Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

By means of experiments involving pin-pricking, compositions containing 10% ketocaine base in a mixture of 2-propanol, glycerol and water were found to produce a high frequency of block to cutaneous pain following application to volunteers under an occlusive dressing. The local analgesic efficacy was found to be directly related to the degree of saturation of ketocaine in the vehicle and time of application. The degree of hyperaemia observed in the treated skin areas was found to be related to the degree of local analgesia produced.
 ...
PMID:Local effects produced on intact skin by epicutaneously applied anaesthetic formulations. An experimental study in man. 58 20

A selective high-performance liquid chromatographic method for the determination of bupivacaine in human serum is described. The technique is based on a single extraction of the drug from alkalinized serum with a mixture of hexane-isopropanol-chloroform. Desmethyldoxepin is used as internal standard. The chromatographic system consists of a home-packed Nucleosil C8 (10 microns) column; the mobile phase is acetonitrile--0.05 M potassium phosphate buffer (pH 3.3) (28:72, v/v). The method can accurately measure serum bupivacaine concentrations down to 20 micrograms/l using 500 microliters of sample. The coefficient of variation for intra-assay variability of bupivacaine is 2.1% (n = 13) and for inter-assay variability of bupivacaine 5.7% (n = 11) at 1.00 mg/l. The calibration graph is linear over the range 0.02-5.00 mg/l and the extraction efficiency is 91.8 +/- 3.8% (+/- S.D., n = 7). The method is accurate and sensitive for both clinical and pharmacokinetic studies on bupivacaine in man. The method is applied to the analysis of serum samples obtained from orthopaedic patients during both spinal and epidural analgesia.
 ...
PMID:High-performance liquid chromatographic determination of bupivacaine in human serum. 648 Jul 88

Ane-Pad (A 2358, Astra Lakemedel AB), a new local anesthetic formulation for application to the skin has been tested in the removal of split skin grafts. Ane-Pad is a thin cotton pad, containing a solution of 10% ketocaine base in a solvent mixture of isopropanol, glycerol and water. The pad has been used on the donor sites of 173 patients with a minimum application time of 1 h before surgery. Eighteen patients complained of slight, transient irritation immediately after application. After removal of the pad erythema was present in 39 patients and oedema in eight. In 157 patients (90.8%) analgesia was adequate. Two patients (1.1%) needed additional anaesthesia. The concentration of ketocaine in the blood was measured in 101 patients and did not exceed 850 ng ml--1. Therewere no systemic side-effects.
 ...
PMID:New anaesthetic formulation for epicutaneous application tested for cutting split skin grafts. 699 Sep 49

Our study describes an original technique of continuous popliteal sciatic nerve block (CPSB) (Group A, 60 patients) and compares its analgesic efficacy after foot surgery with intramuscular (IM) opioids (Group B, 15 patients) and intravenous patient-controlled analgesia (IV PCA) with morphine (Group C, 45 patients). CPSB was performed using Singelyn's landmarks. The sciatic nerve was localized with a short-beveled needle connected to a peripheral nerve stimulator. A 20-gauge catheter was placed at the same depth as the needle with a Seldinger technique. Thirty milliliters of 1% mepivacaine with epinephrine 1/200,000 was injected and followed by a continuous infusion of 0.125% bupivacaine with sufentanil 0.1 microgram/mL and clonidine 1 microgram/mL at 7 mL/h for 48 h. Postoperative analgesia (intravenous [IV] propacetamol [PRO] and/or IM piritramide [DIPI]) was standardized. Postoperative pain score (PPS), supplemental analgesia, and side effects were noted. CPSB was easy to perform in 55 patients (92%). In Group A, highest and mean PPS were significantly lower, and the mean dose of PRO was reduced by 62% and 36% when compared with Group B and C, respectively. Only 8% of patients required postoperative opioid in Group A compared with 91% and 100% in Groups B and C, respectively. No immediate or delayed complications other than postoperative technical problems (kinked or broken catheter 25%) were noted in Group A. In conclusion, CPSB is easy to perform, safe, and a more efficient technique than parenteral opioid for providing postoperative analgesia after foot surgery.
 ...
PMID:Continuous popliteal sciatic nerve block: an original technique to provide postoperative analgesia after foot surgery. 902 34

The recently identified 17-amino acid peptide nociceptin (orphanin FQ) is the endogenous ligand for the opioid receptor-like-1 (ORL-1) receptor. A physiologic role for nociceptin (OFQ) activation of the ORL-1 receptor (OFQR) may be to modulate opioid-induced analgesia. The molecular mechanism by which nociceptin (OFQ) and ORL-1 (OFQR) modify opioid-stimulated effects, however, is unclear. Both ORL-1 (OFQR) and opioid receptors mediate pertussis toxin (PTX)-sensitive signal transduction, indicating these receptors are capable of coupling to Gi/Go proteins. This study determines that nociceptin stimulates an intracellular signaling pathway, leading to activation of mitogen-activated protein (MAP) kinase in CHO cells expressing ORL-1 receptor (OFQR). Nociceptin (OFQ)-stimulated MAP kinase activation was inhibited by PTX or by expression of the carboxyl terminus of beta-adrenergic receptor kinase (betaARKct), which specifically blocks Gbetagamma-mediated signaling. Expression of the proline-rich domain of SOS (SOS-PRO), which inhibits SOS interaction with p21ras, also attenuated nociceptin (OFQ)-stimulated MAP kinase activation. The phosphatidylinositol 3-kinase (PI-3K) inhibitors wortmannin and LY294002 reduced nociceptin (OFQ)-stimulated MAP kinase activation, whereas inhibition of protein kinase C (PKC) activity by bisindolylmaleimide I or cellular depletion of PKC had no effect. In a similar manner, in cells expressing mu-opioid receptor, [D-Ala2,N-Me-Phe4,Gly-ol]-enkephalin (DAMGO; a mu-opioid receptor-selective agonist) stimulated PTX-sensitive MAP kinase activation that was inhibited by wortmannin, LY294002, betaARKct expression, or SOS-PRO expression but not affected by inhibition of PKC activity. These results indicate that both ORL-1 (OFQR) and mu-opioid receptors mediate MAP kinase activation via a signaling pathway using the betagamma-subunit of Gi, a PI-3K, and SOS, independent of PKC activity. In cells expressing both ORL-1 (OFQR) and mu-opioid receptors, pretreatment with nociceptin decreased subsequent nociceptin (OFQ)- or DAMGO-stimulated MAP kinase activation. In contrast, pretreatment of cells with DAMGO decreased subsequent DAMGO-stimulated MAP kinase but had no effect on subsequent nociceptin (OFQ)-stimulated MAP kinase activation. These results demonstrate that nociceptin (OFQ) activation of ORL-1 (OFQR) can modulate mu-opioid receptor signaling in a cellular system.
 ...
PMID:Nociceptin (ORL-1) and mu-opioid receptors mediate mitogen-activated protein kinase activation in CHO cells through a Gi-coupled signaling pathway: evidence for distinct mechanisms of agonist-mediated desensitization. 972 27

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.
 ...
PMID:Stereoselective high-performance liquid chromatographic determination of ketamine and its active metabolite, norketamine, in human plasma. 1107 75

Continuous peripheral nerve blocks refer to a local anesthetic solution administered via perineurally placed catheters in an effort to extend the benefits of a single-shot peripheral nerve block. They offer several advantages in the postoperative period including excellent analgesia, reduced opioid consumption and associated side effects, enhanced rehabilitation and improved patient satisfaction. The current trend towards less invasive, one-day surgery and enhanced recovery programs may decrease the requirement of catheter use. Prolonged motor block in particular is associated with undesirable outcomes. Should we routinely use continuous peripheral nerve blocks in our daily practice? This PRO-CON debate aims at answering the question from the experts' perspectives. Fascial compartment and wound catheters are outside the scope of this debate.
 ...
PMID:Catheter use in regional anesthesia: pros and cons. 3163 May 6