Parasympathomime

tic drug

A parasympathomimetic drug, somet imes called a cholinomimetic drug [1] or cholinergic

receptor stimulating agent,[2] is a subst ance t hat st imulat es t he parasympat het ic nervous
syst em (PSNS).[3][2] These chemicals are also called cholinergic drugs because
acet ylcholine (ACh) is t he neurot ransmit t er used by t he PSNS.[1][4] Chemicals in t his family
can act eit her direct ly by st imulat ing t he nicot inic or muscarinic recept ors (t hus mimicking
acet ylcholine), or indirect ly by inhibit ing cholinest erase, promot ing acet ylcholine release, or
ot her mechanisms.[5]

Some chemical weapons such as sarin or VX, non-let hal riot cont rol agent s such as t ear gas,
and insect icides such as diazinon fall int o t his cat egory.

Structure activity relationships for

parasympathomimetic drugs[6]

For a cholinergic agent , t he following crit eria describe t he st ruct ure act ivit y relat ionship:

1. Ing's Rule of 5: t here should be no more t han five at oms bet ween t he nit rogen and t he
t erminal hydrogen for muscarinic (or cholinergic) act ivit y;

2. t he molecule must possess a nit rogen at om capable of bearing a posit ive charge,
preferably a quat ernary ammonium salt ;

3. for maximum pot ency, t he size of t he alkyl groups subst it ut ed on t he nit rogen should
not exceed t he size of a met hyl group;
 4. t he molecule should have an oxygen at om, preferably an est er-like oxygen capable of
part icipat ing in a hydrogen bond;

5. t here should be a t wo-carbon unit bet ween t he oxygen at om and t he nit rogen at om.

Pharmaceuticals/Supplements

Direct-acting
…
These act by st imulat ing t he nicot inic or muscarinic recept ors.

Choline esters
Acet ylcholine (all acet ylcholine recept ors)

Bet hanechol (M3 recept ors)

Carbachol (all muscarinic recept ors and some nicot inic recept ors)

Met hacholine (all muscarinic recept ors)

Plant alkaloids
Arecoline

Nicot ine

Muscarine

Pilocarpine (M3 recept ors)

Indirect-acting
…
Indirect act ing parasympat homimet ic subst ances may be eit her reversible cholinest erase
inhibit ors, irreversible cholinest erase inhibit ors or subst ances t hat promot e ACh release or
ant i-adrenergics. The lat t er inhibit s t he ant agonist ic syst em, t he sympat het ic nervous
syst em.

Reversible cholinesterase inhibitors

Donepezil

Edrophonium

Neost igmine

Physost igmine

Pyridost igmine

Rivast igmine

Tacrine
 Caffeine (non-compet it ive)[7]

Huperzine A

Irreversible cholinesterase inhibitors

Echot hiophat e

Isoflurophat e

Malat hion

ACh release promoters

Alpha GPC

Cisapride

Droperidol

Domperidone

Met oclopramide

Risperidone

Paliperidone

Trazodone – via blockade of t he α adrenergic recept ors

Anti-adrenergics: See also alpha blocker and bet a blocker

Clonidine (α-recept or agonist , α2 > α1, giving negat ive feedback)

Met hyldopa (α2 agonist , giving negat ive feedback)

Propranolol (β-recept or ant agonist )

Met oprolol (β-recept or ant agonist )

At enolol (β 1 ant agonist )

Prazosin (α1 ant agonist )

Oxymet azoline (part ial α2 adrenergic agonist )

See also

Sympat homimet ic drug

References

1. Dowd, Frank (2017). Pharmacology and therapeutics for dentistry: Chapter 6 - Cholinergic Agonists
and Muscarinic Receptor Antagonists. St. Louis, Missouri: Elsevier. p. 82-97. ISBN 978-0-323-39307-
2. OCLC 958121223 (https://www.worldcat.org/oclc/958121223) .
 2. Forrester, John V.; Dick, Andrew D.; McMenamin, Paul G.; Roberts, Fiona; Pearlman, Eric (2016).
"General and ocular pharmacology". The Eye. Elsevier. pp. 338–369.e1. doi:10.1016/b978-0-7020-
5554-6.00006-x (https://doi.org/10.1016%2Fb978-0-7020-5554-6.00006-x) . ISBN 978-0-7020-
5554-6. "Parasympathomimetics are a group of drugs that act either by directly stimulating the
muscarinic receptor, for example pilocarpine, or by inhibiting the enzyme acetylcholinesterase, which
hydrolyses the acetylcholine in the synapse."

3. "Dorlands Medical Dictionary:parasympathomimetic" (https://web.archive.org/web/2009072617422

5/http://www.mercksource.com/pp/us/cns/cns_hl_dorlands_split.jsp?pg=%2Fppdocs%2Fus%2Fcom
mon%2Fdorlands%2Fdorland%2Fsix%2F000078652.htm) . Archived from the original (http://www.
mercksource.com/pp/us/cns/cns_hl_dorlands_split.jsp?pg=/ppdocs/us/common/dorlands/dorland/
six/000078652.htm) on 2009-07-26.

4. Parasympathomimetics (https://www.ncbi.nlm.nih.gov/mesh/68010277)

5. Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-
7757-6

. "Medicinal Chemistry of Adrenergics and Cholinergics" (https://web.archive.org/web/201011040227

42/http://pharmaxchange.info/notes/medicinal_chemistry/adrenergics_cholinergics.html) .
Archived from the original (http://pharmaxchange.info/notes/medicinal_chemistry/adrenergics_choli
nergics.html) on 2010-11-04. Retrieved 2010-10-23.

7. 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 (https://doi.org/10.1016%2F0378-4274%2891%2990015-X) .
PMID 2003276 (https://pubmed.ncbi.nlm.nih.gov/2003276) .

External links

Parasympat homimet ics (ht t ps://meshb.nlm.nih.gov/record/ui?name=Parasympat homimet i

cs) at t he US Nat ional Library of Medicine Medical Subject Headings (MeSH)

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