Micronase 1.25mg 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
B
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FDA Approved
Jun 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 then helps lower your blood sugar levels. It's important to take it exactly as prescribed, usually with your first meal of the day, and to follow a healthy diet and exercise plan.
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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. 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

  • Follow a consistent meal plan and avoid skipping meals to prevent low blood sugar.
  • Engage in regular physical activity as advised by your doctor.
  • Limit or avoid alcohol consumption, as it can increase the risk of low blood sugar.
  • 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 low blood sugar.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 1.25 mg to 5 mg once daily with breakfast or first main meal. Maintenance: 1.25 mg to 20 mg once daily. Doses >10 mg/day may be divided.
Dose Range: 1.25 - 20 mg

Condition-Specific Dosing:

Type 2 Diabetes Mellitus: Initial: 1.25 mg to 5 mg once daily. Adjust dose by 1.25 mg to 5 mg at weekly intervals based on blood glucose response. Maximum: 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: Use with caution; consider lower initial dose and careful titration.
Moderate: Use with caution; consider lower initial dose (e.g., 1.25 mg daily) and careful titration. Monitor closely for hypoglycemia.
Severe: Generally not recommended due to increased risk of hypoglycemia and accumulation of active metabolites. Insulin is preferred.
Dialysis: Not recommended. Insulin is preferred.

Hepatic Impairment:

Mild: Use with caution; consider lower initial dose and careful titration.
Moderate: Use with caution; consider lower initial dose (e.g., 1.25 mg daily) and careful titration. Monitor closely for hypoglycemia.
Severe: Generally not recommended due to increased risk of hypoglycemia. Insulin is preferred.

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 cell membrane, influx of calcium, and subsequent exocytosis of insulin.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 100% (micronized formulation)
Tmax: 2-4 hours
FoodEffect: Food may delay absorption but does not significantly affect the extent of absorption.

Distribution:

Vd: Approximately 10 L
ProteinBinding: >98% (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: <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

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 immediate medical attention:

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. Contact your doctor if you experience:
+ Signs of infection, such as fever, chills, or sore throat
+ Unexplained bruising or bleeding
+ Feeling very tired or weak
Liver problems. Seek medical help 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 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

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, shakiness, dizziness, confusion, hunger, irritability, rapid heartbeat. Treat immediately with a fast-acting sugar source.
  • Symptoms of allergic reaction: rash, itching, swelling (especially of face/tongue/throat), severe dizziness, trouble breathing. Seek immediate medical attention.
  • Symptoms of liver problems: yellowing of skin or eyes (jaundice), dark urine, persistent nausea or vomiting, severe stomach pain. Contact your doctor immediately.
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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. Do not initiate, 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, 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 safely manage them.

If you are also 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 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. It is crucial to discuss the risks and management of low blood sugar with your doctor.

There is an increased risk of death from heart disease associated with this medication. Discuss this risk with your doctor to understand the benefits and risks of taking this medication.

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 any unusual sunburn or sensitivity.

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, inform your doctor. It is essential to discuss the potential benefits and risks of taking this medication during pregnancy or breastfeeding. Low blood sugar has been reported in newborns born to mothers who took similar medications until the time of delivery. If you are taking this medication during pregnancy, your doctor may advise you to stop taking it before your due date.
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Overdose Information

Overdose Symptoms:

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

What to Do:

Immediately consume a fast-acting sugar source. If severe or unconscious, 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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Major Interactions

  • Bosentan (increased risk of hepatotoxicity)
  • Miconazole (oral, increased 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 (increased glyburide levels, hypoglycemia)
  • NSAIDs (increased glyburide levels, hypoglycemia)
  • Sulfonamides (increased glyburide levels, hypoglycemia)
  • Chloramphenicol (increased glyburide levels, hypoglycemia)
  • Coumarin derivatives (potentiate or inhibit anticoagulant effect)
  • MAOIs (increased glyburide levels, hypoglycemia)
  • Probenecid (increased glyburide levels, hypoglycemia)
  • Cimetidine (increased glyburide levels, hypoglycemia)
  • Thiazide diuretics (decreased hypoglycemic effect)
  • Corticosteroids (decreased hypoglycemic effect)
  • Phenothiazines (decreased hypoglycemic effect)
  • Thyroid products (decreased hypoglycemic effect)
  • Estrogens/Oral Contraceptives (decreased hypoglycemic effect)
  • Phenytoin (decreased hypoglycemic effect)
  • Nicotinic acid (decreased hypoglycemic effect)
  • Sympathomimetics (decreased hypoglycemic effect)
  • Calcium channel blockers (decreased hypoglycemic effect)
  • Isoniazid (decreased hypoglycemic effect)
  • Colesevelam (decreased glyburide absorption, administer glyburide 4 hours before)

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 (SCr, eGFR)

Rationale: To assess kidney function as glyburide is partially renally eliminated 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 primarily metabolized by the liver.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Fasting Plasma Glucose (FPG)

Frequency: Daily (patient self-monitoring) or as directed by healthcare provider.

Target: 80-130 mg/dL (individualized)

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

Postprandial Glucose (PPG)

Frequency: Periodically (patient self-monitoring) or as directed by healthcare provider.

Target: <180 mg/dL (individualized)

Action Threshold: >180 mg/dL

Hemoglobin A1c (HbA1c)

Frequency: Every 3-6 months.

Target: <7% (individualized)

Action Threshold: >7% (consider dose adjustment or alternative therapy)

Signs/Symptoms of Hypoglycemia

Frequency: Ongoing, patient education is crucial.

Target: N/A

Action Threshold: Any occurrence requires immediate action (consume fast-acting carbohydrate).

Renal Function (SCr, eGFR)

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

Target: Normal eGFR

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

Hepatic Function (ALT, AST, Bilirubin)

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

Target: Normal ranges

Action Threshold: Significant elevation (consider discontinuation).

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Symptom Monitoring

  • Symptoms of hypoglycemia: sweating, tremor, dizziness, confusion, hunger, irritability, rapid heartbeat, blurred vision, slurred speech, headache, weakness, anxiety.
  • Symptoms of allergic reaction: rash, itching, hives, swelling of face/lips/tongue/throat, difficulty breathing.
  • Symptoms of liver problems: yellowing of skin/eyes (jaundice), dark urine, persistent nausea/vomiting, severe stomach pain.

Special Patient Groups

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Pregnancy

Glyburide is generally not recommended for use during pregnancy. While classified as Pregnancy Category B, insulin is the preferred treatment for diabetes during pregnancy due to better glycemic control and lower risk of neonatal complications.

Trimester-Specific Risks:

First Trimester: Limited data, but generally considered low risk of teratogenicity. However, optimal glycemic control is crucial.
Second Trimester: Risk of neonatal hypoglycemia and macrosomia if glycemic control is poor. Insulin is preferred.
Third Trimester: Increased risk of neonatal hypoglycemia if used close to delivery, as glyburide crosses the placenta.
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Lactation

Glyburide is excreted into breast milk in small amounts. While the risk to the infant appears low, monitoring the infant for signs of hypoglycemia (e.g., lethargy, poor feeding) is recommended. Insulin is generally preferred during lactation.

Infant Risk: Low to moderate risk of hypoglycemia in the infant. Monitor for signs of hypoglycemia.
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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 polypharmacy. Start with the lowest effective dose (e.g., 1.25 mg daily) and titrate slowly with careful monitoring of blood glucose.

Clinical Information

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Clinical Pearls

  • Glyburide has a relatively long duration of action, increasing the risk of prolonged hypoglycemia, especially in elderly patients or those with renal/hepatic impairment.
  • Always take glyburide with the first main meal of the day to minimize the risk of hypoglycemia.
  • Micronized formulations (e.g., Glynase PresTab) may have different bioavailability compared to non-micronized forms (e.g., DiaBeta, Micronase) and are not interchangeable on a milligram-for-milligram basis.
  • Educate patients thoroughly on the symptoms and management of hypoglycemia.
  • Avoid in patients with severe renal or hepatic impairment; insulin is a safer alternative in these populations.
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Alternative Therapies

  • Metformin (Biguanide)
  • 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., Canagliflozin, Dapagliflozin)
  • Thiazolidinediones (e.g., Pioglitazone, Rosiglitazone)
  • Insulin
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets (generic 5mg)
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 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 is a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, do not 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 details about the medication taken, the amount, and the time it happened.