Your activity: 2 p.v.

Cevimeline: Drug information

Cevimeline: Drug information
(For additional information see "Cevimeline: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Evoxac
Pharmacologic Category
  • Cholinergic Agonist
Dosing: Adult
Xerostomia

Xerostomia (associated with Sjögren syndrome): Oral: 30 mg 3 times/day.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral, as hydrochloride:

Evoxac: 30 mg

Generic: 30 mg

Generic Equivalent Available: US

Yes

Use: Labeled Indications

Xerostomia (associated with Sjögren syndrome): Treatment of symptoms of dry mouth in patients with Sjögren syndrome.

Medication Safety Issues
Sound-alike/look-alike issues:

Cevimeline may be confused with Savella

Evoxac may be confused with Eurax

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not always defined.

>10%:

Dermatologic: Diaphoresis (19%)

Gastrointestinal: Nausea (14%)

Respiratory: Sinusitis (12%), rhinitis (11%), upper respiratory tract infection (11%)

1% to 10%:

Cardiovascular: Chest pain, edema, palpitations, peripheral edema

Central nervous system: Fatigue (3%), insomnia (2%), depression, hypertonia, hypoesthesia, hyporeflexia, migraine, vertigo

Dermatologic: Dermatological disease, erythematous rash, pruritus

Endocrine & metabolic: Hot flash (2%), increased amylase

Gastrointestinal: Abdominal pain (8%), vomiting (5%), sialorrhea (2%), anorexia, aphthous stomatitis, constipation, eructation, flatulence, gastroesophageal reflux disease, hiccups, salivary gland pain, sialadenitis, toothache, xerostomia

Genitourinary: Urinary tract infection (6%), cystitis, vaginitis

Hematologic & oncologic: Anemia

Hypersensitivity: Hypersensitivity reaction

Infection: Abscess, candidiasis, fungal infection, infection

Neuromuscular & skeletal: Back pain (5%), arthralgia (4%), skeletal pain (3%), weakness (1%), leg cramps, myalgia, tremor

Ophthalmic: Eye disease, eye infection, eye pain, visual disturbance, xerophthalmia

Otic: Otalgia, otitis media

Respiratory: Cough (6%), bronchitis (4%), epistaxis, flu-like symptoms, pneumonia

Miscellaneous: Accidental injury (5%), fever

<1%, postmarketing, and/or case reports: acute exacerbations of multiple sclerosis, aggressive behavior, alopecia, angina pectoris, anterior chamber eye hemorrhage, aphasia, apnea, arthropathy, avascular necrosis of femoral head, bronchospasm, bullous rash, bundle branch block, cardiac arrhythmia, cardiac disease, cholecystitis, cholelithiasis, cholinergic syndrome, deafness, dehydration, delirium, dementia, depersonalization, diabetes mellitus, dyskinesia, ECG abnormality, emotional lability, eosinophilia, esophageal stenosis, esophagitis, extrasystoles, facial edema, gastric ulcer, gastrointestinal hemorrhage, gingival hyperplasia, glaucoma, granulocytopenia, hallucination, hematoma, hematuria, hepatic insufficiency, hyperglycemia, hyperkalemia, hypertension, hypoglycemia, hypotension, hypothyroidism, immune thrombocytopenia, impotence, increased liver enzymes, intestinal obstruction, inversion T wave on ECG, irritable bowel syndrome, leukopenia, lymphocytosis, manic reaction, menstrual disease, myocardial infarction, nephrolithiasis, neuropathy, paralysis, paranoia, paresthesia, peptic ulcer, pericarditis, peripheral ischemia, skin photosensitivity reaction, pleural effusion, pulmonary embolism, pulmonary fibrosis, rectal disease, renal insufficiency, seizure, sepsis, supraventricular tachycardia, syncope, systemic lupus erythematosus, tachycardia, tenosynovitis, thrombocytopenia, thrombophlebitis, ulcerative colitis, urinary retention, urination disorder, vasculitis

Contraindications

Hypersensitivity to cevimeline or any component of the formulation; uncontrolled asthma; when miosis is undesirable (eg, narrow-angle glaucoma, acute iritis)

Warnings/Precautions

Concerns related to adverse effects:

• Parasympathomimetic effects: Toxicity is characterized by an exaggeration of parasympathomimetic effects (eg, atrioventricular block, bradycardia, cardiac arrhythmia, hypotension, lacrimation, sweating, respiratory distress, tachycardia, tremors, vomiting); excessive sweating may lead to dehydration in some patients.

• Visual effects: May cause blurred vision, decreased visual acuity (particularly at night and in patients with central lens changes) and impaired depth perception. Patients should be cautioned about driving at night or performing hazardous activities in reduced lighting.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with significant cardiovascular disease (including angina, myocardial infarction); may alter cardiac conduction and/or heart rate.

• Cholelithiasis: Use with caution in patients with a history of cholelithiasis; may induce contractions of the gallbladder or biliary smooth muscle, precipitating complications such as cholangitis, cholecystitis, or biliary obstruction.

• Nephrolithiasis: Use with caution in patients with a history of nephrolithiasis; may induce smooth muscle spasms, precipitating renal colic or ureteral reflux in patients with nephrolithiasis.

• Respiratory disease: Use with caution in patients with controlled asthma, COPD, or chronic bronchitis; may increase bronchial smooth muscle tone, airway resistance, and bronchial secretions.

Special populations:

• Patients with CYP2D6 deficiency: Patients with a known or suspected deficiency of CYP2D6 may be at higher risk of adverse effects.

Metabolism/Transport Effects

Substrate of CYP2D6 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May enhance the adverse/toxic effect of Cholinergic Agonists. Specifically, cholinergic effects may be enhanced or increased. Risk C: Monitor therapy

Beta-Blockers: May enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction. Risk C: Monitor therapy

Cimetropium: Cholinergic Agonists may diminish the anticholinergic effect of Cimetropium. Risk C: Monitor therapy

Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Risk D: Consider therapy modification

Pregnancy Considerations

Adverse effects were observed in animal reproduction studies.

Breastfeeding Considerations

It is not known if cevimeline is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, the manufacturer recommends a decision be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of treatment to the mother.

Mechanism of Action

Binds to muscarinic (cholinergic) receptors, causing an increase in secretion of exocrine glands (such as salivary and sweat glands) and increase tone of smooth muscle in gastrointestinal and urinary tracts

Pharmacokinetics

Absorption: Rapid; food decreases rate of absorption.

Distribution: Vd: 6 L/kg.

Protein binding: <20%.

Metabolism: Hepatic via CYP2D6, CYP3A3, and CYP3A4; metabolites: cis and trans-sulfoxide, glucuronic acid conjugate, N-oxide metabolite.

Half-life elimination: 5 ± 1 hours.

Time to peak: 1.5 to 2.9 hours.

Excretion: Urine (84% in 24 hours, 97% in 7 days); feces (0.5% in 7 days).

Pricing: US

Capsules (Cevimeline HCl Oral)

30 mg (per each): $3.48 - $3.49

Capsules (Evoxac Oral)

30 mg (per each): $9.77

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Evoxac (JP, TW);
  • Saligren (JP)


For country code abbreviations (show table)
  1. Evoxac (cevimeline) [prescribing information]. South Plainfield, NJ: Cosette Pharmaceuticals Inc; February 2022.
Topic 8884 Version 164.0