• 제목/요약/키워드: 항콜린제

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The Effects of Ethanol on Cholinesterase Inactivation by Organophosphorous (에탄올이 유기인제 농약에 의한 Cholinesterase 불활성화에 미치는 영향)

  • Choi, Hyoung-Chul;Kim, Jong-Ho;Ha, Jeoung-Hee;Lee, Kwang-Yoon;Kim, Won-Joon;Woo, Hyun-Jae;Huh, Chang-Uk;Son, Soo-Min;Chun, Eun-Jin
    • Journal of Yeungnam Medical Science
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    • v.16 no.2
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    • pp.326-332
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    • 1999
  • Background: In korea the agricultural community widely uses organophosphorous, and organophosphorous poisonings are increasing every year. We compared change in activity of acetylcholinesterase and pseudocholinesterase by organophosphorous and by the interaction of ethanol and organophosphorous. We also compared the effect of reversible anticholinesterase drugs, physostigmine and neostigmine The object of this study is to investigate the effects of several anticholinesterase drugs and on how ethanol influences the activity of cholinesterase. Materials and Methods: Fifteen male university students were randomly selected, and blood samples were taken from the antecubital vein. The acetylcholinesterase in the RBC and the pseudocholinesterase in the serum were extracted and separated. The enzyme activity change was measured by the electrometric method. After adding acetylcholine, the pH change was measured with a pH meter. Results and Conclusion: Our results indicated that reversible anticholinesterase drugs decreased the cholinesterase activity more efficiently than organophosphorous. The acetyl cholinesterase and pseudocholinosterase activity were decreased by ethanol. When ethanol was added, oxime a cholinesterase activator, increased acetylcholinesterase activity but does not increased pseudocholinesterase activity.

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Autonomic Nervous Properties of Atropine and Glycopyrrolate on Heart Rate Variability during Anesthesia with Ketamine-Xylazine in Dogs (개에서 케타민-자일라진 마취동안 심박변이도에 대한 아트로핀과 글리코피롤레이트의 자율신경적 특성)

  • Park, Woo-Young;Bae, Chun-Sik;Lee, Soo-Han;Park, Woo-Dae
    • Journal of Veterinary Clinics
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    • v.26 no.3
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    • pp.212-219
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    • 2009
  • Anticholinergics, which are commonly given as a pre-anesthetic medication to prevent adverse effects in canine anesthesia, can cause cardiac adverse effects. To determine the effects of atropine and glycopyrrolate on the balance of sympathetic nervous tone and parasympathetic nervous tone of the heart during ketamine anesthesia in beagle dogs, heart rate variability(HRV), duration of anesthesia and behavioral changes were evaluated. There were no significant temporal domain differences between atropine and glycopyrrolate. Concerning the frequency domain component, atropine and glycopyrrolate effects were significantly lower(P<0.05) than the control saline-treated group. However, the root mean square of the interval differences between consecutive R peaks(RMSSD) and the standard deviation of Poincare plot perpendicular to the line-of-identity(SD1) in atropine were significantly decreased(P<0.05) from the baseline value, and the low frequency/high frequency ratio(LF:HF ratio) in glycopyrrolate was significantly increased from baseline value(P<0.05). The change of SD1 agreed with that of the high frequency(HF) in the frequency domain component and also with those of respiratory rate and $SpO_2-R$. Our results prove that glycopyrrolate is more suitable as a pre-anesthetic anticholinergic in ketamine anesthesia of dogs with respect to safety and duration of action.

Stability of Dicyclomine HCl in Aqueous Solution ( II ) (수용액(水溶液)에서의 염산디싸이클로민의 안정성(安定性) (제 2 보)(第 2 報))

  • Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.14 no.3
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    • pp.131-135
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    • 1984
  • The effect of pH and magnesium ion on the hydrolysis of dicyclomine HCl was investigated by comparing the rate constant and activation energy. The hydrolysis of dicyclomine HCl was acid-base catalytic reaction and the most stable range of pH was $3{\sim}5$. The magnesium ion accelerated the hydrolysis of dicyclomine HCl in aqueous solution.

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Pharmacological Studies on Human Vas Deferens -Coexistence of Adrenergic and Cholinergic Receptors, and Effect of Diazepam- (인체 정관의 약리학적 검색 -아드레날린성 및 콜린성 수용체의 공존과 Diazepam의 작용-)

  • Kim, Won-Joon;Lee, Kwang-Youn;Ha, Jeoung-Hee;Park, Tong-Choon
    • The Korean Journal of Pharmacology
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    • v.24 no.2
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    • pp.189-195
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    • 1988
  • This study aimed to investigate the autonomic innervations of human vas deferens and the effect of diazepam, a benzodiazepine sedative antianxiety drug, on the smooth muscle contractility of vas deferens. The specimens were obtained from healthy volunteers undergoing elective vasectomy with local anesthesia. The muscle preparation did not show any spontaneous contraction, but showed a good contraction induced by norepinephrine exerting the strongest response at $33^{\circ}C$. Phentolamine inhibited the norepinephrine-induced contraction concentration-dependently. Isoproterenol, a beta-adrenergic agonist evoked a considerable extent of contraction, and this contractile activity was antagonized by propranolol, a beta-adrenergic blocking agent. Acetylcholine induced a dashing contraction of the human vas deferens, and atropine, a muscarinic receptor blocking agent abolished the acetylcholine-induced contraction. Diazepam inhibited the norepinephrine-induced contraction in a concentration dependent manner. These results suggest that the smooth muscle of human vas deferens has cholinergic muscarinic and beta adrenergic receptors as well as the predominant alpha adrepergic receptor. Diazepam inhibits the motility, especially norepinephrine-induced contraction of human vas deferens.

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In vitro antioxidant, anti-diabetic, anti-cholinesterase, tyrosinase and nitric oxide inhibitory potential of fruiting bodies of Coprinellus micaceus (갈색먹물버섯 자실체의 메탄올과 열수추출물의 항산화, 항당뇨, 항콜린에스테라아제, 항티로시나아제 및 Nitric oxide의 저해 효과)

  • Nguyen, Trung Kien;Lee, Min Woong;Yoon, Ki Nam;Kim, Hye Young;Jin, Ga-Heon;Choi, Jae-Hyuk;Im, Kyung Hoan;Lee, Tae Soo
    • Journal of Mushroom
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    • v.12 no.4
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    • pp.330-340
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    • 2014
  • Coprinellus micaceus, belongs to family Psathyrellaceae of Agaricales, Basidiomycota, has been used for edible purposes in the world. This study was initiated to evaluate the antioxidant, anti-diabetic, anti-cholinesterase, anti-tyrosinase, and nitric oxide inhibitory activities of fruiting bodies from C. micaceus extracted with methanol and hot water. The HPLC analysis of phenolic compounds from the mushroom extracts identified 4 phenolic compounds including procatechuic acid, chlorogenic acid, (-)-epicatechin, and naringin. In 1,1-diphenyl-2-picrylhydrazyl(DPPH) free radical scavenging assay, the scavenging activities of methanol and hot water extracts were lower than that of positive control, BHT. The chelating effects of methanol and hot water extracts were significantly higher than that of BHT, the positive control at the all concentrations tested. In the reducing power assay, methanol and hot water extracts exhibited the lower activities compared with positive control at the 0.125-0.2 mg/ml. The methanol and hot water extracts of the mushroom inhibited the ${\alpha}$-glucosidase activity by 62.26% and 67.59%, respectively at the 2.0 mg/ml, while acarbose, the positive control, inhibited the ${\alpha}$-glucosidase activity by 81.81% at the same concentration. In the acetylcholinesterase(AChE) inhibitory activity assay, methanol and hot water extracts of the mushroom inhibited the AChE by 94.64% and 74.19%, respectively at 1.0 mg/ml, whereas the galanthamine, standard drug, inhibited the AChE activity by 97.80% at the same concentration. The tyrosinase inhibitory activities of methanol and hot water extracts were 91.33% and 91.99% at 2.0 mg/ml, while the inhibitory activity of kojic acid, the positive control, was 99.61% at the same concentration. Nitric oxide(NO) production in lipopolysaccahride (LPS) activated RAW 264.7 cells were inhibited by the methanol and hot water extracts in a concentration dependent manner. Therefore, it is concluded that fruiting bodies of C. micaceus contained natural antioxidant, anti-acetylcholinesterase and ${\alpha}$-glucosidase inhibitory, anti-inflammatory, anti-tyrosinase substances which might be used for promoting human health.

The Effect of an Anticholinergic Agent(Oxybutynin) on Spontaneous Resolution of Primary Vesicoureteral Reflux (항콜린제(옥시부티닌)가 원발성 방광요관역류의 자연 소실에 미치는 영향)

  • Ahn So-Hyun;Shim So-Yun;Lee Jung-Won;Cho Su-Jin;Lee Seung-Joo
    • Childhood Kidney Diseases
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    • v.7 no.2
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    • pp.174-180
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    • 2003
  • Purpose : Unstable bladder has been known to be one of the reasons for the genesis and persistance of primary vesicoureteral reflux(VUR) in children. And treatment of unstable bladder by anticholinergic agent may contribute to the resolution of primary VUR. We evaluated the effect of an anticholinergic agent(oxybutynin) on the resolution of primary VUR in children with different toilet training and voiding functions. Methods : 152 children with persistant primary VUR after one year of follow up were randomly assigned to the oxybutynin group(n=59, oxybutynin 0.2 mg/kg twice daily) and the control group(n=93, no oxybutynin) at Ewha Womans University Mok-Dong Hospital from October 1996 to April 2002. The resolution rate of the VUR and the difference according to the status of toilet training and voiding dysfunction were analyzed. Statistical analysis was done by the Chi-square test and a P-value of less than 0.05 was considered as significant. Results : VUR was resolved in 49.2%, improved in 20.3% and not changed in 30.5% in the oxybutynin group(n=59) which was not significantly different to 45.2%, 16.1%, 38.7% in the control group(n=93), respectively. In the non-toilet trained young children, VUR was resolved in 50.0%, improved in 23.5% and not changed in 26.5% in the oxybutynin group(n=34) which was not significantly different to 44.2%, 19.2%, 36.6% in the control group(n=52), respectively. In the toilet trained older children, VUR was resolved in 48.0%, improved in 16.0% and not changed in 36.0% in the oxybutynin group(n=25) which was not significantly different to 46.3%, 12.2%, 41.5% in the control group(n=41), respectively. In the toilet trained older children with no voiding dysfunction, VUR was resolved in 33.3%, improved in 11.1% and not changed in 55.5% in the of oxybutynin group(n=9) which was not significantly different to 53.6 %, 10.7%, 35.7% in the control group(n=28), respectively. In the toilet trained older children with voiding dysfunction, VUR was resolved in 56.3%, improved in 18.7% and not changed in 25.0% in the oxybutynin group(n=16), which looked higher than 30.7%, 15.4%, 53.9% in the control group(n=13), respectively, but these were not significantly different either. Conclusion : Oxybutynin was not effective in the resolution of primary VUR in non-toilet trained young children and toilet trained older children. Oxybutynin showed slightly higher tendency of reflux resolution in toilet-trained older children with voiding dysfunction but the difference was not statistically significant. Judicious use of oxybutynin is required in selected older children with VUR and voiding dysfunction.

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Clinical Subtypes of Delirium (섬망의 임상적 아형)

  • Seo, Jeong-Seok;Moon, Seok-Woo;Kim, Tae-Ho;Nam, Beom-Woo
    • Korean Journal of Psychosomatic Medicine
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    • v.16 no.2
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    • pp.69-74
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    • 2008
  • Delirium is an organic psychiatric syndrome characterized by an acute onset, prominent disturbance of consciousness and cognitive impairment with fluctuating course. Although there is not a clear consensus concerning the optimal classification system for delirium subtypes, Lipowski(1983) firstly classified delirium by psychomotor activity, namely hyperactive, hypoactive, and mixed. According results of several following studies, prevalence of hypoactive delirium were not less than that of hyperactive delirium. But a diagnosis of hypoactive delirium often missed, which is most frequently misdiagnosed as depression and dementia. Hyperactive delirium can be caused by alcohol or benzodiazepine withdrawal, would be related with excessive dopamine and cholinergic deficiency, and is more responsive to high-potency antipsychotics therapy. Hypoactive delirium would be caused by metabolic encephalopathy, and tends to present a less responsiveness to antipsychotics and poorer overall prognosis with a prolonged duration of admission than hyperactive delirium. Delirium is not a homogenous syndrome. Because of different subtypes, it may have dissimilar underlying pathogenetic pathways. So different treatment strategies between various subtypes may be needed.

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Inhibitory Effects of ${\gamma}$-Aminobutyric Acid on the Contractility of Isolated Rat Vas Deferens (흰쥐의 적출 정관 수축성에 대한 ${\gamma}$-Aminobutyric Acid의 억제작용)

  • Ahn, Ki-Young;Kwon, Oh-Cheol;Ha, Jeoung-Hee;Lee, Kwang-Youn;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.9 no.2
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    • pp.382-395
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    • 1992
  • GABA is an inhibitory neurotransmitter in central nervous system and produce sedative, antianxiety and muscle reaxing effects via $GABA_A$ receptor or $GABA_B$ receptor. Recently it is known that GABA is widely distributed throughout peripheral organs and may playa physiological role in certain organ. The vas deferens is innervated by species-difference. These study, therefore, was performed to investigate the mode and the mechanism of action of GABA on the norepiniphrine-, ATP- and electric stimulation-induced contraction of vas deferens of rat. Sprague-Dawley rats were sacrificed by cervical dislocation. The smooth muscle strips were isolated from the prostastic portion and were mounted in the isolated muscle bath. PSS in the bath was aerated with 95/5%-$O_2/CO_2$ at $33^{\circ}C$. Muscle tensions were measured by isometric tension transducer and were recorded by biological recording system. 1. GABA, muscimol, a $GAB_A$ agonist, and baclofen, a $GABA_B$ agonist inhibited the electric field stimulation(EFS, 0.2Hz, 1mSec, 80 V, monophasic square wave)-induced contraction with a rank order of potency of GABA greater than baclofen greater than muscimol. 2. The inhibitory effect of GABA was antagonized by delta aminovaleric acid(DAVA), a $GABA_B$ antagonist, but not by bicuculline, a $GABA_A$ mtagonist. 3. The inhibitory effect of baclofen was antagonized by DAVA, but the effect of muscimol was not antagonized by bicuculline. 4. Exogenous norepinephrine(NE) and ATP contracted muscle strip concentration dependently, but the effect of acetylcholine was negligible : and GABA did not affect the NE-and ATP-induced contractions. 5. GABA, baclofen and muscimol did not affect basal tone, and GABA did not affect the NE-and ATP-induced contractionsm 6. EFS-induced contraction was including 2 distinctable components. The first phasic component was inhibited by beta gamma-methylene ATP(mATP), a desensitizing agent of APT receptor and the second tonic component was reduced by pretreatment of reserpine(3 mg/Kg, IP). 7. GABA inhibited the EFS-induced contraction of reserpinized strips, but not the mATP-treated strips. These results suggest that in the prostatic portion of the rat vas deferens, adrenergic and purinergic neurotransmissions are exist, and GABA inhibits the release of ATP via presynaptic $GABA_B$ receptor on the excitatory neurons.

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Association Between Psychiatric Medications and Urinary Incontinence (정신과 약물과 요실금의 연관성)

  • Jaejong Lee;SeungYun Lee;Hyeran Ko;Su Im Jin;Young Kyung Moon;Kayoung Song
    • Korean Journal of Psychosomatic Medicine
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    • v.31 no.2
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    • pp.63-71
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    • 2023
  • Urinary incontinence (UI), affecting 3%-11% of males and 25%-45% of females globally, is expected to rise with an aging population. It significantly impacts mental health, causing depression, stress, and reduced quality of life. UI can exacerbate psychiatric conditions, affecting treatment compliance and effectiveness. It is categorized into transient and chronic types. Transient UI, often reversible, is caused by factors summarized in the acronym DIAPPERS: Delirium, Infection, Atrophic urethritis/vaginitis, Psychological disorders, Pharmaceuticals, Excess urine output, Restricted mobility, Stool impaction. Chronic UI includes stress, urge, mixed, overflow, functional, and persistent incontinence. Drug-induced UI, a transient form, is frequently seen in psychiatric treatment. Antipsychotics, antidepressants, and other psychiatric medications can cause UI through various mechanisms like affecting bladder muscle tone, altering nerve reflexes, and inducing other conditions like diabetes or epilepsy. Specific drugs like lithium and valproic acid have also been linked to UI, though mechanisms are not always clear. Managing UI in psychiatric patients requires careful monitoring of urinary symptoms and judicious medication management. If a drug is identified as the cause, options include discontinuing, reducing, or adjusting the dosage. In cases where medication continuation is necessary, additional treatments like desmopressin, oxybutynin, trihexyphenidyl, or amitriptyline may be considered.

The Aqueous Extract of Rubus coreanus Miquel Improves Scopolamine-Induced Memory Impairment in ICR Mice (마우스에서 복분자 물추출물의 기억력 감퇴에 대한 개선 효과)

  • Choi, Mi-Ran;Lee, Min-Young;Hong, Ji-Eun;Lee, Jae-Yong;Chun, Jang-Woo;Kim, Tae-Hwan;Shin, Hyun-Kyung;Kim, Eun-Ji
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.2
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    • pp.192-196
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    • 2012
  • In the present study, we examined the effect of the aqueous extract of Rubus coreanus Miquel (RCM-Ex) on scopolamine-induced memory impairment in male ICR mice. Mice were fed the diet containing 100 mg/kg body weight/day of RCM-Ex for 4 weeks. To induce amnesia, scopolamine (an antagonist of muscarinic acetylcholine receptor, 1 mg/kg of body weight) was intraperitoneally injected into mice 30 min before starting the behavior tests. RCM-Ex reversed scopolamine-induced memory impairments in mice as evidence by the passive avoidance test and Morris water maze test. In addition, acetylcholineasterase activities were decreased in the brains of mice treated with RCM-Ex. These results suggest that RCM-Ex may be an effective agent for the prevention of the memory impairment induced by cholinergic dysfunction.