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Cevimeline

Pronunciation

(se vi ME leen)

Index Terms

  • Cevimeline HCl
  • Cevimeline Hydrochloride

Dosage Forms

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

Capsule, Oral, as hydrochloride:

Evoxac: 30 mg

Generic: 30 mg

Brand Names: U.S.

  • Evoxac

Pharmacologic Category

  • Cholinergic Agonist

Pharmacology

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

Absorption

Rapid; food decreases rate of absorption

Distribution

Vd: 6 L/kg

Metabolism

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

Excretion

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

Time to Peak

1.5 to 2 hours

Half-Life Elimination

5 ± 1 hours

Protein Binding

<20%

Use: Labeled Indications

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

Contraindications

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

Dosing: Adult

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

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustment provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment

There are no dosage adjustment provided in the manufacturer’s labeling.

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Acetylcholinesterase Inhibitors: May enhance the adverse/toxic effect of Cholinergic Agonists. 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. Management: Administer these agents in combination with caution, and monitor for conduction disturbances. Avoid methacholine with any beta blocker due to the potential for additive bronchoconstriction. Monitor therapy

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

Adverse Reactions

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: Fever

<1% (Limited to important or life-threatening): 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

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.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse effects were observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience decreased night vision, rhinorrhea, rhinitis, cough, or abdominal pain. Have patient report immediately to prescriber shortness of breath, severe nausea, severe vomiting, severe diarrhea, angina, tachycardia, bradycardia, abnormal heartbeat, confusion, vision changes, severe headache, tremors, painful urination, polyuria, sweating a lot, dehydration, watery eyes, swelling of arms or legs, severe dizziness, or passing out (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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