The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers

@article{Oda2003TheEO,
  title={The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers},
  author={M. Oda and Tsutomu Kotegawa and Kimiko Tsutsumi and Yasukiyo Ohtani and Keiji Kuwatani and Shigeyuki Nakano},
  journal={European Journal of Clinical Pharmacology},
  year={2003},
  volume={59},
  pages={615-619}
}
  • M. OdaT. Kotegawa S. Nakano
  • Published 27 September 2003
  • Medicine, Biology, Psychology
  • European Journal of Clinical Pharmacology
Rationale and objectiveBromazepam, an anti-anxiety agent, has been reported to be metabolized by cytochrome P450 (CYP). However, the enzyme responsible for the metabolism of bromazepam has yet to be determined. The purpose of this study was to examine whether the inhibition of CYP3A4 produced by itraconazole alters the pharmacokinetics and pharmacodynamics of bromazepam.MethodsEight healthy male volunteers participated in this randomized double-blind crossover study. The subjects received a 6… 

Bioanalytical methods for the determination of itraconazole and hydroxyitraconazole: overview from clinical pharmacology, pharmacokinetic, pharmacodynamic and metabolism perspectives.

This review focuses on providing comprehensive details on the bioanalytical methods available for the quantitation of both itraconazole and hydroxyitraconazer, and provides an overview of the clinical pharmacology, pharmacokinetics, pharmacodynamics and metabolism related aspects of itraconsazole.

5 1-Nucleotidase Activity In Albino Rats Treated With Talen ® Tablets ( Sedative ) 1

It is suggested that Talen® may be toxic to the hepatobiliary system as revealed by increase in 5 1 -Nucleotidase levels, which varied with the doses.

Understanding the pharmacokinetics of anxiolytic drugs

A need for a more balanced assessment of the benefits and risks associated with benzodiazepine use, particularly considering pharmacokinetic profile of the drugs to ensure that patients, who would truly benefit from these agents, are not denied appropriate treatment.

Clinically relevant drug interactions of current antifungal agents

The pharmacokinetic properties of antifungal agents and their clinically relevant drug interactions are reviewed and the echinocandins have the lowest propensity to interact with other medicines.

Assisted suicide by fentanyl intoxication due to excessive transdermal application

Fentanyl was the leading toxic noxa in a case of an assisted suicide committed by application of 34 matrix-based fentanyl-containing transdermal therapeutic systems (TTS) with different release rates.

Concomitant polypharmacy is associated with irinotecan-related adverse drug reactions in patients with cancer

It was found that multiple concomitant medicines were significantly associated with severe irinotecan-related toxicity, indicating that polypharmacy must be effectively managed to decrease the risk of adverse drug reactions in patients with cancer who received ir inotecans-based chemotherapy.

Drug–drug interactions of antifungal agents and implications for patient care

This article reviews drug interactions involving antifungal agents that affect other agents and implications for patient care are highlighted.

Fundamental Toxicological Sciences

Epoxidized fatty acids are generated during food processing and detected in various lipidand oil-containing foods. Although compounds with an epoxide structure have high reactivity and there is

References

SHOWING 1-10 OF 25 REFERENCES

Effect of Fluconazole on the Pharmacokinetics and Pharmacodynamics of Oral and Rectal Bromazepam: An Application of Electroencephalography as the Pharmacodynamic Method

The EEG method provided pharmacodynamic data that clearly reflected the pharmacokinetics of bromazepam and fluconazole and may be due to avoidance of degradation occurring in the gastrointestinal tract.

Effect of itraconazole on the single oral dose pharmacokinetics and pharmacodynamics of alprazolam

It is suggested that itraconazole, a potent CYP3A4 inhibitor, increases plasma concentration of alprazolam via its inhibitory effects on alpazolam metabolism, which supports previous studies suggesting that CYP 3A4 is the major enzyme catalyzing the metabolism of al prazol am.

Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole

Inhibition of the cytochrome P450IIIA by ketoconazole and itraconazole may explain the observed pharmacokinetic interaction and prescription of midazolam for patients receiving ketocon Razolam and itRaconazoles should be avoided.

Drug interactions with fluconazole.

Higher doses of fluconazole (200 mg) did not affect endogenous steroids, but coadministration resulted in changes in the pharmacodynamics of warfarin and the pharmacokinetics of phenytoin and cyclosporin A.

Effects of the Antifungal Agents on Oxidative Drug Metabolism

The interactions of ketoconazole with cyclosporin and tacrolimus have been applied for therapeutic purposes to allow a lower dosage and cost of the immunosuppressant and a reduced risk of fungal infections.

Bromazepam pharmacokinetics: Influence of age, gender, oral contraceptives, cimetidine, and propranolol

Bromazepam clearance is significantly impaired in elderly individuals, by coadministration of cimetidine and possibly propranolol, and in 11 young female users of oral contraceptive steroids, compared with seven age‐ and weight‐matched control women not using oral contraceptives.

Clinical pharmacokinetics of lorazepam: a review.

The clinical pharmacokinetics of lorazepam indicate that it is rapidly and readily absorbed, reaching peak concentrations in the blood proportional to the dose approximately 2 hours after oral administration, and the active drug and the glucuronide conjugate are completely eliminated from the blood within 1 week following the last dose.

Clinically Relevant Pharmacology of Selective Serotonin Reuptake Inhibitors

  • S. Preskorn
  • Medicine, Biology
    Clinical pharmacokinetics
  • 1997
An overview of the clinically relevant pharmacology of selective serotonin reuptake inhibitors (SSRIs) with an emphasis on their pharmacokinetics and effects on cytochrome P450 (CYP) enzymes is presented.

Metabolites of bromazepam, a benzodiazepine, in the human, dog, rat, and mouse.

The biotransformation of bromazepam, 7-bromo-1,3-dihydro-5-(2-pyridyl)-2H- 1,4-benzodiazepin-2-one, was studied in four species and the N4-oxide was a minor metabolite in dog urine and in the excreta of the human, dog, rat, and mouse.

Absence of significant interaction of fluconazole with cyclosporin.

It is concluded that fluconazole may be administered to cyclosporin treated patients without enhanced risk of toxicity, and a lack of clinically relevant pharmacokinetic interaction of flu Conazole with cyclOSporin is suggested.