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Details

Stereochemistry RACEMIC
Molecular Formula C10H17NOS
Molecular Weight 199.313
Optical Activity ( + / - )
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CEVIMELINE

SMILES

C[C@H]1O[C@]2(CS1)CN3CC[C@H]2CC3

InChI

InChIKey=WUTYZMFRCNBCHQ-WPRPVWTQSA-N
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-/m0/s1

HIDE SMILES / InChI

Molecular Formula C10H17NOS
Molecular Weight 199.313
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Cevimeline is a cholinergic agonist, which binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands and increase tone of the smooth muscle in the gastrointestinal and urinary tracts. Cevimeline is indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s Syndrome. Known side effects include nausea, vomiting, diarrhea, excessive sweating, rash, headache, runny nose, cough, drowsiness, hot flashes, blurred vision, and difficulty sleeping. Cevimeline should be administered with caution to patients taking beta adrenergic antagonists, because of the possibility of conduction disturbances. Drugs with para-sympathomimetic effects administered concurrently with cevimeline can be expected to have additive effects. Cevimeline might interfere with desirable antimuscarinic effects of drugs used concomitantly.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
EVOXAC

Cmax

ValueDoseCo-administeredAnalytePopulation
0.09 mg/g
30 mg single, oral
CEVIMELINE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
0.52 mg × h/g
30 mg single, oral
CEVIMELINE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
0.09 h
30 mg single, oral
CEVIMELINE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
80%
CEVIMELINE plasma
Homo sapiens

Doses

AEs

OverviewOther

Other InhibitorOther SubstrateOther Inducer




Drug as perpetrator​

Drug as victim

Sourcing

PubMed

Sample Use Guides

In Vivo Use Guide
The recommended dose of cevimeline hydrochloride is 30 mg taken three times a day.
Route of Administration: Oral
In Vitro Use Guide
Cevimeline increased the intracellular Ca2+ concentration of parotid gland acinar and duct cells over 1 uM in a dose-dependent manner.
Substance Class Chemical
Record UNII
K9V0CDQ56E
Record Status Validated (UNII)
Record Version