Glycopyrrolate 1mg/5ml Oral Soln
It is used to reduce drooling.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Anticholinergic, Antimuscarinic
Pharmacologic Class
Muscarinic receptor antagonist
Pregnancy Category
Category B
FDA Approved
Jul 2010
DEA Schedule
Not Controlled
Overview
What is this medicine?
Glycopyrrolate is a medicine that helps reduce the amount of saliva (spit) your body makes. It's often used for children who have a lot of drooling due to certain medical conditions. It works by blocking signals that tell your salivary glands to produce spit.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel well.
Take your medication on an empty stomach, at least 1 hour before or 2 hours after meals, unless your doctor has given you different instructions. When taking a liquid dose, measure it carefully using the measuring device that comes with your medication. If no device is provided, ask your pharmacist for a suitable measuring device.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, consult 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 is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel well.
Take your medication on an empty stomach, at least 1 hour before or 2 hours after meals, unless your doctor has given you different instructions. When taking a liquid dose, measure it carefully using the measuring device that comes with your medication. If no device is provided, ask your pharmacist for a suitable measuring device.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, consult 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 is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Take this medicine on an empty stomach, at least 1 hour before or 2 hours after meals, as food can reduce its absorption.
- Drink plenty of fluids to help with dry mouth and prevent constipation.
- Avoid activities that could lead to overheating (e.g., strenuous exercise in hot weather), as this medicine can reduce sweating.
- Be cautious when driving or operating machinery until you know how this medicine 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:
Not typically used for chronic severe drooling in adults. For other indications (e.g., peptic ulcer), doses vary significantly.
Condition-Specific Dosing:
pepticUlcer:
1-2 mg orally 2-3 times daily (older formulations/indications)
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For chronic severe drooling (ages 3-16 years): Initial dose 0.02 mg/kg orally 3 times daily. Titrate in increments of 0.02 mg/kg every 5-7 days. Maximum dose 0.1 mg/kg per dose, not to exceed 3 mg per dose or 6 mg total daily.
Adolescent:
For chronic severe drooling (ages 3-16 years): Initial dose 0.02 mg/kg orally 3 times daily. Titrate in increments of 0.02 mg/kg every 5-7 days. Maximum dose 0.1 mg/kg per dose, not to exceed 3 mg per dose or 6 mg total daily.
Dose Adjustments
Renal Impairment:
Mild:
Use with caution; consider dose reduction.
Moderate:
Use with caution; consider dose reduction.
Severe:
Avoid use or use with extreme caution and significant dose reduction due to primary renal excretion.
Dialysis:
Not well studied; likely not dialyzable due to low molecular weight and protein binding. Avoid or use with extreme caution.
Hepatic Impairment:
Mild:
No specific adjustment recommended, as hepatic metabolism is minimal.
Moderate:
No specific adjustment recommended.
Severe:
No specific adjustment recommended.
Pharmacology
Mechanism of Action
Glycopyrrolate is a synthetic quaternary ammonium anticholinergic agent. It competitively blocks the action of acetylcholine at muscarinic receptors, primarily reducing the volume of salivary, tracheobronchial, and pharyngeal secretions. Due to its quaternary ammonium structure, it is highly ionized and does not readily cross the blood-brain barrier, resulting in fewer central nervous system (CNS) side effects compared to tertiary amines like atropine.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 3% (oral solution)
Tmax:
3-4 hours
FoodEffect:
Food significantly decreases the rate and extent of absorption (AUC and Cmax reduced by 60-80% when taken with a high-fat meal).
Distribution:
Vd:
0.2-0.6 L/kg
ProteinBinding:
Low (approximately 10%)
CnssPenetration:
Limited
Elimination:
HalfLife:
0.83-1.25 hours (IV); oral elimination half-life is longer due to absorption phase (reported up to 3 hours in some studies).
Clearance:
Not precisely quantified for oral solution, but primarily renal.
ExcretionRoute:
Renal (85% unchanged drug within 48 hours)
Unchanged:
Approximately 85%
Pharmacodynamics
OnsetOfAction:
30-60 minutes
PeakEffect:
3-4 hours
DurationOfAction:
6-8 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 or irregular heartbeat
Fast breathing rate
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 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 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 or irregular heartbeat
Fast breathing rate
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 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 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 dry mouth that interferes with eating or speaking
- Severe constipation or inability to have a bowel movement
- Difficulty urinating or inability to urinate
- Blurred vision or eye pain
- Signs of overheating (e.g., fever, hot/dry skin, confusion, rapid heart rate)
- Rash or allergic reaction (hives, swelling of face/lips/tongue/throat, difficulty 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. Describe the allergic reaction you experienced, including the symptoms that occurred.
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
+ Difficulty urinating
A history of having an enlarged colon
Current use of potassium tablets
Use of medications that can slow the movement of the GI tract or increase the risk of bowel blockage. There are many medications that can cause this effect, so ask 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, consult 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 dose 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. Describe the allergic reaction you experienced, including the symptoms that occurred.
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
+ Difficulty urinating
A history of having an enlarged colon
Current use of potassium tablets
Use of medications that can slow the movement of the GI tract or increase the risk of bowel blockage. There are many medications that can cause this effect, so ask 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, consult 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 dose 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.
Discuss the use of alcohol, marijuana, or other cannabis products, as well as prescription or over-the-counter medications that may cause drowsiness, with your doctor before consumption.
If you experience constipation, consult your doctor, as there may be ways to mitigate this side effect.
Be cautious in hot weather and during 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, exercise caution when using this medication, as you may be more susceptible to side effects.
When administering this medication to children, use it with caution, as the risk of certain side effects may be higher in this population.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor, as you will need 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.
Discuss the use of alcohol, marijuana, or other cannabis products, as well as prescription or over-the-counter medications that may cause drowsiness, with your doctor before consumption.
If you experience constipation, consult your doctor, as there may be ways to mitigate this side effect.
Be cautious in hot weather and during 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, exercise caution when using this medication, as you may be more susceptible to side effects.
When administering this medication to children, use it with caution, as the risk of certain side effects may be higher in this population.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor, as you will need to discuss the potential benefits and risks to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe dry mouth
- Blurred vision
- Dilated pupils
- Flushing
- Fever
- Rapid heart rate (tachycardia)
- Urinary retention
- Constipation
- CNS excitation (restlessness, confusion, hallucinations, seizures, delirium)
- Respiratory depression (in severe cases)
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive; physostigmine may be used in severe cases of central anticholinergic toxicity.
Drug Interactions
Contraindicated Interactions
- Potassium chloride (solid oral dosage forms, especially wax-matrix formulations) - increased risk of GI lesions.
Major Interactions
- Other anticholinergic agents (e.g., tricyclic antidepressants, phenothiazines, antihistamines, quinidine, disopyramide) - additive anticholinergic effects (dry mouth, constipation, urinary retention, blurred vision, heat intolerance).
- Drugs that prolong QT interval (theoretical risk, monitor if co-administered with other QT prolonging agents).
Moderate Interactions
- Drugs requiring specific pH for absorption (e.g., ketoconazole, digoxin) - glycopyrrolate may decrease gastric motility and increase gastric pH, potentially altering absorption.
- Antacids - may decrease absorption of glycopyrrolate; separate administration by at least 1 hour.
Monitoring
Baseline Monitoring
Baseline drooling assessment
Rationale: To establish severity and track treatment efficacy.
Timing: Prior to initiation of therapy
Renal function (CrCl)
Rationale: Glycopyrrolate is primarily renally excreted; dose adjustment may be needed in renal impairment.
Timing: Prior to initiation of therapy
Routine Monitoring
Efficacy (reduction in drooling)
Frequency: Regularly during dose titration and periodically thereafter
Target: Clinically significant reduction in drooling without intolerable side effects
Action Threshold: If no improvement or intolerable side effects, consider dose adjustment or discontinuation.
Adverse effects (e.g., dry mouth, constipation, urinary retention, flushing, hyperthermia, blurred vision)
Frequency: Regularly during dose titration and periodically thereafter
Target: Absence or minimal severity of side effects
Action Threshold: If severe or persistent side effects, consider dose reduction or discontinuation.
Fluid intake and hydration status
Frequency: Periodically
Target: Adequate hydration
Action Threshold: If signs of dehydration, encourage fluid intake or adjust dose.
Symptom Monitoring
- Dry mouth
- Constipation
- Urinary retention or difficulty urinating
- Blurred vision
- Flushing
- Signs of overheating (e.g., fever, decreased sweating, hot/dry skin)
- Nausea
- Vomiting
- Abdominal distension
Special Patient Groups
Pregnancy
Glycopyrrolate is 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 and the potential benefits outweigh the potential risks.
Trimester-Specific Risks:
First Trimester:
Low risk based on animal data, but human data limited.
Second Trimester:
Low risk based on animal data, but human data limited.
Third Trimester:
Low risk based on animal data, but human data limited. Potential for anticholinergic effects in neonate if used close to delivery (e.g., decreased heart rate variability).
Lactation
Glycopyrrolate is excreted into breast milk. While the amount is likely small due to poor oral absorption, potential for anticholinergic effects in the infant (e.g., dry mouth, constipation, decreased sweating) exists. Use with caution; monitor infant for side effects. Consider alternative agents or temporary discontinuation of breastfeeding.
Infant Risk:
L3 (Moderately Safe - probably compatible with breastfeeding, but monitor infant for anticholinergic effects).
Pediatric Use
Approved for chronic severe drooling in patients aged 3-16 years. Safety and efficacy in children younger than 3 years have not been established. Children are more susceptible to the side effects of anticholinergic agents, especially hyperthermia.
Geriatric Use
Use with caution in elderly patients due to increased sensitivity to anticholinergic effects (e.g., dry mouth, constipation, urinary retention, confusion, blurred vision). Start with lower doses and titrate slowly. Avoid in elderly patients with cognitive impairment or glaucoma.
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.
- Dose titration is crucial for optimizing efficacy while minimizing side effects, especially in pediatric patients.
- Administer on an empty stomach to maximize absorption. If taken with food, absorption is significantly reduced.
- Patients should be advised about the risk of hyperthermia, especially in hot environments or during physical activity, due to reduced sweating.
- Ensure adequate fluid intake to mitigate dry mouth and constipation.
Alternative Therapies
- Scopolamine (transdermal patch, off-label for drooling)
- Atropine eye drops (used off-label orally for drooling)
- Botulinum toxin injections (into salivary glands for severe drooling)
- Behavioral interventions (e.g., oral motor therapy, positioning)
Cost & Coverage
Average Cost:
Varies widely by pharmacy and formulation (generic vs. brand) per 150 ml bottle (1mg/5ml)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (generic often Tier 1 or 2, brand Tier 3 or higher)
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 medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.