• The Korean Journal of Pharmacology
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• v.23 no.2
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• pp.133-141
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• 1987

The effects of verapamil and tetracaine on acetylcholine-and oxytocin-induced contraction of uterus from estrogen-treated rat were examined. Isometric tensions were recorded on the Physiograph and stored in TriGem 20XT computer as digitized data for off-line analysis of the components, which described the contraction patterns: trought tension (T), peak tension (P), contraction frequency (F), and duration (D). In the acetylcholine-induced contraction, verapamil $(0.25\;{\mu}M)$ significantly decreased P and D. In contrast, tetracaine $(42{\mu}M)$ decreased F, but increased D. In the low oxytocin-induced contraction, verapamil $(0.25\;{\mu}M)$ decreased P and D, and tetracaine $(42{\mu}M)$ decreased F but increased D. In the high oxytocin-induced contraction, verapamil decreased P and D, but tetracaine decreased P without affecting on other components. These results suggest that the analysis of effects of a certain inhibitor on the components of contraction allow to postulate its specific inhibitory mechanism of the smooth muscle contraction.

• Journal of Yeungnam Medical Science
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• v.7 no.2
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• pp.121-130
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• 1990

Plain 0.5% bupivacaine and hyperbaric 0.5% tetracaine were compared for spinal anesthesia in 40 patients undergoing operation of lower extremities. Lumbar puncture was performed with a 22 gauge spinal needle with the patient in the lateral recumbent position. The third lumbar interspace was chosen for the puncture, when a free flow of clear CSF was obtained, the local anesthetic solution (2.5ml of 0.5% bupivacaine or 2.0ml of hyperbaric 0.5% tetracaine) was injected at a rate of 0.1ml/sec without barbotage. After injection of anesthetics, clinical features were observed and compared between the two groups. The results were as follows : 1. The two groups were well matched for age, sex, height and weight. 2. In both groups, sensory block to $T_{12}$ dermatome was obtained within 4 minutes, mean maximal level of analgesia was $T_{6-7}$, and the mean time for maximal level was around 20 minutes. 3. The onset times of motor block were similar in both groups and complete motor block was obtained in all cases within 20 minutes. 4. The duration of analgesia above the $T_{12}$ dermatome was 3 hours, postoperative analgesia was 7 hours. These values were significantly prolonged than those of the tetracaine group(p<0.05). 5. The changes in systolic pressure in the bupivacaine group were significantly less than those of the tetracaine group(p<0.05). 6. The complications after spinal anesthesia were headache, numbness, urinary retention and backpain, and were no significant difference in both groups. From the obtained results, we concluded that plain 0.5% bupivacaine was a relatively satisfactory agent for spinal anesthesia for operation of lower extremities. The time of onset, height of block and the complications of postoperative period were similar in both groups. The advantages of plain 0.5% bupivacaine were less hypotension and long duration of analgesia.

• The Korean Journal of Pharmacology
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• v.32 no.1
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• pp.57-66
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• 1996

To investigate properties of Ca-release channel in the reptile skeletal muscle, electrophoretical analysis, purification of RyR, $[^3H]ryanodine$binding study, and $^{45}Ca-release$ were carried out in the SR vesicles prepared from the snake skeletal muscle. The snake SR vesicle has the single high molecular weight protein band on SDS-PAGE, and its mobility was similar with that of rat skeletal SR vesicles. The high molecular weight band on SDS-PACE was found in the $[^3H]ryanodine$ peak fractions $(Fr_{5-7})$ obtained from the purification step of the RyR. Maximal binding site and Kd of the snake SR RyR were 6.36 pmole/mg protein and 17.62 nM, respectively. Specific binding of $[^3H]ryanodine$ was significantly increased by calcium and AMP (P<0.05), but not or slightly inhibited by tetracaine, ruthenium red (5.4%), or $MgCl_2$ (21%). $^{45}Ca-release$ from the SR vesicles loaded passively was significantly increased by the low concentration of calcium $(1{\sim}10{\mu}M)$ and AMP (5 mM)(P<0.05), but significantly decreased by the high concentration $(300{\mu}M)$ of calcium, tetracaine (1 mM), ruthenium red $(10{\mu}M)$, and $MgCl_2$ (2 mM)(P <0.05). From the above results, it is suggested that snake SR vesicles also have the RyR showing the similar properties to those of mammalian skeletal RyR with the exceptions of no or slight inhibition of $[^3H]ryanodine-binding$ by tetracaine, ruthenium red, or $MgCl_2$.

• International Journal of Oral Biology
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• v.35 no.4
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• pp.159-167
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• 2010

To provide a basis for studying the pharmacological actions of tetracaine HCl, we analyzed the membrane activities of this local anesthetic. The n-(9-anthroyloxy) stearic and palmitic acid (n-AS) probes (n = 2, 6, 9, 12 and 16) have been used previously to examine fluorescence polarization gradients. These probes can report the environment at a graded series of depths from the surface to the center of the membrane bilayer structure. In a dosedependent manner, tetracaine HCl decreased the anisotropies of 6-AS, 9-AS, 12-AS and 16-AP in the hydrocarbon interior of synaptosomal plasma membrane vesicles isolated from bovine cerebral cortex (SPMV), and liposomes derived from total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. However, this compound increased the anisotropy of 2-AS at the membrane interface. The magnitude of the membrane rotational mobility reflects the carbon atom numbers of the phospholipids comprising SPMV, SPMVTL and SPMVPL and was in the order of the 16, 12, 9, 6, and 2 positions of the aliphatic chains. The sensitivity of the effects of tetracaine HCl on the rotational mobility of the hydrocarbon interior or surface region was dependent on the carbon atom numbers in the descending order 16-AP, 12-AS, 9-AS, 6-AS and 2-AS and on whether neuronal or model membranes were involved in the descending order SPMV, SPMVPL and SPMVTL.

• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.33-35
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• 1995

Microspheres containing tetracaine or bupivacaine with poly-lactic-glycolic acid were prepared with a range of compositions. Using the rat scicatic nerve model in vivo it was found that prolonged blockade for periods of 2-7 days. depending on composition variables. Polymer-local anesthetics microspheres are feasible delivery vehicle for prolonged regional nerve blockade.

• The Journal of the Korean dental association
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• v.12 no.6
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• pp.419-423
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• 1974

The authors have investigated the roles of cortisone and calcium on the depressive effects of local anesthetics on the acetylcholine-induced skeletal muscle contraction in frog. The results are as follows. 1. Tetracaine, cocaine, lidocaine and procaine decreased the acetylcholine-induced skeletal muscle contraction. 2. Cortisone increased the depressive effects of local anesthetics on the acetyl-choline-induced skeletal muscle contraction. 3. There was a tendency that in high calcium concentration, the depressive effects of cocaine and lidocaine on acetylcholine-induced skeletal muscle contraction were increased.

• The Korean Journal of Physiology and Pharmacology
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• v.1 no.4
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• pp.377-384
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• 1997

To investigate the properties of ryanodine binding sites of the bird skeletal SR vesicles, SDS PAGE, purification of RyR, and $[^3H]ryanodine$ binding study were carried out in the SR vesicles prepared from the chicken pectoral muscle. The chicken SR vesicles have two high molecular weight (HMW) protein bands as in eel SR vesicles on SDS PAGE. The HMW bands on SDS PAGE were found in the $[^3H]ryanodine$ peak fraction $(Fr_{3-5})$ obtained from the purification step of the ryanodine receptor protein. Bmax and KD of the chicken $[^3H]ryanodine$ binding sites were 12.52 pmol/mg protein and 14.53 nM, respectively. Specific $[^3H]ryanodine$ binding was almost maximal at $50{\sim}100$ ${\mu}M$ $Ca^{2+}$, but was not increased by 5 mM AMP and not inhibited by high $Ca^{2+}$. Binding was significantly inhibited by $20{\sim}100$ ${\mu}M$ ruthenium red and 1 mM tetracaine, but slightly inhibited by $Mg^{2+}$. From the above results, it is suggested that chicken SR vesicles have the ryanodine binding sites to which the binding of ryanodine is almost maximal at $50{\sim}10$ ${\mu}M$ $Ca^{2+}$, is significantly inhibited by ruthenium red and tetracaine, slightly inhibited by $Mg^{2+}$, but not affected by AMP and not inhibited by high $Ca^{2+}$.

• The Korean Journal of Physiology and Pharmacology
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• v.7 no.3
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• pp.119-124
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• 2003

To elucidate the molecular mechanism of pharmacological action of local anesthetics, we studied membrane actions of tetracaine, bupivacaine, lidocaine, prilocaine and procaine. Fluorescence polarization of n-(9-anthroyloxy)stearic acid (n-AS) was used to examine the effects of these local anesthetics on differential rotational mobility of different positions of the number of synaptosomal plasma membrane vesicle (SPMV) phospholipid carbon atoms. The four membrane components differed with respect to 3, 6, 9 and 16-(9-anthroyloxy)stearic acid (3-AS, 6-AS, 9-AS and 16-AP) probes, indicating that differences in the membrane fluidity might be present. Degrees of the rotational mobility of 3-AS, 6-AS, 9-AS and 16-AP were different depending on depth of hydrocarbon interior. In a dose-dependentmanner, tetracaine, bupivacaine, lidocaine, prilocaine and procaine decreased anisotropy of 3-AS, 6-AS, 9-AS and 16-AP in the hydrocarbon interior of the SPMV. These results indicate that local anesthetics have significant disordering effects on hydrocarbon interior of the SPMV, thus affecting the transport of $Na^+$ and $K^+$ in nerve membranes and leading to anesthetic action.

• The Korean Journal of Pharmacology
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• v.30 no.1
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• pp.125-136
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• 1994

To characterize the SR Ca-release channel protein complex of crustacean, $^{45}Ca-release,\;[^3H]ryanodine$ binding, and immunoblot studies were carried out in the crayfish and/or lobster skeletal sarcoplasmic reticulum. Bmax and affinity of crayfish SR to ryanodine were lower than those of lobster SR. AMP (5mM) increased $[^3H]ryanodine$ binding significantly in both vesicles (P<0.05). $Mg^{2+}$(5mM) or tetracaine(1mM) inhibited $[^3H]ryanodine$ binding significantly in both vesicles (P<0.001), but ruthenium red $(10\;{\mu}M)$ inhibited it moderately. In SDS polyacrylamide gel electrophoretic analysis of crayfish SR vesicles, there was a high molecular weight band that showed similar mobility with Ca-release channel protein of lobster skeletal SR, but more rapid mobility (HMWBr) than that of rabbit skeletal SR (HMWBS). Immunoblot analysis showed that polyclonal Ab to lobster skeletal SR Ca-release channel protein was react with HMWBr of crayfish skeletal SR, but not with that of HMWBs of rabbit skeletal SR. ^{45}Ca-release from crayfish skeletal SR vesicles was increased by the increase of extravesicular calcium from $1{\mu}M$ to 1mM. This Ca-release phenomenon was similar, but more sensitive in the low concentration of $Ca^{2+}$, compared to that from lobster SR vesicles. AMP (5mM) or caffeine (10mM) did not affect to $^{45}Ca-release.\;^{45}Ca-release$ was inhibited slightly ($3{\sim}8%\;by\;Mg^{2+}$) (5mM) or tetracaine (1mM), and moderately (23%) by high concentration of ruthenium red $(300\;{\mu}M)$. From the above results, it is suggested that SR Ca-release channel protein of crustacean has different properties from that of the rabbit, and similar properties between crayfish and lobster in functional and immunological aspects, but Ca-release via crayfish channel may be more sensitive to calcium.

• Journal of Pharmaceutical Investigation
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• v.26 no.2
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• pp.125-135
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• 1996

Solid lipid nanoparticles(SLN) are particulate systems for parenteral drug administration and suitable for controlled release. SLN were prepared by homogenization process. Dispersion at increased temperature (molten lipid) was performed to yield SLN loaded with lipophilic drugs. Tetracaine base, lidocaine base, prednisolone, methyltestosterone and ethinylestradiol were used as model drugs to access the loading capacity and to study the release behavior. To investigate production parameters(lipids, surfactant concentration, homogenizing rpm) in the formation of SLN, particle size was performed by laser diffraction analysis. The mean particle size of SLN with stearic acid or trilaurin was below 1 micron. By decreasing the particle size and increasing the surfactant concentration, the release rate was increased especially in the case of highly lipophilic drug loaded SLN. Methyltestosterone or ethinylestradiol loaded SLN showed a distinctly prolonged release over a few days.