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calcineurin inhibitor
Indications:
- chronic maintenance immunosuppression after organ transplantation
Adverse effects:
- hypertension (treated with thiazide diuretics)
- oral calcineurin inhibitors cyclosporine & tacrolimus are associated with excess risk for non-melamoma skin cancers & lymphomas
- topical calcineurin inhibitors tacrolimus & pimecrolimus are not [3]
- topical calcineurin inhibitors are associated with increased risk of lymphomas (RR=1.9) [4]
Drug interactions:
- drugs that increase calcineurin inhibitor levels
- antimicrobial agents
- capsofungin
- azole
- macrolides
- chloroquine
- antiviral protease inhibitor
- ofloxacin
- calcium channel blockers
- diltiazem
- verapamil
- amlodipine (less so)
- felodipine (less so)
- nicardipine
- benzodiazepines
- alprozolam
- diazepam
- danazol
- grapefruit juice
- allopurinol
- setralins
- drugs that decrease calcineurin inhibitor levels
- antimicrobial agents
- rifampin
- rifabutin
- anticonvulsants
- carbamazepine
- phenobarbital
- phenytoin
- orlisat
- St John's wort
Mechanism of action:
- agents that inhibit calcineurin
Interactions
drug adverse effects of calcineurin inhibitors
Related
calcineurin; serine/threonine protein phosphatase 3 (formerly PP2B)
Specific
calcineurin-binding protein cabin-1; calcineurin inhibitor; CAIN (CABIN1, KIAA0330)
cyclosporin A (Sandimmune, Neoral [CsA])
pimecrolimus (Elidel)
tacrolimus; FK506; fujimycin (Prograf, Advagraf, Envarsus XR)
voclosporin (Lupkynistm)
General
enzyme inhibitor
pharmaceutical agent
References
- Medical Knowledge Self Assessment Program (MKSAP) 17, 18.
American College of Physicians, Philadelphia 2015, 2018.
- Moes AD, Hesselink DA, Zietse R et al
Calcineurin inhibitors and hypertension: a role for pharmacogenetics?
Pharmacogenomics. 2014 Jun;15(9):1243-51. Review.
PMID: 25141899
- Asgari MM et al.
Association between topical calcineurin inhibitor use and keratinocyte
carcinoma risk among adults with atopic dermatitis.
JAMA Dermatol 2020 Aug 12; [e-pub]
PMID: 32785626
https://jamanetwork.com/journals/jamadermatology/fullarticle/2768937
- Lam M, Zhu JW, Tadrous M et al
Association Between Topical Calcineurin Inhibitor Use and Risk of Cancer,
Including Lymphoma, Keratinocyte Carcinoma, and Melanoma.
A Systematic Review and Meta-analysis.
JAMA Dermatol. Published online March 31, 2021
PMID: 33787818
https://jamanetwork.com/journals/jamadermatology/fullarticle/2778024