DESCRIPTION

Glycopyrrolate tablets contain the synthetic anticholinergic, glycopyrrolate.  Glycopyrrolate is a quaternary ammonium compound with the following chemical name:
3-[(cyclopentylhydroxyphenylacetyl)oxy]-1, 1-dimethylpyrrolidinium bromide.

The structural formula of Glycopyrrolate is represented below:

Inactive ingredients:
Calcium Phosphate Dibasic, Calcium Stearate, Lactose Anhydrous, Povidone, Sodium Starch Glycolate.

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 but 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.

INDICATIONS AND USAGE

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

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; ulcerative colitis; toxic megacolon complicating ulcerative colitis; myasthenia gravis.  Glycopyrrolate tablets are contraindicated in those patients with a hypersensitivity to glycopyrrolate.

WARNINGS

In the presence of a high environmental temperature, heat prostration (fever and heat stroke due to decreased sweating) can occur with use of glycopyrrolate.

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 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.

PRECAUTIONS

Use Glycopyrrolate 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 “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.

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; dilatation 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 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.

OVERDOSAGE

The symptoms of overdosage of glycopyrrolate are peripheral in nature rather than central.

1. To guard against further absorption of the drug–use gastric lavage, cathartics and/or enemas.
2. To combat peripheral anticholinergic effects (residual mydriasis, dry mouth,etc.)–utilize a quaternary ammonium anticholinesterase, such as neostigmine methylsulfate.
3. To combat hypotension–(norepinephrine, metaraminol) i.v.; and supportive care.
4. To combat respiratory depression–administer oxygen; utilize a respiratory stimulant such as Dopram® i.v.; artificial respiration.

DOSAGE AND ADMINISTRATION

The dosage of glycopyrrolate 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, 1 mg tablets:
The recommended initial dosage of glycopyrrolate 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, 2 mg tablets:
The recommended dosage of glycopyrrolate for adults is one tablet two or three times daily at equally spaced intervals.

Glycopyrrolate tablets are not recommended for use in pediatric patients under the age of 12 years.

DRUG INTERACTIONS

There are no known drug interactions.

HOW SUPPLIED

Glycopyrrolate 1 mg tablets are scored, white, round tablets, embossed “BP” above bisect, “601” below bisect.
Glycopyrrolate, 1 mg tablets in bottles of 100 (NDC 64376-601-01).

Glycopyrrolate, 1 mg tablets in bottles of 30 (NDC 64376-601-31).

Glycopyrrolate 2 mg tablets are scored, white, round tablets, embossed “BP” above bisect, “602” below bisect.
Glycopyrrolate, 2 mg tablets in bottles of 100 (NDC 64376-602-01).

Glycopyrrolate, 2 mg tablets in bottles of 30 (NDC 64376-602-31).

PHARMACIST: Dispense in a tight, light-resistant container with a child-resistant closure.

PACKAGE LABEL.PRINCIPAL DISPLAY PANEL

NDC 64376-601-31

1 mg: Bottle of 30 Tablets

NDC 64376-602-31

2 mg: Bottle of 30 Tablets