ACEPROMAZINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H22N2OS
Molecular Weight	326.456
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)CCCN1C2=C(SC3=C1C=C(C=C3)C(C)=O)C=CC=C2

InChI

InChIKey=NOSIYYJFMPDDSA-UHFFFAOYSA-N

InChI=1S/C19H22N2OS/c1-14(22)15-9-10-19-17(13-15)21(12-6-11-20(2)3)16-7-4-5-8-18(16)23-19/h4-5,7-10,13H,6,11-12H2,1-3H3

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Description
Sources: https://www.drugs.com/vet/acepromazine-maleate-injection.html | https://www.petmd.com/pet-medication/acepromazine

Acepromazine a potent neuroleptic agent with a low order of toxicity, is of particular value in the tranquilization of dogs, cats and horses. Its rapid action and lack of hypnotic effect are added advantages. Acepromazine is a commonly used tranquilizer/sedative in dogs, cats, horses, and other animals. Veterinarians typically prescribe acepromazine to quiet agitated animals or use it as a part of an anesthetic protocol. It is important to note that when used alone, acepromazine is not an effective pain reliever and does little if anything to relieve a pet’s anxiety or fear. Acepromazine can also be used to treat motion sickness and nausea associated with car or plane rides. The mechanism by which acepromazine decreases a pet’s alertness is not fully understood. It is thought to block dopamine receptors in the brain or inhibit the activity of dopamine in other ways.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dopamine receptor 60 Target ID: CHEMBL2096905 Sources: https://www.petmd.com/pet-medication/acepromazine \| https://www.drugbank.ca/drugs/DB01614	Antagonist 2778
neurological system process 6 Target ID: GO:0050877 Sources: https://www.drugs.com/vet/acepromazine-maleate-injection.html \| https://www.petmd.com/pet-medication/acepromazine	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Agitation (veterinary) 3 Sources: https://www.drugs.com/vet/acepromazine-maleate-injection.html https://www.petmd.com/pet-medication/acepromazine	Primary		Approved 8429	ACEPROMAZINE MALEATE Approved Use Actions: Acepromazine maleate has a depressant effect on the central nervous system and therefore, causes sedation, muscular relaxation and a reduction in spontaneous activity. It acts rapidly, exerting a prompt and pronounced calming effect. Indications: Dogs and Cats: Acepromazine Maleate Injection can be used as an aid in controlling intractable animals during examination, treatment, grooming, x-ray and minor surgical procedures; to alleviate itching as a result of skin irritation; as an antiemetic to control vomiting associated with motion sickness. Acepromazine Maleate Injection is particularly useful as a preanesthetic agent (1) to enhance and prolong the effects of barbiturates, thus reducing the requirements for general anesthesia; (2) as an adjunct to surgery under local anesthesia. Horses: Acepromazine Maleate Injection can be used as an aid in controlling fractious animals during examination, treatment, loading and transportation. Particularly useful when used in conjunction with local anesthesia for firing, castration, neurectomy, removal of skin tumors, ocular surgery and applying casts.
Schizophrenia 298 Sources: https://www.ncbi.nlm.nih.gov/pubmed/13536530	Primary		Not Provided 504	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Comparisons of the effects of anesthesia and stress on release of tumor necrosis factor-alpha, leptin, and nitric oxide in adult male rats.	2001 Apr	11368420
Effects of hydromorphone or oxymorphone, with or without acepromazine, on preanesthetic sedation, physiologic values, and histamine release in dogs.	2001 Apr 1	11318359
Effects of acetylpromazine or morphine on urine production in halothane-anesthetized dogs.	2001 Dec	11763182
Propofol and methohexital have no significant effect on mucus secretion or clearance in the anesthetized dog.	2001 May	11378620
Cardiopulmonary effects of three different anaesthesia protocols in cats.	2001 Nov	11765236
Survey on small animal anaesthesia.	2001 Sep	11702932
Pulp histology after Er:YAG laser cavity preparation in subhuman primates--a pilot study.	2002 Aug	12428525
Intraocular pressure and tear production in five herbivorous wildlife species.	2002 Aug 31	12233828
Effects of treatment with oxytocin, xylazine butorphanol, guaifenesin, acepromazine, and detomidine on esophageal manometric pressure in conscious horses.	2002 Dec	12492291
In vitro effects of oxytocin, acepromazine, detomidine, xylazine, butorphanol, terbutaline, isoproterenol, and dantrolene on smooth and skeletal muscles of the equine esophagus.	2002 Dec	12492290
Effect of acepromazine and butorphanol on isoflurane minimum alveolar concentration in goats.	2002 Feb	11874529
Mask induction of anaesthesia with isoflurane or sevoflurane in premedicated cats.	2002 Jan	11833817
The effects of xylazine, detomidine, acepromazine and butorphanol on equine solid phase gastric emptying rate.	2002 Jul	12358052
Physiology and behavior of dogs during air transport.	2002 Jul	12146895
Murine models of chronic Pseudomonas aeruginosa lung infection.	2002 Jul	12144741
Comparison between meloxicam and carprofen for postoperative analgesia after feline ovariohysterectomy.	2002 Jul	12137147
Cerebral blood volume measurements by rapid contrast infusion and T2*-weighted echo planar MRI.	2002 Jun	12111961
Development of a mouse model to determine the systemic activity of potential flea-control compounds.	2002 Mar 20	11812623
Effects of carprofen on renal function and results of serum biochemical and hematologic analyses in anesthetized dogs that had low blood pressure during anesthesia.	2002 May	12013473
Effects of preoperative administration of ketoprofen on anesthetic requirements and signs of postoperative pain in dogs undergoing elective ovariohysterectomy.	2002 Nov 1	12418691
Reduced resident time and pharmacodynamic effects of acepromazine after subclinical multiple dosage in exercised thoroughbreds.	2002 Oct	12423229
The effects of doxapram hydrochloride (dopram-V) on laryngeal function in healthy dogs.	2002 Sep-Oct	12322700
Effects of two preanesthetic regimens for ophthalmic surgery on intraocular pressure and cardiovascular measurements in dogs.	2002 Spring	12050831
The sedative and behavioral effects of nalbuphine in dogs.	2003 Jul	12906398
Changes in intraocular pressure and pupil size following intramuscular administration of hydromorphone hydrochloride and acepromazine in clinically normal dogs.	2003 Mar	12641847
Inhibition has little effect on response latencies in the inferior colliculus.	2003 Mar	12183767
Effects of acepromazine on renal function in anesthetized dogs.	2003 May	12755300
Analysis of phenothiazine and its derivatives using LC/electrochemistry/MS and LC/electrochemistry/fluorescence.	2003 Sep 15	14674461
Development of a rapid screening test for veterinary sedatives and the beta-blocker carazolol in porcine kidney by ELISA.	2004 Feb	14752562
Comparison of preoperative carprofen and postoperative butorphanol as postsurgical analgesics in cats undergoing ovariohysterectomy.	2004 Jul	15268687
Intense (18)F-FDG uptake in brown fat can be reduced pharmacologically.	2004 Jul	15235065
Elevated nociceptive thresholds in rats with multifocal brain damage induced with single subcutaneous injections of lithium and pilocarpine.	2004 Jun	15209296
NF-kappaB p50 facilitates neutrophil accumulation during LPS-induced pulmonary inflammation.	2004 Jun 9	15189567
Effect of meloxicam and carprofen on renal function when administered to healthy dogs prior to anesthesia and painful stimulation.	2004 Oct	15524325
Neuroleptanalgesia in wild Asian elephants (Elephas maximus maximus).	2004 Oct	15509293
Effects of doxapram HCl on laryngeal function of normal dogs and dogs with naturally occurring laryngeal paralysis.	2004 Oct	15509290
Effects of chronic baroreceptor unloading on blood pressure in the dog.	2005 Apr	15563576
Overdose during chemical restraint in a black rhinoceros (Diceros bicornis).	2005 Jan	15663740
Muscle metabolic changes associated with long-term inhalation anaesthesia in the horse analysed by muscle biopsy and microdialysis techniques.	2005 Mar	15737180
Results of 24-hour ambulatory electrocardiography in dogs undergoing ovariohysterectomy following premedication with medetomidine or acepromazine.	2005 Mar 1	15776946

Patents

Sample Use Guides

In Vivo Use Guide

Acepromazine Maleate Injection may be given intravenously, intramuscularly or subcutaneously. The following schedule may be used as a guide to IV, IM or SC injections: Dogs: 0.25-0.5 mg/lb of body weight. Cats: 0.5-1 mg/lb of body weight. Horses: 2-4 mg/100 lb of body weight. 0.25 - 3 mg per kg body weight by oral administration.

Route of Administration: Other

In Vitro Use Guide

The crude extract of Chlamydia pneumoniae induced the differentiation of monocytes into macrophages in 45 ± 5% of the cells. Acepromazine significantly reduced the mean percentage of differentiated cells: with 10−5 M ACP, 18 ± % (p < 0.005) of the cells differentiated into macrophages and with 10−4 M the mean percentage of differentiated cells was equivalent to the control values: 5 ± 1% (p < 0.001). Viability of the differentiated and nondifferentiated THP-1 was = 98%.

Name

Type

Language

ACEPROMAZINE

Official Name

English

ATRAVET

Brand Name

English

CONCENTRAT VO34

Brand Name

English

ETHANONE, 1-(10-(3-(DIMETHYLAMINO)PROPYL)-10H-PHENOTHIAZIN-2-YL)-

Systematic Name

English

ACEPROMAZINE [MI]

Common Name

English

acepromazine [INN]

Common Name

English

ACEPROMAZINE [MART.]

Common Name

English

ACEZINE 2

Brand Name

English

ACETYLPROMAZINE

Common Name

English

10-(3-(DIMETHYLAMINO)PROPYL)PHENOTHIAZIN-2-YL METHYL KETONE

Systematic Name

English

ACP

Common Name

English

ACE

Common Name

English

Acepromazine [WHO-DD]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QN05AA04