Glycopyrrolate: Uses, Mechanism, and Considerations

Glycopyrrolate, also known as glycopyrronium, is an anticholinergic medication with a wide range of applications in various medical settings. It functions primarily as a muscarinic receptor antagonist. This article explores the uses of glycopyrrolate, its mechanism of action, potential side effects, and important considerations for its use.

Indications and Uses

Glycopyrrolate is indicated for several conditions, including:

• Preoperative Medication: It is widely used preoperatively to inhibit salivary gland and respiratory secretions, producing an antisialagogue, sedative, or amnesic effect and to prevent reflex bradycardia. Glycopyrrolate is among the most commonly used anticholinergic medications for these purposes. Clinicians use glycopyrrolate to reduce pharyngeal, tracheal, bronchial, and sialagogue effects preoperatively; decreased secretions are the desired effect during anesthesia when a tracheal tube is in place. A blockade of reflexive vagal cardiac inhibition reflexes may also occur during intubation and anesthetic induction.
• Hyperhidrosis: The topical formulation of glycopyrrolate is indicated to treat primary axillary hyperhidrosis in patients 9 years and older.
• Drooling: Glycopyrrolate is helpful in reducing severe or chronic drooling in pediatric patients with neurologic conditions, such as cerebral palsy.
• Reversal of Vagal Reflexes and Neuromuscular Blockade: The intravenous formulation of glycopyrrolate classically reverses vagal reflexes and bradycardia intraoperatively and reverses the muscarinic effects of cholinergic agents such as neostigmine or pyridostigmine. Glycopyrrolate may be administered to reverse the neuromuscular blockade due to nondepolarizing muscle relaxants postoperatively and is frequently used in conjunction with neostigmine, a cholinesterase inhibitor.
• Chronic Obstructive Pulmonary Disease (COPD): Various oral inhalation formulations of glycopyrrolate are indicated for the long-term maintenance treatment of airflow obstruction in patients with COPD. Inhaled glycopyrrolate is used to treat air flow blockage and prevent worsening of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. COPD is a long-term lung disease that causes bronchospasm (difficulty with breathing). Glycopyrrolate is available only with your doctor's prescription.

Glycopyrrolate is also commonly used to reduce burning, pain, and other symptoms of stomach ulcers. It may also be used in people with medical conditions that cause too much drooling. Glycopyrrolate may also be used for other conditions as determined by your healthcare provider.

Mechanism of Action

Glycopyrrolate's primary mechanism of action is the blockage of acetylcholine's effects at the parasympathetic sites in various tissues. This blockage primarily occurs in the central nervous system, smooth muscle, and secretory glands. Glycopyrrolate also reduces the rate of salivation by preventing the stimulation of the acetylcholine receptors themselves. Muscarinic receptor sites are located in the brain's cerebral cortex, thalamus, hippocampus, and reticular activating system. They are also present in the postganglionic parasympathetic nervous system and other sites like sweat glands.

Pharmacokinetics and Administration

Glycopyrrolate has a 2 to 4-hour duration of action after intravenous administration, while atropine has 30 minutes.

Read also: Weight Loss Guide Andalusia, AL

Injection

Glycopyrrolate comes packaged as a 0.2 mg/mL solution for injection. Before intravenous administration, the syringe should be inspected to ensure no particulate matter. Intramuscular or intravenous administration requires no dilution and should be at 0.2 mg over 1 to 2 minutes. Additionally, it may be administered via the tubing of a running intravenous infusion of a compatible solution. The drug should be stored in a cool, dry area protected from light before administration. Any unused solution should be discarded as it is unstable at a pH greater than 6.

Oral

Glycopyrrolate tablets are available in 1 mg, 1.5 mg, and 2 mg strengths. The oral solution is available in a 1 mg/5 mL formulation.

Pregnancy and Breastfeeding Considerations

Typical glycopyrrolate doses do not influence the fetal heart rate or fetal heart rate variability to a significant extent. After parenteral administration, there is a low concentration of glycopyrrolate in umbilical venous and arterial blood and the amniotic fluid. Glycopyrrolate does not appear to penetrate through the placental barrier significantly. As animal reproduction studies are not consistently predictive of human response, this drug should be used during pregnancy only if needed.

Glycopyrrolate is a quaternary ammonium compound; it is not likely to be absorbed and reach the infant's bloodstream, particularly when inhaled or applied topically on the skin. Long-term oral use of glycopyrrolate might reduce milk production or milk letdown, but a single dose is unlikely to interfere with breastfeeding.

Renal and Hepatic Impairment

According to product labeling, dose adjustments may be necessary for patients with renal impairment. The product labeling does not provide information about patients with impaired liver function.

Read also: Beef jerky: A high-protein option for shedding pounds?

Pediatric Patients

Glycopyrrolate should generally be avoided in neonates. Patients receiving higher than recommended dosages can potentially experience a hyperexcitability reaction. Use of inhaled glycopyrrolate is not recommended in children. Safety and efficacy have not been established.

Potential Adverse Effects

Potential adverse reactions associated with glycopyrrolate administration include anticholinergic symptoms such as mydriasis, hyperthermia, tachycardia, and cardiac arrhythmia. They may also include blurred vision, constipation, cycloplegia, dry mouth, dry skin, flushing, photophobia, urinary retention, and xerophthalmia. Glycopyrrolate may affect the patient's ability to perform tasks requiring mental alertness. For example, patients may not be able to operate heavy machinery safely. Additionally, the medication may induce drowsiness or blurred vision, which is exacerbated by the consumption of alcohol.

Other potential adverse effects include dry mouth, difficulty urinating, headaches, diarrhea, and constipation.

Serious Side Effects

While less common, the most serious side effects of glycopyrrolate are described below, along with what to do if they happen.

• Severe Allergic Reactions. Glycopyrrolate may cause allergic reactions, which can be serious. Stop taking glycopyrrolate and get help right away if you have any of the following symptoms of a serious allergic reaction:

  Read also: Inspiring Health Transformation

  • Breathing problems or wheezing
  • Racing heart
  • Fever or general ill feeling
  • Swollen lymph nodes
  • Swelling of the face, lips, mouth, tongue, or throat
  • Trouble swallowing or throat tightness
  • Itching, skin rash, or pale red bumps on the skin called hives
  • Nausea or vomiting
  • Dizziness, feeling lightheaded, or fainting
  • Stomach cramps
  • Joint pain

• Constipation. Some people taking glycopyrrolate may develop severe constipation that could require a hospital stay. Stop taking glycopyrrolate and get help right away if you have severe constipation.

• Blockage of the Gut. Some people taking glycopyrrolate may develop a blockage of the gut, especially if they have an ileostomy or colostomy (openings made in the belly to collect poop). Stop taking glycopyrrolate and call your healthcare provider right away if you have diarrhea. This can be an early sign that you have a blockage in your gut.

• Body Temperature Regulation. Glycopyrrolate can affect your ability to regulate your body temperature. This could make you become very hot, especially in hot weather or after exercising a lot. You should drink water and avoid overheating and dehydration. Call your healthcare provider right away if you are severely ill and have the following symptoms:

  • Excessive or no sweating
  • Dry mouth
  • Feeling very hot
  • Feeling thirsty
  • Not able to pee

Contraindications

Glycopyrrolate is contraindicated for patients with hypersensitivity to glycopyrronium, excipients, or other ingredients in the anticholinergic class. The following is a list of medical conditions that would preclude the use of anticholinergic therapy, categorized by the system:

• Ophthalmic: angle-closure glaucoma
• Cardiovascular: mitral stenosis and cardiovascular instability in patients with acute hemorrhage
• Gastrointestinal: hiatal hernia, gastrointestinal obstruction, paralytic ileus, reflux esophagitis, severe ulcerative colitis, toxic megacolon, intestinal atony in older or debilitated patients
• Neuromuscular: myasthenia gravis
• Urologic: obstructive uropathy

Additionally, patients receiving solid oral potassium chloride formulations require close monitoring if coadministering with glycopyrrolate.

Who should not use glycopyrrolate?

• Allergies to Ingredients. People who are allergic to any of the following should not take glycopyrrolate.

  • Glycopyrrolate
  • Cuvposa
  • Robinul
  • Robinul Forte
  • Any of the ingredients in the specific product dispensed

  Your pharmacist can tell you all of the ingredients in the specific glycopyrrolate products they stock.

• Glaucoma. Glaucoma is a condition that may lead to trouble seeing or blindness because of damage to the optic nerve in your eye. Glycopyrrolate can make this condition worse or can block the effects of medicines used to treat glaucoma. It should not be used if you have glaucoma.

• Blockage of the Urinary Tract. Glycopyrrolate should not be used if you have a blockage in your urinary tract, also called obstructive uropathy. Glycopyrrolate can make this condition worse.

• Enlarged Prostate. Glycopyrrolate should not be used if you have an enlarged prostate, also called benign prostatic hyperplasia (BPH). Glycopyrrolate can make this condition worse.

• Gut Blockage. Glycopyrrolate should not be used if you have a blockage of your gut (bowel obstruction). Glycopyrrolate can make this worse.

• Slowed Gut Movement. Paralytic ileus is a type of ileus where your intestines are unable to move food through them. Glycopyrrolate can make this condition worse.

• Stomach Bleeding. Glycopyrrolate should not be used if you have a stomach ulcer that is bleeding. It can make this condition worse.

• Severe Ulcerative Colitis. Ulcerative colitis is an inflammatory bowel disease that can cause pain and sores in the lining of your large intestine. Glycopyrrolate can make this condition worse.

• Toxic Megacolon. Toxic megacolon is a rare and serious condition that can cause your colon to swell, weaken, and stop working properly. Glycopyrrolate can make this condition worse.

• Myasthenia gravis. Myasthenia gravis is a condition that can cause muscle weakness. Glycopyrrolate can make this condition worse. It should not be used if you have a history of this condition.

Monitoring

Glycopyrronium reduces the body's ability to sweat. Therefore, it may cause hyperthermia and heat stroke in hot environments. Other potential adverse effects include dry mouth, difficulty urinating, headaches, diarrhea, and constipation. Clinicians should monitor heart rate and maintain adequate hydration in patients receiving this drug.

A dose adjustment may be necessary if urinary retention occurs. Existing renal impairment may be further complicated. In the general population, administration of this medication may increase the risk of confusion, hallucinations, and anticholinergic effects.

Clinicians should administer glycopyrrolate cautiously in patients with a hiatal hernia and reflux esophagitis. This drug can worsen prostatic hyperplasia symptoms or bladder neck destruction and increase the risk of urinary retention. In patients with ulcerative colitis, a high dose may inhibit intestinal motility and worsen toxic megacolon or ileus symptoms. Glycopyrrolate administration is contraindicated for patients with ulcerative colitis. Since gastrointestinal motility may decline, constipation or intestinal pseudo-obstruction may occur. If the latter condition arises, it may result in painful abdominal distention, nausea, or vomiting. If intestinal obstruction of any type is suspected, it is imperative to discontinue use and simultaneously reevaluate. Symptoms such as diarrhea, particularly in patients who have undergone bowel resections of the ileum or colon, warrant a lower threshold for clinical suspicion. When an obstruction is suspected, or if the patient has diarrhea, promptly discontinue treatment.

Toxicity

Acute toxicity with glycopyrrolate is secondary to an extension of the pharmacologic effects on the muscarinic cholinergic receptors. CNS toxicity as a result of glycopyrrolate administration may also called central anticholinergic syndrome, as central nervous system toxicity can be an undesirable side effect of any anticholinergic medication. This condition manifests as delirium or prolonged somnolence after anesthesia. While this is more likely to occur with scopolamine than atropine, the incidence should be low with proper dosages. However, older patients may be more susceptible. According to product labeling, a quaternary ammonium anticholinesterase such as neostigmine (which does not cross the blood-brain barrier) can be given to combat peripheral anticholinergic effects parenterally in increments of 0.25 mg in adults. This may be repeated every 5 to 10 minutes until anticholinergic overactivity is reversed or up to a maximum of 2.5 mg. If CNS symptoms (eg, restlessness, excitement, psychotic behavior, convulsions) are present, physostigmine (which does cross the blood-brain barrier) should be administered. Physostigmine in doses of 0.5 to 2 mg can be administered intravenously and repeated up to 5 mg in adults. To combat hypotension, IV fluids, pressor agents, and supportive care are administered.

Drug Interactions

Glycopyrrolate should not be taken while you are using certain other medicines. Always tell your healthcare provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using.

In particular, make sure that you discuss if you are using any of the following before taking glycopyrrolate:

• An anticholinergic medicine, which includes antihistamines and medicines commonly used for overactive bladder, Parkinson’s disease, or stomach problems
• Potassium chloride (Klor-Con and others), which is a medicine used to raise potassium levels
• A tricyclic antidepressant, such as amitriptyline, nortriptyline, or protriptyline, even if it is not used for depression
• Any medicine for seizures, such as carbamazepine, phenytoin, or phenobarbital
• A medicine used to control your heart rate or rhythm (antiarrhythmic)
• A muscle relaxant, such as carisoprodol (Soma), cyclobenzaprine, or tizanidine (Zanaflex)
• Amantadine (Gocovri), which is a medicine that may be used to treat Parkinson’s disease
• An antipsychotic, which is a medicine for certain mental health conditions
• Digoxin (Lanoxin), which is a medicine used to treat irregular heartbeat and some types of heart failure
• Atenolol, a medicine that may be used for certain heart conditions or to reduce blood pressure
• Metformin, a medicine for diabetes
• Haloperidol, a medicine used for certain mental health conditions
• Levodopa, which is a medicine for Parkinson’s disease
• Any other medicine that causes dizziness and sleepiness, such as prescription pain medicines, sleep medicines, and medicines for anxiety

Glycopyrrolate may alter the blood levels of some other medicines. Tell your healthcare provider about all medicines that you take or have recently taken.

Additional Considerations

• It is very important that your doctor check your progress at regular visits to make sure the medicine is working properly. Blood and urine tests may be needed to check for any unwanted effects.
• Tell your doctor if you are also using any other medicine for your COPD. Your doctor may want you to use it only during a severe COPD attack. Follow your doctor's instructions on how you should take your medicine.
• This medicine should not be used if you are having a severe COPD attack, or if symptoms of COPD attack has already started. Your doctor may prescribe another medicine for you to use in case of an acute COPD attack. If the other medicine does not work as well, tell your doctor right away.
• This medicine may increase the risk of worsening asthma, which may lead to hospitalization, intubation, and death in patients with asthma who take this medicine without an inhaled steroid medicine. Talk to your doctor if you have concerns about this.
• This medicine may cause paradoxical bronchospasm, which means your breathing or wheezing will get worse. This may be a life-threatening situation. Check with your doctor right away if you have a cough, difficulty with breathing, shortness of breath, or wheezing after using this medicine.
• This medicine may cause serious allergic reactions, including angioedema, which can be life-threatening and require immediate medical attention. Tell your doctor right away if you have a rash, itching, hoarseness, trouble breathing, trouble swallowing, or any swelling of your hands, face, or mouth after using this medicine.
• This medicine may cause heart or blood vessel problems, including heart rhythm problems. Check with your doctor right away if you have chest pain or tightness, decreased urine output, dilated neck veins, extreme fatigue, irregular heartbeat, swelling of the face, fingers, feet, or lower legs, troubled breathing, or weight gain.
• Call your doctor right away if blurred vision, difficulty in reading, seeing halos around lights, or any other change in vision occurs during or after treatment. Your doctor may want your eyes be checked by an ophthalmologist (eye doctor).
• Check with your doctor right away if you have a decrease in urine volume, decrease in the frequency of urination, difficulty in passing urine, or painful urination.
• Hypokalemia (low potassium in the blood) may occur while you are using this medicine. Check with your doctor right away if you have more than one of the following symptoms: decreased urine, dry mouth, increased thirst, loss of appetite, mood changes, muscle pain or cramps, nausea or vomiting, numbness or tingling in the hands, feet, or lips, seizures, uneven heartbeat, or unusual tiredness or weakness.
• This medicine may affect blood sugar levels. If you are diabetic and notice a change in the results of your blood or urine sugar tests, check with your doctor.
• Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.
• Along with its needed effects, glycopyrrolate/indacaterol may cause some unwanted effects. Some side effects of glycopyrrolate / indacaterol may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine.

Enhancing Healthcare Team Outcomes

Glycopyrrolate is a medication frequently prescribed by nurse practitioners, primary care providers, anesthesiologists, and internists. All providers prescribing this agent should be aware of its potential adverse effects. Glycopyrronium may cause hyperthermia and heat stroke in hot environments as it reduces the body's ability to sweat. Clinicians should monitor liver function tests in patients with hepatic impairment. Nursing staff should monitor and inform the prescriber if urinary retention occurs or if existing renal impairment worsens. The use of glycopyrrolate in the general population may increase the risk of confusion, hallucinations, and other anticholinergic effects.

Before administering glycopyrrolate therapy, nurses should counsel patients for common adverse effects like dry mouth, difficulty urinating, headaches, diarrhea, and constipation. Pharmacists should verify the dose and possible drug-disease interactions. Pharmacists should warn the patient that the medication may induce drowsiness or blurred vision, which is exacerbated by alcohol consumption. As healthcare team members, all MDs, DOs, PAs, NPs, nursing staff, and pharmacists should collaborate to improve care coordination and communicate to advance better outcomes using glycopyrrolate when indicated.

Glycopyrrolate and Weight Loss

The provided information does not directly address the relationship between glycopyrrolate and weight loss. However, some of the side effects associated with glycopyrrolate, such as loss of appetite, nausea, and vomiting, could potentially lead to weight loss. Conversely, other side effects like constipation and fluid retention might contribute to weight gain.

It is important to note that any weight changes experienced while taking glycopyrrolate are likely to be secondary effects of the medication and not a direct result of its intended mechanism of action. If you are concerned about weight changes while taking glycopyrrolate, it is essential to consult with your healthcare provider. They can assess your individual situation, consider any other medications you are taking, and provide personalized advice.

tags: #glycopyrrolate #and #weight #loss