Glucotrol XL 2.5mg Tablets

Manufacturer PFIZER Active Ingredient Glipizide Extended-Release Tablets(GLIP i zide) Pronunciation GLIP-ih-zyde
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
Sep 1994
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Glucotrol XL is a medication used to help control high blood sugar in people with type 2 diabetes. It works by helping your body release more insulin, a hormone that lowers blood sugar. It's an extended-release tablet, meaning it releases the medicine slowly over the day, so you usually take it only once daily.
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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 your first meal of the day. Swallow the tablet whole - do not chew, break, crush, or dissolve it. If you have any changes in your eating habits, such as skipping a meal or not eating as much as usual, be sure to ask your doctor for guidance on how to take your medication.

Storing and Disposing of Your Medication

Keep your medication at room temperature in a dry place, away from the bathroom. Store it in its original container to protect it from moisture and other environmental factors. Keep all medications in a safe and 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. 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 dose.
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Lifestyle & Tips

  • Take Glucotrol XL exactly as prescribed, usually once daily with breakfast or your first main meal.
  • Do not crush, chew, or divide the extended-release tablets.
  • 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 by your doctor.
  • Carry a source of sugar (e.g., glucose tablets, hard candy, fruit juice) to treat mild hypoglycemia.
  • Inform your doctor about all other medications, supplements, and herbal products you are taking.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 5 mg once daily with breakfast or the first main meal. Maintenance: 5-20 mg once daily.
Dose Range: 2.5 - 20 mg

Condition-Specific Dosing:

Type 2 Diabetes Mellitus: Initial: 5 mg once daily. Titrate in increments of 2.5-5 mg/day at intervals of at least 3 days, based on blood glucose response. Maximum recommended dose is 20 mg once 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 dose adjustment required, but monitor closely.
Moderate: Consider starting with 2.5 mg once daily and titrate cautiously. Monitor blood glucose and renal function frequently.
Severe: Use with caution; consider alternative agents. If used, start with 2.5 mg once daily and monitor closely for hypoglycemia.
Dialysis: Not recommended due to risk of prolonged hypoglycemia. Insulin is generally preferred.

Hepatic Impairment:

Mild: No specific dose adjustment required, but monitor closely.
Moderate: Consider starting with 2.5 mg once daily and titrate cautiously. Monitor blood glucose and hepatic function frequently.
Severe: Use with extreme caution or avoid. Glipizide is extensively metabolized by the liver. Increased risk of severe hypoglycemia. Insulin is generally preferred.

Pharmacology

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Mechanism of Action

Glipizide, a second-generation sulfonylurea, 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 depolarization of the beta-cell membrane opens voltage-gated calcium channels, resulting in an influx of calcium and subsequent exocytosis of insulin-containing granules. It also may increase peripheral glucose utilization and decrease hepatic glucose production, though these effects are secondary.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 100%
Tmax: 2-3 hours (for ER formulation)
FoodEffect: Absorption may be delayed by food, but the extent of absorption is not significantly affected. Should be taken with breakfast or the first main meal to minimize the risk of hypoglycemia.

Distribution:

Vd: Approximately 10-11 liters
ProteinBinding: Greater than 98% (primarily to albumin)
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 10-14 hours (for ER formulation)
Clearance: Not available
ExcretionRoute: Renal (approximately 80% as metabolites), Fecal (approximately 10% as metabolites)
Unchanged: Less than 1% (renal)
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Pharmacodynamics

OnsetOfAction: 1-2 hours
PeakEffect: 6-12 hours
DurationOfAction: 24 hours

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

Additionally, low blood sugar (hypoglycemia) can occur, especially when this medication is used with other diabetes medications. If you experience any of the following symptoms, contact your doctor right away:

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.

Other Possible Side Effects

Most people 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 if they bother you or do not go away:

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, blurred vision, slurred speech, headache, rapid heartbeat. If these occur, treat immediately with a fast-acting sugar source.
  • Symptoms of high blood sugar (hyperglycemia): increased thirst, increased urination, fatigue, blurred vision.
  • Unusual weight gain or swelling.
  • Yellowing of skin or eyes (jaundice), dark urine, or persistent nausea/vomiting (signs of liver problems).
  • Severe skin rash or allergic reaction.
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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.
A known sulfa allergy.
Any narrowing of the gastrointestinal (GI) tract or a bowel blockage.
Acidic blood conditions, such as acidosis.
* If you have type 1 diabetes, as this medication is not intended to treat this condition.

This list is not exhaustive, and it is crucial to discuss all your medications (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 drugs 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. 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 patients 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 discuss the benefits and risks of this medication with their doctor. If you are planning to become pregnant, inform your doctor, as they will need to weigh the benefits and risks to both you and the baby.

You may notice the tablet shell in your stool, but this is a normal occurrence and not a cause for concern. However, if you are taking this medication during pregnancy, you will need to stop taking it before your due date to minimize the risk of low blood sugar in your infant. Consult with your doctor to determine the best course of action.
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Overdose Information

Overdose Symptoms:

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

What to Do:

Seek immediate medical attention. For conscious patients, administer oral glucose. For unconscious patients, administer intravenous glucose or glucagon. Call 1-800-222-1222 (Poison Control Center) or emergency services.

Drug Interactions

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Major Interactions

  • Bosentan (increased risk of hepatotoxicity)
  • Miconazole (oral, severe hypoglycemia)
  • Alcohol (disulfiram-like reaction, increased risk of hypoglycemia)
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Moderate Interactions

  • Beta-blockers (mask symptoms of hypoglycemia, may prolong hypoglycemia)
  • NSAIDs (enhance hypoglycemic effect)
  • Salicylates (enhance hypoglycemic effect)
  • Sulfonamides (enhance hypoglycemic effect)
  • Chloramphenicol (enhance hypoglycemic effect)
  • Probenecid (enhance hypoglycemic effect)
  • Coumarin derivatives (potentiate or diminish anticoagulant effect)
  • Diuretics (thiazides, loop diuretics - may cause hyperglycemia)
  • Corticosteroids (may cause hyperglycemia)
  • Thyroid hormones (may cause hyperglycemia)
  • Sympathomimetics (may cause hyperglycemia)
  • Phenytoin (may cause hyperglycemia)
  • Nicotinic acid (may cause hyperglycemia)
  • Calcium channel blockers (may cause hyperglycemia)
  • Isoniazid (may cause hyperglycemia)
  • Rifampin (decreased glipizide levels)
  • Fluconazole (increased glipizide levels, increased risk of hypoglycemia)
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Minor Interactions

  • Chromium (may enhance hypoglycemic effect)
  • Garlic (may enhance hypoglycemic effect)

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 glycemic control and guide initial therapy.

Timing: Prior to initiation of therapy.

Renal Function (SCr, eGFR)

Rationale: To assess kidney function as glipizide metabolites are renally excreted and dose adjustment may be needed in impairment.

Timing: Prior to initiation of therapy.

Hepatic Function (ALT, AST, Bilirubin)

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

Timing: Prior to initiation of therapy.

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Routine Monitoring

HbA1c

Frequency: Every 3-6 months

Target: < 7% (individualized)

Action Threshold: > 7% (consider dose adjustment or add-on therapy)

Fasting Plasma Glucose (FPG)

Frequency: Daily to weekly (patient self-monitoring) or at clinic visits

Target: 80-130 mg/dL (individualized)

Action Threshold: < 70 mg/dL (hypoglycemia, requires action); > 130 mg/dL (hyperglycemia, consider dose adjustment)

Postprandial Glucose (PPG)

Frequency: Periodically (patient self-monitoring) or at clinic visits

Target: < 180 mg/dL (individualized)

Action Threshold: > 180 mg/dL (consider dose adjustment)

Signs/Symptoms of Hypoglycemia

Frequency: Ongoing

Target: N/A

Action Threshold: Any occurrence (requires immediate treatment and dose review)

Renal Function (SCr, eGFR)

Frequency: Annually or more frequently in patients with impairment or risk factors

Target: Stable

Action Threshold: Significant decline (consider dose adjustment)

Hepatic Function (ALT, AST)

Frequency: Annually or more frequently in patients with impairment or risk factors

Target: Stable

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

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Symptom Monitoring

  • Symptoms of hypoglycemia (e.g., sweating, tremor, dizziness, confusion, hunger, irritability, blurred vision, slurred speech, headache, palpitations)
  • Symptoms of hyperglycemia (e.g., increased thirst, increased urination, fatigue, blurred vision)
  • Gastrointestinal disturbances (e.g., nausea, diarrhea, constipation)
  • Skin reactions (e.g., rash, pruritus)
  • Weight changes

Special Patient Groups

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Pregnancy

Generally not recommended during pregnancy. Insulin is the preferred treatment for diabetes during pregnancy. Glipizide may cause severe neonatal hypoglycemia.

Trimester-Specific Risks:

First Trimester: Potential for teratogenicity, though data are limited and conflicting. Insulin is preferred.
Second Trimester: Risk of fetal hyperinsulinemia and neonatal hypoglycemia if used close to delivery.
Third Trimester: High risk of severe and prolonged neonatal hypoglycemia if used near term. Discontinue at least one month before expected delivery.
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Lactation

Not recommended during breastfeeding. Glipizide is excreted into breast milk and can cause hypoglycemia in the nursing infant.

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 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, especially in those with impaired renal or hepatic function. Start with a lower dose (e.g., 2.5 mg once daily) and titrate slowly. Monitor blood glucose closely.

Clinical Information

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Clinical Pearls

  • Glucotrol XL should be taken with breakfast or the first main meal of the day to optimize absorption and reduce the risk of hypoglycemia.
  • Do not crush, chew, or divide Glucotrol XL tablets, as this will disrupt the extended-release mechanism and can lead to rapid drug release and potential hypoglycemia.
  • Patients may notice a tablet 'ghost' in their stool; this is the inert matrix of the extended-release tablet and does not mean the medication was not absorbed.
  • Educate patients thoroughly on the signs and symptoms of hypoglycemia and how to treat it.
  • Alcohol consumption should be avoided or limited due to increased risk of hypoglycemia and potential disulfiram-like reactions.
  • Consider alternative agents or significant dose reduction in patients with moderate to severe renal or hepatic impairment due to increased risk of prolonged hypoglycemia.
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Alternative Therapies

  • Metformin (first-line for most Type 2 DM)
  • DPP-4 inhibitors (e.g., sitagliptin, saxagliptin)
  • SGLT2 inhibitors (e.g., empagliflozin, canagliflozin)
  • GLP-1 receptor agonists (e.g., liraglutide, semaglutide)
  • Thiazolidinediones (TZDs) (e.g., pioglitazone, rosiglitazone)
  • Insulin
  • Meglitinides (e.g., repaglinide, nateglinide) - shorter acting insulin secretagogues
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets (generic)
Generic Available: Yes
Insurance Coverage: Tier 1 (Generic) or Tier 2 (Brand)
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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's a good idea to check with your pharmacist for more information. 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 details about the medication, including the amount taken and the time it happened, to facilitate prompt and appropriate care.