cevimeline

REMS

Treatment of the symptoms of dry mouth associated with Sjögren's syndrome.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
When miosis is undesirable (acute iritis, angle-closure glaucoma);
Lactation: Discontinue or bottle feed.

Use Cautiously in:

Cardiovascular disease including angina pectoris or history of MI;
Pulmonary disease including asthma, chronic bronchitis, or chronic obstructive pulmonary disease;
Nephrolithiasis or cholelithiasis;
Geri: May be more sensitive to toxicity;
OB: Use only if potential benefit justifies potential risk to the fetus;
Pedi: Safety not established.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: excessive sweating, hot flashes

EENT: rhinitis, visual disturbances

GI: nausea, diarrhea, excessive salivation

Neuro: coughing

Interactions ⬆ ⬇

Drug-drug:

Concurrent beta blocker therapy may ↑ the risk of cardiac conduction disturbances.
Additive parasympathetic and muscarinic effects may occur with drugs that have parasympathetic or muscarinic properties.
Drugs that inhibit CYP2D6 and CYP3A3/4 liver enzymes may inhibit the metabolism of cevimeline and ↑ its effects and risk of toxicity.

Drug-Natural Products:

St. John's wort may ↑ the metabolism of cevimeline and ↓ its levels.
Angel's trumpet, jimson weed, and scopolia may antagonize cholinergic effects.

Availability ⬆ ⬇

(Generic available)

Capsules: 30 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 30 mg 3 times daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Direct cholinergic (muscarinic) effects result on increased secretion of exocrine glands including salivary and sweat glands, and increased smooth muscle tone in the gastrointestinal and urinary tracts.

Therapeutic effects:

Improved symptoms of dry mouth in patients with Sjögren's syndrome.

Classifications ⬆ ⬇

Therapeutic Classification: xerostomia therapy adjuncts

Pharmacologic Classification: cholinergics, muscarinic agonists, sialagogues

Pharmacokinetics ⬆ ⬇

Absorption: Rapidly absorbed following oral administration.

Distribution: Extensively bound to tissues.

Metabolism/Excretion: Mostly metabolized by the liver (CYP2D6 and CYP3A3/4 isoenzymes) (the CYP2D6 enzyme system exhibits genetic polymorphism; ~7% of population may be poor metabolizers and may have significantly ↑ cevimeline concentrations and an ↑ risk of adverse effects); 16% excreted unchanged in urine.

Half-Life: 5 hr.

Time/Action Profile ⬆ ⬇

(blood levels)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1.5–2 hr	unknown

Patient/Family Teaching ⬆ ⬇

Instruct patient to take cevimeline as directed.
May cause visual disturbances, especially at night, that could impair ability to drive safely.
Advise patient to drink extra water if sweating excessively. May cause dehydration.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Advise female patients to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

section name header

Indications ⬇