Disease relevance of DETOMIDINE

• The functional alpha2-adrenoceptor antagonistic effect of MPV-1743 A III was demonstrated by studying the ability of orally administered MPV-1743 A III to reverse and prevent the alpha2-adrenoceptor agonist detomidine-induced mydriasis in rat [1].
• Prazosin somewhat inhibited but did not eliminate the hyperthermia seen with the very high doses of detomidine [2].
• Bradycardia (heart rate < 145 beats/min) was detected at each evaluation time in cats treated orally with detomidine and ketamine and in all cats treated i.m. Minimal differences among groups were detected for heart and respiratory rates, rectal temperature, and hemoglobin oxygen saturation [3].
• The BIS was calculated before (awake) and after (sedated) administration of detomidine (0.01 mg/kg of body weight, IV) and butorphanol (0.01 mg/kg, IV) [4].
• Results indicate that use of detomidine for CEA and CSA in mares probably induces local spinal and CNS effects, marked sedation, moderate ataxia, mild cardiopulmonary depression, and renal diuresis [5].

Psychiatry related information on DETOMIDINE

• Development and characterization of an equine behaviour chamber and the effects of amitraz and detomidine on spontaneous locomotor activity [6].
• Detomidine was a good analgesic in control animals; their pain thresholds were significantly elevated for about 60 minutes [7].
• Several alpha-2 adrenoceptor agonists reduce wakefulness and inhibit paradoxical sleep, whereas novel imidazoline derivatives, such as detomidine, display sedative and analgesic properties which have been related to the activation of central alpha-2 adrenoceptors [8].

High impact information on DETOMIDINE

• 5. In contrast to previous reports of the actions of alpha2-adrenoceptor agonists on the in vitro spinal cord preparation, at concentrations ten fold higher than the above EC50 values xylazine, romifidine, detomidine and dexmedetomidine depressed the initial population spike of motoneurons (MSR) [9].
• Approximately 68% of detomidine was bound to plasma protein and 53% was bound to red blood cells [10].
• Comparison of the effects of detomidine and xylazine on some alpha 2-adrenoceptor-mediated responses in the central and peripheral nervous systems [2].
• After i.v. administration of 3-100 micrograms/kg detomidine and 0.1-3 mg/kg xylazine to conscious rats, detomidine was more active in reducing the heart rate than in lowering the blood pressure [11].
• A low dose of detomidine into the vertebral artery was more effective than i.v. application in reducing blood pressure [11].

Chemical compound and disease context of DETOMIDINE

• The central alpha 2-adrenoceptor blocking effect of atipamezole (0.1 mg/kg per h s.c.) was confirmed to be at the same level after one, three or seven days' infusion, as assessed by measuring the antagonism of detomidine-induced mydriasis in the rat [12].
• One minute after the end of exercise, horses were treated i.v. with xylazine (2.2 mg/kg of body weight), detomidine (0.04 mg/kg), a combination of xylazine (2.2 mg/kg) and acepromazine (0.04 mg/kg), or saline (0.9% NaCl) solution [13].
• Romifidine led to more severe hypotension than detomidine, despite administration of dobutamine to more romifidine-treated horses [14].
• The nonselective alpha-adrenoceptor antagonist, tolazoline at 6 mg/kg, i.v., also prevented the detomidine-induced mydriasis [15].
• Epinephrine infusion did not modify the incidence of cardiac arrhythmias in detomidine-treated horses at the doses tested [16].

Biological context of DETOMIDINE

• In unanaesthetized rats, detomidine both caused sedation and induced complex changes in body temperature [2].
• Some effects of multiple administration of detomidine during the last trimester of equine pregnancy [17].
• Heart rate, respiratory rate, and cardiac output decreased following detomidine administration [18].
• Detomidine was administered throughout 10 pregnancies in eight mares [19].
• Influence of detomidine and buprenorphine on motor-evoked potentials in horses [20].

Anatomical context of DETOMIDINE

• It is concluded that detomidine is a potent and rather specific alpha 2-adrenoceptor agonist in the central and peripheral nervous systems [2].
• Detomidine caused a concentration-dependent inhibition of the twitch response in electrically stimulated mouse vas deferens with a pD2 value of 8 [21].
• Idazoxan (0.3 mg/kg i.v. and 0.03 mg/kg into the vertebral artery) antagonized the hypotensive and bradycardiac effects of detomidine injected into the femoral vein or vertebral artery, respectively [11].
• The effects of the selective alpha 2-adrenoceptor agonist detomidine on gastric acid secretion from pylorus-ligated and stomach-perfused rats have been investigated [22].
• The mares exhibited conductive disturbances 2 min after detomidine administration, but fetal heart rhythm remained regular [17].

Associations of DETOMIDINE with other chemical compounds

• The clinical relaxant effects on the proximal portion of the esophagus reported of drugs such as oxytocin, detomidine, and acepromazine may be the result of centrally mediated mechanisms [23].
• PROCEDURE: After premedication with detomidine (10 microg/kg, IV), anesthesia was induced with climazolam (0.06 mg/kg, IV) and ketamine (2.2 mg/kg, IV) and maintained with a constant rate infusion of detomidine (0.024 mg/kg/h), climazolam (0.036 mg/kg/h), and ketamine (2.4 mg/kg/h) [24].
• Reversal of sedative and clinicophysiological effects of epidural xylazine and detomidine with atipamezole and yohimbine in buffaloes (Bubalus bubalis) [25].
• Procedures-Standing horses were administered a nonsteroidal anti-inflammatory drug and a caudal epidural injection of detomidine hydrochloride and underwent laparoscopic cryptorchidectomy [26].
• In a double blind study, eight horses were treated intravenously at seven-day intervals with detomidine at doses of 10, 20 and 40 micrograms/kg, or with romifidine at doses of 40, 80 and 120 micrograms/kg, or with a placebo solution [27].

Gene context of DETOMIDINE

• The antibodies were raised in rabbits against a conjugate of detomidine and bovine thyroglobulin prepared by diazo reaction [28].

Analytical, diagnostic and therapeutic context of DETOMIDINE

• Evaluation of detomidine-induced analgesia in horses with chronic hoof pain [29].
• Detomidine produced a dose-dependent increase in HCT and a decrease in the subjective grade of hoof withdrawal response through 55 min after treatment [29].
• Slow injection (particularly of the low dose rates) and premedication with detomidine resulted in a longer time to collapse (median 46 seconds) [30].
• Radioimmunoassay of detomidine, a new benzylimidazole drug with analgesic sedation properties [28].
• METHODS: Six healthy, mature horses were sedated with an i.v. bolus of detomidine (0.02 mg/kg bwt) and butorphanol (0.02 mg/kg bwt) and instrumented to determine the changes in cardiopulmonary function, haematology, serum chemistry and PF values during and after pneumoperitoneum with CO2 to 15 mmHg pressure for standing laparoscopy [31].

References