Nateglinide 60mg Tablets
It is used to lower blood sugar in patients with high blood sugar (diabetes).
Drug Class
Antidiabetic agent
Pharmacologic Class
Meglitinide; Insulin secretagogue
Pregnancy Category
Category C
FDA Approved
Dec 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Nateglinide 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 from your pancreas, especially right after you eat. This helps lower your blood sugar levels after meals.
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 1 to 30 minutes before meals. If you skip a meal, skip your dose for that meal.
Storing and Disposing of Your Medication
Keep your medication at room temperature in a dry place, avoiding storage in a bathroom. Ensure all medications are stored in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, skip it and resume your normal dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your dose 1 to 30 minutes before meals. If you skip a meal, skip your dose for that meal.
Storing and Disposing of Your Medication
Keep your medication at room temperature in a dry place, avoiding storage in a bathroom. Ensure all medications are stored in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, skip it and resume your normal dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take Nateglinide 1 to 30 minutes before each main meal (breakfast, lunch, and dinner).
- If you skip a meal, skip your dose of Nateglinide for that meal to avoid low blood sugar.
- Do not take Nateglinide if you are not going to eat a meal.
- Follow your doctor's recommendations for diet and exercise, as these are crucial for managing diabetes.
- 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.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
60 mg orally three times daily, 1 to 30 minutes before each main meal. May be increased to 120 mg three times daily if HbA1c response is inadequate after 1-2 weeks.
Dose Range:
60 - 120 mg
Condition-Specific Dosing:
initial_therapy:
60 mg three times daily for patients with HbA1c near target (e.g., <8%) or who are at risk of hypoglycemia.
inadequate_response:
Increase to 120 mg three times daily if HbA1c response is inadequate after 1-2 weeks at 60 mg.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required (CrCl > 50 mL/min)
Moderate:
No dose adjustment required (CrCl 30-50 mL/min), but monitor for hypoglycemia.
Severe:
Use with caution and monitor closely for hypoglycemia (CrCl < 30 mL/min). Not recommended for routine use.
Dialysis:
Use with caution and monitor closely for hypoglycemia. Not recommended for routine use in ESRD patients on dialysis due to limited data and potential for accumulation of active metabolites.
Hepatic Impairment:
Mild:
Use with caution and monitor closely for hypoglycemia.
Moderate:
Use with caution and monitor closely for hypoglycemia. Consider lower starting dose.
Severe:
Not recommended due to increased risk of hypoglycemia and prolonged drug exposure.
Pharmacology
Mechanism of Action
Nateglinide is a meglitinide derivative that lowers blood glucose by stimulating insulin secretion from the pancreatic beta cells. It achieves this by binding to the sulfonylurea receptor 1 (SUR1) on the beta cell membrane, leading to the closure of ATP-dependent 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 granules.
Pharmacokinetics
Absorption:
Bioavailability:
High (absolute bioavailability not precisely determined but well absorbed)
Tmax:
Approximately 1 hour (range 0.5 to 1.5 hours)
FoodEffect:
Food delays absorption and reduces Cmax (peak concentration) but does not significantly affect AUC (total exposure). Should be taken before meals.
Distribution:
Vd:
Approximately 10 L
ProteinBinding:
Approximately 98% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 1.5 hours
Clearance:
Approximately 13 L/hour
ExcretionRoute:
Primarily renal (83%), with a smaller portion (10%) excreted in feces.
Unchanged:
Less than 10% of the dose is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Rapid (within 20-30 minutes)
PeakEffect:
Approximately 1 hour
DurationOfAction:
Short (approximately 4 hours)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience 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
Low blood sugar (hypoglycemia), which may be more likely to occur 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, 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
Like all medications, this drug can cause side effects. While 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 or seek medical help:
* Signs of a common cold
Reporting Side Effects
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.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience 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
Low blood sugar (hypoglycemia), which may be more likely to occur 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, 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
Like all medications, this drug can cause side effects. While 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 or seek medical help:
* Signs of a common cold
Reporting Side Effects
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.
Seek Immediate Medical Attention If You Experience:
- Symptoms of low blood sugar (hypoglycemia): sweating, shakiness, dizziness, confusion, hunger, irritability, blurred vision, headache, rapid heartbeat. If these occur, treat immediately with sugar and notify your doctor.
- Symptoms of high blood sugar (hyperglycemia): increased thirst, increased urination, fatigue, blurred vision. Report these to your doctor.
- Signs of liver problems: unexplained nausea, vomiting, stomach pain, unusual tiredness, loss of appetite, dark urine, yellowing of skin or eyes (jaundice). Seek medical attention immediately.
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.
Certain health conditions, including:
+ Acidic blood problems
+ Type 1 diabetes
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting 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.
Certain health conditions, including:
+ Acidic blood problems
+ Type 1 diabetes
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
This drug may cause low blood sugar (hypoglycemia), which can be severe and lead to seizures, loss of consciousness, permanent brain damage, and even death. To manage this risk, it is crucial to discuss your condition with your doctor. If you experience low blood sugar, do not drive, as this can significantly increase your risk of being involved in an accident. Monitor your blood sugar levels as directed by your doctor to ensure timely intervention if your levels drop.
Regular blood tests are necessary to assess the effects of this medication on your body. Adhere to the schedule recommended by your doctor and discuss any concerns or questions you may have. Additionally, consult your doctor before consuming alcohol, as it may interact with your medication.
To effectively manage your condition, follow the personalized diet and exercise plan provided by your doctor. Be aware that stress, such as fever, infection, injury, or surgery, can affect blood sugar control. Changes in physical activity, exercise routines, or diet can also impact your blood sugar levels.
If you are pregnant or planning to become pregnant, it is vital to discuss the potential benefits and risks of using this medication during pregnancy with your doctor. This will help you make an informed decision about your treatment plan.
This drug may cause low blood sugar (hypoglycemia), which can be severe and lead to seizures, loss of consciousness, permanent brain damage, and even death. To manage this risk, it is crucial to discuss your condition with your doctor. If you experience low blood sugar, do not drive, as this can significantly increase your risk of being involved in an accident. Monitor your blood sugar levels as directed by your doctor to ensure timely intervention if your levels drop.
Regular blood tests are necessary to assess the effects of this medication on your body. Adhere to the schedule recommended by your doctor and discuss any concerns or questions you may have. Additionally, consult your doctor before consuming alcohol, as it may interact with your medication.
To effectively manage your condition, follow the personalized diet and exercise plan provided by your doctor. Be aware that stress, such as fever, infection, injury, or surgery, can affect blood sugar control. Changes in physical activity, exercise routines, or diet can also impact your blood sugar levels.
If you are pregnant or planning to become pregnant, it is vital to discuss the potential benefits and risks of using this medication during pregnancy with your doctor. This will help you make an informed decision about your treatment plan.
Overdose Information
Overdose Symptoms:
- Severe hypoglycemia (very low blood sugar)
- Loss of consciousness
- Seizures
What to Do:
Call 911 or your local emergency number immediately. If the person is conscious, give them a source of fast-acting sugar (e.g., glucose tablets, sugar water, fruit juice). If unconscious, do not give anything by mouth. Emergency medical personnel may administer glucagon or intravenous glucose. Call 1-800-222-1222 for Poison Control advice.
Drug Interactions
Major Interactions
- Gemfibrozil (increases nateglinide exposure, increasing hypoglycemia risk)
- Rifampin (decreases nateglinide exposure, reducing efficacy)
Moderate Interactions
- Nonselective beta-blockers (mask hypoglycemia symptoms, increase hypoglycemia risk)
- NSAIDs (may enhance hypoglycemic effect)
- Salicylates (may enhance hypoglycemic effect)
- MAOIs (may enhance hypoglycemic effect)
- ACE inhibitors (may enhance hypoglycemic effect)
- Other antidiabetic agents (additive hypoglycemia risk)
- Thiazide diuretics (may decrease hypoglycemic effect)
- Corticosteroids (may decrease hypoglycemic effect)
- Thyroid products (may decrease hypoglycemic effect)
- Sympathomimetics (may decrease hypoglycemic effect)
- Calcium channel blockers (may decrease hypoglycemic effect)
- Isoniazid (may decrease hypoglycemic effect)
Monitoring
Baseline Monitoring
HbA1c (Glycated Hemoglobin)
Rationale: To establish baseline glycemic control and guide initial dosing.
Timing: Prior to initiation of therapy.
Fasting Plasma Glucose (FPG)
Rationale: To establish baseline glycemic control.
Timing: Prior to initiation of therapy.
Renal Function (e.g., CrCl, eGFR)
Rationale: To assess kidney function, as dose adjustments or caution may be needed in severe impairment.
Timing: Prior to initiation of therapy.
Hepatic Function (e.g., ALT, AST, bilirubin)
Rationale: To assess liver function, as dose adjustments or caution may be needed in impairment.
Timing: Prior to initiation of therapy.
Routine Monitoring
HbA1c (Glycated Hemoglobin)
Frequency: Every 3-6 months
Target: <7% (individualized based on patient factors)
Action Threshold: If HbA1c remains above target, consider dose adjustment or addition/change of therapy.
Self-monitoring of Blood Glucose (SMBG)
Frequency: As directed by healthcare provider (e.g., pre-meal, 1-2 hours post-meal, bedtime)
Target: FPG: 80-130 mg/dL; Postprandial: <180 mg/dL (individualized)
Action Threshold: Persistent readings outside target range, or frequent hypoglycemic episodes, require re-evaluation of therapy.
Signs and Symptoms of Hypoglycemia
Frequency: Continuously
Target: N/A
Action Threshold: Immediate intervention (e.g., consume fast-acting carbohydrates) if symptoms occur. Report frequent episodes to healthcare provider.
Symptom Monitoring
- Symptoms of hypoglycemia (e.g., sweating, tremor, dizziness, confusion, hunger, irritability, blurred vision, headache, rapid heartbeat)
- Symptoms of hyperglycemia (e.g., increased thirst, increased urination, fatigue, blurred vision)
- Signs of liver dysfunction (e.g., unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, dark urine, jaundice)
Special Patient Groups
Pregnancy
Nateglinide is Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Insulin is generally preferred for glycemic control during pregnancy.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm cannot be ruled out based on animal studies. Insulin is generally preferred.
Second Trimester:
Potential for fetal harm cannot be ruled out. Insulin is generally preferred.
Third Trimester:
Potential for fetal harm cannot be ruled out. Insulin is generally preferred.
Lactation
It is not known whether nateglinide is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for hypoglycemia in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Unknown; potential for hypoglycemia in nursing infant.
Pediatric Use
Safety and effectiveness of nateglinide in pediatric patients have not been established. Use is not recommended.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly (âĨ65 years) and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. Monitor renal function.
Clinical Information
Clinical Pearls
- Nateglinide is a rapid-acting insulin secretagogue, primarily effective at reducing postprandial glucose excursions.
- It has a short duration of action, which contributes to a lower risk of hypoglycemia compared to longer-acting sulfonylureas, especially between meals or overnight.
- Patients must take nateglinide immediately before (1-30 minutes) each main meal. If a meal is skipped, the dose should be skipped to avoid hypoglycemia.
- It is often used in combination with metformin or thiazolidinediones for improved glycemic control.
- Consider starting with the 60 mg dose for patients with HbA1c close to target or those prone to hypoglycemia.
Alternative Therapies
- Repaglinide (another meglitinide)
- Sulfonylureas (e.g., glipizide, glyburide, glimepiride)
- Metformin (biguanide)
- DPP-4 inhibitors (e.g., sitagliptin, saxagliptin)
- GLP-1 receptor agonists (e.g., liraglutide, semaglutide)
- SGLT2 inhibitors (e.g., empagliflozin, dapagliflozin)
- Thiazolidinediones (e.g., pioglitazone, rosiglitazone)
- Insulin
Cost & Coverage
Average Cost:
Varies, typically $10-$50 per 30 tablets (generic 60mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
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 taken, the amount, and the time it occurred.