Glycopyrrolate 0.6mg/3ml 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
Jul 1961
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Glycopyrrolate is a medication that helps reduce body secretions like saliva and stomach acid. It's often used before surgery to dry up secretions in the mouth and airways, or to protect the heart during certain procedures. It can also be used to reverse the effects of some muscle relaxants given during surgery.
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How to Use This Medicine

To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all provided guidelines. This medication is administered via injection into a muscle or vein.

For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.

If you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
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Lifestyle & Tips

  • Report any difficulty urinating or severe constipation.
  • Be aware of potential for dry mouth; sips of water or sugar-free candy may help.
  • Avoid activities requiring mental alertness if blurred vision or dizziness occurs.

Dosing & Administration

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Adult Dosing

Standard Dose: Preoperative: 0.1-0.2 mg IV/IM, 30-60 minutes prior to anesthesia. Reversal of Neuromuscular Blockade: 0.2 mg IV for each 1 mg neostigmine or 5 mg pyridostigmine, administered concurrently.
Dose Range: 0.004 - 0.008 mg

Condition-Specific Dosing:

Preoperative (IV/IM): 0.004 mg/kg, typically 0.1-0.2 mg, up to 0.4 mg single dose.
Reversal of Neuromuscular Blockade (IV): 0.2 mg for each 1 mg neostigmine or 5 mg pyridostigmine, administered concurrently.
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Pediatric Dosing

Neonatal: Not established for routine use; use with caution and reduced doses if necessary.
Infant: Preoperative (IM/IV): 0.004-0.008 mg/kg, not to exceed 0.1 mg per dose. Reversal of Neuromuscular Blockade (IV): 0.2 mg for each 1 mg neostigmine or 5 mg pyridostigmine, administered concurrently.
Child: Preoperative (IM/IV): 0.004-0.008 mg/kg, not to exceed 0.2 mg per dose. Reversal of Neuromuscular Blockade (IV): 0.2 mg for each 1 mg neostigmine or 5 mg pyridostigmine, administered concurrently.
Adolescent: Preoperative (IM/IV): 0.004-0.008 mg/kg, not to exceed 0.2 mg per dose. Reversal of Neuromuscular Blockade (IV): 0.2 mg for each 1 mg neostigmine or 5 mg pyridostigmine, administered concurrently.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment recommended, but monitor for exaggerated effects.
Moderate: Consider dose reduction (e.g., 50%) and extend dosing interval due to primary renal excretion.
Severe: Significant dose reduction (e.g., 50-75%) and extended dosing interval required. Avoid if possible.
Dialysis: Glycopyrrolate is not significantly removed by hemodialysis. Dose adjustment based on residual renal function.

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

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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 smooth muscle, cardiac muscle, and exocrine glands. Due to its quaternary ammonium structure, it is highly ionized and does not readily cross the blood-brain barrier, resulting in minimal central nervous system effects at usual doses.
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Pharmacokinetics

Absorption:

Bioavailability: Not applicable for IV/IM injection; oral bioavailability is poor (<3%).
Tmax: IV: 1-2 minutes (peak effect); IM: 30-45 minutes.
FoodEffect: Not applicable for injection.

Distribution:

Vd: Approximately 0.42 L/kg (adults).
ProteinBinding: Approximately 10-30%.
CnssPenetration: Limited (due to quaternary ammonium structure).

Elimination:

HalfLife: IV: 0.83-1.25 hours (terminal elimination half-life).
Clearance: Approximately 0.54 L/kg/hr.
ExcretionRoute: Primarily renal (85% unchanged drug), with some biliary excretion.
Unchanged: Approximately 85% (renal).
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Pharmacodynamics

OnsetOfAction: IV: 1 minute (cardiac effects), 2-3 minutes (antisecretory effects). IM: 10-15 minutes.
PeakEffect: IV: 1-2 minutes (cardiac), 30-45 minutes (antisecretory).
DurationOfAction: Antisecretory: 2-3 hours (IV), 6-8 hours (IM). Cardiac: 20-30 minutes (IV).

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

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. 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 or difficulty swallowing
  • Blurred vision or eye pain
  • Difficulty urinating or inability to urinate
  • Severe constipation or abdominal pain
  • Fast or irregular heartbeat
  • Confusion or agitation (rare with injection)
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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. 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
- Bleeding ulcer
+ 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 effect, 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 list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including:

Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Health problems

Verify that it is safe to take this medication with all your other medications and health conditions. Do not initiate, stop, or modify the dose of any medication without 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.

When starting this medication, be cautious and avoid driving or performing tasks that require alertness and clear vision until you understand how it affects you.

Before consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter (OTC) medications that may cause drowsiness, consult with your doctor to discuss potential interactions.

If you experience constipation, consult your doctor, as there may be ways to mitigate this side effect.

Be aware that heat stroke has occurred in individuals taking this medication. Therefore, exercise caution in hot weather and during physical activity to minimize this risk.

Unless your doctor advises you to limit fluid intake, drink plenty of non-caffeinated liquids after taking this medication to stay hydrated.

You may find that bright lights are bothersome; wearing sunglasses can help alleviate this discomfort.

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.

For pediatric patients, this medication should be used with caution, as the risk of certain side effects may be higher in children.

Some formulations of this medication contain benzyl alcohol. If possible, avoid using products with benzyl alcohol in newborns or infants, as serious side effects can occur in these young patients, particularly when combined with other medications containing benzyl alcohol. Consult your doctor to determine if the product you are using contains benzyl alcohol.

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 of this medication to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Exaggerated anticholinergic effects: severe dry mouth, blurred vision, dilated pupils, flushing, fever, tachycardia, hypertension, central nervous system excitation (restlessness, confusion, delirium, hallucinations, seizures), urinary retention, paralytic ileus.

What to Do:

Contact emergency services or poison control immediately (Call 1-800-222-1222). Treatment is supportive. Physostigmine may be used to reverse central anticholinergic effects if severe and life-threatening.

Drug Interactions

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Major Interactions

  • Potassium chloride (oral solid dosage forms): Increased risk of GI lesions due to decreased GI motility.
  • Other anticholinergics (e.g., atropine, scopolamine, tricyclic antidepressants, phenothiazines, antihistamines): Potentiation of anticholinergic effects (dry mouth, urinary retention, blurred vision, constipation).
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Moderate Interactions

  • Opioid analgesics: May exacerbate constipation and urinary retention.
  • Antacids: May decrease absorption of oral glycopyrrolate (not relevant for injection).
  • Drugs that prolong QT interval: Theoretical risk of additive effect, though glycopyrrolate's effect on QT is minimal at therapeutic doses.

Monitoring

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Baseline Monitoring

Patient history (glaucoma, urinary retention, prostatic hypertrophy, tachycardia)

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

Frequency: Continuously during anesthesia; periodically post-op.

Target: Maintain within acceptable physiological limits.

Action Threshold: Significant tachycardia or bradycardia (if used for vagal block).

Secretions (salivary, bronchial)

Frequency: Clinical observation.

Target: Reduced to desired level.

Action Threshold: Excessive secretions or overly dry mucous membranes.

Urinary Output

Frequency: Periodically, especially in post-operative period.

Target: Adequate urinary flow.

Action Threshold: Urinary retention.

Bowel Sounds/Motility

Frequency: Clinical observation.

Target: Return of normal bowel function post-op.

Action Threshold: Severe constipation or ileus.

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Symptom Monitoring

  • Dry mouth
  • Blurred vision
  • Urinary retention
  • Constipation
  • Tachycardia
  • Flushing
  • Dizziness
  • Nausea/Vomiting

Special Patient Groups

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Pregnancy

Category B. Animal studies have not shown fetal harm, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed.

Trimester-Specific Risks:

First Trimester: No known specific risks identified, but generally avoided unless essential.
Second Trimester: Considered relatively safe if indicated.
Third Trimester: May inhibit uterine contractions and lactation. Use with caution near term.
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Lactation

Excreted in breast milk. Potential for anticholinergic effects in the infant (e.g., dry mouth, constipation, decreased sweating, tachycardia). May also decrease milk production. Use with caution; consider alternatives or monitor infant closely.

Infant Risk: Low to Moderate (L3 - L4 depending on dose and infant age/health).
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Pediatric Use

Dosing is weight-based. Infants and young children may be more susceptible to the effects of anticholinergics, especially hyperthermia. Use with caution in infants with Down syndrome, spastic paralysis, or brain damage due to increased sensitivity.

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Geriatric Use

Increased sensitivity to anticholinergic effects (e.g., dry mouth, constipation, urinary retention, confusion, blurred vision). Start with lower doses and titrate carefully. Increased risk of falls due to potential for dizziness or blurred vision.

Clinical Information

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Clinical Pearls

  • Glycopyrrolate is preferred over atropine for preoperative antisialagogue effects when CNS effects are undesirable, as it does not readily cross the blood-brain barrier.
  • When used for reversal of neuromuscular blockade, it should be administered concurrently with the cholinesterase inhibitor (e.g., neostigmine) to minimize muscarinic side effects.
  • Monitor for urinary retention, especially in elderly males with prostatic hypertrophy.
  • Can cause significant dry mouth, which can be uncomfortable for patients.
  • The 0.6mg/3ml concentration means 0.2mg/ml, which is a common concentration for injection.
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Alternative Therapies

  • Atropine (another anticholinergic, but crosses BBB)
  • Scopolamine (another anticholinergic, crosses BBB, often used for nausea/vomiting)
  • Hyoscyamine (another anticholinergic, primarily for GI spasms)
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Cost & Coverage

Average Cost: Varies widely by supplier and contract per 3ml vial
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (Generic)
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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, and do not take medication prescribed for someone else. 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. Unless instructed otherwise, avoid flushing medications down the toilet or pouring them down the drain. If you are unsure about the correct disposal method, consult your pharmacist for guidance. Many communities offer 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, 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 amount, and the time it was taken to ensure timely and effective treatment.