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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Cycloaminoalkylnaphthalene 3 shows interesting opioid-like analgesic properties. It possesses two chiral centers and can exist as two racemic pairs and four diastereomers. Since the binding of opioids with receptors is stereoselective, it was important to have the two racemic pairs as well as the four diastereomers. In this paper the synthesis of the (2R,3S/2S,3R) racemate and the (2R,3S) and (2S,3R) enantiomers of the 1,2-dimethyl-3-[2-(6-hydroxynaphthyl)]-3-hydroxypyrrolidine 3 is considered and the determination of absolute configuration is described. The (2R,3S/2S,3R)-3 racemate and the (2R,3S)-3 and (2S,3R)-3 enantiomers were prepared by reaction of the racemic and optically active 1,2-dimethyl-3-pyrrolidone 2, respectively, with the lithiation product obtained from 2-bromo-6-tetrahydropyranyloxy-naphthalene 1 and acidic hydrolysis. The above-mentioned enantiomers of 3 were also obtained by optical resolution via fractional crystallization of the salts with D- and L-tartaric acids. The configuration of the optically active compounds was determined by X-ray analysis of a crystal of (-)-(2S,3R)-3.HCl.H2O. The pharmacological test HPT showed that (-)-(2S,3R)-3.HCl.H2O enantiomer is able to induce opioid-like analgesia with a relative potency 1.5 times that of (2R,3S/2S,3R)-3 and approximately 1.5 times that of morphine.
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PMID:Preparation and configuration of racemic and optically active analgesic cycloaminoalkylnaphthalenes. 991 49

Seventeen recently trapped opossum, Didelphis virginiana, (median weight 2.45 kg; range = 1.6-5.0 kg; quartiles = 1.8-3.3 kg) were immobilized with either telazol (15 or 30 mg/kg) or a mixture of medetomidine (100 micrograms/kg), butorphanol (0.2 mg/kg), and ketamine HCl (10 mg/kg) based on estimated weights. Anesthetized animals were subjected to cardiac puncture for blood withdrawal and toe pinch. Euthanasia was accomplished by intracardiac administration of 1 ml of concentrated pentobarbital sodium/phenytoin solution. Weights were underestimated for 14 of 17 animals, but were within 0.5 kg of the actual weight. Both drug combinations provided rapid and calm immobilization. Median time to recumbency for the medetomidine-butorphanol-ketamine group (n = 5) was 6 min (range = 4-10 min; quartiles = 6 and 8 min). The median time to recumbency was not statistically different for the low (n = 6) and high dose (n = 6) telazol groups, 3 and 3.5 min respectively (quartiles 3; 3.5 and 4; 5.5 min). The stronger heart beat with telazol immobilization facilitated cardiac puncture. All five animals administered the medetomidine-butorphanol-ketamine mixture and three of six animals given the low telazol dose reacted to cardiac puncture. Only one of six animals given the estimated 30 mg/kg dose of telazol reacted slightly to cardiac puncture. We conclude that 30 mg/kg telazol provides sufficient immobilization and analgesia to allow accurate cardiac puncture of the opossum if the procedure is performed within 5 to 10 min of recumbency. Intracardiac administration of concentrated pentobarbital sodium/phenytoin solution followed by bilateral thoracotomy provides appropriate euthanasia suitable for field situations.
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PMID:Field immobilization and euthanasia of American opossum. 1007 67

Transcutaneous electrical nerve stimulation (TENS) has been suggested as a means to reduce the amount of intravenous analgesia/sedation in patients undergoing extracorporeal shock wave lithotripsy (ESWL). A retrospective analysis of 79 ESWL procedures on 73 consecutive unselected patients was done in an attempt to determine the effectiveness of TENS in reducing the amount of intravenous fentanyl citrate and/or midazolam HCl needed to control pain and anxiety during the ESWL procedure. The study was divided into two parts: (1) all patients receiving TENS (n = 44) versus a non-TENS group (n = 35), and (2) comparison of the early (n = 22) and late non-TENS (n = 22) groups against each other; separately the late non-TENS group was compared to the entire TENS group. In the study, TENS reduce the amount of fentanyl citrate needed to control anxiety by 22.9% (P less than 0.025). No difference was noted when the early and late non-TENS group of patients were compared to each other. A gender difference was noted with a significant reduction in the dose of fentanyl citrate only in female patients receiving TENS (45.4%). Likewise, there was a significant reduction in the dose of midazolam HCl only in males who had TENS (38.9%). The data suggests that TENS may be a useful addition to reduce the amount of sedation and analgesia during ESWL.
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PMID:The use of transcutaneous electrical nerve stimulation during the biliary lithotripsy procedure. 1014 74

In order to evaluate the stressing role of swim hypothermia in producing swim stress-induced analgesia (SSIA), we examined whether a mere decrease in the animals' core temperature without swimming would be sufficient to elicit analgesia. The subjects were Swiss-Webster mice selectively bred for 37 and 40 generations for divergent magnitudes of SSIA. High (HA) and low analgesia (LA) mice were exposed for 15 min to temperatures in the range between -5 and +20 degrees C in 79% He/21% O2 (Heliox) atmosphere. The Heliox exposure produced ambient temperature-dependent hypothermia and analgesia, as assessed with a hot-plate test (56 degrees C). The post-Heliox analgesia was of much higher magnitude in HA than in LA mice. The steeper slope of regression of the magnitude of analgesia upon hypothermia in HA mice indicates that these mice are far more sensitive to the analgesic effect of hypothermia than LA mice. Naltrexone HCl (10 mg/kg i.p.) attenuated analgesia in ambient temperature-dependent manner in HA, but not in LA mice. In view of the apparent similarity of Heliox-induced analgesia and SSIA we suggest that hypothermia is a powerful component of swim stress to induce SSIA in the mouse.
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PMID:Analgesia in selectively bred mice exposed to cold in helium/oxygen atmosphere. 1022 87

A retrospective study was undertaken at Morristown Memorial Hospital to evaluate the cost impact of buprenorphine HCl, a Schedule V injectable analgesic, versus the Schedule II drugs morphine and meperidine HCl. Time-and-motion studies were conducted in the pharmacy and nursing units. Algorithms were used to determine the cost of auditing, ordering, dispensing, recording, and administering a single dose of Schedule II and Schedule V injectable analgesics. Based on acquisition costs and duration of analgesia, total 24-hour dose costs were calculated for buprenorphine, morphine, and meperidine. The resultant cost comparisons demonstrated that the use of buprenorphine as an alternative to morphine and meperidine for moderate to severe postoperative pain is highly cost-effective and, in this hospital, resulted in a total cost avoidance of up to 67% of analgesic cost per patient per day.
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PMID:Buprenorphine: a cost-effective alternative to Schedule II analgesics for moderate to severe pain relief. 1031 32

An oral solution available as ethanol-free droplets of the fixed drug combination tilidine-HCl 50 mg/naloxone-HCl 4 mg (CAS 27107-79-5 and CAS 465-65-6, respectively; Tilidin-ratiopharm plus Tropfen) was investigated in 12 healthy volunteers together with an ethanol-containing reference preparation for comparable bioavailability. The study was conducted in an open, randomized, two-way cross-over design applying single doses of 20 droplets (equivalent to 50 mg tilidine-HCl/4 mg naloxone-HCl) of either formulation in the fasting state. The drug plasma profiles were monitored for a period of 48 h by means of LC-MS/MS for tilidine and its active metabolite nortilidine, whereas GC-MS was employed in order to determine naloxone and its phase I metabolite, 6-beta-naloxole. Maximum concentrations (Cmax) achieved were 22.28 ng/ml (tilidine) and 92.78 ng/ml (nortilidine) for the test preparation. Corresponding values for the reference preparation were 24.95 ng/ml (tilidine) and 100.73 ng/ml (nortilidine). The extent of drug absorption (AUC0-infinity) amounted to 38.83 ng h/ml and 467.63 ng h/ml for the prodrug tilidine and the metabolite nortilidine of the test preparation and corresponded well to 43.81 ng h/ml and 493.85 ng h/ml of the reference. Regarding the rate of drug absorption, essentially identical tmax and Rabs values for both tilidine and nortilidine of either preparation in addition pointed to well comparable liquid formulations and equipotent analgesia may be inferred from opioid pharmakokinetic profiles. Pharmacokinetics of the opioid antagonist naloxone and 6-beta-naloxole were also determined and resulted in well coinciding profiles for both preparations. Thus despite the fact that only minimum oral naloxone bioavailabilities were observed, plasma level monitoring of naloxone and 6-beta-naloxole allowed for demonstration of systemic exposure of opioid antagonistic compounds throughout a period of 2-3 h after oral drug administration. Due to the limited number of subjects involved, the primary aim of the study did not consist in demonstration of drug bioequivalence. Rather a comparable bioavailability between preparations was assumed if AUC and Cmax point estimators of 90% confidence intervals would be contained within a 0.80-1.20 range. The study outcome revealed that all four investigated analytes met this requirement, whilst nortilidine pharmacokinetic parameters even fulfilled commonly accepted bioequivalence criteria, i.e. inclusion of 90% confidence intervals of AUC- and Cmax-ratios within acceptance limits of 80% and 125%. Increased data variation observed with bioavailability parameters of tilidine, naloxone and 6-beta-naloxole prevented their bioequivalence demonstration based on only 12 study participants. In conclusion, single doses of two different tilidine/naloxone 50 mg/4 mg liquid formulations revealed well comparable bioavailability for all 4 analytes investigated. Both treatments were fairly well tolerated. Most frequently reported adverse events were dizziness, headache and nausea, which all recovered without sequelae and necessity of concomitant treatment.
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PMID:Bioavailability investigation of a new tilidine/naloxone liquid formulation compared to a reference formulation. 1044 8

The present study was carried out in order to compare the effects of xylazine and lidocaine on analgesia and cardiopulmonary parameters following epidural injection in goats. Twelve healthy Small East African goats of both sexes (mean +/- SD; 15.6 +/- 1.9 kg body weight) were used. The goats were randomly assigned to two groups of five and seven animals. The first group (n = 5) was given 2% lidocaine-HCl at 4400 micrograms/kg body weight. The second group (n = 7) was administered 2% xylazine-HCl at 150 micrograms/kg body weight. All drugs were diluted in 5 ml of sterile water and were injected epidurally through the lumbosacral interspace with the injection taking over 20 s. Both drugs induced analgesia within 5 min. Signs of sedation, cardiopulmonary changes and lateral recumbency developed within 5-7 min after administration of epidural xylazine. Tail flaccidity and hind limb paralysis developed 3 min after epidural administration of lidocaine. The time from recumbency to regaining normal stance was 60 and 158 min for xylazine- and lidocaine-treated animals respectively. Xylazine induced adequate analgesia of the flank and perineum, which extended to the head and forelimbs. In contrast, lidocaine induced adequate bilateral flank and perineal analgesia extending up to the third thoracic vertebra. For both drugs, analgesia of the flank and perineum persisted for the entire 180-min observational period. Epidural injection of xylazine and lidocaine caused variable depression effects on the cardiopulmonary values but was not so low as to cause concern. It is concluded that lumbosacral epidural injection of xylazine at 150 micrograms/kg body weight in 5 ml of water for injection offers the most desirable sedation and analgesia of the flank and perineum. The longer duration of analgesia may be useful for postoperative analgesia and relief of continuous straining in goats.
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PMID:Comparison of xylazine and lidocaine effects for analgesia and cardiopulmonary functions following lumbosacral epidural injection in goats. 1063 98

Various monoolein-water systems containing tramadol HCl, a potent analgesic, were formulated to obtain sustained-release dosage forms which could be administered by subcutaneous, intramuscular or intrathecal injections. They were examined for their in vitro drug-release profiles and in vivo analgesic properties in rats in a 14 h period following intramuscular administration. In order to obtain a lower viscosity, we have substituted a part of monoolein by oleic acid and phospholipids. Both binary (monoolein-water) and quaternary (oleic acid-phospholipid-monoolein-water) formulations exhibited controlled drug-release profiles which were accelerated by surfactant adjunction. This surfactant action was probably due to structural changes in the lipid arrangement and was much more pronounced for the modified formulations. According to the results obtained in vitro, formulations with slower drug release (i.e. the native formulation and the modified one without surfactant) were selected for assessment of their in vivo properties. Both formulations demonstrated prolonged analgesic activities in the rat tail flick test manifested by stable pain relief during more than 10 h compared with the 3 to 4 h analgesia obtained with the commercially available tramadol HCl solution. The sustained-release capabilities were evaluated by using a modified half value duration (HVD) ratio and all sustained-released formulations exhibited a HVD ratio equal or superior to 3.9.
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PMID:In vitro/in vivo characterization of a tramadol HCl depot system composed of monoolein and water. 1082 77

Since the introduction of cocaine local analgesia in 1886, and the subsequent development of procaine (1904) and other closely related ester-type compounds, dentistry has prided itself on being as close to 'painless' as possible. In the late 1940s the newest group of the local anesthetic compounds, the amides, was introduced. The initial amide local analgesic, lignocaine (Xylocaine), revolutionised pain control in dentistry worldwide. In succeeding years other amide-type local anesthetics, mepivacaine, prilocaine, bupivacaine and etidocaine, were introduced. They gave the dental practitioner a local anesthetic armamentarium which provided pulpal analgesia for periods of from 20 minutes (mepivacaine) to as long as three hours (bupivacaine and etidocaine with adrenaline). In addition these popular drugs proved to be more rapid-acting than the older ester-type drug and, at least from the perspective of allergenicity, more safe. In 1976, in Germany, the newest amide local analgesic, carticaine HCl was introduced into dentistry. Articaine (the generic name was changed) possesses properties similar to lignocaine but has additional properties which made the drug quite attractive to the general dental practitioner. In 1986 articaine was introduced in North America (Canada) where it has become the most used local anesthetic, supplanting lignocaine. Articaine has been approved for use in the United Kingdom. In this introductory discussion we review the development of articaine and discuss its place in the dental local analgesic armamentarium.
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PMID:[New anesthetics]. 1103 79

We studied the cannabimimetic properties of N-vanillyl-arachidonoyl-amide (arvanil), a potential agonist of cannabinoid CB(1) and capsaicin VR(1) receptors, and an inhibitor of the facilitated transport of the endocannabinoid anandamide. Arvanil and anandamide exhibited similar affinities for the cannabinoid CB(1) receptor, but arvanil was less efficacious in inducing cannabinoid CB(1) receptor-mediated GTPgammaS binding. The K(i) of arvanil for the vanilloid VR(1) receptor was 0.28 microM. Administered i.v. to mice, arvanil was 100 times more potent than anandamide in producing hypothermia, analgesia, catalepsy and inhibiting spontaneous activity. These effects were not attenuated by the cannabinoid CB(1) receptor antagonist N-(piperidin-1-yl)-5-(4-chloro-phenyl)-1-(2, 4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide.HCl (SR141716A). Arvanil (i.t. administration) induced analgesia in the tail-flick test that was not blocked by either SR141716A or the vanilloid VR(1) antagonist capsazepine. Conversely, capsaicin was less potent as an analgesic (ED(50) 180 ng/mouse, i.t.) and its effects attenuated by capsazepine. The analgesic effect of anandamide (i.t.) was also unaffected by SR141716A but was 750-fold less potent (ED(50) 20.5 microg/mouse) than capsaicin. These data indicate that the neurobehavioral effects exerted by arvanil are not due to activation of cannabinoid CB(1) or vanilloid VR(1) receptors.
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PMID:Neurobehavioral activity in mice of N-vanillyl-arachidonyl-amide. 1104 Mar 43


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