Single- and multiple-dose kinetics of estazolam, a triazolo benzodiazepine

  title={Single- and multiple-dose kinetics of estazolam, a triazolo benzodiazepine},
  author={Marcia Divoll Allen and David J Greenblatt and John D. Van Arnold},
The pharmacokinetic properties of estazolam, a triazolo benzodiazepine hypnotic agent, were assessed in a series of healthy volunteers following single and multiple doses. After single oral doses of 2–16 mg, peak plasma concentrations were reached within 6 h. Values of elimination half-life ranged from 8.3–31.2 h (mean 17.0 h) and did not vary significantly with dose. During 3 weeks of therapy, steady-state plasma concentrations increased approximately in proportion to increasing doses, and… 
Benzodiazepine: Bedeutung der Kinetik für die Therapie
  • H. Ochs
  • Medicine, Biology
    Klinische Wochenschrift
  • 2005
Pharmacokinetic classification may assist in understanding differences among benzodiazepines, but does not explain all of their clinical actions.
Clinical Pharmacokinetics and Pharmacodynamics of Anxiolytics and Sedative/Hypnotics
Benzodiazepines continue to be one of the most commonly prescribed agents available in a variety of dosage formulations used for all age groups and gender can be another significant factor as females were found to have significantly higher zolpidem plasma concentrations than males and when given comparative doses also displayed more pronounced psychomotor impairment.
Determination of estazolam in plasma by high-performance liquid chromatography with solid-phase extraction.
A high-performance liquid chromatography (HPLC) assay was developed and applicable for accurately monitoring the plasma level of estazolam in healthy subjects participating in scientific research.
Pharmacological Treatment of Insomnia
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Effects of estazolam as a premedication in mentally retarded patients
Estazolam was found to be an effective drug for premedication in mentally retarded patients and clinically effective in 94% of patients, no patient needing either additional drugs for sedation or heavy restraint.
Homicidal Poisoning of Heroin and Estazolam: Autopsy and Pathological Findings, Toxicological Analysis
An unusual homicidal case in which a 40-year-old woman was deceived into drinking a cup of milk that had 72 tablets of estazolam dissolved in and then being injected heroin aqueous solution on the right deltoid region, taught a lesson that the determination of other drugs, particularly central nervous system depressants in heroin poisoning were quite important in forensic expertise.
Anxiety disorder: An overview
The underlying pathophysiology and drug therapy of anxiety disorder is revealed, and many gamma-aminobutyric acid facilitating drugs since the 1960s for anxiety treatment are revealed.
Bezpieczne i skuteczne stosowanie benzodiazepin w zaburzeniach psychiatrycznych i towarzyszących im innych schorzeniach
Benzodiazepiny są grupą lekow psychotropowych stosowanych w leczeniu stanow lekowych, bezsenności i innych zaburzen psychiatrycznych. Nalezą do najcześciej przepisywanych lekow w Polsce i na świecie.


Single- and multiple-dose kinetics of oral lorazepam in humans: The predictability of accumulation
Overall, the rate and extent of lorazepam accumulation during multiple dosage were reasonably well predicted by the single-dose kinetic study, however, accurate prediction for any specific individual was not always achieved.
Clinical Pharmacokinetics of Hydralazine
Since there is no clear-cut correlation between the plasma concentration of the drug and its effect upon blood pressure, there is at present no reason to routinely measure plasma levels of hydrallazine in treated hypertensive patients.
Pharmacokinetics and Bioavailability of Intravenous, Intramuscular, and Oral Lorazepam in Humans
Six healthy volunteers received single 2- and 4-mg doses of lorazepam by 5-min intravenous infusion, in tablet form by mouth in the fasting state, and by deltoid intramuscular injection in a six-way
Simultaneous gas-chromatographic analysis for diazepam and its major metabolite, desmethyldiazepam, with use of double internal standardization.
Electron-capture gas-liquid chromatography was used for simultaneous quantitation of plasma diazepam (I) and its major metabolite, desmethyldiazepam(II) and the applicability of the method to single-dose pharmacokinetic studies of I in humans is illustrated.
Spectrophotometric assay of antipyrine in plasma: a reevaluation.
The spectrophotometric assay for antipyrine is suitable for most clinical pharmacokinetic studies and has high between-day replicability as well as stability during prolonged storage at -20 degrees C.
Assessment of pharmacokinetic constants from postinfusion blood curves obtained after I.V. infusion.
A mathematical equation is presented which enables one to determine the parameters identical to an i.v. bolus injection curve by utilizing the postinfusion blood curve, applicable to all compartmental models that may be described by linear first-order differential equations with constant coefficients.
Analysis of lorazepam and its glucuronide metabolite by electron-capture gas--liquid chromatography. Use in pharmacokinetic studies of lorazepam.
This paper describes a rapid and sensitive method for analysis of lorazepam and its glucuronide metabolite in plasma and urine following therapeutic doses of lOrazepAm in humans, and the applicability of the method to pharmacokinetic studies of l orazepAM is demonstrated.
The estimation of antipyrine in biological materials.
Determination of desmethyldiazepam in plasma by electron-capture GLC: application to pharmacokinetic studies of clorazepate.
Plasma desmethyldiazepam concentrations were quantitated by a rapid and sensitive technique using electron-capture GLC. Following addition of diazepam as the internal standard, plasma is extracted at