Robinul 1mg Tablets
It is used to treat GI (gastrointestinal) ulcers.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
Jun 1961
DEA Schedule
Not Controlled
Overview
What is this medicine?
Glycopyrrolate is a medication that helps reduce certain body secretions, like stomach acid, saliva, and sweat. It works by blocking the action of a natural chemical in your body called acetylcholine. It's often used to treat conditions like excessive drooling or to help with stomach ulcers.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature in a dry location, avoiding bathrooms. Keep all medications in a secure place, out of the reach of children and pets. 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. Instead, consult with your pharmacist for guidance on the proper disposal method. You may also want to inquire about drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature in a dry location, avoiding bathrooms. Keep all medications in a secure place, out of the reach of children and pets. 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. Instead, consult with your pharmacist for guidance on the proper disposal method. You may also want to inquire about drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take this medication on an empty stomach, at least one hour before or two hours after meals, to ensure proper absorption.
- Drink plenty of water to help with dry mouth and prevent constipation.
- Avoid activities that may lead to overheating, as this medication can reduce sweating and increase the risk of heat stroke.
- Be cautious when driving or operating machinery until you know how this medication affects you, as it can cause blurred vision or dizziness.
- Avoid alcohol, as it may worsen side effects like dizziness or drowsiness.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
1 mg three times daily or 2 mg two to three times daily
Dose Range:
1 - 8 mg
Condition-Specific Dosing:
peptic_ulcer:
1 mg three times daily or 2 mg two to three times daily. Some patients may require 2 mg three times daily. Maximum recommended daily dosage is 8 mg.
excessive_secretions_sialorrhea:
1-2 mg two to three times daily, adjusted to patient response and tolerability. Max 8 mg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for Robinul tablets. For sialorrhea, glycopyrrolate oral solution (Cuvposa) is available for children 3-16 years: initial 0.02 mg/kg three times daily, titrated up to 0.1 mg/kg three times daily (max 1.5-3 mg/dose or 6-12 mg/day depending on weight).
Adolescent:
Not established for Robinul tablets. For sialorrhea, glycopyrrolate oral solution (Cuvposa) is available for children 3-16 years: initial 0.02 mg/kg three times daily, titrated up to 0.1 mg/kg three times daily (max 1.5-3 mg/dose or 6-12 mg/day depending on weight).
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment guidelines, use with caution.
Moderate:
Use with caution; consider lower doses and monitor for anticholinergic effects due to renal excretion.
Severe:
Use with caution; consider lower doses and monitor for anticholinergic effects due to renal excretion. Avoid if possible.
Dialysis:
Not well studied; likely not dialyzable. Use with extreme caution and monitor closely.
Hepatic Impairment:
Mild:
No specific adjustment guidelines, as hepatic metabolism is minor.
Moderate:
No specific adjustment guidelines, as hepatic metabolism is minor.
Severe:
No specific adjustment guidelines, as hepatic metabolism is minor.
Pharmacology
Mechanism of Action
Glycopyrrolate is a synthetic quaternary ammonium anticholinergic agent. It competitively inhibits the action of acetylcholine at muscarinic receptors located on smooth muscles, cardiac muscle, exocrine glands, and in peripheral ganglia. It reduces the volume and acidity of gastric secretions and inhibits excessive pharyngeal, tracheal, and bronchial secretions. 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 therapeutic doses.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 3% (oral)
Tmax:
1-3 hours
FoodEffect:
Food significantly decreases the extent of absorption (AUC) and peak concentration (Cmax) of glycopyrrolate. Should be taken at least one hour before or two hours after meals.
Distribution:
Vd:
Not readily available for oral form, but generally high due to tissue distribution. For IV, ~0.42 L/kg.
ProteinBinding:
Not readily available, but generally low for quaternary ammonium compounds.
CnssPenetration:
Limited
Elimination:
HalfLife:
0.83 hours (oral, terminal half-life can be longer, up to 3.3 hours in some studies)
Clearance:
Not readily available for oral form.
ExcretionRoute:
Primarily renal (urine) and biliary/fecal.
Unchanged:
Approximately 85% of an intravenous dose is excreted unchanged in urine within 48 hours. For oral, a significant portion is unabsorbed and excreted in feces.
Pharmacodynamics
OnsetOfAction:
Within 1 hour (oral)
PeakEffect:
1-3 hours
DurationOfAction:
4-6 hours
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help 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 attention 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 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 medical attention 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 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 constipation or abdominal pain
- Difficulty urinating or inability to urinate
- Severe blurred vision or eye pain
- Rapid or irregular heartbeat
- Signs of heat stroke (e.g., fever, confusion, hot dry skin)
- Allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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 situations to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reaction you experienced, including the symptoms.
Certain health conditions, such as:
+ Heart problems caused by bleeding
+ Glaucoma
+ Gastrointestinal (GI) issues, including 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 slow GI tract movement or increase the risk of bowel blockage. There are many medications that can cause this; consult your doctor or pharmacist if you are unsure.
Concurrent 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 disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions to your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your existing treatments and health status. Never start, stop, or adjust the dosage of any medication without consulting your doctor.
It is essential to inform your doctor about the following conditions and situations to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reaction you experienced, including the symptoms.
Certain health conditions, such as:
+ Heart problems caused by bleeding
+ Glaucoma
+ Gastrointestinal (GI) issues, including 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 slow GI tract movement or increase the risk of bowel blockage. There are many medications that can cause this; consult your doctor or pharmacist if you are unsure.
Concurrent 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 disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions to your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your existing treatments and health status. Never start, stop, or adjust the dosage of any medication without 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 any activity that requires alertness and clear vision, ensure 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 mitigate this side effect.
Be cautious when exposed to high temperatures or engaging in 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.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to both you and your baby.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, ensure 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 mitigate this side effect.
Be cautious when exposed to high temperatures or engaging in 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.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to both you and your baby.
Overdose Information
Overdose Symptoms:
- Exaggerated anticholinergic effects: severe dry mouth, blurred vision, dilated pupils, hot dry skin, fever, flushing, rapid heart rate, high blood pressure, urinary retention, constipation, central nervous system excitation (restlessness, confusion, hallucinations, delirium, seizures, coma).
What to Do:
Call 911 or your local poison control center immediately (1-800-222-1222 in the US). Medical management may include supportive care, gastric lavage, activated charcoal, and physostigmine (an acetylcholinesterase inhibitor) for severe central anticholinergic symptoms.
Drug Interactions
Contraindicated Interactions
- Potassium chloride (solid oral dosage forms) - increased risk of GI lesions due to prolonged contact time.
- Other anticholinergics (e.g., atropine, scopolamine, tricyclic antidepressants, phenothiazines, quinidine, disopyramide, antihistamines) - additive anticholinergic effects.
Major Interactions
- Drugs that slow GI motility (e.g., opioids, antidiarrheals) - increased risk of severe constipation or paralytic ileus.
- Antacids - may interfere with absorption of glycopyrrolate; administer glycopyrrolate at least 1 hour before antacids.
- Drugs with narrow therapeutic index that require specific GI transit time for absorption (e.g., digoxin, ketoconazole) - altered absorption.
Moderate Interactions
- Corticosteroids - may increase intraocular pressure.
- Monoamine Oxidase Inhibitors (MAOIs) - theoretical risk of additive effects on blood pressure (less likely with glycopyrrolate due to limited CNS penetration).
- Topical ophthalmic anticholinergics - additive mydriatic effect.
Minor Interactions
- None specifically noted for minor severity.
Monitoring
Baseline Monitoring
Baseline vital signs (heart rate, blood pressure)
Rationale: To establish baseline and monitor for anticholinergic effects like tachycardia.
Timing: Prior to initiation of therapy.
Assessment of urinary function (e.g., history of urinary retention)
Rationale: To identify predisposition to urinary retention, a common anticholinergic side effect.
Timing: Prior to initiation of therapy.
Ophthalmic examination (e.g., history of glaucoma)
Rationale: To identify risk of acute angle-closure glaucoma, a contraindication.
Timing: Prior to initiation of therapy.
Routine Monitoring
Anticholinergic side effects (dry mouth, blurred vision, constipation, urinary retention, tachycardia)
Frequency: Regularly, especially during dose titration and with long-term use.
Target: Minimize to tolerable levels.
Action Threshold: If severe or intolerable, consider dose reduction or discontinuation.
Bowel movements
Frequency: Daily/weekly
Target: Regular, soft stools.
Action Threshold: If severe constipation develops, consider laxatives or dose adjustment.
Urinary output/difficulty
Frequency: Daily
Target: Normal voiding pattern.
Action Threshold: If urinary retention or significant difficulty voiding, seek medical attention.
Symptom Monitoring
- Dry mouth
- Blurred vision
- Constipation
- Urinary retention or difficulty urinating
- Tachycardia (fast heart rate)
- Dizziness
- Headache
- Nervousness
- Difficulty swallowing
- Heat intolerance (due to decreased sweating)
Special Patient Groups
Pregnancy
Glycopyrrolate is Pregnancy Category B. While animal studies have not shown harm, there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed.
Trimester-Specific Risks:
First Trimester:
No increased risk of congenital anomalies observed in animal studies.
Second Trimester:
No specific risks identified.
Third Trimester:
May inhibit uterine contractions and cause fetal tachycardia. Use with caution near term.
Lactation
Glycopyrrolate is excreted in breast milk. Due to the potential for serious adverse reactions in breastfed infants (e.g., anticholinergic effects, reduced milk production), a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Risk L3 (Moderately Safe - Possible risk to infant; use only if benefit outweighs risk).
Pediatric Use
Safety and effectiveness of Robinul tablets in pediatric patients have not been established. For sialorrhea in children, a specific oral solution formulation (Cuvposa) is available with age-specific dosing guidelines.
Geriatric Use
Elderly patients may be more susceptible to the anticholinergic effects of glycopyrrolate, particularly dry mouth, constipation, urinary retention, and confusion. Use with caution and consider lower initial doses and slower titration. Monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Glycopyrrolate's quaternary ammonium structure limits its ability to cross the blood-brain barrier, leading to fewer CNS side effects (e.g., sedation, confusion) compared to tertiary anticholinergics like atropine or scopolamine.
- Oral bioavailability is low, and food significantly reduces absorption, so consistent administration on an empty stomach is crucial for efficacy.
- Primarily used for reducing secretions (e.g., pre-operatively, for sialorrhea in neurological conditions) and historically for peptic ulcer disease (though less common now due to PPIs/H2 blockers).
- Patients should be advised about potential for dry mouth, constipation, and urinary retention. Strategies like increased fluid intake, fiber, and regular voiding should be discussed.
- Due to reduced sweating, patients should be warned about the risk of heat prostration in hot environments or during exercise.
Alternative Therapies
- For peptic ulcer disease: Proton Pump Inhibitors (PPIs) (e.g., omeprazole, pantoprazole), H2-receptor antagonists (e.g., famotidine, ranitidine).
- For sialorrhea: Botulinum toxin injections (into salivary glands), scopolamine patches (transdermal, but with more CNS effects), atropine eye drops (off-label sublingual).
- For excessive sweating (hyperhidrosis): Topical antiperspirants (aluminum chloride), botulinum toxin injections, iontophoresis, oral oxybutynin (off-label).
Cost & Coverage
Average Cost:
Varies, typically $30-$100+ per 100 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (generic), Tier 3 (brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.