A previously unidentified acepromazine metabolite in humans: implications for the measurement of acepromazine in blood. (1/45)

High-performance liquid chromatography-diode-array detection results obtained during the investigation of two cases involving acepromazine prompted us to study the stability of the drug in blood. It was found that acepromazine can undergo in vitro conversion by human red blood cells to 2-(1-hydroxyethyl)promazine, a product that has been reported as a minor urinary metabolite in horse urine but not previously identified in humans. Further, our analytical findings in the two cases examined suggest that 2-(1-hydroxyethyl)promazine may be the major unconjugated metabolite of acepromazine in humans. These findings have important implications for the analytical toxicology of acepromazine.  (+info)

The effect of opioid and acepromazine premedication on the anesthetic induction dose of propofol in cats. (2/45)

The median effective dosage (ED50) for induction of anesthesia with propofol was determined by using the up-and-down method in 31 unpremedicated cats, in 30 cats premedicated with butorphanol, 0.4 mg/kg body weight (BW), and acepromazine, 0.1 mg/kg BW, intramuscularly, and in 30 cats premedicated with morphine, 0.2 mg/kg BW, and acepromazine, 0.1 mg/kg BW, intramuscularly. The dose required for a satisfactory anesthetic induction in 50% of unpremedicated cats (ED50) was 7.22 mg/kg BW and of premedicated cats was 5.00 mg/kg BW. The reduction in dose was statistically significant in both premedicated groups compared with no premedication. There was no significant difference in ED50 between premedication regimes. Cyanosis was the most common adverse effect observed in all groups following anesthetic induction with propofol.  (+info)

Effect of general anesthetics on IOP in rats with experimental aqueous outflow obstruction. (3/45)

PURPOSE: To determine the effect of several common general anesthetics on intraocular pressure (IOP) after experimental aqueous outflow obstruction in the rat. METHODS: A single episcleral vein injection of hypertonic saline was used to sclerose aqueous humor outflow pathways and produce elevated IOP in Brown Norway rats. Animals were housed in either standard lighting or a constant low-level light environment. Awake IOPs were determined using a TonoPen (Mentor, Norwell, MA) immediately before induction of anesthesia by either isoflurane, ketamine, or a mixture of injectable anesthetics (xylazine, ketamine, and acepromazine). For each anesthetic, IOPs were measured immediately after adequate sedation (time 0) and at 5-minute intervals, up to 20 minutes. RESULTS; Awake IOPs ranged from 18 to 52 mm Hg. All anesthetics resulted in a statistically significant (P: < 0.01) reduction in measured IOP at every duration of anesthesia when compared with the corresponding awake IOP. With increasing duration of anesthesia, measured IOP decreased approximately linearly for both the anesthetic mixture and isoflurane. However, with ketamine, IOP declined to 48% +/- 11% (standard lighting) and 60% +/- 7% (constant light) of awake levels at 5 minutes of anesthesia, where it remained stable. In fellow eyes, the SD of the mean IOP in animals under anesthesia was always greater than the corresponding SD of the awake mean. Anesthesia's effects in normal eyes and eyes with elevated IOP were indistinguishable. CONCLUSIONS: All anesthetics resulted in rapid and substantial decreases in IOP in all eyes and increased the interanimal variability in IOPs. Measurement of IOP in awake animals provides the most accurate documentation of pressure histories for rat glaucoma model studies.  (+info)

Self-mutilation in rabbits following intramuscular ketamine-xylazine-acepromazine injections. (4/45)

Following hind leg intramuscular injections of ketamine, xylazine, and acepromazine, 4 of 6 rabbits exhibited self-mutilation of the digits. At necropsy, the affected sciatic nerve appeared enlarged. Lymphohistiocytic perineural inflammation and fibrosis were observed, together with nerve degeneration. Neuronal regeneration as the reason for self-mutilation is discussed.  (+info)

Structure of TAR RNA complexed with a Tat-TAR interaction nanomolar inhibitor that was identified by computational screening. (5/45)

HIV-1 TAR RNA functions critically in viral replication by binding the transactivating regulatory protein Tat. We recently identified several compounds that experimentally inhibit the Tat-TAR interaction completely at a 100 nM concentration. We used computational screening of the 181,000-compound Available Chemicals Directory against the three-dimensional structure of TAR [1]. Here we report the NMR-derived structure of TAR complexed with acetylpromazine. This structure represents a new class of compounds with good bioavailability and low toxicity that bind with high affinity to TAR. NMR data unambiguously show that acetylpromazine binds only to the unique 5' bulge site to which the Tat protein binds. Specificity and affinity of binding are conferred primarily by a network of base stacking and hydrophobic interactions. Acetylpromazine alters the structure of free TAR less than Tat peptides and neomycin do.  (+info)

Physiology and behavior of dogs during air transport. (6/45)

Twenty-four beagles were used to measure physiological and behavioral reactions to air transport. Each of 3 groups of 4 sedated (with 0.5 mg/kg body weight of acepromazine maleate) and 4 non-sedated (control) dogs was flown on a separate flight between Montreal, Quebec, and Toronto, Ontario, after being transported by road from Quebec City to Montreal. Saliva and blood samples were taken before ground and air transport and after air transport. The heart rate was monitored during the whole experiment except during ground transport, and behavior was monitored by video during air transport. Sedation did not affect any of the variables measured. The mean plasma cortisol concentration was significantly higher (P < 0.05) after ground transport than at baseline (225.3 vs 134.5 nmol/L); the mean salivary cortisol concentration was significantly higher (P < 0.05) after both ground and air transport than at baseline (16.2 and 14.8, respectively, vs 12.6 nmol/L). The mean neutrophil count was significantly higher (P < 0.05) after both ground and air transport than at baseline (80.6 and 81.4, respectively, vs 69.5 per 100 white blood cells), whereas the mean lymphocyte count was significantly lower (P < 0.05) (13.2 and 13.7, respectively, vs 22.4 per 100 white blood cells). Loading and unloading procedures caused the largest increase in heart rate. On average, the dogs spent more than 50% of the time lying down, and they remained inactive for approximately 75% of the time, except during take-off. These results suggest that transportation is stressful for dogs and that sedation with acepromazine, at the dosage and timing used, does not affect the physiological and behavioral stress responses of dogs to air transport.  (+info)

Inhibition has little effect on response latencies in the inferior colliculus. (7/45)

The inferior colliculi of all mammals are characterized by a wide range of first-spike response latencies that can greatly exceed the minimum time required for the transmission of input through the lower brainstem. The mechanisms that account for long response latencies of up to 50 ms are unclear, but one hypothesis is that an early inhibition plays a role in shaping latency. To test this hypothesis, response latencies were measured in the inferior colliculi of the pallid and mustached bats before and during the blockade of GABAa and glycine receptors. The effect of blocking inhibition on response latency was compared under stimulus conditions that produced the shortest latency in the predrug condition. Multibarrel "piggyback" electrodes were used to iontophoretically apply bicuculline and strychnine sequentially while recording from single neurons. Predrug latencies ranged from 9 to 26 ms in the pallid bat and from 4 to 17 ms in the mustached bat. Despite large increases in response magnitude and response duration following disinhibition, the blockade of inhibitory receptors had modest effects on response latency. In the pallid bat, blocking GABA receptors produced latency changes that ranged from -3.8 to +0.2 ms, while blocking glycine receptors produced changes from -0.1 to +1.7 ms. Similarly, in the mustached bat, blocking GABA receptors caused changes ranging from -10.3 to +1.4 ms; blocking glycine receptors in the mustached bat caused changes from -3.6 to +1.0 ms. The large change of -10.3 ms was an exception. In both species, the majority of neurons showed changes of <1 ms. We conclude that a fast, early inhibitory input does not appear to play a significant role in shaping the wide range of response latencies present in the inferior colliculi of mustached and pallid bats.  (+info)

Application of pulsed Doppler ultrasound for the evaluation of small intestinal motility in dogs. (8/45)

The purpose of this study was to verify whether small intestinal peristalsis could be observed and quantitatively assessed using pulsed-Doppler ultrasound. Pulsed-Doppler ultrasound was used to evaluate small intestinal peristalsis after a meal in ten normal dogs and ten sedated dogs. The small intestinal peristalses were measured 0, 1, 3, 6, 9, 12, and 24 hours after a 24-hour fast and after feeding. The number of small intestinal peristalsis were 0.133/min, 0.100/min, 0.033/min, 0.167/min, 0.070/min, 0.067/min, and 0.100/min in the fasted dogs, and 1.667/ min, 0.933/min, 1.133/min, 1.234/min, 1.933/min, 1.533/ min, and 0.533/min in fed dogs, respectively. In the dogs sedated with xylazine HCl, the number of small intestinal peristalsis was significantly reduced (p<0.01). However, in the dogs treated with ketamine HCl and acepromazine, the number of small intestinal peristalsis remained unchanged. Therefore, it can be concluded that pulsed-Doppler ultrasound allows graphic visualization of the intestinal movements, which can be subjected to qualitative and quantitative analysis, and may be suitable for a non-invasive study of small intestinal motility.  (+info)

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