ACEPROMAZINE MALEATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H22N2OS.C4H4O4
Molecular Weight	442.528
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C/C(O)=O.CN(C)CCCN1C2=C(SC3=C1C=C(C=C3)C(C)=O)C=CC=C2

InChI

InChIKey=FQRHOOHLUYHMGG-BTJKTKAUSA-N

InChI=1S/C19H22N2OS.C4H4O4/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;5-3(6)1-2-4(7)8/h4-5,7-10,13H,6,11-12H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1-

HIDE SMILES / InChI

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
Effect of propofol at two injection rates or thiopentone on post-intubation apnoea in the dog.	2001 Feb	11263701
Prospective survey of tick paralysis in dogs.	2001 Jun	11491220
Normal spatial memory following postseizure treatment with ketamine: selective damage attenuates memory deficits in brain-damaged rodents.	2001 Mar	11328682
Propofol and methohexital have no significant effect on mucus secretion or clearance in the anesthetized dog.	2001 May	11378620
Human exposure to pet prescription medications.	2002 Aug	12136968
Cardiopulmonary effects of xylazine and acepromazine in pregnant cows in late gestation.	2002 Dec	12492284
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
Effects of preoperative administration of ketoprofen on anesthetic requirements and signs of postoperative pain in dogs undergoing elective ovariohysterectomy.	2002 Nov 1	12418691
Effects of two preanesthetic regimens for ophthalmic surgery on intraocular pressure and cardiovascular measurements in dogs.	2002 Spring	12050831
Postoperative hypoxemia and hypercarbia in healthy dogs undergoing routine ovariohysterectomy or castration and receiving butorphanol or hydromorphone for analgesia.	2003 Feb 1	12564595
The sedative and behavioral effects of nalbuphine in dogs.	2003 Jul	12906398
A comparison of the analgesic effects of butorphanol with those of meloxicam after elective ovariohysterectomy in dogs.	2003 Jul	12892286
Hypotensive effect of push-pull gravitational stress occurs after autonomic blockade.	2003 Jul	12794095
Changes in intraocular pressure and pupil size following intramuscular administration of hydromorphone hydrochloride and acepromazine in clinically normal dogs.	2003 Mar	12641847
Method for the noninvasive measurement of intraocular pressure in mice.	2003 Mar	12601041
Effects of acepromazine on renal function in anesthetized dogs.	2003 May	12755300
Orthologous gene-expression profiling in multi-species models: search for candidate genes.	2004	15128448
Investigation of the effect of acepromazine on intravenous glucose tolerance tests in dogs.	2004 Aug	15334847
Intense (18)F-FDG uptake in brown fat can be reduced pharmacologically.	2004 Jul	15235065
NF-kappaB p50 facilitates neutrophil accumulation during LPS-induced pulmonary inflammation.	2004 Jun 9	15189567
Effects of various anesthetic agents on laryngeal motion during laryngoscopy in normal dogs.	2004 Mar-Apr	15027970
An animal model for ultrasound lung imaging.	2004 May	15183237
Normal spatial and contextual learning for ketamine-treated rats in the pilocarpine epilepsy model.	2004 May	15159140
Sonographic features of drug-induced splenic congestion.	2004 May-Jun	15200260
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
Intentional overdose of Large Animal Immobilon.	2004 Oct	15359207
Effects of ovariohysterectomy on canine blood neutrophil respiratory burst: a chemiluminescence study.	2004 Sep-Oct	15362995
Therapeutic effects of Holmium-166 chitosan complex in rat brain tumor model.	2005 Feb 28	15744805
Effects of acepromazine on pulmonary gas exchange and circulation during sedation and dissociative anaesthesia in horses.	2005 Mar	15762913
Muscle metabolic changes associated with long-term inhalation anaesthesia in the horse analysed by muscle biopsy and microdialysis techniques.	2005 Mar	15737180
Analgesic efficacy of preoperative administration of meloxicam or butorphanol in onychectomized cats.	2005 Mar 15	15786993
Gamma scintigraphic evaluation of a miniaturized AERx pulmonary delivery system for aerosol delivery to anesthetized animals using a positive pressure ventilation system.	2005 Spring	15741772

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 MALEATE

Official Name

English

Acepromazine maleate [WHO-DD]

Common Name

English

ACEPROMAZINE MALEATE [MI]

Common Name

English

ACEPROMAZINE MALEATE [GREEN BOOK]

Common Name

English

NSC-264522

Code

English

10-[3-(Dimethylamino)propyl]phenothiazin-2-yl methyl ketone maleate (1:1)

Systematic Name

English

ACEPROMAZINE MALEATE [USAN]

Common Name

English

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

Systematic Name

English

ACEPROMAZINE MALEATE [USP MONOGRAPH]

Common Name

English

ACEPROMAZINE MALEATE [USP-RS]

Common Name

English

ACEPROMAZINE MALEATE [MART.]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66883