Midazolam pharmacokinetics following intravenous and buccal administration

被引:77
作者
Schwagmeier, R
Alincic, S
Striebel, HW
机构
[1] Free Univ Berlin, Benjamin Franklin Med Ctr, Dept Anesthesiol & Intens Care Med, D-1000 Berlin, Germany
[2] Goethe Univ Frankfurt, Teaching Hosp, Muncipal Hosp Frankfurt Hochst, Dept Anaesthesiol Intens Care & Emergency Med, Frankfurt, Germany
关键词
buccal; intravenous; midazolam; pharmacokinetics;
D O I
10.1046/j.1365-2125.1998.00781.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Aims Midazolam has good anxiolytic qualities and is a well established premedication agent before anaesthesia or short surgical procedures. The objective of the present study was to determine pharmacokinetic data from individual plasma concentration profiles obtained following intravenous and buccal administration of midazolam. Methods Eight young healthy volunteers received single doses of 5 mg midazolam i.v. and after a period of 1 week buccally in a cross over manner. Blood samples were obtained up to 480 min. The measurement of plasma midazolam concentrations was by gas-chromatography. Results The maximum plasma concentration was 55.9 ng ml(-1) (range 35.6-77.9 ng.ml(-1)) at 30 min (range 15-90 min) following bucca! administration. AUC was calculated to be 15016 ng ml(-1) min (s.d. 3778 ng ml(-1) min) following i.v. and 11191 ng ml(-1) min (s.d. 1777 ng ml(-1) min) following buccal midazolam. This gave a mean midazolam bioavailabilty of 74.5%. Conclusions The pharmacokinetic data presented in this study demonstrate a high bioavailability and reliable plasma concentrations following buccal midazolam. The clinical benefit of buccal midazolam may be in particular patient controlled premedication or sedation in adults.
引用
收藏
页码:203 / 206
页数:4
相关论文
共 20 条
[1]   MIDAZOLAM KINETICS [J].
ALLONEN, H ;
ZIEGLER, G ;
KLOTZ, U .
CLINICAL PHARMACOLOGY & THERAPEUTICS, 1981, 30 (05) :653-661
[2]  
[Anonymous], ADV PAIN RES THERAPY
[3]   INTRANASAL MIDAZOLAM FOR RAPIDLY SEDATING AN ADULT PATIENT [J].
CHENG, ACK .
ANESTHESIA AND ANALGESIA, 1993, 76 (04) :904-904
[4]   DRUG ABSORPTION BY SUBLINGUAL AND RECTAL ROUTES [J].
DEBOER, AG ;
DELEEDE, LGJ ;
BREIMER, DD .
BRITISH JOURNAL OF ANAESTHESIA, 1984, 56 (01) :69-82
[5]   EFFECT OF AGE, GENDER, AND OBESITY ON MIDAZOLAM KINETICS [J].
GREENBLATT, DJ ;
ABERNETHY, DR ;
LOCNISKAR, A ;
HARMATZ, JS ;
LIMJUCO, RA ;
SHADER, RI .
ANESTHESIOLOGY, 1984, 61 (01) :27-35
[6]   AUTOMATED GAS-CHROMATOGRAPHY FOR STUDIES OF MIDAZOLAM PHARMACOKINETICS [J].
GREENBLATT, DJ ;
LOCNISKAR, A ;
OCHS, HR ;
LAUVEN, PM .
ANESTHESIOLOGY, 1981, 55 (02) :176-179
[7]  
HUSSAIN A, 1989, J PHARM SCI, V79, P261
[8]   TRANSMUCOSAL ADMINISTRATION OF MIDAZOLAM FOR PREMEDICATION OF PEDIATRIC-PATIENTS - COMPARISON OF THE NASAL AND SUBLINGUAL ROUTES [J].
KARL, HW ;
ROSENBERGER, JL ;
LARACH, MG ;
RUFFLE, JM .
ANESTHESIOLOGY, 1993, 78 (05) :885-891
[9]   PLASMA-CONCENTRATIONS OF MIDAZOLAM AFTER .4. NASAL OR RECTAL ADMINISTRATION IN CHILDREN [J].
MALINOVSKY, JM ;
LEJUS, C ;
SERVIN, F ;
LEPAGE, JY ;
LENORMAND, Y ;
TESTA, S ;
COZIAN, A ;
PINAUD, M .
BRITISH JOURNAL OF ANAESTHESIA, 1993, 70 (06) :617-620
[10]   INTRANASAL MIDAZOLAM FOR CLAUSTROPHOBIA IN MRI [J].
MOSS, ML ;
BUONGIORNO, PA ;
CLANCY, VA .
JOURNAL OF COMPUTER ASSISTED TOMOGRAPHY, 1993, 17 (06) :991-992