Skip to main content
Log in

Pharmacokinetics of fluconazole after oral administration in children with human immunodeficiency virus infection

  • Pharmacokinetics and Disposition
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Abstract

The objective of this study was to determine the pharmacokinetics of fluconazole after oral administration in children with human immunodeficiency virus (HIV) infection. After an overnight fast, a single dose of either 2 mg·kg−1 or 8 mg·kg−1 was administered in a suspension; five children received 2 mg·kg−1 and four 8 mg·kg−1 (ages 5–13 years). Blood samples were collected at various times on day 1, and once daily on days 2–7 after the dose. Fluconazole serum concentrations were measured by gas chromatography. At the dose of 2 mg·kg−1, the Cmax, AUC (0–∞), and t1/2 ranged from 2.3–4.4 μg·ml−1, 84.9–136 μg·h·ml−1, and 19.8–34.8 h, respectively. At the dose of 8 mg·kg−1 the Cmax, AUC (0–∞), and t1/2 ranged from 5.4–12.1 μg·ml−1, 330–684 μgh·ml−1, and 25.6–42.3 h, respectively. When compared with published data in healthy adults, fluconazole achieved similar serum concentrations in the present group of children, indicating a nearly complete degree of absorption.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Debruyne D, Ryckelynck J (1993) Clinical pharmacokinetics of fluconazole. Clin Pharm 24:10–27

    Google Scholar 

  2. Grant SM, Clissold SP (1990) Fluconazole — a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in superficial and systemic mycosis. Drugs 39:877–916

    Google Scholar 

  3. Stern JJ, Harman BJ, Sharkey P, Rowland V, Squires K, Murray HW, Graybill JR (1988) Oral fluconazole therapy for patients with acquired immunodeficiency syndrome and cryptococcosis: experience with 22 patients. Am J Med 85:477–480

    Google Scholar 

  4. Sugar AM, Saunders C (1988) Oral fluconazole as suppressive therapy of disseminated cryptococcosis in patients with acquired immunodeficiency syndrome. Am J Med 85:481–489

    Google Scholar 

  5. DeWit S, Urbain D, Rahir F, Weerts D, Clumeck N (1991) Efficacy of oral fluconazole in the treatment of AIDS associated oesophageal candidiasis. Eur J Clin Microbiol Infect Dis 10:503–505

    Google Scholar 

  6. Lake-Bakaar, Beidas S, Elsakr M, Iyer S, Staus E (1987) Impaired gatric acid secretion in AIDS. Gastroenterology 92:1488A

  7. Guttman D, Raymond JA, Gelb A, Ehya H, Mather U, Mildran D, et al (1983) Virus-associated colitis in homosexual men: two case reports. Am J Gastroenterol 78:167–169

    Google Scholar 

  8. Kotler DP, Gaetz HP, Lange (1984) Enteropathy associated with the acquired immunodeficiency syndrome. Ann Int Med 101:421–428

    Google Scholar 

  9. Levinson W, Bennetts RW (1985) Cytomegalovirus colitis is acquired immunodeficiency syndrome — a chronic disease with varying manifestations. Am J Gastroenterol 80:445–447

    Google Scholar 

  10. Harris SC, Wallace JE, Foulds G, Rinaldi MG (1989) Assay of fluconazole by megabore capillary gas liquid chromatography with nitrogen selective detecttion. Antimicrob Agents Chemother 33:714–716

    Google Scholar 

  11. Farrow PR, Faulkner JK, Brammer KW (1988) The pharmacokinetics of fluconazole. Symposium on fluconazole: a novel advance in therapy for systemic fungal infections, Dorado, Puerto Rico, Oct 8–9, abstract no. 14-199

  12. Foulds G, Wajszczuk C, Weidler DJ, Garg DC, Gibso P (1987) Steady state parenteral kinetics of fluconazole in man. First International Conference on Drug Research in Immunologic and Infectious Diseases: antifungal drugs, Oct 8–10 abstract no. P-6

  13. Hughes W, Leoung G, Krame F, Bozett S, Safrin S, et al (1993) Comparison of atovaquone (566C80) with trimethoprim-sulfamethoxazole to treate Pneumocystis carinii pneumonia in patients with AIDS. N Engl J Med 328:1521–1527

    Google Scholar 

  14. Macnab KA, Gill MJ, Sutherland LR, Visser ND, Church D (1993) Erratic zidovudine bioavailability of HIV seropositive patients. J Antimicrob Chemother 31:421–428

    Google Scholar 

  15. Fletcher CV, Rhame FS, Beatty CC, Simpson M, Balfour HH (1992) Comparative pharmacokinetics of zidovudine in healthy volunteers and in patients with AIDS with and without hepatic disease. Pharmacotherapy 12:429–434

    Google Scholar 

  16. Gatti G, Verotta D, Flaherty J, Borin M, Gamertoglio J ⊠ VIIth Int. Conf. AIDS/IIIrd STD World Congress, abstract no. PoB 3176

  17. Gatti G, Verotta D, Flaherty J, Borin M, Gambertoglio J (1993) Absorption profile of oral clindamycin in patients with AIDS and in healthy volunteers (abstract). Clin Pharmacol Ther 53:208

    Google Scholar 

  18. Hughes WT, Kennedy W, Shenep JL, Flynn PM, Hetherington SV, Fullen G, et al (1991) Safety and pharmacokinetics of 566C80, a dydroxynaphthoquinone with anti-Pneumocystis carinii activity: a phase I study in human immunodeficiency virus (HIV)-infected men. J Infect Dis 163:843–848

    Google Scholar 

  19. DeMuria D, Forrest A, Rich J, Scavone JM, Cohen LG, Kazanjian PH (1993) Pharmacokinetics and bioavailability of fluconazole in patients with AIDS. Antimicrob Agents Chemother 37:2187–2192

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Nahata, M.C., Brady, M.T. Pharmacokinetics of fluconazole after oral administration in children with human immunodeficiency virus infection. Eur J Clin Pharmacol 48, 291–293 (1995). https://doi.org/10.1007/BF00198314

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00198314

Key words

Navigation