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)

A stereoselective high-performance liquid chromatographic method for the determination of the enantiomers of ketamine and its active metabolite, norketamine, in human plasma is described. The compounds were extracted from plasma by liquid-liquid extraction three times in a combination of cyclohexane with 2.5 M NaOH, 1 mM HCl and 1 M carbonate buffer. Stereoselective separation was achieved on a Chiralcel OD column with a mobile phase of n-hexane-2-propanol (98:2, v/v). The detection wavelength was 215 nm. The lower limits of the determination of the method were 5 ng/ml for ketamine and 10 ng/ml for norketamine. The intra- and inter-day coefficients of variation ranged from 2.9 to 9.8% and from 3.4 to 10.7% for all compounds, respectively. The method was sensitive and sufficiently reproducible for stereoselective monitoring of ketamine and norketamine in human plasma during pharmacokinetic studies after the administration of ketamine for analgesia.
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PMID:Stereoselective high-performance liquid chromatographic determination of ketamine and its active metabolite, norketamine, in human plasma. 1107 75

Pain control is an important consideration after any surgical procedures. Especially in children, more attention and care are needed during the period of postoperative pain control, which must be both sufficiently safe and effective. In this respect, intravenous patient-controlled analgesia provides improved titration of analgesic drugs, thereby maintaining optimal analgesic status with few side effects. Thirty pediatric patients were randomly divided into two groups: the intravenous patient-controlled analgesia group (with nalbuphine HCl and ketorolac tromethamine) and the conventional pethidine HCl intramuscular group. The degree of analgesia was assessed every 4 hours until the second postoperative day. The intravenous patient-controlled analgesia group had significantly lower pain scores and took less time until they were able to walk to the bathroom, but as many side effects as the control group. We concluded that intravenous patient-controlled analgesia is safe and effective for pediatric patients who have moderate to severe pain after operations such as rib cartilage graft, iliac bone graft, and large flap surgeries.
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PMID:Postoperative pain management using intravenous patient-controlled analgesia for pediatric patients. 1131 21

The pathogenesis of gastric antral hemorrhage and ulceration is unclear. This paper first proposes that antral hemorrhagic ulcers produced in rats are associated with attenuation of defensive parameters (such as mucosal glutathione levels and histamine release, as well as aggravation of aggressive factors) including gastric acid back-diffusion and oxyradical generation. The protective effects of lysozyme chloride and antioxidants on this ulcer model were also evaluated. After being deprived of food for 24 hours followed by refeeding for 1 hour, rats were injected with 1.0 mol HCl/L intragastrically under potent analgesia of diethylether-anesthesia to induce antral ulcer. Control rats received a normal saline solution only. Rats were then given free access to water and food for 4 days. Before the experiment began, rats were again deprived of food for 24 hours. Following anesthetization, their stomachs were irrigated for 3 hours with either normal saline or a physiological acid solution containing 100 mmol HCl/L and 54 mmol NaCl/L. Aggravation of various aggressive and defensive parameters in antral mucosa was observed in refed rats that had received 1.0 mol HCl/L. A high relationship of mucosal glutathione level (r = -0.8754, P <.05) or lipid peroxides generation (r = 0.8198) to antral ulceration was obtained in those ulcerated rats. Intragastric lysozyme chloride (50-200 mg/kg) injected three times daily produced a dose-dependent attenuation of various gastric parameters in the acid-irrigated stomachs of antral ulcer rats. Intraperitoneal injections of various antioxidants, including exogenous glutathione, allopurinol, or dimethylsulfoxide also attenuated antral ulcer. In conclusion, the imbalance of aggressive factors, such as acid back-diffusion and oxyradicals-as well as defensive factors including glutathione and histamine-is important in modulating antral hemorrhagic ulcers that can be ameliorated by lysozyme chloride or antioxidants in rats.
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PMID:Role of acid back-diffusion, glutathione, oxyradical, and histamine in antral hemorrhagic ulcer in rats: the protective effect of lysozyme chloride and antioxidants. 1227 Dec 71

Swiss-Webster mice selectively bred for high swim stress-induced analgesia (SSIA) were exposed to continuous ambient cold (5 degrees C) for 6 weeks or to daily 3-min swims for 14 consecutive days either in 20 or 32 degrees C water. Thereafter, mice subjected to the particular procedure were injected intraperitoneally with 10 mg/kg of naltrexone HCl and were tested for modification of the opioid and nonopioid component of SSIA. SSIA was reduced following swims at either water temperature and was antagonized by naltrexone to greater extent than in nonswimming mice. Thus, the nonopioid (i.e. naltrexone-resistant) portion of the overall SSIA was significantly reduced, whereas the opioid (naltrexone-sensitive) portion became relatively augmented. In contrast, SSIA differed neither in magnitude nor in sensitivity to naltrexone between cold-acclimated and unacclimated mice. Swim hypothermia as well as the nonopioid component of SSIA were decreased after repeated swimming at 32 and 20 degrees C, but remained unchanged after cold acclimation. This argues for the essential role of an extrathermal, probably emotional in nature, factor not only in the elicitation of nonopioid SSIA, but also in the modulation of thermoregulatory processes during swimming. We suggest that the emergency component of swim stress, together with initial moderate hypothermic challenge, first produces the opioid form of SSIA, and subsequently, as the swim continues, also affects the thermoregulatory processes maintaining thermal homeostasis. This causes further increase in swim hypothermia and raises its stressing property to induce the nonopioid form of SSIA.
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PMID:Effect of cold acclimation and repeated swimming on opioid and nonopioid swim stress-induced analgesia in selectively bred mice. 1267 68

To determine the effects of burdizzo castration alone or in combination with ketoprofen (K), local anesthesia (LA), or caudal epidural anesthesia (EPI) on plasma cortisol, acute-phase proteins, interferon-gamma production, growth, and behavior of beef cattle, 50 Holstein x Friesian bulls (13 mo old, 307 +/- 5.3 kg) were assigned to (n = 10/treatment): 1) control (handled; C); 2) burdizzo castration (B); 3) B following K (3 mg/ kg of BW i.v.; BK); 4) B following LA (8 mL into each testis and 3 mL s.c. along the line where the jaws of the burdizzo were applied with 2% lidocaine HCl; BLA); and 5) B following EPI (0.05 mg/kg of BW of xylazine HCl and 0.4 mg/kg of BW of lidocaine HCl as caudal epidural; BEPI). The area under the cortisol curve against time was lower (P < 0.05) in BK than in B, BLA, or BEPI animals. On d 1 after treatment, plasma haptoglobin concentrations were higher (P < 0.05) in B, BLA, and BEPI than in BK animals. On d 3, haptoglobin and plasma fibrinogen concentrations were higher (P < 0.05) in all castration groups than in C. On d 7, haptoglobin and fibrinogen concentrations remained higher (P < 0.05) in BLA than in B and C animals. On d 1, concanavalin A-induced interferon-gamma production was lower (P < 0.05) in B, BLA, and BEPI than in C, but there was no difference between BK and C animals. From d -1 to 35, ADG was lower (P < 0.05) in B, BLA, and BEPI animals, but not in BK compared with C animals. Overall, there was a higher (P < 0.05) incidence of combined abnormal postures in B than in C, BK and BEPI animals. Although the use of K and EPI decreased (P < 0.05) these postures compared with B alone or B with LA, there was no difference between the K and EPI treatment. In conclusion, burdizzo castration increased plasma cortisol and acute-phase proteins, and suppressed immune function and growth rates. Local anesthesia prolonged the increase in acute-phase proteins. Ketoprofen was more effective than LA or EPI in decreasing cortisol and partially reversed the reduction in ADG following castration. The use of K or EPI was more effective than LA in decreasing pain-associated behavioral responses observed during the first 6 h after treatment. Systemic analgesia with ketoprofen, a non-steroidal antiinflammatory drug, was more effective in reducing inflammatory responses associated with castration than LA or EPI.
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PMID:Effect of ketoprofen, lidocaine local anesthesia, and combined xylazine and lidocaine caudal epidural anesthesia during castration of beef cattle on stress responses, immunity, growth, and behavior. 1277 56

Avinza is a once-daily, extended-release oral morphine preparation. It has a pharmacokinetic profile that exhibits less peak-to-trough fluctuations in plasma concentration whilst providing analgesia statistically identical to that produced by MS Contin (controlled-release morphine sulfate), Oxycontin (oxycodone HCl controlled-release) and six doses of oral morphine sulfate administered every 4 h. Avinza improves quality of sleep by several measures but interestingly gives the best sleep improvement when given in the morning rather than at night. It causes the same side effects of other opioids: constipation, nausea, vomiting, somnolence and mood swings. Doses of 30 - 60 mg/day have been shown to be well tolerated by patients with osteoarthritis (even in the elderly), who have failed other medications.
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PMID:Avinza - 24-h sustained-release oral morphine therapy. 1499 42

The current use of multimodal analgesia for the management of postoperative pain has resulted in reduced side effects and improved pain relief. Limitations of the technology associated with current pump- or catheter-based systems have prompted the development of continuous delivery systems and extended-duration techniques for pain relief. Among these are morphine sulfate sustained-release liposome injection (Morphine SR, DepoMorphine) and the patient-controlled transdermal system (PCTS, E-TRANS). Morphine SR utilizes the novel DepoFoam technology, a novel delivery system that allows the drug to be gradually released into the surrounding epidural space. Morphine SR is compatible with anticoagulation therapy and eliminates interference from pump and intravenous (IV) equipment. Administration of Morphine SR during hip arthroplasty significantly reduced patients' postoperative consumption of fentanyl. E-TRANS fentanyl PCTS is a transdermal system attached to the patient's arm or upper chest; a button on the device is controlled by the patient to deliver doses of fentanyl. In a study comparing fentanyl HCl PCTS with conventional IV-patient-controlled analgesia (PCA) morphine, PCTS was found to be as safe and effective as PCA for the treatment of postoperative pain. Novel delivery systems that are less invasive, that are compatible with anticoagulation regimens, and that provide continuous delivery, thus preventing analgesic gaps, will facilitate rehabilitation and recovery and ultimately improve patient outcomes.
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PMID:Emerging techniques for postoperative analgesia in orthopedic surgery. 1519 38

Tramadol is an analgesic and antitussive agent that is metabolized to O-desmethyltramadol (M1), which is also active. Tramadol and M1 exert their mode of action through complex interactions between opiate, adrenergic, and serotonin receptors. The pharmacokinetics of tramadol and M1 were examined following intravenous and oral tramadol administration to six healthy dogs, as well as intravenous M1 to three healthy dogs. The calculated parameters for half-life, volume of distribution, and total body clearance were 0.80 +/- 0.12 h, 3.79 +/- 0.93 L/kg, and 54.63 +/- 8.19 mL/kg/min following 4.4 mg/kg tramadol HCl administered intravenously. The systemic availability was 65 +/- 38% and half-life 1.71 +/- 0.12 h following tramadol 11 mg/kg p.o. M1 had a half-life of 1.69 +/- 0.45 and 2.18 +/- 0.55 h following intravenous and oral administration of tramadol. Following intravenous M1 administration the half-life, volume of distribution, and clearance of M1 were 0.94 +/- 0.09 h, 2.80 +/- 0.15 L/kg, and 34.93 +/- 5.53 mL/kg/min respectively. Simulated oral dosing regimens at 5 mg/kg every 6 h and 2.5 mg/kg every 4 h predict tramadol and M1 plasma concentrations consistent with analgesia in humans; however, studies are needed to establish the safety and efficacy of these doses.
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PMID:Pharmacokinetics of tramadol and the metabolite O-desmethyltramadol in dogs. 1530 53

The aim of the investigation was to assess the pharmacokinetic characteristics and safety of articaine HCl used in tumescent local anesthesia for liposuction. Maximum plasma concentrations of articaine HCl were observed from 136 to 264 ng/mL, on average, from 1.2 to 4.3 hours after the start of infiltration, depending on the area of liposuction. The average extent of absorption ranged from 827 to 2203 ng*h/mL. Average maximum plasma concentrations of articainic acid ranged from 1719 to 7292 ng/mL. The high articainic acid concentrations at 1 hour after the start of infiltration indicate that articaine HCl was hydrolyzed rapidly by esterases in tissue and plasma. Although up to 38.2 mg/kg body weight articaine HCl was applied, no cardiac side effects or symptoms of central nervous intoxication occurred. Articaine HCl provided a safe and sufficient analgesia for tumescent liposuction.
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PMID:Pharmacokinetics of articaine hydrochloride in tumescent local anesthesia for liposuction. 1549 46

Although it is widely accepted that delta9-tetrahydrocannabinol (delta9-THC) is the primary psychoactive constituent of marijuana, questions persist as to whether other components contribute to marijuana's pharmacological activity. The present experiments assessed the cannabinoid activity of marijuana smoke exposure in mice and tested the hypothesis that delta9-THC mediates these effects through a CB1 receptor mechanism of action. First, the effects of delta9-THC on analgesia, hypothermia, and catalepsy were compared with those of a marijuana extract with equated delta9-THC content after either i.v. administration or inhalation exposure. Second, mice were exposed to smoke of an ethanol-extracted placebo plant material or low-grade marijuana (with minimal delta9-THC but similar levels of other cannabinoids) that were impregnated with varying quantities of delta9-THC. To assess doses, delta9-THC levels in the blood and brains of drug-exposed mice were determined following both i.v. and inhalation routes of administration. Both marijuana and delta9-THC produced comparable levels of antinociception, hypothermia, and catalepsy regardless of the route of administration, and these effects were blocked by pretreatment with the CB1 antagonist SR141716 [N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide HCl]. Importantly, the blood and brain levels of delta9-THC were similar in mice exhibiting similar pharmacological effects, regardless of the presence of non-delta9-THC marijuana constituents. The present experiments provide evidence that the acute cannabinoid effects of marijuana smoke exposure on analgesia, hypothermia, and catalepsy in mice result from delta9-THC content acting at CB1 receptors and that the non-delta9-THC constituents of marijuana (at concentrations relevant to those typically consumed) influence these effects only minimally, if at all.
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PMID:Delta9-tetrahydrocannbinol accounts for the antinociceptive, hypothermic, and cataleptic effects of marijuana in mice. 1583 44


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