ROMIFIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C9H9BrFN3
Molecular Weight	258.09
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

FC1=CC=CC(Br)=C1NC2=NCCN2

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)

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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 2678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Sedation 4 Sources: http://files.boehringer.com.au/files/CMI/Sedivet%20ANZ.pdf	Primary		Approved 8429	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 2004

PubMed

Title	Date	PubMed
Effect of two anaesthetic regimens on airway nitric oxide production in horses.	2001 Jan	11575389
Analgesic and cardiopulmonary effects of intrathecally administered romifidine or romifidine and ketamine in goats (Capra hircus).	2001 Jun	11513266
Effect of romifidine on gastrointestinal motility, assessed by transrectal ultrasonography.	2001 Nov	11720028
Comparison of the cardiopulmonary effects of anesthesia maintained by continuous infusion of romifidine, guaifenesin, and ketamine with anesthesia maintained by inhalation of halothane in horses.	2002 Dec	12492279
A comparison of the antinociceptive effects of xylazine, detomidine and romifidine on experimental pain in horses.	2003 Jul	14498850
Problems associated with perioperative morphine in horses: a retrospective case analysis.	2003 Jul	14498846
[Standing behavior in horses after inhalation anesthesia with isoflurane (Isoflo) and postanesthetic sedation with romifidine (Sedivet) or xylazine (Rompun)].	2003 Jun	12866257
Effects of alpha-2 adrenoceptor agonists during recovery from isoflurane anaesthesia in horses.	2003 Mar	12638794
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
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
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
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
The effects of detomidine, romifidine or acepromazine on echocardiographic measurements and cardiac function in normal horses.	2007 Jan	17238956
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
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
Partial intravenous anaesthesia in 5 horses using ketamine, lidocaine, medetomidine and halothane.	2009 Dec	20458864
Anaesthetic and cardiorespiratory effects of romifidine/ketamine combinations in cats.	2009 Jul	19470145
Influence of calcium chloride on the cardio-respiratory effects of a bolus of enoximone in isoflurane anaesthetized ponies.	2009 Mar	19239648
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
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.

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