Glucotrol 10mg Tablets

Manufacturer PFIZER U.S. Active Ingredient Glipizide Tablets(GLIP i zide) Pronunciation GLIP i zide
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
Jun 1984
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Glipizide 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 before a meal, and to monitor your blood sugar regularly.
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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 30 minutes before eating, specifically 30 minutes before your first meal of the day if you are taking it once daily. It's essential to understand what to do if you don't eat as much as usual or if you skip a meal, so be sure to discuss this with your doctor.

Storing and Disposing of Your Medication

Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. Instead, check with your pharmacist for guidance on the best disposal method, and consider participating in a drug take-back program in your area.

Missing a Dose

If you miss a dose, take it as soon as you remember. 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 a missed one.
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Lifestyle & Tips

  • 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.
  • 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.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 5 mg once daily, 30 minutes before breakfast. Maintenance: 5-20 mg once daily or in divided doses.
Dose Range: 2.5 - 40 mg

Condition-Specific Dosing:

initialDose: 5 mg once daily, 30 minutes before breakfast. For elderly or patients with liver disease, consider 2.5 mg.
titration: Increase dose in increments of 2.5-5 mg as needed, based on blood glucose response. Allow several days between titrations. Max single dose: 15 mg. Doses >15 mg should be divided.
maximumDailyDose: 40 mg
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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: Consider lower initial dose (2.5 mg) and titrate cautiously. Monitor closely for hypoglycemia.
Severe: Use with extreme caution or avoid due to increased risk of hypoglycemia. Consider alternative agents.
Dialysis: Not dialyzable. Use with extreme caution or avoid due to increased risk of hypoglycemia.

Hepatic Impairment:

Mild: Consider lower initial dose (2.5 mg) and titrate cautiously. Monitor closely for hypoglycemia.
Moderate: Consider lower initial dose (2.5 mg) and titrate cautiously. Monitor closely for hypoglycemia.
Severe: Use with extreme caution or avoid due to increased risk of hypoglycemia. Consider alternative agents.

Pharmacology

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Mechanism of Action

Glipizide is a second-generation sulfonylurea that lowers blood glucose primarily 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. It also has some extrapancreatic effects, such as increasing insulin sensitivity in peripheral tissues and reducing hepatic glucose production, though these are considered minor compared to its primary mechanism.
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Pharmacokinetics

Absorption:

Bioavailability: Nearly 100%
Tmax: 1-3 hours
FoodEffect: Food (especially high-fat meals) delays absorption and reduces peak plasma concentrations. Should be taken 30 minutes before a meal.

Distribution:

Vd: Approximately 10 liters
ProteinBinding: >98% (primarily to albumin)
CnssPenetration: Limited

Elimination:

HalfLife: 2-4 hours
Clearance: Not available (primarily hepatic metabolism)
ExcretionRoute: Mainly renal (80%) as inactive metabolites, with a small amount (10%) excreted in feces.
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Approximately 30 minutes
PeakEffect: 1-3 hours
DurationOfAction: 10-24 hours (variable, depending on dose and individual response)

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 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
Slurred speech
Tingling
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling extremely tired or weak
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. To manage low blood sugar, follow your doctor's instructions, which may include taking glucose tablets, liquid glucose, or some fruit juices.

Other Possible Side Effects

Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you notice 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:

Dizziness
Diarrhea
Feeling nervous and excitable
Gas

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, extreme hunger, irritability, headache, blurred vision, rapid heartbeat. If these occur, treat immediately with fast-acting sugar.
  • Symptoms of high blood sugar (hyperglycemia): increased thirst, frequent urination, increased hunger, fatigue, blurred vision. Report these to your doctor.
  • Symptoms of liver problems: unusual tiredness, dark urine, yellowing of skin or eyes (jaundice), nausea, vomiting, 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.
A known sulfa allergy, as this may affect your ability to take this medication.
Acidic blood problems, such as acidosis, which may require special consideration when taking this drug.
Type 1 diabetes, as this medication is not intended to treat this condition. If you have type 1 diabetes, your doctor will need to discuss alternative treatment options with you.

This list is not exhaustive, and it is crucial to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you are experiencing. Your doctor and pharmacist need this information to ensure safe use of this medication. Never start, stop, or change the dose of any medication without first consulting your doctor to confirm that it is safe to do so.
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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. Before engaging in activities that require alertness, such as driving, wait until you understand how this drug affects you. Monitor your blood sugar levels as instructed by your doctor.

Regular blood tests will be necessary, as directed by your doctor. Be sure to discuss any concerns or questions with your doctor during these appointments. Additionally, inform all healthcare providers and laboratory personnel that you are taking this medication, as it may impact certain lab test results.

Adhere to the diet and exercise plan recommended by your doctor. If you experience low blood sugar, avoid driving, as this can increase your risk of being involved in an accident. It is also recommended to avoid consuming alcohol while taking this medication.

If you are taking colesevelam, take it at least 4 hours after taking this drug. Be aware that stress, such as fever, infection, injury, or surgery, can affect blood sugar control. Changes in physical activity, exercise, or diet may also impact blood sugar levels.

Individuals with low levels of the enzyme G6PD should exercise caution, as they may be at a higher risk of developing anemia. This enzyme deficiency is more common in people of African, South Asian, Middle Eastern, and Mediterranean descent.

There is an increased risk of death from heart disease associated with this medication. Discuss this risk with your doctor. Low blood sugar is a potential side effect, and severe cases can lead to seizures, loss of consciousness, long-term brain damage, and even death. Consult with your doctor about this risk.

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant or breastfeeding women should inform their doctor, as the benefits and risks of this medication need to be carefully considered. If you are pregnant, be aware that low blood sugar has occurred in infants born to mothers taking similar medications. Your doctor will advise you on when to stop taking this medication before your due date.
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Overdose Information

Overdose Symptoms:

  • Severe hypoglycemia (extremely low blood sugar)
  • Confusion
  • Slurred speech
  • 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, seek emergency medical attention. Call 911 or 1-800-222-1222 (Poison Control Center) for advice.

Drug Interactions

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Major Interactions

  • Bosentan (increased risk of hepatotoxicity)
  • Miconazole (oral, IV, topical) (potentiates hypoglycemic effect)
  • Alcohol (potentiates hypoglycemic effect, disulfiram-like reaction)
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Moderate Interactions

  • Beta-blockers (mask symptoms of hypoglycemia, impair glucose counter-regulation)
  • Fluconazole, other azole antifungals (increase glipizide levels)
  • NSAIDs (enhance hypoglycemic effect)
  • Sulfonamides (enhance hypoglycemic effect)
  • Warfarin (may alter anticoagulant effect, monitor INR)
  • Chloramphenicol (enhance hypoglycemic effect)
  • Probenecid (enhance hypoglycemic effect)
  • Salicylates (high doses, enhance hypoglycemic effect)
  • Corticosteroids (decrease hypoglycemic effect)
  • Thiazide diuretics (decrease hypoglycemic effect)
  • Thyroid hormones (decrease hypoglycemic effect)
  • Sympathomimetics (decrease hypoglycemic effect)
  • Phenytoin (decrease hypoglycemic effect)
  • Rifampin (decrease glipizide levels)
  • Clarithromycin (increase glipizide levels)
  • Gemfibrozil (increase glipizide levels)
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Minor Interactions

  • Cimetidine (minor increase in glipizide levels)
  • Digoxin (minor interaction, monitor)

Monitoring

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Baseline Monitoring

Fasting Plasma Glucose (FPG)

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

Timing: Prior to initiation of therapy.

Hemoglobin A1c (HbA1c)

Rationale: To assess long-term glycemic control (average blood glucose over 2-3 months).

Timing: Prior to initiation of therapy.

Renal Function (SCr, eGFR)

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

Timing: Prior to initiation of therapy.

Hepatic Function (ALT, AST, Bilirubin)

Rationale: To assess liver function, as glipizide is metabolized in 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 (provider)

Target: 80-130 mg/dL (ADA target for most non-pregnant adults)

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

Hemoglobin A1c (HbA1c)

Frequency: Every 3-6 months

Target: <7.0% (ADA target for most non-pregnant adults)

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

Symptoms of Hypoglycemia

Frequency: Ongoing patient self-monitoring

Target: N/A

Action Threshold: Any occurrence of symptoms (e.g., sweating, tremor, confusion) requires immediate action and dose review.

Renal Function (SCr, eGFR)

Frequency: Annually, or more frequently if clinically indicated (e.g., with dose changes, new medications, or worsening renal function)

Target: Stable eGFR

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

Hepatic Function (ALT, AST)

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

Target: Within normal limits

Action Threshold: Elevated liver enzymes (investigate cause, consider discontinuation).

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Symptom Monitoring

  • Symptoms of hypoglycemia: sweating, tremor, dizziness, confusion, hunger, irritability, headache, blurred vision, rapid heartbeat, slurred speech, weakness, anxiety.
  • Symptoms of hyperglycemia (less common with glipizide monotherapy unless dose is insufficient): increased thirst, frequent urination, increased hunger, fatigue, blurred vision.
  • Symptoms of liver dysfunction: persistent nausea, vomiting, abdominal pain, dark urine, jaundice, fatigue.

Special Patient Groups

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Pregnancy

Glipizide is generally not recommended during pregnancy due to the risk of neonatal hypoglycemia. Insulin is the preferred treatment for diabetes during pregnancy.

Trimester-Specific Risks:

First Trimester: Potential for fetal harm not fully established, but generally avoided.
Second Trimester: Risk of neonatal hypoglycemia if used close to delivery.
Third Trimester: High risk of severe and prolonged neonatal hypoglycemia if used near term. Should be discontinued at least one month before expected delivery.
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Lactation

Glipizide is excreted into breast milk and can cause hypoglycemia in the nursing infant. It is generally not recommended during breastfeeding. Insulin or other agents with better safety profiles are preferred.

Infant Risk: Risk of hypoglycemia in the infant. Monitor infant for signs of hypoglycemia (e.g., lethargy, poor feeding, jitteriness).
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Pediatric Use

Safety and effectiveness in pediatric patients have not been established. Glipizide is not recommended for use in children.

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Geriatric Use

Elderly patients are at increased risk for hypoglycemia due to age-related decline in renal and hepatic function, and potential for polypharmacy. Start with a lower initial dose (2.5 mg) and titrate cautiously. Monitor blood glucose closely.

Clinical Information

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Clinical Pearls

  • Glipizide should be taken 30 minutes before the first main meal of the day to optimize absorption and reduce postprandial glucose.
  • For doses exceeding 15 mg daily, it is recommended to divide the dose to reduce gastrointestinal side effects and potentially improve glycemic control.
  • Patients should be educated thoroughly on the symptoms and management of hypoglycemia.
  • Alcohol consumption should be limited or avoided due to increased risk of hypoglycemia and potential disulfiram-like reactions.
  • Glipizide is generally considered a second-line agent after metformin, or used in combination with metformin, for Type 2 Diabetes.
  • Due to its short half-life, glipizide (immediate release) may be preferred over longer-acting sulfonylureas in patients with renal impairment, but still requires careful monitoring and dose adjustment.
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Alternative Therapies

  • Metformin (first-line)
  • Other sulfonylureas (e.g., glyburide, glimepiride)
  • DPP-4 inhibitors (e.g., sitagliptin, saxagliptin)
  • SGLT2 inhibitors (e.g., empagliflozin, canagliflozin)
  • GLP-1 receptor agonists (e.g., liraglutide, semaglutide)
  • Thiazolidinediones (e.g., pioglitazone)
  • Insulin
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Cost & Coverage

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