Micronase 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
Category C
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FDA Approved
Mar 1984
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Micronase (glyburide) is a medication used to treat type 2 diabetes. It helps your body make more insulin, which lowers your blood sugar. It's important to take it 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 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 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 container 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 balanced diet as 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.
  • Carry a source of fast-acting sugar (e.g., glucose tablets, hard candy, fruit juice) to treat low blood sugar (hypoglycemia).
  • Limit or avoid alcohol consumption, as it can increase the risk of low blood sugar.
  • Inform all healthcare providers, including dentists, that you are taking glyburide.
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Available Forms & Alternatives

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 once daily or in divided doses.
Dose Range: 1.25 - 20 mg

Condition-Specific Dosing:

Type 2 Diabetes Mellitus: Initial: 2.5-5 mg once daily. Titrate by 2.5 mg increments at weekly intervals based on blood glucose response. Max: 20 mg/day.
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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 for hypoglycemia.
Moderate: Use with caution; consider lower initial doses (e.g., 1.25 mg daily) and careful titration. Increased risk of hypoglycemia.
Severe: Contraindicated or not recommended due to high risk of prolonged hypoglycemia. Insulin is generally preferred.
Dialysis: Not recommended; insulin is preferred. Glyburide is not significantly removed by dialysis.

Hepatic Impairment:

Mild: Use with caution; consider lower initial doses (e.g., 1.25 mg daily) and careful titration.
Moderate: Use with extreme caution; increased risk of hypoglycemia. Consider alternative agents.
Severe: Contraindicated or not recommended due to high risk of prolonged hypoglycemia and impaired drug clearance.

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 the 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 85-100%
Tmax: 2-4 hours (for Micronase, a non-micronized formulation)
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 control.

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% renal (urine) and 50% hepatic (bile/feces) as metabolites.
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Approximately 1 hour
PeakEffect: Approximately 2-4 hours
DurationOfAction: Approximately 12-24 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. Contact your doctor right away if you experience:
+ Signs of infection, such as fever, chills, or sore throat
+ Unexplained bruising or bleeding
+ Feeling very tired or weak
Liver problems. Contact your doctor right away 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 experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:

Feeling full
Upset stomach
Heartburn
* Weight gain

Reporting Side Effects

This is not a comprehensive list of all 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, headache, blurred vision, rapid heartbeat, weakness, slurred speech, anxiety, numbness or tingling around the mouth. If these occur, check blood sugar and treat immediately.
  • Symptoms of high blood sugar (hyperglycemia): increased thirst, frequent urination, fatigue, blurred vision. Report these to your doctor.
  • Symptoms of allergic reaction: rash, itching, swelling (especially of 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:

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. 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, 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 with your other medications and health conditions. Never start, stop, or adjust the dose 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 significantly 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, if severe, can lead to seizures, loss of consciousness, long-term brain damage, and even death. It is crucial to discuss the risks of low blood sugar with your doctor.

Additionally, this medication may increase the risk of death from heart disease. Discuss this potential risk with your doctor.

You may be more susceptible to sunburn while taking this medication. Take necessary 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 experiencing side effects.

If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor. It is essential to discuss the benefits and risks of taking this medication during pregnancy or breastfeeding.

It is also important to note that infants born to mothers who took a similar medication during pregnancy may be at risk of developing low blood sugar. If you are taking this medication during pregnancy, your doctor will advise you on when to stop taking it before your due date.
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Overdose Information

Overdose Symptoms:

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

What to Do:

Immediately consume a source of fast-acting sugar. If the person is unconscious or unable to swallow, call emergency services (e.g., 911 in the US) or your local poison control center (1-800-222-1222 in the US). Medical management may include intravenous glucose or glucagon administration.

Drug Interactions

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Contraindicated Interactions

  • Bosentan (increased risk of liver enzyme elevation)
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Major Interactions

  • Alcohol (disulfiram-like reaction, increased risk of hypoglycemia)
  • Beta-blockers (mask symptoms of hypoglycemia, impair glucose recovery)
  • Fluconazole (significantly increases glyburide levels, leading to severe hypoglycemia)
  • Miconazole (oral, parenteral, topical - severe hypoglycemia)
  • NSAIDs (e.g., ibuprofen, naproxen - enhance hypoglycemic effect)
  • Sulfonamides (e.g., sulfamethoxazole/trimethoprim - enhance hypoglycemic effect)
  • Chloramphenicol (enhance hypoglycemic effect)
  • Warfarin (potentiates anticoagulant effect, increased risk of bleeding)
  • Probenecid (enhances hypoglycemic effect)
  • Salicylates (high doses - enhance hypoglycemic effect)
  • MAO inhibitors (enhance hypoglycemic effect)
  • Cimetidine (enhances hypoglycemic effect)
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Moderate Interactions

  • Corticosteroids (decrease hypoglycemic effect)
  • Thiazide diuretics (decrease hypoglycemic effect)
  • Loop diuretics (decrease hypoglycemic effect)
  • Thyroid hormones (decrease hypoglycemic effect)
  • Sympathomimetics (e.g., decongestants, bronchodilators - decrease hypoglycemic effect)
  • Phenothiazines (decrease hypoglycemic effect)
  • Phenytoin (decrease hypoglycemic effect)
  • Nicotinic acid (decrease hypoglycemic effect)
  • Oral contraceptives (decrease hypoglycemic effect)
  • Calcium channel blockers (decrease hypoglycemic effect)
  • Isoniazid (decrease hypoglycemic effect)
  • Rifampin (decreases glyburide levels, reducing efficacy)
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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 therapy.

Timing: Prior to initiation of therapy.

Fasting Plasma Glucose (FPG)

Rationale: To establish baseline glucose levels and guide initial therapy.

Timing: Prior to initiation of therapy.

Renal Function (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 (ALT, AST, Bilirubin)

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 and periodically thereafter.

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Routine Monitoring

HbA1c

Frequency: Every 3-6 months

Target: <7% (individualized)

Action Threshold: If target not met, consider dose adjustment or addition of other agents.

Self-Monitoring Blood Glucose (SMBG)

Frequency: Daily or as directed by healthcare provider (e.g., pre-meal, post-meal, bedtime)

Target: FPG: 80-130 mg/dL; Post-prandial: <180 mg/dL (individualized)

Action Threshold: Persistent readings outside target range, or frequent hypoglycemic episodes, require dose adjustment or re-evaluation of therapy.

Signs and Symptoms of Hypoglycemia

Frequency: Ongoing, patient education is key

Target: N/A

Action Threshold: If symptoms occur, confirm with blood glucose reading and treat immediately. Adjust therapy if recurrent.

Renal and Hepatic Function

Frequency: Annually or more frequently if clinically indicated (e.g., changes in health status, new medications)

Target: Within normal limits

Action Threshold: Significant decline may necessitate dose reduction or discontinuation of glyburide.

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Symptom Monitoring

  • Symptoms of hypoglycemia: sweating, tremor, dizziness, confusion, hunger, irritability, headache, blurred vision, rapid heartbeat, weakness, slurred speech, anxiety, numbness/tingling around the mouth.
  • Symptoms of hyperglycemia (if control is inadequate): increased thirst, increased urination, fatigue, blurred vision.
  • Symptoms of liver dysfunction (rare): persistent nausea, vomiting, abdominal pain, dark urine, yellowing of skin/eyes (jaundice).

Special Patient Groups

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Pregnancy

Glyburide is generally not recommended during pregnancy. Insulin is the preferred treatment for diabetes in pregnant women due to the risk of neonatal hypoglycemia with sulfonylureas, as glyburide crosses the placenta.

Trimester-Specific Risks:

First Trimester: Potential for teratogenicity is low, but insulin is preferred for optimal glycemic control.
Second Trimester: Risk of fetal hyperinsulinemia and subsequent neonatal hypoglycemia.
Third Trimester: Increased risk of severe and prolonged neonatal hypoglycemia 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. Not recommended for use in children.

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Geriatric Use

Use with extreme caution in elderly patients due to increased risk of severe and prolonged hypoglycemia. Start with the lowest effective dose (e.g., 1.25 mg daily) and titrate slowly. Avoid in patients with significant renal or hepatic impairment. Consider alternative agents with lower hypoglycemia risk.

Clinical Information

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Clinical Pearls

  • Glyburide is a potent sulfonylurea; careful dosing and patient education are crucial to minimize hypoglycemia risk.
  • Always take glyburide with breakfast or the first main meal to reduce the risk of hypoglycemia and gastrointestinal upset.
  • Patients should be educated on the symptoms of hypoglycemia and how to treat it immediately.
  • Avoid in patients with significant renal or hepatic impairment due to increased risk of prolonged hypoglycemia.
  • Consider alternative agents in elderly patients or those at high risk for hypoglycemia.
  • Micronase is a non-micronized formulation of glyburide; Glynase PresTab is a micronized formulation, which has different absorption characteristics and is not interchangeable on a milligram-for-milligram basis.
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Alternative Therapies

  • Metformin (Biguanide)
  • Glipizide (Sulfonylurea)
  • Glimepiride (Sulfonylurea)
  • Pioglitazone (Thiazolidinedione)
  • Rosiglitazone (Thiazolidinedione)
  • Sitagliptin (DPP-4 inhibitor)
  • Saxagliptin (DPP-4 inhibitor)
  • Linagliptin (DPP-4 inhibitor)
  • Empagliflozin (SGLT2 inhibitor)
  • Canagliflozin (SGLT2 inhibitor)
  • Dapagliflozin (SGLT2 inhibitor)
  • Liraglutide (GLP-1 receptor agonist)
  • Semaglutide (GLP-1 receptor agonist)
  • Insulin
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets (5mg generic)
Generic Available: Yes
Insurance Coverage: Tier 1 (Generic)
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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.