FDA

Glycopyrrolate

Approved 21 Apr 2022Intramuscular, IntravenousSolution

The FDA lists this product in 60 strengths and forms.

Indications

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 Injection is an anticholinergic indicated: in anesthesia (adult and pediatric patients) for reduction of airway or gastric secretions, and 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.

( 1 ) in peptic ulcer (adults) as adjunctive therapy for the treatment of peptic ulcer when rapid anticholinergic effect is desired or oral medication is not tolerated.

Contraindications

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.

Known hypersensitivity to glycopyrrolate or any of its inactive ingredients. ( 4 ) Peptic ulcer patients with glaucoma; obstructive uropathy; obstructive disease of the gastrointestinal tract; 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. ( 4 )

Indications

( 1 ) in peptic ulcer (adults) as adjunctive therapy for the treatment of peptic ulcer when rapid anticholinergic effect is desired or oral medication is not tolerated.

Contraindications

Warnings and precautions

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 )

5.1Precipitation 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 in the event that they experience symptoms of acute angle closure glaucoma (pain and reddening of the eyes, accompanied by dilated pupils).

5.2Drowsiness or Blurred Vision 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.

5.3 Heat Prostration 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.

5.4Intestinal Obstruction

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.

5.5Tachycardia

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.

5.6Risk of Use in Patients with Renal Impairment

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 ) ]

5.7 Autonomic Neuropathy, Hepatic Disease, Ulcerative Colitis, Prostatic Hypertrophy, or Hiatal Hernia 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.

5.8Delayed Gastric Emptying/Gastric Stasis

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.

5.9Light Sensitivity

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

Pregnancy and breastfeeding

8.1Pregnancy

Risk summary Limited data are available with glycopyrrolate use during pregnancy have not identified a drug-associated risk of birth defects and miscarriage, however, most of the reported exposures occurred after the first trimester. Most of the available data are based on studies with exposures that occurred at the time of Cesarean-section delivery, and these studies have not identified an adverse effect on maternal outcomes or infant Apgar scores ( see Data ).

In animal reproduction studies in pregnant rats and rabbits administered glycopyrrolate orally (rats) and intramuscularly (rabbits) during the period of organogenesis, no teratogenic effects were seen at 320-times and 5 times the maximum recommended human dose (MRHD) of 2 mg (on a mg/m 2 basis), respectively ( see Data ). The estimated background risk for major birth defects and miscarriage for the indicated population is unknown.

All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in the clinically recognized pregnancies is 2-4% and 15−20%, respectively. Data Human Data Published, randomized, controlled trials over several decades, which compared the use of glycopyrrolate to another antimuscarinic agent in pregnant women during Cesarean section, have not identified adverse maternal or infant outcomes.

In normal doses (0.004 mg/kg), glycopyrrolate does not appear to affect fetal heart rate or fetal heart rate variability to a significant degree. Concentrations of glycopyrrolate in umbilical venous and arterial blood and in the amniotic fluid are low after intramuscular administration to parturients. Therefore, glycopyrrolate does not appear to penetrate through the placental barrier in significant amounts. There are no studies on the safety of glycopyrrolate exposure during the period of organogenesis, and therefore, it is not possible to draw any conclusions on the risk of birth defects following exposure to glycopyrrolate during pregnancy.

In addition, there are no data on the risk of miscarriage following fetal exposure to glycopyrrolate. Animal Data Reproduction studies with glycopyrrolate were performed in rats at a dietary dose of approximately 65 mg/kg/day (exposure was approximately 320 times the maximum recommended daily human dose of 2 mg on a mg/m 2 basis) and rabbits at intramuscular doses of up to 0.5 mg/kg/day (exposure was approximately 5 times the maximum recommended daily human dose on a mg/m 2 basis).

These studies produced no teratogenic effects to the fetus. A preclinical study on reproductive performance of rats given glycopyrrolate resulted in a decreased rate of conception and survival at weaning.

Adverse reactions

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. Most common adverse reactions are related to anticholinergic pharmacology and 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; bradycardia; palpitation; and decreased sweating. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Fresenius Kabi USA, LLC at 1-800-551-7176 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Glycopyrrolate

Indications

Contraindications

Two medicines in one question?

Glycopyrrolate

Indications

Contraindications

Two medicines in one question?

Warnings and precautions

5.1Precipitation of Acute Glaucoma Glycopyrrolate

5.2Drowsiness or Blurred Vision Glycopyrrolate

5.4Intestinal Obstruction

5.5Tachycardia

5.6Risk of Use in Patients with Renal Impairment

5.8Delayed Gastric Emptying/Gastric Stasis

5.9Light Sensitivity

Interactions

Pregnancy and breastfeeding

8.1Pregnancy

Adverse reactions

Composition

Strengths and forms

Official product information

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