Glyburide 2.5mg Tablets

Manufacturer TEVA PHARMACEUTICALS USA Active Ingredient Glyburide(GLYE byoor ide) Pronunciation GLYE-byoor-ide
It is used to help control blood sugar in people with type 2 diabetes.
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Drug Class
Antidiabetic Agent
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Pharmacologic Class
Sulfonylurea
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Pregnancy Category
Category C
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FDA Approved
Aug 1984
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Glyburide is a medicine used to help control high blood sugar in people with type 2 diabetes. It works by helping your body release more insulin, a natural hormone that lowers blood sugar.
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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, preferably with the first meal of the day if you are taking it once daily. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel well. Establish a routine by taking your medication at the same time every day. Additionally, 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 is 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.
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Lifestyle & Tips

  • Take glyburide exactly as prescribed, usually once daily with breakfast or your first main meal.
  • Do not skip meals while taking this medication, as it can increase the risk of low blood sugar (hypoglycemia).
  • Follow a healthy diet plan recommended by your doctor or dietitian.
  • Engage in regular physical activity as advised by your healthcare provider.
  • Monitor your blood sugar levels regularly as instructed by your doctor.
  • Carry a source of fast-acting sugar (e.g., glucose tablets, hard candy, fruit juice) to treat low blood sugar.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 2.5-5 mg once daily with breakfast or first main meal. Maintenance: 1.25-20 mg daily.
Dose Range: 1.25 - 20 mg

Condition-Specific Dosing:

Type 2 Diabetes Mellitus: Initial: 2.5-5 mg once daily. Titrate in increments of 1.25-2.5 mg at weekly intervals based on blood glucose response. Max: 20 mg daily. Doses >10 mg/day may be divided twice daily.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment, but monitor closely.
Moderate: Use with caution; consider lower initial doses (e.g., 1.25 mg daily) and careful titration. Increased risk of hypoglycemia.
Severe: Contraindicated (CrCl < 30 mL/min) due to increased risk of severe, prolonged hypoglycemia.
Dialysis: Contraindicated. Not significantly removed by hemodialysis.

Hepatic Impairment:

Mild: Use with caution; consider lower initial doses (e.g., 1.25 mg daily) and careful titration.
Moderate: Use with caution; consider lower initial doses (e.g., 1.25 mg daily) and careful titration. Increased risk of hypoglycemia.
Severe: Contraindicated due to increased risk of severe, prolonged hypoglycemia.

Pharmacology

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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 closure of ATP-sensitive potassium channels, depolarization of the membrane, opening of voltage-gated calcium channels, and subsequent influx of calcium, which triggers insulin exocytosis.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 100%
Tmax: 2-4 hours
FoodEffect: Food may slightly delay absorption but does not significantly affect bioavailability. Should be taken with breakfast or the first main meal.

Distribution:

Vd: Approximately 0.1 L/kg
ProteinBinding: >98% (primarily to albumin)
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 10 hours (range 4-10 hours)
Clearance: Not available
ExcretionRoute: Approximately 50% via urine and 50% via bile/feces
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Approximately 1 hour
PeakEffect: 2-4 hours
DurationOfAction: Up to 24 hours

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
Changes in eyesight
Muscle or joint pain
Low blood sugar (hypoglycemia), which may be more likely when this medication is used with other diabetes medications. Symptoms of low blood sugar may include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
If you experience any of these symptoms, contact your doctor right away and follow their instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or some fruit juices.
Low blood cell counts, which can increase the risk of bleeding problems, infections, or anemia. If you notice any of the following symptoms, contact your doctor right away:
+ Signs of infection, such as fever, chills, or sore throat
+ Unexplained bruising or bleeding
+ Feeling very tired or weak
Liver problems, which can be indicated by:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes

Other Possible Side Effects

Most people do not experience significant side effects, but some may occur. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:

Feeling full
Upset stomach
Heartburn
* Weight gain

Reporting Side Effects

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.
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Seek Immediate Medical Attention If You Experience:

  • Symptoms of low blood sugar (hypoglycemia): sweating, shakiness, dizziness, confusion, hunger, irritability, rapid heartbeat, blurred vision, headache, weakness.
  • Symptoms of high blood sugar (hyperglycemia): increased thirst, increased urination, fatigue, blurred vision, dry mouth.
  • Signs of liver problems: yellowing of skin or eyes (jaundice), dark urine, persistent nausea or vomiting, severe stomach pain.
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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. Be sure to describe the allergic reaction and its symptoms.
If you have a condition that affects the acidity of your blood.
If you have type 1 diabetes. Note that this medication is not intended to treat type 1 diabetes.
If you are currently taking bosentan.
* If the patient is a child, as this medication is not suitable for children.

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication alongside your other treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first 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.

If you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), you may be at a higher risk of developing anemia. This deficiency is more common in individuals of African, South Asian, Middle Eastern, and Mediterranean descent.

Regularly monitor your blood sugar levels as instructed by your doctor. 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 increase your risk of being involved in an accident.

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 your blood sugar control. Changes in physical activity, exercise, or diet can also impact your blood sugar levels.

This medication can cause low blood sugar, which can lead to seizures, loss of consciousness, long-term brain damage, and even death in severe cases. Discuss this risk with your doctor.

There is also an increased risk of death from heart disease associated with this medication. Talk to your doctor about this potential risk.

You may be more susceptible to sunburn while taking this medication. Take precautions when spending time in the sun, and inform your doctor if you experience increased sensitivity to the sun.

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, planning to become pregnant, or breastfeeding, consult with your doctor to discuss the benefits and risks of taking this medication. It is essential to note that low blood sugar has occurred in infants born to mothers who took a similar medication until the time of delivery. If you are taking this medication during pregnancy, you may need to stop taking it before your due date. Discuss this with your doctor to determine the best course of action.
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Overdose Information

Overdose Symptoms:

  • Severe hypoglycemia (extremely low blood sugar)
  • Confusion
  • Seizures
  • Loss of consciousness
  • Coma

What to Do:

If you suspect an overdose, seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment involves administering glucose (oral if conscious, IV dextrose if unconscious) and close monitoring for prolonged hypoglycemia.

Drug Interactions

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Contraindicated Interactions

  • Bosentan (increased risk of hepatotoxicity)
  • Miconazole (oral, increased risk of severe hypoglycemia)
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Major Interactions

  • Alcohol (increased risk of hypoglycemia, disulfiram-like reaction)
  • Beta-blockers (mask hypoglycemia symptoms, impair glucose counter-regulation)
  • Fluconazole (increased glyburide levels, increased hypoglycemia risk)
  • NSAIDs (increased glyburide levels, increased hypoglycemia risk)
  • Salicylates (high doses, increased glyburide levels, increased hypoglycemia risk)
  • Sulfonamides (increased glyburide levels, increased hypoglycemia risk)
  • Chloramphenicol (increased glyburide levels, increased hypoglycemia risk)
  • Probenecid (increased glyburide levels, increased hypoglycemia risk)
  • Warfarin (altered anticoagulant effect, increased glyburide levels)
  • Corticosteroids (hyperglycemic effect, may require increased glyburide dose)
  • Thiazide diuretics (hyperglycemic effect, may require increased glyburide dose)
  • Thyroid hormones (hyperglycemic effect, may require increased glyburide dose)
  • Sympathomimetics (hyperglycemic effect, may require increased glyburide dose)
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Moderate Interactions

  • ACE inhibitors (may enhance glucose-lowering effect)
  • MAO inhibitors (may enhance glucose-lowering effect)
  • Cimetidine (may increase glyburide levels)
  • Rifampin (decreased glyburide levels, reduced efficacy)
  • Colesevelam (decreased glyburide absorption, administer glyburide 4 hours before)
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Minor Interactions

  • Not available

Monitoring

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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 (e.g., SCr, eGFR)

Rationale: To assess kidney function, as glyburide is partially renally cleared and risk of hypoglycemia increases with renal impairment.

Timing: Prior to initiation and periodically thereafter.

Hepatic Function (e.g., ALT, AST)

Rationale: To assess liver function, as glyburide is extensively metabolized by the liver and risk of hypoglycemia increases with hepatic impairment.

Timing: Prior to initiation and periodically thereafter.

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Routine Monitoring

HbA1c

Frequency: Every 3-6 months

Target: <7% (individualized)

Action Threshold: If HbA1c remains above target, consider dose adjustment or addition of other agents.

Fasting Plasma Glucose (FPG)

Frequency: Periodically (e.g., weekly to monthly during titration, then less frequently)

Target: 80-130 mg/dL (individualized)

Action Threshold: If FPG consistently outside target range, adjust dose or evaluate adherence/lifestyle.

Self-Monitoring Blood Glucose (SMBG)

Frequency: Daily (as directed by healthcare provider)

Target: Pre-meal: 80-130 mg/dL; Post-meal: <180 mg/dL (individualized)

Action Threshold: If frequent hypoglycemia (<70 mg/dL) or hyperglycemia, adjust dose or lifestyle.

Renal Function (e.g., SCr, eGFR)

Frequency: Annually or more frequently if clinically indicated (e.g., with concomitant nephrotoxic drugs, worsening diabetes control)

Target: Not applicable

Action Threshold: If eGFR < 50 mL/min, use with caution; if < 30 mL/min, discontinue.

Hepatic Function (e.g., ALT, AST)

Frequency: Annually or more frequently if clinically indicated

Target: Not applicable

Action Threshold: If significant elevation, consider discontinuation or dose reduction.

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Symptom Monitoring

  • Symptoms of hypoglycemia (e.g., sweating, tremor, dizziness, confusion, hunger, irritability, rapid heartbeat, blurred vision)
  • Symptoms of hyperglycemia (e.g., increased thirst, increased urination, fatigue, blurred vision)
  • Signs of liver dysfunction (e.g., jaundice, dark urine, persistent nausea/vomiting, abdominal pain)

Special Patient Groups

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Pregnancy

Category C. Glyburide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Insulin is generally preferred for glycemic control in pregnancy. If used for gestational diabetes, the micronized form is often preferred due to lower placental transfer.

Trimester-Specific Risks:

First Trimester: Potential for fetal harm cannot be ruled out. Insulin is generally preferred.
Second Trimester: Potential for fetal harm cannot be ruled out. Insulin is generally preferred.
Third Trimester: Potential for fetal harm cannot be ruled out. Increased risk of neonatal hypoglycemia if used near term.
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Lactation

L3 (Moderately Safe). Glyburide is excreted into breast milk. While the amount is generally small, there is a potential for hypoglycemia in the breastfed infant. Monitor infant for signs of hypoglycemia. Insulin is generally preferred during lactation.

Infant Risk: Low to moderate risk of hypoglycemia in the infant. Monitor for signs of lethargy, poor feeding, or jitteriness.
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Pediatric Use

Safety and effectiveness in pediatric patients have not been established for type 2 diabetes. Not generally recommended for use in children.

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Geriatric Use

Use with caution in elderly patients due to increased risk of hypoglycemia, particularly in those with impaired renal or hepatic function. Start with lower doses (e.g., 1.25 mg daily) and titrate slowly. Elderly patients may be more susceptible to the hypoglycemic effects and may have difficulty recognizing symptoms of hypoglycemia.

Clinical Information

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Clinical Pearls

  • Glyburide has a relatively long duration of action, increasing the risk of prolonged hypoglycemia, especially in patients with renal or hepatic impairment.
  • Weight gain is a common side effect of sulfonylureas, including glyburide.
  • Secondary failure (loss of glycemic control over time) can occur with sulfonylureas.
  • Patients should be educated on the symptoms and management of hypoglycemia.
  • Avoid in patients with G6PD deficiency due to risk of hemolytic anemia.
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Alternative Therapies

  • Other sulfonylureas (e.g., Glipizide, Glimepiride)
  • Metformin
  • Thiazolidinediones (e.g., Pioglitazone)
  • DPP-4 inhibitors (e.g., Sitagliptin)
  • SGLT2 inhibitors (e.g., Empagliflozin)
  • GLP-1 receptor agonists (e.g., Liraglutide)
  • Insulin therapy
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (preferred generic)
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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 detailed information about the overdose, including the medication taken, the amount, and the time it occurred.