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)

Tramadol is an important spinal drug which produces analgesia following intrathecal injection. It is well known that fatty acids (FAs) play an important role in membrane fluidity of the blood-brain barrier (BBB) tissue, which blocks and/or controls the transportation of toxic substances into the brain. The aim of this study was to investigate the effect of a spinal drug (tramadol) on the concentrations and compositions of fatty acid in BBB tissues of New Zealand male rabbits. The total cellular fatty acid profiles of the tissues in three spinal cord sections (cervical, thoracal and lumbar) and in the brain of rabbits with or without drug administration were determined by gas chromatography using Sherlock Microbial Identification System (MIS) software (Microbial ID, Newark, DE, U.S.A.) with a database of FAME profiles for eukary. The relative percentage of the fatty acid methyl ester (FAME), 24 : 1 omega9c nervonic and 17 : 1 omega8c, did not change with tramadol treatments. However, there was an increase in the concentration of the FA 16 : 0, 18 : 1 omega7c DMA, 18 : 1 omega9c, sum in future 4, sum in future 8, sum in future 9, 18 : 0, 20 : 4 omega6c, sum in future 14, 22 : 4 omega6c, in contrast to a decrease in the percentages of the following FAMEs; 20 : 0, 20 : 1 omega9c. In the brain, there was an increase in the concentration of the FA 18 : 1 omega9c, sum in future 8 and 18 : 0, in contrast to a decrease in the percentages of two FAMEs, 16 : 0, 20 : 4 omega6c and 22 : 6 omega3c. The number of fatty acids were 20 in the spinal cord sections and 8 in the brain tissues of control animals compared to 15-18 fatty acids in the spinal cord section and 7 in the brain tissues of drug administered animals. The overall changes in the concentrations and numbers of FAs suggest that the spinal drug tested in this study has a side effect of disrupting of membrane fluidity of the BBB, which may cause neurotoxicity.
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PMID:Effect of the spinal drug tramadol on the fatty acid compositions of rabbit spinal cord and brain. 1451 44

Posture and baricity during induction of spinal anesthesia with intrathecal drugs are believed to be important in determining spread within the cerebrospinal fluid. In this double-blind prospective study, 150 patients undergoing elective cesarean delivery were randomized to receive a hyperbaric, isobaric, or hypobaric intrathecal solution of 10 mg bupivacaine during spinal anesthesia induced in either the sitting or right lateral position. After an intrathecal injection using a combined-spinal technique patients were placed in the supine wedged position. We determined the densities of the three intrathecal solutions from a previously validated formula and measured using a DMA-450 density meter. Data collection included sensory level, motor block, episodes of hypotension, and ephedrine use. Statistical analysis included analysis of variance and Cuzick's trend. In the lateral position, baricity had no effect on the spread of sensory levels for bupivacaine compared to the sitting position, where there was a statistically significant difference in spread with the hypobaric solution producing higher levels of analgesia than the hyperbaric solution (P = 0.002). However, the overall differences in maximal spread only differed by one dermatome, with the hyperbaric solution achieving a median maximum sensory level to T3 compared with T2 for the isobaric and hypobaric solutions. Motor block was significantly (P = 0.029) reduced with increasing baricity and this trend was significant (P = 0.033) for the lateral position only. Hypotension incidence and ephedrine use increased with decreasing baricity (P = 0.003 and 0.004 respectively), with the hypobaric sitting group having the most frequent incidence of hypotension (76%) as well as cervical blocks (24%; P = 0.032).
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PMID:The effect of posture and baricity on the spread of intrathecal bupivacaine for elective cesarean delivery. 1578 38

The pharmacological and neuroprotective properties of two ester analogs of the endocannabinoids, arachidonoylethyleneglycol (AA-EG) and alpha,alpha,-dimethyl arachidonoylethyleneglycol (DMA-EG), were investigated. We examined the interaction of both compounds with cannabinoid receptors (CB1 and CB2) and their efficacy in functional assays. In competition binding assays, AA-EG and DMA-EG had low potency to displace the CB1/CB2 agonist [3H]CP-55,940 in membrane preparations expressing rodent or human receptors. Binding data correlate with low efficacy of both compounds as regards to inhibition of adenylyl cyclase activity. It was also shown that DMA-EG resists hydrolysis by rat brain membranes while AA-EG undergo complete splitting under these conditions. In the cannabinoid tetrad, AA-EG induced hypomotility, analgesia, catalepsy and decreased rectal temperature indicating cannabimimetic activity. By contrast, DMA-EG was completely inactive in the same models. DMA-EG and AA-EG potently protected rat cortical neurons in culture against oxygen deprivation at nanomolar concentrations. In glutamate-induced damage, the compounds were less active protecting neurons at micromolar concentrations. The data obtained indicate that the ester endocannabinoid template can be used for the development of new compounds with potent biological activity lacking some of the undesirable behavioral side effects.
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PMID:Different pharmacological profile of two closely related endocannabinoid ester analogs. 1589 37