[Pharmacokinetics of itraconazole]. 1994

G Cauwenbergh
Janssen Pharmaceutica, Beerse, Belgien.

Itraconazole is a lipophilic triazole antifungal with a broad spectrum of activity. Most of the important fungal pathogens respond to itraconazole concentrations of 100 ng/ml. Therefore, itraconazole is suitable for treatment of a variety of systemic mycoses, as aspergillosis, cryptococcosis, candidosis as well as non-European endemic mycoses. The lipophilicity of the molecule is the reason for a pronounced tissue affinity meaning that the tissue levels of the drug usually are substantially higher than the corresponding plasma levels. This fact has to be kept in mind when plasma measurements are being used to decide a therapeutic approach for a systemic fungal infection. In contrast to the skin, internal organs will not show a long term retention of itraconazole in the tissues. This means that for systemic mycoses the therapy needs to be continued until clinical and mycological cure is obtained. Reduced itraconazole absorption may occur in a minority of patients because of underlying chemotherapy or dramatic changes in stomach pH. This is occasionally seen in patients with allogeneic bone marrow transplants and end-stage AIDS patients. Use of antacida and H2-antagonists somewhat reduces the absorption of itraconazole, however, often not in a clinically meaningful way. Itraconazole increases the levels of cyclosporin A. Itraconazole levels are decreased by rifampicin, phenytoin and phenobarbital. Caution is required in patients on concomitant anticoagulants.

UI MeSH Term Description Entries
D007408 Intestinal Absorption Uptake of substances through the lining of the INTESTINES. Absorption, Intestinal
D008826 Microbial Sensitivity Tests Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses). Bacterial Sensitivity Tests,Drug Sensitivity Assay, Microbial,Minimum Inhibitory Concentration,Antibacterial Susceptibility Breakpoint Determination,Antibiogram,Antimicrobial Susceptibility Breakpoint Determination,Bacterial Sensitivity Test,Breakpoint Determination, Antibacterial Susceptibility,Breakpoint Determination, Antimicrobial Susceptibility,Fungal Drug Sensitivity Tests,Fungus Drug Sensitivity Tests,Sensitivity Test, Bacterial,Sensitivity Tests, Bacterial,Test, Bacterial Sensitivity,Tests, Bacterial Sensitivity,Viral Drug Sensitivity Tests,Virus Drug Sensitivity Tests,Antibiograms,Concentration, Minimum Inhibitory,Concentrations, Minimum Inhibitory,Inhibitory Concentration, Minimum,Inhibitory Concentrations, Minimum,Microbial Sensitivity Test,Minimum Inhibitory Concentrations,Sensitivity Test, Microbial,Sensitivity Tests, Microbial,Test, Microbial Sensitivity,Tests, Microbial Sensitivity
D009181 Mycoses Diseases caused by FUNGI. Fungus Diseases,Fungal Diseases,Fungal Infections,Fungus Infections,Disease, Fungal,Disease, Fungus,Diseases, Fungal,Diseases, Fungus,Fungal Disease,Fungal Infection,Fungus Disease,Fungus Infection,Infection, Fungal,Infection, Fungus,Infections, Fungal,Infections, Fungus
D009894 Opportunistic Infections An infection caused by an organism which becomes pathogenic under certain conditions, e.g., during immunosuppression. Infection, Opportunistic,Infections, Opportunistic,Opportunistic Infection
D005658 Fungi A kingdom of eukaryotic, heterotrophic organisms that live parasitically as saprobes, including MUSHROOMS; YEASTS; smuts, molds, etc. They reproduce either sexually or asexually, and have life cycles that range from simple to complex. Filamentous fungi, commonly known as molds, refer to those that grow as multicellular colonies. Fungi, Filamentous,Molds,Filamentous Fungi,Filamentous Fungus,Fungus,Fungus, Filamentous,Mold
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D017088 AIDS-Related Opportunistic Infections Opportunistic infections found in patients who test positive for human immunodeficiency virus (HIV). The most common include PNEUMOCYSTIS PNEUMONIA, Kaposi's sarcoma, cryptosporidiosis, herpes simplex, toxoplasmosis, cryptococcosis, and infections with Mycobacterium avium complex, Microsporidium, and Cytomegalovirus. HIV-Related Opportunistic Infections,Opportunistic Infections, AIDS-Related,Opportunistic Infections, HIV-Related,AIDS Related Opportunistic Infections,AIDS-Related Opportunistic Infection,HIV Related Opportunistic Infections,HIV-Related Opportunistic Infection,Infection, HIV-Related Opportunistic,Infections, HIV-Related Opportunistic,Opportunistic Infection, AIDS-Related,Opportunistic Infection, HIV-Related,Opportunistic Infections, AIDS Related,Opportunistic Infections, HIV Related
D017964 Itraconazole A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis. Orungal,R-51211,Sporanox,R 51211,R51211

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