Glipizide XL 2.5mg Tablets

Manufacturer GREENSTONE 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
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?

Glipizide 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 natural hormone that lowers blood sugar. Because it's an extended-release tablet, it releases the medicine slowly over the day, so you usually only need to take it once daily.
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How to Use This Medicine

Taking Your Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your dose with your first meal of the day. Swallow the tablet whole - do not chew, break, crush, or dissolve it. If you have a change in your eating habits or skip a meal, be sure to understand how to adjust your medication schedule accordingly.

Storing and Disposing of Your Medication

Keep your medication at room temperature in a dry place, avoiding storage in a bathroom. Store the medication in its original container to maintain its potency. It is essential to keep all medications in a safe location, out of the reach of children and pets, to prevent accidental ingestion.

Missing a Dose

If you miss a dose, take it as soon as you remember. 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

  • Take Glipizide XL once daily with breakfast to ensure proper absorption and reduce the risk of stomach upset.
  • Do not crush, chew, or divide the extended-release tablets; swallow them whole.
  • 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 fast-acting sugar (e.g., glucose tablets, hard candy, fruit juice) to treat mild to moderate hypoglycemia.
  • Limit or avoid alcohol consumption, as it can increase the risk of low blood sugar and cause a disulfiram-like reaction.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 5 mg once daily with breakfast. Maintenance: 5-20 mg once daily.
Dose Range: 2.5 - 20 mg

Condition-Specific Dosing:

initial_therapy: Start with 5 mg once daily. For patients sensitive to hypoglycemic agents, start with 2.5 mg once daily.
dose_titration: Increase dose in increments of 2.5 mg or 5 mg, usually at weekly intervals, based on blood glucose response. Maximum recommended daily dose is 20 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 recommended, but monitor closely.
Moderate: Use with caution. Consider starting at 2.5 mg once daily and titrate slowly. Monitor blood glucose closely.
Severe: Use with caution. Consider starting at 2.5 mg once daily and titrate slowly. Monitor blood glucose closely. Avoid if possible due to increased risk of hypoglycemia.
Dialysis: Not recommended for use in patients on dialysis due to prolonged half-life and increased risk of hypoglycemia.

Hepatic Impairment:

Mild: Use with caution. Consider starting at 2.5 mg once daily and titrate slowly. Monitor blood glucose closely.
Moderate: Use with caution. Consider starting at 2.5 mg once daily and titrate slowly. Monitor blood glucose closely. Increased risk of hypoglycemia.
Severe: Contraindicated due to increased risk of severe and prolonged hypoglycemia.

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 closure of ATP-sensitive potassium channels, depolarization of the membrane, and opening of voltage-gated calcium channels. The influx of calcium triggers insulin secretion. Glipizide also has extrapancreatic effects, including increased peripheral glucose utilization and decreased hepatic glucose production, though these are considered minor compared to its insulinotropic effect.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 100%
Tmax: 6-12 hours (for extended-release formulation)
FoodEffect: Absorption may be delayed by food, but the extent of absorption is not significantly affected. Should be taken with breakfast.

Distribution:

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

Elimination:

HalfLife: 10-16 hours (for extended-release formulation)
Clearance: Not available (variable)
ExcretionRoute: Renal (approximately 80% as metabolites), Fecal (approximately 10% as metabolites)
Unchanged: Less than 1% (renal)
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Pharmacodynamics

OnsetOfAction: Within 1-2 hours (for immediate release; extended release has a more gradual onset)
PeakEffect: 6-12 hours (for extended-release formulation)
DurationOfAction: 24 hours (for extended-release formulation)

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. Follow your doctor's instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or consuming certain fruit juices.

Other Possible Side Effects

Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:

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, 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, headache, blurred vision, rapid heartbeat. If these occur, consume a quick source of sugar and notify your doctor.
  • Symptoms of high blood sugar (hyperglycemia): increased thirst, frequent urination, fatigue, blurred vision. If these occur, notify your doctor.
  • Signs of liver problems: unusual tiredness, nausea, vomiting, stomach pain, dark urine, yellowing of skin or eyes. Seek immediate medical attention if these occur.
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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 conditions to ensure safe treatment:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
A known sulfa allergy, as this may affect your ability to take this medication.
Any narrowing of the gastrointestinal (GI) tract or a bowel block, as this may impact the absorption or passage of the medication.
Acidic blood problems, which may require special consideration when taking this medication.
Type 1 diabetes, as this medication is not intended to treat this condition. If you have type 1 diabetes, your doctor will discuss alternative treatment options with you.

Additionally, it is crucial to disclose all your medications, including:

Prescription and over-the-counter (OTC) drugs
Natural products
Vitamins

Share this information with both your doctor and pharmacist to ensure that it is safe to take this medication with your existing treatments and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor to avoid potential interactions or complications.
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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 work is necessary, so follow your doctor's recommendations for check-ups and discuss any concerns with them. Be aware that this medication may interfere with certain laboratory tests, so notify all healthcare providers and lab personnel that you are taking this drug.

Adhere to the diet and exercise plan outlined by your doctor. If you experience low blood sugar, avoid driving, as it increases the risk of accidents. Additionally, refrain from consuming alcohol while taking this medication.

If you are also 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, particularly those of African, South Asian, Middle Eastern, or Mediterranean descent, should exercise caution, as they may be more prone to anemia.

This medication may increase the risk of heart disease-related death; discuss this 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, or even death. Consult your doctor if you experience any symptoms.

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant or breastfeeding women, or those planning to become pregnant, should discuss the benefits and risks of this medication with their doctor.

You may notice the tablet shell in your stool, but this is a normal occurrence and not a cause for concern. However, if you take this medication during pregnancy, you may need to stop taking it before your due date, as low blood sugar has been reported in infants born to mothers who took similar medications. Consult your doctor to determine the best course of action.
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Overdose Information

Overdose Symptoms:

  • Severe hypoglycemia (extremely low blood sugar)
  • Confusion
  • Slurred speech
  • Tremor
  • 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 911 or your local emergency number. Call 1-800-222-1222 (Poison Control Center).

Drug Interactions

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Contraindicated Interactions

  • Bosentan (increased risk of hepatotoxicity)
  • Miconazole (oral, systemic) (potentiates hypoglycemic effect)
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Major Interactions

  • Beta-blockers (may mask symptoms of hypoglycemia, prolong hypoglycemic episodes)
  • Fluconazole (increases glipizide levels, risk of hypoglycemia)
  • NSAIDs (e.g., ibuprofen, naproxen) (potentiate hypoglycemic effect)
  • Sulfonamides (e.g., sulfamethoxazole/trimethoprim) (potentiate hypoglycemic effect)
  • Warfarin (may alter anticoagulant effect, monitor INR)
  • Alcohol (potentiates hypoglycemic effect, disulfiram-like reaction)
  • Corticosteroids (decrease hypoglycemic effect of glipizide)
  • Thiazide diuretics (decrease hypoglycemic effect of glipizide)
  • Sympathomimetics (e.g., pseudoephedrine, epinephrine) (decrease hypoglycemic effect of glipizide)
  • Thyroid hormones (decrease hypoglycemic effect of glipizide)
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Moderate Interactions

  • ACE inhibitors (may enhance glucose-lowering effect)
  • MAO inhibitors (may enhance glucose-lowering effect)
  • Chloramphenicol (potentiates hypoglycemic effect)
  • Cimetidine (may increase glipizide levels)
  • Clarithromycin (may increase glipizide levels)
  • Gemfibrozil (may increase glipizide levels)
  • Probenecid (may increase glipizide levels)
  • Salicylates (high doses) (potentiate hypoglycemic effect)
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Minor Interactions

  • Chromium supplements (may enhance glucose-lowering effect)
  • Garlic (may enhance glucose-lowering 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 Mellitus.

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 (e.g., eGFR, creatinine)

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

Timing: Prior to initiation of therapy.

Hepatic Function (e.g., ALT, AST)

Rationale: To assess liver function as glipizide is metabolized in the liver and 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 (laboratory)

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)

Signs/Symptoms of Hypoglycemia

Frequency: Ongoing, patient education for self-monitoring

Target: N/A

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

Renal Function (e.g., eGFR, creatinine)

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

Target: Stable, within normal limits

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

Hepatic Function (e.g., ALT, AST)

Frequency: Annually or more frequently if clinically indicated (e.g., with concomitant hepatotoxic drugs, new symptoms)

Target: Stable, within normal limits

Action Threshold: Significant elevation (consider discontinuation).

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Symptom Monitoring

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

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 if used near term. Discuss risks and benefits with a healthcare provider.

Trimester-Specific Risks:

First Trimester: Potential for teratogenicity, though data are limited and conflicting. Insulin is preferred.
Second Trimester: Risk of fetal hypoglycemia and macrosomia if glycemic control is poor. Insulin is preferred.
Third Trimester: High risk of severe neonatal hypoglycemia if used near term, as glipizide crosses the placenta. Discontinue at least one month before expected delivery.
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Lactation

Not recommended during breastfeeding. Glipizide is excreted into breast milk and may cause hypoglycemia in the nursing infant. Insulin is generally preferred for glycemic control in lactating mothers.

Infant Risk: L4 (Possibly hazardous) - Potential for infant hypoglycemia, especially in neonates or infants with impaired renal/hepatic function. Monitor infant for signs of hypoglycemia.
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Pediatric Use

Safety and effectiveness have not been established in pediatric patients. Use is not recommended.

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Geriatric Use

Use with caution in elderly patients due to increased susceptibility to hypoglycemia, particularly those with impaired renal or hepatic function. Start with the lowest effective dose (e.g., 2.5 mg once daily) and titrate slowly. Monitor blood glucose closely.

Clinical Information

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Clinical Pearls

  • Glipizide XL should always be taken with breakfast to optimize absorption and minimize gastrointestinal upset.
  • Patients should be educated on the signs and symptoms of hypoglycemia and how to treat it immediately.
  • The 'ghost tablet' (the insoluble matrix of the extended-release tablet) may be seen in the stool, which is normal and does not indicate that the medication was not absorbed.
  • Avoid alcohol due to increased risk of hypoglycemia and potential disulfiram-like reactions.
  • Regular monitoring of HbA1c and blood glucose is crucial for dose adjustments and to prevent complications.
  • Consider alternative therapies or dose adjustments in patients with significant renal or hepatic impairment due to increased risk of prolonged hypoglycemia.
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Alternative Therapies

  • Metformin (first-line for Type 2 Diabetes)
  • 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, rosiglitazone)
  • Insulin therapy
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Cost & Coverage

Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (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 emergency medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to help healthcare professionals provide the best possible care.