Glycopyrrolate 2mg Tablets
It is used to treat GI (gastrointestinal) ulcers.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Anticholinergic
Pharmacologic Class
Muscarinic receptor antagonist
Pregnancy Category
Category B
FDA Approved
Jun 1961
DEA Schedule
Not Controlled
Overview
What is this medicine?
Glycopyrrolate is a medication that helps reduce certain body secretions, like stomach acid, saliva, and sweat. It works by blocking specific signals in your body. It's often used to treat stomach ulcers or to reduce excessive sweating.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry location, avoiding bathrooms. Keep all medications in a secure place, out of reach of children and pets. Properly dispose of any unused or expired medication. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your doctor or pharmacist. If you have questions about disposing of your medication, consult with your pharmacist, who can also inform you about potential drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Avoid taking two doses at the same time or taking extra doses, as this can increase the risk of side effects.
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry location, avoiding bathrooms. Keep all medications in a secure place, out of reach of children and pets. Properly dispose of any unused or expired medication. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your doctor or pharmacist. If you have questions about disposing of your medication, consult with your pharmacist, who can also inform you about potential drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Avoid taking two doses at the same time or taking extra doses, as this can increase the risk of side effects.
Lifestyle & Tips
- Take this medication on an empty stomach, at least one hour before or two hours after meals, for best absorption.
- Drink plenty of water to help with dry mouth, a common side effect.
- Be aware of reduced sweating, especially in hot weather or during exercise, as this can lead to overheating. Stay hydrated and avoid strenuous activity in high temperatures.
- Avoid alcohol, as it can worsen some side effects like dizziness or drowsiness.
- Use caution when driving or operating machinery until you know how this medication affects you, as it can cause blurred vision or dizziness.
Available Forms & Alternatives
Available Strengths:
- Glycopyrrolate 0.2mg/ml Inj, 20ml
- Glycopyrrolate 0.2mg/ml Inj, 5ml
- Glycopyrrolate 2mg Tablets
- Glycopyrrolate 1mg Tablets
- Glycopyrrolate 1mg Tablets
- Glycopyrrolate 0.2mg/ml Inj, 2ml
- Glycopyrrolate 0.2mg/ml Inj, 2ml
- Glycopyrrolate 0.2mg/ml Inj, 1ml
- Glycopyrrolate 1mg/5ml Oral Soln
- Glycopyrrolate 0.2mg/ml Inj, 5ml
- Glycopyrrolate 0.2mg/ml Inj, 2ml
- Glycopyrrolate 0.2mg/ml Inj, 2ml
- Glycopyrrolate 0.4mg/2ml Inj, 2ml
- Glycopyrrolate 0.6mg/3ml Pf Inj 3ml
- Glycopyrrolate 0.6mg/3ml Inj, 3ml
- Glycopyrrolate 1mg/5ml Oral Soln
Dosing & Administration
Adult Dosing
Standard Dose:
1 to 2 mg orally two or three times daily (for peptic ulcer) or 1 to 2 mg orally once daily (for hyperhidrosis)
Dose Range:
1 - 8 mg
Condition-Specific Dosing:
pepticUlcer:
1 to 2 mg orally two or three times daily, up to 8 mg daily in divided doses if needed.
hyperhidrosis:
1 to 2 mg orally once daily, may increase to 2 mg twice daily if needed. Max 4 mg/day.
preoperative:
Not typically used orally for this indication; injectable form is preferred.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for oral tablets for general use. For chronic drooling (sialorrhea) in patients 3-16 years: 0.02 mg/kg orally three times daily, not to exceed 1.5 mg per dose or 8 mg total daily dose.
Adolescent:
Not established for oral tablets for general use. For chronic drooling (sialorrhea) in patients 3-16 years: 0.02 mg/kg orally three times daily, not to exceed 1.5 mg per dose or 8 mg total daily dose.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
Use with caution. Consider lower doses or extended dosing intervals.
Severe:
Use with caution. Consider lower doses or extended dosing intervals. Avoid if possible.
Dialysis:
Not well studied. Glycopyrrolate is primarily eliminated renally. Avoid or use with extreme caution.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended, but use with caution.
Severe:
No specific dose adjustment recommended, but use with caution.
Pharmacology
Mechanism of Action
Glycopyrrolate is a synthetic quaternary ammonium anticholinergic agent. It competitively inhibits the action of acetylcholine at muscarinic receptors located on smooth muscles, cardiac muscle, secretory glands, and in peripheral ganglia. This antagonism reduces gastrointestinal motility and secretions (e.g., gastric acid, saliva, sweat). Due to its quaternary ammonium structure, it is poorly lipid-soluble and does not readily cross the blood-brain barrier, resulting in minimal central nervous system effects at therapeutic doses.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 3% to 10% (oral)
Tmax:
Approximately 1 to 3 hours
FoodEffect:
Food significantly reduces the extent of absorption (AUC) and peak plasma concentrations (Cmax) of glycopyrrolate. Should be taken at least one hour before or two hours after meals.
Distribution:
Vd:
Not readily available for oral form, but generally low due to poor lipid solubility.
ProteinBinding:
Not readily available, but generally low.
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 0.83 hours (IV), 3.2 hours (oral)
Clearance:
Not readily available for oral form.
ExcretionRoute:
Primarily renal (unchanged drug) and biliary/fecal.
Unchanged:
Approximately 80% (IV) to 85% (oral) excreted unchanged in urine and feces.
Pharmacodynamics
OnsetOfAction:
Approximately 30-60 minutes (oral)
PeakEffect:
Approximately 1-3 hours (oral)
DurationOfAction:
Approximately 4-6 hours (oral), but effects on sweating can last longer (up to 8-12 hours).
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Inability to sweat during physical activity or in warm temperatures
Difficulty urinating
Chest pain or pressure, rapid heartbeat, or irregular heartbeat
Rapid breathing
Fever
Enlarged pupils
Changes in vision, eye pain, or severe eye irritation
Confusion
Diarrhea or constipation
Bloating
Abdominal swelling
Stomach pain
Erectile dysfunction
Muscle weakness
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
Dry mouth
Upset stomach or vomiting
Nasal congestion
Dizziness, drowsiness, fatigue, or weakness
Blurred vision
Flushing
Changes in taste
Headache
Nervousness or excitability
* Sleep disturbances
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Inability to sweat during physical activity or in warm temperatures
Difficulty urinating
Chest pain or pressure, rapid heartbeat, or irregular heartbeat
Rapid breathing
Fever
Enlarged pupils
Changes in vision, eye pain, or severe eye irritation
Confusion
Diarrhea or constipation
Bloating
Abdominal swelling
Stomach pain
Erectile dysfunction
Muscle weakness
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
Dry mouth
Upset stomach or vomiting
Nasal congestion
Dizziness, drowsiness, fatigue, or weakness
Blurred vision
Flushing
Changes in taste
Headache
Nervousness or excitability
* Sleep disturbances
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent dry mouth that interferes with speaking or swallowing.
- Blurred vision or eye pain.
- Difficulty urinating or inability to urinate.
- Severe constipation or abdominal pain.
- Rapid or irregular heartbeat.
- Signs of overheating (e.g., hot, dry skin; confusion; dizziness; rapid pulse) in hot environments.
- Any signs of an allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble breathing).
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health problems, such as:
+ Heart issues related to bleeding
+ Glaucoma
+ Gastrointestinal (GI) problems, including bowel blockage, slow-moving GI tract, colitis, or bleeding ulcers
+ Myasthenia gravis
+ Difficulty urinating
A history of an enlarged colon
Current use of potassium tablets
Use of medications that slow GI tract movement or increase the risk of bowel blockage. There are many medications that can cause this effect, so consult your doctor or pharmacist if you are unsure.
Concurrent use of anticholinergic medications, such as ipratropium or oxybutynin. If you are unsure whether any of your medications belong to this class, ask your doctor.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dose of any medication without consulting your doctor.
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health problems, such as:
+ Heart issues related to bleeding
+ Glaucoma
+ Gastrointestinal (GI) problems, including bowel blockage, slow-moving GI tract, colitis, or bleeding ulcers
+ Myasthenia gravis
+ Difficulty urinating
A history of an enlarged colon
Current use of potassium tablets
Use of medications that slow GI tract movement or increase the risk of bowel blockage. There are many medications that can cause this effect, so consult your doctor or pharmacist if you are unsure.
Concurrent use of anticholinergic medications, such as ipratropium or oxybutynin. If you are unsure whether any of your medications belong to this class, ask your doctor.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dose of any medication without consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, ensure you understand how this medication affects you.
Consult your doctor before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions.
If you experience constipation, discuss this with your doctor, as there may be ways to mitigate this side effect.
Be cautious when exposed to high temperatures or engaging in physical activity, as this medication can increase the risk of heat stroke.
Unless your doctor advises you to limit fluid intake, drink plenty of non-caffeinated liquids after taking this medication.
You may be sensitive to bright lights; wearing sunglasses can help alleviate this issue.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, plan to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, ensure you understand how this medication affects you.
Consult your doctor before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions.
If you experience constipation, discuss this with your doctor, as there may be ways to mitigate this side effect.
Be cautious when exposed to high temperatures or engaging in physical activity, as this medication can increase the risk of heat stroke.
Unless your doctor advises you to limit fluid intake, drink plenty of non-caffeinated liquids after taking this medication.
You may be sensitive to bright lights; wearing sunglasses can help alleviate this issue.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, plan to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Severe dry mouth and throat
- Blurred vision
- Dilated pupils
- Flushing of the skin
- Fever
- Tachycardia (very fast heart rate)
- Hypertension (high blood pressure)
- Urinary retention
- Paralytic ileus (bowel obstruction)
- Central nervous system effects (e.g., excitement, confusion, delirium, hallucinations, seizures, coma)
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive and may include physostigmine for severe anticholinergic toxicity.
Drug Interactions
Major Interactions
- Potassium chloride (solid oral dosage forms): Increased risk of GI lesions due to prolonged GI transit time.
- Other anticholinergics (e.g., atropine, scopolamine, tricyclic antidepressants, phenothiazines, antihistamines): Additive anticholinergic effects.
Moderate Interactions
- Drugs that affect GI motility (e.g., metoclopramide, domperidone): Glycopyrrolate may antagonize their effects.
- Antacids: May interfere with absorption of glycopyrrolate; separate administration by at least 1 hour.
- Digoxin (oral): Glycopyrrolate may increase digoxin absorption due to reduced GI motility.
- Topiramate: May increase risk of hyperthermia and anhidrosis.
Monitoring
Baseline Monitoring
Baseline symptoms (e.g., peptic ulcer pain, sweat production)
Rationale: To assess efficacy of treatment.
Timing: Prior to initiation of therapy.
Renal function (eGFR, BUN, creatinine)
Rationale: Glycopyrrolate is primarily renally eliminated; dose adjustment may be needed in severe impairment.
Timing: Prior to initiation, especially in elderly or those with known renal issues.
Routine Monitoring
Symptom relief (e.g., reduction in ulcer pain, decrease in sweating)
Frequency: Regularly, as clinically indicated.
Target: Significant improvement or resolution of target symptoms.
Action Threshold: Lack of improvement or worsening of symptoms may require dose adjustment or alternative therapy.
Anticholinergic side effects (e.g., dry mouth, blurred vision, urinary retention, constipation, tachycardia)
Frequency: Regularly, especially during dose titration.
Target: Minimal to tolerable side effects.
Action Threshold: Severe or intolerable side effects may require dose reduction or discontinuation.
Fluid intake and hydration status
Frequency: Daily, especially in hot environments or during physical activity.
Target: Adequate hydration.
Action Threshold: Signs of dehydration or heat intolerance (e.g., dizziness, weakness) require immediate intervention.
Symptom Monitoring
- Dry mouth
- Blurred vision
- Urinary retention (difficulty urinating)
- Constipation
- Tachycardia (fast heart rate)
- Dizziness
- Headache
- Nervousness
- Heat intolerance (reduced sweating leading to overheating)
Special Patient Groups
Pregnancy
Category B. Animal studies have not shown harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed.
Trimester-Specific Risks:
First Trimester:
No increased risk of congenital anomalies observed in animal studies.
Second Trimester:
No specific risks identified.
Third Trimester:
No specific risks identified. Potential for reduced fetal heart rate variability with IV use, but less likely with oral form.
Lactation
Lactation Risk Category L3 (Moderately Safe). It is unknown if glycopyrrolate is excreted in human milk. Due to its quaternary ammonium structure, it is unlikely to be significantly excreted into breast milk or absorbed by the infant. However, anticholinergics can potentially decrease milk production. Use with caution.
Infant Risk:
Low risk of adverse effects in the infant due to poor oral absorption and limited CNS penetration. Monitor for signs of anticholinergic effects (e.g., dry mouth, constipation, urinary retention) or decreased milk supply in the mother.
Pediatric Use
Oral tablets are not generally recommended for routine use in children under 12 years for peptic ulcer disease. A specific oral solution (Cuvposa) is approved for chronic severe drooling in pediatric patients aged 3-16 years. Dosing is weight-based. Children are more susceptible to anticholinergic side effects, especially heat intolerance.
Geriatric Use
Elderly patients may be more sensitive to the anticholinergic effects of glycopyrrolate, particularly dry mouth, constipation, urinary retention, and cognitive impairment (though less likely with glycopyrrolate due to limited CNS penetration compared to tertiary amines). Use with caution, starting with lower doses and titrating slowly.
Clinical Information
Clinical Pearls
- Glycopyrrolate's quaternary ammonium structure limits its ability to cross the blood-brain barrier, leading to fewer CNS side effects (e.g., sedation, confusion) compared to tertiary anticholinergics like atropine or scopolamine.
- The oral bioavailability is low, and food significantly reduces absorption, so advise patients to take it on an empty stomach.
- Patients should be counselled on the risk of heat intolerance due to reduced sweating, especially in warm climates or during physical activity.
- For hyperhidrosis, patients often find the effects on sweating to be dose-dependent and may require titration to find the optimal balance between efficacy and side effects.
- Consider alternative agents or careful monitoring in patients with conditions exacerbated by anticholinergics, such as glaucoma (narrow-angle), prostatic hypertrophy, or urinary retention.
Alternative Therapies
- For peptic ulcer: H2-receptor antagonists (e.g., famotidine), Proton pump inhibitors (e.g., omeprazole), sucralfate.
- For hyperhidrosis: Topical antiperspirants (aluminum chloride), botulinum toxin injections, iontophoresis, other oral anticholinergics (e.g., oxybutynin - off-label), surgery (sympathectomy).
- For chronic drooling: Scopolamine patch (off-label), atropine eye drops (off-label, sublingual), botulinum toxin injections into salivary glands.
Cost & Coverage
Average Cost:
Varies widely, typically $20-$100+ per 30 tablets (2mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (generic), Tier 3 or 4 (brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.