Glycopyrrolate 1mg 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 Acetylcholine 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 the action of a natural chemical in your body called acetylcholine. It's often used to treat conditions like stomach ulcers or excessive drooling.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to use it 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 place, avoiding bathrooms. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to explore local 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 adverse effects.
To get the most benefit from your medication, it's essential to use it 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 place, avoiding bathrooms. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to explore local 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 adverse effects.
Lifestyle & Tips
- Stay hydrated by drinking plenty of water, especially to help with dry mouth.
- Avoid activities that may lead to overheating (e.g., strenuous exercise in hot weather) as this medication can reduce sweating and increase the risk of heatstroke.
- Use sugar-free candies or gum to help with dry mouth.
- Maintain good oral hygiene to prevent dental problems associated with dry mouth.
- Be cautious 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:
For peptic ulcer: 1-2 mg orally 2-3 times daily. For sialorrhea: 1-2 mg orally 2-3 times daily.
Dose Range:
1 - 8 mg
Condition-Specific Dosing:
pepticUlcer:
1-2 mg orally 2-3 times daily, maximum 8 mg/day.
sialorrhea:
1-2 mg orally 2-3 times daily, maximum 8 mg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for tablets; oral solution (Cuvposa) is approved for chronic severe drooling in pediatric patients 3-16 years of age.
Child:
For chronic severe drooling (sialorrhea) in patients 3-16 years: Initial 0.02 mg/kg orally 3 times daily, titrate in increments of 0.02 mg/kg every 5-7 days. Max 0.1 mg/kg/dose or 2 mg/dose, whichever is less. Max total daily dose 4-8 mg depending on weight.
Adolescent:
For chronic severe drooling (sialorrhea) in patients 3-16 years: Initial 0.02 mg/kg orally 3 times daily, titrate in increments of 0.02 mg/kg every 5-7 days. Max 0.1 mg/kg/dose or 2 mg/dose, whichever is less. Max total daily dose 4-8 mg depending on weight.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, but use with caution.
Moderate:
Use with caution; consider lower doses and monitor for anticholinergic effects.
Severe:
Avoid use or use with extreme caution; significant accumulation may occur. Consider lower doses and extended intervals.
Dialysis:
Not dialyzable. Avoid use or use with extreme caution.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended, but use with caution as some biliary excretion occurs.
Severe:
No specific adjustment recommended, but use with caution as some biliary excretion occurs.
Pharmacology
Mechanism of Action
Glycopyrrolate is a synthetic quaternary ammonium anticholinergic agent. It competitively blocks the action of acetylcholine at muscarinic receptors located on smooth muscles, cardiac muscle, secretory glands, and peripheral ganglia. Its quaternary ammonium structure limits its ability to cross the blood-brain barrier, resulting in minimal central nervous system effects at therapeutic doses. It reduces gastric acid secretion, gastrointestinal motility, and salivary, bronchial, and sweat gland secretions.
Pharmacokinetics
Absorption:
Bioavailability:
<10% (oral)
Tmax:
1-3 hours
FoodEffect:
Food may decrease the rate and extent of absorption.
Distribution:
Vd:
Not extensively studied for oral form, but generally low due to poor tissue penetration.
ProteinBinding:
Not extensively protein bound.
CnssPenetration:
Limited (due to quaternary ammonium structure)
Elimination:
HalfLife:
Oral elimination half-life: 3-4 hours (variable); IV half-life: 0.83 hours.
Clearance:
Primarily renal clearance of unchanged drug.
ExcretionRoute:
Renal (major), Biliary (minor)
Unchanged:
Approximately 85% (renal)
Pharmacodynamics
OnsetOfAction:
Within 1 hour (oral)
PeakEffect:
1-2 hours (oral)
DurationOfAction:
4-6 hours
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
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
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only mild 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 persist, 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, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
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
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only mild 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 persist, 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 eating or speaking.
- Blurred vision or eye pain.
- Difficulty urinating or inability to urinate.
- Severe constipation or abdominal pain.
- Fast or irregular heartbeat.
- Signs of heatstroke (e.g., fever, confusion, hot/dry skin).
- Allergic reaction (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:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced.
Certain health conditions, including:
+ Heart problems caused by bleeding
+ Glaucoma
+ Gastrointestinal (GI) issues, such as bowel blockage, slow-moving GI tract, colitis, or bleeding ulcers
+ Myasthenia gravis
+ Urination difficulties
A history of having an enlarged colon
Current use of potassium tablets
Use of medications that can slow GI tract movement or increase the risk of bowel blockage. There are many medications that can cause this; consult your doctor or pharmacist if you are unsure.
Use of anticholinergic medications, such as ipratropium or oxybutynin. If you are unsure whether any of your medications are anticholinergic, ask your doctor.
This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. This will help ensure your safety when taking this medication. Never start, stop, or change the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced.
Certain health conditions, including:
+ Heart problems caused by bleeding
+ Glaucoma
+ Gastrointestinal (GI) issues, such as bowel blockage, slow-moving GI tract, colitis, or bleeding ulcers
+ Myasthenia gravis
+ Urination difficulties
A history of having an enlarged colon
Current use of potassium tablets
Use of medications that can slow GI tract movement or increase the risk of bowel blockage. There are many medications that can cause this; consult your doctor or pharmacist if you are unsure.
Use of anticholinergic medications, such as ipratropium or oxybutynin. If you are unsure whether any of your medications are anticholinergic, ask your doctor.
This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. This will help ensure your safety when taking this medication. Never start, stop, or change the dosage of any medication without first 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, wait until 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, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to both you and your baby.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until 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, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe dry mouth and throat
- Blurred vision
- Dilated pupils
- Flushing of the skin
- Fever
- Tachycardia (rapid heart rate)
- Arrhythmias
- Hypertension (high blood pressure)
- Urinary retention
- Constipation
- Central nervous system effects (e.g., excitement, confusion, delirium, hallucinations, seizures, coma)
What to Do:
Seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Treatment is supportive and symptomatic. Physostigmine may be used in severe cases of central anticholinergic toxicity.
Drug Interactions
Major Interactions
- Potassium chloride (oral solid dosage forms): Increased risk of gastrointestinal lesions due to prolonged contact with the GI mucosa.
- Other anticholinergic agents (e.g., atropine, scopolamine, tricyclic antidepressants, phenothiazines, antihistamines): Additive anticholinergic effects (e.g., dry mouth, blurred vision, urinary retention, constipation).
Moderate Interactions
- Drugs that require gastric acidity for absorption (e.g., ketoconazole, itraconazole, iron salts): Glycopyrrolate may decrease absorption due to reduced gastric motility and pH.
- Antacids: May interfere with absorption of glycopyrrolate; administer glycopyrrolate at least 1 hour before antacids.
- Drugs affecting GI motility (e.g., metoclopramide, domperidone): Antagonistic effects.
- Opioid analgesics: Increased risk of severe constipation and paralytic ileus.
Monitoring
Baseline Monitoring
Baseline vital signs (heart rate, blood pressure)
Rationale: To establish a baseline and monitor for anticholinergic effects like tachycardia.
Timing: Prior to initiation of therapy.
Assessment of urinary function
Rationale: To identify pre-existing urinary retention or risk factors.
Timing: Prior to initiation of therapy.
Assessment of bowel habits
Rationale: To identify pre-existing constipation or risk factors.
Timing: Prior to initiation of therapy.
Routine Monitoring
Heart rate
Frequency: Periodically, especially during dose titration.
Target: Within patient's normal range, or as clinically indicated.
Action Threshold: Significant or symptomatic tachycardia; consider dose reduction or discontinuation.
Bowel movements
Frequency: Daily/weekly
Target: Regular, soft stools.
Action Threshold: Development or worsening of constipation; consider laxatives or dose adjustment.
Urinary output/symptoms
Frequency: Daily
Target: Normal voiding pattern.
Action Threshold: Development of urinary hesitancy, decreased output, or retention; consider dose adjustment or discontinuation.
Dry mouth/oral hygiene
Frequency: Daily
Target: Manageable dryness.
Action Threshold: Severe dry mouth impacting quality of life or leading to dental issues; consider symptomatic relief or dose adjustment.
Symptom Monitoring
- Dry mouth
- Blurred vision
- Constipation
- Urinary retention or hesitancy
- Tachycardia
- Dizziness
- Headache
- Nervousness
- Difficulty swallowing
- Heat intolerance (reduced sweating)
Special Patient Groups
Pregnancy
Glycopyrrolate is classified as 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 during pregnancy only if clearly needed.
Trimester-Specific Risks:
First Trimester:
No specific increased risk of congenital malformations identified in animal studies.
Second Trimester:
No specific increased risk identified.
Third Trimester:
May inhibit uterine contractions and cause fetal tachycardia. Use with caution near term.
Lactation
Glycopyrrolate is excreted into breast milk in small amounts. Due to the potential for anticholinergic effects in the infant (e.g., decreased GI motility, dry mouth, sedation) and potential for decreased milk production, caution is advised. Monitor the infant for adverse effects.
Infant Risk:
Low to moderate risk. Potential for anticholinergic effects (e.g., constipation, dry mouth, sedation) and theoretical risk of reduced milk supply. Consider alternative agents or monitor infant closely.
Pediatric Use
Oral tablets are not approved for general pediatric use, but the oral solution (Cuvposa) is approved for chronic severe drooling in patients 3-16 years of age. Use with caution in children due to increased sensitivity to anticholinergic effects and potential for hyperthermia.
Geriatric Use
Elderly patients are more susceptible to the anticholinergic side effects of glycopyrrolate, particularly dry mouth, constipation, urinary retention, and central nervous system effects (e.g., confusion, delirium). Use with caution and consider lower starting doses and slower titration. Monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Glycopyrrolate's quaternary ammonium structure limits its CNS penetration, making it less likely to cause central anticholinergic side effects (e.g., confusion, delirium) compared to tertiary amines like atropine or scopolamine.
- It is often preferred for reducing secretions in surgical settings or for chronic drooling due to its peripheral action.
- Patients should be advised about potential for reduced sweating and increased risk of heatstroke, especially in hot environments or during exercise.
- Administer at least 1 hour before or 2 hours after antacids to avoid interference with absorption.
- For peptic ulcer disease, it is typically used as an adjunct therapy, not monotherapy.
Alternative Therapies
- For peptic ulcer disease: Proton pump inhibitors (PPIs), H2-receptor antagonists, sucralfate, bismuth subsalicylate.
- For sialorrhea (chronic drooling): Scopolamine patch, atropine drops (sublingual), botulinum toxin injections into salivary glands, surgery.
- For hyperhidrosis: Topical antiperspirants (aluminum chloride), botulinum toxin injections, iontophoresis, oral oxybutynin, surgery (sympathectomy).
Cost & Coverage
Average Cost:
$10 - $50 per 30 tablets (generic 1mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
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 your 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 medication taken, the amount, and the time it occurred.