• 제목/요약/키워드: blockers

검색결과 303건 처리시간 0.036초

Effect of the Volatile Oil of Nigella sativa Seeds and Its Components on Body Temperature of Mice: Elucidation of the Mechanisms of Action

  • Ashour, M.M.;Tahir, K.E.H.El.;Morsi, M.G.;Aba-Alkhail, N.A.
    • Natural Product Sciences
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    • 제12권1호
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    • pp.14-18
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    • 2006
  • The effect(s) of the volatile oil (VO) of Nigella sativa and its two components, ${\alpha}-pinene$ and ${\rho}-cymene$ on body temperature of male and female conscious mice were studied. Further investigations to delineate the mechanism(s) of action of the observed effect(s) by using various blockers involved in the central regulation of body temperature were made. VO and ${\alpha}-pinene$ caused significant reductions in rectal body temperature at is and 30 minute after treatment. ${\rho}-cymene$ had negligible effect on body temperature of mice. Cyproheptadine inhibited VO and ${\alpha}-pinene-induced$ hypothermia significantly. Nalbuphine inhibited ${\alpha}-pinene-induced$ hypothermia significantly but did not affect VO-induced hypothermia. Droperidol potentiated VO and ${\alpha}-pinene-induced$ hypothermia to a non-significant level; whereas atropine potentiated VO-induced hypothermia non-significantly. The study confirms further the role of serotoninergic receptors in the mechanism(s) of the observed pharmacological effects of the VO of Nigella sativa. It also indicated a possible role of opioid receptors in ${\alpha}-pinene-induced$ hypothermia.

Drug-induced Gingival Overgrowth Related to Sirolimus and Felodipine

  • Park, Youn-Jung;Lee, Joo-Hee;Kim, Young-Gun;Kwon, Jeong-Seung;Ahn, Hyung-Joon;Choi, Jong-Hoon
    • Journal of Oral Medicine and Pain
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    • 제42권1호
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    • pp.20-24
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    • 2017
  • Drug-induced gingival overgrowth (DIGO) is an adverse drug reaction mainly described with three types of commonly prescribed drugs, namely, calcium channel blockers (CCBs) (nifedipine, diltiazem, and verapamil), anti-convulsants (phenytoin), and immunosuppressive agents (cyclosporine). Numerous reports have associated gingival overgrowth with the newer generation of immunosuppressive agents (tacrolimus, sirolimus, and everolimus), and CCBs (amlodipine, felodipine, nicardipine, and manidipine). Especially, patients concomitantly medicated with an immunosuppressive agent and CCB have a higher DIGO chance. Dentists need to be aware of drugs that induce gingival overgrowth, the possibility of DIGO, and risk factors, and also prevent the progression of DIGO by early detection of DIGO, consultation about the drug change, and the maintenance of strict dental hygiene regimes.

Enflurane으로 인하여 발생한 마취 중 급성과민증 (Intraoperative Anaphylatic Reaction to Enflurane -A Case Report -)

  • 박창주;서광석;김현정;최진영;염광원
    • 대한치과마취과학회지
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    • 제4권1호
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    • pp.25-29
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    • 2004
  • Anaphylactic reactions to anesthetic drugs could potentially produce life-threatening immune-mediated crisis. Most published reports are associated with neuromuscular blockers and anaphylactic reactions to inhalation anesthetics are rare. A 25-year-old male patient with no significant medical history and no previous abnormal drug reaction was scheduled for orthognathic surgery under general anesthesia. After uneventful anesthetic induction and nasotracheal intubation, generalized urticaria and erythema were detected during the maintenance period with $O_2-N_2O$-enflurane. No severe changes of vital signs and no ventilation problem were accompanied. The operation was cancelled and the cutaneous lesions were faded away during the recovery with 100% $O_2$. The skin-prick and intradermal tests showed that he was hypersensitive to all halogenated inhalation anesthetics including enflurane and not to intravenous anesthetics and neuromuscular blockers. The re-operation was safely carried out under intravenous anesthesia with propofol-fentanyl-vecuronium. We report this case of intraoperative anaphylactic reaction to enflurane with literature review.

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흰쥐 대동맥에서 fluoxetine의 혈관 이완 효과 (Vasorelaxant effect of fluoxetine in isolated rat aorta)

  • 김상진;강형섭;김진상
    • 대한수의학회지
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    • 제44권4호
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    • pp.515-522
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    • 2004
  • The vasorelaxant effect of serotonin reuptake inhibitor fluoxetine was investigated in rat isolated thoracic aorta. Fluoxetine induced a concentration-dependent relaxation in aorta precontracted with phenylephrine (PE) and KCl. These relaxations were suppressed by removal of the endothelium (-E) or pretreatment of nitric oxide synthase inhibitors, N(G)-nitro-L-arginine (L-NNA) and N(omega)-nitro-Larginine methyl ester (L-NAME), guanylate cyclase inhibitors, methylene blue (MB) and 1H-[1,2,4]oxadiazolo [4,3-a]quinoxalin-1-one (ODQ), and $Ca^{2+}$ channel blockers, nifedipine and verapamil, in PE-precontracted +E rings. However, fluoxetine-induced relaxations were not suppressed by pretreatment of $K^{+}$ channel blockers, tetrabutylammonium and glibenclamide, in PE-precontracted endothelium intact (+E) rings. The fluoxetine-induced relaxations were not suppressed by removal of the endothelium or pretreatment of LNNA and MB in KCl-precontracted +E rings. Also, fluoxetine inhibited PE-induced sustained contraction in +E rings. These inhibitory effects of fluoxetine on contractions could be reversed by removal of the endothelium or pretreatment of L-NNA, L-NAME, MB, ODQ, nifedipine and verapamil, but not by pretreatment of etrabutylammonium and glibenclamide. These findings suggest that the vasorelaxant effect of fluoxetine is modulated by intracellular $Ca^{2+}$ with an involvement of endothelial NO-cGMP pathway and also may be related to the inhibition of $Ca^{2+}$ entry through voltage-gated channel.

TREK통로 차단제의 한우 정자 생존성 및 운동성 억제 효과 (Inhibitory Effect of TREK Channel Blockers on Sperm Viability and Motility of Korean Native Bull)

  • 강다원;김은진;한재희
    • 한국수정란이식학회지
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    • 제32권3호
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    • pp.243-248
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    • 2017
  • Antioxidants have been added to cryoprotectant or in vitro culture medium for sperm to reduce the detrimental damage, such as reactive oxygen species. However, curcumin, an antioxidant, shows dual effect on the viability and progressive motility of bovine sperm exposed to hydrogen peroxide. Low concentration of curcumin increases sperm viability and progressive motility, whereas high concentration of curcumin reduces them. This study was performed to identify whether TREK-1 channel is related to low sperm viability and motility induced by high concentration of curcumin. Curcumin reduced TREK-1 channel activity in a dose-dependent manner. TREK-1 channel was expressed in sperm obtained from Korean native bull. Treatment with TREK-1 channel blockers, such as curcumin, fluoxetine, $GdCl_3$, and spadin, significantly reduced sperm viability and motility (p < 0.05). However, TREK-1 channel activators showed different effect; linoleic acid showed an increase in sperm viability and motility, and wogonin did not affect them. These results show that TREK-1 channel is involved in the regulation of sperm viability and motility. In particular, high concentration of curcumin might reduce sperm viability and progressive motility of Korean native bull through blockage of TREK-1 channel.

개의 기관근 수축성에 대한 Diazepam의 작용기전 (The Action Mechanism of Diazepam on the Contractility of Canine Trachealis Muscle)

  • 권오철;최은미;최형철;김용대;하정희;서장수;이광윤
    • 대한기관식도과학회지
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    • 제4권1호
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    • pp.64-72
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    • 1998
  • This study aimed at observing the effect of diazepam on the contractility of trachealis muscle isolated from canine trachea, possible involvement of central or peripheral type benzodiazepine receptor, and the calcium related mechanism of action of diazepam. Trachealis muscle strips of 15 mm long were suspended in an isolated organ bath containing 1 ml of physiologic salt solution maintained at $37^{\circ}C$, and aerated with 95% $O_2$ /5% $CO_2$. Isometric myography was performed. Diazepam reduced the basal tone concentration dependently, and this inhibitory action was not affected by neither flumazenil, a central benzodiazepine receptor antagonist, nor PK11195, a peripheral benzodiazepine receptor antagonist. Pretreatment with diazepam showed the inhibitory effect on the concentration-response curves to agonists such as bethanechol, 5-hydroxytryptamine and histamine. Diazepam also caused concentration-related inhibition of contraction with potassium chloride 30 mM. The effect of diazepam on the basal tone and potassium chloride-induced contraction with calcium channel blockers were compared. Similar results were obtained in canine trachealis with verapamil, nifedipine and diltiazem. These results suggest that diazepam relax an airway muscle not via specific receptors but by a similar action as calcium channel blockers in canine trachealis muscle.

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Medical Management of Patients With Heart Failure and Reduced Ejection Fraction

  • Barry Greenberg
    • Korean Circulation Journal
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    • 제52권3호
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    • pp.173-197
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    • 2022
  • Treatment options for patients with heart failure (HF) with reduced ejection fraction (HFrEF) have expanded considerably over the past few decades. Whereas neurohormonal modulation remains central to the management of patients with HFrEF, other pathways have been targeted with drugs that have novel mechanisms of action. The angiotensin receptor-neprilysin inhibitors (ARNIs) which enhance levels of compensatory molecules such as the natriuretic peptides while simultaneously providing angiotensin receptor blockade have emerged as the preferred strategy for inhibiting the renin angiotensin system. Sodium glucose cotransporter 2 (SGLT2) inhibitors which were developed as hypoglycemic agents have been shown to improve outcomes in patients with HF regardless of their diabetic status. These agents along with beta blockers and mineralocorticoid receptor antagonists are the core medical therapies for patients with HFrEF. Additional approaches using ivabradine to slow heart rate in patients with sinus rhythm, the hydralazine/isosorbide dinitrate combination to unload the heart, digoxin to provide inotropic support and vericiguat to augment cyclic guanosine monophosphate production have been shown in well-designed trials to have beneficial effects in the HFrEF population and are used as adjuncts to the core therapies in selected patients. This review provides an overview of the medical management of patients with HFrEF with focus on the major developments that have taken place in the field. It offers prospective of how these drugs should be employed in clinical practice and also a glimpse into some strategies that may prove to be useful in the future.

심혈관질환약물과 향정신성약물의 약물상호작용 (Drug Interactions between Cardiovascular Agents and Psychotropic Drugs)

  • 박주언;정경희
    • 정신신체의학
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    • 제19권2호
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    • pp.57-65
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    • 2011
  • 많은 심혈관질환약물과 향정신성약물 간에 다양한 약물상호작용이 존재하며 이러한 약물들의 대부분이 시트크롬(cytochrome, CYP)450 효소의 기질, 억제제, 유도제로 작용하면서 약물상호작용이 일어나게 된다. 주로 CYP2D6와 CYP3A4를 억제하는 향정신성약물로 인해 같이 투여되는 심혈관질환약물의 효과가 변할 수 있고 부작용까지 나타날 수 있다. 이런 상황을 고려하고 반대의 경우도 포함하여 흔히 처방되는 두 종류의 약물을 병용 투여하는 경우 고려해야 할 부분에 대해서 심혈관질환약물 분류에 따라 논하였다. 대부분의 베타차단제는 CYP2D6의 대사에 의존하므로 이 대사를 억제하는 bupropion, chlorpromazine, haloperidol, SSRIs, quinidine 등을 사용했을 때 베타차단제의 독성이 나타날 수 있다. 앤지오텐신 관련 약물과 이뇨제가 lithium의 농도를 변화시키는 점도 고려하여야 한다. 칼슘통로차단제 및 콜레스테롤강하제를 CYP3A4의 강력한 억제제인 amiodarone, diltiazem, fluvoxamine, nefazodone, verapamil 등과 함께 사용하였을 때 약물 상호작용에 따른 부작용에 유의하여야 한다. 항부정맥제를 복용하는 환자에서 QT 간격 증가를 야기하는 약물이나 관련 CYP450 효소를 억제하는 약물을 동시에 투여하는 것은 삼가거나 적극적인 관찰이 필요하다. Digoxin과 warfarin이 병용 투여되는 향정신성약물로 인해 혈중 농도가 변하는 것도 임상적으로 중요하다.

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LC-MS/MS를 이용한 베타락탐계 항생제와 베타차단제의 동시분석 (Simultaneous analysis of β-lactam antibiotics and β-blockers by LC-MS/MS)

  • 손보영;김준일;안치화;이수원;김복순;정득모
    • 분석과학
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    • 제29권4호
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    • pp.179-185
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    • 2016
  • 물 시료 중에 잔류하는 β-차단제 3종(아테놀롤, 메토프롤롤, 프로프라놀롤)과 β-락탐계 항생제 6종(아목시실린, 페니실린G, 세파클러, 세파드록실, 세파렉신, 세프라딘)을 다른 두 종류의 카트리지를 사용하여 효과적인 분석방법을 정립하였다. 고분자 친수성-친유성 균형 카트리지(Hydrophile-lipophile balance, HLB)와 강한 양이온 교환 혼합 모드인 고분자 흡수 카트리지(Mixed mode cation exchange, MCX)를 사용하여 자동고체상 추출장치(Solid-phase extraction, SPE)로 전처리를 하였다. 충분한 크로마토그래피 분리를 위해 XDB-C18 (1.8 μm; 3.0 mm × 100 mm) 컬럼을 사용하였다. 정량을 위한 검정곡선의 상관계수(r²)가 0.995 이상으로 우수한 직선성을 나타내었다. 방법검출한계(Method detection limits, MDL)와 정량한계(Limit of quantitation, LOQ)는 각각 1.1~3.9 ng/L와 5~13 ng/L이었다. 이 분석방법으로 한강으로 유입되는 지천과 원수를 실태 조사 한 결과 N.D.~0.209 μg/L 농도로 검출되었다.

Molecular Dynamics Simulation of Enantioselectivity in Metoprolol in complex

  • Jang, Seok-Young;Park, Kyung-Lae
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.356.3-357
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    • 2002
  • Metoprolol (MT) is one kinds of adrenergic beta-blockers. Its (S)-enantiomer is known to be more active than the (R). Recently. the x-ray structure of beta-blocker. (S)-propranolol (a-naphthyl analogue), complexed in a mould fungal cellulase. Cel7A. was reported and the (R)-form did not build any complex. And in our previous study the conformation and stability of MT in carboxymethylated beta-cyclodextrin (BCD) complex was determined by NMR. HPLC, UV and electrophoresis measurement. (omitted)

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