What is glycopyrrolate, and how does it work (mechanism of action)?

Glycopyrrolate is a synthetic anti-cholinergic medication. Glycopyrrolate works by blocking acetylcholine activity on smooth muscles and other tissues. Acetylcholine is neurotransmitter, a chemical that nerves use for communicating. Blocking of acetylcholine leads to decrease in volume and acidity of stomach secretions and decrease in pharyngeal, tracheal, and bronchial secretions. It also reverses symptoms of excessive bronchial secretions, bronchospasm, low heart rate, and intestinal hypermotility caused by medications that increase the action of acetylcholine. The FDA approved glycopyrrolate in August 1961.

What brand names are available for glycopyrrolate?

Robinul, Robinul Forte, Cuvposa, Glycate

Is glycopyrrolate available as a generic drug?

Yes

Do I need a prescription for glycopyrrolate?

Yes

What are the side effects of glycopyrrolate?

Common side effects of glycopyrrolate are:

What is the dosage for glycopyrrolate?

Adults

  • Preanesthetic medication: Inject 0.004 mg/kg intramuscularly or intravenously 30 to 60 minutes prior to surgery.
  • Intraoperative medication: Inject 0.1 mg as a single dose intravenously every 2 to 3 minutes as needed.
  • Reversal of neuromuscular blockade: Inject 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine given.
  • Peptic ulcer: Inject 0.1 mg intramuscularly or intravenously at 4-hour intervals, up to 3 to 4 times daily. May increase to 0.2 mg if needed.

Children

  • Preanesthetic medication (children over 2 years of age): Inject 0.004 mg/kg intramuscularly, given 30 to 60 minutes prior to anesthesia, narcotic, or sedative.
  • Preanesthetic medication (Infants of 1 month to 2 years of age): Inject up to 0.009 mg/kg.
  • Intraoperative medication: Inject 0.004 mg/kg as single dose intravenously every 2 to 3 minutes as needed. Do not exceed 0.1 mg in a single dose.
  • Reversal of neuromuscular blockade: Inject 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine given.

Glycopyrrolate Injection is not recommended for the treatment of peptic ulcer in pediatric patients.

QUESTION

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Which drugs or supplements interact with glycopyrrolate?

Glycopyrrolate should not be used with anti-cholinergic drugs such as phenothiazines, Parkinson's drugs, or tricyclic antidepressants because it can significantly increase anticholinergic side effects like mydriasis (pupil dilation), high blood pressure (hypertension), flushing, fever, and increased heart rate.

Glycopyrrolate should be used with caution with potassium chloride because concomitant use can decrease bowel movement and can cause irritation or lesions in the stomach and intestine.

Is glycopyrrolate safe to take if I'm pregnant or breastfeeding?

There are no adequate studies done on glycopyrrolate to determine safe and effective use in pregnant women. It has been shown that small amounts of glycopyrrolate will pass the placental barrier.

It is not known whether glycopyrrolate enters breast milk; therefore, it is best to be cautious before using it in nursing mothers. Anticholinergics may cause suppression of lactation.

What else should I know about glycopyrrolate?

What preparations of glycopyrrolate are available?

Glycopyrrolate injection is available in 0.2 mg/ml strength in 1 ml and 2 ml single-use vials. It is also available in 5 ml and 20 ml multi-use vials. All vials contain benzyl alcohol 0.9% as preservative.

How should I keep glycopyrrolate stored?

Store Glycopyrrolate injection at room temperature between 20 C and 25 C (68 F and 77 F).

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Summary

Glycopyrrolate (Robinul, Robinul Forte, Cuvposa, Glycate) is an injection medication used as a postoperative medications to prevent secretions during surgery; and to reverse neuromuscular blockage, irregular heart rate. Side effects, drug interactions, dosage, storage, and pregnancy safety information should be reviewed prior to administering this medication.

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Medically Reviewed on 3/14/2019
References
Medically reviewed by John P. Cunha, DO, FACOEP; Board Certified Emergency Medicine

REFERENCE:

FDA Prescribing Information.
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