Glycopyrrolate 0.2mg/ml Inj, 2ml

Manufacturer MEITHEAL PHARMACEUTICALS 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
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 is a medication given by injection, often before surgery or during anesthesia. It helps to dry up saliva and other secretions in your mouth and airways, making it safer for procedures. It can also help to reverse the effects of certain muscle relaxants used 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. Adhere to the dosage instructions provided by your healthcare team. This medication is administered via injection into a muscle or vein.

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

If you miss a dose, contact your doctor promptly to receive guidance on the next steps to take.
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Lifestyle & Tips

  • Report any difficulty urinating or severe constipation.
  • Report any vision changes or eye pain.
  • Stay hydrated to help with dry mouth.

Dosing & Administration

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Adult Dosing

Standard Dose: Pre-anesthetic: 0.004 mg/kg IM/IV 30-60 min prior to anesthesia. Reversal of Neuromuscular Blockade: 0.2 mg IV for each 1 mg neostigmine or 5 mg pyridostigmine administered simultaneously.
Dose Range: 0.004 - 0.008 mg

Condition-Specific Dosing:

pre_anesthetic: 0.004 mg/kg IM/IV, up to 0.2 mg total, 30-60 min prior to anesthesia or at time of induction. Max single dose 0.4 mg.
reversal_neuromuscular_blockade: 0.2 mg IV for each 1 mg neostigmine or 5 mg pyridostigmine administered simultaneously. Administer IV as a single dose or in divided doses up to a total of 1 mg.
peptic_ulcer_adjunct: 0.1 mg IM/IV every 4 hours, 3-4 times daily (rarely used for this indication now).
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Pediatric Dosing

Neonatal: Not established for routine use. Use with extreme caution in infants with spastic paralysis or brain damage due to increased sensitivity to anticholinergics.
Infant: Pre-anesthetic (1 month to 2 years): 0.004-0.008 mg/kg IM/IV. Reversal of Neuromuscular Blockade: 0.2 mg IV for each 1 mg neostigmine or 5 mg pyridostigmine administered simultaneously.
Child: Pre-anesthetic (>2 years): 0.004-0.008 mg/kg IM/IV. Reversal of Neuromuscular Blockade: 0.2 mg IV for each 1 mg neostigmine or 5 mg pyridostigmine administered simultaneously.
Adolescent: Pre-anesthetic: 0.004-0.008 mg/kg IM/IV. Reversal of Neuromuscular Blockade: 0.2 mg IV for each 1 mg neostigmine or 5 mg pyridostigmine administered simultaneously.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment recommended.
Moderate: Use with caution. Consider dose reduction or extended dosing interval due to primary renal excretion.
Severe: Use with caution. Consider significant dose reduction or extended dosing interval. Avoid if possible.
Dialysis: Glycopyrrolate is not significantly removed by hemodialysis. Dose adjustment likely needed 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 blocks the action of acetylcholine at muscarinic receptors located on exocrine glands, smooth muscles, and the heart. This blockade leads to a reduction in salivary, tracheobronchial, and pharyngeal secretions, as well as a decrease in the volume and acidity of gastric secretions. It also produces vagal blockade, resulting in increased heart rate and bronchodilation. Due to its quaternary ammonium structure, it is highly ionized and does not readily cross the blood-brain barrier, minimizing central nervous system effects.
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Pharmacokinetics

Absorption:

Bioavailability: Not available (IV/IM administration bypasses absorption phase)
Tmax: IM: 30-45 minutes; IV: Immediate
FoodEffect: Not applicable for injectable form

Distribution:

Vd: 0.42 Âą 0.22 L/kg (adults)
ProteinBinding: Not extensively protein bound (approx. 10-30%)
CnssPenetration: Limited

Elimination:

HalfLife: IV: 0.83 Âą 0.27 hours (initial), 1.6 Âą 0.5 hours (terminal); IM: 0.33-1.25 hours
Clearance: 0.54 Âą 0.14 L/kg/hr
ExcretionRoute: Primarily renal (85% unchanged drug)
Unchanged: Approximately 85% (renal)
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Pharmacodynamics

OnsetOfAction: IV: 1 minute; IM: 15-30 minutes
PeakEffect: IV: 1-2 minutes (cardiac effects), 5-10 minutes (antisialagogue); IM: 30-45 minutes
DurationOfAction: IV: 2-3 hours; IM: 6-8 hours (antisialagogue effect)

Safety & Warnings

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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
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 persist, contact your doctor:

Dry mouth
Upset stomach or vomiting
Nasal congestion
Dizziness, drowsiness, fatigue, or weakness
Blurred vision
Flushing
Changes in taste
Headache
Feeling nervous or restless
* 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 eye pain
  • Difficulty urinating or inability to urinate
  • Severe constipation or abdominal pain
  • Fast or irregular heartbeat
  • Confusion or unusual excitement (rare with injectable form)
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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 conditions and circumstances to ensure safe treatment:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reactions you experienced, including the symptoms that occurred.
Certain health problems, including:
+ Heart issues related to bleeding
+ Glaucoma
+ Gastrointestinal (GI) problems, such as:
- Bowel blockage
- Slow-moving GI tract
- Colitis
- Bleeding ulcer
+ Myasthenia gravis
+ Difficulty urinating
A history of 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 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 belong to this class, ask your doctor.

This list is not exhaustive, and it is crucial to disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems to your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dose of any medication without consulting your doctor first.
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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, using marijuana or other cannabis products, or taking prescription or over-the-counter 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 this medication can increase the risk of heat stroke, especially in hot weather or during physical activity. Take necessary precautions to stay cool and hydrated.

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

You may be sensitive to bright lights while taking this medication. 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.

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

Some formulations of this medication may contain benzyl alcohol. If possible, avoid using products with benzyl alcohol in newborns or 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 the product contains benzyl alcohol.

If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
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Overdose Information

Overdose Symptoms:

  • Exaggerated anticholinergic effects: severe dry mouth, blurred vision, dilated pupils, hot/dry skin, fever, flushing, tachycardia, palpitations, urinary retention, constipation, CNS excitation (restlessness, confusion, hallucinations, delirium, seizures), respiratory depression, coma.

What to Do:

Call 911 or Poison Control (1-800-222-1222). Treatment is supportive. Physostigmine may be used to reverse severe central anticholinergic effects, but is generally avoided due to potential for adverse effects (e.g., bradycardia, seizures).

Drug Interactions

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Major Interactions

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

  • Cholinesterase inhibitors (e.g., donepezil, rivastigmine, galantamine): Glycopyrrolate may antagonize the therapeutic effects of cholinesterase inhibitors.
  • Antacids: May interfere with absorption of oral glycopyrrolate (not relevant for injectable form, but good to note for general drug class).
  • Opioid analgesics: Increased risk of severe constipation and/or paralytic ileus.
  • Digoxin: May increase digoxin levels due to delayed gastric emptying (for oral forms).

Monitoring

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Baseline Monitoring

Patient history (glaucoma, urinary retention, GI obstruction, cardiac disease)

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 anticholinergic effects.

Timing: Prior to administration

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Routine Monitoring

Heart rate

Frequency: Continuously during anesthesia/reversal; periodically post-op

Target: Individualized, avoid significant tachycardia

Action Threshold: Persistent tachycardia, arrhythmias

Secretions (oral, respiratory)

Frequency: Continuously during anesthesia/reversal; periodically post-op

Target: Reduced to desired level

Action Threshold: Excessive secretions, aspiration risk

Urinary output

Frequency: Periodically post-op

Target: Adequate

Action Threshold: Urinary retention

Bowel sounds/function

Frequency: Periodically post-op

Target: Return of normal function

Action Threshold: Constipation, ileus

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Symptom Monitoring

  • Dry mouth
  • Blurred vision
  • Urinary retention
  • Constipation
  • Tachycardia
  • Palpitations
  • Dizziness
  • Headache
  • Nervousness
  • Flushing
  • Fever (especially in children)

Special Patient Groups

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Pregnancy

Category B. Animal studies have not shown harm, but human studies are limited. Use only if clearly needed.

Trimester-Specific Risks:

First Trimester: Limited data, but generally considered low risk based on animal studies.
Second Trimester: Limited data, generally considered low risk.
Third Trimester: Limited data. May inhibit uterine contractions and cause fetal tachycardia. Use with caution near term.
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Lactation

Excreted in breast milk in small amounts. Potential for anticholinergic effects in the infant (e.g., dry mouth, constipation, urinary retention, decreased milk production). Use with caution, monitor infant for adverse effects.

Infant Risk: L3 (Moderate risk - possible adverse effects on breastfed infant; use only if benefits outweigh risks).
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Pediatric Use

Infants and young children, especially those with spastic paralysis or brain damage, may be more sensitive to the effects of anticholinergics and are more prone to developing fever due to suppression of sweat glands. Use with caution and monitor closely for signs of anticholinergic toxicity or hyperthermia.

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Geriatric Use

Elderly patients may be more susceptible to anticholinergic side effects, particularly urinary retention, constipation, and confusion (though CNS effects are less common with glycopyrrolate due to poor BBB penetration). Use with caution and consider lower initial doses.

Clinical Information

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Clinical Pearls

  • Glycopyrrolate is preferred over atropine for reversal of neuromuscular blockade due to less tachycardia and less CNS effects.
  • Its quaternary ammonium structure limits CNS penetration, making it less likely to cause central anticholinergic side effects (e.g., delirium, sedation) compared to tertiary amines like atropine or scopolamine.
  • Primarily eliminated unchanged by the kidneys; dose adjustment is crucial in renal impairment.
  • Effective antisialagogue, often used pre-operatively to reduce oral and respiratory secretions and prevent aspiration.
  • Can cause significant dry mouth, which can be distressing for patients.
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Alternative Therapies

  • Atropine (for antisialagogue or bradycardia, but with more CNS effects and tachycardia)
  • Scopolamine (for antisialagogue, but with significant CNS effects)
  • Hyoscyamine (for GI spasm, but less commonly used as injectable antisialagogue)
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Cost & Coverage

Average Cost: Varies widely per 2ml 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 for further guidance. 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 to do so by a healthcare professional, do not flush medications down the toilet or drain. 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 medical attention. Be prepared to provide information about the medication taken, the amount, and the time of ingestion.