Complete SPL Sections#
DESCRIPTION
DESCRIPTION SECTION
Each scored biconvex, very light to light blue Oxybutynin Chloride Tablet, USP 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 C 22 H 31 NO 3 •HCl. The structural formula appears below: Oxybutynin chloride is a white crystalline solid with a molecular weight of 393.9. It is readily soluble in water and acids, but relatively insoluble in alkalis. Oxybutynin Chloride Tablets, USP also contain FD&C Blue # 1/Brilliant Blue FCF aluminum lake, lactose anhydrous, magnesium stearate, microcrystalline cellulose and sodium starch glycolate. Oxybutynin Chloride Tablets, USP are for oral administration. Therapeutic Category: Antispasmodic, anticholinergic. USP Dissolution Test 2 used.
CLINICAL PHARMACOLOGY
CLINICAL PHARMACOLOGY SECTION
Oxybutynin chloride exerts a direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. Oxybutynin chloride exhibits only one fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the antispasmodic activity. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects). Oxybutynin chloride relaxes bladder smooth muscle. In patients with conditions characterized by involuntary bladder contractions, cystometric studies have demonstrated that oxybutynin chloride increases bladder (vesical) capacity, diminishes the frequency of uninhibited contractions of the detrusor muscle, and delays the initial desire to void. Oxybutynin chloride thus decreases urgency and the frequency of both incontinent episodes and voluntary urination. Antimuscarinic activity resides predominately in the R-isomer. A metabolite, desethyloxybutynin, has pharmacological activity similar to that of oxybutynin in in vitro studies.
CLINICAL STUDIES
CLINICAL STUDIES SECTION
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.
INDICATIONS AND USAGE
INDICATIONS & USAGE SECTION
Oxybutynin chloride is 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).
CONTRAINDICATIONS
CONTRAINDICATIONS SECTION
Oxybutynin chloride is contraindicated in patients with urinary retention, gastric retention and other severe decreased gastrointestinal motility conditions, uncontrolled narrow-angle glaucoma and in patients who are at risk for these conditions. Oxybutynin chloride is also contraindicated in patients who have demonstrated hypersensitivity to the drug substance or other components of the product.
WARNINGS
WARNINGS SECTION
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.
PRECAUTIONS
PRECAUTIONS SECTION
Central Nervous System Effects Oxybutynin is associated with anticholinergic central nervous system (CNS) effects (see ADVERSE REACTIONS ). A variety of CNS anticholinergic effects have been reported, including hallucinations, agitation, confusion and somnolence. Patients should be monitored for signs of anticholinergic CNS effects, particularly in the first few months after beginning treatment or increasing the dose. If a patient experiences anticholinergic CNS effects, dose reduction or drug discontinuation should be considered. Oxybutynin chloride should be used with caution in patients with preexisting dementia treated with cholinesterase inhibitors due to the risk of aggravation of symptoms. Oxybutynin chloride should be used with caution in patients with Parkinson’s disease due to the risk of aggravation of symptoms.
ADVERSE REACTIONS
ADVERSE REACTIONS SECTION
The safety and efficacy of oxybutynin chloride was evaluated in a total of 199 patients in three clinical trials. These participants were treated with oxybutynin chloride 5-20 mg/day for up to 6 weeks. Table 3 shows the incidence of adverse events judged by investigators to be at least possibly related to treatment and reported by at least 5% of patients. Table 3 Incidence (%) of Adverse Events Reported by ≥ 5% of Patients Using oxybutynin chloride (5-20 mg/day) The most common adverse events reported by patients receiving oxybutynin chloride 5-20 mg/day were the expected side effects of anticholinergic agents. The incidence of dry mouth was dose-related. In addition, the following adverse events were reported by 1 to < 5% of patients using oxybutynin chloride (5 to 20 mg/day) in all studies. Infections and Infestations: nasopharyngitis, upper respiratory tract infection, bronchitis, cystitis, fungal infection; Metabolism and Nutrition Disorders: fluid retention; Psychiatric Disorders: confusional state; Nervous System Disorders: dysgeusia, sinus headache; Eye Disorders: keratoconjunctivitis sicca, eye irritation; Cardiac Disorders: palpitations, sinus arrhythmia; Vascular Disorders: flushing; Respiratory, Thoracic and Mediastinal Disorders: nasal dryness, cough, pharyngolaryngeal pain, dry throat, sinus congestion, hoarseness, asthma, nasal congestion; Gastrointestinal Disorders: diarrhea, abdominal pain, loose stools, flatulence, vomiting, abdominal pain upper, dysphagia, aptyalism, eructation, tongue coated; Skin and Subcutaneous Tissue Disorders: dry skin, pruritis; Musculoskeletal and Connective Tissue Disorders: back pain, arthralgia, pain in extremity, flank pain; Renal and Urinary Disorders: dysuria, pollakiuria; General Disorders and Administration Site Conditions: fatigue, edema peripheral, asthenia, pain, thirst, edema; Investigations: blood pressure increased, blood glucose increased, blood pressure decreased; Injury, Poisoning, and Procedural Complications: fall. Postmarketing Surveillance Because postmarketing adverse events 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. The following additional adverse events have been reported from worldwide postmarketing experience with oral oxybutynin chloride: Psychiatric Disorders: psychotic disorder, agitation, hallucination, memory impairment; Nervous System Disorders: convulsions; Eye Disorders: cycloplegia, mydriasis, glaucoma; Cardiac Disorders: tachycardia, QT interval prolongation, chest discomfort; Gastrointestinal Disorders: decreased gastrointestinal motility, frequent bowel movements; Skin and Subcutaneous Tissue Disorders: rash, decreased sweating; Renal and Urinary Disorders: impotence; Reproductive System and Breast Disorders: suppression of lactation; General Disorders and Administration Site Conditions: hypersensitivity reactions, including angioedema with airway obstruction, urticaria, and face edema; rare anaphylactic reactions requiring hospitalization for emergency treatment; Metabolism and Nutrition Disorders: anorexia; Respiratory, Thoracic and Mediastinal Disorders: dysphonia. To report SUSPECTED ADVERSE REACTIONS, contact KVK-Tech, Inc. at 1-215-579-1842 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
OVERDOSAGE
OVERDOSAGE SECTION
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.
DOSAGE AND ADMINISTRATION
DOSAGE & ADMINISTRATION SECTION
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.
HOW SUPPLIED
HOW SUPPLIED SECTION
Oxybutynin Chloride Tablets USP, 5 mg, are very light to light blue, round biconvex tablets, debossed with “A” and “44”, separated by a horizontal score on one side and plain on the other side. The tablets are supplied as follows: Bottles of 30: NDC 43063-931-30 Pharmacist: Dispense in a tight, light-resistant container as defined in the USP. Store at 20°C to 25°C (68°F to 77°F); excursions permitted within 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].
REFERENCES
REFERENCES SECTION
1. Yong C et al. Effect of Food on the Pharmacokinetics of Oxybutynin in normal subjects. Pharm Res . 1991; 8 (Suppl.): S-320. 2. Hughes KM et al. Measurement of oxybutynin and its N -desethyl metabolite in plasma, and its application to pharmacokinetic studies in young, elderly and frail elderly volunteers. Xenobiotica . 1992; 22 (7): 859–869. 3. Ouslander J et al. Pharmacokinetics and Clinical Effects of Oxybutynin in Geriatric Patients. J. Urol . 1988; 140: 47–50. 4. Yarker Y et al. Oxybutynin: A review of its Pharmacodynamic and Pharmacokinetic Properties, and its Therapeutic Use in Detrusor Instability. Drugs & Aging . 1995; 6 (3): 243–262. Manufactured by: KVK-Tech, Inc. 110 Terry Drive Newtown, PA 18940 Manufacturer’s code: 10702 Item ID #: 6288/03 Rev.: 02/2019
PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
Oxybutynin Chloride Tablets, USP 5 mg Rx Only
