Efavirenz

PD Dialyzability: Unlikely

Pharmacokinetic Parameters [1] [2] [3]

  Efavirenz
Molecular Weight (Da) 315.6
Plasma Protein Binding (%) 99.75
Volume of Distribution (L/Kg) 4
Hepatic Metabolism Primarily via CYP3A4 and CYP2B6
Excreted Unchanged (%) < 1
Half-Life; Normal Renal Function (hours) 40 - 55
Half-Life; ESRD (hours) Unknown

CAPD/CCPD Dosing:

No large studies are available to provide dosing recommendations for efavirenz in PD patients. Two case reports suggest that efavirenz 600 mg PO daily can be used in CAPD [4] [5]. Due to extensive protein binding, primarily hepatic metabolism, and minimal renal clearance of unchanged drug, it is unlikely that dosing adjustment of efavirenz is required.

Literature Summary:

Title Patient Intervention Outcome Note
Efavirenz dosing in patients receiving continuous ambulatory peritoneal dialysis [4]
  • 53-year-old HIV positive male on CAPD (chronic renal failure secondary to hypertension)
  • Efavirenz 600mg PO daily with indinavir 1000 mg PO q8h
  • Efavirenz blood levels following 2 weeks of treatment were consistent with levels seen in patients without renal failure.
 None
Experience with efavirenz in end-stage renal disease [5]
  • 40-year-old HIV positive African female on CAPD (chronic renal failure secondary to hypertension)
  • Efavirenz 600mg PO daily + zidovudine 100mg TID + lamivudine 50mg once daily
  • Over 41 weeks: Viral load (copies/mL): 34800 🡪 <50. CD4 (x10^6/L): 230 🡪 340.
  • No side effects or problems reported

References

[1]Tseng A, Foisy M. Selected properties of efavirenz. Immunodeficiency Clinic [Internet]. 2014 Dec [cited 2018 Feb 20]. 1-7. Available from www.hivclinic.ca.
[2]Wishart DS, Knox C, Guo AC, Shrivastava S, Hassanali M, Stothard P, et al. Drugbank: a comprehensive resource for in silico drug discovery and exploration. Nucleic Acids Res. 2006 Jan 1: 34(database issue):D668-672.
[3]Adult Drug Book. Kidney Disease Program [Internet]. Unknown [cited 2018 Feb 20]. Available from: https://kdpnet.kdp.louisville.edu/drugbook/adult/
[4](1, 2) Gill JM, Ostrop NJ, Fiske WD, Brennan JM. Efavirenz dosing in patients receiving continuous ambulatory peritoneal dialysis. AIDS 2000;14(8):1062.
[5](1, 2) Prime KP, Woolfson RG, Pakianathan MR. Experience with efavirenz in end-stage renal disease. Int J STD AIDS 2003;14(7):497-498.