Oxybutynin chloride 5 MG Oral Tablet
WARNINGS
Angioedema of the face, lips, tongue and/or larynx has been reported with oxybutynin.
In some cases, angioedema occurred after the first dose.
Angioedema associated with upper airway swelling may be life-threatening.
If involvement of the tongue, hypopharynx, or larynx occurs, oxybutynin should be promptly discontinued and appropriate therapy and/or measures necessary to ensure a patent airway should be promptly provided.
DRUG INTERACTIONS
Drug Interactions The concomitant use of oxybutynin with other anticholinergic drugs or with other agents which produce dry mouth, constipation, somnolence (drowsiness), and/or other anticholinergic-like effects may increase the frequency and/or severity of such effects.
Anticholinergic agents may potentially alter the absorption of some concomitantly administered drugs due to anticholinergic effects on gastrointestinal motility.
This may be of concern for drugs with a narrow therapeutic index.
Mean oxybutynin chloride plasma concentrations were approximately 3 to 4 fold higher when oxybutynin chloride was administered with ketoconazole, a potent CYP3A4 inhibitor.
Other inhibitors of the cytochrome P450 3A4 enzyme system, such as antimycotic agents (e.g., itraconazole and miconazole) or macrolide antibiotics (e.g., erythromycin and clarithromycin), may alter oxybutynin mean pharmacokinetic parameters (i.e., Cmax and AUC).
The clinical relevance of such potential interactions is not known.
Caution should be used when such drugs are co-administered.
OVERDOSAGE
Treatment should be symptomatic and supportive.
Activated charcoal as well as a cathartic may be administered.
Overdosage with oxybutynin chloride has been associated with anticholinergic effects including central nervous system excitation (e.g., restlessness, tremor, irritability, convulsions, delirium, hallucinations), flushing, fever, dehydration, cardiac arrhythmia, vomiting, and urinary retention.
Other symptoms may include hypotension or hypertension, respiratory failure, paralysis, and coma.
Ingestion of 100 mg oxybutynin chloride in association with alcohol has been reported in a 13 year old boy who experienced memory loss, and a 34 year old woman who developed stupor, followed by disorientation and agitation on awakening, dilated pupils, dry skin, cardiac arrhythmia, and retention of urine.
Both patients fully recovered with symptomatic treatment.
DESCRIPTION
Each scored oxybutynin chloride tablet contains 5 mg of oxybutynin chloride.
Chemically, oxybutynin chloride is d,l (racemic) 4-diethylamino-2-butynyl phenylcyclohexylglycolate hydrochloride.
The empirical formula of oxybutynin chloride is C22H31NO3•HCl.
The structural formula appears below: Oxybutynin chloride is a white crystalline solid with a molecular weight of 393.95.
It is readily soluble in water and acids, but relatively insoluble in alkalis.
This is an image of the structural formula for Oxybutynin Chloride.
Oxybutynin Chloride Tablets also contain: FD&C Blue #1 aluminum lake, magnesium stearate, microcrystalline cellulose, and pregelatinized starch.
Oxybutynin Chloride Tablets are for oral administration.
Therapeutic Category: Antispasmodic, anticholinergic.
CLINICAL STUDIES
Oxybutynin chloride was well tolerated in patients administered the drug in controlled studies of 30 days’ duration and in uncontrolled studies in which some of the patients received the drug for 2 years.
HOW SUPPLIED
Product: 76237-216
GERIATRIC USE
Geriatric Use Clinical studies of oxybutynin chloride did not include sufficient numbers of subjects age 65 and over to determine whether they respond differently from younger patients.
Other reported clinical experience has not identified differences in responses between healthy elderly and younger patients; however, a lower initial starting dose of 2.5 mg given 2 or 3 times a day has been recommended for the frail elderly due to a prolongation of the elimination half-life from 2 to 3 hours to 5 hours.2,3,4 In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
INDICATIONS AND USAGE
Oxybutynin chloride tablets are indicated for the relief of symptoms of bladder instability associated with voiding in patients with uninhibited neurogenic or reflex neurogenic bladder (i.e., urgency, frequency, urinary leakage, urge incontinence, dysuria).
PEDIATRIC USE
Pediatric Use The safety and efficacy of oxybutynin chloride administration have been demonstrated for pediatric patients 5 years of age and older (see DOSAGE AND ADMINISTRATION ).
The safety and efficacy of oxybutynin chloride tablets were studied in 30 children in a 24-week, open-label trial.
Patients were aged 5 to 15 years, all had symptoms of detrusor overactivity in association with a neurological condition (e.g., spina bifida), all used clean intermittent catheterization, and all were current users of oxybutynin chloride.
Study results demonstrated that the administration of oxybutynin chloride was associated with improvement in clinical and urodynamic parameters.
At total daily doses ranging from 5 mg to 15 mg, treatment with oxybutynin chloride tablets was associated with an increase from baseline in mean urine volume per catheterization from 122 mL to 145 mL, an increase from baseline in mean urine volume after morning awakening from 148 mL to 168 mL, and an increase from baseline in the mean percentage of catheterizations without a leaking episode from 43% to 61%.
Urodynamic results in these patients were consistent with the clinical results.
Treatment with oxybutynin chloride tablets was associated with an increase from baseline in maximum cystometric capacity from 230 mL to 279 mL, a decrease from baseline in mean detrusor pressure at maximum cystometric capacity from 36 cm H2O to 33 cm H2O, and a reduction in the percentage of patients demonstrating uninhibited detrusor contractions (of at least 15 cm H2O) from 39% to 20%.
As there is insufficient clinical data for pediatric populations under age 5, oxybutynin chloride is not recommended for this age group.
PREGNANCY
Pregnancy Category B.
Reproduction studies using oxybutynin chloride in the hamster, rabbit, rat, and mouse have shown no definite evidence of impaired fertility or harm to the animal fetus.
The safety of oxybutynin chloride administered to women who are or who may become pregnant has not been established.
Therefore, oxybutynin chloride should not be given to pregnant women unless, in the judgment of the physician, the probable clinical benefits outweigh the possible hazards.
NUSRING MOTHERS
Nursing Mothers It is not known whether this drug is excreted in human milk.
Because many drugs are excreted in human milk, caution should be exercised when oxybutynin chloride is administered to a nursing woman.
INFORMATION FOR PATIENTS
Information for Patients Patients should be informed that oxybutynin may produce angioedema that could result in life-threatening airway obstruction.
Patients should be advised to promptly discontinue oxybutynin therapy and seek immediate medical attention if they experience edema of the tongue, edema of the laryngopharynx, or difficulty breathing.
Patients should be informed that heat prostration (fever and heat stroke due to decreased sweating) can occur when anticholinergics such as oxybutynin chloride are administered in the presence of high environmental temperature.
Because anticholinergic agents such as oxybutynin may produce drowsiness (somnolence), or blurred vision, patients should be advised to exercise caution.
Patients should be informed that alcohol may enhance the drowsiness caused by anticholinergic agents such as oxybutynin.
INACTIVE INGREDIENTS
Oxybutynin Chloride Tablets also contain: FD&C Blue #1 aluminum lake, magnesium stearate, microcrystalline cellulose, and pregelatinized starch.
DOSAGE AND ADMINISTRATION
Adults The usual dose is one 5-mg tablet two to three times a day.
The maximum recommended dose is one 5-mg tablet four times a day.
A lower starting dose of 2.5 mg two or three times a day is recommended for the frail elderly.
Pediatric patients over 5 years of age The usual dose is one 5-mg tablet two times a day.
The maximum recommended dose is one 5-mg tablet three times a day.