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Cevimeline

From Wikipedia, the free encyclopedia
Pharmaceutical drug
Pharmaceutical compound
Cevimeline
Clinical data
Trade namesEvoxac
AHFS/Drugs.comMonograph
MedlinePlusa608025
Pregnancy
category
  • C
Routes of
administration
By mouth (capsules)
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding<20%
Identifiers
  • (2R,2R)-2'-Methylspiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxathiolane]
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC10H17NOS
Molar mass199.31 g·mol−1
3D model (JSmol)
  • O1[C@H](SC[C@@]12CN3CCC2CC3)C
  • InChI=1S/C10H17NOS/c1-8-12-10(7-13-8)6-11-4-2-9(10)3-5-11/h8-9H,2-7H2,1H3/t8-,10-/m1/s1 checkY
  • Key:WUTYZMFRCNBCHQ-PSASIEDQSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Cevimeline (trade nameEvoxac) is a synthetic analog of the natural alkaloidmuscarine with a particular agonistic effect onM1 andM3 receptors. It is used in the treatment ofdry mouth andSjögren's disease.

Medical uses

[edit]

Cevimeline is used in the treatment ofxerostomia (dry mouth)[1][2] andSjögren's syndrome.[1] It increases the production of saliva.[2]

Side effects

[edit]

Known side effects includenausea,vomiting,diarrhea, excessivesweating,rash,headache,runny nose,cough,drowsiness,hot flashes,blurred vision, anddifficulty sleeping.[3]

Contraindications includeasthma andangle closure glaucoma.[citation needed]

Mechanism of action

[edit]

Cevimeline is a cholinergic agonist.[2] It has a particular effect onM1 andM3 receptors.[2] By activating the M3 receptors of theparasympathetic nervous system, cevimeline stimulates secretion by thesalivary glands, thereby alleviating dry mouth.

See also

[edit]
  • Pilocarpine — a similar parasympathomimetic medication for dry mouth (xerostomia)
  • Bethanechol — a similar muscarinic parasympathomimetic with longer-lasting effect

References

[edit]
  1. ^abOno M, Takamura E, Shinozaki K, Tsumura T, Hamano T, Yagi Y, Tsubota K (July 2004). "Therapeutic effect of cevimeline on dry eye in patients with Sjögren's syndrome: a randomized, double-blind clinical study".American Journal of Ophthalmology.138 (1):6–17.doi:10.1016/j.ajo.2004.02.010.PMID 15234277.
  2. ^abcdFox RI, Fox CM (2019). "Management of Sjögren's".Dubois' Lupus Erythematosus and Related Syndromes (9th ed.).Elsevier. pp. 745–758.doi:10.1016/B978-0-323-47927-1.00060-8.ISBN 978-0-323-47927-1.
  3. ^"Cevimeline".MedicineNet. Retrieved12 October 2007.

External links

[edit]
mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(andprodrugs)
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