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)

Ketorolac is a new chiral nonsteroidal anti-inflammatory drug (NSAID) which is marketed for analgesia as the racemate. The drug is administered as the water soluble tromethamine salt and is available in tablets or as an intramuscular injection. The absorption of ketorolac is rapid, Cmax being attained between 20 to 60 min. Its oral bioavailability is estimated to range from 80 to 100%. The drug is extensively bound (> 99%) to plasma proteins and has a volume of distribution (0.1 to 0.3 L/kg) comparable with those of other NSAIDs. Only small concentrations of ketorolac are detectable in umbilical vein blood after administration to women in labour. The elimination half-life is between 4 and 6h and is moderate in comparison with other NSAIDs. The area under the plasma concentration-time curve of ketorolac is proportional to the dose after intramuscular administration of therapeutic doses to young healthy volunteers. Ketorolac is extensively metabolised through glucuronidation and oxidation; little if any drug is eliminated unchanged. Most of the dose of ketorolac is recovered in the urine as conjugated drug. Although ketorolac is excreted into the breast milk, the amount of drug transferred comprises only a small fraction of the maternal exposure. Little stereoselectivity was present in the pharmacokinetics of ketorolac in a healthy volunteer receiving single intravenous or oral doses. The elderly exhibit reduced clearance of the drug. Renal insufficiency appears to cause an accumulation of ketorolac in plasma, although hepatic disease may not affect the pharmacokinetics.
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PMID:Clinical pharmacokinetics of ketorolac tromethamine. 2751 22

The analgesia induced in rats by morphine is potentiated by restraint-stress exposure and is reduced in rats that have been consuming a sweet solution. The purpose of the present study was to determine whether the potentiation of morphine-induced analgesia following restraint immobilization would be attenuated in rats consuming a sweet solution. Groups of rats were maintained on unsweetened water or allowed 2 h of daily access to a solution of saccharin and glucose (SG). Half of the rats in each of these groups were subjected to 1 h of restraint stress (groups RS and RS+SG) and the other half in each group were not stressed (groups NS and NS+SG). Rats then underwent 1 h of RS treatment or were nonstressed (NS). The next day all rats were injected subcutaneously with morphine (0.0, 4.0, 8.0, or 16 mg/kg) and analgesia was assessed using the tail flick assay. ED50S (mg/kg) were calculated for each treatment group; NS = 5.8, RS = 1.6, NS+SG = 6.4, and RS+SG = 4.4. Our results demonstrate that RS potentiated morphine-induced analgesia in rats given access to SG as well as non-SG exposed rats that displayed ED50S 1.5 and 3.9 times lower than their respective controls. RS-treated rats that consumed SG solution had significantly lower tail flick latencies than did non-SG exposed rats. Additionally, tail flick latencies of rats in the nonstressed and NS+SG groups did not significantly differ. We conclude that the brain mechanism(s) responsible for RS-induced potentiation of morphine antinociception are attenuated by intake of a sweet solution.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Intake of sweet water attenuates restraint-stress-induced potentiation of morphine analgesia in rats. 147 17

A combination of tiletamine HCl and zolazepam HCl is frequently used as an anesthetic, but little is known about the antinociceptive properties of tiletamine-zolazepam. The antinociceptive properties of tiletamine-zolazepam alone or combined with xylazine or butorphanol were determined in the adult male rate using the tail-flick test. Changes in tail-flick latency were determined at 15, 45, and 75 min after IP drug administration of sterile water, sodium pentobarbital, morphine, tiletamine-zolazepam, xylazine, butorphanol, and tiletamine-zolazepam plus xylazine or butorphanol. Tail-flick latency approximated 100% maximum possible effect (MPE) at 15-75 min postinjection in morphine-treated rats. Tiletamine-zolazepam, xylazine, and butorphanol alone, at any dose utilized, produced less than 50% MPE. However, the combination of tiletamine-zolazepam with butorphanol or xylazine increased tail-flick latency approximately three times greater than tiletamine-zolazepam alone. These results demonstrate that: a) consonant with earlier findings, analgesia and anesthesia are independent states; b) tiletamine-zolazepam is not an effective combination with respect to analgesia; but c) in concert with appropriate drugs, it can exhibit potent antinociceptive properties.
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PMID:Antinociceptive properties of tiletamine-zolazepam improved by addition of xylazine or butorphanol. 147 95

The technique of combined spinal epidural anaesthesia (CSE) combines the versatility of spinal with the variability of epidural anaesthesia. Spinal application of the local anaesthetic achieves a fast response, reliable sensorial and motor block at a low dose with little toxicity. The epidural catheter allows for the duration of surgical anaesthesia to be extended and provides analgesia for the postoperative period. As the incidence of post dural puncture headache (PDPH) is inversely related to the size of the spinal needle, PDPH rarely or never occurs when 29 gauge needles are used. In 1775 parturients receiving spinal anaesthesia for caesarean section, Dittmann et al. [4] reported an incidence of PDPH of 1.37% with 29 gauge needles. The 29 gauge needle produced by Becton-Dickinson is the one now most frequently used for this technique. It is recommended that these needles be reused after resterilization. The objective of this study was to examine how clean 29 gauge spinal needles really are after resterilization. MATERIALS AND METHODS. Fifteen needles (29 gauge; Becton-Dickinson) were routinely used for combined spinal epidural anaesthesia. After identification of the epidural space at the L3-4 spinal segment with the 18 gauge Tuohy needle, the 29 gauge needle was advanced through the Tuohy needle. Immediately after use the needles were cleaned, rinsed with 20 ml distilled water, dried with pressurized air and subsequently resterilized in gas. Preparation of the used needles was in accordance with the manufacturer's recommendations ("wash, rinse, dry, sterilize before initial and each subsequent use") and with generally accepted principles [6]. Two needles were additionally cleaned in an ultrasonic bath for 15 min. The needles were examined using a scanning electron microscope. After this analyses, eight needles were sterilized again and then taken for hygienic examination. They were incubated with trypticase soy broth and checked for bacterial growth. RESULTS. Scanning electron microscopy (ScEM) showed organic impurities on all needles. These impurities were equally distributed among all needles. Even the two cleaned in the ultrasonic bath were not free of organic particles. However, no material defects or damage could be seen. Hygienic evaluation proved sterility as no bacterial growth could be detected. CONCLUSION. Owing to the possibility of medico-legal consequences, which sometimes occur a long time after anaesthesia has been given, we think it is unwise to reuse such needles. We hope that disposable and cheap 29 gauge needles will soon become available.
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PMID:[The reuse of 29-gauge spinal needles following combined spinal-epidural anesthesia]. 148 76

This study was designed to test analgesia, duration, and cardiovascular changes induced by meperidine (MEP) and oxymorphone (OXY) following methoxyflurane (MOF) and halothane (HAL) anesthesia. Eight healthy dogs were given atropine and acepromazine, and anesthesia was induced with thiamylal and maintained with 1.5 minimal alveolar concentration of MOF or HAL for 1 hour during controlled ventilation. Eight treatments were given with each anesthetic: 3 with MEP (0.5, 1.0, and 2.0 mg/kg, IV), 3 with oxymorphone (OXY; 0.05, 0.1, and 0.2 mg/kg, IV), and 2 placebos with sterile water. Test drugs were given at the end of anesthesia when early signs of recovery were evident. Minimal threshold stimulus/response nociception was assessed by use of an inflatable soft plastic colonic balloon. Blood pressures and pulse rate were measured with a noninvasive monitor. Meperidine and OXY were found to be effective analgesics and could be reversed with naloxone. Intravenous administration of 2.0 mg of MEP/kg provided analgesia for 36 +/- 6 minutes and 39 +/- 15 minutes after MOF and HAL, respectively. In contrast, OXY was effective at all 3 doses with effects of IV administration of 0.2 mg of OXY/kg lasting 154 +/- 13 minutes and 152 +/- 12 minutes, after MOF and HAL, respectively. Analgesia could not be demonstrated after anesthesia for acepromazine, MOF, or HAL. Blood pressure was not changed by either anesthetic nor was it influenced by MEP or OXY. Pulse rate was significantly depressed by the higher doses of OXY following HAL, but was not changed by MEP following either anesthetic.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Analgesia and behavioral responses of dogs given oxymorphone-acepromazine and meperidine-acepromazine after methoxyflurane and halothane anesthesia. 151 Mar 12

Chronic treatment of adult animals with morphine results in tolerance but there are fewer reports on the effects of chronic opiates during ontogeny. The present experiments assessed the development of morphine-induced tolerance and withdrawal in infant rats. Pups were injected with morphine twice daily from ages 1-7 days and then tested on day 7 for morphine-induced analgesia in a hot-water immersion test, and separation-induced ultrasonic vocalizations in response to isolation from the dam and littermates at 7 and 10 days of age. Tolerance occurred to the analgesic effects of morphine but not to its suppression of ultrasonic vocalizations. Separation-induced vocalizations were greatly increased in chronic morphine-treated pups following naltrexone-precipitated withdrawal at 7 days of age. The increase in ultrasonic vocalizations following naltrexone treatment in morphine exposed pups may be a developmentally unique sign of opiate withdrawal.
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PMID:Tolerance and withdrawal to chronic morphine treatment in the week-old rat pup. 151 48

The effect of LPSw, a lipopolysaccharide from a water extract of wheat flour, on pain response was investigated using an acetic acid-induced writhing test in mice. LPSw inhibited writhing dose-dependently in the range of 10 ng-10 micrograms/mouse i.v. This effect reached its maximum 1.5-3 h after the LPSw inoculation and was detectable even after 8 h. The analgesic effect of LPSw was inhibited by i.v. injection of naloxone and also beta-endorphin was detected in serum and brain tissue following injection of LPSw. Preliminary clinical trials were done in which LPSw was administered percutaneously to relieve the pain of patients with herpes. The results showed that pain was relieved by this application. LPSw may be the best analgesic drug so far known, since it induces the endogenous mediator of analgesia, beta-endorphin.
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PMID:Homeostasis as regulated by activated macrophage. IV. Analgesic effect of LPSw, a lipopolysaccharide of wheat flour. 152 27

Moderate drinking for the elderly of both genders is no more than one drink per day, where a drink is defined as 12 oz of beer, 5 oz of wine, or 1.5 oz of spirits. Age does not affect the rate of absorption or elimination of alcohol. Lean body mass decreases and adipose tissue increases with age, however, resulting in a corresponding decrease in the volume of total body water. With a smaller volume of distribution, an alcohol dose identical to that administered to a younger individual of the same size and gender will produce a higher blood alcohol concentration in the elderly. Low-dose alcohol stimulates appetite and promoters regular bowel function. In the well-nourished nonalcoholic elderly, the negative impact of alcohol consumption on nutrition is minimal. Alcohol consumption improves mood by increasing feelings of happiness and freedom from care while lessening inhibitions, stress, tension, and depression. Although in the laboratory low-dose alcohol improves certain types of cognitive function in young men, in other types of task performance, alcohol induces impairment, which worsens with age. The effects of alcohol on sleep are primarily detrimental, worsening both insomnia and breathing disturbances during sleep. Although the role of alcohol consumption in mortality from heart disease has not been investigated in the elderly, moderate drinking appears safe. Under some circumstances low-dose alcohol may produce analgesia whereas in others it may worsen pain. The elderly use a significant proportion of both prescription and over-the-counter medication, a large variety of which interact with alcohol. Alcoholic beverage consumption may exacerbate cognitive impairment and dementias of other etiology. Although some studies suggest that moderate use of alcohol by institutionalized senior citizens appears to produce benefits including improved socialization, separation of the effects of the social situation from those specifically attributable to alcohol remains to be accomplished. Older individuals who want to drink, have no medical contraindications, and take no drugs (prescription or over-the-counter) that interact with alcohol, may consider one drink a day to be a prudent level of alcohol consumption. Patients should be counseled to avoid alcohol consumption immediately prior to going to bed in order to avoid sleep disturbances. They also should be cautioned against potential drug-alcohol interactions and told to avoid alcohol ingestion prior to activities such as driving. The decision to recommend a particular level of alcohol consumption in any given patient must, however, be carefully tailored not only to that individual's specific medical needs but to his or her social and environmental circumstances as well.
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PMID:Alcohol and the elderly. 157 71

Studies of various strains of mice revealed marked differences in their analgesic sensitivity towards morphine (mu), U50,488H (kappa 1) and naloxone benzoylhydrazone (NalBzoH; kappa 3). Sensitivity to mu and kappa analgesia varied independently of the other. Analgesic sensitivity to morphine remained relatively consistent among 3 different nociceptive assays for each strain. However, the sensitivity of an individual strain to NalBzoH remained highly dependent upon the assay used. CD-1 mice were sensitive to NalBzoH in all 3 assays, but in BALB/c mice NalBzoH produced analgesia only in the hot plate and cold water tail-flick assays. In Swiss-Webster mice, NalBzoH was active in the radiant heat and cold water tail-flicks but inactive in the hot plate. Although the levels of mu, kappa 1 and kappa 3 binding in whole brain homogenates did vary somewhat, they did not correlate with analgesic sensitivity. These results suggests that the genetic controls over mu and kappa analgesia operate independently and further illustrate the many difficulties in evaluating potential analgesics.
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PMID:Genetic influences in opioid analgesic sensitivity in mice. 166 10

The sites of action of spinally administered opiates are specific receptors (mu kappa delta) located in the spinal dorsal horn. Pharmacokinetics of spinally administered opiates are determined by their lipophilic property. Morphine has a weak octanol-water partition coefficient and remains in the CSF during a long period following the cephalic movements of lumbar CSF to the supraspinal structures. More lipophilic opiates are rapidly eliminated from the CSF. Nevertheless, significant pethidine concentrations are documented in the ventricular CSF, due to vascular absorption of the drug. Pharmacokinetics features of different opiates determine the duration of analgesia and the risk of respiratory depression after spinal injection.
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PMID:[Pharmacology and mechanism of action of opiates administered by the subarachnoid route]. 167 77


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