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Romifidine

目录号 : GC67683

Romifidine 是 α2 肾上腺素受体激动剂。Romifidine 在体内显示出镇定作用。

Romifidine Chemical Structure

Cas No.:65896-16-4

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10mg
¥2,340.00
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产品描述

Romifidine is an α2 adrenergic receptor agonist. Romifidine shows sedation effects in vivo[1][2].

Romifidine (80 μg/kg; i.v. once) produces sedative effects with significantly greater drooping during the 45-90 min time period in welsh mountain ponies[1].
Romifidine (40, 80 and 120 mg/kg; i.v. at seven-day intervals) shows a shallower and shorter-lived sedation than with detomidine in horses[2].

[1]. England GC, et al. A comparison of the sedative effects of three alpha 2-adrenoceptor agonists (romifidine, detomidine and xylazine) in the horse. J Vet Pharmacol Ther. 1992 Jun;15(2):194-201.
[2]. Hamm D, et al. Sedative and analgesic effects of detomidine and romifidine in horses. Vet Rec. 1995 Apr 1;136(13):324-7.

Chemical Properties

Cas No. 65896-16-4 SDF Download SDF
分子式 C9H9BrFN3 分子量 258.09
溶解度 DMSO : 250 mg/mL (968.65 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mM 3.8746 mL 19.3731 mL 38.7462 mL
5 mM 0.7749 mL 3.8746 mL 7.7492 mL
10 mM 0.3875 mL 1.9373 mL 3.8746 mL
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Research Update

Comparative evaluation of sedative and anti-nociceptive effects of epidural Romifidine, romifidine-lidocaine, and lidocaine in donkeys ( Equus asinus)

Front Vet Sci 2022 Dec 1;9:966715.PMID:36570502DOI:10.3389/fvets.2022.966715.

Background: Local and regional anesthetic procedures are valuable tools in veterinary practice. Caudal epidural administration of local anesthetic agents is widely reported for surgical interventions of the tail, anus, rectum, vulva, vagina, urethra, and bladder in the standing horse. Epidural analgesia is also obtained using various drugs such as alpha-2 adrenoceptor agonists, dissociative anesthetics, and opioids. The present study evaluates the anti-nociceptive and sedative effects of epidural administration of Romifidine, a romifidine-lidocaine combination, and lidocaine alone in donkeys. Materials and methods: In a randomized prospective study, twenty-four healthy adult donkeys were assigned to four groups (three experimental and one control; n = 6) received either 50 μg/kg of Romifidine, 0.30 mg/kg of lidocaine, combined Romifidine (50 μg/kg) and lidocaine (0.30 mg/kg) diluted in 0.9% sterile normal saline solution to a total injection volume of 12 ml, or an equivalent volume of sterile saline epidurally. After epidural injection of each treatment, the onset, degree, and duration of sedation and anatomical extension of anti-nociception were documented. Observations began immediately (time 0) pre-administration and at 5, 15, 30, 45, 60, and 30-min intervals subsequently until 210 min after drug injection. Time to onset of perineal analgesia was documented every minute after the epidural injection by evaluating the animal's response to pinpricks. Results: Only Romifidine and romifidine-lidocaine induced mild to moderate sedation. Romifidine, romifidine-lidocaine, and lidocaine induced complete bilateral caudal epidural analgesia with loss of sensation in the perineum, tail, inguinal region, caudal aspect of the upper hind limb, chest areas, and extended distally to the dorsal metatarsal area. Sedation lasted longer (p < 0.05) with Romifidine (160 ± 15.4 min) than with romifidine-lidocaine (141.6 ± 13.2 min). Longer-lasting analgesia (p < 0.05) was obtained with Romifidine (158.3 ± 9.8 min) and romifidine-lidocaine (165 ± 9.4 min) than with lidocaine (75.8 ± 8 min). Conclusions: Epidural administration of a single dose of Romifidine or a combination of romifidine-lidocaine produced mild to moderate sedation and complete anti-nociception in the perineal and inguinal regions of donkeys. The clinical usefulness of epidural Romifidine or romifidine-lidocaine combinations to perform obstetric procedures in donkeys needs to be assessed.

Romifidine and low doses of tiletamine-zolazepam in dogs

Vet Anaesth Analg 2013 Nov;40(6):e40-7.PMID:23782643DOI:10.1111/vaa.12054.

Objective: To evaluate clinical effects of Romifidine and low doses of tiletamine-zolazepam (TZ) in dogs. Study design: Randomized "blinded" cross-over study. Animals: Six healthy beagle dogs (two males, four females). Methods: In separate preliminary experiments dogs received intravenous (IV) tiletamine-zolazepam (TZ) at 1 and 2 mg kg(-1). For the main trial, dogs received Romifidine (R) followed 5 minutes later by IV at six dose regimens: R40TZ1, R60TZ1, R80TZ1 (Romifidine at 40, 60, 80 μg kg(-1) and TZ at 1 mg kg(-1)), R40TZ2, R60TZ2 and R80TZ2 (Romifidine at 40, 60, 80 μg kg(-1) and TZ at 2 mg kg(-1)). Dogs underwent endotracheal intubation, but breathed room air. Cardiorespiratory variables were measured and arterial blood analyzed. Quality of sedation, duration of anaesthesia and time to recovery (TR) were recorded. Data were analysed by anova or Friedman test as relevant. Results: Endotracheal intubation was possible with all Romifidine/TZ combinations but not with TZ alone. Mean times (minutes) from TZ injection to return of pedal reflex were 1-3 minutes for TZ alone, and 9-17 minutes for Romifidine combinations. In the main trial (Romifidine combinations) mean time (minutes) to standing increased with increasing dosage (R40TZ1 13; R80TZ2 32). Five minutes after TZ administration, when compared with baseline arterial blood pressures and arterial carbon dioxide had increased, and respiratory rate, pH and arterial oxygen tensions decreased, these changes becoming statistically significant with the higher dose rates. One dog in R60TZ2 and three dogs in R80TZ2 became hypoxaemic. Conclusions and clinical relevance: Romifidine improves the quality and lengthens the duration of anaesthesia induced by TZ. The combination provides a suitable protocol for induction of or short-term anaesthesia in healthy dogs. However, the higher doses cause cardiovascular stimulation and respiratory depression, and precautions should be taken accordingly.

Development of a Romifidine constant rate infusion with or without butorphanol for standing sedation of horses

Vet Anaesth Analg 2012 Jan;39(1):12-20.PMID:22151873DOI:10.1111/j.1467-2995.2011.00681.x.

Objective: To determine constant rate infusion (CRI) protocols for Romifidine (R) and Romifidine combined with butorphanol (RB) resulting in constant sedation and Romifidine plasma concentrations. Study design: Blinded randomized crossover study. Animals: Ten adult research horses. Methods: Part I: After determining normal height of head above ground (HHAG = 100%), loading doses of Romifidine (80 μg kg(-1)) with butorphanol (RB: 18 μg kg(-1)) or saline (R) were given intravenously (IV). Immediately afterwards, a butorphanol (RB: 25 μg kg(-1) hour(-1)) or saline (R) CRI was administered for 2 hours. The HHAG was used as marker of sedation depth. Sedation was maintained for 2 hours by additional Romifidine (20 μg kg(-1) ) whenever HHAG > 50%. The dose rate of Romifidine (μg kg(-1) hour(-1)) required to maintain sedation was calculated for both treatments. Part II: After loading doses, the Romifidine CRIs derived from part I were administered in parallel to butorphanol (RB) or saline (R). Sedation and ataxia were evaluated periodically. Romifidine plasma concentrations were measured by HPLC-MS-MS at 0, 5, 10, 15, 30, 45, 60, 90, 105, and 120 minutes. Data were analyzed using paired t-test, Fisher's exact test, Wilcoxon signed rank test, and two-way anova for repeated measures (p < 0.05). Results: There was no significant difference in Romifidine requirements (R: 30; RB: 29 μg kg(-1) hour(-1)). CRI protocols leading to constant sedation were developed. Time to first additional Romifidine bolus was significantly longer in RB (mean ± SD, R: 38.5 ± 13.6; RB: 50.5 ± 11.7 minutes). Constant plasma concentrations of Romifidine were achieved during the second hour of CRI. Ataxia was greater when butorphanol was added. Conclusion: Romifidine bolus, followed by CRI, provided constant sedation assessed by HHAG. Butorphanol was ineffective in reducing Romifidine requirements in unstimulated horses, but prolonged the sedation caused by the initial Romifidine bolus. Clinical relevance: Both protocols need to be tested under clinical conditions.

Effects of detomidine or Romifidine during maintenance and recovery from isoflurane anaesthesia in horses

Vet Anaesth Analg 2022 Nov;49(6):624-633.PMID:36175293DOI:10.1016/j.vaa.2022.07.004.

Objective: To evaluate the effects of detomidine or Romifidine on cardiovascular function, isoflurane requirements and recovery quality in horses undergoing isoflurane anaesthesia. Study design: Prospective, randomized, blinded, clinical study. Animals: A total of 63 healthy horses undergoing elective surgery during general anaesthesia. Methods: Horses were randomly allocated to three groups of 21 animals each. In group R, horses were given Romifidine intravenously (IV) for premedication (80 μg kg-1), maintenance (40 μg kg-1 hour-1) and before recovery (20 μg kg-1). In group D2.5, horses were given detomidine IV for premedication (15 μg kg-1), maintenance (5 μg kg-1 hour-1) and before recovery (2.5 μg kg-1). In group D5, horses were given the same doses of detomidine IV for premedication and maintenance but 5 μg kg-1 prior to recovery. Premedication was combined with morphine IV (0.1 mg kg-1) in all groups. Cardiovascular and blood gas variables, expired fraction of isoflurane (Fe'Iso), dobutamine or ketamine requirements, recovery times, recovery events scores (from sternal to standing position) and visual analogue scale (VAS) were compared between groups using either anova followed by Tukey, Kruskal-Wallis followed by Bonferroni or chi-square tests, as appropriate (p < 0.05). Results: No significant differences were observed between groups for Fe'Iso, dobutamine or ketamine requirements and recovery times. Cardiovascular and blood gas measurements remained within physiological ranges for all groups. Group D5 horses had significantly worse scores for balance and coordination (p = 0.002), overall impression (p = 0.021) and final score (p = 0.008) than group R horses and significantly worse mean scores for VAS than the other groups (p = 0.002). Conclusions and clinical relevance: Detomidine or Romifidine constant rate infusion provided similar conditions for maintenance of anaesthesia. Higher doses of detomidine at the end of anaesthesia might decrease the recovery quality.

Dose-dependent effect of Romifidine on intraocular pressure in clinically healthy buffalo ( Bubalus bubalis)

Heliyon 2019 Dec 4;5(12):e02930.PMID:31867457DOI:10.1016/j.heliyon.2019.e02930.

In the present study, changes in intraocular pressure (IOP) associated with Romifidine sedation in buffalo were evaluated. Eighteen healthy adult, non-pregnant, buffalo without ocular abnormalities were used in a prospective randomized trial. Buffalo were allocated into three groups (six each). Buffalo in the treated groups received an intramuscular injection (IM) of Romifidine at 40 or 50 μg/kg. The control group was administrated an equivalent volume of sterile saline (0.9% NaCl; 0.4 ml/100 kg). Baseline IOP (T0) values were obtained using applanation tonometry. Immediately afterwards, Romifidine was administered and IOP values of both eyes were measured at 5, 15, 30, 45, 60, 90, 120, and 180 min post-administration. The pre-administration values (T0) of IOP for both the left and right eyes ranged from 30-36 (mean, 33 ± 1.5) mmHg and 30-35 (mean, 33.7 ± 1.4), respectively. IOP values decreased significantly after administration of both doses of Romifidine compared with the placebo (P < 0.01). Compared with the control, the IOP decreased significantly in animals treated with both doses from 5-90 min post-administration in both eyes (P < 0.05). In the right eye, the lowest IOP value in the Romifidine treated groups was observed at T30 (21.6 ± 1.0 and 23.3 ± 1.4 mmHg), respectively. In the left eye, the lowest IOP was observed at T60 (22.5 ± 3.0 and 23.3 ± 2.8 mmHg), respectively. In conclusion, Romifidine could be recommended as an alternative analgesic in buffalo, especially for ocular affections associated with increased IOP. A dose of 40 μg/kg could be used at a low cost.