• Title/Summary/Keyword: Antihypertensive agent

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Effects of Guanabenz on Renal Function in Dog (개의 신장기능에 미치는 Guanabenz의 영향)

  • Lee, Sang-Hyun;Ko, Suk-Tai
    • YAKHAK HOEJI
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    • v.32 no.4
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    • pp.258-273
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    • 1988
  • In this study attempts were made to observe the effects of guanabenz on renal function in dog, which manifests the antihypertensive action by inhibition of sympathetic tone through stimulating the presynaptic adrenoceptor (${\alpha}_2-adrenoceptor$). Guanabenz, when injected at a dose of $30.0{\mu}g/kg$, or infused at a dose of $3.0{\mu}g/kg/min$ intravenously, produced diuretic action with increased amounts of $Na^+\;and\;K^+$ in urine, and with decreased reabsorption rates of $Na^+\;and\;K^+$ in renal tubules. It was also observed that the rates of osmolar and free water clearances were increased, but the glomerular filtration rate and renal plasma flow were not changed. Guanabenz injected at a dose of $3.0{\mu}g/kg$ into a carotid artery or infused intravenously at a dose of $3.0{\mu}g/kg/min$ in a state of water diuresis elicited the diuretic action of the similar aspect as a case of guanabenz given intravenously. The diuretic action produced by guanabenz was completly blocked by pretreatment of i.v. prazosin, ${\alpha}_1-adrenoblocking$ agent, or of i.v. yohimbine, ${\alpha}_2-adrenergic$ blocking agent. Prazosin, when given into a renal artery, inhibited the diuretic action by i.v. guanabenz in only injected kidney, whereas in case of yohimbine the action was inhibited in both kidney. Guanabenz infused at a dose of $1.0{\mu}g/kg/min$ into a renal artery exhibited no significant changes of renal function in both kidney. In denervation experiments, guanabenz given intravenously produced typical diuretic action in innervated kidney, whereas in denervated kidney, it did not affect the action at initial period but exhibited the action with increase of only free water clearance at later period. These results suggest that guanabenz produced diuretic action in dog by inhibition of electrolyte reabsorption rates in renal tabules, mainly proximal tubule and of ADH release, which is mediated by stimulating of central sympathetic ${\alpha}_2-receptor$.

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Effects of Allicin on the Gene Expression Profile of Mouse Hepatocytes in vivo with DNA Microarray Analysis

  • Park, Ran-Sook
    • Nutritional Sciences
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    • v.8 no.1
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    • pp.23-27
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    • 2005
  • The major garlic component, Allicin [diallylthiosulfinate, or (R, S)-diallyldissulfid-S-oxide] is known for its medicinal effects, such as antihypertensive activity, microbicidal activity, and antitumor activity. Allicin and diallyldisulfide, which is a converted form of allicin, inhibited the cholesterol level in hepatocytes, in vivo and in vitro. The metabolism of allicin reportedly occurs in the microsomes of hepatocytes, predominantly with the contribution of cytochrome P-450. However, little is known about how allicin affects the genes involved in the activity of hepatocytes in vivo. In the present study, we used the short-term intravenous injection of allicin to examine the in vivo genetic profile of hepatocytes. Allicin up-regulate ten genes in the hepatocytes. For example, the interferon regulator 1 (IRF-I), the wingless-related MMTV (mouse mammary tumor virus) integration site 4 (wnt-4), and the fatty acid binding protein 1. However, allicin down-regulated three genes: namely, glutathione S-transferase mu6, a-2-HS glycoprotein, and the corticosteroid binding globulin of hepatocytes. The up-regulated wnt-4, IRF-1, and mannose binding lectin genes can enhance the growth factors, cytokines, transcription activators and repressors that are involved in the immune defense mechanism. These primary data, which were generated with the aid of the Atlas Plastic Mouse 5 K Microarray, help to explain the mechanism which enables allicin to act as a therapeutic agent, to enhance immunity, and to prevent cancer. The data suggest that these benefits of allicin are partly caused by the up-regulated or down-regulated gene profiles of hepatocytes. To evaluate the genetic profile in more detail, we need to use a more extensive mouse genome array.

Two Cases Report of Epidural Clonidine Analgesia in Cancer Patient and in Patient Tolerant to Opioids (Epidural Clonidine의 제통효과에 관한 증례 2례 보고)

  • Kim, Byung-Jung;Kim, Young-Mi;Kwon, Kwang-Jun;Yoon, Young-Joon;Jin, Sang-Ho
    • The Korean Journal of Pain
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    • v.7 no.2
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    • pp.282-286
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    • 1994
  • The central antihypertensive agent clonidine is an ${\alpha}_2$-adrenergic agonist that possesses pain-relieving properties. It has been administered epidurally in the treatment of cancer pain and for postoperative analgesia. 1) Case 1, 62-year-old woman who suffered from neurogenic pain syndrome due to metastatic squamous cell carcinoma of spinal canal was treated. 2) Case 2, 51-year-old woman undergoing lower abdominal surgery, epidurally administered morphine did not produced postoperative analgesia. In these cases, continuous epidural administeration of clonidine (200ug/day) and 0.3% bupivacaine(12 ml/day) produce high quality pain relief. These results suggest that antinociceptive effect of epidural clonidine is assumed to result from activation of ${\alpha}_2$-adrenergic receptors in the dorsal horn of the spinal cord.

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The Effect of Centrally Active Antihypertensive Agent on Biosynthetic Enzyme Activity of Neurotransmitter in Brain (중추성 항고혈압약이 뇌내 신경전달물질의 생합성 효소에 미치는 영향)

  • 윤재순
    • YAKHAK HOEJI
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    • v.29 no.4
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    • pp.165-175
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    • 1985
  • It has been reported that clonidine is $\alpha_2$-adrenergic agonist, potnet new hypotensive drug in human with low dose. The change in blood pressure is implicated in the concentration, release, uptake and metabalism of catecholamine and activity of catecholamine synthesizing enzyme in specific brain areas. Thus the experiment was set up to investigate the effect on the enzyme activity of clonidine alone and that of clonidine pretreated with imipramine or tranylcypromine by measuring activity of the Dopa-forming enzyme, tyrosine hydroxylase (TH) and epinephrine forming enzyme, phenylethanolamine-N-methyl transferase (PNMT) in brain and adrenal gland. The TH activity in brainstem and substantia nigra is decreased by intraperitoneally administered clonidine 0.1mg/kg twice a day for 5 days, but increased in the rats pretreated with imipramine 10mg/kg intraperitoneally given 26 hrs and 5 hrs before decaptitation. However the TH activity in all regions of brain is increased in rats pretreated with tranylcypromine 10mg/kg intraperitoneally twice a day for 5 days. The effect of clonidine on TH activity is due to inhibition release of norepinephrine by activation of presynaptic $\alpha_2$-adrenoreceptor, axon terminal result in the decrease of TH activity in brain. The increasing of TH activity in brain results in attenuation of the role of clonidine by pretreated with imipramine or tranylcypromine in rats. The activity of PNMT was not significantly affected by clonidine, imipramine and tranylcypromine in adrenal gland.

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A comprehensive review on Tukhme Kunjud (Sesamum indicum Linn.) with special reference to Unani System of Medicine.

  • Khatoon, Rizwana;Abbasi, Hana;Aslam, Mohammad;Chaudhary, Shahid Shah
    • CELLMED
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    • v.9 no.3
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    • pp.2.1-2.7
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    • 2019
  • Sesame (Sesamum indicum L.) is a rich source of edible oil most commonly it is used as a food product mainly in bakeries and also use as a common source of oil in daily kitchen needs. Due to the presence of some special phytochemicals like proteins, fibers, oil, minerals and antioxidants it is highly used for medicinal and therapeutic purposes. It is a good source of energy and act as an antiaging agent. Its seeds are used as Anti-helmintic, antihypertensive, antimicrobial, cytotoxic and Hepatoprotective but its seed coat which is a byproduct of sesame and a cherished source of fibers is normally use for animal feedstuff. In Unani system of medicine it is used both as drug & diet (dawa wa ghida). In classical Unani literature it is indicated in various disorders like Asthma, Dry Cough, Gastritis (due to any drug, excessive use of alcohol), Dryness of Intestine, Dryness in throat, Renal Stone, Bleeding Piles, Amenorrhea, Retention of urine, Dysuria, Orchitis, Sexual Debility, Anorexia. The present review article, an attempt have been made to compile all the pharmacological and Pharmacognostical characters of Sesamum indicum with special reference to Unani literature.

Clinical Efficacy of Transdermal Clonidine (St 155 BS) for Anesthetic Management in Hypertensive Patients (고혈압 환자 마취시 Transdermal Clonidine (St 155 BS)의 임상적 유용성)

  • Lee, Hyun-Hwa;Kim, Dong-Ok;Kim, Keon-Sik;Choi, Young-Kyoo;Shin, Ok-Young;Kwon, Moo-Il;Lee, Doo-Ik
    • The Korean Journal of Pain
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    • v.6 no.2
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    • pp.231-236
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    • 1993
  • Clonidine, a centrally-acting antihypertensive agent known to reduce central sympathetic outflow and modulate presynaptic transmitter's release, has shown to suppress central noradrenergic hyperactivity induced by immobilization stress in animals, by decreasing the MAC of halothane and the dose of narcotics required to prevent reflex cardiovascular response to noxious stimuli, and to have potent analgesic properties in humans. These characteristics suggest that clonidine might be a useful adjunct to the anesthetic management of patients with preexisting hypertension. Accordingly, we determined the clinical efficacy and safety on analgesia, sedation and hemodynamic stability in the perioperative period. Thirty patients(ASA physical status II-III) with a history of arterial hypertension, scheduled for elective orthopedic surgery were randomly assigned to two groups. We applied CPA-clonidine patch($6.9\;mg/cm^2$, 0.2 mg delivered daily) or placebo patch to each groups, 48 hours prior to induction of anesthesia. Antihypertensive medication was continued until the morning of the scheduled surgery. All patients received premedication of atropine and lorazepam, and induced anesthesia with thiopental and succinylcholine, and maintained with enflurane and 50% nitrous oxide, while sustaining the BP and pulse rate at acceptable range. For the relief of pain postoperatively, diclofenac and fentanyl were administered intramuscularly on demand. The results were as follows: 1) The change of hemodynamic responses in clonidine group was less compared to the placebo group. 2) Intraoperative anesthetic requirement for enflurane in clonidine group were significantly lower than placebo group. 3) Postoperative analgetic requirement in clonidine group were significantly lower than placebo group. In clonidine group, 5 cases out of 15 cases were required no analgetics, and the incidence of administration of additional fentanyl was decreased to 5 cases, comparing with 10 cases in placebo group.

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Comparisons of Renoprotective Activities between White Ginseng Radix and Rootlet in Spontaneously Hypertensive Rats with Diabetes

  • Chung, Sung-Hyun;Ko, Sung-Kwon;Park, Se-Ho
    • The Korean Journal of Physiology and Pharmacology
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    • v.6 no.1
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    • pp.57-61
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    • 2002
  • The renoprotective activities of white ginseng radix and rootlet were compared in spontaneously hypertensive rat (SHR) with diabetes. During oral administration of white ginseng radix (Ginseng Radix Alba, GRA) and white ginseng rootlet (Ginseng Radix Palva, GRP) for four weeks, arterial blood pressure and blood glucose levels were determined at every 10 days. In both GRA- and GRP-treatment groups, arterial blood pressures started to go down after 10 days of administration and maintained throughout the study period. After four weeks administrations of GRA and GRP, diastolic blood pressures were significantly decreased with 17% and 9%, respectively. GRA treatment also decreased blood glucose levels after 10 days of administration when compared with diabetic SHR group. At the end of the experiment, serum creatinine (Scr) and blood urea nitrogen (BUN) were not significantly different between the groups, except 62% higher value of BUN in diabetic SHR group when compared with SHR group. In the diabetic SHR group, the excretion of urinary albumin was increased significantly when compared with SHR. The level of urinary albumin in GRA treated group was markedly reduced when compared with diabetic SHR group $(67.8{\pm}4.7\;vs.\;131.3{\pm}13.5\;mg/24\;h).$ To examine the effects of ginseng radices on an overt diabetic nephropathy, index of kidney hypertrophy and transforming growth $factor-{\beta}1\;(TGF-{\beta}1)$ protein levels were evaluated. The glomerular and tubular cells stained positive for $TGF-{\beta}1$ seemed to be more abundant in diabetic SHR than in those with SHR, and GRA treated rats showed somewhat less $TGF-{\beta}1$ protein in glomerular and tubular cells when compared with diabetic SHR. Our results suggest that GRA might be a useful antihypertensive and antidiabetic agent with renoprotective effect.

Inhibitory Effect of Nicardipine on hERG Channel

  • Chung, Eun-Yong;Cho, Hea-Young;Cha, Ji-Hun;Kwon, Kyoung-Jin;Jeon, Seol-Hee;Jo, Su-Hyun;Kim, Eun-Jung;Kim, Hye-Soo;Chung, Hye-Ju
    • Biomolecules & Therapeutics
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    • v.18 no.4
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    • pp.448-453
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    • 2010
  • Drug-induced long QT syndrome is known to be associated with the onset of torsades de pointes (TdP), resulting in a fatal ventricular arrhythmia. QT interval prolongation can result from blocking the human ether-a-go-go-related gene (hERG) channel, which is important for the repolarization of cardiac action potential. Nicardipine, a Ca-channel blocker and antihypertensive agent, has been reported to increase the risk of occasional serious ventricular arrhythmias. We studied the effects of nicardipine on hERG $K^+$ channels expressed in HEK293 cells and Xenopus oocytes. The cardiac electrophysiological effect of nicardipine was also investigated in this study. Our results revealed that nicardipine dose-dependently decreased the tail current of the hERG channel expressed in HEK293 cells with an $IC_{50}$ of 0.43 ${\mu}M$. On the other hand, nicardipine did not affect hERG channel trafficking. Taken together, nicardipine inhibits the hERG channel by the mechanism of short-term channel blocking. Two S6 domain mutations, Y652A and F656A, partially attenuated (Y652A) or abolished (F656A) the hERG current blockade, suggesting that nicardipine blocks the hERG channel at the pore of the channel.

Anti-Inflammatory Effect of Chlorella ellipsoidea Extracted from Seawater by Organic Solvents (해수산 클로렐라(Chlorella ellipsoidea) 유기용매 추출물의 항염증 효과)

  • Choi, Yoo-Jin;Jo, Wol-Soon;Kim, Hyoun-Ji;Nam, Byung-Hyouk;Kang, Eun-Young;Oh, Su-Jung;Lee, Gye-An;Jeong, Min-Ho
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.43 no.1
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    • pp.39-45
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    • 2010
  • Chlorella has been reported to have certain beneficial physiological effects, including hypocholesterolemic, antihypertensive, antioxidative, and anti-tumor activities in animal and human studies. The aim of this study was to determine the anti-inflammatory activities of an 80% methanol extract(CE-Met), hexane fraction (CE-Hex), and ethyl acetate fraction (CE-EA) of Chlorella ellipsoidea in lipopolysaccharide (LPS)-stimulated RAW 264.7 murine macrophage. Treatment with various concentrations of the C. ellipsoidea extract resulted m a significant, dose-dependent reduction in nitric oxide (NO) production by LPS-induced macrophages. The C. ellipsoidea extract significantly inhibited LPS-induced NO production accompanied by an attenuation of IL-6 and TNF-$\alpha$ formation in macrophages. These results suggest potent inhibit이y effects on the production of inflammatory mediators by a C. ellipsoidea extract. Thus, C. ellipsoidea extract may be a potent anti-inflammatory agent for troubled skin.

Treatment of chronic kidney disease in children (소아의 만성신장질환의 치료)

  • Lee, Joo Hoon
    • Clinical and Experimental Pediatrics
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    • v.52 no.10
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    • pp.1061-1068
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    • 2009
  • The treatment of pediatric patients with chronic renal disease comprises management of nutritional imbalance, fluid, electrolyte, and acid-base disturbances, mineral bone disease, anemia, hypertension, and growth retardation. The treatment also includes administration of appropriate renal replacement therapy, if required. Adequate dietary intake of carbohydrates, fats, and proteins and caloric intake must be encouraged in such patients to ensure proper growth and development. In addition, fluid, electrolyte, and acid-base status must be regularly monitored and should be well maintained. Serum calcium, phosphorus, and parathyroid hormone levels must be maintained at their target range, which are determined on the basis of the glomerular filtration rate, to avoid the development of mineral bone disease. This can be achieved by using phosphorus binders and vitamin D analogues. An erythropoiesis-stimulating agent must be administered along with iron supplementation to maintain the hemoglobin level of the patients between 11-12 g/dL. Hypertension must be controlled with adequate water and sodium balance and appropriate antihypertensive agents. Administration of recombinant human growth hormone is recommended to improve the final adult heights.