Glycopyrrolate

ADVERSE REACTIONS Anticholinergics produce certain effects, most of which are extensions of their fundamental pharmacological actions. Adverse reactions to anticholinergics in general may include xerostomia; decreased sweating; urinary hesitancy and retention; blurred vision; tachycardia; palpitations; dilation of the pupil; cycloplegia; increased ocular tension; loss of taste; headaches; nervousness; mental confusion; drowsiness; weakness; dizziness; insomnia; nausea; vomiting; constipation; bloated feeling; impotence; suppression of lactation; severe allergic reaction or drug idiosyncrasies including anaphylaxis, urticaria and other dermal manifestations. Glycopyrrolate Tablets, USP is chemically a quaternary ammonium compound; hence, its passage across lipid membranes, such as the blood-brain barrier, is limited in contrast to atropine sulfate and scopolamine hydrobromide. For this reason the occurrence of CNS related side effects is lower, in comparison to their incidence following administration of anticholinergics which are chemically tertiary amines that can cross this barrier readily. Call your doctor for medical advice about side effects. To report SUSPECTED ADVERSE REACTIONS, contact LGM Pharma Solutions, LLC at 1-877-288-1495 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. Overdosage The symptoms of overdosage of glycopyrrolate are peripheral in nature rather than central. To guard against further absorption of the drug – use gastric lavage, cathartics, and/or enemas. To combat peripheral anticholinergic effects (residual mydriasis, dry mouth, etc.) - utilize a quaternary ammonium anticholinesterase, such as neostigmine methylsulfate. To combat hypotension - use pressor amines (norepinephrine, metaraminol) i.v.; and supportive care. To combat respiratory depression - administer oxygen; utilize a respiratory stimulant such as Dopram® i.v.; artificial respiration.

CONTRAINDICATIONS Glaucoma; obstructive uropathy (for example, bladder neck obstruction due to prostatic hypertrophy); obstructive disease of the gastrointestinal tract (as in achalasia, pyloroduodenal stenosis, etc.); paralytic ileus; intestinal atony of the elderly or debilitated patient; unstable cardiovascular status in acute hemorrhage; severe ulcerative colitis; toxic megacolon complicating ulcerative colitis; myasthenia gravis. Glycopyrrolate tablets are contraindicated in those patients with a hypersensitivity to glycopyrrolate.

DESCRIPTION Glycopyrrolate Tablets, USP 1.5 mg contains the synthetic anticholinergic, glycopyrrolate. Glycopyrrolate is a quaternary ammonium compound with the following chemical name: 3-[(cyclopentylhydroxyacetyl)oxy]-1, 1-dimethylpyrrolidinium bromide. Each tablet contains: Glycopyrrolate, USP ............................. 1.5 mg Inactive Ingredients: Dibasic Calcium Phosphate, Anhydrous Lactose, Magnesium Stearate, Povidone, Sodium Starch Glycolate. Glycopyrrolate Tablets, USP 1.5 mg contains the synthetic anticholinergic, glycopyrrolate. Glycopyrrolate is a quaternary ammonium compound with the following chemical name: 3-[(cyclopentylhydroxyacetyl)oxy]-1, 1-dimethylpyrrolidinium bromide.

DOSAGE AND ADMINISTRATION The dosage of Glycopyrrolate Tablets, USP should be adjusted to the needs of the individual patient to assure symptomatic control with a minimum of adverse reactions. The presently recommended maximum daily dosage of glycopyrrolate is 8 mg. Glycopyrrolate Tablets, USP 1 mg. The recommended initial dosage of Glycopyrrolate 1 mg tablets for adults is one tablet three times daily (in the morning, early afternoon, and at bedtime). Some patients may require two tablets at bedtime to assure overnight control of symptoms. For maintenance, a dosage of one tablet twice a day is frequently adequate. Glycopyrrolate Tablets, USP 2 mg. The recommended dosage of Glycopyrrolate 2 mg tablets for adults is one tablet two or three times daily at equally spaced intervals. Glycopyrrolate Tablets, USP 1.5 mg. The Glycopyrrolate 1.5 mg tablets may be used to provide intermediate titration doses based on response of the patient. Glycopyrrolate Tablets, USP are not recommended for use in pediatric patients under the age of 12 years.

INDICATIONS AND USAGE For use as adjunctive therapy in the treatment of peptic ulcer.

WARNINGS In the presence of a high environmental temperature, heal prostration (fever and heat stroke due to decreased sweating) can occur with the use of Glycopyrrolate Tablets, USP. Diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. In this instance treatment with this drug would be inappropriate and possibly harmful. Glycopyrrolate Tablets, USP may produce drowsiness or blurred vision. In this event, the patient should be warned not to engage in activities requiring mental alertness such as operating a motor vehicle or other machinery, or performing hazardous work while taking this drug. Theoretically, with overdosage, a curare-like action may occur, i.e., neuro-muscular blockade leading to muscular weakness and possible paralysis.

Overdosage The symptoms of overdosage of glycopyrrolate are peripheral in nature rather than central. To guard against further absorption of the drug – use gastric lavage, cathartics, and/or enemas. To combat peripheral anticholinergic effects (residual mydriasis, dry mouth, etc.) - utilize a quaternary ammonium anticholinesterase, such as neostigmine methylsulfate. To combat hypotension - use pressor amines (norepinephrine, metaraminol) i.v.; and supportive care. To combat respiratory depression - administer oxygen; utilize a respiratory stimulant such as Dopram® i.v.; artificial respiration.

CLINICAL PHARMACOLOGY Glycopyrrolate, like other anticholinergic (antimuscarinic) agents, inhibits the action of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine by lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of smooth muscle, cardiac muscle, the sino-atrial node, the atrioventricular node, exocrine glands, and, to a limited degree, in the autonomic ganglia. Thus, it diminishes the volume and free acidity of gastric secretions and controls excessive pharyngeal, tracheal, and bronchial secretions. Glycopyrrolate antagonizes muscarinic symptoms (e.g., bronchorrhea, bronchospasm, bradycardia, and intestinal hypermotility) induced by cholinergic drugs such as the anticholinesterases. The highly polar quaternary ammonium group of glycopyrrolate limits its passage across lipid membranes, such as the blood-brain barrier, in contrast to atropine sulfate and scopolamine hydrobromide, which are non-polar tertiary amines which penetrate lipid barriers easily.

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Glycopyrrolate Glycopyrrolate GLYCOPYRROLATE GLYCOPYRRONIUM CALCIUM PYROPHOSPHATE ANHYDROUS LACTOSE MAGNESIUM STEARATE POVIDONE, UNSPECIFIED SODIUM STARCH GLYCOLATE TYPE A POTATO WHITE TO OFF-WHITE GP;15 ROUND TABLET; DEBOSSED ON BOTH SIDES

ANDA091522

Glycopyrrolate

Glycopyrrolate

79739-7097

HUMAN PRESCRIPTION DRUG

ORAL

PRINCIPAL DISPLAY PANEL NDC 79739-7097-1 Glycopyrrolate Tablets, USP 1.5 mg WHITE DYE-FREE Each Tablet Contains: Glycopyrrolate, USP ..... 1.5 mg LGM Pharma Rx only 100 Tablets Usual Adult Dosage: Please see package insert for detailed prescribing information. Store and Dispense: Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (58-86°F)[See USP] Dispense in a tight container. Keep this and all medication out of the reach of children. Mfg. by: LGM Pharma Solutions, LLC Irvine, California 92614 7097-PD Rev 01/2023 NDC 79739-7097-1 Glycopyrrolate Tablets, USP 1.5 mg WHITE DYE-FREE Each Tablet Contains: Glycopyrrolate, USP ..... 1.5 mg LGM Pharma Rx only 100 Tablets Usual Adult Dosage: Please see package insert for detailed prescribing information. Store and Dispense: Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (58-86°F)[See USP] Dispense in a tight container. Keep this and all medication out of the reach of children. Mfg. by: LGM Pharma Solutions, LLC Irvine, California 92614 7097-PD Rev 01/2023

GLYCOPYRROLATE TABLETS, USP 1.5 MG PRODUCT OVERVIEW: Glycopyrrolate TABLET

Nursing mothers It is not known whether this drug is excreted in human milk. As a general rule, nursing should not be undertaken while a patient is on a drug since many drugs are excreted in human milk.

Pediatric use Since there is no adequate experience in pediatric patients who have received this drug, safety and efficacy in pediatric patients have not been established.

Pregnancy The safety of this drug during pregnancy has not been established. The use of any drug during pregnancy requires that the potential benefits of the drug be weighed against possible hazards to mother and child. Reproduction studies in rats revealed no teratogenic effects from glycopyrrolate; however, the potent anticholinergic action of this agent resulted in diminished rates of conception and of survival at weaning, in a dose-related manner. Other studies in dogs suggest that this may be due to diminished seminal secretion which is evident at high doses of glycopyrrolate. Information on possible adverse effects in the pregnant female is limited to uncontrolled data derived from marketing experience. Such experience has revealed no reports of teratogenic or other fetus-damaging potential. No controlled studies to establish the safety of the drug in pregnancy have been performed.

HOW SUPPLIED Glycopyrrolate Tablets, USP 1.5 mg are compressed white tablets debossed GP on one side and 1.5 on the other and are supplied in bottles of 100 (NDC 79739-7097-1). Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container, as defined in USP, using a child-resistant closure. KEEP OUT OF THE REACH OF CHILDREN. Rx only Manufactured by: LGM Pharma Solutions, LLC Irvine, CA 92614 7097-PD Rev 01/2023

PRECAUTIONS Use Glycopyrrolate Tablets, USP with caution in the elderly and in all patients with: Autonomic neuropathy. Hepatic or renal disease. Ulcerative colitis - large doses may suppress intestinal motility to the point of producing a paralytic ileus and for this reason may precipitate or aggravate the "toxic megacolon," a serious complication of the disease. Hyperthyroidism, coronary heart disease, congestive heart failure, cardiac tachyarrhythmias, tachycardia, hypertension and prostatic hypertrophy. Hiatal hernia associated with reflux esophagitis, since anticholinergic drugs may aggravate this condition. Interactions There are no known drug interactions. Pregnancy The safety of this drug during pregnancy has not been established. The use of any drug during pregnancy requires that the potential benefits of the drug be weighed against possible hazards to mother and child. Reproduction studies in rats revealed no teratogenic effects from glycopyrrolate; however, the potent anticholinergic action of this agent resulted in diminished rates of conception and of survival at weaning, in a dose-related manner. Other studies in dogs suggest that this may be due to diminished seminal secretion which is evident at high doses of glycopyrrolate. Information on possible adverse effects in the pregnant female is limited to uncontrolled data derived from marketing experience. Such experience has revealed no reports of teratogenic or other fetus-damaging potential. No controlled studies to establish the safety of the drug in pregnancy have been performed. Nursing mothers It is not known whether this drug is excreted in human milk. As a general rule, nursing should not be undertaken while a patient is on a drug since many drugs are excreted in human milk. Pediatric use Since there is no adequate experience in pediatric patients who have received this drug, safety and efficacy in pediatric patients have not been established.