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

WordNet

1. exhibiting mimicry; "mimetic coloring of a butterfly"; "the mimetic tendency of infancy"- R.W.Hamilton
2. characterized by or of the nature of or using mimesis; "a mimetic dance"; "the mimetic presentation of images"

PrepTutorEJDIC

1. 模倣の,まねをする / 見せかけの,模擬の

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/05/27 05:54:11」(JST)

wiki en

[Wiki en表示]

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 widely 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

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

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

• 1. 成人における肥満：薬物療法obesity in adults drug therapy [show details]
  …chronic opioid use, and use within 14 days of taking monamine oxidase inhibitors The available sympathomimetic drugs (phentermine, diethylpropion, benzphetamine, and phendimetrazine) are only approved by …
• 2. 覚醒剤：急性中毒methamphetamine acute intoxication [show details]
  … Methamphetamine is a sympathomimetic amine that belongs to a class of compounds, the phenethylamines, with a variety of stimulant, anorexiant, euphoric, and hallucinogenic effects. Methamphetamine was …
• 3. 起立性低血圧および食後低血圧の治療treatment of orthostatic and postprandial hypotension [show details]
  …months due primarily to worsening supine hypertension, edema, and congestive heart failure . Two sympathomimetic pressor agents are approved by the FDA for the treatment of neurogenic orthostatic hypotension: …
• 4. 成人における薬物中毒への一般的アプローチgeneral approach to drug poisoning in adults [show details]
  …preferred over indirect-acting agents. Such patients have decreased sympathomimetic tone due to decreased release of sympathomimetic neurotransmitters, which is overcome by dopamine. Seizure – Seizures …
• 5. コカイン：急性中毒cocaine acute intoxication [show details]
  …which are discussed below. Blockade of reuptake of biogenic amines – Cocaine is an indirect sympathomimetic agent, which increases the availability of biogenic amines at adrenergic receptors by blocking…

English Journal

• Ketamine in adult cardiac surgery and the cardiac surgery Intensive Care Unit: An evidence-based clinical review.

• Mazzeffi M1, Johnson K, Paciullo C.
• Annals of cardiac anaesthesia.Ann Card Anaesth.2015 Apr-Jun;18(2):202-9. doi: 10.4103/0971-9784.154478.
• Ketamine is a unique anesthetic drug that provides analgesia, hypnosis, and amnesia with minimal respiratory and cardiovascular depression. Because of its sympathomimetic properties it would seem to be an excellent choice for patients with depressed ventricular function in cardiac surgery. However,
• PMID 25849690

• Assessment of potential cardiovascular risks of methylphenidate in comparison with sibutramine: do we need a SCOUT (trial)?

• Antel J1, Albayrak Ö, Heusch G, Banaschewski T, Hebebrand J.
• European archives of psychiatry and clinical neuroscience.Eur Arch Psychiatry Clin Neurosci.2015 Apr;265(3):233-47. doi: 10.1007/s00406-014-0522-8. Epub 2014 Aug 23.
• With the recent approval of methylphenidate (MPH) for treating attention-deficit/hyperactivity disorder (ADHD) in adults, the number of patients exposed will increase tremendously. The ongoing debate on the cardiovascular safety of MPH has triggered two large retrospective cohort studies in children
• PMID 25149468

• Improving the functionality of intra-operative nerve monitoring during thyroid surgery: is lidocaine an option?

• Govindarajan R1, Shah A2, Reddy VS2, Parithivel V2, Ravikumar S3, Livingstone D1.
• Journal of clinical medicine research.J Clin Med Res.2015 Apr;7(4):282-5. doi: 10.14740/jocmr2025w. Epub 2015 Feb 9.
• Intra-operative nerve monitoring (IONM) is rapidly becoming a standard of care in many institutions across the country. In the absence of neuromuscular blocking agents to facilitate the IONM, the depth of anesthesia required to abolish the laryngo tracheal reflexes often results in profound hemodyna
• PMID 25699129

Japanese Journal

• 症例検討カンファレンス形式の静脈麻酔教育

• 日本臨床麻酔学会誌 36(1), 79-82, 2016
• NAID 130005125754

• 肥満と薬物療法

• 循環器内科 = Cardioangiology 77(6), 585-589, 2015-06
• NAID 40020522201

• 高機能患者シミュレータの薬学教育への応用:－交感神経作動薬による循環器系バイタルサインの変動－

• 医療薬学 41(2), 98-107, 2015
• NAID 130005125781

Related Links

• Sympathomimetic | definition of sympathomimetic by Medical ...

sympathomimetic Of any agent that simulates or stimulates the sympathetic nervous system. ADRENERGIC. Sympathomimetic action can increase the heart output by 100 per cent over resting values. It can constrict arteries and ...

• Sympathomimetic drugs | definition of sympathomimetic ...

Drugs that produce an effect similar to that obtained by stimulation of the sympathetic nervous system. Some of these predominantly act on the adrenergic alpha ... For instance, sympathomimetic drugs can lead to rapid increase in ...

• sympathomimeticの意味・使い方｜英辞郎 on the WEB：アルク

sympathomimetic 【名】交感神経様作用薬 【形】交感神経様作用の - アルクがお届けするオンライン英和・和英辞書検索サービス。 ... 内因性交感神経刺激作用 ｛ないいん せい こうかん しんけい しげき さよう｝

---

★リンクテーブル★

リンク元	「交感神経作動薬」「sympathomimetic agent」「sympathomimetic amine」
拡張検索	「parasympathomimetic」「parasympathomimetic agent」「parasympathomimetics」「directly acting parasympathomimetic agent」「indirect sympathomimetics」

「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 agent」

　　[★]

• 交感神経刺激薬、交感神経作動薬

関

sympathomimetic、sympathomimetic amine、sympathomimetic drug

「sympathomimetic amine」

　　[★]

• 交感神経刺激アミン

関

sympathomimetic、sympathomimetic agent、sympathomimetic drug

「parasympathomimetic」

　　[★]

• adj.

• 副交感神経刺激様の

• n.

• 副交感神経刺激薬

関

parasympathomimetic agent、parasympathomimetics

　

「parasympathomimetic agent」

　　[★]

• 副交感神経刺激薬、副交感神経作動薬

関

parasympathomimetic、parasympathomimetics

「parasympathomimetics」

　　[★]

副交感神経刺激薬

関

parasympathomimetic、parasympathomimetic agent

「directly acting parasympathomimetic agent」

　　[★] 交感神経直接作動薬

「indirect sympathomimetics」

　　[★] 交感神経間接作動薬