ROMIFIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C9H9BrFN3
Molecular Weight	258.0901
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

c1cc(c(c(c1)F)NC2=NCCN2)Br

InChI

InChIKey=KDPNLRQZHDJRFU-UHFFFAOYSA-N

InChI=1S/C9H9BrFN3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14)

HIDE SMILES / InChI

Molecular Formula	C9H9BrFN3
Molecular Weight	258.0901
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.fda.gov/ohrms/dockets/98fr/141-229-fois001.pdf

Romifidine is an alpha2-adrenergic agonist, which as a sedative and analgesic in horses. The drug was approved by FDA under the name Sedivet. It has no use in humans.

CNS Activity

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Alpha-2B adrenergic receptor 13 Target ID: O77721 Gene ID: NA Gene Symbol: ADRA2B Target Organism: Equus caballus (Horse) Sources: https://www.fda.gov/ohrms/dockets/98fr/141-229-fois001.pdf	Agonist 2470

Conditions

Condition	Modality	Targets	Highest Phase	Product
Sedation 4 Sources: http://files.boehringer.com.au/files/CMI/Sedivet%20ANZ.pdf	Primary		Approved 8043	SEDIVET Approved Use For use as a sedative and analgesic to facilitate handling, clinical examinations, clinical procedures, and minor surgical procedures in adult horses; and for use as a preanesthetic prior to the induction of general anesthesia in adult horses. Launch Date 1.0862208E12

PubMed

Title	Date	PubMed
Romifidine-ketamine anaesthesia in atropine and triflupromazine pre-medicated buffalo calves.	2004 Dec	15610485
Effects of tiletamine/zolazepam-romifidine-atropine in ocelots (Leopardus pardalis).	2004 Jul	15268694
Sedative, analgesic and cardiorespiratory effects of romifidine in cats.	2004 Jul	15268691
A romifidine and morphine combination for epidural analgesia of the flank in cattle.	2004 Nov	15600157
Cardiopulmonary effects of romifidine/ketamine or xylazine/ketamine when used for short duration anesthesia in the horse.	2004 Oct	15581222
Comparison of morphine and butorphanol as pre-anaesthetic agents in combination with romifidine for field castration in ponies.	2005 Jan	15663735
Standing oral extraction of cheek teeth in 100 horses (1998--2003).	2005 Mar	15779621
Effects of acepromazine on pulmonary gas exchange and circulation during sedation and dissociative anaesthesia in horses.	2005 Mar	15762913
Effect of romifidine on the nociceptive withdrawal reflex and temporal summation in conscious horses.	2005 Nov	16334961
High inspired oxygen concentrations increase intrapulmonary shunt in anaesthetized horses.	2005 Nov	16297043
Romifidine or medetomidine premedication before propofol-sevoflurane anaesthesia in dogs.	2005 Oct	16207314
Characterization of the stereoselective biotransformation of ketamine to norketamine via determination of their enantiomers in equine plasma by capillary electrophoresis.	2005 Oct	16167314
Dissociative anaesthesia during field and hospital conditions for castration of colts.	2006	16722301
Heart rate responses during acclimation of horses to water treadmill exercise.	2006 Aug	17402403
Risk factors for colic in horses after general anaesthesia for MRI or nonabdominal surgery: absence of evidence of effect from perianaesthetic morphine.	2006 Jul	16866208
Effect of intratesticular injection of lidocaine on cardiovascular responses to castration in isoflurane-anesthetized stallions.	2006 Mar	16506900
A2-agonists in sheep: a review.	2006 Mar	16475998
[Alpha-2-agonists: everyday anesthetic treatment in veterinary medicine, but far from safe. The consequences of accidental self injection].	2006 Mar 15	16613236
Comparison of romifidine and medetomidine pre-medication in propofol-isoflurane anaesthetised dogs.	2006 Nov	17054484
Cardiorespiratory effects of desflurane in dogs given romifidine or medetomidine before induction of anesthesia with propofol.	2006 Oct	17042386
The use of alpha-2 agonists in the equine practice: comparison between three molecules.	2007 Aug	17682902
Pharmacokinetics of intramuscular ketamine in young ostriches premedicated with romifidine.	2007 Feb	17359455
The effects of detomidine, romifidine or acepromazine on echocardiographic measurements and cardiac function in normal horses.	2007 Jan	17238956
Bilateral Polydactyly in a foal.	2007 Jun	17519577
Evaluation of the anaesthetic effects of combinations of ketamine, medetomidine, romifidine and butorphanol in European badgers (Meles meles).	2007 Nov	17565574
Metabolism before, during and after anaesthesia in colic and healthy horses.	2007 Nov 15	18001483
Anaesthesia of pigs with a combination of romifidine, butorphanol and ketamine.	2008 Dec 13	19074790
Sparing effect of a low dose of intrathecal morphine on fentanyl requirements during spinal surgery: a preliminary clinical investigation in dogs.	2008 Feb	18251809
Epithelial expression of mRNA and protein for IL-6, IL-10 and TNF-alpha in endobronchial biopsies in horses with recurrent airway obstruction.	2008 Feb 23	18294392
Comparison of ketamine and S(+)-ketamine, with romifidine and diazepam, for total intravenous anesthesia in horses.	2008 Jan	17565569
Sedative and cardiorespiratory effects of three doses of romifidine in comparison with medetomidine in five cats.	2008 Jan 19	18204032
Effects of dobutamine on cardiovascular function and respiratory gas exchange after enoximone in isoflurane-anaesthetized ponies.	2008 Jul	19522889
Clinical evaluation of ketamine and lidocaine intravenous infusions to reduce isoflurane requirements in horses under general anaesthesia.	2008 Jul	19522888
A comparison of recovery times and characteristics with sevoflurane and isoflurane anaesthesia in horses undergoing magnetic resonance imaging.	2008 Sep	18466165
The influence of body mass and thoracic dimensions on arterial oxygenation in anaesthetized horses and ponies.	2008 Sep	18466164
Partial intravenous anaesthesia in 5 horses using ketamine, lidocaine, medetomidine and halothane.	2009 Dec	20458864
Comparison of the effects of the alpha-2 agonists detomidine, romifidine and xylazine on nociceptive withdrawal reflex and temporal summation in horses.	2009 Jul	19538573
Sedative and analgesic effects of romifidine in camels (Camelus dromedarius).	2009 Jul	19538572
Anaesthetic and cardiorespiratory effects of romifidine/ketamine combinations in cats.	2009 Jul	19470145
Castration of horses under total intravenous anaesthesia: analgesic effects of lidocaine.	2009 Mar	19239656
Influence of calcium chloride on the cardio-respiratory effects of a bolus of enoximone in isoflurane anaesthetized ponies.	2009 Mar	19239648
Alterations in the glutathione metabolism could be implicated in the ischemia-induced small intestinal cell damage in horses.	2009 Mar 18	19296836
Comparison between lithium dilution and pulse contour analysis techniques for cardiac output measurement in isoflurane anaesthetized ponies: influence of different inotropic drugs.	2009 May	19397771
Effect of sedation with detomidine and butorphanol on pulmonary gas exchange in the horse.	2009 May 7	19422714
Alfaxalone in cyclodextrin for induction and maintenance of anaesthesia in ponies undergoing field castration.	2009 Sep	19709052
Human exposures to immobilising agents: results of an online survey.	2010 Aug 28	20802186
Alpha-2 agonists as pain therapy in horses.	2010 Dec	21056297
Cardiovascular effects following epidural injection of romifidine in isoflurane-anaesthetized dogs.	2010 Mar	20230558
Effects of adding butorphanol to a balanced anaesthesia protocol during arthroscopic surgery in horses.	2010 Mar 13	20228366
Romifidine as a constant rate infusion in isoflurane anaesthetized horses: a clinical study.	2010 Sep	20712609

Patents

Sample Use Guides

In Vivo Use Guide

Sedative doses ranged between 30 and 100 mcg/kg; preanesthetic doses ranged between 40 and 100 mcg/kg.

Route of Administration: Intravenous

In Vitro Use Guide

Rat spinal cord preparations were treated with romifidine at concentrations from 1 to 1000 nM. The drug depressed both the high intensity and low intensity excitatory postsynaptic potential with EC50 value of 23.4 nM.

Substance Class	Chemical Created by `admin` on `Sat Jun 26 09:50:52 UTC 2021` Edited by `admin` on `Sat Jun 26 09:50:52 UTC 2021`
Record UNII	876351L05K
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ROMIFIDINE

Official Name

English

SEDIVET

Brand Name

English

ROMIFIDINE [MART.]

Common Name

English

ROMIFIDINE [MI]

Common Name

English

ROMIFIDINE [INN]

Common Name

English

Classification Tree Code System Code

CFR

21 CFR 522.2076