Cevimeline drug data and news

Cevimeline drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Cevimeline
Brand Names/Synonyms AF 102B; AF-102B; Cevimeline; Cevimeline Hydrochloride; Cevimeline Hydrochloride Hydrate; Cevimeline, Hydrochloride Salt; Cevimelinehydrochloride Salt; Evoxac; Fks 508; Sni 2011
Indication For the treatment of symptoms of dry mouth in patients with Sjogren's Syndrome
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Description Not Available
Pharmacology Cevimeline is a cholinergic agonist which binds to muscarinic receptors. Cevimeline is indicated for the treatment of symptoms of dry mouth in patients with Sjogren's Syndrome.
Mechanism Of Action Muscarinic agonists such as cevimeline 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.
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Dosage Forms Not Available
Drug_Category Parasympathomimetics; Muscarinic Agonists
Absorption Rapidly absorbed with peak concentration after 1.5 to 2 hours
Interactions Interactions for Cevimeline:

Cevimeline should be administered with caution to patients taking beta adrenergic antagonists, because of the possibility of conduction disturbances. Drugs with parasympathomimetic effects administered concurrently with cevimeline can be expected to have additive effects. Cevimeline might interfere with desirable antimuscarinic effects of drugs used concomitantly.

Drugs which inhibit CYP2D6 and CYP3A3/4 also inhibit the metabolism of cevimeline. Cevimeline should be used with caution in individuals known or suspected to be deficient in CYP2D6 activity, based on previous experience, as they may be at a higher risk of adverse events. In an in vitro study, cytochrome P450 isozymes 1A2, 2A6, 2C9, 2C19, 2D6, 2E1, and 3A4 were not inhibited by exposure to cevimeline.

Toxicity Not Available
Organisms Affected Humans and other mammals
Chemical IUPAC Name 2-Methyspiro(1,3-oxathiolane-5,3)quinuclidine
Chemical Formula C10H17NOS
Molecular Weight 489.565 g/mol
Smiles String CC1OC2(CN3CCC2CC3)CS1
Melting Point 201-203 oC (HCl salt)
Water Solubility Very soluble
State Solid
LogP/Hphobicity Not Available
Isoelectric Point Not Available
Biotransformation Primarily hepatic by CYP2D6 and CYP3A4. 45% of dose is converted to cis and trans sulfoxides and 25% is converted to the glucuronic acid conjugate
Half Life 5 +/-1 hours
Protein Binding [%] <20%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Cevimeline.html
http://www.rxlist.com/cgi/generic2/cevimeline.htm
Drug Type Approved Drug
Accession No APRD00224
CAS Registry Number 107223-08-9
KEGG Compound ID C07772
PubChem ID SID:9974
PharmGKB ID PA448916
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available

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