Rx only 

Glycopyrrolate Injection, USP is a synthetic anticholinergic agent. 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. 

For Intramuscular (IM) or Intravenous (IV) administration. Solution does not contain preservatives.

Glycopyrrolate is a quaternary ammonium salt with the following chemical name:
3[(cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethyl pyrrolidinium bromide. The molecular formula is C19H28BrNO3 and the molecular weight is 398.33.

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.

Unlike atropine, glycopyrrolate is 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).

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.

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.

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.

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.

This drug should be used with great caution, if at all, in patients with glaucoma.

Glycopyrrolate Injection may produce drowsiness or blurred vision. The patient should be cautioned regarding activities requiring mental alertness such as operating a motor vehicle or other machinery or performing hazardous work while taking this drug.

In addition, in the presence of fever, high environmental temperature and/or during physical exercise, heat prostration can occur with use of anticholinergic agents including glycopyrrolate (due to decreased sweating), particularly in children and the elderly.

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

Anticholinergics, including Glycopyrrolate Injection, can produce certain effects, most of which are extensions of their pharmacologic actions. Adverse reactions may 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.

In addition, 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.

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.

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.

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, in the following indications.

Glycopyrrolate Injection, USP, 0.2 mg per mL is available as a preservative-free, clear, colorless solution supplied in single-dose prefilled syringes as follows:

1 mL single-dose prefilled disposable syringe packaged in 10s (NDC 0641-6212-10)

2 mL single-dose prefilled disposable syringe packaged in 10s (NDC 0641-6213-10)

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

Discard unused portion.

Sensitive to heat – Do not autoclave.

Do not place syringe on a sterile field.

To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

For Product Inquiry call 1-877-845-0689.

CAUTION: Glass syringes may malfunction, break or clog when connected to some Needleless Luer Access Devices (NLADs) and needles. The external collar must remain attached to the syringe (See Figure 1). Spontaneous disconnection of this glass syringe from needles and NLADs with leakage of drug product may occur. Assure that the needle or NLAD is securely attached before beginning the injection. Inspect the glass syringe-needle or glass syringe –NLAD connection before and during drug administration.

Figure 1

Syringe Image

Glycopyrrolate Injection may be administered intramuscularly or intravenously. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.

1. Inspect the outer packaging (plastic tube) and the syringe label by verifying:

- plastic tube integrity

- drug name

- drug strength

- fill volume

- route of administration

- expiration date to be sure that the drug has not expired

- sterile field applicability

Do not use if package has been damaged.

2. Open the outer packaging and remove the syringe from the tube.

3. Perform visual inspection on the syringe by verifying:

- absence of syringe damage

- absence of external particles

- absence of internal particles

- proper drug color

4.Push plunger rod slightly to break the stopper loose while tip cap is still on.

5. Remove tip cap by twisting it off. (See Figure 2)

Figure 2

Figure 2

6. Discard the tip cap.

7. Expel air bubble.

8. Adjust dose into sterile material (if applicable).

9. Connect the syringe to appropriate injection connection depending on route of administration.

-Before injection, ensure that the syringe is securely attached to the needle or NLAD.

10. Depress plunger rod to deliver the required dose of medication. Ensure that pressure is maintained on the plunger rod during the entire administration.

11. Remove the syringe from NLAD (if applicable) and discard into appropriate receptacle.

When a needle is connected to the syringe, to prevent needle-stick injuries, do not recap needles.

NOTES:

• All steps must be performed sequentially
• Do not autoclave syringe
• Do not use this product on a sterile field
• Do not introduce any other fluid into the syringe at any time
• This product is for single dose only; discard unused portion

Manufactured by:

Hikma Pharmaceuticals USA Inc.

Berkeley Heights, NJ 07922

462-059-00

Revised July 2024

NDC 0641-6212-01Rx only

1 mL Single-Dose Prefilled Syringe

Glycopyrrolate Injection, USP
0.2 mg/mL
For IM or IV Use

Preservative-Free. Discard unused portion.

NDC 0641-6212-10 Rx only

Glycopyrrolate Injection, USP
0.2 mg/mL
For Intramuscular or Intravenous Use

Preservative-Free.

10 x 1 mL Single-Dose Prefilled Syringes

Discard unused portion.

NDC 0641-6213-01Rx only

2 mL Single-Dose Prefilled Syringe

Glycopyrrolate Injection, USP
0.4 mg per 2 mL (0.2 mg/mL)
For IM or IV Use. Preservative-Free. Discard unused portion.

NDC 0641-6213-10 Rx only

Glycopyrrolate Injection, USP
0.4 mg per 2 mL (0.2 mg/mL)
For Intramuscular or Intravenous Use

Preservative-Free.

10 x 2 mL Single-Dose Prefilled Syringes

Discard unused portion.