiveness to IL-2.
Important side-effects of sirolimus? –> answer = dyslipidemia; does not cause nephrotoxicity.
Summary table
| MEHLMANMEDICAL | MOA | ↓ Calcineurin? | Effect on IL-2? | Nephrotoxic? |
| Cyclosporine | Inhibits cyclophilin | Yes | ↓ Transcription | Yes |
| Tacrolimus | Inhibits FK-506 | Yes | ↓ Transcription | Yes |
| Sirolimus | Inhibits mTOR | No | ↓ Responsiveness | No |
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