Disease relevance of Marcaine

• 3. This synergistic effect of systemic morphine on the extent of neural blockade with epidural bupivacaine may have an important role in improving postoperative pain relief [1].
• However, accidental intravascular injection of bupivacaine can produce severe arrhythmias and cardiac depression [2].
• METHODS AND RESULTS: Forty patients with unstable angina refractory to standard anti-anginal therapy were randomized to receive either continuous epidural infusion of bupivacaine (TEA, Th1 to Th5) or to standard anti-anginal therapy including beta-blockers, calcium antagonists, aspirin, heparin, and nitroglycerin infusion (control group) [3].
• Bupivacaine also inhibited alcohol-induced GIRK currents in the absence of functional pertussis toxin-sensitive G proteins [4].
• In contrast, fibers from the esophagus (which we show to be more fatigable than flexor digitorum brevis fibers) and from the highly glycolytic extensor digitorum longus didn't undergo pyridine nucleotide oxidation upon the addition of bupivacaine and were resistant to bupivacaine toxicity [5].

Psychiatry related information on Marcaine

• In Experiment 1, bilateral inactivation of the BLA via infusion of bupivacaine impaired decision making, reducing the preference for the HR arm [6].
• Preoperative lumbar epidural blockade with bupivacaine and morphine reduces the incidence of phantom limb pain in the first year after operation [7].
• Between group comparison revealed only that the mean % slow-wave sleep (SWS) in the fentanyl group (6.0%, 2.0%, and 14.7%) was different from the bupivacaine group (7.8%, 9.1%, and 10.6%) in the postoperative period after adjusting for the preoperative night % SWS (p=0.021) [8].
• Injections of the local anesthetic, bupivacaine, into the medial striatum, did not impair place acquisition, but impaired place reversal learning [9].
• RESULTS: Inflammatory hypersensitivity was selectively attenuated by very low doses of bupivacaine (concentration range. 0.004-0.0625%), which did not affect the sensory threshold in the contralateral uninflamed limb [10].

High impact information on Marcaine

• RESULTS: The patients who received epidural fentanyl or bupivacaine prior to surgical incision (preemptive analgesia) experienced 33% less pain while hospitalized (P=.007) [11].
• METHODS: In a randomised, double-blind trial, 60 patients scheduled for lower-limb amputation were randomly assigned epidural bupivacaine (0.25% 4-7 mL/h) and morphine (0.16-0.28 mg/h) for 18 h before and during the operation (29 patients; blockade group) or epidural saline (4-7 mL/h) and oral or intramuscular morphine (31 patients; control group) [12].
• For standard epidural analgesia, 25 mg (10 mL of 0.25%) bupivacaine was injected into the epidural space, followed by top-ups of 6-10 mL 0.25% bupivacaine, as required [13].
• Bupivacaine inhibited GIRK channels within seconds of application, regardless of whether channels were activated through the muscarinic receptor or directly via coexpressed G protein G(beta)gamma subunits [4].
• Mechanism underlying bupivacaine inhibition of G protein-gated inwardly rectifying K+ channels [4].

Chemical compound and disease context of Marcaine

• Human volunteers tolerated a higher intravenous dosage of ropivacaine than bupivacaine before developing initial signs of toxicity [14].
• Rats were implanted with subcutaneous miniosmotic pumps that continuously delivered lidocaine (2 mg.kg-1.h-1), bupivacaine (0.4 mg.kg-1.h-1), tetracaine (1 mg.kg-1.h-1), or saline vehicle, and 6 h later the rats were subjected to 30 min of renal ischemia or to sham operation [15].
• However, current preclinical safety and toxicity data show an advantage for levobupivacaine over bupivacaine [16].
• Management of intractable back pain from caudal ependymoma with spinal methylprednisolone, bupivacaine and morphine [17].
• The authors examined the efficacy of tetrodotoxin with and without epinephrine or bupivacaine for producing prolonged-duration sciatic nerve blockade in the rat, and they assessed the degree of concomitant toxicity [18].

Biological context of Marcaine

• After bupivacaine inhalation, the heart rate response (0.27 +/- 1.04 beats/min/%) was unchanged from control [19].
• In contrast, low levels of bupivacaine block produced significant increases in tonic BP (158.8 +/- 6.4 versus 169.0 +/- 6.5 mm Hg BP), whereas there was no effect on dynamic baroreflex sensitivity (-0.85 +/- 0.08 versus -0.73 +/- 0.08 mm Hg BP/mm Hg CSP) [20].
• It was blocked with high affinity by tetrodotoxin (IC50, approximately 10 nmol/L) and local anesthetics (bupivacaine and lidocaine; IC50, approximately 100 nmol/L) and by Cd2+ (IC50, approximately 300 mumol/L) [21].
• These results suggest that (1) the bupivacaine binding site is located in the inner mouth of the pore, (2) stereoselective block displays subfamily selectivity, and (3) a polar interaction with T505 combined with hydrophobic interactions with L508 and V512 are required for stereoselective block [22].
• Its levels are highest during a period of fetal development that coincides with the emergence of specific fiber types and transiently increases in regenerating muscles damaged by bupivacaine [23].

Anatomical context of Marcaine

• Randomised trial of epidural bupivacaine and morphine in prevention of stump and phantom pain in lower-limb amputation [12].
• Stereoselective block of cardiac sodium channels by bupivacaine in guinea pig ventricular myocytes [2].
• Pharmacological blockade of the spontaneous electrical activity present in primary cultures of rat myotubes by growth in bupivacaine, tetrodotoxin, or KCl was found to increase the number of voltage-sensitive Na+ channels 38-83% as measured by the specific binding of [3H]saxitoxin [24].
• To abolish the effect of rapidly adapting receptors, we used inhaled bupivacaine aerosol, and to abolish the effect of slowly adapting stretch receptor activity, we used sulfur dioxide insufflation [19].
• Evidence for a specific receptor site for lidocaine, quinidine, and bupivacaine associated with cardiac sodium channels in guinea pig ventricular myocardium [25].

Associations of Marcaine with other chemical compounds

• We have investigated the effects of the myotoxic local anesthetic bupivacaine on rat skeletal muscle mitochondria and isolated myofibers from flexor digitorum brevis, extensor digitorum longus, soleus, and from the proximal, striated portion of the esophagus [5].
• In isolated mitochondria, bupivacaine caused a concentration-dependent mitochondrial depolarization and pyridine nucleotide oxidation, which were matched by an increased oxygen consumption at bupivacaine concentrations of 1.5 mm or less at pH 7.4, whereas respiration was inhibited at higher concentrations [5].
• As a consequence of depolarization, bupivacaine caused the opening of the permeability transition pore (PTP), a cyclosporin A-sensitive inner membrane channel that plays a key role in many forms of cell death [5].
• The adipogenicity of cells from bupivacaine hydrochloride (BPVC)-treated and untreated muscle was compared in vitro [26].
• Influence of bupivacaine on mepivacaine protein binding [27].

Gene context of Marcaine

• CONCLUSION: Ipsilateral or contralateral sciatic blockade using either bupivacaine or tetrodotoxin does not inhibit carrageenan-induced activation of cytokines and p-38 MAPK in spinal cord and DRGs [28].
• In the current study, the authors examined cytokine and p38 mitogen-activated protein kinase (MAPK) activation in lumbar dorsal root ganglia (DRGs) and spinal cord after carrageenan paw injections and sciatic blocks with either bupivacaine or tetrodotoxin [28].
• Cells were preincubated with bupivacaine before and during the transient addition of substance P [29].
• These results demonstrated that bupivacaine degradation into PPX was mediated in humans by CYP3A [30].
• Five days after bupivacaine injection, IGF-II mRNA was increased 46-fold in young rats but was only increased fourfold in adult rats [31].

Analytical, diagnostic and therapeutic context of Marcaine

• Eight patients undergoing abdominal surgery received epidural analgesia with 0.5% plain bupivacaine at a fixed dose rate (8 ml/h) for postoperative pain relief [1].
• Bupivacaine concentration and obstetric delivery [32].
• Findings of case-control study showed that all "cases" received dialysis after the early morning shift, compared to 50% of controls (p = 0.01), and all cases used a multiple-dose vial of local anesthetic (bupivacaine), compared to 58% of controls (p = 0.03) [33].
• BACKGROUND: Bupivacaine is a potent local anesthetic widely used for prolonged local and regional anesthesia [2].
• Finally, T3 and T5 muscles were soaked in a myotoxin, Marcaine, before reimplantation [34].

References