• Korean Journal of Adult Nursing
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• v.20 no.3
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• pp.386-394
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• 2008

Purpose: The purpose of this study was to examine the effect of topical lidocaine cream on pain and anxiety during the AV fistula puncture among hemodialysis patients. Methods: The study employed one group repeated measurement design. The data were collected from 50 hemodialysis patients who received AV fistula puncture. The topical lidocaine cream was applied 30 minutes before the puncture. The data were measured total 3 times (T1=without lidocaine, T2=2% lidocaine, T3=5% lidocaine). Pain was measured by VAS and a behavioral checklist. Anxiety was measured by Korean manual of SCL-90-R. Results: Patients with 5% lidocaine cream reported significantly lower of VAS pain score than those with 2% lidocaine and without lidocaine. Patients with 2% lidocaine cream reported significantly lower of behavioral pain scores than those without lidocaine, but less effective than 5% lidocaine cream. Patients with 2% lidocaine cream reported significantly lower of anxiety scores than those without lidocaine, but less effective than 5% lidocaine cream. Conclusion: Topical application of lidocaine cream for 30 minutes before AV fistula puncture significantly decreased pain and anxiety among hemodialysis patients. Specifically 5% lidocaine was more effective than 2% lidocaine for both pain and anxiety.

• Applied Chemistry for Engineering
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• v.9 no.7
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• pp.1090-1097
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• 1998

Lidocaine compounds have widely been used as local anesthetics. Regarding the molecular mechanism for anesthesia by lidocaine, it is proposed that lidocaine molecules penetrate to the hydrophobic region of cell membrane and expand the membrane volume, producing a change in protein conformation that blocks sodium permeability or lidocaine molecules directly adsorb into lidocaine receptor in the protein channel without expanding the cell membrane. But these proposals have never been proven experimentally. In this study, the expansion of cell membrane by lidocaine compounds was investigated by employing lipid monolayer at the air/water interface as the mimetic system of cell membrane. It was found that oil-soluble lidocaine contracted the area/molecule of lipid in the monolayer of phosphatidyl choline, sphingomyelin, DS-PL95E and lipoid, but expanded the monolayer of phosphatidyl ethanolamine only in a certain range of mixing ratios. On the contrary, water-soluble lidocaine-HCl salt expanded the monolayers of all lipids used in this study.

• Clinics in Shoulder and Elbow
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• v.24 no.4
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• pp.224-230
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• 2021

Background: Local anesthetics often are used in rotator cuff tears as therapeutic tools, although some cases have reported that they have detrimental effects. Neurotropin (NTP) is used widely in Japan as a treatment for various chronic pain conditions and is shown to have protective effects on cartilage and nerve cells. In this study, we investigated the protective effect of NTP against lidocaine-induced cytotoxicity. Methods: Tenocytes from rotator cuff tendons were incubated with lidocaine, NTP, lidocaine with NTP, and a control medium. Cell viability was evaluated using the WST-8 assay. Cell apoptosis was detected via annexin V staining using flow cytometry. The expression of BCL-2 and cytochrome c, which are involved in the intrinsic mitochondrial pathway of apoptosis, was evaluated via Western blotting and immunohistochemical staining. Results: In the cell viability assay, lidocaine decreased cell viability in a dose-dependent manner, and NTP did not affect cell viability. Moreover, NTP significantly inhibited the cytotoxic effect of lidocaine. The flow cytometry analysis showed that lidocaine significantly induced apoptosis in tenocytes, and NTP considerably inhibited this lidocaine-induced apoptosis. Western blotting experiments showed that lidocaine decreased the protein expression of BCL-2, and that NTP conserved the expression of BCL-2, even when used with lidocaine. Immunohistochemical staining for cytochrome c showed that 0.1% lidocaine increased cytochrome c-positive cells, and NTP suppressed lidocaine-induced cytochrome c expression. Conclusions: NTP suppresses lidocaine-induced apoptosis of tenocytes by inhibiting the mitochondrial apoptotic pathway. Intra-articular/bursal injection of NTP with lidocaine could protect tenocytes in rotator cuff tendons against lidocaine-induced apoptosis.

• The Korean Journal of Pain
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• v.14 no.1
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• pp.26-31
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• 2001

Background: Sympathetic blocks with local anesthetics are used to differentiate sympathetically- maintained pain (SMP) from sympathetically-independent pain (SIP). However, systemic lidocaine is also used in the management of neuropathic pain. Therefore, there may be possibility of a false positive response in relieving their pain by systemic absorption of lidocaine following a diagnostic sympathetic block in patients with SIP. In this study, we measured the plasma lidocaine concentrations after a stellate ganglion block (SGB) using three volumes of 1% lidocaine. Methods: This prospective, crossover study was performed in 3 patients who experience sudden hearing loss and in 4 volunteers. Each person received SGB three times using three different volumes (6 ml, 12 ml and 16 ml) of 1% lidocaine at one week intervals. SGB was performed using a 23 G butterfly needle via a paratracheal approach by two persons. Two ml of venous blood was obtained from a prepared contra-lateral sided venous route at 1, 3, 5, 7, 10, 20 and 60 min after SGB. Plasma lidocaine level was analyzed by immunoassay. Results: Mean plasma lidocaine concentrations correlated well with the volumes of 1% lidocaine used in SGB; larger volumes showed higher concentrations (P < 0.01). Mean peak plasma concentrations were $1.08{\pm}0.18$ in 6 ml, $1.90{\pm}0.47$ in the 12 ml and $2.74{\pm}0.67{\mu}g/ml$ in the 16 ml groups (P < 0.01). The mean time to reach peak plasma concentration was not significantly different between the three groups. Conclusions: The peak plasma lidocaine concentrations in SGB using large volume were found to be similar to that of IV lidocaine infusion in the management of neuropathic pain. These data suggest that diagnostic sympathetic block may result in many false positive responses for SMP. Part of its effect may be related to systemic local anesthetic absorption and not to a sympathetic block. Therefore, physicians may be required to use optimal volumes and minimal concentration of local anesthetic in diagnostic sympathetic block procedures and also make a careful assessment of the performance of a permanent sympathetic block.

• The Korean Journal of Pharmacology
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• v.24 no.1
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• pp.17-29
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• 1988

The author examined the effects of lidocaine on the veratrine-or potassium-induced release of neurotransmitters to determine the possible role of amino acid neurotransmitters in lidocaine-induced convulsion. The examined transmitters were gamma-aminobutyric acid (GABA), aspartic acid, glutamic acid and norepinephrine which are released from the synaptosomes. Furthermore, the effects of lidocaine on the binding to receptors and synaptosomal uptake of the two transmitters, GABA and glutamic acid, were determined in crude synaptic membranes and synaptosomes. In addition, the effects of propranolol, norepinephrine and serotonin on the release of amino acid neurotransmitters were also examined. The veratrine-induced release of GABA was most severely inhibited by lidocaine and propranolol, while norepinephrine and serotonin reduced the release of aspartic acid and glutamic acid more than the GABA release. Generally the potassium-induced release was much more resistant to the lidocaine action than the veratrine-induced release. Among the neurotransmitters examined, the aspartic acid release was most prone to the lidocaine action, while the GABA release was most resistant. Concentrations of lidocaine below 1 mM did not significantly change the GABA and glutamic acid receptor binding and uptake. These results indicate that the blocking of sodium channels by lidocaine can result in the selective depression of the GABA release. This may result in unlimited excitation of the central nervous system.

• Journal of Yeungnam Medical Science
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• v.11 no.1
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• pp.30-34
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• 1994

Local anesthetics produce pain during infiltration into skin. The relationship between local anesthetic-induced pain and pH of the local anesthetic solution has not been fully investigated. Commercial preparation of local anesthetics are prepared as acidic solutions of the salts to promote solubility and stability. And the acidity of local anesthetic solition may be related with the pain during infiltration of the solutione. So, we tried to neutralize the lidocaine hydrochloride solution which is one of the most frequently used local anesthetic agent. Sodium bicarbonate was used for neutralization. Sodium bicarbonate was mixed with lidocaine hydrochloride until the resulting pH of the solution become 7.4 which is identical to the acidity of body fluid. To identify the effect of neutralized lidocaine solution, we had a course of double blind test to 6 volunteers. Both forearm of each volunteer were injected with neutralized lidocaine and plain one, and the degree of pain was estimated by each volunteers. According to subjective description by the volinteers, everyone felt neutralized lidocaine injection site was less painful than plain lidocaine. We concluded that we could reduce pain from infiltration of lidocaine hydrochloride by neutralization of the anesthetic solution with sodium bicarbonate.

• The Korean Journal of Pharmacology
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• v.26 no.2
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• pp.121-126
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• 1990

The contractility of isolated rat atria, suspended in Krebs-Ringer bicarbonate medium containing 5.5mM glucose, was depressed approximately 50% by 0.1 mM of lidocaine. Partial recovery of the lidocaine-depressed contractility was achieved by the metabolizable substrates pyruvate, acetate, and fructose, but not by addition of glucose. Glucose produced the dose-dependent increase in the force of contraction of normal atria, whereas pyruvate, acetate, and fructose produced no significant effect in the contractile activity of the normal atria. In the absence of exogenous glucose lidocaine produced more marked depression of atrial contractility than that in the presence of exogenous glucose. The results of this study may confirm that the utilization of cardiac glycogen is also inhibited by lidocaine at sites of the glucose phosphate isomerase step or step between glycogen to glucose-6-phosphate.

• Maxillofacial Plastic and Reconstructive Surgery
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• v.27 no.3
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• pp.276-282
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• 2005

Inferior alveolar nerve block using lidocaine is the most frequent local anesthetic method in the dental treatment, but clinically it is not always successful. The 2% lidocaine cartridge has been used commonly in dental anesthesia. It contains vasoconstrictor and antioxidant, which presents low pH which provides chemical stability and longer shelf life. But alkalinized local anesthetics has less tissue trauma, easier dissociation of the non-ionized base which penetrates nerve sheath, rapid onset and more intensity. In this study, in inferior alveolar nerve block, alkalinized lidocaine using sodium bicarbonate (experimental group) is compared with plain lidocaine (control group) about injection pain, anesthetic onset, duration and postinjection discomfort. In inferior alveolar nerve block, alkalinized lidocaine using sodium bicarbonate showed lower injection pain. There was significant difference statistically from plain lidocaine(p=0.019). Comparing with plain lidocaine, alkalinized lidocaine produced more rapid onset (lip & pulp anesthetic onset), there was no significant difference(p>0.05). but there was boundary significance (0.050.05). These results suggest that addition of sodium bicarbonate to 2% lidocaine(1:100,000 epinephrine) for inferior alveolar nerve block is more effective for reduction of injection pain and onset time.

• Journal of Pharmaceutical Investigation
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• v.37 no.3
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• pp.149-158
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• 2007

To investigate the permeability of lidocaine, percutaneous absorption studies were performed using excised hairless mouse skin and the penetration of lidocaine via the skin was determined. To increase the skin permeation of lidocine, the effects of $Labrasol^{(R)}$, $Labrafil^{(R)}$, $Labrafac^{(R)}$ and $Transcutol^{(R)}$ were investigated. The skin permeation of lidocaine was increased when $Labrasol^{(R)}$ and $Transcutol^{(R)}$ were used as permeation enhancer. To evaluate the influence of ultrasound, various factors such as application modes (continuous mode and pulsed mode), frequency (1.0 and 3.0 MHz) and intensity (1.0, 1.5 and 2.0 w/$cm^2$) were investigated with lidocaine hydrogel. The pronounced effect of ultrasound on the skin permeation of lidocaine was observed at all ultrasound energy levels. The influence of frequency having an effect on skin permeation rate was higher in the case of using 1 MHz, 2.0 w/$cm^2$ and continuous treatment. As the intensity of ultrasound increased, the permeation of lidocaine was accelerated. The in vivo anesthetic effects were evaluated by two aspects as mechanical threshold and electrical threshold. Six healthy volunteers consented to the randomized, double-blind, and cross-over designed study in each group. In each subject, 3 groups were adapted such as K group (ultrasound with gel base only), L group (lidocaine gel) and B group (ultrasound with lidocaine gel). In conclusion, lidocaine was potent anesthetic which could be block pain threshold effectively. And ultrasound could accelerate the skin penetration of lidocaine. The phonophoretic delivery system could be a good candidate for lidocaine as a local anaesthetic to improve the skin permeation and in vivo anaesthetic effect.

• Archives of Craniofacial Surgery
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• v.20 no.4
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• pp.239-245
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• 2019

Background: Lidocaine spray is a local anesthetic that improves random-pattern skin flap survival. The fractional ablative carbon dioxide laser (FxCL) produces vertical microchannels that delivers topically applied drugs to the skin. In this study, we hypothesized that FxCL therapy would enhance the lidocaine effect to improve random-pattern skin flap survival in rats. Methods: McFarlane random-pattern skin flaps were elevated in 48 rats, which were divided into four groups according to treatment: FxCL+lidocaine, FxCL, lidocaine, and nontreatment (control). On postoperative day 7, necrotic flap areas, the number of capillary vessels, and neutrophil count were evaluated. Anti-rat vascular endothelial growth factor (VEGF) and CD31 antibody activity were also evaluated by immunohistochemical staining. Results: Flap survival rate was $53.41%{\pm}5.43%$, $58.16%{\pm}4.80%$, $57.08%{\pm}5.91%$, and $69.08%{\pm}3.20%$ in the control, lidocaine, FxCL, and FxCL+lidocaine groups, respectively. Mean neutrophil count in the intermediate zone excluding the necrotic tissue was $41.70{\pm}8.40$, $35.43{\pm}6.41$, $37.23{\pm}7.15$, and $27.20{\pm}4.24cells/field$ in the control, lidocaine, FxCL, and FxCL+lidocaine groups, respectively. Anti-rat VEGF and CD31 antibody activity were the highest in the FxCL+lidocaine group. Conclusion: FxCL with lidocaine had a positive effect on random-pattern skin flap survival in rats. Thus, FxCL with lidocaine spray should be considered as a new treatment option to improve flap viability.