sympathomimetic effect

• 交感神経刺激作用、交感神経作動作用

WordNet

1. act so as to bring into existence; "effect a change"
2. a symptom caused by an illness or a drug; "the effects of sleep loss"; "the effect of the anesthetic"
3. (of a law) having legal validity; "the law is still in effect" (同)force
4. the central meaning or theme of a speech or literary work (同)essence, burden, core, gist
5. an impression (especially one that is artificial or contrived); "he just did it for effect"
6. produce; "The scientists set up a shock wave" (同)effectuate, set_up
7. property of a personal character that is portable but not used in business; "she left some of her personal effects in the house"; "I watched over their effects until they returned" (同)personal_effects

PrepTutorEJDIC

1. 〈C〉〈U〉『結果』 / 〈C〉〈U〉(…への)『効果』,効きめ,影響《+『on』(『upon』)+『名』》 / 〈C〉(色・音・形などの)印象,感銘 / 《複数形で》品物;身の回り品;動産,財産 / (結果として)…‘を'『もたらす』;〈目的など〉‘を'果たす,遂行する

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/04/13 01:47:25」(JST)

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Epinephrine

Norepinephrine

Dopamine

Chemical structures of catecholamines.

Sympathomimetic drugs mimic the effects of transmitter substances of the sympathetic nervous system such as catecholamines, epinephrine (adrenaline), norepinephrine (noradrenaline), dopamine, etc. Such drugs are used to treat cardiac arrest and low blood pressure, or even delay premature labor, among other things.

These drugs act at the postganglionic sympathetic terminal, either directly activating postsynaptic receptors, blocking breakdown and reuptake, or stimulating production and release of catecholamines.

Mechanisms of action

The mechanisms of sympathomimetic drugs can be direct-acting, such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting, such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors that increase the levels of endogenous catecholamines.

Structure-activity relationship

For maximum sympathomimetic activity a drug must have the following; 1. Amine group two carbons away from an aromatic group. 2. A hydroxyl group at the chiral beta position in the R-configuration 3. Hydroxyl groups in the meta and para position of the aromatic ring to form a Catechol which is essential for receptor binding

The structure can be modified to alter binding. If the amine is primary or secondary it will have direct action, but if the amine is tertiary it will have poor direct action. Also if the amine has bulky substituents then it will have greater Beta adrenergic receptor activity, but it the substituent is non-bulky then it will favor the alpha adrenergic receptors.

Direct-acting

Adrenergic receptor agonists

Main article: Adrenergic agonist

Direct stimulation of the α- and β-adrenergic receptors can produce sympathomimetic effects. Salbutamol is a very commonly used direct-acting β₂-agonist. Other examples include phenylephrine, isoproterenol, and dobutamine.

Dopaminergic agonists

Stimulation of the D1 receptor by dopaminergic agonists such as fenoldopam is used intravenously to treat hypertensive crisis.

Indirect-acting

Norepinephrine and Dopamine transporter blockade

Classical sympathomimetic drugs are amphetamines (including MDMA), ephedrine, and cocaine, which act by blocking and reversing norepinephrine transporter (NET) activity. NET is a transport protein expressed on the surface of some cells that clears noradrenaline and adrenaline from the extracellular space and into cells, terminating the signaling effects.

Structure-activity relationship

A primary or secondary aliphatic amine separated by 2 carbons from a substituted benzene ring is minimally required for high agonist activity. The pKa of the amine is approximately 8.5-10. 1- Substitution on aromatic ring-

The presence of hydroxy group in the benzene ring at 3rd and 4th position shows maximum alpha and beta activity

Cross-reactivity

Substances like cocaine also affect dopamine, and some substances like MDMA affect serotonin.

Norepinephrine is synthesized by the body into epinephrine, causing central nervous system stimulation. Thus, all sympathomimetic amines fall into the larger group of stimulants (see psychoactive drug chart). Many of these stimulants have therapeutic use and abuse potential, can induce tolerance, and possibly physical dependence. Stimulates do not produce physical dependence in a way like opioids or sedatives will. The symptoms of physical withdrawal from stimulates are commonly described as being tired, sluggish, or general non-motivation. Physical withdrawal from most Sedatives can be potentially lethal. Opioid withdrawal is very uncomfortable, often describes as a bad case of the flu, but not lethal unless the user has an underlying condition.

Comparison

"Parasympatholytic" and "sympathomimetic" are similar, but not identical. For example, both cause mydriasis, but parasympatholytics reduce accommodation (cycloplegia) while sympathomimetics do not.

Examples

• ephedrine (found in Ephedra)
• pseudoephedrine (also found in Ephedra species)
• amphetamine
• methamphetamine
• methylphenidate (Ritalin)
• lisdexamfetamine (Vyvanse)
• cocaine (found in Erythroxylum coca, Coca)
• cathinone (found in Catha edulis, Khat)
• cathine (also found in Catha edulis)
• methcathinone
• benzylpiperazine (BZP)
• methylenedioxypyrovalerone (MDPV)
• 4-methylaminorex
• pemoline (Cylert)
• phenmetrazine (Preludin)
• propylhexedrine (Benzedrex)

See also

• Sympathetic nervous system

References

External links

• Amines, Sympathomimetic at the US National Library of Medicine Medical Subject Headings (MeSH)
• Sympathomimetic+amine at eMedicine Dictionary
• Sympathomimetic at eMedicine Dictionary

UpToDate Contents

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English Journal

• Sympathetic regulation of cerebral blood flow in humans: a review.

• Ter Laan M, van Dijk JM, Elting JW, Staal MJ, Absalom AR.SourceDepartment of Neurosurgery.
• British journal of anaesthesia.Br J Anaesth.2013 Sep;111(3):361-7. doi: 10.1093/bja/aet122. Epub 2013 Apr 24.
• Cerebral blood flow (CBF) is regulated by vasomotor, chemical, metabolic, and neurogenic mechanisms. Even though the innervation of cerebral arteries is quite extensively described and reviewed in the literature, its role in regulation of CBF in humans remains controversial. We believe that insuffic
• PMID 23616589

• The Effect of Mydriatic Solutions on Cognitive Function.

• Dersu II, Spencer HT, Grigorian PA, Evans M, Harper R.SourceDepartment of Ophthalmology, Jones Eye Institute, University of Arkansas for Medical Sciences , Little Rock, Arkansas , USA .
• Seminars in ophthalmology.Semin Ophthalmol.2013 Aug 16. [Epub ahead of print]
• Abstract Introduction: Anticholinergic and sympathomimetic ophthalmic solutions are used for mydriasis. These solutions have well-documented systemic side effects despite their topical administration. However, no studies have been conducted regarding the effect of mydriatic drops on cognitive functi
• PMID 23952181

• The concept of peripheral modulation of bladder sensation.

• Eastham JE, Gillespie JI.SourceUro-physiology Research Group; The Dental and Medical School; Newcastle University; Newcastle upon Tyne, England.
• Organogenesis.Organogenesis.2013 Aug 5;9(3). [Epub ahead of print]
• It is recognized that, as the bladder fills, there is a corresponding increase in sensation. This awareness of the volume in the bladder is then used in a complex decision making process to determine if there is a need to void. It is also part of everyday experience that, when the bladder is full an
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Japanese Journal

• Effects of Monochromatic Light on Different Time Perception

• Huang Jing-Shi,Shimomura Yoshihiro,Katsuura Tetsuo
• 人間-生活環境系学会英文誌 15(1), 21-29, 2012
• … The results of SDPTG which is an index of autonomic nervous system measured with photoplethysmography (PPG), in which there was a significant trend to be faster in the blue I light condition than in the green or blue II light conditions, showed that blue light might have a sympathomimetic effect. … We suggest that red light has an active effect in a short time interval through the visual processing pathway and decays with time. …
• NAID 130004938280

• Characterization of Intrinsic Sympathomimetic Activity of Carteolol in Rat Cardiovascular Preparations

• Floreani Maura,Froldi Guglielmina,Cavalli Maurizio [他],BOVA Sergio,GIRON Maria Cecilia,VARANI Katia,GESSI Stefania,BOREA Pier Andrea,DORIGO Maria Teresa,DORIGO Paola
• Journal of pharmacological sciences 95(1), 115-123, 2004-05-20
• … We evaluated in vitro, in myocardial and vascular preparations isolated from reserpine-treated rats, the intrinsic sympathomimetic activity (ISA) of carteolol, a β1/β2-adrenoceptor blocking agent used in cardiovascular and non-cardiovascular diseases. …
• NAID 10013054716

• 高齢者に対するｃａｒｖｅｄｉｌｏｌの心血行動態に及ぼす作用と忍容性の検討

• 浅井 俊亘,葛谷 雅文,小池 晃彦,神田 茂,前田 恵子,井口 昭久
• 日本老年医学会雑誌 39(2), 187-192, 2002
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• NAID 130003652815

Related Links

• Sympathomimetic | definition of sympathomimetic by Medical ...

sympathomimetic [sim″pah-tho-mi-met´ik] 1. producing effects resembling those of impulses transmitted by the postganglionic fibers of the sympathetic nervous system. See also adrenergic. 2. an agent that produces such an effect.

• What are the effects of sympathomimetic drugs in ...

1 Answer - Posted in: therapeutic, hypotension, arrhythmia, tachyarrhythmia - Answer: Sympathomimetic drugs mimic the effects of sympathetic ... ... Drugs.com provides accurate and independent information on more than 24,000 ...

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★リンクテーブル★

リンク元	「交感神経作動作用」「交感神経刺激作用」
関連記事	「effect」「sympathomimetic」「effected」

「交感神経作動作用」

　　[★]

英

sympathomimetic effect

関

交感神経刺激作用

「交感神経刺激作用」

　　[★]

英

sympathomimetic effect

関

交感神経作動作用

「effect」

　　[★]

• n.

• 結果。遂行、成就。
• 効果。効力。効き目、効能、影響。
• [美術・芸術]色彩、形の配合、光景、趣き、印象。外観、見え、体裁
• 趣旨、意図。本質、基本的意味

• vt.

• (変化などを)もたらす。(目的・計画など)果たす、遂げる。実施/施行する

関

act, action, affect, efficacy, impact, impinge, indication, influence, potency, effected

　 　 　 　 　 　 　

「sympathomimetic」

　　[★]

mimetic

• adj.

• 交感神経興奮性の

• n.

• 交感神経興奮剤、交感神経作動薬

関

sympathomimetic agent、sympathomimetic amine、sympathomimetic drug

「effected」

　　[★]

• adj.

• 結果として生じる

関

effect