Gelnique Information
Gelnique (Oxybutynin) Indications And Usage
Gelnique (Oxybutynin) is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency [ )].
Gelnique (Oxybutynin) Dosage And Administration
The contents of one sachet of Gelnique (Oxybutynin) should be applied once daily to dry, intact skin on the abdomen, upper arms/shoulders, or thighs. Application sites should be rotated. Application of Gelnique (Oxybutynin) should not be made to the same site on consecutive days .
Gelnique (Oxybutynin) is for topical application only and should not be ingested.
Gelnique (Oxybutynin) Dosage Forms And Strengths
Gelnique (Oxybutynin) Contraindications
The use of Gelnique (Oxybutynin) is contraindicated in the following conditions:
Gelnique (Oxybutynin) Warnings And Precautions
Administer Gelnique (Oxybutynin) with caution to patients with gastrointestinal obstructive disorders because of the risk of gastric retention.
Gelnique (Oxybutynin) , like other anticholinergic drugs, may decrease gastrointestinal motility and should be used with caution in patients with conditions such as ulcerative colitis or intestinal atony. Gelnique (Oxybutynin) should be used with caution in patients who have gastroesophageal reflux and/or who are concurrently taking drugs (such as bisphosphonates) that can cause or exacerbate esophagitis.
Angioedema requiring hospitalization and emergency medical treatment has occurred with the first or subsequent doses of oral oxybutynin. In the event of angioedema, oxybutynin-containing product should be discontinued and appropriate therapy promptly provided.
Gelnique (Oxybutynin) Adverse Reactions
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trial of another drug and may not reflect the rates observed in practice.
Gelnique (Oxybutynin) Drug Interactions
No specific drug-drug interaction studies have been performed with Gelnique (Oxybutynin) .
Gelnique (Oxybutynin) Use In Specific Populations
Pregnancy Category B
There are no adequate and well-controlled studies of topical or oral oxybutynin use in pregnant women. Subcutaneous administration to rats at doses up to 25 mg/kg (approximately 50 times the human exposure based on surface area) and to rabbits at doses up to 0.4 mg/kg (approximately 1 times the human exposure) revealed no evidence of harm to the fetus due to oxybutynin chloride. The safety of Gelnique (Oxybutynin) administration to women who are or who may become pregnant has not been established. Therefore, Gelnique (Oxybutynin) should not be given to pregnant women unless, in the judgment of the physician, the probable clinical benefits outweigh the possible hazards.
Gelnique (Oxybutynin) Overdosage
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 100 mg oxybutynin chloride in association with alcohol has been reported in a 13-year-old boy who experienced memory loss, and in 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 recovered fully with symptomatic treatment.
Plasma concentrations of oxybutynin begin to decline 24 hours after Gelnique (Oxybutynin) application. If overexposure occurs, monitor patients until symptoms resolve.
Gelnique (Oxybutynin) Description
Oxybutynin is an antispasmodic, antimuscarinic agent. Gelnique (Oxybutynin) (oxybutynin chloride) is a clear and colorless hydroalcoholic gel containing 100 mg oxybutynin chloride per gram of gel. Gelnique (Oxybutynin) is available in a 1 gram (1.14 mL) unit dose. Each dose contains 100 mg oxybutynin chloride. Oxybutynin is delivered as a racemate of R- and S- isomers. Chemically, oxybutynin chloride is d, l (racemic) 4-(Diethylamino)-2-butynyl (±)-α-phenylcyclohexaneglycolate hydrochloride.
The empirical formula of oxybutynin is CHNO HCl. Its structural formula is:
Oxybutynin chloride is a white powder with a molecular weight of 393.95.
Inactive ingredients in Gelnique (Oxybutynin) are alcohol, USP; glycerin, USP; hydroxypropyl cellulose, NF; sodium hydroxide, NF; and purified water, USP.
Gelnique (Oxybutynin) Clinical Pharmacology
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. Absorption of oxybutynin is similar when Gelnique (Oxybutynin) is applied to the abdomen, upper arm/shoulders or thighs. 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 4.7, 5.2, and 5.5 ng/mL for the abdomen, upper arm/shoulder and thigh application sites, respectively (Table 2).
Oxybutynin is widely distributed in body tissues following systemic absorption. The volume of distribution was estimated to be 193 L after intravenous administration of 5 mg oxybutynin chloride.
Oxybutynin is metabolized primarily by the cytochrome P450 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. The AUC ratio of N-desethyloxybutynin metabolite to parent compound following multiple transdermal applications is approximately 1:1 for Gelnique (Oxybutynin) .
Following intravenous administration, the elimination half-life of oxybutynin is approximately 2 hours. After the final steady-state dose of Gelnique (Oxybutynin) , 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 0.1% of the administered dose excreted unchanged in the urine. Less than 0.1% of the administered dose is excreted as the metabolite N-desethyloxybutynin.
The potential for dermal transfer of oxybutynin from a treated person to an untreated person was evaluated in a single-dose study where subjects dosed with Gelnique (Oxybutynin) engaged in vigorous contact with an untreated partner for 15 minutes, either with (N = 14 couples) or without (N = 12 couples) clothing covering the application area. The untreated partners not protected by clothing demonstrated detectable plasma concentrations of oxybutynin (mean C = 0.94 ng/mL). Two of the 14 untreated subjects participating in the clothing-to-skin contact regimen had measurable oxybutynin plasma concentrations (C ≤ 0.1 ng/mL) during the 48 hours following contact with treated subjects; oxybutynin was not detectable with the remaining 12 untreated subjects.
The effect of sunscreen on the absorption of oxybutynin when applied 30 minutes before or 30 minutes after Gelnique (Oxybutynin) application was evaluated in a single-dose randomized crossover study (N = 16). Concomitant application of sunscreen, either before or after Gelnique (Oxybutynin) application, had no effect on the systemic exposure of oxybutynin.
The effect of showering on the absorption of oxybutynin was evaluated in a randomized, steady-state crossover study under conditions of no shower, or showering 1, 2 or 6 hours after Gelnique (Oxybutynin) application (N = 20). The results of the study indicate that showering after one hour does not affect the overall systemic exposure to oxybutynin.
The effect of race on the pharmacokinetics of Gelnique (Oxybutynin) has not been studied.
Specific Populations:
Gelnique (Oxybutynin) Clinical Studies
The efficacy of Gelnique (Oxybutynin) was evaluated in a single randomized, double-blind, placebo-controlled, parallel group 12-week study for the treatment of overactive bladder with symptoms of urge incontinence, urgency and frequency. Key entry criteria included adults with symptomatic overactive bladder with an average of ≥ 4 incontinence episodes in a 3-day period and at least 8 micturitions per day. Patients were randomized to daily applications of Gelnique (Oxybutynin) 1 gram or matching placebo gel. A total of 389 patients received Gelnique (Oxybutynin) and 400 patients received placebo gel. The majority of patients were Caucasian (86.3%) and female (89.2%), with a mean age of 59.4 years (range: 18 to 88 years). The average duration of urinary incontinence was approximately 8.5 years and approximately 75% of patients had no prior pharmacological treatment for urinary incontinence.
Patients treated with Gelnique (Oxybutynin) experienced a statistically significant decrease in the number of urinary incontinence episodes per day from baseline to endpoint compared with placebo (p
Mean and median change from baseline in daily incontinence episodes (primary endpoint), urinary frequency, and urinary void volume (secondary endpoints) between placebo and Gelnique (Oxybutynin) are summarized in Table 3.
Gelnique (Oxybutynin) How Supplied/storage And Handling
Unit Dose: Heat-sealed sachet containing 1 gram (1.14 mL) of Gelnique (Oxybutynin) gel for topical use.
Carton of 30 Sachets ()
Store at 20-25°C (68-77°F). [See USP controlled room temperature.] Protect from moisture and humidity. Apply immediately after the sachets are opened and contents expelled. Discard used sachets in household trash in a manner that prevents accidental application or ingestion by children, pets, or others.
Gelnique (Oxybutynin) Patient Counseling Information
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Gelnique (Oxybutynin) is for topical application only and should not be ingested.
Gelnique (Oxybutynin) should not be applied to recently shaved skin surfaces. 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.
Alcohol based gels are flammable. Avoid open fire or smoking until the gel has dried.
Gelnique (Oxybutynin)
Gelnique (Oxybutynin) Principal Display Panel
Gelnique (Oxybutynin) (oxybutynin chloride) Gel, 10%Carton 30 SachetsNDC 52544-084-30
