Generic Name
Glycopyrrolate
Brand Names
Robinul, Glyrx-Pf, Dartisla Odt, Cuvposa, Bevespi, Prevduo, Glycate
FDA approval date: February 06, 1975
Classification: Cholinergic Muscarinic Antagonist
Form: Injection, Aerosol, Tablet, Liquid, Solution
What is Robinul (Glycopyrrolate)?
In Anesthesia Glycopyrrolate injection is indicated for use as a preoperative antimuscarinic to reduce salivary, tracheobronchial, and pharyngeal secretions; to reduce the volume and free acidity of gastric secretions; and to block cardiac vagal inhibitory reflexes during induction of anesthesia and intubation. When indicated, glycopyrrolate injection may be used intraoperatively to counteract surgically or drug- induced or vagal reflexes associated arrhythmias. Glycopyrrolate protects against the peripheral muscarinic effects of cholinergic agents such as neostigmine and pyridostigmine given to reverse the neuromuscular blockade due to non-depolarizing muscle relaxants. In Peptic Ulcer For use in adults as adjunctive therapy for the treatment of peptic ulcer when rapid anticholinergic effect is desired or when oral medication is not tolerated.
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Brand Information
Robinul (Robinul)
1DESCRIPTION
ROBINUL (glycopyrrolate) Injection is a synthetic anticholinergic agent. Each 1 mL contains:
Glycopyrrolate, USP 0.2 mg
For Intramuscular (IM) or Intravenous (IV) administration.
Glycopyrrolate is a quaternary ammonium salt with the following chemical name: 3[(cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethyl pyrrolidinium bromide. The molecular formula is C
Its structural formula is as follows:
C
Unlike atropine, glycopyrrolate is completely ionized at physiological pH values. ROBINUL (glycopyrrolate) Injection is a clear, colorless, sterile liquid; pH 2.0– 3.0. The partition coefficient of glycopyrrolate in a n-octanol/water system is 0.304 (log
2CLINICAL PHARMACOLOGY
Glycopyrrolate, like other anticholinergic (antimuscarinic) agents, inhibits the action of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, exocrine glands and, to a limited degree, in the autonomic ganglia. Thus, it diminishes the volume and free acidity of gastric secretions and controls excessive pharyngeal, tracheal, and bronchial secretions.
Glycopyrrolate antagonizes muscarinic symptoms (e.g., bronchorrhea, bronchospasm, bradycardia, and intestinal hypermotility) induced by cholinergic drugs such as the anticholinesterases.
The highly polar quaternary ammonium group of glycopyrrolate limits its passage across lipid membranes, such as the blood-brain barrier, in contrast to atropine sulfate and scopolamine hydrobromide, which are highly non-polar tertiary amines which penetrate lipid barriers easily.
With intravenous injection, the onset of action is generally evident within one minute. Following intramuscular administration, the onset of action is noted in 15 to 30 minutes, with peak effects occurring within approximately 30 to 45 minutes. The vagal blocking effects persist for 2 to 3 hours and the antisialagogue effects persist up to 7 hours, periods longer than for atropine.
2.1Pharmacokinetics
The following pharmacokinetic information and conclusions were obtained from published studies that used nonspecific assay methods.
2.1.1DISTRIBUTION
The mean volume of distribution of glycopyrrolate was estimated to be 0.42±0.22 L/kg.
2.1.2METABOLISM
The
2.1.3EXCRETION
The mean clearance and mean T
3CONTRAINDICATIONS
Known hypersensitivity to glycopyrrolate or any of its inactive ingredients.
In addition, in the management of
4WARNINGS
This drug should be used with great caution, if at all, in patients with glaucoma.
Exposure to excessive amounts of benzyl alcohol has been associated with toxicity (hypotension, metabolic acidosis), particularly in neonates, and an increased incidence of kernicterus, particularly in small preterm infants. There have been rare reports of deaths, primarily in preterm infants, associated with exposure to excessive amounts of benzyl alcohol. The amount of benzyl alcohol from medications is usually considered negligible compared to that received in flush solutions containing benzyl alcohol. Administration of high dosages of medications containing this preservative must take into account the total amount of benzyl alcohol administered. The amount of benzyl alcohol at which toxicity may occur is not known. If the patient requires more than the recommended dosages or other medications containing this preservative, the practitioner must consider the daily metabolic load of benzyl alcohol from these combined sources (see
ROBINUL Injection may produce drowsiness or blurred vision. The patient should be cautioned regarding activities requiring mental alertness such as operating a motor vehicle or other machinery or performing hazardous work while taking this drug.
In addition, in the presence of fever, high environmental temperature and/or during physical exercise, heat prostration can occur with use of anticholinergic agents including glycopyrrolate (due to decreased sweating), particularly in children and the elderly.
Diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. In this instance treatment with ROBINUL Injection would be inappropriate and possibly harmful.
5ADVERSE REACTIONS
Anticholinergics, including ROBINUL Injection, can produce certain effects, most of which are extensions of their pharmacologic actions. Adverse reactions may include xerostomia (dry mouth); urinary hesitancy and retention; blurred vision and photophobia due to mydriasis (dilation of the pupil); cycloplegia; increased ocular tension; tachycardia; palpitation; decreased sweating; loss of taste; headache; nervousness; drowsiness; weakness; dizziness; insomnia; nausea; vomiting; impotence; suppression of lactation; constipation; bloated feeling; severe allergic reactions including anaphylactic/anaphylactoid reactions; hypersensitivity; urticaria, pruritus, dry skin, and other dermal manifestations; some degree of mental confusion and/or excitement, especially in elderly persons.
In addition, the following adverse events have been reported from post-marketing experience with ROBINUL: malignant hyperthermia; cardiac arrhythmias (including bradycardia, ventricular tachycardia, ventricular fibrillation); cardiac arrest; hypertension; hypotension; seizures; and respiratory arrest. Post-marketing reports have included cases of heart block and QTc interval prolongation associated with the combined use of glycopyrrolate and an anticholinesterase. Injection site reactions including pruritus, edema, erythema, and pain have also been reported.
ROBINUL is chemically a quaternary ammonium compound; hence, its passage across lipid membranes, such as the blood-brain barrier is limited in contrast to atropine sulfate and scopolamine hydrobromide. For this reason the occurrence of CNS-related side effects is lower, in comparison to their incidence following administration of anticholinergics which are chemically tertiary amines that can cross this barrier readily.
6OVERDOSAGE
To combat peripheral anticholinergic effects, a quaternary ammonium anticholinesterase such as neostigmine methylsulfate (which does not cross the blood-brain barrier) may be given intravenously in increments of 0.25 mg in adults. This dosage may be repeated every five to ten minutes until anticholinergic overactivity is reversed or up to a maximum of 2.5 mg. Proportionately smaller doses should be used in pediatric patients. Indication for repetitive doses of neostigmine should be based on close monitoring of the decrease in heart rate and the return of bowel sounds.
If CNS symptoms (e.g., excitement, restlessness, convulsions, psychotic behavior) occur, physostigmine (which does cross the blood–brain barrier) may be used. Physostigmine 0.5 to 2 mg should be slowly administered intravenously and repeated as necessary up to a total of 5 mg in adults. Proportionately smaller doses should be used in pediatric patients.
To combat hypotension, administer IV fluids and/or pressor agents along with supportive care.
Fever should be treated symptomatically.
Following overdosage, a curare-like action may occur, i.e., neuromuscular blockade leading to muscular weakness and possible paralysis. In the event of a curare-like effect on respiratory muscles, artificial respiration should be instituted and maintained until effective respiratory action returns.
7DOSAGE AND ADMINISTRATION
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.
ROBINUL Injection may be administered intramuscularly, or intravenously, without dilution, in the following indications.
7.1Pediatric Patients
(see
7.1.1PREANESTHETIC MEDICATION
The recommended dose of ROBINUL Injection in pediatric patients is 0.004 mg/kg intramuscularly, given 30 to 60 minutes prior to the anticipated time of induction of anesthesia or at the time the preanesthetic narcotic and/or sedative are administered.
7.1.2INFANTS
(1 month to 2 years of age) may require up to 0.009 mg/kg.
7.1.3INTRAOPERATIVE MEDICATION
Because of the long duration of action of ROBINUL Injection if used as preanesthetic medication, additional ROBINUL Injection for anticholinergic effect intraoperatively is rarely needed; in the event it is required the recommended pediatric dose is 0.004 mg/kg intravenously, not to exceed 0.1 mg in a single dose which may be repeated, as needed, at intervals of 2 to 3 minutes. The usual attempts should be made to determine the etiology of the arrhythmia, and the surgical or anesthetic manipulations necessary to correct parasympathetic imbalance should be performed.
7.1.4REVERSAL OF NEUROMUSCULAR BLOCKADE
The recommended pediatric dose of ROBINUL Injection is 0.2 mg for each 1.0 mg of neostigmine or 5.0 mg of pyridostigmine. In order to minimize the appearance of cardiac side effects, the drugs may be administered simultaneously by intravenous injection and may be mixed in the same syringe.
7.1.5PEPTIC ULCER
ROBINUL Injection is not recommended for the treatment of peptic ulcer in pediatric patients (see
7.2Diluent Compatibilities
Dextrose 5% and 10% in water, or saline, dextrose 5% in sodium chloride 0.45%, sodium chloride 0.9%, and Ringer’s Injection.
7.3Diluent Incompatibilities
Lactated Ringer’s solution
8HOW SUPPLIED
ROBINUL (glycopyrrolate) Injection, 0.2 mg/mL, is available in:
1 mL single dose vials packaged in 25s (NDC 0641-6104-25)
Store at controlled room temperature, between 20°C and 25°C (68°F and 77°F).
To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceuticals Corp. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or
For Product Inquiry call 1-877-845-0689.
Manufactured by:
WEST-WARDA HIKMA COMPANY
Eatontown, NJ 07724 USA
Eatontown, NJ 07724 USA
Revised June 2017
462-185-06
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