Micronase 2.5mg Tablets

Manufacturer PFIZER 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
C
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FDA Approved
Feb 1984
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Glyburide is a medication used to treat type 2 diabetes. It helps your body make more insulin, which lowers your blood sugar. It's usually taken once a day with your first meal.
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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, 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, 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 the missed one.
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Lifestyle & Tips

  • Take glyburide exactly as prescribed, usually with breakfast or the first main meal of the day.
  • Do not skip meals while taking this medication, as it can increase the risk of low blood sugar (hypoglycemia).
  • Follow a healthy diet plan and engage in regular physical activity as recommended by your doctor or dietitian.
  • Monitor your blood sugar 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 hypoglycemia.
  • Limit or avoid alcohol consumption, as it can increase the risk of low blood sugar.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

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

Condition-Specific Dosing:

type2Diabetes: Initial: 2.5 mg once daily. May increase by 1.25-2.5 mg at weekly intervals based on blood glucose response. Max: 20 mg/day. Doses >10 mg/day may be given in divided doses.
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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/day) and titrate slowly. Increased risk of hypoglycemia.
Severe: Contraindicated or not recommended due to high risk of severe, prolonged hypoglycemia.
Dialysis: Contraindicated or not recommended. Glyburide is not significantly removed by dialysis.

Hepatic Impairment:

Mild: Use with caution; consider lower initial doses (e.g., 1.25 mg/day) and titrate slowly. Increased risk of hypoglycemia.
Moderate: Use with caution; consider lower initial doses and close monitoring. Increased risk of hypoglycemia.
Severe: Contraindicated or not recommended 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 pancreatic beta-cell membrane, leading to the closure of ATP-sensitive potassium channels. This depolarization of the beta-cell membrane opens voltage-gated calcium channels, resulting in an influx of calcium and subsequent exocytosis of insulin granules.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 85-100%
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: >98% (primarily to albumin)
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 10 hours (range 4-24 hours, depending on formulation and individual variability)
Clearance: Not readily available, but primarily hepatic metabolism and renal/biliary excretion.
ExcretionRoute: Approximately 50% renal (as metabolites), 50% biliary/fecal (as metabolites).
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Approximately 1 hour
PeakEffect: 2-4 hours
DurationOfAction: Up to 24 hours (depending on dose and individual response)

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 used with other diabetes medications. Symptoms may 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 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 do not experience serious side effects, and many have only minor or no side effects at all. However, 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

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, blurred vision, rapid heartbeat, headache, slurred speech, weakness. If these occur, treat immediately with fast-acting sugar.
  • Symptoms of high blood sugar (hyperglycemia): increased thirst, frequent urination, fatigue, blurred vision. Report these to your doctor.
  • 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:

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 you experienced, including any 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 in combination with your other medications 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.

Monitor your blood sugar levels as directed by your doctor. Regular blood tests will also be necessary, as advised by your doctor, to ensure your safety while taking this medication.

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, take it at least 4 hours after taking this medication to minimize potential interactions.

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 may lead to seizures, loss of consciousness, permanent brain damage, and even death in severe cases. Discuss the risks and management of low blood sugar with your doctor.

Additionally, this medication may increase the risk of death from heart disease. Consult with your doctor to understand this risk and how to mitigate it.

You may be more susceptible to sunburn while taking this medication. Take precautions when exposed to 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, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor. It is essential to weigh the potential risks to you and your baby.

It is crucial to note that infants born to mothers who took a similar medication during pregnancy may experience low blood sugar after birth. If you are taking this medication during pregnancy, 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 (profound weakness, confusion, seizures, loss of consciousness, coma)

What to Do:

Immediately consume fast-acting sugar. If unconscious or unable to swallow, seek emergency medical attention. Call 911 or your local emergency number. For advice, call a poison control center at 1-800-222-1222.

Drug Interactions

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Contraindicated Interactions

  • Bosentan (increased risk of hepatotoxicity)
  • Miconazole (oral, systemic, or topical; severe hypoglycemia)
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Major Interactions

  • Alcohol (increased risk of hypoglycemia)
  • Beta-blockers (mask symptoms of hypoglycemia, may prolong hypoglycemia)
  • Fluconazole (increased glyburide levels, increased hypoglycemia risk)
  • NSAIDs (e.g., ibuprofen, naproxen; increased hypoglycemia risk)
  • Salicylates (e.g., aspirin; increased hypoglycemia risk)
  • Sulfonamides (increased hypoglycemia risk)
  • Chloramphenicol (increased hypoglycemia risk)
  • Coumarin derivatives (e.g., warfarin; altered anticoagulant effect)
  • MAOIs (increased hypoglycemia risk)
  • Probenecid (increased hypoglycemia risk)
  • Rifampin (decreased glyburide levels, reduced efficacy)
  • Corticosteroids (decreased hypoglycemic effect)
  • Thiazide diuretics (decreased hypoglycemic effect)
  • Thyroid hormones (decreased hypoglycemic effect)
  • Sympathomimetics (e.g., decongestants; decreased hypoglycemic effect)
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Moderate Interactions

  • Cimetidine (potential for increased glyburide levels)
  • Clarithromycin (potential for increased glyburide levels)
  • Gemfibrozil (increased hypoglycemia risk)
  • Colesevelam (decreased glyburide absorption; administer glyburide 4 hours before colesevelam)
  • Phenytoin (altered glucose control)
  • Oral contraceptives (potential for decreased hypoglycemic effect)
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Minor Interactions

  • Chromium supplements (may enhance glucose lowering)
  • Garlic supplements (may enhance glucose lowering)

Monitoring

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Baseline Monitoring

Fasting Plasma Glucose (FPG)

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

Timing: Prior to initiation of therapy.

Hemoglobin A1c (HbA1c)

Rationale: To establish baseline long-term glycemic control.

Timing: Prior to initiation of therapy.

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

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

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 hepatic impairment increases hypoglycemia risk.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Fasting Plasma Glucose (FPG)

Frequency: Daily (patient self-monitoring) or at each clinic visit.

Target: 80-130 mg/dL (individualized)

Action Threshold: <70 mg/dL (hypoglycemia) or consistently >180 mg/dL (hyperglycemia)

Hemoglobin A1c (HbA1c)

Frequency: Every 3-6 months.

Target: <7.0% (individualized)

Action Threshold: >7.0% (consider dose adjustment or additional therapy)

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

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

Target: Stable, within normal limits for age/sex

Action Threshold: Significant decline in eGFR (e.g., <50 mL/min/1.73m2) may require dose reduction or discontinuation.

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

Frequency: Annually or more frequently if clinically indicated (e.g., with symptoms of liver dysfunction).

Target: Stable, within normal limits

Action Threshold: Significant elevation (e.g., >3x ULN) may require discontinuation.

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Symptom Monitoring

  • Symptoms of hypoglycemia (e.g., sweating, tremor, dizziness, confusion, hunger, irritability, blurred vision, palpitations, headache, slurred speech, weakness)
  • 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)
  • Unexplained weight gain

Special Patient Groups

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Pregnancy

Generally not recommended during pregnancy. Insulin is typically the preferred treatment for gestational diabetes or pre-existing diabetes in pregnant women due to better glycemic control and lower risk of neonatal hypoglycemia compared to sulfonylureas. Glyburide is Pregnancy Category C, meaning animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Trimester-Specific Risks:

First Trimester: Potential for teratogenicity, though human data are limited and conflicting.
Second Trimester: Risk of fetal hyperinsulinemia and macrosomia.
Third Trimester: Increased risk of neonatal hypoglycemia, especially if used close to delivery.
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Lactation

Not recommended during breastfeeding. Glyburide is excreted into breast milk and can cause hypoglycemia in the nursing infant. Insulin is generally preferred for glycemic control in lactating mothers.

Infant Risk: High risk of hypoglycemia in the infant.
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Pediatric Use

Safety and efficacy have not been established in pediatric patients. Use is generally not recommended.

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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/day) 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 is a potent sulfonylurea with a relatively long duration of action, increasing the risk of hypoglycemia, especially in patients with irregular meal patterns, renal/hepatic impairment, or those on interacting medications.
  • Always instruct patients to take glyburide with a meal to minimize the risk of hypoglycemia.
  • Weight gain is a common side effect associated with sulfonylureas due to increased insulin levels.
  • Consider alternative agents in patients prone to hypoglycemia or with significant renal/hepatic dysfunction.
  • Micronized glyburide (Glynase PresTab) has higher bioavailability and is not interchangeable on a milligram-for-milligram basis with non-micronized glyburide (Micronase).
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Alternative Therapies

  • Metformin (first-line for most Type 2 Diabetes patients)
  • Other sulfonylureas (e.g., glipizide, glimepiride)
  • DPP-4 inhibitors (e.g., sitagliptin, saxagliptin)
  • GLP-1 receptor agonists (e.g., liraglutide, semaglutide)
  • SGLT2 inhibitors (e.g., empagliflozin, canagliflozin)
  • Thiazolidinediones (e.g., pioglitazone)
  • Insulin therapy
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets (generic 2.5mg)
Generic Available: Yes
Insurance Coverage: Tier 1 (Preferred Generic) on most formularies
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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 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.