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)

Midazolam, a water soluble bensodiasepine, has proven to induce a sleep pattern and amnesic effect that makes it preferable for use as a premedication for outpatient surgery. Used in addition to the regular anesthesia, Midazolam obviates the ineffectiveness of the analgesic drug. Since 1970, neuroleptic analgesia has been used as a method of outpatient anesthesia. Unfortunately, neuroleptic analgesia has provided inadequate coverage of pain relief causing pain and discomfort to patients. When a sedation and anxiolytic premedication are used, the patient acceptance increases. In a study in Ramathibodi hospital, Bangkok, Thailand effectiveness of midazolam as a premedication drug in laparoscopic interval sterilization, 150 women capable of reproduction and who were schelduled for the operation were studied. All of the women received 15mg midazolam orally either 60 or 90 minutes before the operation. The women were divided into 3 groups of 50 classified by the type of analgesic administered (tramadol or pethidine). Heart and respiratory rates and blood pressure were measured prior to, during, and after the operation. No difference in the rate of amnesia was found among the 3 groups, and a rate of 36% of amnesia was found in the study. Those results were lower than earlier reports, possibly due to circumstances at the hospital such as lack of coordination between administration of the medication and timing of the surgery.
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PMID:Amnesic effect of midazolam as premedication in interval laparoscopic sterilization. 318 58

beta-endorphin, administered into the cerebral ventricles of rats, provokes a sequence of behavioural and electroencephalographic (EEG) responses similar to those observed with general anaesthetics used clinically. Initial behavioural and EEG excitation, motor incoordination and exaggerated responsiveness to sensory stimuli are followed by a stage of rigid immobility with maintenance of local reflexes (withdrawal, corneal) and EEG arousal in response to stimulation. Finally, there is immobility associated with both EEG and behavioural unresponsiveness to severely noxious stimuli. Such a state of unconsciousness with complete analgesia defines general anaesthesia. This state was completely and rapidly reversed by the specific opiate antagonist, naloxone. The induction of general anaesthesia by a water-soluble neurohormonal peptide acting at specific receptor sites has important implications for traditional theories of anaesthesia.
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PMID:beta-Endorphin induces general anaesthesia by an interaction with opiate receptors. 626 98

Mice were used for a study of the interaction between morphine and phencyclidine (PCP) in relation to lethality, motor incoordination, locomotor activity and rearing, together with the half-life of PCP, following continuous administration of morphine by pellet (75 mg base) implantation for 72 h and after removal of the pellets for 6 and 24 h. PCP induced motor incoordination and suppressed locomotor activity and rearing; these effects were enhanced in morphine 'pellet-implanted' mice and were attenuated in morphine 'pellet-removed' groups. The enhancing effect of morphine on the PCP responses was attributable more to the presence of residual morphine than to the alterations in its disposition. The morphine-induced increase in locomotor activity and analgesia was attenuated in PCP (40 mg/kg per day i.p. for 5 days) tolerant mice. The rate of decay of PCP in serum and brain or morphine pellet-implanted animals was not different; however, in the 24 h 'pellet-removed' group, the rate of decay of PCP was increased. The results indicate that there is a two-way cross-tolerance development between PCP and morphine. The phenomenon appears to involve both dispositional and functional adaptation mechanisms.
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PMID:Attenuation of pharmacological effects and increased metabolism of phencyclidine in morphine tolerant mice. 649 21

The study was conducted to evaluate the effects of romifidine alone (50 microg/kg) and a combination of romifidine (50 microg/kg) and ketamine (2.5 mg/kg) after intrathecal administration in goats. Ten adult goats of either sex weighing between 15 and 20 kg were randomly placed in 2 groups (groups I and II). The agents were administered at the lumbosacral subarachnoid space. Clinico-physiological parameters such as analgesia, motor incoordination, sedation, salivation, heart rate, respiratory rate, arterial pressure, central venous pressure and rectal temperature were studied. Other haematobiochemical parameters monitored were packed cell volume, haemoglobin, plasma proteins, glucose, urea and creatinine. The onset of analgesia was faster in group II (35.5 +/- 6.25 s) compared to that of group I (5.2 +/- 0.54 min). Analgesia of the tail, perineum, hind limbs, flank and thorax was mild to moderate in group I, but complete analgesia of tail, perineum and hind limbs was recorded in group II. Motor incoordination was mild in group I and severe in group II. Significant reduction in heart rate (more pronounced in group I) and respiratory rate (more pronounced in group II), and a significant increase in central venous pressure were recorded in both groups. Mean arterial pressure was reduced in both groups, but more markedly in group I. Sedation, electrocardiogram, rectal temperature and haemato-biochemical parameters did not show significant differences between the 2 groups. The results of this study indicated a possible synergistic analgesic interaction between intrathecally administered romifidine and ketamine, without causing any marked systemic effects in goats.
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PMID:Analgesic and cardiopulmonary effects of intrathecally administered romifidine or romifidine and ketamine in goats (Capra hircus). 1151 66

The effect of baclofen, a GABA(B) agonist, has been studied in the hot plate test in mice, to analyze the possible involvement of the GABAergic system in baclofen analgesia. Baclofen (1-3 mg kg(-1) intraperitoneal (i.p.)) was found to elicit a dose-dependent antinociceptive effect. The antinociceptive effect of baclofen cannot be due to motor incoordination or sedation as the doses of baclofen which produce analgesia did not induce these effects during the rota-rod test. The antinociceptive effect of baclofen was reversed by 2-hydroxysaclofen, a GABA(B) antagonist by both systemic (3 mg kg(-1)) and intra cisterna magna (intracisternal (i.c.)) (0.3 mg kg(-1)) administration. The antagonist dose administered via i.c. produced a complete blockade and was 10-fold lower than the dose employed in i.p. administration. The data suggest that the antinociceptive effect of baclofen is GABA(B) receptor-mediated and reveal a central location of the analgesic effect of baclofen.
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PMID:Baclofen analgesia: involvement of the GABAergic system. 1222 Sep 72

The present study was designed to test the hypothesis that a synergistic interaction could be recorded after epidural administration of ketamine-an N-methyl-D-aspartate (NMDA) antagonist and pethidine--an opioid agonist. Twelve adult mongrel dogs of either sex were randomly divided in three groups A, B and C of four animals each. Ketamine (5%) at 2.5 mg/kg and pethidine (3%) 2 mg/kg were injected at lumbosacral epidural space in animals of groups A and B, respectively. In animals of group C ketamine (2.5 mg/kg) and pethidine (2 mg/kg) were injected. Heart rate increased significantly up to 15 min in group A, whereas in groups B and C, the increase was non-significant for a period of 10 and 45 min, respectively. Respiration increased gradually up to 45-60 min in group A and for 15-20 min in group B. However, in animals of group C respiration fell below the baseline during the first 10-15 min and then returned near the baseline. Rectal temperature decreased only marginally in all the groups. Ketamine alone produced complete analgesia at tail and perineal region for a period of 5-10 min and then moderate analgesia for the next 20-30 min. Analgesia at the flank was moderate to complete between 5 and 15 min. In group B complete analgesia was only moderate at the tail and perineal region up to 30 min. In animals of group C, complete analgesia was observed only at perineal region for a very short period (5 min). Analgesia was not associated with sedation in any of the groups but animals of groups A and C showed signs of motor incoordination. Results of the study suggest rather antagonistic than synergistic interaction between epidurally administered ketamine and pethidine. Further studies are needed to confirm the antagonistic interaction between the two drugs.
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PMID:Interaction between epidurally administered ketamine and pethidine in dogs. 1456 13

The efficacy of ketamine and bupivacaine in enhancing the epidural analgesia induced by medetomidine was evaluated in 10 buffalo calves utilized repeatedly after a gap of 10 days so that each drug combination was tested in 4 randomly selected animals. In group A, medetomidine (15 microg/kg), in group B ketamine (2.0 mg/kg), in group C bupivacaine (0.125 mg/kg), in group D medetomidine and ketamine (15 microg/kg and 2.0 mg/kg), and in group E medetomidine and bupivacaine (15 microg/kg and 0.125 mg/kg) was administered epidurally. Onset of analgesia was significantly earlier in animals of groups B and D compared to the animals of groups A, C and E. Medetomidine alone or in combination with ketamine/bupivacaine produced complete analgesia of the tail, perineum, inguinal region and upper parts of hind limbs. Ketamine produced a very short duration of complete analgesia at the tail and perineum. Bupivacaine alone produced only mild to moderate analgesia. Both ketamine and bupivacaine prolonged the duration of analgesia. Motor incoordination was mild to moderate in animals of all the groups, but animals remained standing throughout the period of observation. Animals of groups A, D and E showed mild to moderate sedation during the observation period. Ruminal movements decreased nonsignificantly in animals of groups A and E. Mild salivation was observed in animals of all the groups except group C. Significant decrease in heart rate (HR) was recorded after epidural administration of medetomidine or bupivacaine; however, ketamine caused short duration of tachycardia. The administration of ketamine with medetomidine caused lesser decrease in HR compared to medetomidine alone or in combination with bupivacaine. Significant fall in respiratory rate (RR) was recorded after epidural administration of medetomidine or bupivacaine alone, but an increase in RR was recorded after ketamine administration. The fall in RR was less pronounced in animals in which medetomidine was used with ketamine compared to the animals in which medetomidine was used alone or in combination with bupivacaine. Mean arterial pressure (MAP) decreased and central venous pressure (CVP) increased significantly after epidural administration of medetomidine in combination with ketamine or bupivacaine. The ECG changes included tall T wave, QS pattern, RS pattern and ST elevation and heart blocks at different intervals, which were more frequent and pronounced in animals given bupivacaine with medetomidine. It can be concluded that epidural administration of medetomidine can produce complete analgesia of the tail, perineum, inguinal region and upper hind limbs in buffaloes. However, significant depression of cardiovascular parameters was recorded. Administration of ketamine along with medetomidine resulted in significantly early onset and slightly longer duration of analgesia with lesser cardiopulmonary side-effects compared to medetomidine alone or medetomidine with bupivacaine. Addition of ketamine to medetomidine thus seems to be useful for producing epidural analgesia; however, addition of bupivacaine failed to provide any advantage over medetomidine alone.
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PMID:Medetomidine with ketamine and bupivacaine for epidural analgesia in buffaloes. 1572 87

The antinociceptive actions of honokiol and magnolol, two major bioactive constituents of the bark of Magnolia officinalis, were evaluated using tail-flick, hot-plate and formalin tests in mice. The effects of honokiol and magnolol on the formalin-induced c-Fos expression in the spinal cord dorsal horn as well as motor coordination and cognitive function were examined. Data showed that honokiol and magnolol did not produce analgesia in tail-flick, hot-plate paw-shaking and neurogenic phase of the overt nociception induced by intraplantar injection of formalin. However, honokiol and magnolol reduced the inflammatory phase of formalin-induced licking response. Consistently, honokiol and magnolol significantly decreased formalin-induced c-Fos protein expression in superficial (I-II) laminae of the L4-L5 lumbar dorsal horn. However, honokiol and magnolol did not elicit motor incoordination and memory dysfunction at doses higher than the analgesic dose. These results demonstrate that honokiol and magnolol effectively alleviate the formalin-induced inflammatory pain without motor and cognitive side effects, suggesting their therapeutic potential in the treatment of inflammatory pain.
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PMID:Effects of honokiol and magnolol on acute and inflammatory pain models in mice. 1782 2

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

Mu-opioids (i.e. morphine, oxycodone, hydrocodone) are considered to be the primary drugs for treatment of moderate to severe acute, chronic and cancer pain. Despite their analgesic effectiveness they have several clinically significant side-effects (cognitive, motor, respiratory, cardiovascular, gastrointestinal). They also have a limited spectrum of action, being more effective for nociceptive than neuropathic pain. In an effort to identify other opioid analgesics with greater effectiveness in mixed pain states and with a better side-effect profile compared to the classical mu-opioid agonist, morphine, a relatively little-known morphine derivative, morphine-6-O-sulfate, was characterized using a range of well-established rodent pain models. The present data demonstrated that morphine-6-O-sulfate was efficacious after several routes of administration, including neuroaxial (intrathecal), parenteral (intraperitoneal) and oral in the rat. It showed potent, dose-related, analgesic activities against acute nociceptive pain (the tail flick test), neuropathic pain (chronic constriction nerve injury hyperalgesia and allodynia) and inflammatory pain (formalin test). It had a good separation based on dose (at least 10-fold) between side-effects (incoordination, hypolocomotion, inhibition of gastrointestinal motility) and analgesia in all models of pain tested. In addition, morphine-6-O-sulfate had a more favorable potency ratio for delay of gastrointestinal transit and analgesia when compared to morphine. These preclinical findings suggest that morphine-6-O-sulfate is a potential candidate for development as a novel opioid for management of nociceptive, neuropathic and mixed pain states.
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PMID:Antinociceptive effects and toxicity of morphine-6-O-sulfate sodium salt in rat models of pain. 2082 49


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