sympathomimetic agent

• 交感神経刺激薬、交感神経作動薬

関

sympathomimetic、sympathomimetic amine、sympathomimetic drug

WordNet

1. a substance that exerts some force or effect
2. a businessman who buys or sells for another in exchange for a commission (同)factor, broker
3. any agent or representative of a federal agency or bureau (同)federal agent
4. a representative who acts on behalf of other persons or organizations
5. an active and efficient cause; capable of producing a certain effect; "their research uncovered new disease agents"
6. how long something has existed; "it was replaced because of its age"
7. a time of life (usually defined in years) at which some particular qualification or power arises; "she was now of school age"; "tall for his eld" (同)eld
8. begin to seem older; get older; "The death of his wife caused him to age fast"
9. make older; "The death of his child aged him tremendously"

PrepTutorEJDIC

1. 『代理人』;周旋人 / 働き(作用)を起こすもの;作用物,薬剤 / (政府機関,特にFBI,CIAなどの)部員,機関員
2. 〈U〉(一般に)『年齢』,寿命;〈C〉(個々の)『年齢』,年 / 〈U〉成年(おとなとしての資格・権利を得る年齢;通例18または21歳) / 〈U〉『老齢』;《集合的に》老人たち / 〈U〉(人生の)『一時期』;〈C〉世代(generation) / 〈U〉〈C〉《しばしばA-》(歴史上の)『時代』 / 〈C〉《話》長い間 / 年をとる,ふける;〈物が〉古くなる / 〈年〉'を'とらせる;〈物〉'を'古びさせる

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/20 19:37:51」(JST)

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Epinephrine

Norepinephrine

Dopamine

Chemical structures of catecholamines.

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

These drugs can act through several mechanisms, such as directly activating postsynaptic receptors, blocking breakdown and reuptake of certain neurotransmitters, 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:

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 if the substituent is not 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

Classic examples of indirect 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

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 such as cocaine also affect dopamine, and some substances such as MDMA affect serotonin.

Norepinephrine is synthesized by the body from the amino acid tyrosine, and is used in the synthesis of epinephrine, which is a stimulating neurotransmitter of the central nervous system. Thus, all sympathomimetic amines fall into the larger group of stimulants (see psychoactive drug chart). In addition to intended therapeutic use, many of these stimulants have abuse potential, can induce tolerance, and possibly physical dependence, although not by the same mechanism(s) as opioids or sedatives. The symptoms of physical withdrawal from stimulants can include fatigue, dysphoric mood, increased appetite, vivid or lucid dreams, hypersomnia or insomnia, increased movement or decreased movement, anxiety, and drug craving, as is apparent in the rebound withdrawal from certain substituted amphetamines. Physical withdrawal from some sedatives can be potentially lethal, for instance benzodiazepine withdrawal syndrome. Opioid withdrawal is very uncomfortable, often described as a bad case of the flu, with possibly severe abdominal cramps and diarrhoea as central symptoms, but it is rarely lethal unless the user has a comorbid 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

• amphetamine (Benzedrine)
• benzylpiperazine (BZP)
• cathine (found in Catha edulis)
• cathinone (found in Catha edulis, khat)
• cocaine (found in Erythroxylum coca, coca)
• ephedrine (found in Ephedra)
• lisdexamfetamine (Vyvanse)
• maprotiline (Ludiomil)
• MDMA (Ecstasy, Molly)
• methamphetamine (Meth, Crank, Desoxyn)
• methcathinone
• methylenedioxypyrovalerone (MDPV)
• methylphenidate (Ritalin)
• 4-methylaminorex
• oxymetazoline (Afrin, Vicks Sinex)
• pemoline (Cylert)
• phenmetrazine (Preludin)
• propylhexedrine (Benzedrex)
• pseudoephedrine (Sudafed, SudoGest, also found in Ephedra species)

See also

• Sympathetic nervous system

References

External links

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

UpToDate Contents

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English Journal

• Antenatal exposure to sulindac and risk of necrotizing enterocolitis.

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• PMID 25088864

• A new strategy to prevent chemotherapy and radiotherapy-induced alopecia using topically applied vasoconstrictor.

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• In a new strategy, we sought to determine whether topically applied vasoconstrictor, with its accompanying transient skin hypoxia and exclusion of systemic drug, would prevent or suppress radiotherapy or chemotherapy-induced alopecia. Topical vasoconstrictor was applied to 1-cm(2) skin patches on th
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• Pharmacotherapy of binge-eating disorder: a review.

• Goracci A1, di Volo S, Casamassima F, Bolognesi S, Benbow J, Fagiolini A.
• Journal of addiction medicine.J Addict Med.2015 Jan-Feb;9(1):1-19. doi: 10.1097/ADM.0000000000000089.
• OBJECTIVES: The purpose of this article is to provide a comprehensive review of pharmacotherapy for binge eating disorder, including new therapeutic approaches such as centrally acting sympathomimetics, nootropics, lisdexamfetamine, and substance abuse treatment agents such as acamprosate, sodium ox
• PMID 25629881

Japanese Journal

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

• , , [他], , , , , , ,
• 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

• The sympathomimetic agent, 6-hydroxydopamine, accelerates cutaneous wound healing

• KIM LR
• Eur J Pharmacol 376, 257-264, 1999
• NAID 80011210564

• マウスにおけるピロカルピン誘導唾液分泌反応に及ぼすレセルピンの影響

• 齊藤裕志
• 歯科基礎医学会雑誌 39(4), 314-324, 1997-08-20
• NAID 110003165577

Related Links

• Sympathomimetic AgentsCardiovascular Use Drug Information ...

Sympathomimetic agent therapy is not a substitute for replacement of blood, plasma, fluids, and/or electrolytes. {02} {03} Prior to initiation of therapy, hypovolemia should be fully corrected, if possible, with either whole blood or a ...

• 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.

Related Pictures

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★リンクテーブル★

リンク元	「交感神経作動薬」「sympathomimetic amine」
拡張検索	「parasympathomimetic agent」「directly acting parasympathomimetic agent」
関連記事	「agent」「sympathomimetic」「age」

「交感神経作動薬」

　　[★]

英

sympathomimetic agent, sympathomimetic drug, sympathomimetic

同

交感神経刺激薬、交感神経興奮薬、交感神経様作用薬、交感神経刺激薬 sympathetic stimulant、アドレナリン様作用薬 adrenomimetic、アドレナリン作用薬 adrenergic agents

関

交感神経作動薬一覧。交感神経模倣薬

「sympathomimetic amine」

　　[★]

• 交感神経刺激アミン

関

sympathomimetic、sympathomimetic agent、sympathomimetic drug

「parasympathomimetic agent」

　　[★]

• 副交感神経刺激薬、副交感神経作動薬

関

parasympathomimetic、parasympathomimetics

「directly acting parasympathomimetic agent」

　　[★] 交感神経直接作動薬

「agent」

　　[★]

• n.

• 代行者、代理人。代理業者
• 政府職員、官吏
• ある後位をする人、ある作用をするもの。動員、動力因、作用因。(文法)動作主。科学的変化を起こさせるもの、薬品、～剤。病原体

関

agonist、agonistic、attorney、delegate、drug、etiologic agent、fomes、fomites、mediator、pathogen、pathogenic、pharmaceutical preparation、vector、vehicle

　 　 　 　 　 　

「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

「age」

　　[★]

• n.

• 年齢、歳

• v.

• 加齢する、熟成する

関

aged、ageing、aging、year old