glycopyrrolate

glycopyrrolate /gly·co·pyr·ro·late/ (-pir´o-lat) a synthetic anticholinergic used as a gastrointestinal antispasmodic, a preanesthetic antisialagogue, and an antiarrhythmic for anesthesia- or surgery-associated arrhythmias.

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gly·co·pyr·ro·late (glk-pîr-lt)

n.

A parasympatholytic compound used as premedication to general anesthesia, as an antagonist to the bradycardic effects of neostigmine during curare reversal, and as an adjunct in the treatment of peptic ulcer.

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glycopyrrolate, glycopyrronium

an anticholinergic used to reduce gastric acid secretion and hypermotility.

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glycopyrrolate (glycopyrronium)

Robinul, Robinul Forte

Pharmacologic class: Anticholinergic

Therapeutic class: Antispasmodic, antimuscarinic, parasympatholytic

Pregnancy risk category B

Action

Inhibits action of acetylcholine on muscarinic receptors that mediate effects of parasympathetic postganglionic impulses. This inhibition relaxes cardiac smooth muscle, inhibits vagal reflexes, and decreases tracheal and bronchial secretions.

Availability

Injection: 0.2 mg/ml

Tablets: 1 mg, 2 mg

⊘Indications and dosages

➣ Adjunct in peptic ulcer disorders

Adults: 1 mg P.O. t.i.d. or 2 mg (Forte) two to three times daily, to a maximum of 8 mg/day; or 0.1 to 0.2 mg I.M. or I.V. three or four times daily

➣ To diminish secretions and block cardiac vagal reflexes before surgery

Adults and children ages 2 and older: 0.0044 mg/kg I.M. 30 to 60 minutes before anesthesia

Children ages 1 month to 2 years: 0.0088 mg/kg I.M. 30 to 60 minutes before anesthesia

➣ To diminish secretions and block cardiac vagal reflexes during surgery

Adults: 0.1 mg I.V. May repeat as needed at 2- to 3-minute intervals.

Children: 0.004 mg/kg I.V., not to exceed 0.1 mg as a single dose. May repeat at 2- to 3-minute intervals.

➣ To diminish or block cholinergic effects caused by anticholinesterase

Adults and children: 0.2 mg I.V. for each 1 mg neostigmine or 5 mg pyridostigmine. May give I.V. undiluted or with dextrose injection by infusion.

Off-label uses

• Sweating

Contraindications

• Hypersensitivity to drug
• Arrhythmias
• Chronic obstructive pulmonary disease
• GI disease, infection, atony or ileus
• Myasthenia gravis
• Glaucoma
• Obstructive uropathy
• Severe prostatic hypertrophy

Precautions

Use cautiously in:
• cardiovascular disease, heart failure, hypertension, renal or hepatic disease, Down syndrome, hyperthyroidism, hiatal hernia, ulcerative colitis, mild to moderate prostatic hypertrophy, autonomic neuropathy, spasticity, suspected brain damage
• pregnant or breastfeeding patients.

Administration

• Give oral dose 30 to 60 minutes before meals.
• For I.V. injection, give either undiluted or diluted with dextrose 5% or 10% in water or saline solution. Give each 0.2 mg over 1 to 2 minutes.
☞ Keep resuscitation equipment on hand to treat curare-like effects of overdose.

Route	Onset	Peak	Duration
P.O.	Unknown	Unknown	8-12 hr
I.V.	1 min	Unknown	3-7 hr
I.M., subcut.	15-30 min	30-45 min	3-7 hr

Adverse reactions

CNS: weakness, nervousness, insomnia, drowsiness, dizziness, headache, confusion, excitement

CV: palpitations, tachycardia

EENT: blurred vision, photophobia, mydriasis, increased intraocular pressure, cycloplegia

GI: nausea, vomiting, constipation, abdominal distention, epigastric distress, heartburn, gastroesophageal reflux, dry mouth, paralytic ileus

GU: urinary hesitancy or retention, lactation suppression, erectile dysfunction

Skin: urticaria, decreased sweating or anhidrosis

Other: loss of taste, fever, allergic reaction, irritation at I.M. injection site, anaphylaxis, malignant hyperthermia

Interactions

Drug-drug. Amantadine, antihistamines, antiparkinsonian drugs, disopyramide, glutethimide, meperidine, phenothiazines, procainamide, quinidine, tricyclic antidepressants: additive anticholinergic effects

Patient monitoring

☞ Check for signs and symptoms of anaphylaxis and malignant hyperthermia.
• Monitor neurologic and cardiovascular status.
☞ Assess for curare-like effects (neuromuscular blockade leading to muscle weakness and possible paralysis), which indicate overdose.
• Assess fluid intake and output. Have patient void before each dose to avoid urinary retention.

Patient teaching

• Advise patient to take oral dose 30 to 60 minutes before meals.
☞ Tell patient to immediately report signs and symptoms of serious adverse effects, especially anaphylaxis.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, vision, and alertness.
• Tell patient to minimize GI upset by eating frequent, small servings of food and drinking adequate fluids.
• Advise patient to report urinary hesitancy or retention.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.