New sedative in intensive care, dexmedetomidine hydrochloride (Precedex), its pharmacological characteristics and clinical study result

Folia Pharmacologica Japonica

Volumn 124, Issue 3, 2004, Pages 171-179

  Taiji, Kazuko ^a  

^a Abbott Japan Co Ltd   (Japan)

Author keywords

Analgesia; Dexmedetomidine hydrochloride; Intensive care; Sedation; 2 adrenoreceptor agonist

Indexed keywords

ALPHA 2 ADRENERGIC RECEPTOR; ALPHA 2 ADRENERGIC RECEPTOR STIMULATING AGENT; ALPHA 2A ADRENERGIC RECEPTOR; ATIPAMEZOLE; CAFFEINE; CHLORPROMAZINE; DEXMEDETOMIDINE; LEVOMEDETOMIDINE; MORPHINE; PROPOFOL; SEDATIVE AGENT; UNCLASSIFIED DRUG; ALPHA ADRENERGIC RECEPTOR STIMULATING AGENT; HYPNOTIC SEDATIVE AGENT;

BRAIN CORTEX; CLINICAL TRIAL; DOSE RESPONSE; DRUG EFFICACY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; HUMAN; HYPERTENSION; HYPOTENSION; INTENSIVE CARE; INTUBATION; JAPAN; LOCUS CERULEUS; RECEPTOR AFFINITY; REVIEW; RIGHTING REFLEX; SEDATION; ANIMAL; DRUG EFFECT; DRUG POTENTIATION; ESCAPE BEHAVIOR; MOTOR ACTIVITY; MOUSE; MULTICENTER STUDY; PAIN; PHASE 2 CLINICAL TRIAL; PHASE 3 CLINICAL TRIAL; RAT;

ADRENERGIC ALPHA-AGONISTS; ANIMALS; CLINICAL TRIALS, PHASE II; CLINICAL TRIALS, PHASE III; DEXMEDETOMIDINE; DOSE-RESPONSE RELATIONSHIP, DRUG; ESCAPE REACTION; HUMANS; HYPNOTICS AND SEDATIVES; INTENSIVE CARE; LOCUS COERULEUS; MICE; MOTOR ACTIVITY; MULTICENTER STUDIES; PAIN; RATS; RECEPTORS, ADRENERGIC, ALPHA-2;

EID: 4644262326     PISSN: 00155691     EISSN: None     Source Type: Journal    
DOI: 10.1254/fpj.124.171     Document Type: Review

References (30)

1. Aitkenhead AR. Analgesia and sedation in intensive care. Br J Anaesth. 1989;63:196-206.
2. Greenblatt DJ, Divoll M, Abernethy DR, Ochs HR, Shader RI. Clinical pharmacokinetics of the newer benzodiazepines. Clin Pharmacokinet. 1983;8:233-252.
3. Anesthesia. 2000;2:45-49.
4. Katsanoulas C. Concluding remarks: redefining intensive care unit sedation. International Congress and Symposium Series. 1998;221:83-88.
5. Mantz J, Singer M. Importance of patient orientation and rousability as components of intensive care unit sedation. International Congress and Symposium Series. 1998;221:23-29.
6. Aston-Jones G, Bloom FE. Activity of norepinephrine-containing locus coeruleus neurons in behaving rats anticipates fluctuations in the sleep-waking cycle. J Neurosci. 1981;1:876-886.
7. De Sarro GB, Ascioti C, Froio F, Libri V, Nistico G. Evidence that locus coeruleus is the site where clonidine and drugs acting at alpha 1- and alpha 2-adrenoceptors affect sleep and arousal mechanisms. Br J Pharmacol. 1987;90:675-685.
8. 2 agonist, is mediated in the locus coeruleus in rats. Anesthesiology. 1992;76:948-952.
9. MacMillan LB, Hein L, Smith MS, Piascik MT, Limbird LE. Central hypotensive effects of the alpha2a-adrenergic receptor subtype. Science. 1996;273:801-803.
10. Chabre O, Conklin BR, Brandon S, Bourne HR, Limbird LE. Coupling of the alpha 2A-adrenergic receptor to multiple G-proteins. A simple approach for estimating receptor-G-protein coupling efficiency in a transient expression system. J Biol Chem. 1994;269:5730-5734.
11. 2A-adrenergic receptor via "hit and run" gene targeting reveals the role of this subtype in sedative, analgesic, and anesthetic-sparing responses in vivo. Proc Natl Acad Sci USA. 1997;94:9950-9955.
12. Jorm CM, Stamford JA. Actions of the hypnotic anesthetic, dexmedetomidine, on noradrenaline release and cell firing in rat locus coeruleus slices. Br J Anesth. 1993;71:447-449.
13. Correa-Sales C, Nacif-Coelho C, Reid K, Maze M. Inhibition of adenylate cyclase in the locus coeruleus mediates the hypnotic response to an alpha-2 agonist in the rat. J Pharmacol Exp Ther. 1992;263:1046-1049.
14. Doze VA, Chen BX, Tinklenberg JA, Segal IS, Maze M. Pertussis toxin and 4-aminopyridine differentially affect the hypnotic-anesthetic action of dexmedetomidine and pentobarbital. Anesthesiology. 1990;73:304-307.
15. Sullivan AF, Kalso EA, McQuay HJ, Dickenson AH. The antinociceptive actions of dexmedetomidine on dorsal horn neuronal responses in the anesthetized rat. Eur J Pharmacol. 1992;215:127-133.
16. Guo TZ, Jiang JY, Buttermann AE, Maze M. Dexmedetomidine injection into the locus coeruleus produces antinociception. Anesthesiology. 1996;84:873-881.
17. 2 receptor agonist dexmedetomidine in dogs. Antinociception and carbon dioxide response. Anesthesiology. 1994;80:1057-1072.
18. Eddy NB, Leimbach D. Synthetic analgesics. II. Dithienylbutenyl- and dithienylbutylamines. J Pharmacol Exp Ther. 1953;107:385-393.
19. 3H-dexmedetomidine in healthy, adult volunteers. Dexmedetomidine Clinical Study Report DEX-96-018. 1997.
20. Virtanen R. The effects of dexmedetomidine N-glucuronides on alpha-2 adrenoceptors in vitro and in vivo. Orion CNS 97122100010. 1997.
21. 3H- clonidine binding by enantiomers of medetomidine in rat cerebrocortical membranes. Orion Corporation ORION PHARMA, 1988;November 7.
22. 2 adrenoceptor subtypes. Orion Corporation ORION PHARMA. 1992.
23. Gillon J-Y, Kato G, Allgoewer G et al. RECEPTO-GRAM™ OF SIX COMPOUNDS. Battelle-Europe, Geneva, Switzerland, 9 July 1992.
24. Roux S, Froger C, Hay AM et al. A-85499. 1 (I.V.) CNS General pharmacology profile in the mouse and the rat. R&D 96/500. 1996.