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Topic: Bupivacaine

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	Comparative efficacy and pharmacokinetics of racemic bupivacaine and S-bupivacaine in third molar surgery
		Bupivacaine is an amide type local anesthetic widely used in surgery and obstetrics for sustained peripheral and central nerve blockade.
		The highest blood concentration of bupivacaine hydrochloride in our study was 738 ng ml-1 (equivalent to 655 ng ml-1 of bupivacaine free base) after dosing with S-bupivacaine.
		Abraham, I., Fawcett, J.P., Kennedy, J., Kumar, A. and Ledger, R., Simultaneous analysis of lignocaine and bupivacaine enantiomers in plasma by high-performance liquid chromatography.
	www.ualberta.ca /~csps/JPPS5(2)/J.Fawcett/buppivacaine.htm (3139 words)

	Local anesthetic bacterial activity
		Bupivacaine at a concentration of 2.5 mg/ml inhibited the growth of the sensitive S. epidermidis strain, S. pyogenes, and S. pneumoniae, and all of the others except P. aeruginosa at a concentration of 5 mg/ml.
		The pathogen was exposed to 0.5% bupivacaine for 1, 3, 6, 12, and 24 h at 37 degrees C and room temperature.
		The pathogen was exposed to 0.5% bupivacaine with preservatives or to the preservatives alone for 1, 3, 6, 12, and 24 hours at 37 degrees C and at room temperature.
	www.csen.com /anesthesia/ropivacaine.htm (2685 words)

	Bupivacaine news articles (Site not responding. Last check: 2007-10-12)
		The anesthetic mixture consisted of 0.5 mL/kg of bupivacaine 0.5% and lidocaine hydrocarbonate 2% (1:3 vol.) with epinephrine 1:200,000.
		Spinal anesthesia induced with 12.5 mg bupivacaine was administered to all patients.
		The main concern with the use of the long-acting local anesthetics bupivacaine and ropivacaine is inadvertent IV injection, which exposes the heart to toxic...
	www.mongabay.com /drugs/drugs/Bupivacaine.html (1400 words)

	Marcaine Online, Description, Chemistry, Ingredients - Bupivacaine - RxList Monographs
		Sensorcaine® (bupivacaine HCl) injections are sterile isotonic solutions that contain a local anesthetic agent with and without epinephrine (as bitartrate) 1:200,000 and are administered parenterally by injection.
		However, bupivacaine possesses a greater degree of lipid solubility and is protein bound to a greater extent than lidocaine.
		Bupivacaine is related chemically and pharmacologically to the aminoacyl local anesthetics.
	www.rxlist.com /cgi/generic2/bupivacaine.htm (340 words)

	British Journal of Pharmacology - Effects of levobupivacaine, ropivacaine and bupivacaine on HERG channels: ...
		Bupivacaine is an amide-type local anaesthetic widely used for regional anaesthesia (Strichartz, 1987) that exhibits a high cardiotoxicity, likely due to its ability to depress the intracardiac conduction velocity and cardiac contractility (Kotelko et al., 1984).
		Bupivacaine induced cardiotoxicity has been mostly related to the effects of its R(+) enantiomer (Luduena et al., 1972; Aberg, 1972), which exhibits a higher potency for blocking cardiac Na and hKv1.5 channels (Valenzuela et al., 1995a, b; Nau et al., 2000).
		At physiological pH, levobupivacaine, ropivacaine and bupivacaine are predominantly positively charged (pKa=8.1) and this voltage dependence of block can be interpreted as the consequence of the effects of the transmembrane electrical field on the interaction between the cationic form of the drugs and their receptor site at the channel.
	www.nature.com /bjp/journal/v137/n8/full/0704978a.html (5649 words)

	Oxidative Metabolism of Bupivacaine into Pipecolylxylidine in Humans Is Mainly Catalyzed by CYP3A -- Gantenbein et al. ...
		Bupivacaine is used to provide prolonged anesthesia and postoperative analgesia.
		Bupivacaine, introduced in 1963, is a widely used amide local anesthetic.
		Bupivacaine and PPX were kindly provided by Janssen (Boulogne, France).
	dmd.aspetjournals.org /cgi/content/full/28/4/383 (1835 words)

	How can we use ropivacaine in clinical practice ?
		At higher concentration, the difference between bupivacaine and ropivacaine in terms of motor blockade is tenuous (8).
		On the other hand, when comparing 0.175% ropivacaine with 0.2% bupivacaine, both combined with sufentanil (1 mcg.ml-1), and given as a 5 ml.h-1 epidural infusion after abdominal surgery, it appears that 80% of the patients achieved satisfactory ambulation on the first postoperative day with ropivacaine, versus 60% with bupivacaine.
		infusions of ropivacaine, bupivacaine and placebo in volunteers.
	www.euroanesthesia.org /education/rc_vienna/08rc2.HTM (1979 words)

	Caudal Ropivacaine Versus Bupivacaine For Paediatric Day-case Circumcision Procedures
		Although a total of 115 patients were recruited for the study, 2 patients in the ropivacaine group and 1 patient from the bupivacaine group were withdrawn due to block failure.
		Ropivacaine administered by the caudal route is reported to be ~ 40% less potent than bupivacaine at equal doses [15], implying that when higher concentrations of ropivacaine are used for centroneuraxial blockade (at equipotent doses as bupivacaine), significant motor block and delayed hospital discharge may ensue.
		In our study, we chose to compare ropivacaine and bupivacaine at a lower concentration of 0.2% to elicit if ropivacaine could produce effective sensory blockade with even less motor blockade, since significant motor block may be concentration-dependent.
	www.ispub.com /ostia/index.php?xmlFilePath=journals/ija/vol4n4/caud.xml (1859 words)

	Clinical Trial: Rofecoxib and Bupivacaine to Prevent Pain after Third Molar (Wisdom Tooth) Extraction
		Bupivacaine is a local anesthetic similar to lidocaine, but longer acting.
		Healthy normal volunteers between 16 and 35 years of age who are in general good health and require extraction of their two lower wisdom teeth may be eligible for this study.
		The combination regimen with bupivacaine and rofecoxib is predicted to maximally suppress the onset and intensity of postoperative dental pain to a greater extent than all other groups through a blockade of the nociceptive input from both surgery and inflammation.
	www.clinicaltrials.gov /ct/gui/show/NCT00050362 (1123 words)

	American Journal of Critical Care: Use of intercostal bupivacaine with epinephrine after surgery to decrease use of ... (Site not responding. Last check: 2007-10-12)
		In a recent case study, (2) 0.025% bupivacaine was injected into 2 small catheters placed in the intercostal tissues in a 56-year-old woman after open heart surgery.
		Those in group A were given infusions of bupivacaine via the intercostal catheter for 24 hours and then infusions of isotonic sodium chloride solution for 24 hours; those in group B were given isotonic sodium chloride solution first and then bupivacaine.
		We also hypothesized that infiltration of bupivacaine with epinephrine, a nonnarcotic analgesic, into the intercostal tissues just before closure of the mediastinum after open heart surgery would decrease pain and thus decrease the amount of narcotics used postoperatively.
	www.findarticles.com /p/articles/mi_m0NUB/is_5_11/ai_91473104 (1376 words)

	Comparison of ropivacaine 0.1%-fentanyl and bupivacaine 0.125% - fentanyl infusions for epidural labour analgesia -- ...
		Comparison of bupivacaine- and ropivacaine -induced conduction blockade in the isolated rabbit vagus nerve.
		Relative analgesic potencies of ropivacaine and bupivacaine for epidural analgesia in labor.
		A double-blind comparison of 0.125% ropivacaine with sufentanil and 0.125% bupivacaine with sufentanil for epidural labor analgesia.
	www.cja-jca.org /cgi/content/full/47/8/740 (2531 words)

	Bupivacaine Myotoxicity Is Mediated by Mitochondria -- Irwin et al. 277 (14): 12221 -- Journal of Biological Chemistry
		Bupivacaine is a local anesthetic that induces rapid degeneration of skeletal muscle fibers (1, 2).
		bupivacaine was ineffective at inducing contracture of striated
		Responses of soleus, EDL, and esophagus fibers to bupivacaine; correlation to fiber MHC composition.
	www.jbc.org /cgi/content/full/277/14/12221 (5273 words)

	A COMPARISON OF EPIDURAL ANAESTHESIA WITH XYLAZINE, BUPIVACAINE IN WEST AFRICAN DWARF GOATS.
		Duration of analgesia was 148.0±23.1min with xylazine, 90.0±2.15 min for bupivacaine and 139.0±57.6min with bupivacaine/xylazine mixture.
		Duration of recumbency was 117.0±17.2min with xylazine, 174.2±62.3min with bupivacaine, and 138.0±63.6min with bupivacaine/xylazine mixture.
		The aim of this study was to compare the effects of the epidurally administered bupivacaine, xylazine and bupivacaine/xylazine mixture in goats with regard to: time to recumbency, onset and duration of analgesia, duration of recumbency, and time to standing.
	www.isrvma.org /article/57_2_4.htm (2685 words)

	BioMed Central \| Full text \| Acetylcholinesterase assay for cerebrospinal fluid using bupivacaine to inhibit ...
		The influence of bupivacaine on the activity of both cholinesterases is demonstrated in Figure 2.
		Three equations (0.1; 0.2 and 0.5 mmol/l bupivacaine concentration) were generated after analysis of pharmacokinetic data (Figure 1).
		Bupivacaine is a save inhibitor and could even be provided together with the substrate ACh, DTNB and eserine salizylate in a standardized test kit.
	www.biomedcentral.com /1471-2091/2/17 (2924 words)

	Assembly with the Kvbeta 1.3 Subunit Modulates Drug Block of hKv1.5 Channels -- González et al. 62 (6): 1456 -- ...
		40 mV in the absence and in the presence of bupivacaine.
		80 to +60 mV in the absence and in the presence of bupivacaine.
		Kasten GW and Martin ST (1985) Bupivacaine cardiovascular toxicity: comparison of treatment with bretylium and lidocaine.
	molpharm.aspetjournals.org /cgi/content/full/62/6/1456 (4025 words)

	Continuous mixed venous oxygen saturation, not mean blood pressure, is associated with early bupivacaine cardiotoxicity ...
		Continuous mixed venous oxygen saturation, not mean blood pressure, is associated with early bupivacaine cardiotoxicity in dogs: [La saturation en oxygene du sang veineux mele, mais non la tension arterielle moyenne, est associee a une cardiotoxicite precoce a la bupivacaine chez les chiens] -- Kim et al.
		Mechanism for bupivacaine depression of cardiac conduction: fast block of sodium channels during the action potential with slow recovery from block during diastole.
		Bupivacaine cardiotoxicity in a patient with renal failure.
	www.cja-jca.org /cgi/content/full/50/4/376 (2324 words)

	Microdialysis (Site not responding. Last check: 2007-10-12)
		Determination of Local Tissue Concentrations of Bupivacaine Released from Biodegradable Microspheres and the Effect of Vasoactive Compounds on Bupivacaine Tissue Clearance Studied by Microdialysis Sampling.
		bupivacaine resulted in decreased bupivacaine delivery compared to bupivacaine alone, whereas the addn.
		Dexamethasone, a vasoconstrictor, decreases the clearance rate of bupivacaine from the tissue resulting in a higher, prolonged tissue concn.
	www.chem.ku.edu /Lunte_Grp/projects/Microdialysis.html (6411 words)

	Local Anesthetic Block of Kv Channels: Role of the S6 Helix and the S5-S6 Linker for Bupivacaine Action -- Nilsson et ...
		374 in the S5-S6 linker decreased the bupivacaine affinity
		The effect of bupivacaine (0, 100, 300, and 1000 µM) on the ionic currents of Kv channels indicated.
		The bupivacaine concentrations are 0, 100, 300, and 1000 µM. B, conductance versus voltage curves (Eq.
	molpharm.aspetjournals.org /cgi/content/full/63/6/1417 (6168 words)

	Developments in local anaesthetic drugs -- Whiteside and Wildsmith 87 (1): 27 -- British Journal of Anaesthesia
		Comparison of bupivacaine and ropivacaine induced conduction blockade in the isolated rabbit vagus nerve.
		Mechanism for bupivacaine depression of cardiovascular conduction: fast block of sodium channels during the action potential with slow recovery from block during diastole.
		Relative analgesic potencies of ropivacaine and bupivacaine for epidural analgesia in labour.
	bja.oxfordjournals.org /cgi/content/full/87/1/27 (5526 words)

	Double Blind Randomized Clinical Trial Examining the Efficacy of Bupivacaine Suprascapular Nerve Blocks in Frozen ... (Site not responding. Last check: 2007-10-12)
		Objective.To determine whether the pain, contracture, and disability associated with idiopathic frozen shoulder are diminished by a series of 3 indirect bupivacaine suprascapular nerve blocks delivered in an ambulatory care clinic.
		The use of bupivacaine suprascapular nerve blocks was effective in reducing the pain of frozen shoulder at one month.
		Clinical studies with a larger number of subjects and a longer study period will help determine the duration and nature of the effect of bupivacaine suprascapular nerve blocks in treating the pain, disability, and glenohumeral joint contracture of frozen shoulder.
	www.jrheum.com /abstracts/abstracts00/1464.html (348 words)

	Stereoselective Block of Cardiac Sodium Channels by Bupivacaine in Guinea Pig Ventricular Myocytes -- Valenzuela et al. ...
		Bupivacaine is therapeutically used as a racemic mixture.
		The level of block induced by both bupivacaine enantiomers at the end of the train was similar, although the kinetics of development of block was different (see Table 3
		Clarkson C, Hondeghem L. Mechanism for bupivacaine depression of cardiac conduction: fast block of sodium channels during the action potential with slow recovery from block during diastole.
	circ.ahajournals.org /cgi/content/full/92/10/3014 (6700 words)

	Bupivacaine from PDR - Childbirth.org
		The elimination of drug from tissue distribution depends largely upon the ability of binding sites in the circulation to carry it to the liver where it is metabolized.
		After injection of MARCAINE for caudal, epidural, or peripheral nerve block in man, peak levels of bupivacaine in the blood are reached in 30 to 45 minutes, followed by a decline to insignificant levels during the next three to six hours.
		Various pharmacokinetic parameters of the local anesthetics can be significantly altered by the presence of hepatic or renal disease, addition of epinephrine, factors affecting urinary pH, renal blood flow, the route of drug administration, and the age of the patient.
	www.childbirth.org /articles/bupiv.html (1051 words)

	A COMPARISON OF EPIDURAL ANAESTHESIA WITH LIGNOCAINE, BUPIVACAINE AND MIXTURES
		A mixture of 2% lignocaine (LIG) and 0.5% bupivacaine (BUP), at respective dose rates of 2.9mg/kg and 1 mg/kg, was compared to LIG (5.7mg/kg) and BUP (2mg/kg) for lumbosacral epidural anaesthesia in five awake dogs.
		Whereas LIG is known to have excellent diffusion and penetrability, as well as produce rapid onset and establishment of surgical anaesthesia, it does not produce prolonged sensory and motor blockade.
		Bupivacaine hydrochloride (Marcain, Astra Pharmaceuticals, UK), supplied as a 0.5% stable, colourless aqueous solution for injection in a 4-ml ampoule.
	www.isrvma.org /article/56_3_2.htm (2150 words)

	Vasodilation Increases the Threshold for Bupivacaine-Induced Convulsions in Rats -- Oda et al. 98 (3): 677 -- ...
		Bupivacaine affects the vascular resistance by peripheral and
		decrease the CNS toxicity of bupivacaine in awake, spontaneously
		plasma concentration of bupivacaine or in concentration of bupivacaine
	www.anesthesia-analgesia.org /cgi/content/abstract/98/3/677 (317 words)

	Patient supplemented epidural analgesia after major abdominal surgery with bupivacaine/fentanyl or ropivacaine/fentanyl ...
		Relative analgesic potencies of ropivacaine and bupivacaine for epidural analgesia in labor: implications for therapeutic indexes.
		Role of spinal opioid receptors in the antinociceptive interactions between intrathecal morphine and bupivacaine.
		Patient-controlled epidural analgesia with bupivacaine and fentanyl on hospital wards.
	www.cja-jca.org /cgi/content/full/47/1/27 (2679 words)

	Bupivacaine inhibits human neuronal Kv3 channels in SH-SY5Y human neuroblastoma cells -- Friederich et al. 88 (6): 864 ...
		Bupivacaine inhibits human neuronal Kv3 channels in SH-SY5Y human neuroblastoma cells -- Friederich et al.
		The aim of this study was to characterize the effects of bupivacaine
		plasma concentrations of bupivacaine that are estimated to cause
	bja.oxfordjournals.org /cgi/content/full/88/6/864 (1171 words)

	Ropivacaine in Obstetric Anaesthesia
		This is not always the case with bupivacaine overdosage (Chapter 12).
		Ropivacaine toxicity from overdosage does not seem to be worsened by pregnancy (unlike bupivacaine) so that the convulsive dose is the same in the pregnant and the non-pregnant female (13, 14).
		Indeed, the dysrhythmia dose threshold is (approximately) bupivacaine 3.4: ropivacaine 1.7 : lignocaine 1.0 (Chapter 37).
	www.manbit.com /oa/c4.htm (951 words)

	Cerebrospinal Fluid Bioavailability and Pharmacokinetics of Bupivacaine and Lidocaine after Intrathecal and Epidural ...
		Deleu D, Sarre S, Ebinger G and Michotte Y (1995) The effect of carbidopa and entacapone pretreatment on the L-dopa pharmacokinetics and metabolism in blood plasma and skeletal muscle in beagle dog: An in vivo microdialysis study.
		Rosenberg PH, Kytta J and Alila A (1986) Absorption of bupivacaine, etidocaine, lignocaine and ropivacaine into n-heptane, rat sciatic nerve, and human extradural and subcutaneous fat.
		Wang Y, Wong SL and Sawchuk RJ (1993) Microdialysis calibration using retrodialysis and zero-net flux: Application to a study of the distribution of zidovudine to rabbit cerebrospinal fluid and thalamus.
	www.jpet.org /cgi/content/full/289/2/1015 (4720 words)

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