Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Two millilitres of solution calculated to contain 0.07 mg/kg xylazine and 0.5 mg/kg lignocaine injected at the sacrococcygeal epidural site provided caudal analgesia within 2 min in 61 sheep. This analgesic protocol eliminated forceful abdominal straining behavior following replacement of vaginal prolapse for at least 24 h in 48 of 52 ewes (92%) and in all 9 ewes with uterine prolapse. Moderate pelvic limb ataxia was observed in 25 sheep (41%) for up to 24 h after epidural injection. Sedation was noted in one ewe but no other systemic effects of xylazine injection, such as excessive salivation or ruminal distension, were observed. No long-term adverse reactions to xylazine injection were noted. The combined epidural injection regimen of xylazine and lignocaine is recommended as an adjunct for pain relief and control of abdominal straining following replacement of vaginal and uterine prolapse in ewes.
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PMID:The use of combined xylazine and lignocaine epidural injection in ewes with vaginal or uterine prolapses. 1672 3

The study was conducted to evaluate the effects of xylazine individually (0.05 mg/kg), ketamine individually (2.5 mg/kg), and a combination of xylazine and ketamine (0.05 mg/kg and 2.5 mg/kg) after lumbar epidural administration in water buffalo calves. Fifteen non-descript, male water buffalo calves of 6-8 months of age weighing between 55 and 75 kg were randomly placed in three groups (groups A, B and C). The agents were administered at the first lumbar epidural space. Clinico-physiological parameters, such as analgesia, ataxia, sedation, salivation, heart rate, respiratory rate and rectal temperature were studied. Other haematological and biochemical parameters monitored were haemoglobin, packed cell volume, total leukocyte count, plasma glucose, cortisol, protein albumin, globulin, blood urea nitrogen (BUN), creatinine, alanineamino transferase (ALT), sodium, potassium and chloride. The onset of analgesia (mean +/- SEM) was faster in group C (3.2 +/- 0.20 min) compared with that of group B (4.6 +/- 0.22 min) and group A (34.0 +/- 1.86 min). Analgesia of the thorax, flank, inguinal region, hind limbs, perineum and tail was complete in group C, but mild to moderate in groups A and B. Ataxia was severe in group C and mild in groups A and B. Mild to deep sedation was produced by groups A and C animals. Group B animals failed to produce sedation. Longer duration and greater depth of analgesia was produced in animals of group C. Heart rate, respiratory rate and rectal temperature decreased in groups A and C. The haematological parameters decreased in all the groups. The biochemical parameters like glucose, cortisol, BUN, creatinine, and ALT increased in all the animals. However, total proteins and albumin decreased in the three groups. The plasma electrolytes sodium, potassium and chloride did not show any significant change. The results of this study indicated a possible synergistic analgesic interaction between epidurally administered xylazine and ketamine, without causing any marked systemic effects in water buffalo calves.
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PMID:Xylazine, ketamine and their combination for lumbar epidural analgesia in water buffalo calves (Bubalus bubalis). 1697 Jun 33

Xylazine-ketamine combination was evaluated for its efficacy and safety after epidural administration in uraemic and healthy goats. The combination (xylazine 0.025 mg/kg and ketamine 2.5 mg/kg) was administered to uraemic (n = 6) and healthy (n = 6) animals in the lumbosacral epidural space. The combination was evaluated in terms of clinical, physiological, haematological and biochemical parameters. The onset of analgesia was faster in healthy animals than in uraemic animals. Xylazine and ketamine produced complete analgesia of tail, perineum, inguinal and thigh regions in all animals of both groups. However, healthy animals showed longer duration of complete analgesia than did uraemic animals. Greater ataxia was recorded in healthy animals than in uraemic animals. The heart rate showed a significant decrease in both groups; however, respiratory rate and rectal temperature did not show any significant changes. Haemoglobin, packed cell volume and total leukocyte count decreased non-significantly in both groups. Total leukocyte count was significantly higher in uraemic animals. A significantly higher value of urea nitrogen and creatinine was recorded in uraemic animals. The blood electrolytes (Na+, K+ and Cl-) and blood gases (PO2 and PCO2) did not show any significant changes in both groups; however, base excess was significantly higher in uraemic animals. The effects produced by the combination on different systems were transient and values normal as the effect of the drugs wore off. The results suggest that the combination when used epidurally in uraemic goats produced effective and safe surgical analgesia.
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PMID:Effects of epidural ketamine-xylazine combination on the clinicophysiological and haematobiochemical parameters of uraemic and healthy goats. 1721 18

The study was conducted in 9 healthy adult goats of either sex, weighing 15-20 kg, to evaluate and compare the clinicophysiological effects of spinally administered ketamine alone and in combination with xylazine and medetomidine. Nine trials each of the three treatments were conducted randomly by injecting ketamine (2.5 mg/kg) (n = 9), ketamine and xylazine (2.5 mg/kg and 0.05 mg/kg) (n = 9) and ketamine and medetomidine (2.5 mg/kg and 10 microg/kg) (n = 9). The drugs were administered at the lumbosacral subarachnoid space under strict aseptic conditions. The treatments were evaluated on the basis of clinicophysiological, haematological, biochemical and haemodynamic observations. Ketamine produced mild to moderate analgesia of the hindquarters. Its combination with either xylazine or medetomidine produced complete analgesia of the hindquarters for 45-60 min. Ataxia was moderate in the ketamine group, whereas animals attained sternal recumbency in the combination groups. A moderate degree of sedation was recorded in the combination groups. Heart rate and respiratory rate depression in the combination groups and heart rate and respiratory rate stimulation in ketamine group were recorded. Haematological parameters decreased in all the groups. Increase in serum glucose, creatinine and urea nitrogen was recorded in all the groups. Serum electrolytes did not show any significant change. The results showed that the combination of ketamine with xylazine or medetomidine at these dose rates produced a comparable degrees of analgesia of hindquarters with transient and minimal cardiopulmonary side effects.
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PMID:Clinicophysiological effects of spinally administered ketamine and its combination with xylazine and medetomidine in healthy goats. 1729 60

Six male buffalo calves aged from six to eight months and weighing 100 to 120 kg were used to evaluate the efficacy and safety of caudal epidural analgesia produced by doses of 37.5 mg (5 ml) and 75 mg (10 ml) ropivacaine (0.75 per cent). The study was completed in two phases. In phase 1, all the animals were used twice to evaluate the analgesic and clinical effects of two doses of ropivacaine. In phase 2, the animals were divided into two groups of three to evaluate the effects of two doses of ropivacaine on some haemodynamic and acid-base parameters. Signs of analgesia, as evidenced by a loss of response to pinprick stimulation, were recorded only at the tail, perineum and hindlimbs of the animals given 5 ml ropivacaine, but they extended from the tail to the thorax (T9) in the animals given 10 ml ropivacaine. The duration of analgesia was five to six hours in the animals given 5 ml ropivacaine and seven to eight hours in the animals given 10 ml ropivacaine. Animals of both groups became recumbent, but the score for ataxia was higher in the animals given 10 ml ropivacaine. The respiratory rate decreased significantly (P<0.05) below the baseline in the animals given 10 ml ropivacaine, but the rectal temperature, heart rate, mean arterial pressure, central venous pressure and acid-base and electrolyte parameters did not change significantly in either group.
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PMID:Comparison of two doses of ropivacaine for lumbosacral epidural analgesia in buffalo calves (Bubalus bubalis). 1754 47

Here, we have investigated the in vitro pharmacology of a muscarinic agonist, (3R,4R)-3-(3-hexylsulfanyl-pyrazin-2-yloxy)-1-aza-bicyclo[2.2.1]heptane (WAY-132983), and we demonstrated its activity in several models of pain. WAY-132983 had a similar affinity for the five muscarinic receptors (9.4-29.0 nM); however, in calcium mobilization studies it demonstrated moderate selectivity for M(1) (IC(50) = 6.6 nM; E(max) = 65% of 10 muM carbachol-stimulation) over the M(3) (IC(50) = 23 nM; E(max) = 41%) and M(5) receptors (IC(50) = 300 nM; E(max) = 18%). WAY-132983 also activated the M(4) receptor, fully inhibiting forskolin-induced increase in cAMP levels (IC(50) = 10.5 nM); at the M(2) receptor its potency was reduced by 5-fold (IC(50) = 49.8 nM). In vivo, WAY-132983 demonstrated good systemic bioavailability and high brain penetration (>20-fold over plasma levels). In addition, WAY-1329823 produced potent and efficacious antihyperalgesic and antiallodynic effects in rodent models of chemical irritant, chronic inflammatory, neuropathic, and incisional pain. It is noteworthy that efficacy in these models was observed at doses that did not produce analgesia or ataxia. Furthermore, a series of antagonist studies demonstrated that the in vivo activity of WAY-132983 is mediated through activation of muscarinic receptors primarily through the M(4) receptor. The data presented herein suggest that muscarinic agonists, such as WAY-132983, may have a broad therapeutic efficacy for the treatment of pain.
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PMID:Pharmacological characterization of the muscarinic agonist (3R,4R)-3-(3-hexylsulfanyl-pyrazin-2-yloxy)-1-aza-bicyclo[2.2.1]heptane (WAY-132983) in in vitro and in vivo models of chronic pain. 1758 24

The aim of the study was to evaluate and compare the effects of caudal epidural administration of meperidine (MP), lidocaine (LD), and a combination of the two (MPLD) in six mature saddle horses. Horses were randomly assigned to receive three treatments (MP 0.3 mg/kg; LD 0.2 mg/kg; and MPLD: MP 0.3 mg/kg and LD 0.2 mg/kg), with at least 1 week between treatments. Drugs were injected into the epidural space between the first and second coccygeal areas in conscious standing horses. Analgesia, ataxia, sedation, cardiovascular and respiratory effects, and rectal temperature were recorded at different intervals before (baseline) and after administration. Epidural administration of MPLD resulted in a longer duration of analgesia of the tail, perineum, and upper hind limb regions than did administration of MP or LD alone.
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PMID:Meperidine prolongs lidocaine caudal epidural anaesthesia in the horse. 1789 57

Ziconotide, a potent, selective, reversible blocker of neuronal N-type voltage-sensitive calcium channels, is approved in the United States for the management of severe chronic pain in patients for whom intrathecal therapy is warranted, and who are intolerant or refractory to other treatment, such as systemic analgesics, adjunctive therapies, or intrathecal morphine. In the European Union, ziconotide is indicated for the treatment of severe chronic pain in patients who require intrathecal analgesia. Nonclinical investigations of ziconotide included a comprehensive characterization of its toxicology, incorporating acute and subchronic toxicity studies in rats, dogs, and monkeys; reproductive toxicity assessments in rats and rabbits; and mutagenic, carcinogenic evaluations performed in vivo and in vitro. Additional investigations assessed the potential for cardiotoxicity (rats) and immunogenicity (mice, rats, and guinea pigs), and the presence or absence of intraspinal granuloma formation and local cell proliferation and apoptosis (dogs). The resulting nonclinical toxicology profile was predictive of human adverse events reported in clinical trials and consistent with ziconotide's pharmacological activity. Frequently observed nonclinical behavioral effects included tremoring, shaking, ataxia, and hyperreactivity. Occurrences were generally transient and reversible upon cessation of treatment, and intolerable effects occurred at doses more than 45 times the maximum recommended clinical dose. Ziconotide was not associated with target organ toxicity, teratogenicity, or treatment-related gross or histopathological changes; it displayed no mutagenic or carcinogenic potential and no propensity to induce local cell proliferation or apoptosis. Although guinea pigs developed systemic anaphylaxis, antibodies to ziconotide were not detected in mice, rats, or guinea pigs, indicating low immunogenic potential. No evidence of granuloma formation was observed with intrathecal ziconotide treatment. In summary, the results from these nonclinical safety assessments revealed no significant toxicological risk to humans treated with ziconotide as recommended.
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PMID:Nonclinical safety of ziconotide: an intrathecal analgesic of a new pharmaceutical class. 1796 28

In the present study, we asked whether multiple intrathecal injections of deltorphin II, a selective delta opioid receptor (DOPR) agonist, induced DOPR tolerance in three behavioral assays. Unilateral inflammation caused by complete Freund's adjuvant (CFA) injection into the rat or mouse hind paw (CFA model) induced thermal hyperalgesic response that was transiently and dose-dependently reduced by intrathecal administration of deltorphin II or morphine. In both rodent species, the effect of deltorphin II was not modified by a single prior administration of deltorphin II, suggesting an absence of acute tolerance in this paradigm. Repeated administration of intrathecal deltorphin II or s.c. SB-235863 (five consecutive injections over 60 h) also failed to impair the antihyperalgesic response to delta opioid receptor agonist, whereas repeated intrathecal or s.c. injections of morphine induced a significant decrease in the subsequent thermal antihyperalgesic response to morphine. In mice, deltorphin II also induced a rapid, transient motor incoordination/ataxia-like behavior as tested with the accelerating rotarod. In contrast to the antihyperalgesic responses, tolerance to the motoric effect of deltorphin II was evident in mice previously exposed to multiple intrathecal agonist injections, but not multiple saline administrations. Using the tail flick antinociceptive test, we found that DOPR-mediated analgesia was significantly reduced by repeated exposure to deltorphin II. Altogether, these observations suggest that repeated injections of DOPR agonists induce differential tolerance effects on antihyperalgesic, antinociceptive, and motor incoordination/ataxia-like behaviors related to DOPR activation by deltorphin II.
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PMID:Differential noxious and motor tolerance of chronic delta opioid receptor agonists in rodents. 1932 39

The influence of increasing the dosage of ketamine on anaesthesia induced by a combination of ketamine, xylazine and midazolam in pigs was determined by assessing the onset of action (OAN), duration of analgesia (DAN), anaesthesia time (ANT), and recovery time (RCT) in 10 growing pigs (Mean weight: 18.2 +/- 1.65 kg) receiving either 10 mg/kg intramuscular (i.m.) injection of 10% ketamine, 2 mg/kg i.m. injection of 2% xylazine and 0.25 mg/kg i.m. injection of 0.1% midazolam (K10XM) or 20 mg/kg i.m. injection of ketamine and 2 mg/kg i.m. injection of xylazine and 0.25 mg/kg i.m. injection of 0.1% midazolam (K20XM). In addition, the heart rates (HR), respiratory rates (RR) and rectal temperatures (RT) were determined immediately after drug administration and at 10 minute intervals over a period of 60 minutes. Analgesia was assessed by the response of the pigs to artery forceps applied at the interdigital space. Recovery was determined as pigs' ability to stand without ataxia. Data were expressed as mean +/- SEM while anaesthetic indices were compared using Student's t-tests. A P value of 0.05 was accepted as significant in all cases. In this study, both the OAN and RCT were significantly (P < 0.05) shorter in K10XM (1.4 +/- 0.2 min; 7.8 +/- 2.2 min) than in K20XM (2.2 +/- 0.2; 18.6 +/- 1.4 min) respectively. Similarly, the duration of anaesthesia was significantly (P < 0.05) shorter in K10XM (55.4 +/- 8.4 min) than in K20XM (92.0 +/- 13.6 min). The pigs that received K20XM combination had analgesia of duration of 41.4 +/- 12.6 min while those that received K10XM combination had no analgesia. However, the HR, RR, and RT were not significantly (P > 0.05) different between K10XM and K20XM. It was therefore concluded that the lower dose ketamine combination is better for the induction of anaesthesia, while the higher dose ketamine combination is preferable for surgery of short duration in pigs.
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PMID:Increasing ketamine dose enhances the anaesthetic properties of ketamine-xylazine-midazolam combinations in growing pigs. 1949 21


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