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Cevimeline Hydrochloride
Overview
What is Cevimeline Hydrochloride?
Cevimeline is cis-2’-methylspiro {1-azabicyclo [2.2.2] octane-3, 5’ -[1,3] oxathiolane} hydrochloride, hydrate (2:1). Its molecular formula is CHNOS.HCl.1/2 HO, and its structural formula is:
Cevimeline has a molecular weight of 244.79. It is a white to off white crystalline powder with a melting point range of 201 to 203°C. It is freely soluble in alcohol and chloroform, very soluble in water, and virtually insoluble in ether. The pH of a 1% solution ranges from 4.6 to 5.6. Inactive ingredients include hydroxypropyl cellulose, lactose monohydrate, and magnesium stearate. Gelatin capsule shells contain: gelatin, monogramming ink, purified water, sodium lauryl sulfate and titanium dioxide. The monogramming ink contains: ammonium hydroxide, iron oxide, isopropyl alcohol, n-butyl alcohol, propylene glycol and shellac.
What does Cevimeline Hydrochloride look like?
What are the available doses of Cevimeline Hydrochloride?
Sorry No records found.
What should I talk to my health care provider before I take Cevimeline Hydrochloride?
Sorry No records found
How should I use Cevimeline Hydrochloride?
Cevimeline hydrochloride is indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s Syndrome.
The recommended dose of cevimeline hydrochloride is 30 mg taken three times a day. There is insufficient safety information to support doses greater than 30 mg tid. There is also insufficient evidence for additional efficacy of cevimeline hydrochloride at doses greater than 30 mg tid.
What interacts with Cevimeline Hydrochloride?
Cevimeline hydrochloride is contraindicated in patients with uncontrolled asthma, known hypersensitivity to cevimeline, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle-closure) glaucoma.
What are the warnings of Cevimeline Hydrochloride?
Cardiovascular Disease
Cevimeline can potentially alter cardiac conduction and/or heart rate. Patients with significant cardiovascular disease may potentially be unable to compensate for transient changes in hemodynamics or rhythm induced by cevimeline. Cevimeline should be used with caution and under close medical supervision in patients with a history of cardiovascular disease evidenced by angina pectoris or myocardial infarction.
Pulmonary Disease
Cevimeline can potentially increase airway resistance, bronchial smooth muscle tone, and bronchial secretions. Cevimeline should be administered with caution and with close medical supervision to patients with controlled asthma, chronic bronchitis, or chronic obstructive pulmonary disease.
Ocular
Ophthalmic formulations of muscarinic agonists have been reported to cause visual blurring which may result in decreased visual acuity, especially at night and in patients with central lens changes, and to cause impairment of depth perception. Caution should be advised while driving at night or performing hazardous activities in reduced lighting.
What are the precautions of Cevimeline Hydrochloride?
General
Cevimeline toxicity is characterized by an exaggeration of its parasympathomimetic effects. These may include: headache, visual disturbance, lacrimation, sweating, respiratory distress, gastrointestinal spasm, nausea, vomiting, diarrhea, atrioventricular block, tachycardia, bradycardia, hypotension, hypertension, shock, mental confusion, cardiac arrhythmia, and tremors.
Cevimeline should be administered with caution to patients with a history of nephrolithiasis or cholelithiasis. Contractions of the gallbladder or biliary smooth muscle could precipitate complications such as cholecystitis, cholangitis and biliary obstruction. An increase in the ureteral smooth muscle tone could theoretically precipitate renal colic or ureteral reflux in patients with nephrolithiasis.
Information for Patients
Patients should be informed that cevimeline may cause visual disturbances, especially at night, that could impair their ability to drive safely.
If a patient sweats excessively while taking cevimeline, dehydration may develop. The patient should drink extra water and consult a health care provider.
Drug Interactions
Cevimeline should be administered with caution to patients taking beta adrenergic antagonists, because of the possibility of conduction disturbances. Drugs with parasympathomimetic effects administered concurrently with cevimeline can be expected to have additive effects. Cevimeline might interfere with desirable antimuscarinic effects of drugs used concomitantly.
Drugs which inhibit CYP2D6 and CYP3A3/4 also inhibit the metabolism of cevimeline. Cevimeline should be used with caution in individuals known or suspected to be deficient in CYP2D6 activity, based on previous experience, as they may be at a higher risk of adverse events. In an study, cytochrome P450 isozymes 1A2, 2A6, 2C9, 2C19, 2D6, 2E1, and 3A4 were not inhibited by exposure to cevimeline.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Lifetime carcinogenicity studies were conducted in CD-1 mice and F-344 rats. A statistically significant increase in the incidence of adenocarcinomas of the uterus was observed in female rats that received cevimeline at a dosage of 100 mg/kg/day (approximately 8 times the maximum human exposure based on comparison of AUC data). No other significant differences in tumor incidence were observed in either mice or rats.
Cevimeline exhibited no evidence of mutagenicity or clastogenicity in a battery of assays that included an Ames test, an chromosomal aberration study in mammalian cells, a mouse lymphoma study in L5178Y cells, or a micronucleus assay conducted in ICR mice.
Cevimeline did not adversely affect the reproductive performance or fertility of male Sprague-Dawley rats when administered for 63 days prior to mating and throughout the period of mating at dosages up to 45 mg/kg/day (approximately 5 times the maximum recommended dose for a 60 kg human following normalization of the data on the basis of body surface area estimates). Females that were treated with cevimeline at dosages up to 45 mg/kg/day from 14 days prior to mating through day seven of gestation exhibited a statistically significantly smaller number of implantations than did control animals.
Pregnancy
Pregnancy Category C.
Cevimeline was associated with a reduction in the mean number of implantations when given to pregnant Sprague-Dawley rats from 14 days prior to mating through day seven of gestation at a dosage of 45 mg/kg/day (approximately 5 times the maximum recommended dose for a 60 kg human when compared on the basis of body surface area estimates). This effect may have been secondary to maternal toxicity. There are no adequate and well-controlled studies in pregnant women. Cevimeline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers
It is not known whether this drug is secreted in human milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants from cevimeline, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established.
Geriatric Use
Although clinical studies of cevimeline included subjects over the age of 65, the numbers were not sufficient to determine whether they respond differently from younger subjects. Special care should be exercised when cevimeline treatment is initiated in an elderly patient, considering the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy in the elderly.
What are the side effects of Cevimeline Hydrochloride?
Cevimeline was administered to 1777 patients during clinical trials worldwide, including Sjögren’s patients and patients with other conditions. In placebo-controlled Sjögren’s studies in the U.S., 320 patients received cevimeline doses ranging from 15 mg tid to 60 mg tid, of whom 93% were women and 7% were men. Demographic distribution was 90% Caucasian, 5% Hispanic, 3% Black and 2% of other origin. In these studies, 14.6% of patients discontinued treatment with cevimeline due to adverse events.
The following adverse events associated with muscarinic agonism were observed in the clinical trials of cevimeline in Sjögren’s syndrome patients:
In addition, the following adverse events (≥3% incidence) were reported in the Sjögren’s clinical trials:
The following events were reported in Sjögren’s patients at incidences of <3% and ≥1%: constipation, tremor, abnormal vision, hypertonia, peripheral edema, chest pain, myalgia, fever, anorexia, eye pain, earache, dry mouth, vertigo, salivary gland pain, pruritus, influenza-like symptoms, eye infection, post-operative pain, vaginitis, skin disorder, depression, hiccup, hyporeflexia, infection, fungal infection, sialoadenitis, otitis media, erythematous rash, pneumonia, edema, salivary gland enlargement, allergy, gastroesophageal reflux, eye abnormality, migraine, tooth disorder, epistaxis, flatulence, toothache, ulcerative stomatitis, anemia, hypoesthesia, cystitis, leg cramps, abscess, eructation, moniliasis, palpitation, increased amylase, xerophthalmia, allergic reaction.
The following events were reported rarely in treated Sjögren’s patients (<1%): Causal relation is unknown:
Body as a Whole Disorders:
Cardiovascular Disorders:
Digestive Disorders:
Endocrine Disorders:
Hematologic Disorders:
Liver and Biliary System Disorders:
Metabolic and Nutritional Disorders:
Musculoskeletal Disorders:
Neoplasms:
Nervous Disorders:
Miscellaneous Disorders:
Resistance Mechanism Disorders:
Respiratory Disorders:
Rheumatologic Disorders:
Skin and Appendages Disorders:
Special Senses Disorders:
Urogenital Disorders:
In one subject with lupus erythematosus receiving concomitant multiple drug therapy, a highly elevated ALT level was noted after the fourth week of cevimeline therapy. In two other subjects receiving cevimeline in the clinical trials, very high AST levels were noted. The significance of these findings is unknown.
Additional adverse events (relationship unknown) which occurred in other clinical studies (patient population different from Sjögren’s patients) are as follows: cholinergic syndrome, blood pressure fluctuation, cardiomegaly, postural hypotension, aphasia, convulsions, abnormal gait, hyperesthesia, paralysis, abnormal sexual function, enlarged abdomen, change in bowel habits, gum hyperplasia, intestinal obstruction, bundle branch block, increased creatine phosphokinase, electrolyte abnormality, glycosuria, gout, hyperkalemia, hyperproteinemia, increased lactic dehydrogenase (LDH), increased alkaline phosphatase, failure to thrive, abnormal platelets, aggressive reaction, amnesia, apathy, delirium, delusion, dementia, illusion, impotence, neurosis, paranoid reaction, personality disorder, hyperhemoglobinemia, apnea, atelectasis, yawning, oliguria, urinary retention, distended vein, lymphocytosis.
The following adverse reaction has been identified during post-approval use of cevimeline. Because post-marketing adverse reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
| Adverse Event | Cevimeline 30 mg | Placebo |
| Excessive Sweating | 18.7% | 2.4% |
| Nausea | 13.8% | 7.9% |
| Rhinitis | 11.2% | 5.4% |
| Diarrhea | 10.3% | 10.3% |
| Excessive Salivation | 2.2% | 0.6% |
| Urinary Frequency | 0.9% | 1.8% |
| Asthenia | 0.5% | 0% |
| Flushing | 0.3% | 0.6% |
| Polyuria | 0.1% | 0.6% |
| Adverse Event | Cevimeline 30 mg | Placebo |
| Headache | 14.4% | 20.1% |
| Sinusitis | 12.3% | 10.9% |
| Upper Respiratory Tract Infection | 11.4% | 9.1% |
| Dyspepsia | 7.8% | 8.5% |
| Abdominal Pain | 7.6% | 6.7% |
| Urinary Tract Infection | 6.1% | 3% |
| Coughing | 6.1% | 3% |
| Pharyngitis | 5.2% | 5.4% |
| Vomiting | 4.6% | 2.4% |
| Injury | 4.5% | 2.4% |
| Back Pain | 4.5% | 4.2% |
| Rash | 4.3% | 6% |
| Conjunctivitis | 4.3% | 3.6% |
| Dizziness | 4.1% | 7.3% |
| Bronchitis | 4.1% | 1.2% |
| Arthralgia | 3.7% | 1.8% |
| Surgical Intervention | 3.3% | 3% |
| Fatigue | 3.3% | 1.2% |
| Pain | 3.3% | 3.0% |
| Skeletal Pain | 2.8% | 1.8% |
| Insomnia | 2.4% | 1.2% |
| Hot Flushes | 2.4% | 0% |
| Rigors | 1.3% | 1.2% |
| Anxiety | 1.3% | 1.2% |
Post-Marketing Adverse Events
Liver and Biliary System Disorders:
Array
What should I look out for while using Cevimeline Hydrochloride?
Cevimeline hydrochloride is contraindicated in patients with uncontrolled asthma, known hypersensitivity to cevimeline, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle-closure) glaucoma.
What might happen if I take too much Cevimeline Hydrochloride?
Sorry No Records found
How should I store and handle Cevimeline Hydrochloride?
Cevimeline Hydrochloride Capsules30 mg capsules is supplied as a white opaque cap and white opaque body with “54 190” printed on the cap and body, containing a white powder. NDC 0054-0334-25: Bottle of 100 CapsulesCevimeline Hydrochloride Capsules30 mg capsules is supplied as a white opaque cap and white opaque body with “54 190” printed on the cap and body, containing a white powder. NDC 0054-0334-25: Bottle of 100 CapsulesCevimeline Hydrochloride Capsules30 mg capsules is supplied as a white opaque cap and white opaque body with “54 190” printed on the cap and body, containing a white powder. NDC 0054-0334-25: Bottle of 100 Capsules
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Non-Clinical Toxicology
Cevimeline hydrochloride is contraindicated in patients with uncontrolled asthma, known hypersensitivity to cevimeline, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle-closure) glaucoma.Clonidine may potentiate the CNS-depressive effects of alcohol, barbiturates or other sedating drugs. If a patient receiving clonidine hydrochloride is also taking tricyclic antidepressants, the hypotensive effect of clonidine may be reduced, necessitating an increase in the clonidine dose. If a patient receiving clonidine is also taking neuroleptics, orthostatic regulation disturbances (e.g., orthostatic hypotension, dizziness, fatigue) may be induced or exacerbated.
Monitor heart rate in patients receiving clonidine concomitantly with agents known to affect sinus node function or AV nodal conduction, , digitalis, calcium channel blockers and beta-blockers. Sinus bradycardia resulting in hospitalization and pacemaker insertion has been reported in association with the use of clonidine concomitantly with diltiazem or verapamil.
Amitriptyline in combination with clonidine enhances the manifestation of corneal lesions in rats (see ).
Based on observations in patients in a state of alcoholic delirium it has been suggested that high intravenous doses of clonidine may increase the arrhythmogenic potential (QT- prolongation, ventricular fibrillation) of high intravenous doses of haloperidol. Causal relationship and relevance for clonidine oral tablets have not been established.
Cevimeline toxicity is characterized by an exaggeration of its parasympathomimetic effects. These may include: headache, visual disturbance, lacrimation, sweating, respiratory distress, gastrointestinal spasm, nausea, vomiting, diarrhea, atrioventricular block, tachycardia, bradycardia, hypotension, hypertension, shock, mental confusion, cardiac arrhythmia, and tremors.
Cevimeline should be administered with caution to patients with a history of nephrolithiasis or cholelithiasis. Contractions of the gallbladder or biliary smooth muscle could precipitate complications such as cholecystitis, cholangitis and biliary obstruction. An increase in the ureteral smooth muscle tone could theoretically precipitate renal colic or ureteral reflux in patients with nephrolithiasis.
Cevimeline was administered to 1777 patients during clinical trials worldwide, including Sjögren’s patients and patients with other conditions. In placebo-controlled Sjögren’s studies in the U.S., 320 patients received cevimeline doses ranging from 15 mg tid to 60 mg tid, of whom 93% were women and 7% were men. Demographic distribution was 90% Caucasian, 5% Hispanic, 3% Black and 2% of other origin. In these studies, 14.6% of patients discontinued treatment with cevimeline due to adverse events.
The following adverse events associated with muscarinic agonism were observed in the clinical trials of cevimeline in Sjögren’s syndrome patients:
In addition, the following adverse events (≥3% incidence) were reported in the Sjögren’s clinical trials:
The following events were reported in Sjögren’s patients at incidences of <3% and ≥1%: constipation, tremor, abnormal vision, hypertonia, peripheral edema, chest pain, myalgia, fever, anorexia, eye pain, earache, dry mouth, vertigo, salivary gland pain, pruritus, influenza-like symptoms, eye infection, post-operative pain, vaginitis, skin disorder, depression, hiccup, hyporeflexia, infection, fungal infection, sialoadenitis, otitis media, erythematous rash, pneumonia, edema, salivary gland enlargement, allergy, gastroesophageal reflux, eye abnormality, migraine, tooth disorder, epistaxis, flatulence, toothache, ulcerative stomatitis, anemia, hypoesthesia, cystitis, leg cramps, abscess, eructation, moniliasis, palpitation, increased amylase, xerophthalmia, allergic reaction.
The following events were reported rarely in treated Sjögren’s patients (<1%): Causal relation is unknown:
Body as a Whole Disorders:
Cardiovascular Disorders:
Digestive Disorders:
Endocrine Disorders:
Hematologic Disorders:
Liver and Biliary System Disorders:
Metabolic and Nutritional Disorders:
Musculoskeletal Disorders:
Neoplasms:
Nervous Disorders:
Miscellaneous Disorders:
Resistance Mechanism Disorders:
Respiratory Disorders:
Rheumatologic Disorders:
Skin and Appendages Disorders:
Special Senses Disorders:
Urogenital Disorders:
In one subject with lupus erythematosus receiving concomitant multiple drug therapy, a highly elevated ALT level was noted after the fourth week of cevimeline therapy. In two other subjects receiving cevimeline in the clinical trials, very high AST levels were noted. The significance of these findings is unknown.
Additional adverse events (relationship unknown) which occurred in other clinical studies (patient population different from Sjögren’s patients) are as follows: cholinergic syndrome, blood pressure fluctuation, cardiomegaly, postural hypotension, aphasia, convulsions, abnormal gait, hyperesthesia, paralysis, abnormal sexual function, enlarged abdomen, change in bowel habits, gum hyperplasia, intestinal obstruction, bundle branch block, increased creatine phosphokinase, electrolyte abnormality, glycosuria, gout, hyperkalemia, hyperproteinemia, increased lactic dehydrogenase (LDH), increased alkaline phosphatase, failure to thrive, abnormal platelets, aggressive reaction, amnesia, apathy, delirium, delusion, dementia, illusion, impotence, neurosis, paranoid reaction, personality disorder, hyperhemoglobinemia, apnea, atelectasis, yawning, oliguria, urinary retention, distended vein, lymphocytosis.
The following adverse reaction has been identified during post-approval use of cevimeline. Because post-marketing adverse reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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