Wash hands after application. Bladder outflow obstruction. GI obstruction. Decreased GI motility. Ulcerative colitis. Intestinal antony. Gastroesophageal reflux. Controlled narrow angle glaucoma. Discontinue if skin hypersensitivity or angioedema develops. Monitor for anticholinergic CNS effects; consider discontinuing if occur. Avoid in myasthenia gravis; discontinue if symptoms occur. Hepatic or renal dysfunction. Minimize skin transference: cover application site with clothing if direct contact is anticipated.
The most common adverse reactions reported during the week open-label extension study were application site reactions 6. The most common reason for premature discontinuation was application site reactions 9 patients or 4.
Two of these 9 patients experienced application site reactions of severe intensity dermatitis, urticaria, and erythema. Because these 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.
Nervous System Disorders: Memory impairment, dizziness, somnolence, confusion Psychiatric Disorders: Delirium, hallucinations. Pharmacokinetic studies have not been performed with patients concomitantly receiving cytochrome P enzyme inhibitors, such as antimycotic agents e.
There are no studies with topical or oral oxybutynin use in pregnant women to inform any drug-associated risks of adverse development outcomes. No adverse developmental outcomes were observed in animal reproduction studies when oxybutynin chloride was administered to pregnant rats and rabbits during organogenesis at approximately 50 and 1 times, respectively, the maximum human dose based on body surface area see Data.
In the general U. There is no information on the presence of oxybutynin or its metabolites in human milk, its effects on milk production or on the breast fed child.
No overall differences in safety or effectiveness were observed between these patients and younger patients, but greater sensitivity of some older individuals cannot be ruled out [see Clinical Pharmacology Overdosage with oxybutynin has been associated with anticholinergic effects including central nervous system excitation, flushing, fever, dehydration, cardiac arrhythmia, vomiting, and urinary retention.
Oral ingestion of mg oxybutynin chloride in association with alcohol has been reported in a year-old boy who experienced memory loss, and in a 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 recovered fully with symptomatic treatment. If overexposure occurs, monitor patients until symptoms resolve. Oxybutynin is an antispasmodic, antimuscarinic agent. Each dose contains mg oxybutynin chloride. Oxybutynin is delivered as a racemate of R- and S- isomers. Its structural formula is:. Oxybutynin acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors, resulting in relaxation of bladder smooth muscle. Oxybutynin is a racemic mixture of R- and S- isomers.
Antimuscarinic activity resides predominantly with the R- isomer. The active metabolite, N-desethyloxybutynin, has pharmacological activity on the human detrusor muscle that is similar to that of oxybutynin in in vitro studies. Oxybutynin is transported across intact skin and into the systemic circulation by passive diffusion across the stratum corneum. Steady-state concentrations are achieved within 7 days of continuous dosing.
Mean plasma concentrations during a randomized, crossover study of the three recommended application sites in 39 healthy men and women are shown in Figure 1. Average steady-state plasma oxybutynin concentrations were 4. Oxybutynin is widely distributed in body tissues following systemic absorption.
The volume of distribution was estimated to be L after intravenous administration of 5 mg oxybutynin chloride. Oxybutynin is metabolized primarily by the cytochrome P enzyme systems, particularly CYP3A4, found mostly in the liver and gut wall. Metabolites include phenylcyclohexylglycolic acid, which is pharmacologically inactive, and N-desethyloxybutynin DEO , which is pharmacologically active. Transdermal administration of oxybutynin bypasses the first-pass gastrointestinal and hepatic metabolism, reducing the formation of the N-desethyloxybutynin metabolite.
Only small amounts of CYP3A4 are found in skin, limiting pre-systemic metabolism during transdermal absorption. Following intravenous administration, the elimination half-life of oxybutynin is approximately 2 hours. After the final steady-state dose of GELNIQUE, oxybutynin and N-desethyloxybutynin demonstrated biphasic elimination with plasma concentrations beginning to decrease 24 hours after dosing.
Elimination was more rapid between 24 and 48 hours after dosing, during which time plasma concentrations of oxybutynin and N-desethyloxybutynin declined by about one-half. This rapid elimination phase was followed by a more prolonged terminal elimination phase. The apparent elimination half-lives including the terminal elimination phase were 64 hours and 82 hours for oxybutynin and DEO, respectively. Oxybutynin is extensively metabolized by the liver, with less than 0.
Less than 0. The results of the study indicate that showering after one hour does not affect the overall systemic exposure to oxybutynin. Geriatric: Available data suggest that there are no significant differences in the pharmacokinetics of oxybutynin based on geriatric status in patients following administration of GELNIQUE [see Use in Specific Populations 8.
Pediatric: The pharmacokinetics of oxybutynin and N-desethyloxybutynin have not been evaluated in individuals younger than 18 years of age [see Use in Specific Populations 8. Gender: Available data suggest that there are no significant differences in the pharmacokinetics of oxybutynin based on gender in healthy volunteers following administration of GELNIQUE.
These doses are approximately 6, 25 and 50 times the maximum exposure in humans taking an oral dose, based on body surface area. Oxybutynin chloride showed no increase of mutagenic activity when tested in Schizosaccharomyces pompholiciformis , Saccharomyces cerevisiae, and Salmonella typhimurium test systems. Reproduction studies with oxybutynin chloride in the mouse, rat, hamster, and rabbit showed no definite evidence of impaired fertility. The efficacy and safety of GELNIQUE were evaluated in a single randomized, double-blind, placebo-controlled, parallel group week study for the treatment of overactive bladder with symptoms of urge incontinence, urgency and frequency.
The majority of patients were Caucasian The average duration of urinary incontinence was approximately 8. Mean and median change from baseline in daily incontinence episodes primary endpoint , urinary frequency, and urinary void volume secondary endpoints between placebo and GELNIQUE are summarized in Table 3. Metered-Dose Pump: Metered-dose pump dispenser capable of delivering 30 metered 1 gram doses.
Unit Dose : Heat-sealed sachet containing 1 gram 1. Apply immediately after the sachets are opened and contents expelled or dose delivered from dispenser. Discard used sachets and empty dispensers in household trash in a manner that prevents accidental application or ingestion by children, pets, or others.
Patients should wash hands immediately after product application. Application sites should not be subject to showering or water immersion for 1 hour after product application.
Application sites should be covered with clothing if close skin-to-skin contact at the application site is anticipated. Patients should be informed that anticholinergic antimuscarinic agents, such as GELNIQUE, may produce clinically significant adverse reactions related to anticholinergic pharmacological activity including:.
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It may harm them.
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