Medical term:

Robinul



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.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved

glycopyrrolate

(glye-koe-pye-roe-late) ,

Cuvposa

(trade name),

Robinul

(trade name),

Robinul-Forte

(trade name)

Classification

Therapeutic: antispasmodics
Pharmacologic: anticholinergics
Pregnancy Category: B (oral, parenteral)
Pregnancy Category: C (oral solution)

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.
Intermediate doses result in increased heart rate.
Larger doses decrease GI and GU tract motility.

Therapeutic effects

Decreased GI and respiratory secretions.

Pharmacokinetics

Absorption: Incompletely absorbed (<10%) after oral administration. Well absorbed after IM administration.
Distribution: Distribution not fully known. Does not significantly cross the blood-brain barrier or eye. Crosses the placenta.
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)

ROUTEONSETPEAKDURATION
PO1 hrunknown8–12 hr
IM15–30 min30–45 min2–7 hr*
IV1–10 minunknown2–7 hr*
*Antisecretory effect lasts up to 7 hr; vagal blockade lasts 2–3 hr

Contraindications/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 dosage forms (oral solution only); Pediatric: Injection contains benzyl alcohol and should not be given to neonates.
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); Obstetric / Lactation: Safety not established; Pediatric: ↑ sensitivity to anticholinergic effects and adverse reactions; Geriatric: ↑ sensitivity to anticholinergic effects and adverse reactions.

Adverse Reactions/Side Effects

Central nervous system

  • headache (most frequent)
  • confusion
  • drowsiness

Ear, Eye, Nose, Throat

  • nasal congestion (most frequent)
  • blurred vision
  • cycloplegia
  • dry eyes
  • mydriasis

Cardiovascular

  • tachycardia (most frequent)
  • orthostatic hypotension
  • palpitations

Gastrointestinal

  • dry mouth (most frequent)
  • vomiting (most frequent)
  • constipation

Genitourinary

  • urinary hesitancy (most frequent)
  • urinary retention

Dermatologic

  • flushing (most frequent)

Interactions

Drug-Drug interaction

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 adsorbentantidiarrheal agents ↓ absorption of anticholinergics.May ↑ GI mucosal lesions in patients taking oral potassium chloride tablets.May ↑ atenolol and metformin levels.May ↓ levels of haloperidol and levodopa.Concurrent use may ↓ absorption of ketoconazole (administer 2 hr after ketoconazole).

Route/Dosage

Control of Secretions during Surgery
Intramuscular (Adults) 4.4 mcg/kg 30–60 min preop (not to exceed 0.1 mg).
Intramuscular (Children > 2 yr) 4.4 mcg/kg 30–60 min preop.
Intramuscular (Children < 2 yr) 4.4–8.8 mcg/kg 30–60 min preop.
Control of Secretions (chronic)
Intramuscular Intravenous (Children) 4–10 mcg/kg/dose q 3–4 hr.
Oral (Children) 40–100 mcg/kg/dose 3–4 times/day.
Cholinergic Adjunct
Intravenous (Adults and Children) 200 mcg for each 1 mg of neostigmine or 5 mg of pyridostigmine given at the same time.
Antiarrhythmic
Intravenous (Adults) 100 mcg, may be repeated q 2–3 min.
Intravenous (Children) 4.4 mcg/kg (up to 100 mcg); may be repeated q 2–3 min.
Peptic Ulcer
Oral (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).
Intramuscular Intravenous (Adults) 100–200 mcg q 4 hr up to 4 times daily.
Chronic Severe Drooling
Oral (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, 2 mg
Injection: 200 mcg (0.2 mg)/mL
Oral solutioncherry-flavor: 1 mg/5 mL

Nursing implications

Nursing assessment

  • Assess heart rate, BP, and respiratory rate before and periodically during parenteral therapy.
  • Monitor intake and output ratios in geriatric or surgical patients; glycopyrrolate may cause urinary retention. Instruct patient to void before parenteral administration.
  • Assess patient routinely for abdominal distention and auscultate for bowel sounds. If constipation becomes a problem, increasing fluids and adding bulk to the diet may help alleviate the constipating effects of the drug.
  • Periodic intraocular pressure determinations should be made for patients receiving long-term therapy.
  • Pediatric: 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 cause ↓ uric acid levels in patients with gout or hyperuricemia.
  • If overdose occurs, neostigmine is the antidote.

Potential Nursing Diagnoses

Impairedoral mucous membrane (Side Effects)
Constipation (Side Effects)

Implementation

  • Do not administer cloudy or discolored solution.
  • Oral: Administer 30–60 min before meals to maximize absorption.
    • For drooling: Administer at least 1 hr before or 2 hr after meals.
    • Do not administer within 1 hr of antacids or antidiarrheal medications.
    • Oral dose is 10 times the parenteral dose.
  • Intramuscular: May be administered undiluted (200 mcg/mL).
  • Intravenous Administration
  • pH: 2.0–3.0.
  • Diluent: May be given undiluted through Y-site.Concentration: 200 mcg/mL.
  • Rate: Administer at a maximum rate of 20 mcg over 1 min.
  • Y-Site Compatibility: acyclovir, alfentanil, amikacin, aminophylline, anidulafungin, argatroban, ascorbic acid, atracurium, atropine, azithromycin, aztreonam, benztropine, bivalirudin, bleomycin, bumetanide, buprenorphine, butorphanol, calcium chloride, calcium gluconate, carmustine, caspofungin, cefazolin, cefoperazone, cefotaxime, cefotetan, cefoxitin, ceftazidime, ceftriaxone, cefuroxime, chloramphenicol, chlorpromazine, cisplatin, clindamycin, cyanocobalamin, cyclosporine, dactinomycin, daptomycin, dexamethasone, dexmedetomidine, digoxin, diltiazem, diphenhydramine, dobutamine, docetaxel, dopamine, doxycycline, enalaprilat, ephedrine, epinephrine, epoetin alfa, ertapenem, erythromycin, esmolol, etoposide, etoposide phosphate, famotidine, fenoldopam, fentanyl, fluconazole, fludarabine, folic acid, ganciclovir, gemcitabine, gentamicin, granisetron, heparin, hydrocortisone, hydromorphone, idarubicin, imipenem/cilastatin, isoproterenol, ketorolac, labetalol, lidocaine, linezolid, lorazepam, magnesium sulfate, mannitol, mechlorethamine, meperidine, metaraminol, methoxamine, methyldopate, methylprednisolone, metoclopramide, metoprolol, metronidazole, midazolam, milrinone, mitoxantrone, morphine, multivitamins, mycophenolate, nafcillin, nalbuphine, naloxone, nesiritide, nitroglycerin, nitroprusside, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, paclitaxel, palonosetron, pamidronate, pancuronium, papaverine, pemetrexed, penicillin G, pentamidine, pentazocine, pentobarbital, phenobarbital, phentolamine, phenylephrine, phytonadione, potassium acetate, potassium chloride, procainamide, promethazine, propofol, propranolol, protamine, pyridoxime, ranitidine, sodium bicarbonate, streptokinase, succinylcholine, sufentanil, tacrolimus, teniposide, theophylline, thiamine, thiotepa, ticarcillin/clavulanate, tigecycline, tirofiban, tobramycin, tolazoline, trimetaphan, vancomycin, vasopressin, vecruonium, verapamil, vinorelbine, voriconazole, zoledronic acid
  • Y-Site Incompatibility: amphotericin B colloidal, amphotericin B lipid complex, dantrolene, diazepam, diazoxide, indomethacin, irinotecan, pantoprazole, phenytoin, piperacillin/tazobactam, trimethoprim/sulfamethoxazole
  • Solution Compatibility: D5/0.45% NaCl, D5W, 0.9% NaCl, Ringer’s solution. Administer immediately after admixing
  • Additive Incompatibility: methylprednisolone sodium succinate

Patient/Family Teaching

  • Instruct patient to take glycopyrrolate as directed and not to take more than the prescribed amount. Take missed doses as soon as remembered if not just before next dose.
  • 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 professional regarding use of saliva substitute if dry mouth persists for more than 2 wk.
  • Advise patient to change positions slowly to minimize the effects of drug-induced orthostatic hypotension.
  • Caution patient to avoid extremes of temperature. This medication decreases the ability to sweat and may increase the risk of heat stroke.
  • Advise patient to notify health care professional immediately if eye pain or increased sensitivity to light occurs. Emphasize the importance of routine eye exams throughout therapy.
  • Advise patient to consult health care professional before taking any OTC medications concurrently with this therapy.
  • Geriatric: Advise geriatric patients about increased susceptibility to side effects and to call health care professional immediately if they occur.
  • Pediatric: Instruct parents to use a calibrated measuring device with solution for accurate dosing.
    • Advise parents to stop glycopyrrolate and notify health care professional if constipation; signs of urinary retention (inability to urinate, dry diapers or undergarments, irritability or crying); or rash, hives, or an allergic reaction occurs.
    • Glycopyrrolate reduces sweating. Advise parents to avoid exposure of the patient to hot or very warm environmental temperatures to avoid overheating and heat exhaustion or heat stroke.

Evaluation/Desired Outcomes

  • Mouth dryness preoperatively.
  • Reversal of cholinergic medications.
  • Decrease in GI motility and pain in patients with peptic ulcer disease.
  • Reduce chronic severe drooling in children with neurologic conditions associated with drooling.
Drug Guide, © 2015 Farlex and Partners

Robinul

A brand name for GLYCOPYRRONIUM BROMIDE.
Collins Dictionary of Medicine © Robert M. Youngson 2004, 2005


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