Glycopyrrolate – Uses

Background

Glycopyrrolate, also known as glycopyrronium, is an anticholinergic drug. It is a synthetically created quaternary amine with pyridine and a cyclopentane moiety within the compound’s structure. Glycopyrrolate has been widely used as a preoperative medication to inhibit salivary gland and respiratory secretions. The most frequent reasons for administering anticholinergics include producing an antisialagogue effect, creating a sedative and amnesic effect, and preventing reflex bradycardia. Anticholinergics are not predictably effective in increasing gastric fluid pH or decreasing gastric fluid volume. Glycopyrrolate is among the most commonly used anticholinergic medications.

Properties and Characteristics of Glycopyrrolate

Drug class	Anticholinergic drug
Brand Names	Cuvposa, Dartisla ODT, Glycate, Robinul, Robinul Forte
Synonyms	Glicopirronio, Glycopyrrolate, Glycopyrrolate ion, Glycopyrronium, Glycopyrronium ion
Molecular Formula	C19H28NO3
Molecular Weight	398.3 g/mol
IUPAC Names	(1,1-dimethylpyrrolidin-1-ium-3-yl) 2-cyclopentyl-2-hydroxy-2-phenylacetate;bromide
Structural formula of main component
Pure active ingredient	Glycopyrrolate
Appearance	White and odourless crystalline powder
Melting Point	193.2-194.5°
Solubility	Soluble in water
Excretion	Urinary excretion and elimination
Available as	Tablets, Injection, Suspension, Aerosol
Storage	Storage in a cool, dry area protected from light before administration
Prescription	Prescription is required

What is Glycopyrrolate (Robinul) used for?

• Anesthesia
• Chronic Obstructive Pulmonary Disease — Maintenance
• Zollinger-Ellison Syndrome
• Peptic Ulcer
• Peptic Ulcer with Hemorrhage
• Peptic Ulcer with Hemorrhage and Perforation
• Peptic Ulcer with Perforation
• Peptic Ulcer with Hemorrhage and Obstruction
• Peptic Ulcer with Perforation and Obstruction
• Peptic Ulcer with Hemorrhage/Perforation/Obstruction
• Peptic Ulcer with Obstruction
• Excessive Salivation

Glycopyrrolate side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Glycopyrrolate may cause serious side effects. Stop using glycopyrrolate and call your doctor at once if you have:

• Severe constipation, severe stomach pain and bloating;
• Diarrhea (especially if you have a colostomy or ileostomy);
• Painful or difficult urination;
• Fast or pounding heartbeats, fluttering in your chest;
• Confusion, severe drowsiness;
• Eye pain, seeing halos around lights;
• Fever, shallow breathing, weak pulse, hot and red skin; or
• (In a child taking glycopyrrolate) dry diapers, fussiness, or excessive crying.

Common side effects of glycopyrrolate may include:

• Constipation, nausea, vomiting, bloating;
• Drowsiness, dizziness, weakness, feeling nervous;
• Slow or fast heartbeats;
• Sleep problems (insomnia);
• Flushing (sudden warmth, redness, or tingly feeling);
• Blurred vision, sensitivity to light;
• Dry mouth, decreased sense of taste;
• Decreased sweating, decreased urination;
• Impotence, sexual problems;
• Headache;

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

Mechanism of action

Glycopyrronium is a muscarinic antagonist with the highest affinity for M1 receptors, followed by M3, M2/M4, and M5.

Muscarinic receptors M1 to M4 are found in the lung, although M3 is predominantly responsible for bronchoconstriction and airway secretions. Secretions from salivary and sweat glands, as well as gastric acid secretions, are also predominantly mediated by the M3 receptor. Salivary and gastric acid secretions are also partially mediated by the M1 receptor. Antagonism of these receptors decreases the volume of their respective secretions, and in the case of the gastrointestinal system, reduces the acidity of the stomach.

In the cardiovascular system, muscarinic receptors M1 to M5 are all present, however the function of M5 has not been described in literature. Under normal circumstances, stimulation of the vagal nerve lowers the heart rate, potentially leading to intraoperative bradycardia. Studies in mice suggest that this stimulation is predominantly mediated by the M3 receptor, and mutant knockout mice are not susceptible to these effects.

Drug Interactions

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Potassium Chloride
• Potassium Citrate

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Aclidinium
• Belladonna
• Carbinoxamine
• Darifenacin
• Fesoterodine
• Glucagon
• Homatropine
• Imipramine
• Loxapine
• Meclizine
• Nortriptyline
• Olanzapine
• Paroxetine
• Quetiapine
• Revefenacin
• Scopolamine
• Terodiline
• Umeclidinium

Other Interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor’s orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For peptic ulcers

For oral dosage form (tablet):

• Adults and children 12 years of age and older—The initial dose is 1 milligram (mg) 3 times a day. Your doctor will adjust the dose as needed. However, the dose is usually not more than 8 mg per day.
• Children younger than 12 years of age—Use is not recommended.

For oral dosage form (disintegrating tablet):

• Adults—1.7 milligrams (mg) 2 to 3 times a day. Your doctor will adjust the dose as needed. However, the dose is usually not more than 6.8 mg per day.
• Children—Use and dose must be determined by your doctor.

For severe drooling

For oral dosage form (solution):

• Children 3 to 16 years of age—Dose is based on body weight and must be determined by your child’s doctor. The dose is 0.02 milligram (mg) per kilogram (kg) of body weight 3 times a day. Your child’s doctor may increase your child’s dose as needed. However, the dose is usually not more than 1.5 to 3 mg per dose.
• Children younger than 3 years of age—Use and dose must be determined by your child’s doctor.

Overdose

Get emergency help immediately if any of the following symptoms of overdose occur:

• Blurred vision
• Confusion
• Dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
• Muscle weakness
• Sweating
• Trouble breathing
• Unusual tiredness or weakness

What special precautions should I follow?

Before taking glycopyrrolate,

• Tell your doctor and pharmacist if you are allergic to glycopyrrolate, any other medications, or any of the ingredients in glycopyrrolate tablets or solution. Ask your pharmacist for a list of the ingredients.
• Tell your doctor if you are taking extended-release (long-acting) potassium chloride tablets or capsules. Your doctor may tell you not to take glycopyrrolate if you are taking this medication.
• Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: amantadine (Symmetrel); atenolol (Tenormin, in Tenoretic); digoxin (Lanoxin); levodopa (in Rytary, in Sinemet, in Stavelo); ipratropium (Atrovent); mediations for anxiety, irritable bowel disease, mental illness, motion sickness, Parkinson’s disease, seizures, ulcers, or urinary problems; sedatives; tranquilizers; and tricyclic antidepressants such as amitriptyline, amoxapine (Asendin), clomipramine (Anafranil), desipramine (Norpramin), doxepin (Sinequan), imipramine (Tofranil), nortriptyline (Aventyl, Pamelor), protriptyline (Vivactil), and trimipramine (Surmontil); Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with glycopyrrolate, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
• Tell your doctor if you have or have ever had glaucoma; difficulty urinating; a blockage or narrowing of your stomach or intestines, paralytic ileus (condition in which digested food does not move through the intestines) toxic megacolon (a serious or life-threatening widening of the intestine), or myasthenia gravis (a disorder of the nervous system that causes muscle weakness). Your doctor may tell you not to take glycopyrrolate.
• Tell your doctor if you have or have ever had enlargement of the prostate, ulcerative colitis (a condition which causes swelling and sores in the lining of the colon [large intestine] and rectum), overactive thyroid, high blood pressure, heart failure, irregular or rapid heartbeats, coronary artery disease, hiatal hernia with reflux, disorders of the nervous system, or kidney or liver disease.
• Tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking glycopyrrolate, call your doctor.
• If you are having surgery, including dental surgery, tell the doctor or dentist that you are taking glycopyrrolate.
• You should know that glycopyrrolate may make you drowsy or cause blurred vision. Do not drive a car or operate machinery until you know how this medication affects you.
• You should know that glycopyrrolate reduces the body’s ability to cool off by sweating. Avoid being in hot or very warm temperatures. If you experience any of the following symptoms, call your doctor immediately: lack of sweating in hot weather; hot, red skin; decreased alertness; loss of consciousness; fast, weak pulse; fast, shallow breathing; or fever.