The pharmacokinetics of midazolam in man

Smith, Maree T.; Eadie, Mervyn J.; Brophy, Tess

doi:10.1007/bf00562804

Cited by 255 publications

(128 citation statements)

References 4 publications

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“…This is due to direct effects on vascular alpha-1 receptors. This was minimized in our study by slowly infusing the drug, but this will take more time to reach sedation end point when compared to midazolam which also has to be given reasonably slowly as it has a relatively slow time to peak effect [31]. There was not statistically significant in incidence of hypotension between the two groups.…”

Section: Discussionmentioning

confidence: 95%

A Comparison of Dexmedetomidine and Midazolam for Sedation in Gynecologic Surgery Under Epidural Anesthesia

Liang

2011

J Curr Surg

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Section: Discussionmentioning

confidence: 95%

A Comparison of Dexmedetomidine and Midazolam for Sedation in Gynecologic Surgery Under Epidural Anesthesia

Liang

2011

J Curr Surg

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“…In several European countries, a tablet form is available for oral use as a sedative-hypnotic. The disposition of midazolam has been studied extensively in healthy subjects after intravenous, intramuscular and oral administration (Allonen et al, 1981;Avram et al, 1983;Bornemann et al,1985Bornemann et al, , 1986Greenblatt et al, 1984;Heizmann & Ziegler, 1981;Heizmann et al, 1983;Holazo etal., 1988;Klotz & Zeigler, 1982;Smith et al, 1981Smith et al, , 1984. Midazolam is bound extensively to plasma proteins (94-96%), it has a large volume of distribution (0.8 to 1.91 kr-'), a high systemic clearance (0.24 to 0.731 h-kg-1) and a short elimination half-life (1.5 to 3 h).…”

Section: Introductionmentioning

confidence: 99%

The pharmacokinetics of midazolam in patients with congestive heart failure.

Patel

Soni

et al. 1990

Brit J Clinical Pharma

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The disposition of midazolam was investigated in six patients with congestive heart failure (CHF) and six age-and weight-matched healthy subjects by administering two single doses of the drug (3.75 mg i.v. and 7.5 mg p.o.) separated by 1 week. Serial blood samples were collected for 24 h after each dose and plasma was assayed for midazolam by GC-MS. In the CHF patients, the elimination half-life was prolonged (4 to 4.5 vs < 3 h), the systemic clearance was lowered (376 vs 551 ml min-1) and the peak plasma drug concentration after the p.o. dose was higher (76 vs 42 ng ml-'). The systemic availability (45 vs 41%), the steady state volume of distribution (111 vs 108 1) and the time of peak plasma drug concentration after the p.o. dose (0.9 vs 0.9 h) were unchanged. The predominant effect of CHF was on the clearance of midazolam which was decreased by 30%. The drug was well tolerated and did not cause any adverse effects.

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“…The 15-mg dose of midazolam was chosen because it is well-tolerated in volunteers and is in clinical use for anaesthesia induction (De Castro et al, 1981). A dose of 9 mg a-hydroxy midazolam was selected with the aim of attaining a plasma concentration of this metabolite approximately equal to that obtained with oral administration of 15 mg midazolam after 60% first-pass metabolism (Smith et al, 1981).…”

Section: Discussionmentioning

confidence: 99%

Comparison of the effects of intravenously administered midazolam, triazolam and their hydroxy metabolites.

Ziegler¹,

Schalch²,

Leishman³

et al. 1983

Brit J Clinical Pharma

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The aim of the study was to compare the pharmacological activity and clinical effect after i.v. administration of midazolam, triazolam and their hydroxy metabolites, and, secondly, to compare the clinical effects of midazolam and triazolam in doses yielding the same duration of action (15 mg and 0.25 mg, respectively). 2 In a randomized, cross-over procedure, six healthy volunteers received one of the following in the morning at approximately weekly intervals: 15 mg midazolam; 9 mg a-hydroxy midazolam; 1 mg triazolam; 1 mg a-hydroxy triazolam; 1 mg 4-hydroxy triazolam. Tests of drug effect (investigator's assessment, psychometric testing, and self-rating by subjects) were carried out at different times in the 24-h period following administration. Triazolam 0.25 mg was also studied in four of these six subjects to supplement the findings in the cross-over study. 3 Triazolam mg was shown to have the strongest, most long-lasting'effect. Midazolam 15 mg had almost the same intensity of effect but this was shorter lasting, i.e. 5 h as against 10 h for 1 mg triazolam. The a-hydroxy metabolites had a duration of action about half that of the parent compounds and a less potent effect, and 4-hydroxy triazolam was virtually devoid of effect. The lower 0.25-mg dose of triazolam had about the same duration of action as 15 mg midazolam but did not achieve the same degree of maximum effect as measured by psychometric tests and self-assessment by subjects. 4 The findings of this study indicate that midazolam would be suitable for use in situations in which a brief but intense hypnotic sedative effect is desired.

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The pharmacokinetics of midazolam in man

Cited by 255 publications

References 4 publications

A Comparison of Dexmedetomidine and Midazolam for Sedation in Gynecologic Surgery Under Epidural Anesthesia

A Comparison of Dexmedetomidine and Midazolam for Sedation in Gynecologic Surgery Under Epidural Anesthesia

The pharmacokinetics of midazolam in patients with congestive heart failure.

Comparison of the effects of intravenously administered midazolam, triazolam and their hydroxy metabolites.

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