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Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Cevimeline is a muscarinic agonist that binds to muscarinic receptors (Weber and Keating 2008). Cevimeline is indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s syndrome (Weber and Keating 2008). After administration of a single 30-mg capsule, cevimeline is rapidly absorbed with a mean time to peak concentration of 1.5 to 2 h. After 24 h, 86.7% of the dose was recovered (16.0% unchanged, 44.5% as cis- and trans-sulfoxide, 22.3% of the dose as glucuronic acid conjugate, and 4% of the dose as N-oxide of cevimeline) (Washio et al. 2003). The mean half-life of cevimeline is ~5 h. CYP2D6 and 3A3/4 are responsible for the metabolism of cevimeline (Washio et al. 2003). Cevimeline does not inhibit CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1, and 3A4.
Non-Neoplastic Salivary Gland Diseases
Published in John C Watkinson, Raymond W Clarke, Terry M Jones, Vinidh Paleri, Nicholas White, Tim Woolford, Head & Neck Surgery Plastic Surgery, 2018
Stephen R. Porter, Stefano Fedele, Valeria Mercadante
Several double-blind studies confirmed that cevimeline significantly reduces symptoms of xerostomia and dry eyes in patients with Sjögren’s syndrome.199 The best results in RCTs were achieved with a dose of 30 mg/8 h.200 The adverse effects of cevimeline mirror those of pilocarpine, with increased gastrointestinal symptoms and rigor but reduced urinary frequency in the case of cevimeline.201
A review of dry eye disease therapies: exploring the qualities of varenicline solution nasal spray
Published in Expert Review of Ophthalmology, 2023
Siddharth Bhargava, Ranjani Panda, Asma M Azam, John D Sheppard
Approximately 34% of basal tear film production is thought to originate from the activation of efferent trigeminal parasympathetic nerves [68]. The trigeminal nerve endings scattered throughout the nasal cavity epithelium possess nicotinic acetylcholine receptors (nAChR’s) [69]. As such, molecular agonists that stimulate nAChR’s could function to activate the NLR, thereby increasing tear film production. Oral formulations of pilocarpine and cevimeline, muscarinic acetylcholine receptor agonists, are used in patients with Sjögren’s syndrome for the treatment of dry mouth. However, studies have reported symptomatic improvement in dry eye symptoms with such systemic administration [70–72]. Expectedly, systemic off-target parasympathetic side effects of the oral delivery route, such as nausea, diarrhea, flushing, and frequent urination, make this a sub-optimal modality for the treatment of dry eyes.
Meta-analysis on pharmacological therapies in the management of xerostomia in patients with Sjogren’s syndrome
Published in Immunopharmacology and Immunotoxicology, 2019
Komali Garlapati, Anuja Kammari, Raj Kumar Badam, Surekha B. E., Mamatha Boringi, Pratima Soni
In the study done by Dianne et al. [6] efficacy of Cevimeline 15 mg and 30 mg 3 times daily for 12 weeks was compared with placebo and 30 mg Cevimeline showed good result in improving saliva flow rate as the visual analog scale findings showed increased efficacy in patients who received 30 mg dosage of Cevimeline compared with patients who received 15 mg dosage of Cevimeline. The most commonly reported drug-related adverse effects were nausea, sinusitis, increased sweating, headache, diarrhea, pharyngitis.
Pharmacological treatments available for the management of underactive bladder in neurological conditions
Published in Expert Review of Clinical Pharmacology, 2018
Seyedeh-Sanam Ladi-Seyedian, Behnam Nabavizadeh, Lida Sharifi-Rad, Abdol-Mohammad Kajbafzadeh
Furthermore, activation of presynaptic muscarinic M1 receptors, located on the bladder efferent nerves, can increase secretion of acetylcholine. Cevimeline, an M1 agonist approved for xerostomia [81], increased non-voiding and phasic contractions at doses of 0.3 mg/kg or higher in rats and guinea pigs. These preclinical findings can justify the evidence for clinical testing of cevimeline in UAB patients [28].