Glyburide 5mg Tablets
It is used to help control blood sugar in people with type 2 diabetes.
Drug Class
Antidiabetic Agent
Pharmacologic Class
Sulfonylurea
Pregnancy Category
Category B (some sources list C, but B is more common for non-micronized glyburide)
FDA Approved
Jun 1984
DEA Schedule
Not Controlled
Overview
What is this medicine?
Glyburide is a medication used to treat type 2 diabetes. It helps your body release more insulin from your pancreas, which lowers your blood sugar levels. It's important to take it exactly as prescribed, usually with your first meal of the day.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication with meals, and if you're taking it once a day, take it with your first meal of the day. Continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well. Establish a routine by taking your medication at the same time every day. Additionally, be sure to follow the diet and exercise plan recommended by your doctor.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry place, avoiding the bathroom. Keep the lid tightly closed and store all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember, with a meal. 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 a missed dose.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication with meals, and if you're taking it once a day, take it with your first meal of the day. Continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well. Establish a routine by taking your medication at the same time every day. Additionally, be sure to follow the diet and exercise plan recommended by your doctor.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry place, avoiding the bathroom. Keep the lid tightly closed and store all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember, with a meal. 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 a missed dose.
Lifestyle & Tips
- Take glyburide with breakfast or the first main meal of the day to reduce the risk of stomach upset and to align with insulin release.
- Maintain a consistent meal schedule and carbohydrate intake to prevent hypoglycemia.
- Engage in regular physical activity as advised by your doctor, as exercise can lower blood sugar.
- Monitor your blood glucose levels regularly as instructed by your healthcare provider.
- Carry a source of fast-acting sugar (e.g., glucose tablets, hard candy, fruit juice) to treat mild to moderate hypoglycemia.
- Avoid or limit alcohol consumption, as it can increase the risk of hypoglycemia and cause a disulfiram-like reaction.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial: 2.5-5 mg once daily with breakfast or first main meal. Maintenance: 1.25-20 mg once daily or in divided doses.
Dose Range:
1.25 - 20 mg
Condition-Specific Dosing:
initial_dose:
2.5-5 mg once daily
maintenance_dose:
1.25-20 mg once daily or in divided doses, adjusted in increments of 2.5 mg at weekly intervals based on blood glucose response.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (generally not recommended for pediatric use)
Dose Adjustments
Renal Impairment:
Mild:
Initial dose reduction may be considered (e.g., 1.25 mg daily).
Moderate:
Use with caution; significant dose reduction required (e.g., 1.25 mg daily or every other day). Increased risk of hypoglycemia.
Severe:
Contraindicated or not recommended due to high risk of severe, prolonged hypoglycemia.
Dialysis:
Contraindicated or not recommended due to high risk of severe, prolonged hypoglycemia.
Hepatic Impairment:
Mild:
Initial dose reduction may be considered (e.g., 1.25 mg daily).
Moderate:
Use with caution; significant dose reduction required (e.g., 1.25 mg daily or every other day). Increased risk of hypoglycemia.
Severe:
Contraindicated or not recommended due to high risk of severe, prolonged hypoglycemia.
Pharmacology
Mechanism of Action
Glyburide is a second-generation sulfonylurea that lowers blood glucose by stimulating the release of insulin from the beta cells of the pancreatic islets. It binds to the sulfonylurea receptor (SUR1) on the beta-cell membrane, leading to the closure of ATP-sensitive potassium channels, depolarization of the membrane, and opening of voltage-gated calcium channels. The influx of calcium triggers insulin secretion.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 50-60% (non-micronized)
Tmax:
2-4 hours
FoodEffect:
Food may delay absorption but does not significantly affect the extent of absorption.
Distribution:
Vd:
Approximately 0.1 L/kg
ProteinBinding:
Greater than 99% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 10 hours (range 4-10 hours)
Clearance:
Not available
ExcretionRoute:
Approximately 50% in urine and 50% in feces (as metabolites)
Unchanged:
Less than 1%
Pharmacodynamics
OnsetOfAction:
Approximately 1 hour
PeakEffect:
Approximately 2-4 hours
DurationOfAction:
Approximately 12-24 hours
Safety & Warnings
Side Effects
Urgent 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 medical attention immediately:
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
Changes in eyesight
Muscle or joint pain
Low blood sugar (hypoglycemia), which may be more likely when taking this medication with other diabetes drugs. Symptoms of low blood sugar include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Follow your doctor's instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or some fruit juices.
Additionally, be aware of the following potentially serious side effects:
Low blood cell counts, which can increase the risk of bleeding problems, infections, or anemia. If you experience:
+ Signs of infection, such as fever, chills, or sore throat
+ Unexplained bruising or bleeding
+ Feeling very tired or weak
Liver problems. If you notice:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Most people taking this medication will not experience serious side effects, but some may occur. If you notice any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
Feeling full
Upset stomach
Heartburn
* Weight gain
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact 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 immediately:
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
Changes in eyesight
Muscle or joint pain
Low blood sugar (hypoglycemia), which may be more likely when taking this medication with other diabetes drugs. Symptoms of low blood sugar include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Follow your doctor's instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or some fruit juices.
Additionally, be aware of the following potentially serious side effects:
Low blood cell counts, which can increase the risk of bleeding problems, infections, or anemia. If you experience:
+ Signs of infection, such as fever, chills, or sore throat
+ Unexplained bruising or bleeding
+ Feeling very tired or weak
Liver problems. If you notice:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Most people taking this medication will not experience serious side effects, but some may occur. If you notice any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
Feeling full
Upset stomach
Heartburn
* Weight gain
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact 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:
- Symptoms of hypoglycemia (low blood sugar): sweating, shakiness, dizziness, confusion, hunger, irritability, headache, blurred vision, rapid heartbeat. If these occur, check blood sugar and consume 15-20 grams of fast-acting carbohydrate.
- Symptoms of severe hypoglycemia: seizures, loss of consciousness. Seek immediate medical attention.
- Symptoms of liver problems (rare): unusual tiredness, yellowing of skin or eyes (jaundice), dark urine, nausea, vomiting, stomach pain. Report these to your doctor immediately.
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 symptoms you experienced.
If you have a condition that affects the acidity of your blood.
If you have type 1 diabetes, as this medication is not intended to treat this condition.
If you are currently taking bosentan, as this may interact with the medication.
* If the patient is a child, as this medication is not suitable for pediatric use.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication in combination with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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 symptoms you experienced.
If you have a condition that affects the acidity of your blood.
If you have type 1 diabetes, as this medication is not intended to treat this condition.
If you are currently taking bosentan, as this may interact with the medication.
* If the patient is a child, as this medication is not suitable for pediatric use.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication in combination with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
If you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), you should exercise caution, as this condition may increase the risk of anemia. Individuals of African, South Asian, Middle Eastern, and Mediterranean descent are more likely to have low G6PD levels.
Follow your doctor's instructions for monitoring your blood sugar levels. Additionally, have your blood work checked as directed by your doctor and discuss the results with them.
Avoid driving if you have experienced low blood sugar, as it can significantly increase the risk of accidents.
Before consuming alcohol, consult with your doctor to discuss any potential risks.
If you are also taking colesevelam, ensure that you take it at least 4 hours after taking this medication.
Be aware that stress, such as fever, infection, injury, or surgery, can affect blood sugar control. Changes in physical activity, exercise, or diet can also impact blood sugar levels.
This medication can cause low blood sugar, which may lead to seizures, loss of consciousness, permanent brain damage, and even death in severe cases. Discuss this risk with your doctor.
There is an increased risk of death from heart disease associated with this medication. Consult with your doctor to understand this risk.
This medication may increase your susceptibility to sunburn. Take necessary precautions when exposed to the sun, and inform your doctor if you experience excessive sunburn while taking this medication.
If you are 65 years or older, use this medication with caution, as you may be more prone to side effects.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor. It is crucial to discuss the benefits and risks of this medication to both you and your baby.
It is also important to note that infants born to mothers who took a similar medication during pregnancy have experienced low blood sugar. If you take this medication during pregnancy, your doctor may advise you to stop taking it before your due date. Consult with your doctor to determine the best course of action.
If you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), you should exercise caution, as this condition may increase the risk of anemia. Individuals of African, South Asian, Middle Eastern, and Mediterranean descent are more likely to have low G6PD levels.
Follow your doctor's instructions for monitoring your blood sugar levels. Additionally, have your blood work checked as directed by your doctor and discuss the results with them.
Avoid driving if you have experienced low blood sugar, as it can significantly increase the risk of accidents.
Before consuming alcohol, consult with your doctor to discuss any potential risks.
If you are also taking colesevelam, ensure that you take it at least 4 hours after taking this medication.
Be aware that stress, such as fever, infection, injury, or surgery, can affect blood sugar control. Changes in physical activity, exercise, or diet can also impact blood sugar levels.
This medication can cause low blood sugar, which may lead to seizures, loss of consciousness, permanent brain damage, and even death in severe cases. Discuss this risk with your doctor.
There is an increased risk of death from heart disease associated with this medication. Consult with your doctor to understand this risk.
This medication may increase your susceptibility to sunburn. Take necessary precautions when exposed to the sun, and inform your doctor if you experience excessive sunburn while taking this medication.
If you are 65 years or older, use this medication with caution, as you may be more prone to side effects.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor. It is crucial to discuss the benefits and risks of this medication to both you and your baby.
It is also important to note that infants born to mothers who took a similar medication during pregnancy have experienced low blood sugar. If you take this medication during pregnancy, your doctor may advise you to stop taking it before your due date. Consult with your doctor to determine the best course of action.
Overdose Information
Overdose Symptoms:
- Severe hypoglycemia (profound weakness, confusion, slurred speech, seizures, coma)
- Hypoglycemic shock
What to Do:
Immediately consume fast-acting carbohydrates. For severe cases, administer glucagon or seek emergency medical attention. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Contraindicated Interactions
- Bosentan (increased risk of hepatotoxicity)
Major Interactions
- Alcohol (increased risk of hypoglycemia, disulfiram-like reaction)
- Beta-blockers (mask symptoms of hypoglycemia, impair glucose counter-regulation)
- Fluconazole (increased glyburide levels, increased risk of hypoglycemia)
- NSAIDs (increased risk of hypoglycemia)
- Sulfonamides (increased risk of hypoglycemia)
- Chloramphenicol (increased risk of hypoglycemia)
- Warfarin (altered anticoagulant effect, increased risk of hypoglycemia)
- Corticosteroids (decreased hypoglycemic effect)
- Thiazide diuretics (decreased hypoglycemic effect)
- Rifampin (decreased glyburide levels, decreased hypoglycemic effect)
Moderate Interactions
- ACE inhibitors (may enhance glucose-lowering effect)
- MAO inhibitors (may enhance glucose-lowering effect)
- Salicylates (may enhance glucose-lowering effect)
- Cimetidine (may increase glyburide levels)
- Clarithromycin (may increase glyburide levels)
- Gemfibrozil (may increase glyburide levels)
- Colesevelam (decreased glyburide absorption, administer glyburide 4 hours before colesevelam)
Minor Interactions
- Chromium (may enhance glucose-lowering effect)
- Garlic (may enhance glucose-lowering effect)
Monitoring
Baseline Monitoring
HbA1c
Rationale: To establish baseline glycemic control and guide initial dosing.
Timing: Prior to initiation of therapy.
Fasting Plasma Glucose (FPG)
Rationale: To establish baseline glycemic control and guide initial dosing.
Timing: Prior to initiation of therapy.
Renal Function (SCr, eGFR)
Rationale: To assess kidney function, as glyburide is renally excreted and risk of hypoglycemia increases with renal impairment.
Timing: Prior to initiation of therapy.
Hepatic Function (ALT, AST, Bilirubin)
Rationale: To assess liver function, as glyburide is metabolized by the liver and risk of hypoglycemia increases with hepatic impairment.
Timing: Prior to initiation of therapy.
Routine Monitoring
HbA1c
Frequency: Every 3-6 months
Target: <7% (individualized)
Action Threshold: If target not met, consider dose adjustment or alternative therapy.
Fasting Plasma Glucose (FPG)
Frequency: Daily (patient self-monitoring) or as clinically indicated
Target: 80-130 mg/dL (individualized)
Action Threshold: Persistent readings outside target range; adjust dose or lifestyle.
Postprandial Glucose (PPG)
Frequency: As clinically indicated (patient self-monitoring)
Target: <180 mg/dL (individualized)
Action Threshold: Persistent readings outside target range; adjust dose or lifestyle.
Symptoms of Hypoglycemia
Frequency: Ongoing patient self-monitoring
Target: N/A
Action Threshold: If symptoms occur, check blood glucose and treat immediately. Report frequent episodes to provider.
Renal Function (SCr, eGFR)
Frequency: Annually or more frequently if clinically indicated (e.g., with concomitant nephrotoxic drugs or worsening renal function)
Target: Stable eGFR
Action Threshold: Significant decline in eGFR may require dose reduction or discontinuation.
Hepatic Function (ALT, AST, Bilirubin)
Frequency: Annually or more frequently if clinically indicated (e.g., with concomitant hepatotoxic drugs or worsening hepatic function)
Target: Within normal limits
Action Threshold: Significant elevation may require dose reduction or discontinuation.
Symptom Monitoring
- Symptoms of hypoglycemia: sweating, tremor, dizziness, hunger, confusion, irritability, headache, blurred vision, rapid heartbeat, anxiety, weakness, slurred speech, seizures, unconsciousness.
- Symptoms of hyperglycemia (if glycemic control is inadequate): increased thirst, increased urination, fatigue, blurred vision.
Special Patient Groups
Pregnancy
Generally not recommended during pregnancy. Insulin is the preferred treatment for glycemic control in pregnant women with diabetes. Glyburide is a Category B drug, but some sources list it as C due to potential for neonatal hypoglycemia. It crosses the placenta.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity, though data are mixed. Insulin is preferred.
Second Trimester:
Risk of neonatal hypoglycemia if used near term. Insulin is preferred.
Third Trimester:
Increased risk of neonatal hypoglycemia, macrosomia, and other adverse outcomes. Insulin is preferred.
Lactation
Not recommended during breastfeeding. Glyburide is excreted into breast milk and may cause hypoglycemia in the nursing infant. Insulin is generally preferred for glycemic control in lactating women.
Infant Risk:
Risk of hypoglycemia in the infant. Monitor infant for signs of hypoglycemia (e.g., lethargy, poor feeding, jitteriness).
Pediatric Use
Not recommended for use in pediatric patients due to lack of established safety and efficacy, and increased risk of hypoglycemia.
Geriatric Use
Use with extreme caution in elderly patients due to increased risk of severe, prolonged hypoglycemia, especially in those with impaired renal or hepatic function. Start with the lowest effective dose (e.g., 1.25 mg daily) and titrate slowly. Avoid in frail elderly or those with multiple comorbidities.
Clinical Information
Clinical Pearls
- Glyburide is a potent sulfonylurea with a relatively long duration of action, increasing the risk of hypoglycemia, especially in elderly patients or those with renal/hepatic impairment.
- Micronized glyburide (Glynase PresTab) has higher bioavailability and is not interchangeable with non-micronized glyburide (Diabeta) on a milligram-for-milligram basis.
- Always take glyburide with the first main meal of the day to minimize the risk of hypoglycemia and improve absorption.
- Patients should be educated on the symptoms and management of hypoglycemia.
- Consider alternative agents in patients with significant renal or hepatic dysfunction due to the high risk of hypoglycemia.
Alternative Therapies
- Other sulfonylureas (e.g., glipizide, glimepiride)
- Metformin
- DPP-4 inhibitors (e.g., sitagliptin, saxagliptin)
- SGLT2 inhibitors (e.g., empagliflozin, canagliflozin)
- GLP-1 receptor agonists (e.g., liraglutide, semaglutide)
- Thiazolidinediones (e.g., pioglitazone)
- Insulin therapy
Cost & Coverage
Average Cost:
$10 - $50 per 30 tablets (5mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (preferred generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is 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 it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't 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. When seeking help, be prepared to provide information about the medication taken, the amount, and the time it happened.