Glycopyrrolate

Trade Names:Robinul- Tablets 1 mg- Injection 0.2 mg/mL

Trade Names:Robinul Forte- Tablets 2 mg

Pharmacology

Exerts anticholinergic effects, resulting in GI smooth muscle relaxation, diminished volume and acidity of GI secretions, and reduced pharyngeal, tracheal, and bronchial secretions.

Pharmacokinetics

Absorption

Absorption is poor and unreliable.

Distribution

Highly polar ammonium group of glycopyrrolate limits its passage across blood-brain barrier and other lipid membranes.

Onset

Within 1 min after IV injection.

Peak

30 to 45 min after IM administration.

Duration

Vagal blocking effects persist for 2 to 3 h. Antisialagogue effects persist up to 7 hours.

Indications and Usage

Adjunctive treatment of peptic ulcer.

Preoperative administration for reduction of salivary, tracheobronchial and pharyngeal secretions, reduction of volume and acidity of gastric secretions, and blockade of cardiac vagal inhibitory reflexes before and during induction of anesthesia and intubation; intraoperatively for counteraction of drug-induced or vagal traction reflexes with associated arrhythmias.

Contraindications

Narrow angle glaucoma; adhesions between iris and lens; obstructive uropathy; obstructive disease of GI tract; paralytic ileus; intestinal atony of elderly or debilitated patients; severe ulcerative colitis; toxic megacolon complicating ulcerative colitis; hepatic or renal disease; tachycardia; myocardial ischemia; unstable cardiovascular status in acute hemorrhage; myasthenia gravis.

Dosage and Administration

PO 1 to 2 mg 2 or 3 times daily. IM/IV 0.1 to 0.2 mg 3 or 4 times daily.

IM 0.004 mg/kg 20 min to 1 h prior to anesthesia.

IM 0.0044 to 0.0088 mg/kg.

IM up to 0.0088 mg/kg.

IV 0.1 mg. May repeat at 2 to 3 min intervals.

IV 0.004 mg/kg (max 0.1 mg in single dose); may repeat at 2 to 3 min intervals.

IV 0.2 mg for each 1 mg neostigmine or 5 mg pyridostigmine. Administer simultaneously.

General Advice

• For IM administration, give drug undiluted or mixed with D5W, D10W, or sodium chloride 0.9%.
• May administer undiluted drug IV.
• Do not administer parenteral solution if cloudy.

Storage/Stability

Store parenteral and oral formulations at room temperature.

Drug Interactions

May cause decreased serum haloperidol levels, worsened schizophrenic symptoms, and tardive dyskinesia.

Incompatibility

Because stability of glycopyrrolate is questionable above pH of 6, do not combine in same syringe with methohexital sodium, chloramphenicol sodium succinate, dimenhydrinate, pentobarbital sodium, thiopental sodium, secobarbital sodium, sodium bicarbonate, diazepam, dexamethasone sodium phosphate, or buffered solution of Lactated Ringer's solution.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations; tachycardia; orthostatic hypotension.

CNS

Headache; flushing; nervousness; drowsiness; weakness; dizziness; confusion; insomnia; fever (especially in children); mental confusion or excitement (especially in elderly, even with small doses); CNS stimulation (restlessness, tremor, hallucinations).

Dermatologic

Severe allergic reactions including anaphylaxis, urticaria, and dermal manifestations.

EENT

Blurred vision; mydriasis; photophobia; cycloplegia; increased IOP; dilated pupils; nasal congestion.

GI

Dry mouth; altered taste perception; nausea; vomiting; dysphagia; heartburn; constipation; bloated feeling; paralytic ileus.

Genitourinary

Urinary hesitancy and retention; impotence.

Miscellaneous

Suppression of lactation; decreased sweating.

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Not recommended for treatment of peptic ulcer in children younger than 12 yr of age.

Elderly

May react with excitement, agitation, drowsiness, and other untoward manifestations even with small doses.

Special Risk Patients

Use with caution in patients with autonomic neuropathy, hepatic or renal disease, ulcerative colitis, hyperthyroidism, coronary heart disease, CHF, cardiac tachyarrhythmias, hypertension, prostatic hypertrophy, hiatal hernia associated with reflux esophagitis.

Anticholinergic psychosis

Reported in sensitive individuals; may include confusion, disorientation, short-term memory loss, hallucinations, dysarthria, ataxia, coma, euphoria, anxiety, fatigue, insomnia, agitation, and inappropriate affect.

Diarrhea

May be symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. Treatment of diarrhea with drug is inappropriate and possibly harmful.

Gastric ulcer

May delay gastric emptying rate and complicate therapy.

Heat prostration

Can occur in presence of high environmental temperature.

Overdosage

Symptoms

Dry mouth, thirst, vomiting, nausea, abdominal distention, difficulty swallowing, muscular weakness, paralysis, fever, coma, circulatory failure, rapid pulse and respiration, vasodilation, tachycardia with weak pulse, hypertension, hypotension, respiratory depression, palpitations.

Patient Information

• Instruct patient that constipation can occur and to institute preventive measures (eg, increase fluids, bulk in diet, and activity).
• Advise patient that urinary hesitancy or retention may be experienced. Instruct patient to assess urination patterns and to notify health care provider if urinary retention is experienced.
• Inform men that impotence is potential adverse reaction and to report this symptom to health care provider.
• Because drug interferes with body's thermoregulation, instruct patient to avoid exposure to high environmental temperature to prevent heat prostration.
• Instruct patient to notify health care provider immediately if eye pain or increased sensitivity to light occurs. Emphasize importance of routine eye examinations throughout therapy.
• Inform patient that dry mouth is a normal adverse reaction. Instruct patient to take sips of water frequently, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
• Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
• Advise patient that drug may cause drowsiness and blurred vision and to use caution while driving or performing other tasks requiring mental alertness.

Copyright © 2009 Wolters Kluwer Health.