GLYCOPYRROLATE- glycopyrrolate tablet
Chartwell RX, LLC
HIGHLIGHTS OF PRESCRIBING INFORMATION
Glycopyrrolate Tablets, USP
These highlights do not include all the information needed to use GLYCOPYRROLATE TABLETS safely and effectively. See full prescribing information for GLYCOPYRROLATE TABLETS. GLYCOPYRROLATE tablets for oral use
Initial U.S. Approval: 1961
INDICATIONS AND USAGE
DOSAGE AND ADMINISTRATION
Important Dosing Information ( 2.1)
Recommended Dosage( 2.2)
DOSAGE FORMS AND STRENGTHS
WARNINGS AND PRECAUTIONS
Adverse reactions include blurred vision, drowsiness, decreased sweating, flushing, vomiting, constipation, dry mouth, tachycardia, and urinary retention. (
USE IN SPECIFIC POPULATIONS
See 17 for PATIENT COUNSELING INFORMATION.
FULL PRESCRIBING INFORMATION: CONTENTS*
7.2 Drugs with Altered Absorption due to Decreased Gastrointestinal Motility and Increased Transit Time
Glycopyrrolate is indicated in adults to reduce symptoms of a peptic ulcer as an adjunct to treatment of peptic ulcer.
Limitations of Use
Glycopyrrolate is not indicated as monotherapy for the treatment of peptic ulcer because effectiveness in peptic ulcer healing has not been established.
Glycopyrrolate tablets are contraindicated in:
Glycopyrrolate may cause increased intraocular pressure in patients with glaucoma and reduce the effects of antiglaucoma agents. Instruct patients to discontinue glycopyrrolate tablets and promptly seek medical care if they experience symptoms of acute angle-closure glaucoma (pain and reddening of the eyes accompanied by dilated pupils) [ see Contraindications (4)].
Glycopyrrolate may worsen intestinal mechanical obstruction, and diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. If partial or complete intestinal obstruction is suspected, discontinue the use of glycopyrrolate tablets and evaluate for potential intestinal obstruction [ see Contraindications (4) ].
Glycopyrrolate reduces gastrointestinal motility and may result in delayed gastric emptying, constipation, and intestinal pseudo-obstruction and may precipitate or aggravate paralytic ileus and toxic megacolon [
see Contraindications (4)
]. The risk of gastrointestinal adverse reactions is further increased with the use of other anticholinergics and other medications that decrease gastrointestinal peristalsis.
Monitor patients for symptoms of decreased gastrointestinal motility. Concomitant use of glycopyrrolate tablets and other anticholinergics or other medications that decrease GI peristalsis is not recommended [ see Drug Interactions (7.2)] .
Glycopyrrolate may produce drowsiness and blurred vision and impair the mental and/or physical abilities required for the performance of hazardous tasks such as driving a motor vehicle, operating machinery, or performing other hazardous work [
see Adverse Reactions (6)
]. Concomitant use of other drugs that have anticholinergic properties may increase these effects [
see Drug Interactions (7.1)].
Inform patients not to operate motor vehicles or other dangerous machinery or perform other hazardous tasks until they are reasonably certain that glycopyrrolate tablets does not affect them adversely.
Discontinue glycopyrrolate tablets if signs or symptoms of cognitive or visual impairment develop.
In the presence of a high environmental temperature, heat prostration resulting in fever and heatstroke can occur with the use of glycopyrrolate tablets due to decreased sweating, particularly in geriatric patients [ see Adverse Reactions (6)]. Advise patients to avoid exposure to hot or very warm environmental temperatures when taking glycopyrrolate tablets. Glycopyrrolate tablets are not recommended in geriatric patients [ see Warnings and Precautions (5.7) ].
Glycopyrrolate tablets are not recommended in patients with other conditions exacerbated by anticholinergic adverse reactions (e.g., autonomic neuropathy, hyperthyroidism, cardiac disease, and hiatal hernia associated with reflux esophagitis) and in patients taking other anticholinergic medications [ see Drug Interactions (7.1)].
Geriatric patients 65 years of age and older are at increased risk of anticholinergic adverse reactions that may lead to complications of urinary retention, bowel obstruction, heat prostration, arrhythmias, delirium, and falls or fractures. Glycopyrrolate tablets are not recommended in geriatric patients and may be contraindicated in some geriatric patients with underlying medical conditions [ see Contraindications (4), Warnings and Precautions (5.2, 5.5), Adverse Reactions (6) and Use in Specific Populations (8.5)].
The following serious or otherwise important adverse reactions are discussed elsewhere in the labeling:
The following adverse reactions associated with the use of glycopyrrolate, or other anticholinergic drugs, were identified in clinical studies or postmarketing reports. Because some of 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.
Cardiac Disorders:chest, pain, hypertension, tachycardia
Endocrine Disorders:decreased sweating
Eye Disorders:blurred vision, cycloplegia, dilatation of the pupil, increased ocular tension
Gastrointestinal Disorders:bloated feeling, constipation, dry mouth, dysgeusia, nausea, vomiting
Immune System Disorders:anaphylaxis [ see Contraindications (4)]
Nervous System Disorders:agitation, dizziness, drowsiness, headache, insomnia, mental confusion, nervousness, weakness
Respiratory Disorders:respiratory depression, throat irritation
Renal and Urinary Disorders:urinary hesitancy, urinary retention
Reproductive System and Breast Disorders:impotence, suppression of lactation
There is potential for an additive interaction between glycopyrrolate and concomitantly used anticholinergic drugs (e.g., tricyclic antidepressants, anti-epileptics, class I antiarrhythmics, anti-spasmodics, amantadine) resulting in increased anticholinergic adverse reactions. Co-administration of antipsychotics with glycopyrrolate may lead to worsening of tardive dyskinesia. Glycopyrrolate tablets are not recommended in patients taking other anticholinergic drugs [ see Warnings and Precautions (5.3, 5.4, 5.6)].
Decreased gastrointestinal motility by glycopyrrolate may impact absorption of other drugs leading to increased or decreased drug exposure. Glycopyrrolate tablets are not recommended in patients taking other drugs that are affected by altered gastrointestinal motility [ see Warnings and Precautions (5.3)].
Oral glycopyrrolate may worsen gastrointestinal mucosal injury reported with solid oral dosage forms of potassium chloride due to decreased gastric motility and increased transit time, leading to prolonged contact with the gastrointestinal mucosa. Glycopyrrolate tablets are not recommended in patients taking solid oral dosage forms of potassium chloride.
Over decades of use, there is an absence of published data on orally administered glycopyrrolate in pregnant women, including an absence of any reports of a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. In animal studies, at non-maternally toxic doses of oral glycopyrrolate, there were no adverse developmental effects in rats or rabbits. A pre- and post-natal development study of oral glycopyrrolate in rats showed a decrease in pup mean bodyweight that recovered post nursing, with no other developmental effects observed ( see Data).
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
At non-maternally toxic doses of oral glycopyrrolate, there were no effects on embryo-fetal development or toxicity in rats or rabbits. A pre- and post-natal development study of oral glycopyrrolate in rats showed a decrease in pup mean bodyweight that recovered post nursing, with no other developmental effects observed.
In a published reproductive and developmental study, male and female rats were administered glycopyrrolate in the diet at 0 mg/kg/day, 32.5 mg/kg/day, 63 mg/kg/day, and 130 mg/kg/day for 3 weeks to 5 weeks and through up to three consecutive litters. There was no indication of abnormalities in the pups of treated dams. There was a decreased rate of conception and in survival rate at weaning for all treated animals in a dose-related manner. Diminished rates of conception may be due to diminished seminal secretion [ see Nonclinical Toxicology (13.1)].
There are no data on the presence of glycopyrrolate in either human or animal milk, the effects on the breastfed infant, or the effects on milk production. As with other anticholinergic drugs, glycopyrrolate may cause suppression of lactation. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for glycopyrrolate tablets and any potential adverse effects on the breastfed infant from glycopyrrolate tablets.
Geriatric patients 65 years of age and older may be more sensitive to the anticholinergic adverse reactions of glycopyrrolate leading to complications of urinary retention, bowel obstruction, heat prostration, arrhythmias, delirium, and falls or fractures; therefore, glycopyrrolate tablets are not recommended in geriatric patients and may be contraindicated in some geriatric patients with underlying medical conditions [ see Contraindications (4)and Warnings and Precautions (5)].
Signs and symptoms of glycopyrrolate overdosage are related to excessive anti-muscarinic anticholinergic activity and are generally peripheral (e.g., flushing, hyperthermia, tachycardia, ileus, urinary retention, loss of ocular accommodation, and light sensitivity due to mydriasis), but central nervous system toxicity (agitation, seizures, hyperthermia) may also occur.
If over-exposure occurs, call the Poison Control Center at 1-800-222-1222 for current information on the management of glycopyrrolate poisoning and overdosage.
Management of glycopyrrolate overdosage is based upon presenting signs and symptoms, including close observation for severe or life-threatening complications which may require respiratory and cardiovascular monitoring and support. Consider administration of activated charcoal and/or use of a reversible anticholinesterase as appropriate or recommended by Poison Control.
Glycopyrrolate tablets contain synthetic anticholinergic glycopyrrolate. Glycopyrrolate is a quaternary ammonium compound with the following chemical name: 3-[(cyclopentyl hydroxyphenylacetyl)oxy]-1,1-dimethylpyrrolidinium bromide. The molecular formula for glycopyrrolate is C 19H 28BrNO 3, the molecular weight is 398.3 g/mol, and the structural formula is:
Each Glycopyrrolate Tablet, USP contains glycopyrrolate, USP 1 mg or 2 mg as the active ingredient. The inactive ingredients are dibasic calcium phosphate, lactose, magnesium stearate, povidone, and sodium starch glycolate.
Glycopyrrolate, an anticholinergic (antimuscarinic) agent, inhibits the action of acetylcholine on parietal cells in the stomach and decreases the volume and acidity of gastric secretions.
Patients with Renal Impairment
In the published literature, glycopyrrolate 4 mcg/kg was administered intravenously (glycopyrrolate tablets are not recommended for intravenous use) in uremic patients undergoing renal transplantation surgery. The mean AUC (10.6 mcg·h/L) and 24-hour urinary excretion (7%) for glycopyrrolate were significantly different from normal healthy adult subjects undergoing general surgery (3.7 mcg·h/L, and 65%, respectively) [ see Use in Specific Populations (8.6)].
Reproduction studies in rats resulted in diminished rates of conception in a dose-related manner. Studies in dogs suggest that diminished rates of conception may be due to diminished seminal secretion, which is evident at high doses of glycopyrrolate.
Glycopyrrolate Tablets, USP, 1 mg are white to off-white, round, flat beveled edge tablet debossed with “MCR 117” separated by a break line on one side and plain on other side. Packaged in bottles of 60 tablets.
Glycopyrrolate Tablets, USP, 2 mg are white to off white, round, flat beveled edge tablet debossed with “AC 108” separated by a break line on one side and plain on other side. Packaged in bottles of 60 tablets.
Store at 20° to 25°C (68° to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Keep out of reach of children.
Dispense in tight container.
Precipitation of Acute Glaucoma
Advise patients to discontinue glycopyrrolate tablets and promptly seek medical care if they experience symptoms of acute angle-closure glaucoma (pain and reddening of the eyes accompanied by dilated pupils) [ see Warnings and Precautions (5.1)].
Partial or Complete Mechanical Intestinal Obstruction
Advise patients to contact their healthcare provider if diarrhea occurs, especially in patients with ileostomy or colostomy [ see Warnings and Precautions (5.2)].
Gastrointestinal Adverse Reactions Due to Decreased Gastrointestinal Motility
Inform patients that glycopyrrolate tablets may cause adverse reactions related to decreased gastrointestinal motility and report to their healthcare provider if they experience symptoms such as vomiting, early satiety, abdominal distention, and constipation [ see Warnings and Precautions (5.3)].
Cognitive and Visual Adverse Reactions
Inform patients that glycopyrrolate tablets may cause cognitive or visual impairment and not operate motor vehicles or other dangerous machinery or perform other hazardous tasks until they are reasonably certain that glycopyrrolate tablets do not affect them adversely. Advise patients to discontinue glycopyrrolate tablets immediately and contact their healthcare provider if symptoms develop (e.g., drowsiness or blurred vision) [ see Warnings and Precautions (5.4)].
Heat Prostration at High Environmental Temperatures
Inform patients that glycopyrrolate tablets can reduce sweating, leading to the possibility of heat exhaustion or heat stroke. Advise patients to avoid exposure to hot or very warm environmental temperatures [ see Warnings and Precautions (5.5)].
Chartwell RX, LLC.
Congers, NY 10920
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