Evoxac
Evoxac - General Information
Evoxac is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors. It is indicated by the Food and Drug Administration for the treatment of dry mouth associated with Sjögren's syndrome. [Wikipedia]
Pharmacology of Evoxac
Evoxac 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.
Evoxac for patients
Patients should be informed that cevimeline may cause visual disturbances, especially at night, that could impair their ability to drive safely. If a patient sweats excessively while taking cevimeline, dehydration may develop. The patient should drink extra water and consult a health care provider.
Evoxac Interactions
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.
Evoxac Contraindications
Cevimeline is contraindicated in patients with uncontrolled asthma, known hypersensitivity to cevimeline, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle-closure) glaucoma.
Additional information about Evoxac
Evoxac Indication: For the treatment of symptoms of dry mouth in patients with Sjögren's Syndrome.
Mechanism Of Action: Muscarinic agonists such as cevimeline bind and activate the muscarinic M1 and M3 receptors. The M1 receptors are common in secretory glands (exocrine glands such as salivary and sweat glands), and their activation results in an increase in secretion from the secretory glands. The M3 receptors are found on smooth muscles and in many glands which help to stimulate secretion in salivary glands, and their activation generally results in smooth muscle contraction and increased glandular secretions. Therefore, as saliva excretion is increased, the symptoms of dry mouth are relieved.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Cevimeline
Synonyms: Cevimeline hydrochloride; Cevimeline hydrochloride hemihydrate; Cevimeline hydrochloride hydrate
Drug Category: Parasympathomimetics; Muscarinic Agonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Cevimeline: Evoxac; Saligren;
Absorption: Rapidly absorbed with peak concentration after 1.5 to 2 hours
Toxicity (Overdose): Not Available
Protein Binding: < 20%
Biotransformation: Primarily hepatic, isozymes CYP2D6 and CYP3A4 are responsible for the metabolism of cevimeline. Approximately 44.5% of the drug is converted to cis and trans-sulfoxide, 22.3% to glucuronic acid conjugate, and 4% to N-oxide of cevimeline. Approximately 8% of the trans-sulfoxide metabolite is then converted into the corresponding glucuronic acid conjugate.
Half Life: 5 ± 1 hours
Dosage Forms of Evoxac: Capsule Oral
Chemical IUPAC Name: (2R,5R)-2-methylspiro[1,3-oxathiolane-5,8'-1-azabicyclo[2.2.2]octane]
Chemical Formula: C10H17NOS
Cevimeline on Wikipedia: https://en.wikipedia.org/wiki/Cevimeline
Organisms Affected: Humans and other mammals
