These Highlights Do Not Include All The Information Needed To Use Glycopyrrolate Injection Safely And Effectively. See Full Prescribing Information For Glycopyrrolate Injection.

Preanesthetic Medication

The recommended dose of Glycopyrrolate Injection is 0.004 mg/kg by intramuscular injection, given 30 to 60 minutes prior to the anticipated time of induction of anesthesia or at the time the preanesthetic narcotic and/or sedative are administered.

PACKAGE LABEL - PRINCIPAL DISPLAY – Glycopyrrolate Injection, USP 3 mL Syringe Label

3 mL Single-Dose Prefilled Syringe. For IM or IV Use. Rx only

Glycopyrrolate Injection, USP

0.6 mg / 3 mL (0.2 mg /mL)

To combat peripheral anticholinergic effects, a quaternary ammonium anticholinesterase such as neostigmine methylsulfate (which does not cross the blood-brain barrier) may be given intravenously in increments of 0.25 mg in adults. This dosage may be repeated every five to ten minutes until anticholinergic overactivity is reversed or up to a maximum of 2.5 mg. Proportionately smaller doses should be used in pediatric patients. Indication for repetitive doses of neostigmine should be based on close monitoring of the decrease in heart rate and the return of bowel sounds.

If CNS symptoms (e.g., excitement, restlessness, convulsions, psychotic behavior) occur, physostigmine (which does cross the blood–brain barrier) may be used. Physostigmine 0.5 to 2 mg should be slowly administered intravenously and repeated as necessary up to a total of 5 mg in adults. Proportionately smaller doses should be used in pediatric patients.

To combat hypotension, administer IV fluids and/or pressor agents along with supportive care.

Fever should be treated symptomatically.

Following overdosage, a curare-like action may occur, i.e., neuromuscular blockade leading to muscular weakness and possible paralysis. In the event of a curare-like effect on respiratory muscles, artificial respiration should be instituted and maintained until effective respiratory action returns.

Glycopyrrolate Injection, USP is a synthetic anticholinergic agent. It is intended for intramuscular or intravenous administration. Each 1 mL contains:

Glycopyrrolate, USP 0.2 mg, Water for Injection, USP q.s., pH adjusted, when necessary, with hydrochloric acid and/or sodium hydroxide. Solution does not contain preservatives.

Glycopyrrolate is a quaternary ammonium salt with the following chemical name:

3[(cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethyl pyrrolidinium bromide.

Its structural formula is as follows:

Glycopyrrolate occurs as a white, odorless crystalline powder. It is soluble in water and alcohol, and practically insoluble in chloroform and ether. It completely ionized at physiological pH values. Glycopyrrolate Injection, USP, is a clear, colorless, sterile liquid; pH 2.0 to 3.0. The partition coefficient of glycopyrrolate in a n-octanol/water system is 0.304 (log₁₀ P= -1.52) at ambient room temperature (24°C).

Investigate any tachycardia before giving Glycopyrrolate Injection because an increase in the heart rate may occur. Use with caution in patients with coronary artery disease, congestive heart failure, cardiac arrhythmias, hypertension, and/or hyperthyroidism.

Safety and effectiveness in pediatric patients have not been established for the management of peptic ulcer.

Dysrhythmias associated with the use of glycopyrrolate intravenously as a premedicant or during anesthesia have been observed in pediatric patients.

Infants, patients with Down's syndrome, and pediatric patients with spastic paralysis or brain damage may experience an increased response to anticholinergics, thus increasing the potential for side effects.

A paradoxical reaction characterized by hyperexcitability may occur in pediatric patients taking large doses of anticholinergics including Glycopyrrolate Injection. Infants and young children are especially susceptible to the toxic effects of anticholinergics.

Clinical Studies of Glycopyrrolate Injection did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other therapy.

Glycopyrrolate Injection is contraindicated in:

• patients with known hypersensitivity to Glycopyrrolate Injection or any of its inactive ingredients.
• peptic ulcer patients with the following concurrent conditions: 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.

The following adverse reactions were identified in clinical studies or postmarketing reports. Because some of these reactions were 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.

Adverse reactions to anticholinergics include xerostomia (dry mouth); urinary hesitancy and retention; blurred vision and photophobia due to mydriasis (dilation of the pupil); cycloplegia; increased ocular tension; tachycardia; palpitation; decreased sweating; loss of taste; headache; nervousness; drowsiness; weakness; dizziness; insomnia; nausea; vomiting; impotence; suppression of lactation; constipation; bloated feeling; severe allergic reactions including anaphylactic/anaphylactoid reactions; hypersensitivity; urticaria, pruritus, dry skin, and other dermal manifestations; some degree of mental confusion and/or excitement, especially in elderly persons.

The following adverse events have been reported from post-marketing experience with glycopyrrolate: malignant hyperthermia; cardiac arrhythmias (including bradycardia, ventricular tachycardia, ventricular fibrillation); cardiac arrest; hypertension; hypotension; seizures; and respiratory arrest. Post-marketing reports have included cases of heart block and QTc interval prolongation associated with the combined use of glycopyrrolate and an anticholinesterase. Injection site reactions including pruritus, edema, erythema, and pain have also been reported.

The concurrent use of Glycopyrrolate Injection with other anticholinergics or medications with anticholinergic activity, such as phenothiazines, antiparkinson drugs, or tricyclic antidepressants, may intensify the antimuscarinic effects and result in an increase in anticholinergic side effects.

Concomitant administration of Glycopyrrolate Injection and potassium chloride in a wax matrix may increase the severity of potassium chloride-induced gastrointestinal lesions as a result of a slower gastrointestinal transit time.

In the presence of fever, high environmental temperature, and/or during physical exercise, heat prostration can occur with use of anticholinergic agents including Glycopyrrolate Injection (due to decreased sweating), particularly in children and the elderly. Advise patients to avoid exertion and high environmental temperature after receiving Glycopyrrolate Injection.

Renal elimination of glycopyrrolate may be severely impaired in patients with renal failure. Dosage adjustments may be necessary [see Clinical Pharmacology (12.3)].

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 highly non-polar tertiary amines which penetrate lipid barriers easily. 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. With intravenous injection, the onset of action is generally evident within one minute. Following intramuscular administration, the onset of action is noted in 15 to 30 minutes, with peak effects occurring within approximately 30 to 45 minutes. The vagal blocking effects persist for 2 to 3 hours and the antisialagogue effects persist up to 7 hours, periods longer than for atropine.

The following pharmacokinetic information and conclusions were obtained from published studies that used nonspecific assay methods.

Patients may experience sensitivity of the eyes to light. Advise patients to protect their eyes from light after receiving Glycopyrrolate Injection.

Glycopyrrolate Injection, USP (0.2 mg/mL) is an anticholinergic indicated for use in:

anesthesia (all ages)

• for reduction of salivary, tracheobronchial, and pharyngeal secretions, reduction of volume and acidity of gastric secretions, and blockade of cardiac inhibitory reflexes during induction of anesthesia and intubation,
• intraoperatively to counteract surgically or drug-induced or vagal reflex-associated arrhythmias, and
• for protection against peripheral muscarinic effects of cholinergic agents such as neostigmine and pyridostigmine given to reverse the neuromuscular blockade due to non-depolarizing agents.

peptic ulcer (adults)

• as adjunctive therapy for the treatment of peptic ulcer when rapid anticholinergic effect is desired or when oral medication is not tolerated.

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 sinoatrial 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.

• Precipitation of Acute Glaucoma: Glycopyrrolate Injection may cause mydriasis and increase intraocular pressure in patients with glaucoma. Advise patients with glaucoma to promptly seek medical care if they experience symptoms of acute angle closure glaucoma. (5.1)
• Drowsiness or Blurred Vision: May cause drowsiness or blurred vision. Advise patients not to drive or perform hazardous work until resolved. (5.2)
• Heat Prostration: Advise patients to avoid exertion and high environmental temperatures after receiving Glycopyrrolate Injection. (5.3)
• Intestinal Obstruction: Diarrhea may be an early symptom of incomplete intestinal obstruction. Avoid use in patients with diarrhea and ileostomy or colostomy. (5.4)
• Tachycardia: Increase in heart rate may occur. Use with caution in patients with coronary artery disease, congestive heart failure, cardiac arrhythmias, hypertension, or hyperthyroidism. (5.5)

Diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. In this instance treatment with Glycopyrrolate Injection is inappropriate and possibly harmful. Avoid use in patients with these conditions.

Glycopyrrolate Injection may be administered intramuscularly, or intravenously, without dilution, in the following indications:

Adults (2.2)

Preanesthetic Medication: 0.004 mg/kg IM, given 30 to 60 minutes prior to the anticipated time of induction of anesthesia

Intraoperative Medication: single doses of 0.1 mg IV and repeated, as needed, at intervals of 2 to 3 minutes

Reversal of Neuromuscular Blockade: 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine

Peptic Ulcer: 0.1 mg IV or IM at 4-hour intervals, 3 or 4 times daily

Pediatric patients (2.3)

Preanesthetic Medication: 0.004 mg/kg IM, given 30 to 60 minutes prior to the anticipated time of induction of anesthesia. Patients under 2 years of age may require up to 0.009 mg/kg

Intraoperative Medication: 0.004 mg/kg IV, not to exceed 0.1 mg in a single dose and repeated, as needed, at intervals of 2 to 3 minutes

Reversal of Neuromuscular Blockade: 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine

Peptic Ulcer: Glycopyrrolate Injection is not indicated for the treatment of peptic ulcer in pediatric patients

Do not use prefilled syringe to administer a dose of less than 0.1 mg (0.5 mL). (2.3)

See Full Prescribing Information for preparation, handling, and instructions for use of pre-filled syringe (2.4, 2.5)

Glycopyrrolate Injection, USP, is a clear, colorless solution available in 0.6 mg/3 mL (0.2 mg/mL) single-dose, prefilled, disposable syringes.

• Pediatric Use: Infants, patients with Down's Syndrome, and pediatric patients with spastic paralysis or brain damage may experience an increased response to anticholinergics, thus increasing the potential for side effects. Large doses may cause hyperexcitability. (8.4)

Glycopyrrolate Injection may cause drowsiness or blurred vision. Warn patients not to participate in activities requiring mental alertness, such as operating a motor vehicle or other machinery, or performing hazardous work, until these issues resolve.

Glycopyrrolate Injection may cause mydriasis and increase intraocular pressure in patients with glaucoma. Advise patients with glaucoma to promptly seek medical care in the event that they experience symptoms of acute angle closure glaucoma (pain and reddening of the eyes, accompanied by dilated pupils).

Glycopyrrolate Injection, USP, 0.2 mg per mL without preservative is available as:

Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature.]

Sensitive to heat – Do not autoclave. Discard unused portion.

Do not place syringe on a sterile field.

The use of anticholinergetic drugs, including Glycopyrrolate Injection, in the treatment of gastric ulcer may produce a delay in gastric emptying due to antral statis. Monitor patients for symptoms such as vomiting, dyspepsia, early satiety, abdominal distention, and increased abdominal pain. Discontinue Glycopyrrolate Injection treatment if these symptoms develop or worsen on treatment.

Figure 1: Outer Packaging and Prefilled Syringe

• Inspect the outer packaging (blister pack) to confirm the integrity of the packaging. Do not use if the blister pack or the prefilled syringe has been damaged.
• Remove the syringe from the outer packaging. (See Figure 2)

  Figure 2
• Visually inspect the syringe. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
• Twist off the syringe tip cap. Do not remove the label around the luer lock collar. (See Figure 3)

  Figure 3
• Expel air bubble(s). Adjust the dose (if applicable).
• Administer the dose ensuring that pressure is maintained on the plunger rod during the entire administration.
• Discard the used syringe into an appropriate receptacle.

• Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.
• Glycopyrrolate Injection may be administered intramuscularly, or intravenously, without dilution.
• Do not introduce any other fluid into the syringe at any time.
• Do not dilute for IV push.
• Do not re-sterilize the syringe.
• Do not use this product on a sterile field.
• This product is for single dose only.

Renal elimination of glycopyrrolate may be severely impaired in patients with renal failure. Dosage adjustments may be necessary in this population [see Pharmacokinetics (12.3)]

Use Glycopyrrolate Injection with caution in the elderly and in all patients with autonomic neuropathy, hepatic disease, ulcerative colitis, prostatic hypertrophy, or hiatal hernia, because anticholinergic drugs may aggravate these conditions. Consider dose reduction and closely monitor the elderly and patients with autonomic neuropathy, hepatic disease, ulcerative colitis, prostatic hypertrophy, or hiatal hernia.

Preanesthetic Medication

The recommended dose of Glycopyrrolate Injection is 0.004 mg/kg by intramuscular injection, given 30 to 60 minutes prior to the anticipated time of induction of anesthesia or at the time the preanesthetic narcotic and/or sedative are administered.

PACKAGE LABEL - PRINCIPAL DISPLAY – Glycopyrrolate Injection, USP 3 mL Syringe Label

3 mL Single-Dose Prefilled Syringe. For IM or IV Use. Rx only

Glycopyrrolate Injection, USP

0.6 mg / 3 mL (0.2 mg /mL)

To combat peripheral anticholinergic effects, a quaternary ammonium anticholinesterase such as neostigmine methylsulfate (which does not cross the blood-brain barrier) may be given intravenously in increments of 0.25 mg in adults. This dosage may be repeated every five to ten minutes until anticholinergic overactivity is reversed or up to a maximum of 2.5 mg. Proportionately smaller doses should be used in pediatric patients. Indication for repetitive doses of neostigmine should be based on close monitoring of the decrease in heart rate and the return of bowel sounds.

If CNS symptoms (e.g., excitement, restlessness, convulsions, psychotic behavior) occur, physostigmine (which does cross the blood–brain barrier) may be used. Physostigmine 0.5 to 2 mg should be slowly administered intravenously and repeated as necessary up to a total of 5 mg in adults. Proportionately smaller doses should be used in pediatric patients.

To combat hypotension, administer IV fluids and/or pressor agents along with supportive care.

Fever should be treated symptomatically.

Following overdosage, a curare-like action may occur, i.e., neuromuscular blockade leading to muscular weakness and possible paralysis. In the event of a curare-like effect on respiratory muscles, artificial respiration should be instituted and maintained until effective respiratory action returns.

Glycopyrrolate Injection, USP is a synthetic anticholinergic agent. It is intended for intramuscular or intravenous administration. Each 1 mL contains:

Glycopyrrolate, USP 0.2 mg, Water for Injection, USP q.s., pH adjusted, when necessary, with hydrochloric acid and/or sodium hydroxide. Solution does not contain preservatives.

Glycopyrrolate is a quaternary ammonium salt with the following chemical name:

3[(cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethyl pyrrolidinium bromide.

Its structural formula is as follows:

Glycopyrrolate occurs as a white, odorless crystalline powder. It is soluble in water and alcohol, and practically insoluble in chloroform and ether. It completely ionized at physiological pH values. Glycopyrrolate Injection, USP, is a clear, colorless, sterile liquid; pH 2.0 to 3.0. The partition coefficient of glycopyrrolate in a n-octanol/water system is 0.304 (log₁₀ P= -1.52) at ambient room temperature (24°C).

Investigate any tachycardia before giving Glycopyrrolate Injection because an increase in the heart rate may occur. Use with caution in patients with coronary artery disease, congestive heart failure, cardiac arrhythmias, hypertension, and/or hyperthyroidism.

Safety and effectiveness in pediatric patients have not been established for the management of peptic ulcer.

Dysrhythmias associated with the use of glycopyrrolate intravenously as a premedicant or during anesthesia have been observed in pediatric patients.

Infants, patients with Down's syndrome, and pediatric patients with spastic paralysis or brain damage may experience an increased response to anticholinergics, thus increasing the potential for side effects.

A paradoxical reaction characterized by hyperexcitability may occur in pediatric patients taking large doses of anticholinergics including Glycopyrrolate Injection. Infants and young children are especially susceptible to the toxic effects of anticholinergics.

Clinical Studies of Glycopyrrolate Injection did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other therapy.

Glycopyrrolate Injection is contraindicated in:

• patients with known hypersensitivity to Glycopyrrolate Injection or any of its inactive ingredients.
• peptic ulcer patients with the following concurrent conditions: 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.

The following adverse reactions were identified in clinical studies or postmarketing reports. Because some of these reactions were 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.

Adverse reactions to anticholinergics include xerostomia (dry mouth); urinary hesitancy and retention; blurred vision and photophobia due to mydriasis (dilation of the pupil); cycloplegia; increased ocular tension; tachycardia; palpitation; decreased sweating; loss of taste; headache; nervousness; drowsiness; weakness; dizziness; insomnia; nausea; vomiting; impotence; suppression of lactation; constipation; bloated feeling; severe allergic reactions including anaphylactic/anaphylactoid reactions; hypersensitivity; urticaria, pruritus, dry skin, and other dermal manifestations; some degree of mental confusion and/or excitement, especially in elderly persons.

The following adverse events have been reported from post-marketing experience with glycopyrrolate: malignant hyperthermia; cardiac arrhythmias (including bradycardia, ventricular tachycardia, ventricular fibrillation); cardiac arrest; hypertension; hypotension; seizures; and respiratory arrest. Post-marketing reports have included cases of heart block and QTc interval prolongation associated with the combined use of glycopyrrolate and an anticholinesterase. Injection site reactions including pruritus, edema, erythema, and pain have also been reported.

The concurrent use of Glycopyrrolate Injection with other anticholinergics or medications with anticholinergic activity, such as phenothiazines, antiparkinson drugs, or tricyclic antidepressants, may intensify the antimuscarinic effects and result in an increase in anticholinergic side effects.

Concomitant administration of Glycopyrrolate Injection and potassium chloride in a wax matrix may increase the severity of potassium chloride-induced gastrointestinal lesions as a result of a slower gastrointestinal transit time.

In the presence of fever, high environmental temperature, and/or during physical exercise, heat prostration can occur with use of anticholinergic agents including Glycopyrrolate Injection (due to decreased sweating), particularly in children and the elderly. Advise patients to avoid exertion and high environmental temperature after receiving Glycopyrrolate Injection.

Renal elimination of glycopyrrolate may be severely impaired in patients with renal failure. Dosage adjustments may be necessary [see Clinical Pharmacology (12.3)].

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 highly non-polar tertiary amines which penetrate lipid barriers easily. 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. With intravenous injection, the onset of action is generally evident within one minute. Following intramuscular administration, the onset of action is noted in 15 to 30 minutes, with peak effects occurring within approximately 30 to 45 minutes. The vagal blocking effects persist for 2 to 3 hours and the antisialagogue effects persist up to 7 hours, periods longer than for atropine.

The following pharmacokinetic information and conclusions were obtained from published studies that used nonspecific assay methods.

Patients may experience sensitivity of the eyes to light. Advise patients to protect their eyes from light after receiving Glycopyrrolate Injection.

Glycopyrrolate Injection, USP (0.2 mg/mL) is an anticholinergic indicated for use in:

anesthesia (all ages)

• for reduction of salivary, tracheobronchial, and pharyngeal secretions, reduction of volume and acidity of gastric secretions, and blockade of cardiac inhibitory reflexes during induction of anesthesia and intubation,
• intraoperatively to counteract surgically or drug-induced or vagal reflex-associated arrhythmias, and
• for protection against peripheral muscarinic effects of cholinergic agents such as neostigmine and pyridostigmine given to reverse the neuromuscular blockade due to non-depolarizing agents.

peptic ulcer (adults)

• as adjunctive therapy for the treatment of peptic ulcer when rapid anticholinergic effect is desired or when oral medication is not tolerated.

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 sinoatrial 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.

• Precipitation of Acute Glaucoma: Glycopyrrolate Injection may cause mydriasis and increase intraocular pressure in patients with glaucoma. Advise patients with glaucoma to promptly seek medical care if they experience symptoms of acute angle closure glaucoma. (5.1)
• Drowsiness or Blurred Vision: May cause drowsiness or blurred vision. Advise patients not to drive or perform hazardous work until resolved. (5.2)
• Heat Prostration: Advise patients to avoid exertion and high environmental temperatures after receiving Glycopyrrolate Injection. (5.3)
• Intestinal Obstruction: Diarrhea may be an early symptom of incomplete intestinal obstruction. Avoid use in patients with diarrhea and ileostomy or colostomy. (5.4)
• Tachycardia: Increase in heart rate may occur. Use with caution in patients with coronary artery disease, congestive heart failure, cardiac arrhythmias, hypertension, or hyperthyroidism. (5.5)

Diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. In this instance treatment with Glycopyrrolate Injection is inappropriate and possibly harmful. Avoid use in patients with these conditions.

Glycopyrrolate Injection may be administered intramuscularly, or intravenously, without dilution, in the following indications:

Adults (2.2)

Preanesthetic Medication: 0.004 mg/kg IM, given 30 to 60 minutes prior to the anticipated time of induction of anesthesia

Intraoperative Medication: single doses of 0.1 mg IV and repeated, as needed, at intervals of 2 to 3 minutes

Reversal of Neuromuscular Blockade: 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine

Peptic Ulcer: 0.1 mg IV or IM at 4-hour intervals, 3 or 4 times daily

Pediatric patients (2.3)

Preanesthetic Medication: 0.004 mg/kg IM, given 30 to 60 minutes prior to the anticipated time of induction of anesthesia. Patients under 2 years of age may require up to 0.009 mg/kg

Intraoperative Medication: 0.004 mg/kg IV, not to exceed 0.1 mg in a single dose and repeated, as needed, at intervals of 2 to 3 minutes

Reversal of Neuromuscular Blockade: 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine

Peptic Ulcer: Glycopyrrolate Injection is not indicated for the treatment of peptic ulcer in pediatric patients

Do not use prefilled syringe to administer a dose of less than 0.1 mg (0.5 mL). (2.3)

See Full Prescribing Information for preparation, handling, and instructions for use of pre-filled syringe (2.4, 2.5)

Glycopyrrolate Injection, USP, is a clear, colorless solution available in 0.6 mg/3 mL (0.2 mg/mL) single-dose, prefilled, disposable syringes.

• Pediatric Use: Infants, patients with Down's Syndrome, and pediatric patients with spastic paralysis or brain damage may experience an increased response to anticholinergics, thus increasing the potential for side effects. Large doses may cause hyperexcitability. (8.4)

Glycopyrrolate Injection may cause drowsiness or blurred vision. Warn patients not to participate in activities requiring mental alertness, such as operating a motor vehicle or other machinery, or performing hazardous work, until these issues resolve.

Glycopyrrolate Injection may cause mydriasis and increase intraocular pressure in patients with glaucoma. Advise patients with glaucoma to promptly seek medical care in the event that they experience symptoms of acute angle closure glaucoma (pain and reddening of the eyes, accompanied by dilated pupils).

Glycopyrrolate Injection, USP, 0.2 mg per mL without preservative is available as:

Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature.]

Sensitive to heat – Do not autoclave. Discard unused portion.

Do not place syringe on a sterile field.

The use of anticholinergetic drugs, including Glycopyrrolate Injection, in the treatment of gastric ulcer may produce a delay in gastric emptying due to antral statis. Monitor patients for symptoms such as vomiting, dyspepsia, early satiety, abdominal distention, and increased abdominal pain. Discontinue Glycopyrrolate Injection treatment if these symptoms develop or worsen on treatment.

Figure 1: Outer Packaging and Prefilled Syringe

• Inspect the outer packaging (blister pack) to confirm the integrity of the packaging. Do not use if the blister pack or the prefilled syringe has been damaged.
• Remove the syringe from the outer packaging. (See Figure 2)

  Figure 2
• Visually inspect the syringe. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
• Twist off the syringe tip cap. Do not remove the label around the luer lock collar. (See Figure 3)

  Figure 3
• Expel air bubble(s). Adjust the dose (if applicable).
• Administer the dose ensuring that pressure is maintained on the plunger rod during the entire administration.
• Discard the used syringe into an appropriate receptacle.

• Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.
• Glycopyrrolate Injection may be administered intramuscularly, or intravenously, without dilution.
• Do not introduce any other fluid into the syringe at any time.
• Do not dilute for IV push.
• Do not re-sterilize the syringe.
• Do not use this product on a sterile field.
• This product is for single dose only.

Renal elimination of glycopyrrolate may be severely impaired in patients with renal failure. Dosage adjustments may be necessary in this population [see Pharmacokinetics (12.3)]

Use Glycopyrrolate Injection with caution in the elderly and in all patients with autonomic neuropathy, hepatic disease, ulcerative colitis, prostatic hypertrophy, or hiatal hernia, because anticholinergic drugs may aggravate these conditions. Consider dose reduction and closely monitor the elderly and patients with autonomic neuropathy, hepatic disease, ulcerative colitis, prostatic hypertrophy, or hiatal hernia.