Glycopyrrolate 0.6mg/3ml Pf Inj 3ml

Manufacturer FRESENIUS KABI USA Active Ingredient Glycopyrrolate Injection(glye koe PYE roe late) Pronunciation glye koe PYE roe late
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.
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Drug Class
Anticholinergic
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Pharmacologic Class
Muscarinic receptor antagonist
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Pregnancy Category
Category B
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FDA Approved
Sep 1961
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Glycopyrrolate injection is a medication used during surgery to help reduce saliva and other body fluids in your mouth and airways. It can also be used to help reverse the effects of certain muscle relaxants given during surgery.
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How to Use This Medicine

Taking Your Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to follow the dosage instructions carefully. This medication is administered via injection into a muscle or vein.

Storing and Disposing of Your Medication

If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.

Missing a Dose

If you miss a dose, contact your doctor immediately to receive guidance on what to do next.
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Lifestyle & Tips

  • Report any unusual symptoms like severe dry mouth, blurred vision, difficulty urinating, or constipation.
  • Avoid activities requiring mental alertness (e.g., driving) until you know how this medication affects you, especially if other sedating medications are also given.

Dosing & Administration

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Adult Dosing

Standard Dose: Preoperative: 0.1-0.2 mg IM/IV 30-60 minutes prior to anesthesia. Reversal of Neuromuscular Blockade: 0.2 mg IV for every 1 mg of neostigmine or 5 mg of pyridostigmine, administered simultaneously.
Dose Range: 0.1 - 0.2 mg

Condition-Specific Dosing:

preoperative: 0.1-0.2 mg IM/IV
neuromuscular_blockade_reversal: 0.2 mg IV per 1 mg neostigmine or 5 mg pyridostigmine
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Pediatric Dosing

Neonatal: Not established for routine use, consult specialist.
Infant: Preoperative (1 month to 2 years): 0.004-0.008 mg/kg IM/IV, not to exceed 0.1 mg per dose. Reversal of Neuromuscular Blockade: 0.2 mg IV for every 1 mg of neostigmine or 5 mg of pyridostigmine, administered simultaneously.
Child: Preoperative (2-12 years): 0.004-0.008 mg/kg IM/IV, not to exceed 0.2 mg per dose. Reversal of Neuromuscular Blockade: 0.2 mg IV for every 1 mg of neostigmine or 5 mg of pyridostigmine, administered simultaneously.
Adolescent: Preoperative (12-16 years): 0.004-0.008 mg/kg IM/IV, not to exceed 0.2 mg per dose. Reversal of Neuromuscular Blockade: 0.2 mg IV for every 1 mg of neostigmine or 5 mg of pyridostigmine, administered simultaneously.
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended, but monitor for anticholinergic effects.
Moderate: Consider dose reduction or extended dosing interval due to primary renal excretion. Monitor for anticholinergic effects.
Severe: Significant dose reduction (e.g., 50%) or extended dosing interval recommended. Monitor closely for anticholinergic effects.
Dialysis: Glycopyrrolate is not significantly removed by hemodialysis. Dose adjustment based on renal function is still necessary.

Hepatic Impairment:

Mild: No specific dose adjustment recommended.
Moderate: No specific dose adjustment recommended.
Severe: No specific dose adjustment recommended.

Pharmacology

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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. Due to its quaternary ammonium structure, it does not readily cross the blood-brain barrier, resulting in minimal central nervous system (CNS) effects at therapeutic doses.
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Pharmacokinetics

Absorption:

Bioavailability: Not applicable for IV/IM injection; rapid and complete absorption from IM site.
Tmax: IM: 30-45 minutes
FoodEffect: Not applicable for injection.

Distribution:

Vd: Not readily available for human IV/IM, but generally low due to poor tissue penetration.
ProteinBinding: Not extensively protein bound.
CnssPenetration: Limited

Elimination:

HalfLife: IV: 0.83 hours (initial), 1.6 hours (terminal); IM: 0.33-1.88 hours
Clearance: Not readily available, but primarily renal.
ExcretionRoute: Renal (urine) and biliary (feces).
Unchanged: Approximately 85% of IV dose excreted unchanged in urine within 48 hours.
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Pharmacodynamics

OnsetOfAction: IV: 1 minute; IM: 15-30 minutes
PeakEffect: IV: 30-45 minutes (for antisialagogue effect); IM: 30-45 minutes
DurationOfAction: IV: 2-3 hours (antisialagogue effect); IM: 6-8 hours (antisialagogue effect)

Safety & Warnings

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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.
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Seek Immediate Medical Attention If You Experience:

  • Severe dry mouth that interferes with speaking or swallowing
  • Blurred vision or difficulty focusing
  • Difficulty urinating or inability to urinate
  • Severe constipation or abdominal pain
  • Fast or irregular heartbeat
  • Dizziness or lightheadedness
  • Confusion or agitation (rare with injection due to limited CNS penetration)
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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 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, so 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 is not an exhaustive list of all potential interactions. Therefore, 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.
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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 forms of cannabis, 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, use this medication with caution, as you may be more susceptible to side effects.

When administering this medication to children, exercise caution, as the risk of certain side effects may be higher in this population.

Some formulations of this medication contain benzyl alcohol. If possible, avoid using products with benzyl alcohol in newborns and infants, as high doses of benzyl alcohol can cause serious 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, planning to become pregnant, or breastfeeding, inform your doctor, as you will need to discuss the potential benefits and risks to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Exaggerated anticholinergic effects: severe dry mouth, blurred vision, dilated pupils, hot and dry skin, fever, flushing, tachycardia, arrhythmias, hypertension, CNS excitation (restlessness, confusion, hallucinations, delirium, seizures), urinary retention, paralytic ileus.

What to Do:

Contact emergency services immediately or call a poison control center (1-800-222-1222). Treatment is supportive. Physostigmine may be used to reverse severe anticholinergic symptoms, particularly CNS effects, but should be used with caution due to potential for bradycardia and seizures.

Drug Interactions

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Major Interactions

  • Potassium chloride (oral forms, especially wax-matrix): Increased risk of GI lesions due to decreased GI motility.
  • Cholinesterase inhibitors (e.g., donepezil, rivastigmine, galantamine): Antagonism of therapeutic effects of cholinesterase inhibitors (except when used for reversal of NMB).
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Moderate Interactions

  • Other anticholinergics (e.g., tricyclic antidepressants, antihistamines, phenothiazines, quinidine, disopyramide): Additive anticholinergic effects (e.g., dry mouth, blurred vision, urinary retention, constipation).
  • Opioid analgesics: May exacerbate constipation and urinary retention.
  • Antacids: May decrease absorption of oral glycopyrrolate (not relevant for injection).
  • Metoclopramide: Antagonizes prokinetic effects.

Monitoring

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Baseline Monitoring

Patient history (glaucoma, urinary retention, GI obstruction)

Rationale: To identify contraindications or conditions requiring caution.

Timing: Prior to administration

Vital signs (heart rate, blood pressure)

Rationale: To establish baseline and monitor for cardiovascular effects.

Timing: Prior to administration

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Routine Monitoring

Heart rate and rhythm

Frequency: Continuously during perioperative use, or as clinically indicated.

Target: Maintain within acceptable physiological limits.

Action Threshold: Significant bradycardia or tachycardia, arrhythmias.

Blood pressure

Frequency: Continuously during perioperative use, or as clinically indicated.

Target: Maintain within acceptable physiological limits.

Action Threshold: Significant hypotension or hypertension.

Secretions (salivary, respiratory)

Frequency: As clinically indicated.

Target: Reduction of excessive secretions.

Action Threshold: Persistent excessive secretions or overly dry mucous membranes.

Urine output

Frequency: As clinically indicated, especially in patients at risk for urinary retention.

Target: Adequate urine output.

Action Threshold: Signs of urinary retention.

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Symptom Monitoring

  • Dry mouth
  • Blurred vision
  • Urinary retention
  • Constipation
  • Tachycardia
  • Palpitations
  • Dizziness
  • Headache
  • Nausea
  • Vomiting
  • Nervousness
  • Insomnia

Special Patient Groups

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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: 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, but may inhibit uterine contractions and cause fetal tachycardia.
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Lactation

L3 (Moderately Safe). Glycopyrrolate is excreted in breast milk in small amounts. It may decrease milk production due to its anticholinergic effects. Monitor infant for anticholinergic effects (e.g., dry mouth, constipation, urinary retention).

Infant Risk: Low to moderate. Potential for anticholinergic effects in infant and reduction in milk supply.
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Pediatric Use

Used in pediatric patients for preoperative antisialagogue effect and reversal of neuromuscular blockade. Dosing is weight-based. Infants and young children may be more susceptible to anticholinergic effects.

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Geriatric Use

Elderly patients may be more sensitive to the anticholinergic effects of glycopyrrolate, particularly urinary retention, constipation, and confusion (though CNS effects are less common with glycopyrrolate than other anticholinergics). Use with caution and monitor closely.

Clinical Information

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Clinical Pearls

  • Glycopyrrolate is a quaternary ammonium compound, meaning it has a charged nitrogen atom that limits its ability to cross the blood-brain barrier. This results in fewer central nervous system (CNS) side effects (e.g., sedation, delirium) compared to tertiary amines like atropine.
  • It is commonly used in combination with neostigmine or pyridostigmine to counteract the muscarinic side effects (e.g., bradycardia, excessive secretions) of these cholinesterase inhibitors when reversing neuromuscular blockade.
  • The onset of action is rapid (especially IV), making it suitable for acute perioperative use.
  • Due to its primary renal excretion, dose adjustment is crucial in patients with renal impairment to avoid accumulation and increased anticholinergic effects.
  • While primarily used for its antisialagogue and vagolytic effects, it can also cause mydriasis and cycloplegia, though less pronounced than atropine.
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Alternative Therapies

  • Atropine (another anticholinergic, but crosses BBB more readily, higher CNS effects)
  • Scopolamine (another anticholinergic, strong CNS effects, primarily for motion sickness/nausea)
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Cost & Coverage

Average Cost: Varies widely per vial
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (generic)
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General Drug Facts

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance.

To ensure safe use, do not share your medication with others, and never take someone else's medication. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.

Proper disposal of unused or expired medications is crucial. Do not dispose of them by flushing down the toilet or pouring down the drain unless specifically instructed to do so. If you are unsure about the best disposal method, consult your pharmacist for guidance. Many communities have drug take-back programs, which your pharmacist can help you locate.

Some medications may come with an additional patient information leaflet. Check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, do not hesitate to discuss them with 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. Be prepared to provide critical information, including the name of the medication, the amount taken, and the time it was ingested, to ensure prompt and effective treatment.