• Archives of Pharmacal Research
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• v.8 no.4
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• pp.205-211
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• 1985

The distribution of local anesthetics between the hydrocarbone interior and surface area of the lipid bilayer of liposomal membrane was calculated employeg fluorescence probe technique. The quenching of fluorescence probe technique. The quenching of fluorescence probe technique. The quenching of fluorescence of 12-(9-anthroyl) stearic acid and N-octadecyl naphthyl-2-amini-6-sulfonic acid by the local anesthetics in liposomal system was used to calculate the distribution. The Stern-Volmer equation was modified and employed for this calculation. The results showed that procaine hydrocloride and benzocaine were mainly distributed on the surface area of the lipid bilayer of the liposoal membrane, while tetracaine hydrochloride penetrated effectively into the hydrocarbon interior and showed even distribution in the lipid bilayer.

• Journal of the Korean Society of Laryngology, Phoniatrics and Logopedics
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• v.31 no.2
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• pp.56-60
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• 2020

Vocal fold injections are usually performed with a patient wake in an office under local anesthesia. For comfortable and safe office-based procedures, thorough anesthesia and premedication should be provided to the following three regions; nasal cavity, oropharynx, and larynx. Topical lidocaine is most widely used anesthetics on office based procedure. Lidocaine has a low to intermediate potency, 45 minutes to 60 minutes' duration of action, and onset of sufficient anesthesia within 90 seconds of topical administration. Tetracaine, prilocaine, ropivacaine, and bupivacaine also have been used in the office-based procedures. Nasal decongestant, oxymetazoline, is also used for widening nasal cavity by constriction of nasal mucosa. The amount of topical and local anesthetics used in vocal fold injection rarely exceeds toxic doses. The physician should know proper anesthesia techniques and must be familiar with the safe dose and complication of all anesthetics used.

• The Korean Journal of Pain
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• v.1 no.1
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• pp.91-97
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• 1988

Herein is a review of eigthy six surgical cases from March to August, 1986 which recieved tetracaine hydrochloride spinal anesthesia. In an attempt to relieve postoperative pain, 0.5 mg morphine sulfate was administrated into the lumbar subarachnoid space. Pruritus, a side effect of intraspinal morphine, was explored in detail. The results were as follows : 1) The incidence of pruritus was 67.4%, 65.5% in man and 71.0% in woman. 2) The time of onset of pruritus was between 30 and 120 minutes with an average of 79.1 minutes. 3) Pruritus primary occurred on the face(87.9%), especially on the nasal, perinasal and periocular areas. Other sites included the scalp, neck, chest, abdomen, shoulder, hip, thigh, flank, and whole body. 4) The severity of pruritus was classified as mild and moderate, but 4 cases(6.9%) were regarded as severe and were treated with naloxone. 5) The duration of pruritus was from 15 minutes to 19 hours with an average of 4.7 hours. 6) There was no significant difference in the prevention of pruritus between the group recieving diphenhydramine and the one which received normal saline.

• The Korean Journal of Pain
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• v.1 no.1
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• pp.98-102
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• 1988

In order to control the pain after hemorrhoidectomy and anal fistulectomy, 6 mg of 0.5% hyperbaric tetracaine without(control, group I) or wilt 0.3 mg(group II) or 0.5 mg (group III) of 0.1% morphine was injected with a 22 gauge spinal needle into the subarachnoid space through L 3-4 interspace of patients in lateral position. About 30 minutes in Fowler' sposition after injection, operation was performed in lithotomy position. All the patients who ha4 morphine showed remarkable relief of postoperative pain for an average of 27 hours. However, the dosage(0.3 or 0.5 mg) of morphine administered did not affect the duration of pain relief. Blood pressure, pulse rate and pupil size were unchanged in all patients. Dysuria after block developed for on average of 5,6, 13.2 and 14.6 hours in group I, II and III respectively. Most of these cases required urethral catheterization. Minor complications such as nausea, vomiting, itching, fever, burning sensation and paresthesia were observed 16.7, 20 and 20% of cases in group I, II and III respectively; however, no treatment was required.

• The Korean Journal of Physiology and Pharmacology
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• v.8 no.2
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• pp.101-110
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• 2004

Voltage-sensitive release mechanism was pharmacologically dissected from the $Ca^{2+}-induced\;Ca^{2+}\;release$ in the SR $Ca^{2+}$ release in the rat ventricular myocytes patch-clamped in a whole-cell mode. SR $Ca^{2+}$ release process was monitored by using forward-mode $Na^+-Ca^{2+}$ exchange after restriction of the interactions between $Ca^{2+}$ from SR and $Na^+-Ca^{2+}$ exchange within micro-domains with heavy cytosolic $Ca^{2+}$ buffering with 10 mM BAPTA. During stimulation every 10 s with a pulse roughly mimicking action potential, the initial outward current gradually turned into a huge inward current of $-12.9{\pm}0.5\;pA/pF$. From the inward current, two different inward $I_{NCX}s$ were identified. One was $10\;{\mu}M$ ryanodine-sensitive, constituting $14.2{\pm}2.3%$. It was completely blocked by $CdCl_2$ (0.1 mM and 0.5 mM) and by $Na^+-depletion$. The other was identified by 5 mM $NiCl_2$ after suppression of $I_{CaL}$ and ryanodine receptor, constituting $14.8{\pm}1.6%$. This latter was blocked by either 10 mM caffeine-induced SR $Ca^{2+}-depletion$ or 1 mM tetracaine. IV-relationships illustrated that the latter was activated until the peak in $30{\sim}35\;mV$ lower voltages than the former. Overall, it was concluded that the SR $Ca^{2+}$ release process in the rat ventricular myocytes is mediated by the voltage-sensitive release mechanism in addition to the $Ca^{2+}-induced-Ca^{2+}\;release$.

• BMB Reports
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• v.33 no.3
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• pp.279-284
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• 2000

Using fluorescence probes, 2-(9-anthroyloxy) stearic acid (2- AS) and 12-(9-anthroyloxy) stearic acid (12-AS), we determined the differential effects of local anesthetics (tetracaine-HCI, bupivacaine-HCI, lidocaine-HCI, prilocaine-HCI and procaine-HCI) on the differential rotational rate between the surface (in carbon number 2 and its surroundings including the head group) and the hydrocarbon interior (in carbon number 12 and its surroundings) of the outer monolayer of the total phospholipid fraction liposome that is extracted from synaptosomal plasma membrane vesicles. The anisotropy (r) values for the hydrocarbon interior and the surface region of the liposome outer monolayer were$0.051{\pm}0.001$ and $0.096{\pm}0.001,$ respectively. This means that the rate of rotational mobility in the hydrocarbon interior is faster than that of the surface region. Local anesthetics in a dosedependent manner decreased the anisotropy of 12-AS in the hydrocarbon interior of the liposome outer monolayer, but increased the anisotropy of 2-AS in the surface region of the monolayer. These results indicate that local anesthetics have significant disordering effects on the hydrocarbon interior, but have significant ordering effects on the surface region of the liposome outer monolayer.

• The Korean Journal of Pain
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• v.12 no.2
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• pp.205-210
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• 1999

Background: Epidural morphine for postoperative pain control has a serious risk of respiratory depression and other side effects such as pruritus, nausea and urinary retention. In recent years, it is known that epidural administration of ketamine potentiates the effect of epidural morphine, and so decrease the side effects of epidural morphine. This study was performed to evaluate the analgesic efficacy of epidurally administered ketamine and whether this epidural administration can decrease the amount of epidural morphine. Methods: Sixty patients scheduled for the elective cesarean section were randomly selected. All patients were given subarachnoid injection of tetracaine 9 mg. Group I received epidural bolus injection of 0.15% bupivacaine 10 ml with morphine 2 mg followed by a continuous infusion of 0.125% bupivacaine 100 ml containing morphine 4 mg after peritoneum closure, and group II received the same method as group I except for the addition of epidural ketamine 30 mg. Analgesic effects were assessed using Numeric Rating Score (NRS) and Prince Henry Score (PHS). Also, the degree of satisfaction and the incidence of the side effects were observed. Results: Analgesic effects were significant in both groups after drug administration. But NRS and PHS were not significantly different between two groups at all times. The incidence of nausea and vomiting was 11 out of 30 in group I and 9 out of 30 in group II and the incidence of itching was 11 out of 30 in group I and 8 out of 30 in group II. Number of patients using additional analgesics were 2 and 1 in group I and II, respectively. Conclusions: Epidural ketamine did not potentiate the analgesic effect of epidural morphine and could not decrease the side effect of epidural morphine.

• The Korean Journal of Pharmacology
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• v.24 no.1
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• pp.43-52
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• 1988

To elucidate the mechanism of action of local anesthetics, the effects of local anethetics on the microenvironment of the lipid bilayers of synaptosomal plasma membrane vesicles (SPMV) isolated from bovine brain and dimyristoylphosphatidylcholine (DMPC) multilamellar liposomes were investigated employing the intermolecular excimer fluorescence technique and differential scanning calorimetry (DSC). The relative intensities of excimer and monomer fluorescence of pyrene are a simple linear function of the viscosity of a homologous series of solvents. The microviscosity(${\eta}$)of the hydrocarbon region of SPMV was measured by this method and the value was $57.3{\pm}5.3\;cP$ at $37^{\circ}C$. In the presence of lidocaine-HCl and procaine-HCl, the values decreased to $46.5{\pm}5.1\;cP$ and $54.7{\pm}4.8\;cP$, respectvely. The differential scanning thermograms of DMPC multilamellar liposomes showed that local anesthetics significantly lowered the phase transition temperature, broadened the thermogram peaks, and reduced the size of the cooperative unit. These results indicate that local anesthetics have significant fluidizing effects on biomembranes and perturbation of membrane lipids may produce some, but not all, of their pharmacological actions.

• The Korean Journal of Pharmacology
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• v.2 no.1 s.2
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• pp.71-82
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• 1966

The inhibitory effect of 5-hydroxytryptamine (5-HT) on the isolated intestinal strips of the tortoise (Amyda japonica), rat, rabbit and guinea pig was investigated. 1) The strips from the middle or lower part of the tortoise intestine responded with relaxation to 5-HT $(10^{-9}{\sim}10^{-5}g/ml)$, and the magnitude of the relaxation was proportional to the dose of 5-HT. The rectal part of the tortoise intestine, in contrast, showed contraction, the magnitude of which also was proportional to the dose of 5-HT. 2) Various blocking agents such as methysergide, morphine, tetracaine, nethalide, bretylium, hexamethonium, mecamylamine and chlorisondamine, showed no selective blocking activity on the relaxant effect of 5-HT on the tortoise intestine. The inhibitory effect of isoproterenol on the tortoise intestine, however, was selectively blocked by nethalide, and the stimulatory effect of 5-HT on the rectal part of the tortoise was blocked by methysergide. 3) In the presence of 5-HT, the stimulatory effect of DMPP on the tortoise intestine was remarkably attenuated, whereas that of acetylcholine and $BaCl_2$ was little affected. In the presence of isoproterenol, the stimulatory effect of acetylcholine and $BaCl_2$ were affected, but that of DMPP was little affected. 4) Large dose of 5-HT($10^{-4}$g/ml) produced inhibitory effect on the strips from the distal part of the isolated colon of the rat, rabbit and guinea pig, when the strips had been exposed to 5-HT($10^{-4}$g/ml), methysergide or phen`oxybenzamine. 5) Bretylium, as well as nethalide, abolished or remarkably reduced, in a few cases of the experiments, the inhibitory effect of the large dose of 5-HT on the distal part of the colon, whereas morphine did not affect it. 6) The ileal strips of the guinea pig also showed relaxation, as in the colonic strips, having been exposed to the large dose of 5-HT or phenoxybenzamine. This effect, however, was not obsered in the case of the rabbit ileum. 7) The property of the action-site of 5-HT in the tortoise intestine seemd to be different from the 5-HT receptors which have been revealed by several investigators. 8) Adrenergic component seemed to be participated in the inhibitory effect of 5-HT on the colon of the rat and rabbit.

• The Korean Journal of Pharmacology
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• v.31 no.2
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• pp.207-217
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• 1995

To investigate the functional and immunological properties of the Ca-release channel in the sarcoplasmic reticulum(SR) of the eel skeletal muscle, $[^3H]ryanodine$ binding, SDS gel electrophoresis, $^{45}Ca\;release$ studies, and immunoblot assay were carried out in the SR of the eel skeletal muscle. Maximal binding sites(Bmax) and $K_D$ values of $[^3H]ryanodine$ for Ca-release channel of the SR of the eel skeletal muscle were $19.44{\pm}1.40\;pmole/mg$ protein and $15.55{\pm}1.69\;nM$, respectively. $[^3H]Ryanodine$ binding to RyR was increased by calcium and AMP. The SR of the eel skeletal muscle has two high molecular weight bands on the SDS PAGE. The mobility of upper band was more slower than the single band of the rabbit skeletal muscle, and that of the lower band was similar with the single band of canine cardiac muscle. Vesicular $^{45}Ca-release$ was activated by calcium. Ca-induced $^{45}Ca-release$ was significantly inhibited by $MgCl_2(2\;mM)$, ruthenium red$(10\;{/mu}M)$ or tetracaine(1 mM), but not by high concentration of calcium itself. AMP-induced $^{45}Ca-release$ was slightly occurred only in the absence of calcium, it was not inhibited by $MgCl_2$ or ruthenium red. Caffeine also increased $^{45}Ca-release$ from the SR vesicles, but it was not affected by $MgCl_2$ or ruthenium red. Polyclonal Ab against rat skeletal muscle RyR is reacted with that of rabbit, but not reacted with that of the eel skeletal muscle. These results suggested that ryanodine receptor of the SR of the eel skeletal muscle is showing some similar properties with that of mammalian skeletal muscle, but might be an another isotype channel having two bands which is less sensitive to AMP, not cross-reacted with antisera against rat RyR, and not inhibited by high concentration of calcium.