Glycopyrrolate 0.2mg/ml Inj, 1ml

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
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 to reverse the effects of certain muscle relaxants. It works by reducing body secretions like saliva and stomach acid, and can help control heart rate during medical procedures. It belongs to a class of drugs called anticholinergics.
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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 guidelines provided. 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 to determine the proper storage procedure.

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

  • Report any difficulty urinating or severe dry mouth.
  • Avoid activities requiring mental alertness (e.g., driving) until effects are known, especially if experiencing blurred vision or dizziness.

Dosing & Administration

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Adult Dosing

Standard Dose: Preoperative: 0.004 mg/kg IM/IV 30-60 minutes prior to anesthesia. Reversal of Neuromuscular Blockade: 0.2 mg IV for each 1 mg neostigmine or 5 mg pyridostigmine, administered simultaneously.
Dose Range: 0.1 - 0.4 mg

Condition-Specific Dosing:

preoperative: 0.004 mg/kg IM/IV, typically 0.1-0.2 mg, not to exceed 0.4 mg single dose or 0.8 mg in 24 hours.
reversal_of_neuromuscular_blockade: 0.2 mg IV for each 1 mg neostigmine or 5 mg pyridostigmine, administered simultaneously. May be given as a single dose or in divided doses up to a total of 1 mg.
peptic_ulcer_disease_acute: Not a primary indication for injection, but historically used 0.1-0.2 mg IM/IV every 4 hours, 3-4 times daily.
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Pediatric Dosing

Neonatal: Not established for routine use. Use with caution, 0.004-0.008 mg/kg IM/IV for preoperative use, not to exceed 0.1 mg single dose.
Infant: 0.004-0.008 mg/kg IM/IV for preoperative use, not to exceed 0.1 mg single dose.
Child: 0.004-0.008 mg/kg IM/IV for preoperative use, not to exceed 0.1 mg single dose.
Adolescent: 0.004 mg/kg IM/IV for preoperative use, not to exceed 0.4 mg single dose.
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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 increased plasma levels and half-life.
Severe: Use with caution. Consider dose reduction (e.g., 50% of usual dose) or extended dosing interval due to significantly increased plasma levels and half-life. Avoid if possible.
Dialysis: 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 smooth muscles, cardiac muscle, secretory glands, and peripheral autonomic ganglia. This antagonism leads to a reduction in salivary, tracheobronchial, and pharyngeal secretions, decreased gastric acid secretion, and blockade of cardiac vagal inhibitory reflexes.
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Pharmacokinetics

Absorption:

Bioavailability: Not applicable for IV/IM. Oral bioavailability is low (approx. 3%).
Tmax: IM: 30-45 minutes. IV: Immediate.
FoodEffect: Not applicable for injection.

Distribution:

Vd: 0.42 Âą 0.22 L/kg (adults)
ProteinBinding: Not extensively protein bound (approx. 10-30%).
CnssPenetration: Limited (due to quaternary ammonium structure, does not readily cross the blood-brain barrier).

Elimination:

HalfLife: 0.83 Âą 0.27 hours (IV, initial phase); 1.2-2.1 hours (terminal phase, IM/IV). Up to 3.3 hours in renal impairment.
Clearance: Not readily available, but primarily renal excretion.
ExcretionRoute: Primarily renal (85% within 48 hours, 50% unchanged). Small amount excreted in bile/feces.
Unchanged: Approximately 50% (IV/IM) to 85% (IV) excreted unchanged in urine.
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Pharmacodynamics

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

Safety & Warnings

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Side Effects

Serious Side Effects: Seek Medical Attention Immediately

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 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 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 anxious 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 or eyes
  • Blurred vision or difficulty focusing
  • Difficulty urinating or inability to urinate
  • Severe constipation
  • Fast or irregular heartbeat
  • Confusion or agitation
  • Fever without sweating
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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 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 reaction 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
+ Urination difficulties
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 drugs 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 discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with 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 change 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.

Before operating a vehicle or engaging in activities that require alertness and clear vision, wait until you understand how this medication affects you.

Consult your doctor before consuming alcohol, using marijuana or other cannabis products, or taking 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 minimize 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 severe side effects, 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, 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/dry skin, fever, flushing, tachycardia, hypertension, urinary retention, paralytic ileus, CNS excitation (restlessness, confusion, hallucinations, delirium, seizures, coma).

What to Do:

Supportive care. Physostigmine (cholinesterase inhibitor) may be used to reverse severe anticholinergic symptoms, particularly CNS effects. Call 1-800-222-1222 (Poison Control).

Drug Interactions

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Major Interactions

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

  • Antacids: May decrease absorption of oral glycopyrrolate (not relevant for injection).
  • Drugs that prolong QT interval: Theoretical risk of additive effect, though glycopyrrolate itself has minimal QT effect.
  • Opioids: Increased risk of constipation and urinary retention.
  • Digoxin: May increase digoxin levels due to delayed gastric emptying (not relevant for injection).
  • Metoclopramide: Antagonizes prokinetic effects of metoclopramide.

Monitoring

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Baseline Monitoring

Patient history (glaucoma, urinary retention, 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 (tachycardia, hypertension).

Timing: Prior to administration

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Routine Monitoring

Heart rate

Frequency: Continuously during anesthesia; periodically post-op

Target: Within patient's normal range, or as clinically indicated

Action Threshold: Significant tachycardia or bradycardia (if vagal blockade is excessive)

Blood pressure

Frequency: Continuously during anesthesia; periodically post-op

Target: Within patient's normal range

Action Threshold: Significant hypertension or hypotension

Urine output

Frequency: As clinically indicated, especially in post-op period

Target: Adequate for age/weight

Action Threshold: Urinary retention

Oral secretions

Frequency: Periodically

Target: Reduced but not excessively dry

Action Threshold: Excessive dryness or continued secretions

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Symptom Monitoring

  • Dry mouth
  • Blurred vision
  • Urinary retention
  • Constipation
  • Tachycardia
  • Palpitations
  • Dizziness
  • Headache
  • Nausea/vomiting
  • Nervousness

Special Patient Groups

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Pregnancy

Category B. Animal studies have not shown fetal harm. Limited human data suggest no increased risk of major birth defects. Use only if clearly needed.

Trimester-Specific Risks:

First Trimester: No increased risk of major birth defects observed in limited human data.
Second Trimester: No specific risks identified.
Third Trimester: May inhibit uterine contractions and cause fetal tachycardia. Use with caution near term.
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Lactation

L3 (Moderate risk). Glycopyrrolate is a quaternary ammonium compound, so it is poorly absorbed orally and poorly excreted into breast milk. However, small amounts may be present. Monitor infant for anticholinergic effects (e.g., dry mouth, constipation, urinary retention, decreased sweating, drowsiness).

Infant Risk: Low to moderate. Potential for anticholinergic effects in infant, especially if infant has impaired renal function or is premature. May decrease milk supply due to anticholinergic effects on prolactin.
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Pediatric Use

Use with caution, especially in infants and young children, due to increased susceptibility to anticholinergic effects (e.g., hyperthermia, CNS effects). Dosing is weight-based. Not recommended for routine use in neonates.

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Geriatric Use

Use with caution. Elderly patients are more susceptible to anticholinergic side effects (e.g., dry mouth, constipation, urinary retention, confusion, blurred vision, tachycardia). Start with lower doses and titrate carefully. Monitor for cognitive impairment and urinary retention.

Clinical Information

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Clinical Pearls

  • Glycopyrrolate is preferred over atropine for reversal of neuromuscular blockade due to less CNS penetration and less tachycardia.
  • Its quaternary ammonium structure limits CNS side effects, making it a good choice when central anticholinergic effects are undesirable.
  • Effective antisialagogue, reducing secretions during surgery and intubation.
  • Can be used to treat bradycardia in specific situations, though atropine is more commonly used for this purpose.
  • Patients with glaucoma (narrow-angle) or urinary retention (e.g., prostatic hypertrophy) are contraindications or require extreme caution.
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Alternative Therapies

  • Atropine (for antisialagogue, bradycardia, reversal of neuromuscular blockade)
  • Scopolamine (for antisialagogue, antiemetic, but with significant CNS effects)
  • Hyoscyamine (for GI spasm, secretions)
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Cost & Coverage

Average Cost: Varies, typically $5 - $20 per 1ml vial (0.2mg/ml)
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 guidance. To ensure your safety and the safety of others, never share your medication with anyone, and do not take medication prescribed to someone else.

All medications should be stored in a secure location, out of the reach of children and pets, to prevent accidental ingestion. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. Instead, consult with your pharmacist to determine the best disposal method, as some communities have drug take-back programs in place.

Additionally, some medications may come with a separate 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, it is crucial to 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 detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred, to ensure prompt and effective treatment.