Glyburide Micro 6mg 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
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Pharmacologic Class
Sulfonylurea
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Pregnancy Category
Category B
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FDA Approved
Aug 1992
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Glyburide Micro is a medication used to help control high blood sugar in people with Type 2 diabetes. It works by helping your body release more insulin from your pancreas, which then helps lower your blood sugar levels. It's important to take this medication exactly as prescribed, usually with your first meal of the day.
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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 to you 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

  • Follow a healthy diet plan recommended by your doctor or dietitian, focusing on balanced meals and controlled carbohydrate intake.
  • 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 mild to moderate hypoglycemia.
  • Limit or avoid alcohol consumption, as it can increase the risk of low blood sugar.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 1.5-3 mg once daily with breakfast or first main meal. Maintenance: 0.75-12 mg once daily.
Dose Range: 0.75 - 12 mg

Condition-Specific Dosing:

Type 2 Diabetes Mellitus: Initial: 1.5-3 mg once daily. May increase by 1.5 mg increments weekly, based on blood glucose response. Max: 12 mg/day.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established (generally not recommended for pediatric type 2 diabetes; insulin or metformin preferred)
Adolescent: Not established (generally not recommended for pediatric type 2 diabetes; insulin or metformin preferred)
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Dose Adjustments

Renal Impairment:

Mild: Use with caution; monitor closely for hypoglycemia.
Moderate: Avoid use or use with extreme caution at reduced doses (e.g., initial 0.75 mg) due to increased risk of hypoglycemia. Contraindicated if CrCl < 50 mL/min by some guidelines.
Severe: Contraindicated due to high risk of severe, prolonged hypoglycemia.
Dialysis: Contraindicated due to high risk of severe, prolonged hypoglycemia.

Hepatic Impairment:

Mild: Use with caution; monitor closely for hypoglycemia.
Moderate: Avoid use or use with extreme caution at reduced doses (e.g., initial 0.75 mg) due to impaired metabolism and increased risk of hypoglycemia.
Severe: Contraindicated due to high 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, influx of calcium, and subsequent exocytosis of insulin.
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Pharmacokinetics

Absorption:

Bioavailability: Nearly complete (micronized form)
Tmax: 2-3 hours (micronized)
FoodEffect: Food may slightly delay absorption but does not significantly affect the extent of absorption. Should be taken with breakfast or the first main meal to reduce gastrointestinal upset and optimize glucose lowering.

Distribution:

Vd: Approximately 0.2 L/kg
ProteinBinding: >98% (primarily to albumin)
CnssPenetration: Limited

Elimination:

HalfLife: 4-10 hours (terminal half-life can be longer due to enterohepatic recirculation)
Clearance: Not readily available, but primarily hepatic metabolism and renal/biliary excretion.
ExcretionRoute: Approximately 50% renal (urine) and 50% biliary/fecal
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Approximately 1 hour
PeakEffect: 2-4 hours
DurationOfAction: Up to 24 hours (though effective glucose-lowering duration may be shorter, allowing for once-daily dosing)

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

While rare, some people may experience severe and potentially life-threatening side effects when 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 this medication is used with other diabetes medications. 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 potential side effects and seek medical attention if you experience:

Low blood cell counts, which can increase the risk of bleeding problems, infections, or anemia. Symptoms may include:
+ Fever
+ Chills
+ 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 are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical attention:

Feeling full
Upset stomach
Heartburn
* Weight gain

This is not an exhaustive list of potential side effects. 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:

  • Symptoms of low blood sugar (hypoglycemia): sweating, shaking, dizziness, confusion, hunger, irritability, rapid heartbeat, blurred vision, weakness, headache. If these occur, consume a quick source of sugar immediately.
  • Symptoms of allergic reaction: rash, itching, swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing. Seek immediate medical attention.
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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.
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, 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 with your existing treatments and health conditions.

Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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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.

Follow your doctor's instructions for monitoring your blood sugar levels. Regular blood tests, as advised by your doctor, are also crucial to ensure your safety while taking this medication. Discuss any concerns or questions you have with your doctor.

Avoid driving if you have experienced low blood sugar, as it can significantly increase your risk of being involved in an accident.

Before consuming alcohol, consult with your doctor to understand the potential risks and how to minimize them.

If you are taking colesevelam, ensure that you take it at least 4 hours after taking this medication to avoid any potential interactions.

Be aware that stress, such as from fever, infection, injury, or surgery, can affect your blood sugar control. Changes in your physical activity, exercise routine, or diet can also impact your blood sugar levels.

This medication can cause low blood sugar, which, if severe, can lead to seizures, loss of consciousness, permanent brain damage, and even death. Discuss the risks and how to manage low blood sugar with your doctor.

There is an increased risk of heart disease-related death associated with this medication. Talk to your doctor about this risk and any concerns you may have.

This medication can make you more susceptible to sunburn. 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, discuss the benefits and risks of this medication with your doctor. It is crucial to weigh the potential effects on both you and your baby.

Note that infants born to mothers who took a similar medication during pregnancy have experienced low blood sugar. If you are taking this medication and become pregnant, your doctor will advise you on when to stop taking it before your due date to minimize this risk.
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Overdose Information

Overdose Symptoms:

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

What to Do:

In case of suspected overdose, seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Management involves administering glucose (oral for conscious patients, IV dextrose or glucagon for unconscious patients) and close monitoring of blood glucose for an extended period due to the prolonged action of glyburide.

Drug Interactions

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Major Interactions

  • Bosentan (increased risk of hepatotoxicity)
  • Miconazole (oral, systemic - significantly increases glyburide levels and risk of severe hypoglycemia)
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Moderate Interactions

  • Alcohol (increased risk of hypoglycemia, disulfiram-like reaction)
  • Beta-blockers (mask hypoglycemia symptoms, impair glucose recovery)
  • Fluconazole (CYP2C9 inhibitor, increases glyburide levels)
  • NSAIDs (e.g., ibuprofen, naproxen - may enhance hypoglycemic effect)
  • Sulfonamides (e.g., sulfamethoxazole/trimethoprim - may enhance hypoglycemic effect)
  • Chloramphenicol (may enhance hypoglycemic effect)
  • Coumarin derivatives (e.g., warfarin - altered anticoagulant effect, increased hypoglycemia risk)
  • MAOIs (may enhance hypoglycemic effect)
  • Probenecid (may enhance hypoglycemic effect)
  • Salicylates (high doses, may enhance hypoglycemic effect)
  • Corticosteroids (decrease hypoglycemic effect)
  • Thiazide diuretics (decrease hypoglycemic effect)
  • Thyroid hormones (decrease hypoglycemic effect)
  • Estrogens/Oral Contraceptives (decrease hypoglycemic effect)
  • Phenothiazines (decrease hypoglycemic effect)
  • Phenytoin (decrease hypoglycemic effect)
  • Sympathomimetics (decrease hypoglycemic effect)
  • Calcium channel blockers (decrease hypoglycemic effect)
  • Isoniazid (decrease hypoglycemic effect)
  • Rifampin (CYP2C9 inducer, decreases glyburide levels)
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Minor Interactions

  • Chromium (may enhance hypoglycemic effect)
  • Garlic (may enhance hypoglycemic effect)

Monitoring

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Baseline Monitoring

HbA1c (Glycated Hemoglobin)

Rationale: To establish baseline glycemic control and confirm diagnosis of Type 2 Diabetes Mellitus.

Timing: Prior to initiation of therapy.

Fasting Plasma Glucose (FPG)

Rationale: To establish baseline glucose levels 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 excreted and risk of hypoglycemia increases with renal impairment.

Timing: Prior to initiation of therapy.

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

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

Timing: Prior to initiation of therapy.

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Routine Monitoring

Fasting Plasma Glucose (FPG)

Frequency: Daily or as directed by healthcare provider (e.g., 1-2 times per week initially, then less frequently once stable)

Target: 80-130 mg/dL (individualized)

Action Threshold: Below 70 mg/dL (hypoglycemia) or consistently above target range (hyperglycemia)

HbA1c (Glycated Hemoglobin)

Frequency: Every 3-6 months

Target: <7% (individualized)

Action Threshold: Above target range (consider dose adjustment or additional therapy)

Signs and Symptoms of Hypoglycemia

Frequency: Daily, patient self-monitoring

Target: N/A

Action Threshold: Any occurrence of symptoms (e.g., sweating, tremor, confusion, hunger, dizziness)

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

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

Target: N/A

Action Threshold: Significant decline in eGFR (consider dose reduction or discontinuation)

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

Frequency: Annually or more frequently if clinically indicated (e.g., with concomitant hepatotoxic drugs or worsening liver function)

Target: N/A

Action Threshold: Significant elevation in liver enzymes (consider discontinuation)

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Symptom Monitoring

  • Symptoms of hypoglycemia: sweating, tremor, dizziness, confusion, hunger, irritability, rapid heartbeat, blurred vision, weakness, headache, slurred speech, anxiety.
  • Symptoms of hyperglycemia (less common with sulfonylureas alone): increased thirst, increased urination, fatigue, blurred vision.

Special Patient Groups

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Pregnancy

Glyburide is Pregnancy Category B. While some studies suggest it may be used in gestational diabetes, insulin is generally the preferred treatment for diabetes during pregnancy due to its established safety profile and lack of placental transfer. If used, careful monitoring of maternal and fetal glucose is essential.

Trimester-Specific Risks:

First Trimester: Limited data, but generally considered low risk for congenital malformations compared to Category C/D drugs.
Second Trimester: May be considered for gestational diabetes if diet and exercise are insufficient, but insulin is preferred.
Third Trimester: Risk of neonatal hypoglycemia if used close to delivery due to placental transfer. Insulin is preferred.
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Lactation

Glyburide is excreted into breast milk. The American Academy of Pediatrics considers it compatible with breastfeeding, but there is a potential risk of hypoglycemia in the breastfed infant. Monitor the infant for signs of hypoglycemia (e.g., lethargy, poor feeding, jitteriness). Insulin is generally preferred during lactation.

Infant Risk: Low to moderate risk of infant hypoglycemia. Monitor infant for signs of low blood sugar.
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Pediatric Use

Safety and efficacy have not been established in pediatric patients. Glyburide is generally not recommended for use in children or adolescents with Type 2 diabetes; metformin or insulin are typically preferred.

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Geriatric Use

Elderly patients are at increased risk of hypoglycemia due to age-related decline in renal function, reduced hepatic metabolism, and potential for irregular meal patterns or polypharmacy. Start with the lowest effective dose (e.g., 0.75 mg) and titrate slowly. Monitor closely for signs of hypoglycemia, which may be atypical or masked in older adults.

Clinical Information

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Clinical Pearls

  • Glyburide Micro (micronized glyburide) has different pharmacokinetic properties and dosing compared to non-micronized glyburide. Doses are not interchangeable mg-for-mg.
  • Always take glyburide with breakfast or the first main meal of the day to minimize gastrointestinal upset and reduce the risk of hypoglycemia.
  • Patients should be educated on the signs and symptoms of hypoglycemia and how to treat it immediately.
  • Due to the risk of prolonged hypoglycemia, especially in elderly patients or those with renal/hepatic impairment, glyburide is often considered a less favorable choice compared to newer antidiabetic agents (e.g., DPP-4 inhibitors, SGLT2 inhibitors, GLP-1 receptor agonists) or even other sulfonylureas (e.g., glipizide, gliclazide) which may have a shorter half-life or less active metabolites.
  • Avoid in patients with severe renal or hepatic impairment due to high risk of severe, prolonged hypoglycemia.
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Alternative Therapies

  • Other Sulfonylureas (e.g., Glipizide, Glimepiride)
  • Metformin (Biguanide)
  • DPP-4 Inhibitors (e.g., Sitagliptin, Saxagliptin)
  • SGLT2 Inhibitors (e.g., Canagliflozin, Dapagliflozin)
  • GLP-1 Receptor Agonists (e.g., Liraglutide, Semaglutide)
  • Thiazolidinediones (e.g., Pioglitazone, Rosiglitazone)
  • Insulin
  • Alpha-glucosidase Inhibitors (e.g., Acarbose, Miglitol)
  • Meglitinides (e.g., Repaglinide, Nateglinide)
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Cost & Coverage

Average Cost: $10 - $50 per 30 tablets (generic Glyburide Micro 6mg)
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 promptly. To ensure safe and effective treatment, 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.