Glycopyrrolate Injection

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• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about glycopyrrolate injection, please talk with your doctor, nurse, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about glycopyrrolate injection. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using glycopyrrolate injection.

Review Date: October 4, 2017

The following pharmacokinetic information and conclusions were obtained from published studies that used nonspecific assay
methods.
Distribution: The mean volume of distribution of glycopyrrolate was estimated to be 0.42 ± 0.22 L/kg.
Metabolism: The in vivo metabolism of glycopyrrolate in humans has not been studied.
Excretion: The mean clearance and mean T1/2 values were reported to be 0.54 ± 0.14 L/kg/hr and 0.83 ± 0.13 hr, respectively post
IV administration. After IV administration of a 0.2 mg radiolabeled glycopyrrolate, 85% of dose recovered was recovered in urine
48 hours postdose and some of radioactivity was also recovered in bile. After IM administration of glycopyrrolate to adults, the
mean T1/2 value is reported to be between 0.55 to 1.25 hrs. Over 80% of IM dose administered was recovered in urine and the bile as
unchanged drug and half the IM dose is excreted within 3 hrs. The following table summarizes the mean and standard deviation of
pharmacokinetic parameters from a study.

*0-12 hr **0-8 hr

SPECIAL POPULATIONS
Gender: Gender differences in pharmacokinetics of glycopyrrolate have not been investigated.
Renal Impairment: In one study glycopyrrolate was administered IV in uremic patients undergoing renal transplantation. The
mean elimination half-life was significantly longer (46.8 minutes) than in healthy patients (18.6 minutes). The mean area-underthe-
concentration-time curve (10.6 hr-mg/L), mean plasma clearance (0.43 L/hr/kg), and mean 3-hour urine excretion (0.7%) for
glycopyrrolate were also significantly different than those of controls (3.73 hr-mg/L, 1.14 L/hr/kg, and 50%, respectively). These
results suggest that elimination of glycopyrrolate is severely impaired in patients with renal failure.
Hepatic Impairment: Pharmocokinetic information in patients with hepatic impairment is unavailable.
Pediatrics: Following IV administration (5 mg/kg glycopyrrolate) to infants and children, the mean T1/2 values were reported to be
between 21.6 and 130.0 minutes and between 19.2 and 99.2 minutes, respectively
.

Known hypersensitivity to glycopyrrolate or any of its inactive ingredients.
In addition, in the management of peptic ulcer patients, because of the longer duration of therapy, Glycopyrrolate Injection may be
contraindicated in 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.

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 bloodbrain
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.

NOTE: CONTAINS BENZYL ALCOHOL (See PRECAUTIONS)
Glycopyrrolate Injection may be administered intramuscularly, or intravenously, without dilution, in the following indications:
Adults:
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.
Intraoperative Medication:
Glycopyrrolate Injection may be used during surgery to counteract drug-induced or vagal reflexes and their associated arrhythmias
(e.g., bradycardia). It should be administered intravenously as single doses of 0.1 mg and repeated, as needed, at intervals of 2 to 3
minutes. The usual attempts should be made to determine the etiology of the arrhythmia, and the surgical or anesthetic manipulations
necessary to correct parasympathetic imbalance should be performed.

Reversal of Neuromuscular Blockade:
The recommended dose of Glycopyrrolate Injection is 0.2 mg for each 1.0 mg of neostigmine or 5.0 mg of pyridostigmine. In order to
minimize the appearance of cardiac side effects, the drugs may be administered simultaneously by intravenous injection and may be
mixed in the same syringe.
Peptic Ulcer:
The usual recommended dose of Glycopyrrolate Injection is 0.1 mg administered at 4-hour intervals, 3 or 4 times daily intravenously
or intramuscularly. Where more profound effect is required, 0.2 mg may be given. Some patients may need only a single dose, and
frequency of administration should be dictated by patient response up to a maximum of four times daily.
Glycopyrrolate Injection is not recommended for the treatment of peptic ulcers in pediatric patients (see PRECAUTIONS-Pediatric
Use).
Pediatric Patients
(see PRECAUTIONS-Pediatric Use)
Preanesthetic Medication: The recommended dose of Glycopyrrolate Injection in pediatric patients is 0.004 mg/kg intramuscularly,
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.
Infants:
(1 month to 2 years of age) may require up to 0.009 mg/kg.
lntraoperative Medication:
Because of the long duration of action of Glycopyrrolate Injection if used as preanesthetic medication, additional glycopyrrolate
injection for anticholinergic effect intraoperatively is rarely needed; in the event it is required the recommended pediatric dose is 0.004
mg/kg intravenously, not to exceed 0.1 mg in a single dose which may be repeated, as needed, at intervals of 2 to 3 minutes. The usual
attempts should be made to determine the etiology of the arrhythmia, and the surgical or anesthetic manipulations necessary to correct
parasympathetic imbalance should be performed.
Reversal of Neuromuscular Blockade:
The recommended pediatric dose of Glycopyrrolate Injection is 0.2 mg for each 1.0 mg of neostigmine or 5.0 mg of pyridostigmine. In
order to minimize the appearance of cardiac side effects, the drugs may be administered simultaneously by intravenous injection and
may be mixed in the same syringe.
Peptic Ulcer:
Glycopyrrolate Injection is not recommended for the treatment of peptic ulcer in pediatric patients (see PRECAUTIONS-Pediatric
Use).
NOTE: Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever
solution and container permit.
DILUENT COMPATIBILITIES
Dextrose 5% and 10% in water, or saline, dextrose 5% in sodium chloride 0.45%, sodium chloride 0.9%, and Ringer's Injection.
DILUENT INCOMPATIBILITIES
Lactated Ringer's solution
ADMIXTURE COMPATIBILITIES
Physical Compatibility: This list does not constitute an endorsement of the clinical utility or safety of coadministration of
glycopyrrolate with these drugs. Glycopyrrolate Injection is compatible for mixing and injection with the following injectable
dosage forms: atropine sulfate, USP; Antilirium® (physostigmine salicylate); Benadryl® (diphenhydramine HCl); codeine
phosphate, USP; Emete-Con® (benz-quinamide HCl); hydromorphone HCl, USP; Inapsine® (droperidol); Levo-Dromoran®
(levorphanol tartrate); lidocaine, USP; meperidine HCl, USP; Mestinon®/Regonol® (pyridostigmine bromide); morphine sulfate,
USP; Nubain® (nalbuphine HCl); Numorphan® (oxymorphone HCl); procaine HCl, USP; promethazine HCl, USP; Prostigmin®
(neostigmine methylsulfate, USP); scopolamine HBr, USP; Stadol® (butorphanol tartrate); Sublimaze® (fentanyl citrate); Tigan®
(trimethobenzamide HCl); and Vistaril® (hydroxyzine HCl). Glycopyrrolate Injection may be administered via the tubing of a running
infusion of normal saline.
ADMIXTURE INCOMPATIBILITIES
Physical Incompatibility: Since the stability of glycopyrrolate is questionable above a pH of 6.0 do not combine glycopyrrolate
injection in the same syringe with Brevital® (methohexital Na); Chloromycetin® (chloramphenicol Na succinate); Dramamine®

(dimenhydrinate); Nembutal® (pentobarbital Na); Pentothal® (thiopental Na); Seconal® (secobarbital Na); sodium bicarbonate
(Abbott); Valium® (diazepam); Decadron® (dexamethasone Na phosphate); or Talwin® (pentazocine lactate). These mixtures will
result in a pH higher than 6.0 and may result in gas production or precipitation.

Glycopyrrolate Injection, USP 0.2 mg/mL is available as follows:
NDC-0517-4601-25 1 mL fill in 2 mL single dose vials Packages of 25
NDC-0517-4602-25 2 mL single dose vials Packages of 25
NDC-0517-4605-25 5 mL multiple dose vials Packages of 25
NDC-0517-4620-25 20 mL multiple dose vials Packages of 25
Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) (See USP Controlled Room Temperature).
AMERICAN
REGENT, INC.
SHIRLEY, NY 11967
IN4601
Rev. 1/09

Consult your pharmacist.