glycopyrrolate


Also found in: Dictionary, Thesaurus, Encyclopedia, Wikipedia.

glycopyrrolate

 [gli″ko-pir´o-lāt]
a synthetic anticholinergic used as an antispasmodic to help treat peptic ulcer and other gastrointestinal disorders, a preanesthetic antisialagogue to decrease salivation and respiratory secretions associated with anesthesia, and an antiarrhythmic to counteract arrhythmias associated with induction of anesthesia or surgery; administered orally, intramuscularly, or intravenously.

glycopyrrolate (glycopyrronium (UK))

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.

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.

References in periodicals archive ?
MAGNAIR, which is designed, optimised and developed by the company, is intended only for use with LONHALA (glycopyrrolate) Inhalation Solution vials in patients with COPD.
One group received sugammadex of 4 mg/kg and the other group received neostigmine 70 [micro]g/kg along with glycopyrrolate of 14 [micro]g/kg for reversal of NMB.
Options include the tricyclic antidepressant amitriptyline (31); alpha-adrenergic agonists or antagonists (donidine, terazosin); and anti-muscarinic medications (benztropine, atropine, trihexyphenidyl, glycopyrrolate) (Table 2 (31)).
Glycopyrrolate, a long-acting muscarinic antagonist, is available as monotherapy.
Koopmann et al., "Glycopyrrolate for sialorrhea in Parkinson disease: a randomized, double-blind, crossover trial," Neurology, vol.
At the end of surgery, when patients had respiratory attempts, the residual neuromuscular blockage was reversed with neostigmine injection and glycopyrrolate. Recovery assessed and extubation was done after thorough throat suction.
California-based Pearl develops inhaled small-molecule therapeutics for respiratory disease, with lead product PT003 combining formoterol fumarate, a long-acting beta-2-agonist (LABA) and glycopyrrolate, a long-acting muscarinic antagonist (LAMA).
Two anticholinergic drugs are available for this purpose, namely, atropine and glycopyrrolate. Glycopyrrolate is the preferred anticholinergic.
Reversal (neostigmine 2.5 mg and glycopyrrolate 500 [micro]g) was administered and recovery was uneventful.
Neostigmine and glycopyrrolate were used to reverse muscle paralysis and the patient was extubated.
The three most commonly used anticholinergic medications to treat the death rattle in the dying patient are hyoscine hydrobromide (Scopolamine[R]), hyoscyamine sulfate (Levsin[R]), and glycopyrrolate (Robinul[R]) (see Table 2).
Glycopyrrolate is a quaternary ammonium compound used perioperatively to reduce salivary and respiratory secretions.