We have located links that may give you full text access.
JOURNAL ARTICLE
REVIEW
Making sense of itraconazole pharmacokinetics.
Journal of Antimicrobial Chemotherapy 2005 September
The triazole, itraconazole, has a wide spectrum of antifungal activity in vitro. Confirming this activity in vivo has been a long and difficult task because of problems with formulation, delivery and uncertainty about effective bioavailability. The physicochemical properties of the drug make it insoluble in water but strongly protein bound. The absorption and blood levels of the original capsular formulation were predictable with non-linear, saturation kinetics in normal volunteers. Tissue penetration was high and sustained. In neutropenic patients with haematological malignancies, levels were very variable and the doses required to achieve effective antifungal levels were higher than predicted from normal subjects' results. The solubility of the drug and predictability of blood levels were improved by the formulation of an oral solution with cyclodextrin. Wash-out times were prolonged in patients with this new formulation implying that tissue penetration was maintained. A high volume of distribution suggests that loading may be necessary. An intravenous cyclodextrin solution is also now available allowing rapid loading and avoidance of the well-known gut side effects of the oral solution. Clinical studies have suggested minimum bioavailable dosage and minimum trough blood levels for effective prophylaxis against systemic fungal infection. Interactions are also now well documented and manageable. The drug can be measured reliably, quickly and comparatively cheaply by HPLC in serum and plasma. The frequency of such testing in clinical practice depends on the need to ensure adequate levels and to avoid unwanted toxicity.
Full text links
Related Resources
Trending Papers
Heart failure with preserved ejection fraction: diagnosis, risk assessment, and treatment.Clinical Research in Cardiology : Official Journal of the German Cardiac Society 2024 April 12
Proximal versus distal diuretics in congestive heart failure.Nephrology, Dialysis, Transplantation 2024 Februrary 30
Efficacy and safety of pharmacotherapy in chronic insomnia: A review of clinical guidelines and case reports.Mental Health Clinician 2023 October
World Health Organization and International Consensus Classification of eosinophilic disorders: 2024 update on diagnosis, risk stratification, and management.American Journal of Hematology 2024 March 30
Get seemless 1-tap access through your institution/university
For the best experience, use the Read mobile app
All material on this website is protected by copyright, Copyright © 1994-2024 by WebMD LLC.
This website also contains material copyrighted by 3rd parties.
By using this service, you agree to our terms of use and privacy policy.
Your Privacy Choices
You can now claim free CME credits for this literature searchClaim now
Get seemless 1-tap access through your institution/university
For the best experience, use the Read mobile app