• Biomolecules & Therapeutics
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• v.15 no.1
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• pp.40-45
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• 2007

The vascular relaxant effects on isolated rat aorta of amlodipine camsylates (S-, R-enantiomer, and R/S-racemate), were evaluated and compared with that of S-amlodipine besylate. Furthermore, antihypertensive effects were measured in spontaneously hypertensive rat (SHR). The S-amlodipine camsylate concentration-dependently inhibited $Ca^{2+}$-induced contraction of rat aorta with a very slow onset of action (reached its maximum at 3.5h; $ED_{50}:\;1.50\;{\pm}\;0.24$ nM), having a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{50}:\;3.36\;{\pm}\;0.91\;nM)$ and similar to those of S-amlodipine besylate $(ED_{50}:\;1.44\;{\pm}\;0.14\;nM)$, whereas the R-amlodipine camsylate has 590-fold lower vasorelaxant activity $(ED_{50}:\;886.4\;{\pm}\;49.7\;nM)$. In SHR, orally administered S-amlodipine camsylate produced a dose-dependent and long-lasting (>>10 h) antihypertensive effect $(ED_{20}:\;0.89\;mg/kg)$, with a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{20}:\;1.82\;mg/kg)$ and similar to those of S-amlodipine besylate $(ED_{20}:\;0.71\;mg/kg)$. In contrast, the R-amlodipine camsylate has no effect even-though administrated high concentration 10 mg/kg. These results suggest that S-amlodipine camsylate has the potency and long-lasting antihypertensive activity as single enantiomer drug, and its antihypertensive effect is not significantly different to that of S-amlodipine besylate.

• Mass Spectrometry Letters
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• v.2 no.4
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• pp.88-91
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• 2011

The pharmacokinetic properties of S-amlodipine were studied using racemic amlodipine and single S-enantiomer (SK310) administration to rats. Plasma levels of the drug were determined using chiral liquid chromatography coupled with tandem mass spectrometry following solid phase extraction. The stereospecific analysis of amlodipine was performed on an ${\alpha}$-acid glycoprotein (AGP) column using a mobile phase comprising 10 mM ammonium acetate (pH 4.0) and propanol at a flow rate of 0.2 mL/min. This method was used to perform a comparative study of the pharmacokinetics of amlodipine and SK310. The results revealed that the pharmacokinetic profile of S-amlodipine after the administration of SK310 was comparable to that following the administration of the racemic mixture.

• Journal of Yeungnam Medical Science
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• v.32 no.1
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• pp.17-21
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• 2015

Amlodipine, a calcium channel blocker of the dihydropyridine group, is commonly used in management of hypertension, angina, and myocardial infarction. Amlodipine overdose, characterized by severe hypotension, arrythmias, and pulmonary edema, has seldom been reported in Korean literature. We report on a fatal case of amlodipine intoxication with complications including rhabdomyolysis and oliguric acute kidney injury. A 70-year-old woman with a medical history of hypertension was presented at the author's hospital 6 hours after ingestion of 50 amlodipine (norvasc) tablets (total dosage 250 mg) in an attempted suicide. Her laboratory tests showed a serum creatinine level of 2.5 mg/dL, with elevated serum creatine phosphokinase and myoglobin. The patient was initially treated with fluids, alkali, calcium gluconate, glucagon, and vasopressors without a hemodynamic effect. High-dose insulin therapy was also started with a bolus injection of regular insulin (RI), followed by continuous infusion of RI and 50% dextrose with water. Despite intensive treatment including insulin therapy, inotropics, mechanical ventilation, and continuous venovenous hemodiafiltration, the patient died of refractory shock and cardiac arrest with no signs of renal recovery 116 hours after her hospital admission.

• 대한임상약리학회:학술대회논문집
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• 2006.11a
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• pp.69-69
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• 2006

• The Korea Journal of Herbology
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• v.39 no.3
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• pp.69-76
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• 2024

Objectives : Hypertension (high blood pressure), one of the world's major chronic diseases, has a high mortality rate due to its high prevalence and complications, but its control rate is low. The proper management and control through appropriate exercise, diet management, and optimal drug choice can reduce the risk of death from hypertension. Although various antihypertensive drugs are used to treat hypertension, they also have numerous adverse effects. Alongside increased interest in the use of Traditional Herbal Formulas (THF) for hypertension treatment, the purpose of this study was to examine the vasodilative effects of 10 THF in the rat thoracic artery pre-contracted by potassiumchloride (KCl). Methods : THF were extracted with distilled water for 2 hours. The rat thoracic artery was suspended and contracted by KCl in the organ bath which contained 10 ml Krebs Henseleit (KH) buffer. THF extracts were added in a dose-dependent increase (10-1,000 ㎍/mL) to examine vasodilative effects. The vasodilative effects produced by THF were expressed as the percentage in response to KCl-induced contraction. Results : Among the 10 THF, Banhasasim-tang, Buhnsimgieum, Sagunja-tang, and Samul-tang showed vasodilative effects. And, Sipjeondaebo-tang, Ssanghwa-tang, Ojeok-san, Onkyung-tang, Yongdamsagan-tang, and Hyangsayukgunja-tang showed no significant vasodilative effects. Also, in co-administration with amlodipine, Banhasasim-tang showed higher vasodilative effects than amlodipine alone, and Buhnsimgieum showed greater vasodilative effects at low concentrations, but inhibited amlodipine's vasodilative effects at high concentrations. Conclusion : As a result of these studies, they will be expected to provide useful data to establish guidelines of combined administration of THF and western antihypertensive drugs for the treatment of hypertension.

• The Korea Journal of Herbology
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• v.39 no.2
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• pp.11-18
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• 2024

Objectives : High blood pressure (also called Hypertension), which is the blood pressure that is higher than normal, is a chronic disease and causes various complications. Historically, Traditional Herbal Prescriptions (THP) have treated many diseases. However, there are not many studies on the treatment of hypertension with THP, very few studies have investigated the interactions between the co-administration of synthetic anti-hypertensives and THP. Therefore, the objective of the present study was to investigate the vasorelaxant activities of 10 THP in rat thoracic aortas pre-contracted with potassium chloride (KCl). Methods : An electric extractor was used to extract THP in distilled water for 2h. Rat thoracic aortas were isolated and pre-contracted using KCl in organ chambers containing 10 ml Krebs Henseleit (KH) buffer. THP extracts were added in increasing concentrations (10-1000 ㎍/mL) to investigate vasorelaxant activities. The vasorelaxant activities induced by THP were expressed as a percentage in response to contraction generated by KCl. Results : Among the 10 THP, Dangguisu-san, Mahwang-tang, Bulwhangeumjeonggi-san, Jakyakgamcho-tang, and Hyangsapyeongwi-san showed significant vasorelaxant activities. Maekmundong-tang, Bojungikgi-tang, Samryeongbaekchul-san, Yukmijihwang-tang, and Insampaedok-san showed no significant effect. Also, in co-administration with amlodipine, Mahwang-tang showed higher vasorelaxant activities than amlodipine alone, and Hyangsapyeongwi-san showed greater vasorelaxant activities at low concentrations but inhibited amlodipine's vasorelaxant activities at high concentrations. Conclusion : The results of these experiments are expected to provide useful data to establish guidelines for THPs and co-administration with western antihypertensive drugs to treat hypertension.

• Korean Journal of Clinical Pharmacy
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• v.22 no.1
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• pp.41-46
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• 2012

Adverse drug reaction (ADR) is a global problem of major concern in health care. ADRs can be accrued in any organs or systems. However, cardiovascular ADRs could be a more serious problem if they are irreversible or severe. For this reason, this study was conducted to analyze pattern and severity of cardiovascular ADRs, and suspicious medication. Total 646 reports including cardiovascular ADRs reported to the KFDA between January and June 2010 were analyzed. Amlodipine besylate (36 reports, 3.3%), iopromide (29 reports, 2.7%), tramadol HCl (28 reports, 2.6%) were most suspicious drugs that occurred cardiovascular ADRs. The most common cardiovascular ADRs were hypotension( 236 reports, 33.1%), palpitation (134 reports, 18.8%), and hypertension (89 reports, 12.5%). The most frequent ADRs were occurred in the age group of more than 60. This result could be of help to prescribers and other healthcare providers to predict and prevent cardiovascular ADRs. Also this study suggested that patients with cardiovascular ADR risk factors should be intensively monitored during the medications.

• The Journal of Korea Assosiation for Disability and Oral Health
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• v.9 no.1
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• pp.36-38
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• 2013

Takayasu's arteritis(TA) is commonly known as Aortitis Syndrome, Pulseless disease. Cardiac involvement due to vascular occlusion or stenosis is common in TA, expressed in forms of heart failure, aorta hypertension, alteration of artery or cardiac muscle. In this case, a 9 year old boy was referred to our dental clinic by his cardiology doctor for delayed eruption and gingival hyperplasia on upper incisor. The patient was diagnosed as TA with history of taking Amlodipine, a calcium channel blocker as hypertension medication. He was diagnosed as drug induced gingival hyperplasia. Under taking preventive antibiotic, gingivectomy was done. In case dental treatment of TA patient, dentist should be aware of two possible problems. First is the antibiotic prophylaxis due to the high risk of endocarditis. Second is the possibility of drug induced gingival hyperplasia.

• 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.