Phenytoin enzyme induction for management of supratherapeutic tacrolimus levels due to drug-drug interaction with nirmatrelvir/ritonavir: Case series and discussion

Am J Health Syst Pharm. 2024 Jun 24;81(13):e345-e352. doi: 10.1093/ajhp/zxae032.

Abstract

Purpose: Nirmatrelvir/ritonavir is one of few options for outpatient treatment of COVID-19, but its use has been limited in transplant recipients due to significant drug interactions with immunosuppressants. Tacrolimus toxicity is possible when the drug is coadministered with nirmatrelvir/ritonavir and may require urgent reduction of tacrolimus levels. This case series describes the use of phenytoin for enzyme induction in 5 adult solid organ transplant recipients with supratherapeutic tacrolimus levels resulting from coadministration with nirmatrelvir/ritonavir.

Summary: Solid organ transplant recipients are at high risk for complications related to COVID-19. Outpatient treatment options are limited, and therapeutic drug monitoring is complex in patients requiring quarantine. The 5 solid organ transplant recipients described herein were initiated on nirmatrelvir/ritonavir in the outpatient setting and subsequently presented with supratherapeutic tacrolimus concentrations greater than 59 ng/mL and developed signs and symptoms of tacrolimus toxicity. In all patients, nirmatrelvir/ritonavir and tacrolimus were discontinued, and oral phenytoin (200-400 mg/day) was given for 2 to 4 days. Tacrolimus was resumed once tacrolimus levels decreased to appropriate levels.

Conclusion: These observations demonstrate that metabolism induction using phenytoin may be a useful strategy in the setting of supratherapeutic tacrolimus levels resulting from concomitant administration with nirmatrelvir/ritonavir.

Keywords: COVID-19; drug interaction; nirmatrelvir/ritonavir; phenytoin; tacrolimus.

Publication types

  • Case Reports

MeSH terms

  • Adult
  • Aged
  • COVID-19 Drug Treatment
  • Cytochrome P-450 CYP3A Inducers / pharmacology
  • Drug Interactions*
  • Drug Monitoring / methods
  • Female
  • Humans
  • Immunosuppressive Agents* / administration & dosage
  • Immunosuppressive Agents* / adverse effects
  • Immunosuppressive Agents* / pharmacokinetics
  • Male
  • Middle Aged
  • Phenytoin* / administration & dosage
  • Phenytoin* / adverse effects
  • Ritonavir* / administration & dosage
  • Ritonavir* / adverse effects
  • Tacrolimus* / administration & dosage
  • Tacrolimus* / adverse effects
  • Transplant Recipients

Substances

  • Phenytoin
  • Tacrolimus
  • Ritonavir
  • Immunosuppressive Agents
  • Cytochrome P-450 CYP3A Inducers