Delving into the Latest Updates on Acepromazine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

1-[10-(3-dimethylamino-propyl)-10H-phenothiazin-2-yl]-ethanone, 10-(3-dimethylaminopropyl)phenothiazin-3-yl methyl ketone, 10-(3-dimethylaminopropyl)phenothiazine-3-ethylone

+ [5]

Target

DRDs

Mechanism

DRDs antagonists(Dopamine receptors antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication

Behavioural disorders

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC19H22N2OS

InChIKeyNOSIYYJFMPDDSA-UHFFFAOYSA-N

CAS Registry61-00-7

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation in dogs. Despite having effective analgesic efficacy, prolonged oral administration has been associated with adverse effects. Transdermal delivery of ketoprofen has reduced the incidence of adverse effects in humans and could potentially be used in veterinary clinical medicine. A transdermal (TD) ketoprofen formulation was recently developed for use in dogs and this study aimed to determine the pharmacodynamic activity of this formulation using surgical castration as an acute inflammatory model. Twelve dogs were randomly assigned to either a Control group (n = 6) or a TD group (n = 6). All dogs were castrated using standard surgical protocols, administered with pre-medication, consisting of acepromazine (0.055 mg/kg) and methadone (0.5 mg/kg) intramuscularly (IM) 30 min prior to induction of general anaesthesia. All dogs were then anaesthetised by injecting alfaxalone (2 mg/kg IV) via a 20 G 3 cm catheter in the left cephalic vein and subsequently maintained using isoflurane. Along with that TD group dogs also received TD ketoprofen (10 mg/kg) 1 h before pre-medication. Bloods were collected at 0 - hour (pre-surgery), and 1 and 2-h post-surgery and analysed for circulating eicosanoids using liquid chromatography mass spectrometry (LCMS) methods. Measured levels of Thromboxane B₂ (TXB₂) at both 1 and 2 h and Prostaglandin E₂ (PGE₂) at 2 h post-surgery were higher in the Control group compared to the TD group, suggesting pre-operative application of TD ketoprofen has a possible inhibitory effect on systemic inflammation and could be used to treat pain and inflammation in dogs.

15 Jan 2025·JAVMA-JOURNAL OF THE AMERICAN VETERINARY MEDICAL ASSOCIATION

Gabapentin and alprazolam pretreatment enhance sedation and reduce propofol requirements but do not improve intravenous catheter placement in cats undergoing elective ovariohysterectomy

Article

Author: Ververidis, Charalampos ; Papageorgiou, Virginia ; Mylonakis, Mathios E. ; Savvas, Ioannis ; Kazakos, George

Abstract:

Objective:

This study aimed to evaluate whether pretreatment with gabapentin or alprazolam in cats increases sedation, facilitates intravenous catheter placement (IVCP), or reduces propofol requirements for intubation compared to placebo.

Methods:

All cats that participated in this prospective, randomized, blinded, controlled clinical trial were admitted for elective ovariohysterectomy at a veterinary teaching hospital from 2022 to 2023. The cats were healthy, were ≥ 6 months old, and weighed > 3 kg. The cats were randomly assigned to 3 groups: group G received gabapentin (100 mg/cat), group A received alprazolam (0.125 mg/cat), and group P received a placebo. Ninety minutes after the pretreatment administration, premedication with acepromazine (0.02 mg/kg) and buprenorphine (0.02 mg/kg) was administered intramuscularly. Thirty minutes later, sedation levels, IVCP difficulty, and propofol requirements for intubation were evaluated.

Results:

A total of 60 cats were finally included, with 20 cats in each group. Sedation scores were significantly higher in both group G and group A compared to group P, with no significant difference observed between group G and group A. No differences were observed in the difficulty of IVCP among the groups. Propofol requirements for intubation were significantly lower in group A (4.6 ± 1.2 mg/kg) compared to both group G (6.7 ± 2.4 mg/kg) and group P (8.4 ± 1.9 mg/kg).

Conclusions:

Pretreatment with gabapentin or alprazolam increased sedation in cats undergoing premedication. Alprazolam reduced the propofol required for intubation, though neither drug facilitated IVCP.

Clinical Relevance:

The findings of our study can have implications for anesthesia protocols in feline patients.

01 Jan 2025·VETERINARY ANAESTHESIA AND ANALGESIA

Influence of acepromazine on the cardiovascular effects of dobutamine in isoflurane-anaesthetised horses premedicated with romifidine

Article

Author: Hosgood, Giselle ; Schier, Mara F ; Drynan, Eleanor ; Wong, Adrian M ; Raisis, Anthea L

OBJECTIVE:

To explore the influence of acepromazine on the cardiovascular effects of dobutamine in isoflurane-anaesthetised horses premedicated with romifidine.

STUDY DESIGN:

Prospective randomised clinical trial.

ANIMALS:

A total of 18 horses undergoing elective arthroscopy were enrolled, of which 12 horses requiring dobutamine were included.

METHODS:

Horses were randomised to receive acepromazine 0.02 mg kg^-1 (Group A+) intravenously (IV) or none (Group A-), 35 minutes before anaesthesia. Horses received xylazine 0.2 mg kg^-1 concurrently to facilitate IV access. Horses were premedicated with romifidine 0.08 mg kg^-1, induced with ketamine 2.2 mg kg^-1 and diazepam 0.08 mg kg^-1 IV, and maintained with isoflurane in oxygen. Dobutamine infusion was commenced when mean arterial pressure (MAP) was < 60 mmHg. Cardiovascular data were collected prior to dobutamine, and at a target MAP of ≥ 70 mmHg. Dobutamine start time from induction, duration and dose to reach target MAP were compared using Mann-Whitney U test. Cardiovascular variables were compared using repeated measures ANOVA and post-hoc Fisher's least significant difference test.

RESULTS:

Cardiac index (CI) and its percentage change from baseline were significantly higher at target MAP in group A+ [62.0 (49.9-74.2) mL minute^-1 kg^-1; 42.8 (17.0-68.7) %] than in A- [49.5 (39.6-59.5) mL minute^-1 kg^-1; -4.05 (-21.2-13.0) %] (p = 0.049; p = 0.003). Group A+ required significantly earlier dobutamine [20 (18-25) minutes] than group A- [36 (27-60) minutes] (p = 0.02). Group A+ required significantly higher dobutamine dose [1.5 (1-2.5) μg kg^-1 minute^-1] to reach target MAP than group A- [0.5 (0.5-1) μg kg^-1 minute^-1] (p = 0.009).

CONCLUSION AND CLINICAL RELEVANCE:

Dobutamine significantly increased MAP and CI following pre-anaesthetic acepromazine sedation, in isoflurane-anaesthetised horses premedicated with romifidine. Without acepromazine, dobutamine increased MAP but not CI. Interactions between acepromazine, romifidine and dobutamine on the cardiovascular system should be considered.

100 Deals associated with Acepromazine

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