Glycopyrrolate 0.2mg/ml Inj, 5ml
It is used to treat GI (gastrointestinal) ulcers.In surgery, it is used to lower secretions such as saliva.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
Aug 1961
DEA Schedule
Not Controlled
Overview
What is this medicine?
Glycopyrrolate injection is a medication used to reduce body fluids like saliva and stomach acid, especially before surgery. It can also help control your heart rate during certain medical procedures or help with stomach and bowel problems. It works by blocking certain natural chemicals in your body.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and read all accompanying information carefully. This medication is administered via injection into a muscle or vein.
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist for guidance on proper storage procedures.
In the event that you miss a dose, contact your doctor promptly to determine the best course of action.
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist for guidance on proper storage procedures.
In the event that you miss a dose, contact your doctor promptly to determine the best course of action.
Lifestyle & Tips
- Avoid overheating: This medication can reduce sweating, making you more prone to heatstroke. Be careful in hot environments and during exercise.
- Stay hydrated: Drink plenty of fluids to help manage dry mouth and prevent constipation.
- Report any unusual symptoms: Inform your healthcare provider if you experience severe dry mouth, difficulty urinating, blurred vision, or a very fast heartbeat.
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:
Varies by indication. For pre-anesthetic: 0.002-0.004 mg/kg IM/IV 30-60 min prior to anesthesia. For reversal of neuromuscular blockade: 0.2 mg IV for every 1 mg neostigmine or 5 mg pyridostigmine. For peptic ulcer (adjunct): 0.1-0.2 mg IM/IV 3-4 times daily.
Dose Range:
0.002 - 0.2 mg
Condition-Specific Dosing:
preAnesthetic:
0.002-0.004 mg/kg IM/IV, max 0.1 mg/dose
neuromuscularBlockadeReversal:
0.2 mg IV per 1 mg neostigmine or 5 mg pyridostigmine
pepticUlcerAdjunct:
0.1-0.2 mg IM/IV 3-4 times daily
Pediatric Dosing
Neonatal:
Not established for routine use; use with extreme caution if at all.
Infant:
Pre-anesthetic: 0.004-0.008 mg/kg IM/IV 30-60 min prior to anesthesia, max 0.1 mg/dose. Reversal of neuromuscular blockade: 0.01 mg/kg IV for every 0.05 mg/kg neostigmine or 0.25 mg/kg pyridostigmine.
Child:
Pre-anesthetic: 0.004-0.008 mg/kg IM/IV 30-60 min prior to anesthesia, max 0.1 mg/dose. Reversal of neuromuscular blockade: 0.01 mg/kg IV for every 0.05 mg/kg neostigmine or 0.25 mg/kg pyridostigmine.
Adolescent:
Pre-anesthetic: 0.002-0.004 mg/kg IM/IV 30-60 min prior to anesthesia, max 0.1 mg/dose. Reversal of neuromuscular blockade: 0.2 mg IV for every 1 mg neostigmine or 5 mg pyridostigmine.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended.
Moderate:
Consider dose reduction due to primary renal excretion.
Severe:
Significant dose reduction required; avoid in end-stage renal disease (ESRD) due to prolonged half-life and accumulation.
Dialysis:
Not dialyzable. Avoid use or use with extreme caution and significant dose reduction.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended as hepatic metabolism is minimal.
Severe:
No specific adjustment recommended as hepatic metabolism is minimal.
Pharmacology
Mechanism of Action
Glycopyrrolate is a synthetic quaternary ammonium anticholinergic agent. It competitively antagonizes the muscarinic actions of acetylcholine at postganglionic parasympathetic receptor sites, including those in exocrine glands, smooth muscle, and the heart. Its quaternary ammonium structure limits its ability to cross the blood-brain barrier, resulting in minimal central nervous system effects at therapeutic doses.
Pharmacokinetics
Absorption:
Bioavailability:
100% (IV), ~10-25% (oral, not relevant for injection)
Tmax:
IV: 1-2 minutes (onset); IM: 30-45 minutes
FoodEffect:
Not applicable for injectable formulation.
Distribution:
Vd:
0.42 Âą 0.22 L/kg
ProteinBinding:
10-30%
CnssPenetration:
Limited
Elimination:
HalfLife:
IV: 0.83 Âą 0.27 hours; IM: 1.3 Âą 0.4 hours
Clearance:
Not readily available for injection, but primarily renal.
ExcretionRoute:
Renal (primarily unchanged drug)
Unchanged:
Approximately 85% (IV) to 90% (IM) excreted unchanged in urine within 24 hours.
Pharmacodynamics
OnsetOfAction:
IV: 1 minute; IM: 15-30 minutes
PeakEffect:
IV: 1-2 minutes (cardiac effects); IM: 30-45 minutes (antisecretory effects)
DurationOfAction:
2-4 hours (antisecretory effects); 6-8 hours (cardiac effects)
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 or seek immediate 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 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 or seek immediate 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 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 or difficulty swallowing
- Difficulty urinating or inability to urinate
- Severe constipation or abdominal pain
- Blurred vision or eye pain
- Very fast or irregular heartbeat
- Confusion or unusual excitement
- Signs of heatstroke (e.g., fever, hot dry skin, dizziness, weakness)
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 be sure to 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 with 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 while 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 be sure to 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 with 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 while 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 activities that require alertness and clear vision, ensure you understand how this medication affects you.
Consult your doctor before consuming alcohol, marijuana, or other cannabis products, as well as 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 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 they may have a higher risk of experiencing certain side effects.
Some formulations of this medication contain benzyl alcohol. If possible, avoid using products with benzyl alcohol in newborns and infants, as high doses can cause severe side effects, particularly when combined with other medications containing benzyl alcohol. Consult your doctor to determine if this product contains benzyl alcohol.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Before operating a vehicle or engaging in activities that require alertness and clear vision, ensure you understand how this medication affects you.
Consult your doctor before consuming alcohol, marijuana, or other cannabis products, as well as 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 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 they may have a higher risk of experiencing certain side effects.
Some formulations of this medication contain benzyl alcohol. If possible, avoid using products with benzyl alcohol in newborns and infants, as high doses can cause severe side effects, particularly when combined with other medications containing benzyl alcohol. Consult your doctor to determine if this product contains benzyl alcohol.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Exaggerated anticholinergic effects: severe dry mouth, blurred vision, dilated pupils, flushing, fever, tachycardia, hypertension, central nervous system stimulation (excitement, confusion, delirium, hallucinations), urinary retention, paralytic ileus.
What to Do:
Contact emergency services or poison control immediately (e.g., 1-800-222-1222). Treatment is primarily supportive. Physostigmine (a cholinesterase inhibitor) may be used as an antidote to reverse severe anticholinergic symptoms, particularly CNS effects, but should be used with caution due to potential for cholinergic crisis.
Drug Interactions
Major Interactions
- Potassium chloride (solid oral dosage forms): Increased risk of gastrointestinal lesions due to prolonged contact time.
- Other anticholinergics (e.g., atropine, scopolamine, tricyclic antidepressants, phenothiazines, quinidine, disopyramide): Additive anticholinergic effects.
Moderate Interactions
- Antacids: May decrease absorption of oral glycopyrrolate (not relevant for injection).
- Drugs that slow GI motility (e.g., opioids): Increased risk of severe constipation or paralytic ileus.
Monitoring
Baseline Monitoring
Vital Signs (Heart Rate, Blood Pressure)
Rationale: To establish baseline and monitor for cardiovascular effects (tachycardia, hypertension).
Timing: Prior to administration.
Assessment for Contraindications
Rationale: To identify conditions like narrow-angle glaucoma, urinary retention, paralytic ileus, or myasthenia gravis (unless used to counteract cholinergic crisis).
Timing: Prior to administration.
Fluid Status/Urine Output
Rationale: To assess for risk of urinary retention, especially in patients with prostatic hypertrophy.
Timing: Prior to administration.
Routine Monitoring
Heart Rate and Rhythm
Frequency: Continuously during acute use (e.g., perioperatively); periodically as clinically indicated.
Target: Individualized, typically within normal physiological limits or as desired for therapeutic effect (e.g., vagolytic effect).
Action Threshold: Significant tachycardia, bradycardia, or arrhythmias requiring intervention.
Urine Output
Frequency: As clinically indicated, especially in patients at risk for urinary retention.
Target: Adequate urine output.
Action Threshold: Signs of urinary retention (e.g., bladder distension, decreased output).
Bowel Function
Frequency: Daily, especially with prolonged use.
Target: Regular bowel movements.
Action Threshold: Severe constipation or signs of ileus.
Symptom Monitoring
- Dry mouth
- Blurred vision
- Urinary retention
- Constipation
- Tachycardia
- Dizziness
- Headache
- Nausea/Vomiting
- Heat intolerance (reduced sweating)
Special Patient Groups
Pregnancy
Glycopyrrolate is classified as Pregnancy Category B. Animal reproduction studies have not demonstrated a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if clearly needed and the potential benefits outweigh the potential risks.
Trimester-Specific Risks:
First Trimester:
No evidence of increased risk of congenital anomalies from limited human data.
Second Trimester:
No specific risks identified.
Third Trimester:
May inhibit uterine contractions and decrease fetal heart rate variability. Use with caution near term.
Lactation
Glycopyrrolate is excreted in breast milk. Due to its quaternary ammonium structure, it is poorly absorbed orally by the infant, minimizing systemic exposure. However, it may decrease milk production due to its anticholinergic effects. Use with caution; monitor infant for anticholinergic effects (e.g., dry mouth, constipation, urinary retention).
Infant Risk:
Low risk of adverse effects due to poor oral absorption, but potential for decreased milk supply. L3 (Moderately Safe).
Pediatric Use
Safe and effective for approved indications in pediatric patients. Dosing is weight-based. Infants and young children may be more susceptible to anticholinergic side effects, particularly hyperthermia due to reduced sweating. Use with caution in neonates due to limited data and potential for increased sensitivity.
Geriatric Use
Geriatric patients may be more susceptible to the anticholinergic side effects of glycopyrrolate, including confusion, memory impairment, urinary retention, and constipation. Start with lower doses and titrate carefully. Monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Glycopyrrolate's quaternary ammonium structure limits its ability to cross the blood-brain barrier, resulting in fewer central nervous system (CNS) side effects (e.g., sedation, delirium) compared to atropine or scopolamine.
- It is particularly useful in situations where reduction of secretions is desired without significant CNS depression, such as during anesthesia or for managing drooling.
- Due to its vagolytic effects, it can be used to prevent or treat bradycardia, especially during procedures or in response to certain medications (e.g., neostigmine).
- Patients should be advised about potential for dry mouth, blurred vision, and urinary retention.
Alternative Therapies
- Atropine (for vagolytic effects, drying secretions, reversal of neuromuscular blockade, but with more CNS effects)
- Scopolamine (for drying secretions, but with more CNS effects and transdermal patch for motion sickness)
- Hyoscyamine (for GI spasm, secretions)
- For excessive drooling: Oral glycopyrrolate, atropine eye drops (off-label), botulinum toxin injections, radiation therapy (severe cases).
- For peptic ulcer disease: Proton pump inhibitors (PPIs), H2-receptor antagonists (H2RAs).
Cost & Coverage
Average Cost:
Varies widely by supplier and quantity per 5ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (generic), Tier 3 (brand) for most commercial and government plans, often covered under medical benefit for inpatient/procedure use.
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. 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 a healthcare professional. If you are unsure about the correct disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the quantity, and the time of ingestion.