Glucotrol 5mg 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 meals. If you are taking it once a day, take it 30 minutes before your first meal of the day. It's also important to know what to do if you don't eat as much as usual or if you skip a meal.

Storing and Disposing of Your Medication

Store your medication at room temperature in a dry place, away from the bathroom. Keep all medications in a safe location, out of the reach of children and pets. When your medication is no longer needed or has expired, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, ask your pharmacist. You may also want to check if there are any drug take-back programs in your area.

What to Do If You Miss 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 dose, skip the missed dose and go back to your regular schedule. Do not take two doses at the same time or take extra doses.
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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: 5 - 40 mg

Condition-Specific Dosing:

Type 2 Diabetes Mellitus: Initial: 5 mg once daily, 30 minutes before breakfast. Dosage may be increased in increments of 2.5-5 mg as needed, usually at intervals of several days, up to a maximum of 40 mg/day. Doses >15 mg/day should be divided and given twice daily.
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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: Start with a lower dose (e.g., 2.5 mg daily) and titrate slowly. Monitor blood glucose closely.
Severe: Use with caution, consider alternative agents. If used, start with 2.5 mg daily and monitor very closely for hypoglycemia.
Dialysis: Not recommended due to risk of prolonged hypoglycemia. Insulin is generally preferred.

Hepatic Impairment:

Mild: Start with a lower dose (e.g., 2.5 mg daily) and titrate slowly. Monitor blood glucose closely.
Moderate: Start with a lower dose (e.g., 2.5 mg daily) and titrate slowly. Monitor blood glucose closely. Increased risk of hypoglycemia.
Severe: Use with extreme caution or avoid. Increased risk of severe and prolonged hypoglycemia. Insulin is generally preferred.

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 pancreatic beta-cell membrane, leading to the closure of ATP-sensitive potassium channels. This depolarizes the cell, opening voltage-gated calcium channels, and the influx of calcium triggers insulin secretion. It also may increase peripheral glucose utilization and decrease hepatic glucose production.
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Pharmacokinetics

Absorption:

Bioavailability: Nearly 100%
Tmax: 1-3 hours
FoodEffect: Food delays absorption and decreases peak plasma concentrations, but the extent of absorption is not significantly affected. Should be taken 30 minutes before a meal for optimal effect.

Distribution:

Vd: 0.11 L/kg
ProteinBinding: >98% (primarily to albumin)
CnssPenetration: Limited

Elimination:

HalfLife: 2-4 hours
Clearance: Not available
ExcretionRoute: Renal (80%), Fecal (10%)
Unchanged: <10% (in urine)
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Pharmacodynamics

OnsetOfAction: Within 30 minutes
PeakEffect: 1-3 hours
DurationOfAction: 10-24 hours

Safety & Warnings

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Side Effects

Urgent 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
Slurred speech
Tingling
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling very tired or weak

Additionally, be aware of the risk of low blood sugar, which may be increased 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.

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 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, fast heartbeat, blurred vision, headache, weakness, anxiety. If these occur, consume a quick source of sugar immediately.
  • Symptoms of high blood sugar (hyperglycemia): increased thirst, increased urination, fatigue, blurred vision. Report these to your doctor.
  • Signs of allergic reaction: rash, itching, hives, swelling of the face, lips, tongue, or throat; difficulty breathing.
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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 existing health problems. Your doctor and pharmacist need this information to ensure safe use and potential interactions with this medication. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to confirm 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 it increases the risk of accidents. 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. If you have a deficiency of the enzyme G6PD, use caution, as you may be more prone to anemia. This deficiency is more common in individuals of African, South Asian, Middle Eastern, and Mediterranean descent.

There is an increased risk of heart disease-related death 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 your doctor if you experience any symptoms of low blood sugar.

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks with your doctor. It is essential to note that infants born to mothers taking this medication may experience low blood sugar. If you become pregnant, 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:

Seek immediate medical attention. Call 911 or your local emergency number. For advice, call a poison control center at 1-800-222-1222. Treatment involves administering glucose (oral or IV) and close monitoring of blood glucose levels.

Drug Interactions

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Major Interactions

  • Bosentan (increased risk of hepatotoxicity)
  • Miconazole (oral, IV, topical): Potentiates hypoglycemic effect, severe hypoglycemia reported.
  • Alcohol (acute ingestion): Potentiates hypoglycemic effect; chronic ingestion may decrease effect.
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Moderate Interactions

  • Beta-blockers (e.g., Propranolol): May mask symptoms of hypoglycemia and prolong hypoglycemic effect.
  • NSAIDs (e.g., Ibuprofen, Naproxen): May enhance hypoglycemic effect.
  • Salicylates (e.g., Aspirin): May enhance hypoglycemic effect.
  • Sulfonamides (e.g., Sulfamethoxazole/Trimethoprim): May enhance hypoglycemic effect.
  • Fluconazole: Increases glipizide plasma concentrations, enhancing hypoglycemic effect.
  • Chloramphenicol: May enhance hypoglycemic effect.
  • Probenecid: May enhance hypoglycemic effect.
  • Coumarin derivatives (e.g., Warfarin): May enhance hypoglycemic effect (rarely clinically significant).
  • MAOIs: May enhance hypoglycemic effect.
  • Corticosteroids: May decrease hypoglycemic effect.
  • Thiazide diuretics: May decrease hypoglycemic effect.
  • Thyroid products: May decrease hypoglycemic effect.
  • Estrogens/Oral Contraceptives: May decrease hypoglycemic effect.
  • Phenytoin: May decrease hypoglycemic effect.
  • Sympathomimetics: May decrease hypoglycemic effect.
  • Calcium channel blockers: May decrease hypoglycemic effect.
  • Isoniazid: May decrease hypoglycemic effect.
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Minor Interactions

  • Chromium supplements: May enhance hypoglycemic effect.

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 glipizide is primarily renally excreted and dose adjustments may be needed in impairment.

Timing: Prior to initiation of therapy.

Hepatic Function (ALT, AST, Bilirubin)

Rationale: To assess liver function as glipizide is metabolized in the liver and dose adjustments may be needed in impairment.

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 physician

Target: <130 mg/dL (individualized)

Action Threshold: >180 mg/dL consistently or <70 mg/dL

Hemoglobin A1c (HbA1c)

Frequency: Every 3-6 months

Target: <7% (individualized)

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

Signs and Symptoms of Hypoglycemia

Frequency: Continuously (patient education for self-monitoring)

Target: N/A

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

Renal Function (SCr, eGFR)

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

Target: Stable, within normal limits

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

Hepatic Function (ALT, AST)

Frequency: Annually or more frequently if clinically indicated

Target: Within normal limits

Action Threshold: Significant elevation (consider dose adjustment or discontinuation)

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Symptom Monitoring

  • Symptoms of hypoglycemia: sweating, tremor, dizziness, confusion, hunger, irritability, rapid heartbeat, blurred vision, headache, weakness, anxiety.
  • Symptoms of hyperglycemia: increased thirst, increased urination, fatigue, blurred vision.
  • Signs of allergic reaction: rash, itching, hives, swelling of face/lips/tongue/throat.

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 teratogenicity, though data are limited and conflicting. Generally avoided.
Second Trimester: Risk of fetal hyperinsulinemia and neonatal hypoglycemia. Insulin is preferred.
Third Trimester: High risk of severe and prolonged neonatal hypoglycemia if used near term. Insulin is preferred.
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Lactation

Glipizide is not recommended during breastfeeding. It is excreted into breast milk and can cause hypoglycemia in the nursing infant. Insulin is the preferred treatment for diabetes in lactating women.

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 caution in elderly patients due to increased risk of hypoglycemia, particularly in those with impaired renal or hepatic function. Start with a lower dose (e.g., 2.5 mg daily) and titrate slowly with close monitoring of blood glucose.

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 excursions.
  • For doses exceeding 15 mg daily, consider dividing the dose and administering twice daily to minimize the risk of hypoglycemia.
  • Educate patients thoroughly on the signs and symptoms of hypoglycemia and how to treat it.
  • Alcohol can significantly increase the risk of hypoglycemia when taken with glipizide.
  • Patients with sulfa allergies may have a cross-sensitivity to glipizide, though this is rare and often not clinically significant. Use with caution.
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Alternative Therapies

  • Metformin (first-line for most Type 2 DM patients)
  • Other sulfonylureas (e.g., Glyburide, Glimepiride)
  • DPP-4 inhibitors (e.g., Sitagliptin, Saxagliptin)
  • SGLT2 inhibitors (e.g., Canagliflozin, Dapagliflozin, Empagliflozin)
  • GLP-1 receptor agonists (e.g., Liraglutide, Semaglutide, Dulaglutide)
  • Thiazolidinediones (e.g., Pioglitazone, Rosiglitazone)
  • Insulin therapy
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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 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 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 information about the medication taken, the amount, and the time it happened.