• Analytical Science and Technology
• /
• v.33 no.2
• /
• pp.59-67
• /
• 2020

Nadolol is a β-blocker drug, which effectively manages hypertension and angina pectoris. Its chemical structure allows the formation of four possible stereoisomers. A coupled column high-performance liquid chromatographic (HPLC) system with UV and fluorescence detection was investigated for simultaneously determining four nadolol enantiomers in human plasma. The plasma samples were prepared using a convenient liquid-liquid extraction process and passed through HPLC. Nadolol was initially separated from the endogenous compounds or other impurities in human plasma on a Phenomenex silica column, and its enantiomers were resolved and determined on a Chirapak AD-H column. The developed HPLC method achieved an effective chiral separation and significantly eliminated endogenous compound interference. This optimal HPLC method was validated following FDA guidelines. The results showed good selectivity, linearity, accuracy (90.50 % - 105.27 %), and precision (RSDs < 9.52 %) for each enantiomer. This method was also successfully applied to determine nadolol enantiomers in the plasma samples of a healthy male volunteer (after orally administering 80 mg racemic nadolol), proving its suitability for nadolol stereoselective pharmacokinetic studies.

• YAKHAK HOEJI
• /
• v.45 no.6
• /
• pp.650-655
• /
• 2001

Carvedilol is a nonselective $\beta$-blocking agent with vasodilating properties that are attributed mainly to its blocking activity at $\alpha$$^{1}$-receptors. Carvedilol is used in the treatment of mild to moderate hypertention and angina pectoris and is often used in combination with other drugs. This study was carried out to evaluate the bioequivalence and pharmacokinetics of two carvedilol 25mg tablet formulations according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty healthy volunteers are enrolled and received a single dose (25mg as carvedilol) of each drug in the fasting state, in a randomized 2-way crossover design. After oral administration, blond samples were collected for a period of 30 hours. Plasma concentrations of carvedilol were determined by a rapid and sensitive HPLC method with spectrofluorometric detection. The major pharmacokinetic parameters such as AU $C_{0-}$30hr/, AU $C_{inf}$ , $C_{max}$, $T_{max}$, $t_{1}$2 / Cl/F and V $_{\beta}$//F were calculated. ANOVA test and t-test were utilized for the statistical analysis of each parameter. The results showed that the differences in AU $C_{0-}$30hr/, $C_{max}$ and $T_{max}$ between two were ~5.66, 1.74 and 0.00%, respectively. Minimum detectable differences ($\Delta$) at $\alpha$=0.05 were less than$\pm$ 20% except $T_{max}$ (8.44, 18.36, and 33.86%, respectively). The 90% confidence intervals of all parameters were within $\pm$20% (-10.60~ -0.72, -9.00~12.49 and -19.81~19.81%, respectively). Therefore, it is concluded that the two formulations are bioequivalent for both the extent and the rate of absorption after single dose administration.ation.ion.ion.ation.ion.n.

• The Journal of Korean Medicine
• /
• v.21 no.2
• /
• pp.60-67
• /
• 2000

Objectives : Radix Angelicae Gigantis(RAG) and Resina Ferulae(RF) have been used in oriental medicine or folk medicine to increase stamina. The aim of this study was the characterization of the mechanism of action of RAG and RF on smooth muscle and macrophages in rats to find new substances for the treatment of erectile dysfunction, cardiovascular diseases and immune dysfunction. Methods : We investigated the effects of the water extracts of RAG and RF on phenylephrine or KCl-contracted rat endothelium-denuded aorta, the production of NO in vascular smooth muscle cell (VSMC) and the production of NO and induction of iNOS in the $IFN-{\gamma}-primed$ RAW 264.7 cells. Results : The water extracts of the RAG and RF showed significant concentration-dependent relaxation effects on phenylephrine or KCl-contracted rat endothelium-denuded aorta. It also reduced the tension of the rat endothelium denuded aorta which was contracted in $Ca^{2+}-free$ media. On the other hand, it increased production of NO in VSMC which was stimulated with $IL-{\beta}$ or $IL-{\beta}$ plus $IFN-{\gamma}$. The water extracts of RAG and RF increased production of NO and induction of iNOS in the $IFN-{\gamma}-primed$ RAW 264.7 cells. Conclusions : According to the above results, the water extracts of RAG and RF relaxed the smooth muscle effectively and increased the production of NO in VSMC and macrophages. So, these herbs can be applied to erectile dysfunction, hypertension, angina pectoris, artherosclerosis and a defense defect for virus or microbe.

• Journal of Ginseng Research
• /
• v.34 no.3
• /
• pp.212-218
• /
• 2010

Korean red ginseng (KRG) has been shown to enhance endothelium-dependent vasorelaxation in experimental animals; however, little is known about its pharmacological effects on vascular stiffness in patients with coronary artery disease (CAD). This randomized, double-blind, placebo-controlled crossover trial was carried out to determine whether KRG has beneficial effects on arterial stiffness, cardiovascular risk factors such as plasma lipid profiles and blood pressure (BP), and Rho-associated kinase (ROCK) activity. Twenty patients (mean age, 62.5 years) with stable angina pectoris were given KRG (2.7 g/day) and a placebo alternatively for 10 weeks. Blood biochemical analysis and pulse wave velocity (PWV) recording were performed on day 0 and after the completion of each treatment. ROCK activity was assessed based on the level of phospho-$Thr^{853}$ in the myosin-binding subunit of myosin light chain phosphatase, determined by Western blot analysis of peripheral blood mononuclear cells. KRG significantly decreased the systolic BP, brachial ankle PWV, and heart femoral PWV in the patients (all p<0.05), but did not significantly alter the serum lipid profiles, including triglycerides and total, high-density lipoprotein, and low-density lipoprotein cholesterol levels. The ROCK activity tended to decrease (p=0.068) following KRG treatment. The placebo did not significantly alter any of the variables. In conclusion, KRG decreased systolic BP and arterial stiffness, probably via the inhibition of ROCK activity, in patients with CAD, but had a neutral effect on serum lipid profiles. Our data suggest that KRG has a therapeutic effect on CAD.

• Journal of Preventive Medicine and Public Health
• /
• v.34 no.1
• /
• pp.21-27
• /
• 2001

Objectives : To develop a model that will predict the mortality of patients undergoing Coronary Artery Bypass Graft (CABG) and evaluate the perfermance of hospitals. Methods : Data from 564 CABGs peformed in six general hospitals were collected through medical record abstraction by registered nurses. Variables studied involved risk factors determined by severity measures. Risk modeling was performed through logistic repression and validated with cross-validation. The statistical performance of the developed model was evaluated using c-statistic, $R^2$, and Hosmer-Lemeshow statistic. Hospital performance was assessed by severity-adjusted mortalities. Results : The developed model included age, sex, BUN, EKG rhythm, Congestive Heart Failure at admission. acute mental change within 24 hours, and previous angina pectoris history. The c-statistic and $R^2$ were 0.791 and 0.001, respectively. Hosmer-Lemeshow statistic was 10.3(p value=0.2415). One hospital had a significantly higher mortality rate than the average mortality rate, while others were net significantly different. Conclusion : Comparing the quality of service by severity adjusted mortality rates, there were significant differences in hospital performance. The severity adjusted mortality rate of CABG surgery may He an indicator for evaluating hospital performance in Korea.

• Journal of Chest Surgery
• /
• v.25 no.7
• /
• pp.685-692
• /
• 1992

In spite of multiple technical advances, large amount of homologous blood transfusions usually required for open heart surgery. Because the complications associated with transfusion are increased as the number of homologous transfusion increase, especially as transfusion related acquired immunodeficiency syndrome has appeared in recent years, such risks have stimulated recent interest in the use of autologous blood. This is a report concerning 23 consecutive adult autologous donors[autologous group] who had elective cardiac surgery at the Yonsei Cardiovascular Center, Yonsei University College of Medicine, from march, 1990 to august, 1991. A similar group of 23 patients operated during the same periods without autologous blood donation was used for comparison [control group] to investigate the effect of predonated autologous blood in decreasing the need of homologous transfusion and to investigate predonation related adverse effect. Autologous group consisted of 15 men and 8 women. Control group consisted of 7 men and 16 women. There were no significant differences in mean age, hemoglobin, hematocrit, RBC count, platelet count and prothrombin time on admission between the two groups. The mean autologous blood donation in autologous group was 2.2 units. In 10[43.5%] of the 23 atuologous group patients, no homologous RBC products transfusion was required. However, all patients required homologous transfusion in control group. In autologous group, patients required less homologous RBC products than control patients[2.1 units versus 5.3 units; p<0.001]. There were no significant differences in hemoglobin, hematocrit, RBC count and platelet count between the two groups before discharge. There were no serious complications related to preoperative blood donation, although 3 patients complained of mild dizziness during donation We conclude that preoperative autologous predonation of blood is a safe and effective method for reducing homologous transfusion and is recomended in all patients undergoing elective cardiac surgery except limited contraindications such as severe aortic valve stenosis or unstable angina pectoris.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.29 no.1
• /
• pp.1-10
• /
• 2015

This article is a study on palpitation of which disease cause, disease mechanism and formulas were analyzed with reference to annotations on "Shanghanlun" and "Jinkuiyaolue". And the scope of modern diseases related with palpitation was drawn by research on clinical papers. The source books are "Zhujieshanghanlun" and "Jinkuiyaoluefanglun" and the clinical papers are searched in China Academic Journals(CAJ) of China National Knowledge Infrastructure(CNKI). 13 clauses in "Shanghanlun" and 9 clauses in "Jinkuiyaolue" and 12 formulas are related with palpitation. Disease mechanisms of palpitation were classified as yang deficiency, yin deficiency, qi deficiency, blood deficiency, retained fluid, cold, etc and these days, qi stagnation, phlegm turbidity, blood stasis and fire heat are also considered as disease mechanisms. Modern diseases related with palpitation are arrhythmia(extrasystole, atrial fibrillation, bradycardia, tachycardia, sick sinus syndrome, atrioventricular block), vascular diseases(arterial occlusion, phlebothrombosis, Buerger's disease, coronary artery disease, vasculitis), blood pressure disorder(hypertension, hypotension) and heart diseases such as heart failure, angina pectoris, myocardial infarction, myocarditis, cardiomyopathy, pericardial effusion. And diseases related with psychological change(cardiac neurosis, anxiety neurosis, neurosis, depression, hyperthyroidism, hypothyroidism), pyrexia, anemia, drug intoxication, etc are also related with palpitation. Zhen Wu Tang showing an efficacy in dilating blood vessels and strengthening cardiac function, Wuling Powder with diuretic effect and Fried Glycyrrhizae Decoction acting on the ${\beta}$ receptor are applied to heart failure in different ways. Fried Glycyrrhizae Decoction(308 cases), Zhen Wu Tang(154), Wuling Powder(54), Xiao Chaihu Tang(34), Sini San(20) are reported to have been clinically applied to cardiovascular diseases and Zhen Wu Tang and Wuling Powder mainly applied to heart failure, Fried Glycyrrhizae Decoction, Lizhong Wan, Sini San and Zhen Wu Tang chiefly applied to arrhythmia related diseases. This study focuses on the general research and consideration on clinical applications and is a preliminary study to understand relations between Korean Medicine's symptoms and categories of modern diseases.

• Journal of Yeungnam Medical Science
• /
• v.18 no.1
• /
• pp.13-29
• /
• 2001

The enzyme activities of creatine kinase (CK), its isoenzyme MB (CK-MB) and of lactate dehydrogenase isoenzyme 1 (LD-1) have been used for years in diagnosing patients with chest pain in order to differentiate patients with acute myocardial infarction (AMI) from non-AMI patients. These methods are easy to perform as automated analyses, but they are not specific for cardiac muscle damage. During the early 90's the situation changed. First, creatine kinase ME mass (CK-MB mass) replaced the measurement of CK-MB activity. Subsequently cardiac-specific proteins, troponin T (cTnT) and troponin I (cTnI) appeared and displacing LD-1 analysis. However, troponin concentrations in blood increase only from four to six hours after onset of chest pain. Therefore a rapid marker such as myoglobin, fatty acid binding protein or glycogen phosphorylase BB could be used in early diagnosis of AMI. On the other hand, CK-MB isoforms alone may also be useful in rapid diagnosis of cardiac muscle damage. Myoglobin, CK-MB mass, cTnT and cTnI are nowadays widely used in diagnosing patients with acute chest pain. Myoglobin is not cardiac-specific and therefore requires supplementation with some other analyses such as troponins to support the myoglobin value. Troponins are very highly cardiac-specific. Only the sera of some patients with severe renal failure, which requires hemodialysis, have elevated cTnT and/or cTnI without there being any evidence of cardiac damage. The latest studies have shown that elevated troponin levels in sera of hemodialysis patients point to an increased risk of future cardiac events in a similar manner to the elevated troponin values in sera of patients with unstable angina pectoris. In addition, the bedside tests for cTnT and cTnI alone- or together with myoglobin and CK-ME mass can be used instead of quantitative analyses in the diagnosis of patients with chest pain. These rapid tests are easy to perform and they do not require expensive instrumentation. For the diagnosis of patient with chest pain, routinely myoglobin and CK-ME mass measurements should be performed whenever they are requested (24 h/day) and cTnT or cTnI on admission to the hospital and then 4-6 and 12 hours later and maintained less than 10% in imprecision.

• Journal of Radiation Industry
• /
• v.10 no.4
• /
• pp.181-187
• /
• 2016

Selective ${\beta}_1$-agonist and antagonists are used for the treatment of cardiac diseases including congestive heart failure, angina pectoris and arrhythmia. Selective ${\beta}_1$-antagonists including nebivolol have high binding affinity on ${\beta}_1$-adrenergic receptor, not ${\beta}_2$-receptor mainly expressed in smooth muscle. Nebivolol is one of most selective ${\beta}_1$-blockers in clinically used ${\beta}_1$-blockers including atenolol and bisoprolol. We tried to develop clinically useful cardiac PET tracers using a selective ${\beta}_1$-blocker. Nebivolol is $C_2$-symmetric and has two chromane moiety with a secondary amino alcohol and aromatic fluorine. We adopted the general synthetic strategy using epoxide ring opening reaction. Unlike formal synthesis of nebivolol, we prepared two chromane building blocks with fluorine and iodine which was transformed to diaryliodonium salt for labelling of $^{18}F$. Two epoxide building blocks were readily prepared from commercially available chromene carboxylic acids (1, 8). Then, the amino alcohol building block (15) was prepared by ammonolysis of epoxide (14) followed by coupling reaction with the other building block, epoxide (7). Diaryliodonium salt, a precursor for $^{18}F$-aromatic substitution, was synthesized in moderate yield which was readily subjected to $^{18}F$-aromatic substitution to give $^{18}F$-labelled nebivolol.

• The Journal of Internal Korean Medicine
• /
• v.42 no.2
• /
• pp.184-196
• /
• 2021

Objectives: This case report presents the effects of Korean medical treatment in a patient with chest pain after percutaneous coronary intervention (PCI). Methods: An 80-year-old woman was treated with Korean herbal medicine, acupuncture, and cupping therapy. Chest pain, sore tongue, and headache were assessed daily using a numeric rating scale (NRS). Results: After 15 days of treatment, chest pain disappeared, as reflected by an NRS change from 9 to 0, and headache was relieved (NRS decreased from 9 to 2). On the eighth day of treatment, the sore tongue was also relieved, as reflected by an NRS change from 9 to 0. Conclusion: These results show that chest pain after PCI can be relieved with Korean medical treatment, and it is expected that major adverse cardiac events (MACEs) may be prevented with Korean medical treatment. However, additional well-designed studies are required to confirm these findings.