• Title/Summary/Keyword: Antihypertensive drug

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Bioequivalence of Carvelol Tablet to Dilatrend Tablet (Carvedilol 25 mg) (딜라트렌 정(카르베딜롤 25 mg)에 대한 카베롤 정의 생물학적 동등성)

  • Cho, Hea-Young;Lee, Moon-Seok;Park, Soon-Cheol;Lim, Dong-Koo;Moon, Jai-Dong;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • v.31 no.4
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    • pp.289-295
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    • 2001
  • Carvedilol is an antihypertensive and antianginal compound that combines nonselective beta-adrenoceptor blocking and vasodilation properties and is devoid of intrinsic sympathomimetic activity. The purpose of the present study was to evaluate the bioequivalence of two carvedilol tablets, $Dilatrend^{TM}$ (Chong Kun Dang Pharmaceutical Co., Ltd.) and $Carvelol^{TM}$ (Dae Won Pharmaceutical Co., Ltd.), according to the prior and revised guidelines of Korea Food and Drug Administration (KFDA). The carvedilol release from the two carvedilol tablets in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution, water and blend of PSB80 into water). Eighteen normal male volunteers, $24.22{\pm}1.86$ years in age and $64.81{\pm}4.56\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 25 mg of carvedilol was orally administered, blood was taken at predetermined time intervals and the concentrations of carvedilol in serum were determined using HPLC method with fluorescence detector. The dissolution profiles of two carvedilol tablets were very similar at all dissolution media. Besides, the pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using non-transformed and logarithmically transformed $AUC_t$ and $C_{max}$. The results showed that the differences in $AUC_t$, $C_{max}$ and $T_{max}$ between two tablets based on the $Dilatrend^{TM}$ were 2.23%, -2.00% and 0.00%, respectively. Minimum detectable differences $({\Delta})$ at ${\alpha}=0.05$ and $1-{\beta}=0.8$ were less than 20% (e.g., 13.55% and 17.61% for $AUC_t$ and $C_{max}$, respectively). The powers $(l-{\beta})$ at ${\alpha}=0.05$, ${\Delta}=0.2$ for $AUC_t$ and $C_{max}$ were 98.08% and 88.81%, respectively. The 90% confidence intervals were within ${\pm}20%$ (e.g., $-5.69{\sim}10.16$ and $-12.30{\sim}8.30$ for $AUC_t$ and $C_{max}$, respectively). There were no sequence effect between two tablets in logarithmically transformed $AUC_t$ and $C_{max}$. The 90% confidence intervals using logarithmically transformed were within the acceptance range of log(0.8) to log(1.25) (e.g., $0.95{\sim}1.11$ and $0.89{\sim}1.09$ for $AUC_t$ and $C_{max}$, respectively). Two parameters met the criteria of prior and revised KFDA guideline for bioequivalence, indicating that $Carvelol^{TM}$ tablet is bioequivalent to $Dilatrend^{TM}$ tablet.

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Angiotensin-Converting Enzyme Inhibitory Activity of Enzymatic Hydrolysates of Crassostrea gigas (Oyster) (굴 효소 가수분해물의 angiotensin converting enzyme 저해작용)

  • Do, Hyung-Joo;Park, Hye-Jin;Kim, Ok-Ju;Kim, Andre;Choi, Yeung-Joon;Choung, Se-Young;Ha, Jong-Myung
    • Journal of Life Science
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    • v.22 no.2
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    • pp.220-225
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    • 2012
  • The peptides of enzymatic hydrolysates from oyster were determined by inhibitory activity against angiotensin-converting enzyme. The ACE inhibitory activity of enzymatic oyster hydrolysates increases with hydrolysis time. Among enzymatic oyster hydrolysates, oyster hydrolysates incubated with Protamex showed the best ACE inhibitory activity after 10 h. Hydrolysates were filtered through a HiSep ultrafiltration membrane (M.W. cut-off 30 kDa, 10 kDa) to obtain the peptide fractions with ACE inhibition activity. These fractions were applied to an HPLC column (watchers 120 ODS-AP $250{\times}4.6$ ($5{\mu}m$)). Six active fractions were collected and the range of ACE inhibition was from 29.56 to 85.85%. Peptide was purified from fraction B, showing the highest ACE inhibitory activity, and its sequence was Leu-Gln-Pro. These results suggest that PEH may be beneficial for developing antihypertensive food and drug.

The Evaluation of Potential Hepatotoxicity by Calcium Channel Blockers, Renin-Angiotensin System Blockade and Diuretics (칼슘채널차단제, 레닌-안지오텐신시스템 차단제, 이뇨제의 잠재적 간독성 평가)

  • Kim, Jae Yun;Lee, Ok Sang;Jung, Sun Hoi;Lee, Hye-Suk;Lee, Chang Ho;Kim, Sang Geon;Lim, Sung Cil
    • Korean Journal of Clinical Pharmacy
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    • v.22 no.4
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    • pp.330-339
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    • 2012
  • Background : Hypertension is treated with both lifestyle modification and pharmacotherapy. The Seventh Report of the Joint National Committee on Detection, Evaluation, and Treatment of High Blood Pressure (JNC-7), published in 2003, provides a streamlined management approach to hypertension for the primary care physician. The JNC-7 is the gold standard also in Korea. According to the JNC-7, special therapeutic considerations are recommended for high-risk individuals with compelling indications. The presence of compelling indications in any given patient should be considered when selecting specific pharmacotherapy to treat hypertension. However, in patients with compelling indications, it is unknown that hepatotoxicity is caused by Calcium Channel Blocker (CCB), one of 1st anti-hypertensive drugs. Now, the CCB is the most used 1st anti-hypertensive drug in Korea Therefore, we evaluated the changes in blood liver function parameters (ALT, AST, Total bilirubin, serum albumin) for the study group. Methods : We randomly collected and retrospectively analyzed Electronic Medical Record data (n=28,788) of patients, and who took calcium channel blockers(non-dihydropyridines; diltiazem, verapamil, dihydropyridines; amlodipine, barnidipine, benidipine, clinidipine, efonidipine, felodipine, isradipine, lacidipine, lercanidipine, nicardipine, nifedipine, nimodipine), with having liver function tests (LFTs) from July 1st 2009 to June 30th 2010 at the Seoul National University Hospital in Korea. Control groups are two antihypertensive agents: RAS blockade (ARB; candesartan, irbesartan, losartan, olmesartan, telmisartan, valsartan, ACE-I; cilazapril, enalapril, fosinopril, imidapril, perindopril, ramipril) and, Diuretics (loop; furosemide, torsemide, thiazide; hydrochlorothiazide[HCTZ], indapamide). Patients not having LFT results at these three standard points of time(baseline, during, medication, and after finishing medication) were excluded. The collected data were analyzed by using the SPSS (Version12.0) and Microsoft Excel (Version2007). Results : 711 patients who were treated CCB (297), RAS blockade (232) or Diuretics (182) monotherapy were selected for the study. In selected patients, liver damage degree(changes of each LFTs value) was higher in diuretics group than other groups, followed by RAS blockade and CCB. In diuretics group's was loop-diuretics group was higher than thiazide-diuretics group. In CCB group, Nondihydropyridine-CCB's damage degree was higher than Dihydropyrine-CCB's that. Conclusions : Despite the limitations due to the retrospective study, among patients with abnormal LFTs, the use of CCBs led to a less liver damage than other 1st anti-hypertensive agents. It can be recommended CCBs as one of the initial treatments of hypertension in patients with liver disease.

An Analysis of Fall Incidence Rate and Its Related Factors of Fall in Inpatients (입원환자 낙상 발생 실태와 원인에 관한 분석 연구)

  • Kim, Chul-Gyu;Suh, Moon-Ja
    • Quality Improvement in Health Care
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    • v.9 no.2
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    • pp.210-228
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    • 2002
  • Background: The purpose of this research was to examine the fall incidence rate and its related factors of fall in inpatients. Methods: The data were collected from the 138 fall incident reports in one tertiary hospital in Seoul from April 1st 1999 to September 30th 2001. The Fall Incident Report Form was originally developed based on that of Massachusetts General Hospital revised in 1995. And this was modified for this survey by the collaborating work of QI team including researcher and department of nursing service of this particular hospital. The contents of Fall Incident Form were general characteristics of patient. factors related to fall. types and places of fall. circumstances, nursing interventions. and outcome. Results: 1) The incidence rate of fall was 0.08% of total discharged patients and 0.081 per 1000 patient-day. This incidence rate is much lower than that of several hospitals in USA. This finding might result from the different incidence report system of each hospital. 2) The characteristics of fall-prone patient were found as follows. They were mostly over 60 years old, in alert mental status, ambulatory with some assistance, and dependent on ambulatory device. The types of diseases related high incidence rate were cerebrovascular disease(3.2), hypertension(1.6), cardiovascular disease(1.4), diabetes(1.3) and liver disease(0.6). 3) The majority of fall events usually occurred m bed. bedside(walking or standing) and bathroom in patient room. Usually they were up on their own when they fell. And there were more falls of elderly occurred during night time than day or evening. 4) 63.8% of fall events resulted in physical injuries such as fracture and usually the patients had diagnostic procedures and some treatment(ex. suture) which caused additional cost to the patients and their families. 5) The found risk factors of fall were drugs(antihypertensive drug, diuretics) and environmental factors like too high bed height, long distance of bedside table and lamp switch, and slippery tile of bathroom floor. Conclusion: Considering these results, every medical and nursing staff should be aware of the risk factors of patients in hospital, and should intervene more actively the preventive managements, specially for the elderly patients during night. Therefore, it is recommended that the development of Fall Prevention Programs based on these results.

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Food Functionality and In Vitro Bioactivity of Olive Flounder Paralichthys olivaceus Roe Concentrates Prepared by Cook-dried Process (가열-건조처리 넙치(Paralichthys olivaceus) 알 농축물의 식품기능성 및 생리활성)

  • In Seong Yoon;Sang in Kang;Jin-Soo Kim;In Sang Kwon;Hyeung Jun Kim;Min Soo Heu
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.56 no.1
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    • pp.7-20
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    • 2023
  • Boil-dried concentrate (BDC) and steam-dried concentrate (SDC) were prepared from olive flounder Paralichthys olivaceus roe using the cook-dried process, and their food functionality and in vitro bioactivity were examined. The buffer capacity of BDC and SDC was found to be stronger in the alkaline region than in the acidic region, and the buffer capacity of SDC was superior to that of BDC. The water holding capacities of these concentrates were 7.6 and 7.4 g/g protein, respectively, both of which were significantly lower than that of freeze-dried concentrate (FDC). The solubility of BDC (13.4%) and SDC (12.7%), foaming capacity of BDC (107.7%) and SDC (110.6%), and oil-in-water emulsifying activity index of BDC (7.7 m2/g) and SDC (9.7 m2/g) were all significantly lower than the corresponding values for FDC (P<0.05). The lower food functionality of BDC and SDC compared with FDC can be attributed to the high-temperature denaturation of proteins during the cook-dried process. The 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical scavenging activities (IC50) of SDC (2.5 mg protein/mL) was 60.4 ㎍/mL, and the angiotensin I converting enzyme inhibitory activity was 80.9%. Olive flounder roe concentrates have good antioxidant and antihypertensive activities, and can be used as materials or ingredients in the processing of seafood and other foods to enhance protein contents and food functionality.

Effect of Supplementation of Fermented Milk Containing Active Peptides(IPP, VPP) in Accordance with Medical Nutrition Therapy in Pre- and Hypertension Subjects (고혈압 전단계 및 고혈압 환자에서 의학영양치료와 병행한 생리활성 펩티드 함유 유산균 발효유 섭취가 혈압에 미치는 영향)

  • Kim, Ji-Young;Kim, Yun-Young;Kim, Hye-Rang;Yun, Sung-Seob;Kim, Wan-Sik;Yea, Hyun-Soo;Chung, Jin-Young;Lee, In-Hoe;Choue, Ryo-Won
    • Journal of the East Asian Society of Dietary Life
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    • v.18 no.6
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    • pp.918-926
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    • 2008
  • It is well known non-drug therapy for hypertension patients can reduce blood pressure. These types of therapy include maintaining ones ideal body weight, quitting smoking, consuming large amounts of fruits and vegetables consuming low levels of saturated fat and salt and regular exercise. Fermented milk protein derived biologically active peptides such as isoleucine-proline-proline_(IPP) or valine-proline-proline_(VPP) have been shown to lower blood pressure in hypertensive subjects. This study was conducted to investigate the antihypertensive effects of medical nutritional therapy _(MNT) in accordance with the consumption of fermented milk enriched with IPP and VPP. To accomplish this, we conducted a randomized case-controlled study of 43 subjects who had blood pressure levels greater than 120/80 mmHg. The subjects in the study group were randomly allocated into two groups, an MNT + fermented milk (100mL/day) group (n=21) and an MNT+L. helveticus fermented milk with tripeptides (IPP=2.2mg, VPP=2.6mg/100mL) group (n=22). The MNT included weight management, reduction of sodium, total fat and saturated fat intake, increased intake of fruits and vegetables, and increased intake of low fat dairy products. The treatments were administered for 12 weeks during which time no drug interventions were conducted. The daily intakes of total calories, fats, cholesterol and Na decreased significantly after 12 weeks of MNT in the control and the experimental groups. In addition, the systolic blood pressure de creased significantly in the control and experimental groups; however, the diastolic blood pressure only decreased significantly in the experimental group. Overall, the results of this study indicate that the intake of fermented milk containing IPP and VPP in conjunction with MNT exerted positive effects on the blood pressure of pre- and hypertensive subjects.

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Study on Health Behavior of Hypertensive Patients and Compliance for Treatment of Antihypertensive Medication (고혈압 환자들의 순응도와 건강행태의 관계)

  • Kim, Joo-Yeon;Lee, Dong-Bae;Cho, Young-Chae;Lee, Sok-Goo;Chang, Seong-Sil;Kwon, Yun-Hyung;Lee, Tae-Yong
    • Journal of agricultural medicine and community health
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    • v.25 no.1
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    • pp.29-49
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    • 2000
  • Objectives: To estimate the prevalence rate of hypertension, the changes of health behavior, and compliance for the drug treatment after diagnosed as hypertension. Methods: 7,030 persons who live in Cheonan City of Chungnam Province were selected by the cluster sampling method, and 5,372 persons were surveyed by questionnaire and health examination. This data is analyzed by Chi-square test on each variable. Results: 49.8%- of men and 38.8%- of women had been diagnosed as hypertension, and the prevalence rate of hypertension was significantly increased with aging in both gender. The prevalence rate tended to decrease in highly educated women group. Unemployed persons or obese persons showed relatively higher prevalence rate. The prevalence rate of hypertension increased in groups with higher total cholesterol levels over 240 mg/dl, and groups with glucose level over 200 mg/dl. 53.1%- of male patients and 66.6%- of female patients showed compliance for antihypertensive treatment. Compliance for treatment was higher in aged group or lower educated group in both gender. Among men, proportion of compliant subjects was higher in unemployed group(49.3%-), and lower in labor or primary industry than the others but among women, there was not any significant difference. And men with compliance for treatment had higher monthly income than the others, but women did not show any. Conclusion : This population had a high prevalence rate of hypertension which may lead to cardiovascular disease. Therefore health education programs and distribution of information must be emphasized in order to increase compliance to treatment and encourage the change of health behavior to promote health.

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The Effects of Majarol on the Blood Pressure and Heart Rate in Rats and Isolated Frog Heart (Majarine 유도체인 majarol의 흰쥐에 있어서 혈압 및 심박동수에 대한 작용과 적출 개구리 심장에 대한 작용)

  • Lee Jong-Hwoa;Park Young-Hyun;Cho Byung-Heon;Kim Yu-Jae;Kim Jong-Bae;Kim Chun-Sook;Cha Young-Deog;Kim Young-Suk
    • The Korean Journal of Pharmacology
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    • v.22 no.1 s.38
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    • pp.34-44
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    • 1986
  • In our previous studies, we had clarified many pharmacological effects of majarine: the bacteriostatic effect in vitro; the potentiation of hypnotic action of alcohol; hypotensive effect in rats and hypothermic effect in mice. This study was undertaken to search for a new antihypertensive drug. Red crystalline was obtained from majarine (which was extracted from Berberis koreana Palibin) by chemical methods. And this crystalline was identified as $C_{19}H_{16}NO_4$ contained one hydroxy group instead of methoxy group of majarine in isoquinoline ring and named 'Majarol' (5,6-Dihydro-9-hydroxy, 10-methoxybenzo-[g]-1,3-benzodioxolo [5,6-a] quinolizinium). We examined the effects of majarol on blood pressure and heart rate in urethane ancsthetized rats and the rate and amplitude of contraction of isolated frog heart. Several drugs: atropine sulfate, diphenhydramine chloride, hexamethonium bromide, phentolamine, epinephrine, propranolol and isoproterenol were used to clarify the mechanism of the hypotensive action of majarol. The results of experimints were as follows; 1. In low dose (0.5-2mg/kg, i.v.), majarol showed a typical transient hypotensive effect and slight decrease in heart rate. In high dose (5-10 mg/kg, i.v.), majarol showed a typical transient and a subsequent prolonged hypotensive effect and a significant prolonged decrease in heart rate was followed. 2. The hypotensive effects of majarol was not abolished by the pretreatments with atropine sulfate, hexamethonium bromide and diphenhydramine. The pretreatment with phentolamine inhibited significantly the hypotensive effects of majarol and the pretreatment wtih majarol blocked markedly the hypertensive effect of epinephrine. The positive chronotropic effect of isoproterenol was not blocked by the pretreatment with majarol. 3. In low dose, majarol increased the amplitude and decreased rate of contraction, but in high dose, majarol inhibited the amplitude and rate of contraction of isolated frog heart.

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Angiotensin Converting Enzyme Inhibition and Antihypertensive Effects of Phyllostachys pubescens Culm Extracts in Spontaneously Hypertensive Rats (맹종죽 줄기 추출물을 투여한 본태성 고혈압 쥐(SHR)의 ACE 저해 활성 및 혈압 강하 효과)

  • Kim, Jung-Suk;Kim, Mi-Jeong;Park, Min-Hee;Ryu, Bog-Mi;Moon, Gap-Soon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.1
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    • pp.27-34
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    • 2008
  • This study investigated the anti-hypertensive effect of Phyllostachys pubescens culm extract (PCE) by examining its effects on renal angiotensin-converting enzyme (ACE) inhibition and blood pressure using the spontaneously hypertensive rat (SHR) system. Systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured weekly for 8 weeks. Also, total antioxidant capacity and protein oxidation of tissues were examined by plasma Trolox Equivalent Antioxidant Capacity assay (TEAC) and hepatic protein carbonyl values, respectively. Twenty male SHR were randomly divided into four groups: PCE50, PCE100, and PCE500 (50, 100, and 500 mg of PCE per kilogram bodyweight daily, respectively), and control group. At week 2, the SBP in all PCE groups appeared to be significantly lower than the control (p<0.05), whereas the DBP were not different until week 4 (p<0.05). At week 8, SBP in the PCE500 was lower by 20% than the control. PCE groups considerably suppressed ACE dose-dependently compared with the control. Plasma TEAC and hepatic protein carbonyl values indicated increased antioxidative activity due to the PCE feed. No adverse effect was observed on the liver of SHR as there was no difference for the GOT and GPT values among the groups. Results of this study suggest that ACE inhibition may be one possible mechanism for the blood pressure lowering effect of PCE; thus, long term consumption of PCE may be beneficial in preventing high blood pressure along with the increased antioxidative status.