Cevimeline

Oral
Dry mouth associated with Sjogren’s syndrome

Uncontrolled asthma, acute iritis, narrow-angle glaucoma.

Patients with cardiovascular disease (e.g. MI, angina pectoris), controlled asthma, chronic bronchitis, COPD, history of nephrolithiasis or cholelithiasis. Pregnancy and lactation. CYP2D6 poor metabolisers.

Significant: Parasympathomimetic effects (e.g. AV block, bradycardia, cardiac arrhythmia, hypotension, lacrimation, respiratory distress, tachycardia, tremor, vomiting).
Cardiac disorders: Palpitation, chest pain.
Gastrointestinal disorders: Nausea, abdominal pain, diarrhoea, salivary gland pain, excessive salivation.
General disorders and administration site conditions: Hyperhidrosis, back pain, fatigue, fever, malaise.
Metabolism and nutrition disorders: Loss of appetite.
Musculoskeletal and connective tissue disorders: Arthralgia, skeletal pain.
Nervous system disorders: Headache.
Psychiatric disorders: Insomnia.
Renal and urinary disorders: Frequent urination, UTI.
Respiratory, thoracic and mediastinal disorders: Rhinitis, sinusitis, upper respiratory tract infection, cough, bronchitis.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Hot flushes.

PO: C

This drug may cause visual disturbances (e.g. blurred vision, decreased visual acuity, impaired depth perception), if affected, do not drive or operate machinery.

May increase risk of conduction disturbances and bronchoconstriction with concomitant use of β-adrenergic agonists. Additive effects with parasympathomimetic agents. Decreased metabolism and increased risk of adverse effects with inhibitors of CYP2D6 and CYP3A3/4.

Decreased rate and extent of absorption with food.

Description:
Mechanism of Action: Cevimeline is a cholinergic agonist that selectively binds to muscarinic receptors resulting in increased secretion of exocrine glands (e.g. salivary, sweat glands) and increased smooth muscle tone in gastrointestinal and urinary tracts.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Decreased rate and extent of absorption with food. Time to peak plasma concentration: 1.5-2 hours.
Distribution: Volume of distribution: Approx 6 L/kg. Plasma protein binding: <20%.
Metabolism: Metabolised in the liver by CYP2D6 and CYP3A3/4 to cis and trans-sulfoxide, glucuronic acid conjugate, and N-oxide metabolites.
Excretion: Mainly via urine (84% in 24 hours; 97% in 7 days); faeces (approx 0.5% in 7 days). Elimination half-life: 5±1 hour.

Source: National Center for Biotechnology Information. PubChem Database. Evoxac, CID=83898, https://pubchem.ncbi.nlm.nih.gov/compound/Evoxac (accessed on Mar. 25, 2020)

Store between 20-25°C.

Other Gastrointestinal Drugs

N07AX03 - cevimeline ; Belongs to the class of other parasympathomimetics.

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Anon. CYP2D6-Cevimeline (Pharmacogenomics). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/11/2019.

Buckingham R (ed). Cevimeline Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/11/2019.

Cevimeline Capsule (Lupin Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/11/2019.