adj.

副交感神経刺激様の

n.

副交感神経刺激薬

関: parasympathomimetic agent、parasympathomimetics

WordNet

having an effect similar to that resulting from stimulation of the parasympathetic nervous system; "parasympathomimetic drugs slow the heart rate"

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/02/28 03:09:46」(JST)

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A parasympathomimetic drug, sometimes called a cholinomimetic drug, is a substance that stimulates the parasympathetic nervous system (PSNS).^[1] These chemicals are also called cholinergic drugs because acetylcholine (ACh) is the neurotransmitter used by the PSNS. Chemicals in this family can act either directly by stimulating the nicotinic or muscarinic receptors (thus mimicking acetylcholine), or indirectly by inhibiting cholinesterase, promoting acetylcholine release, or other mechanisms.^[2]

Some chemical weapons such as sarin or VX, non-lethal riot control agents such as tear gas, and insecticides such as diazinon fall into this category.

Structure activity relationships for parasympathomimetic drugs^[3]

For a cholinergic agent, the following criteria describe the structure activity relationship:

Ing's Rule of 5: there should be no more than five atoms between the nitrogen and the terminal hydrogen for muscarinic (or cholinergic) activity;
the molecule must possess a nitrogen atom capable of bearing a positive charge, preferably a quaternary ammonium salt;
for maximum potency, the size of the alkyl groups substituted on the nitrogen should not exceed the size of a methyl group;
the molecule should have an oxygen atom, preferably an ester-like oxygen capable of participating in a hydrogen bond;
there should be a two-carbon unit between the oxygen atom and the nitrogen atom.

Pharmaceuticals

Direct-acting

These act by stimulating the nicotinic or muscarinic receptors.

Choline esters
- Acetylcholine (all acetylcholine receptors)
- Bethanechol (M3 receptors)
- Carbachol (all muscarinic receptors and some nicotinic receptors)
- Methacholine (all muscarinic receptors)
Plant alkaloids
- Arecoline
- Nicotine
- Muscarine
- Pilocarpine (M3 receptors)

Indirect-acting

Indirect acting parasympathomimetic drugs may be either reversible cholinesterase inhibitors, irreversible cholinesterase inhibitors or drugs that promote ACh release or anti-adrenergics. The latter inhibits the antagonistic system, the sympathetic nervous system.

Reversible cholinesterase inhibitors
- Donepezil
- Edrophonium
- Neostigmine
- Physostigmine
- Pyridostigmine
- Rivastigmine
- Tacrine
- Caffeine (non-competitive)^[4]
- Huperzine A
Irreversible cholinesterase inhibitors
- Echothiophate
- Isoflurophate
- Malathion
ACh release promoters
- Cisapride
- Droperidol
- Domperidone
- Metoclopramide
- Risperidone
- Paliperidone
- Trazodone - via blockade of the α adrenergic receptors
Anti-adrenergics

See also: alpha blocker and beta blocker

- clonidine (α-receptor agonist, α₂ > α₁, giving negative feedback)
- methyldopa (α₂ agonist, giving negative feedback)
- propranolol (β-receptor antagonist)
- atenolol (β₁ antagonist)
- prazosin (α₁ antagonist)
- Oxymetazoline (partial α2 adrenergic agonist)

Notes

^ "Dorlands Medical Dictionary:parasympathomimetic".
^ Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
^ Medicinal Chemistry of Adrenergics and Cholinergics
^ Karadsheh, N; Kussie, P; Linthicum, DS (1991). "Inhibition of acetylcholinesterase by caffeine, anabasine, methyl pyrrolidine and their derivatives". Toxicology letters. 55 (3): 335–42. doi:10.1016/0378-4274(91)90015-X. PMID 2003276.

External links

Parasympathomimetics at the US National Library of Medicine Medical Subject Headings (MeSH)

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Japanese Journal

Scopolamineのマウス移所運動促進作用に対する耐性形成 : 投与直後の自由運動の重要性

栗原久
東京福祉大学・大学院紀要 2(1), 3-11, 2011-08
… Such development of the behavioral tolerance to SCP may be due to the psychopharmacological characteristics of SCP that the harmful symptoms such as dry mouth and eyes produced by blockade of parasympathomimetic nervous systems overwhelm the reward effect (dependence liability) of this drug. …
NAID 120005273535

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, , [他], , ,
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… However, many medications for relief of dry mouth, such as parasympathomimetic (cholinomimetic) drugs, have serious adverse effects. … Palpitation, sweating, nausea, diarrhea and dizziness have all been observed in elderly patients taking parasympathomimetic drugs. … Our data suggests that umami is an effective tool for the relief of hypogeusia without the side effects of parasympathomimetic drugs. …
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, , ,
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Hyposalivation Strongly Influences Hypogeusia in the Elderly

, , [他], , ,
Journal of Health Science 55(5), 689-698, 2009
… Many medications for relief of dry mouth, primarily parasympathomimetic drugs, have serious adverse effects such as palpitation, sweating, nausea, diarrhea or dizziness, particularly in the elderly. …
NAID 130000127955

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