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
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
Cardiovascular effects of romifidine in the standing horse.	2002 Apr	12027592
Evaluation of sedative and cardiorespiratory effects of romifidine and romifidine-butorphanol in cats.	2002 Aug 15	12184699
Analgesic, sedative and haemodynamic effects of spinally administered romifidine in female goats.	2002 Feb	11913823
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
The echocardiographic effects of romifidine in dogs with and without prior or concurrent administration of glycopyrrolate.	2003 Oct	12925178
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
Effects of acepromazine on pulmonary gas exchange and circulation during sedation and dissociative anaesthesia in horses.	2005 Mar	15762913
Romifidine or medetomidine premedication before propofol-sevoflurane anaesthesia in dogs.	2005 Oct	16207314
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
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
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
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
The influence of body mass and thoracic dimensions on arterial oxygenation in anaesthetized horses and ponies.	2008 Sep	18466164
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
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
Effect of sedation with detomidine and butorphanol on pulmonary gas exchange in the horse.	2009 May 7	19422714
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

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