General

Pronunciation:
glye-koe-pye-roe-late

Trade Name(s)

• Cuvposa
• Glycate
• Glyrx-PF
• Robinul

Ther. Class.

antispasmodics

Pharm. Class.

anticholinergics

Indications

• Inhibits salivation and excessive respiratory secretions when given preoperatively.
• Reverses some of the secretory and vagal actions of cholinesterase inhibitors used to treat nondepolarizing neuromuscular blockade (cholinergic adjunct).
• Adjunctive management of peptic ulcer disease.
• Oral solution: Reduce chronic severe drooling in children with neurologic conditions associated with drooling.

Action

• Inhibits the action of acetylcholine at postganglionic sites located in smooth muscle, secretory glands, and the CNS (antimuscarinic activity).
• Low doses decrease sweating, salivation, and respiratory secretions.
• Larger doses decrease GI and GU tract motility.

Therapeutic Effect(s):

Decreased GI and respiratory secretions.

Pharmacokinetics

Absorption: Incompletely absorbed (<10%) after oral administration. Well absorbed after IM administration. IV administration results in complete bioavailability.

Distribution: Distribution not fully known. Does not significantly cross the blood-brain barrier or eye.

Metabolism and Excretion: Eliminated primarily unchanged in the urine and bile.

Half-life: 1.7 hr (0.6–4.6 hr).

TIME/ACTION PROFILE (anticholinergic effects)

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity;
• Angle-closure glaucoma;
• Acute hemorrhage;
• Tachycardia secondary to cardiac insufficiency or thyrotoxicosis;
• Severe ulcerative colitis;
• Toxic megacolon;
• Myasthenia gravis;
• Obstructive uropathy;
• Paralytic ileus;
• Concurrent use of oral potassium chloride dose forms (oral solution only).

Use Cautiously in:

• Patients who may have intra-abdominal infections;
• Prostatic hyperplasia;
• Chronic renal, hepatic, pulmonary, or cardiac disease;
• Hyperthyroidism;
• Down syndrome and children with spastic paralysis or brain damage (may be hypersensitive to antimuscarinic effects);
• OB:   Safety not established in pregnancy;
• Lactation:  Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
• Pedi:  ↑ sensitivity to anticholinergic effects and adverse reactions;
• Geri:   ↑ sensitivity to anticholinergic effects and adverse reactions.

Adverse Reactions/Side Effects

CV: tachycardia, orthostatic hypotension, palpitations

Derm: flushing

EENT: nasal congestion, blurred vision, cycloplegia, dry eyes, mydriasis

GI: dry mouth, vomiting, constipation

GU: urinary hesitancy, urinary retention

Neuro: headache, confusion, drowsiness.

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

• May ↑ GI mucosal lesions in patients taking oral  potassium chloride  tablets; concurrent use with oral glycopyrrolate solution contraindicated.
• Additive anticholinergic effects with other  anticholinergics, including  antihistamines,  phenothiazines,  meperidine,  amantadine,  tricyclic antidepressants,  quinidine, and  disopyramide.
• May alter the absorption of other  orally administered drugs  by slowing motility of the GI tract.
• May ↑ GI transit time of oral  digoxin  and ↑ digoxin levels.
•  Antacids  or  adsorbent   antidiarrheal agents  ↓ absorption of anticholinergics.
• May ↑ GI mucosal lesions in patients taking oral  potassium chloride  tablets.
• May ↑  atenolol  and  metformin  levels.
• May ↓ levels and effectiveness of  haloperidol  and  levodopa.
• May ↓ absorption of  ketoconazole ; administer 2 hr after ketoconazole.

Route/Dosage

Control of Secretions during Surgery

IM (Adults): 4.4 mcg/kg 30–60 min before surgery (not to exceed 0.1 mg).

IM (Children  >2 yr): 4.4 mcg/kg 30–60 min before surgery.

IM (Children  <2 yr): 4.4–8.8 mcg/kg 30–60 min before surgery.

Control of Secretions (chronic)

IM IV (Children): 4–10 mcg/kg/dose every 3–4 hr.

PO (Children): 40–100 mcg/kg/dose 3–4 times/day.

Cholinergic Adjunct

IV (Adults and Children): 200 mcg for each 1 mg of neostigmine or 5 mg of pyridostigmine given at the same time.

Peptic Ulcer

PO (Adults): 1–2 mg 2–3 times daily. An additional 2 mg may be given at bedtime; may be ↓ to 1 mg twice daily (not to exceed 8 mg/day).

IM IV (Adults): 100–200 mcg every 4 hr up to 4 times daily.

Chronic Severe Drooling

PO (Children  3–16 yr): Oral solution:  0.02 mg/kg 3 times daily; may ↑ by 0.02 mg/kg 3 times daily every 5–7 days (not to exceed 0.1 mg/kg 3 times daily or 1.5–3 mg/dose).

Availability (generic available)

Tablets: 1 mg, 1.5 mg, 2 mg

Oral solution (cherry flavor): 1 mg/5 mL

Solution for injection: 200 mcg (0.2 mg)/mL

In Combination with: neostigmine (Prevduo). See combination drugs.

Assessment

• Assess HR, BP, and respiratory rate before and periodically during parenteral therapy.
• Monitor intake and output in older adults or surgical patients; glycopyrrolate may cause urinary retention. Instruct patient to void before parenteral administration.
• Assess routinely for abdominal distention and auscultate for bowel sounds. If constipation occurs, ↑ fluids and add high-fiber foods into diet to help alleviate it.
• Periodic intraocular pressure determinations should be made for patients receiving long-term therapy.

• Pedi:   Monitor amount and frequency of drooling periodically during therapy.

  • Assess for hyperexcitability, a paradoxical response that may occur in children.

Lab Test Considerations:

Antagonizes effects of pentagastrin and histamine during the gastric acid secretion test. Avoid administration for 24 hr preceding the test.

• May ↓ uric acid levels in patients with gout or hyperuricemia.

If overdose occurs, neostigmine is the antidote.

Implementation

• Do not administer cloudy or discolored solution.
• PO Administer 30–60 min before meals to maximize absorption. Do not administer within 1 hr of antacids or antidiarrheal medications.
  • For drooling: Administer >1 hr before or 2 hr after meals.
  • Oral dose is 10 times the parenteral dose.
• IM  Dilution:  Undiluted.  Concentration: 200 mcg/mL.

Patient/Family Teaching

• Explain purpose and side effects of medication to patient. Advise patient to read  Patient Information  before starting therapy. Instruct patient to take as directed and not to take more than the prescribed amount. Take missed doses as soon as remembered if not just before next dose.
• Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications.
• Medication may cause drowsiness and blurred vision. Caution patient to avoid driving or other activities requiring alertness until response to the medication is known.
• Inform patient that frequent oral rinses, sugarless gum or candy, and good oral hygiene may help relieve dry mouth. Consult health care provider regarding use of saliva substitute if dry mouth persists for >2 wk.
• Advise patient to change positions slowly to minimize the effects of drug-induced orthostatic hypotension.
• Caution caregivers and patient to avoid extremes of temperature. This medication ↓ the ability to sweat and may ↑ the risk of heat stroke.
• Advise patient to notify health care provider immediately if eye pain or ↑ sensitivity to light occurs. Emphasize the importance of routine eye exams throughout therapy.
• Rep:  Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.
• Geri:  Advise older adults about ↑ susceptibility to side effects and to call health care provider immediately if they occur.

• Pedi:  Instruct caregivers to use a calibrated measuring device with solution for accurate dosing.

  • Advise caregivers to stop glycopyrrolate and notify health care provider if constipation, signs of urinary retention (inability to urinate, dry diapers or undergarments, irritability, crying), rash, hives, or an allergic reaction occurs.

Evaluation/Desired Outcomes

Decreased GI and respiratory secretions.