Cevimeline Hcl (cevimeline HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Cevimeline hydrochloride is a cholinergic agonist that binds to muscarinic receptors.
Cevimeline hydrochloride, a quinuclidine derivative of acetylcholine, is a cholinergic agonist that binds to muscarinic receptors. In sufficient dosages, muscarinic agonists can increase exocrine (e.g., salivary, sweat) gland secretion and increase GI and urinary tract smooth muscle tone.
Cevimeline is pharmacologically similar to pilocarpine, another oral cholinergic agonist that exerts predominantly muscarinic action. Both drugs stimulate residual salivary gland tissues and have been shown to substantially increase salivary flow. However, the adverse effect profile of the drugs may differ based on differences in selectivity and affinity for specific muscarinic receptor subtypes.
Cevimeline is a more selective muscarinic agonist than pilocarpine and exhibits a 40-fold greater affinity for M3 muscarinic receptors in the lacrimal and salivary glands than for M2 receptors in cardiac tissue.
Cevimeline is rapidly absorbed following oral administration; peak plasma concentrations are reached in approximately 1.5-2 hours. Cevimeline is metabolized by cytochrome P-450 (CYP) isoenzymes 2D6, 3A3, and 3A4. In an in vitro study, CYP isoenzymes 1A2, 2A6, 2C9, 2C19, 2D6, 2E1, and 3A4 were not inhibited by cevimeline.
The drug is excreted principally in urine, with 97 and 0.5% of a 30-mg dose recovered in urine and feces, respectively, after 7 days.
USES: This medication is used to treat symptoms of dry mouth due to a certain immune disease (Sjogren's syndrome). Cevimeline belongs to a class of drugs known as cholinergic agonists. It works by stimulating certain nerves to increase the amount of saliva you produce, making it easier and more comfortable to speak and swallow.
Generic name: cevimeline HCl
Pronunciation: (seh-VIMM-eh-leen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Cevimeline Hcl
Indications
The following indications are listed for Cevimeline Hcl:
- Xerostomia Secondary To Sjogren's Syndrome
Also known as: Xerostomia Secondary To Gougerot-Sjogren Disease, Xerostomia Secondary To Sicca Syndrome, Xerostomia Secondary To Sjogren's Disease.
Dosing
Dosage of cevimeline hydrochloride is expressed in terms of cevimeline.
The recommended adult dosage of cevimeline for treatment of dry mouth secondary to Sjogren syndrome is 30 mg 3 times daily. Safety and efficacy of dosages exceeding 90 mg daily have not been established.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to cevimeline hydrochloride, uncontrolled asthma, and when miosis is undesirable (e.g., acute iritis, angle-closure glaucoma).
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 3% or more of patients receiving cevimeline include excessive sweating, headache, nausea, sinusitis, upper respiratory tract infection, rhinitis, diarrhea, dyspepsia, abdominal pain, urinary tract infection, cough, pharyngitis, vomiting, injury, back pain, rash, conjunctivitis, dizziness, bronchitis, arthralgia, surgical intervention, fatigue, and pain.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of cevimeline have not been established in children.
There are no adequate and well-controlled studies of cevimeline in pregnant women; in animal studies, a reduced number of implantations, possibly due to maternal toxicity was observed when the drug was administered to pregnant rats.
Cevimeline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known whether cevimeline is distributed into milk; a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Response in patients 65 years of age and older does not appear to differ from that of younger adults. However, the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly should be considered.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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