First human administration of mr04a3: A novel water-soluble nonbenzodiazepine sedative

Anesthesiology

Volumn 116, Issue 2, 2012, Pages 385-395

  Sneyd, J Robert ^a   Rigby Jones, Ann E ^b   Cross, Maurice ^c   Tominaga, Hideharu ^d   Shimizu, Satoshi ^d   Ohkura, Takako ^d   Grimsehl, Karen ^e  

^a UNIVERSITY OF PLYMOUTH   (United Kingdom)

^b PENINSULA MEDICAL SCHOOL   (United Kingdom)

^c Pharmaceutical Physician Veeda Limited   (United Kingdom)

^d Maruishi Pharmaceutical Co Ltd   (United Kingdom)

^e DERRIFORD HOSPITAL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

MR 04A 3; PLACEBO; SEDATIVE AGENT; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTERIAL PRESSURE; ARTICLE; BISPECTRAL INDEX; CENTRAL NERVOUS SYSTEM; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG EFFECT; DRUG SAFETY; HEART RATE; HUMAN; HYPNOSIS; MAJOR CLINICAL STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; SEDATION; SIDE EFFECT; SYSTOLIC BLOOD PRESSURE; UPPER RESPIRATORY TRACT OBSTRUCTION;

ADOLESCENT; ADULT; BENZODIAZEPINES; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; HYPNOTICS AND SEDATIVES; ISOINDOLES; MALE; PIPERAZINES; SOLUBILITY; WATER; YOUNG ADULT;

EID: 84856447491     PISSN: 00033022     EISSN: 15281175     Source Type: Journal    
DOI: 10.1097/ALN.0b013e318242b2af     Document Type: Article

References (32)

1. Mould DR, DeFeo TM, Reele S, Milla G, Limjuco R, Crews T, Choma N, Patel IH: Simultaneous modeling of the pharmacokinetics and pharmacodynamics of midazolam and diazepam. Clin Pharmacol Ther 1995; 58:35-43
2. Aitkenhead AR, Pepperman ML, Willatts SM, Coates PD, Park GR, Bodenham AR, Collins CH, Smith MB, Ledingham IM, Wallace PG: Comparison of propofol and midazolam for sedation in critically ill patients. Lancet 1989; 2:704-9 (Pubitemid 19243114)
3. Bührer M, Maitre PO, Crevoisier C, Stanski DR: Electroencephalographic effects of benzodiazepinE.S. II. Pharmacodynamic modeling of the electroencephalographic effects of midazolam and diazepam. Clin Pharmacol Ther 1990; 48: 555-67
4. Staretz LR, Otomo-Corgel J, Lin JI: Effects of intravenous midazolam and diazepam on patient response, percentage of oxygen saturation, and hemodynamic factors during periodontal surgery. J Periodontol 2004; 75:1319-26 (Pubitemid 39517369)
5. Mitchell AR, Chalil S, Boodhoo L, Bordoli G, Patel N, Sulke N: Diazepam or midazolam for external DC cardioversion (the DORM Study). Europace 2003; 5:391-5 (Pubitemid 37336968)
6. Brouillette DE, Leventhal R, Kumar S, Berman D, Kajani M, Yoo YK, Carra J, Tarter R, Van Thiel DH: Midazolam versus diazepam for combined esophogastroduodenoscopy and colonoscopy. Dig Dis Sci 1989; 34:1265-71 (Pubitemid 19202122)
7. Korttila K, Tarkkanen J: Comparison of diazepam and midazolam for sedation during local anaesthesia for bronchoscopy. Br J Anaesth 1985; 57:581-6 (Pubitemid 15058088)
8. Zakko SF, Seifert HA, Gross JB: A comparison of midazolam and diazepam for conscious sedation during colonoscopy in a prospective double-blind study. Gastrointest Endosc 1999; 49:684-9 (Pubitemid 29269664)
9. van Gerven JM, Roncari G, Schoemaker RC, Massarella J, Keesmaat P, Kooyman H, Heizmann P, Zell M, Cohen AF, Dingemanse J: Integrated pharmacokinetics and pharmacodynamics of Ro 48-8684, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects. Br J Clin Pharmacol 1997; 44:487-93 (Pubitemid 27485480)
10. Dingemanse J, van Gerven JM, Schoemaker RC, Roncari G, Oberyé JJ, van Oostenbruggen MF, Massarella J, Segala P, Zell M, Cohen AF: Integrated pharmacokinetics and pharmacodynamics of Ro 48-6791, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects. Br J Clin Pharmacol 1997; 44:477-86 (Pubitemid 27485479)
11. Baker MT, Naguib M: Propofol: The challenges of formulation. Anesthesiology 2005; 103:860-76 (Pubitemid 41415536)
12. Kanamitsu N, Osaki T, Itsuji Y, Yoshimura M, Tsujimoto H, Soga M: Novel water-soluble sedative-hypnotic agents: Isoindolin-1-one derivativE.S. Chem Pharm Bull 2007; 55:1682-8 (Pubitemid 350232538)
13. Takamatsu I, Sekiguchi M, Yonamine R, Wada K, Kazama T: The effect of a new water-soluble sedative-hypnotic drug, JM-1232(-), on long-term potentiation in the CA1 region of the mouse hippocampus. Anesth Analg 2011; 113:1043-9
14. Chiba S, Nishiyama T, Yamada Y: The antinociceptive effects and pharmacological properties of JM-1232(-): A novel isoindoline derivative. Anesth Analg 2009; 108:1008-14
15. Nishiyama T, Chiba S, Yamada Y: Antinociceptive property of intrathecal and intraperitoneal administration of a novel water-soluble isoindolin-1-one derivative, JM-1232(-) in rats. Eur J Pharmacol 2008; 596:56-61
16. Ramsay MA, Savege TM, Simpson BR, Goodwin R: Controlled sedation with alphaxalone-alphadolone. BMJ 1974; 2:656-9
17. Anderson BJ, Holford NH: Mechanistic basis of using body size and maturation to predict clearance in humans. Drug Metab Pharmacokinet 2009; 24:25-36
18. Struys MM, Coppens MJ, De Neve N, Mortier EP, Doufas AG, Van Bocxlaer JF, Shafer SL: Influence of administration rate on propofol plasma-effect site equilibration. Anesthesiology 2007; 107:386-96 (Pubitemid 47329536)
19. Masui K, Kira M, Kazama T, Hagihira S, Mortier EP, Struys MM: Early phase pharmacokinetics but not pharmacodynamics are influenced by propofol infusion rate. Anesthesiology 2009; 111:805-17
20. Varvel JR, Donoho DL, Shafer SL: Measuring the predictive performance of computer-controlled infusion pumps. J Pharmacokinet Biopharm 1992; 20:63-94
21. Holford NH, Peace KE: Results and validation of a population pharmacodynamic model for cognitive effects in Alzheimer patients treated with tacrine. Proc Natl Acad Sci U S A 1992; 89:11471-5
22. Absalom AR, Lee M, Menon DK, Sharar SR, De Smet T, Halliday J, Ogden M, Corlett P, Honey GD, Fletcher PC: Predictive performance of the Domino, Hijazi, and Clements models during low-dose target-controlled ketamine infusions in healthy volunteers. Br J Anaesth 2007; 98:615-23 (Pubitemid 47072615)
23. Avram MJ, Krejcie TC: Using front-end kinetics to optimize target-controlled drug infusions. Anesthesiology 2003; 99: 1078-86 (Pubitemid 37339452)
24. Billard V, Gambus PL, Chamoun N, Stanski DR, Shafer SL: A comparison of spectral edge, delta power, and bispectral index as EEG measures of alfentanil, propofol, and midazolam drug effect. Clin Pharmacol Ther 1997; 61:45-58 (Pubitemid 27072883)
25. Breimer LT, Burm AG, Danhof M, Hennis PJ, Vletter AA, de Voogt JW, Spierdijk J, Bovill JG: Pharmacokinetic-pharmacodynamic modelling of the interaction between flumazenil and midazolam in volunteers by aperiodic EEG analysis. Clin Pharmacokinet 1991; 20:497-508
26. Lu JF, Chen G, Xiang BR, An DK: Pharmacokinetic-pharmacodynamic modeling of electroencephalographic effects of midazolam in eight Chinese men. Zhongguo Yao Li Xue Bao 1994; 15:399-403 (Pubitemid 24285286)
27. Kazama T, Ikeda K, Morita K, Kikura M, Doi M, Ikeda T, Kurita T, Nakajima Y: Comparison of the effect-site k(eO)s of propofol for blood pressure and EEG bispectral index in elderly and younger patients. Anesthesiology 1999; 90: 1517-27 (Pubitemid 29254793)
28. Marsh B, White M, Morton N, Kenny GN: Pharmacokinetic model driven infusion of propofol in children. Br J Anaesth 1991; 67:41-8
29. Schnider TW, Minto CF, Gambus PL, Andresen C, Goodale DB, Shafer SL, Youngs EJ: The influence of method of administration and covariates on the pharmacokinetics of propofol in adult volunteers. Anesthesiology 1998; 88:1170-82 (Pubitemid 28216859)
30. White M, Schenkels MJ, Engbers FH, Vletter A, Burm AG, Bovill JG, Kenny GN: Effect-site modelling of propofol using auditory evoked potentials. Br J Anaesth 1999; 82:333-9 (Pubitemid 29112531)
31. Scott RP, Saunders DA, Norman J: Propofol: Clinical strategies for preventing the pain of injection. Anaesthesia 1988; 43:492-4
32. Dingemanse J, Häussler J, Hering W, Ihmsen H, Albrecht S, Zell M, Schwilden H, Schüttler J: Pharmacokinetic-pharmacodynamic modelling of the EEG effects of Ro 48-6791, a new short-acting benzodiazepine, in young and elderly subjects. Br J Anaesth 1997; 79:567-74 (Pubitemid 27493663)