Nateglinide 120mg Tablets
It is used to lower blood sugar in patients with high blood sugar (diabetes).
Drug Class
Antidiabetic
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 blood sugar levels in people with type 2 diabetes. It works by helping your body release more insulin from your pancreas right after you eat, which helps lower the rise in blood sugar that happens 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 the dose for that meal.
- Do not take Nateglinide if you are not going to eat a meal, as this can increase the risk of low blood sugar (hypoglycemia).
- Follow a healthy diet plan as 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 low blood sugar.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
120 mg orally three times daily, 1 to 30 minutes before each main meal
Dose Range:
60 - 120 mg
Condition-Specific Dosing:
initial_therapy:
60 mg orally three times daily, 1 to 30 minutes before each main meal, for patients with HbA1c near target (e.g., <8%) or who are prone to hypoglycemia.
combination_therapy:
Can be used in combination with metformin.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment necessary.
Moderate:
No dose adjustment necessary.
Severe:
Use with caution; monitor closely. No specific dose adjustment recommended, but consider starting at 60 mg TID.
Dialysis:
Use with caution; monitor closely. Not removed by dialysis. No specific dose adjustment recommended, but consider starting at 60 mg TID.
Hepatic Impairment:
Mild:
No dose adjustment necessary.
Moderate:
Use with caution; consider dose reduction (e.g., 60 mg TID) and close monitoring due to increased exposure.
Severe:
Contraindicated due to lack of studies and potential for increased exposure and hypoglycemia.
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.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 73%
Tmax:
Approximately 1 hour
FoodEffect:
Food delays the rate of absorption (Tmax is prolonged) but does not significantly affect the extent of absorption (AUC).
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:
Approximately 83% in urine (60-70% as metabolites, <10% as unchanged drug), 16% in feces.
Unchanged:
Less than 10% (urinary)
Pharmacodynamics
OnsetOfAction:
Rapid (within 20 minutes)
PeakEffect:
Within 1 hour
DurationOfAction:
Short (approximately 4 hours)
Confidence:
High
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
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 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
Low blood sugar (hypoglycemia), which may be more likely when taking this medication with other diabetes drugs. Symptoms may include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
If you experience any of these symptoms, call 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 are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
* Signs of a common cold
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.
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 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
Low blood sugar (hypoglycemia), which may be more likely when taking this medication with other diabetes drugs. Symptoms may include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
If you experience any of these symptoms, call 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 are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
* Signs of a common cold
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.
Seek Immediate Medical Attention If You Experience:
- Symptoms of low blood sugar (hypoglycemia): sweating, shakiness, dizziness, confusion, hunger, irritability, headache, blurred vision, rapid heartbeat, anxiety. If these occur, check blood sugar and treat immediately.
- Symptoms of high blood sugar (hyperglycemia): increased thirst, increased urination, dry mouth, fruity breath odor, fatigue, blurred vision. Report these to your doctor.
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.
Certain health conditions, including:
+ Acidic blood problems
+ Type 1 diabetes
* If you are breastfeeding. Note that 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 allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Acidic blood problems
+ Type 1 diabetes
* If you are breastfeeding. Note that 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. It is crucial to discuss this risk with your doctor. If you experience low blood sugar, do not drive, as it can significantly increase your risk of being involved in an accident. Monitor your blood sugar levels as instructed by your doctor.
Regular blood tests are necessary to ensure safe treatment. Adhere to the schedule recommended by your doctor and discuss any concerns or questions with them. Additionally, consult your doctor before consuming alcohol.
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, inform your doctor. It is necessary to discuss the potential benefits and risks associated with using this medication during pregnancy to make an informed decision.
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. It is crucial to discuss this risk with your doctor. If you experience low blood sugar, do not drive, as it can significantly increase your risk of being involved in an accident. Monitor your blood sugar levels as instructed by your doctor.
Regular blood tests are necessary to ensure safe treatment. Adhere to the schedule recommended by your doctor and discuss any concerns or questions with them. Additionally, consult your doctor before consuming alcohol.
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, inform your doctor. It is necessary to discuss the potential benefits and risks associated with using this medication during pregnancy to make an informed decision.
Overdose Information
Overdose Symptoms:
- Severe hypoglycemia (extremely low blood sugar)
- Loss of consciousness
- Seizures
What to Do:
Immediately consume a source of fast-acting sugar. For severe hypoglycemia or loss of consciousness, seek emergency medical attention. Glucagon injection may be necessary. Call 911 or 1-800-222-1222 (Poison Control).
Drug Interactions
Major Interactions
- Gemfibrozil (significant increase in nateglinide AUC and Cmax, leading to increased risk of hypoglycemia)
- Other antidiabetic agents (increased risk of hypoglycemia)
Moderate Interactions
- Beta-blockers (may mask symptoms of hypoglycemia)
- Nonsteroidal anti-inflammatory drugs (NSAIDs) (may enhance hypoglycemic effect)
- Salicylates (may enhance hypoglycemic effect)
- Monoamine oxidase inhibitors (MAOIs) (may enhance hypoglycemic effect)
- Sulfonamides (may enhance hypoglycemic effect)
- Corticosteroids (may decrease hypoglycemic effect)
- Thiazide diuretics (may decrease hypoglycemic effect)
- Sympathomimetics (may decrease hypoglycemic effect)
- Thyroid hormones (may decrease hypoglycemic effect)
- Oral contraceptives (may decrease hypoglycemic effect)
- Calcium channel blockers (may decrease hypoglycemic effect)
- Isoniazid (may decrease hypoglycemic effect)
- Rifampin (may decrease nateglinide exposure)
- Phenytoin (may decrease nateglinide exposure)
Monitoring
Baseline Monitoring
HbA1c (Glycated Hemoglobin)
Rationale: To assess long-term glycemic control and establish baseline for treatment efficacy.
Timing: Prior to initiation of therapy.
Fasting Plasma Glucose (FPG)
Rationale: To assess baseline glucose levels.
Timing: Prior to initiation of therapy.
Renal Function (e.g., eGFR, creatinine)
Rationale: To assess kidney function, especially important for drug elimination and to identify patients requiring caution.
Timing: Prior to initiation of therapy.
Hepatic Function (e.g., ALT, AST)
Rationale: To assess liver function, as nateglinide is metabolized hepatically and severe impairment is a contraindication.
Timing: Prior to initiation of therapy.
Routine Monitoring
HbA1c (Glycated Hemoglobin)
Frequency: Every 3-6 months
Target: Individualized, typically <7% for most adults
Action Threshold: If HbA1c remains above target despite optimal dosing, consider dose adjustment or addition/change of therapy.
Fasting Plasma Glucose (FPG)
Frequency: Periodically, or as needed based on patient's control
Target: 80-130 mg/dL (ADA guidelines)
Action Threshold: Persistent FPG outside target range may indicate need for dose adjustment or therapy change.
Postprandial Plasma Glucose (PPG)
Frequency: Periodically, or as needed based on patient's control
Target: <180 mg/dL (1-2 hours after meal, ADA guidelines)
Action Threshold: Persistent PPG outside target range may indicate need for dose adjustment or therapy change, as nateglinide primarily targets postprandial glucose.
Signs and Symptoms of Hypoglycemia
Frequency: Daily, patient self-monitoring
Target: N/A
Action Threshold: If symptoms occur, confirm with blood glucose measurement and treat immediately. Educate patient on recognition and management.
Symptom Monitoring
- Symptoms of hypoglycemia: sweating, tremor, dizziness, confusion, hunger, irritability, headache, blurred vision, rapid heartbeat, anxiety.
Special Patient Groups
Pregnancy
Nateglinide is Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Animal studies have shown adverse effects. Generally, insulin is the preferred treatment for glycemic control in pregnant women with diabetes.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity, though human data are limited.
Second Trimester:
Risk of fetal macrosomia and other complications if glycemic control is poor.
Third Trimester:
Risk of fetal macrosomia and other complications if glycemic control is poor.
Lactation
Nateglinide is excreted in the milk of lactating rats. It is unknown whether nateglinide is excreted in human milk. Due to the potential for hypoglycemia in the infant, 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. Lactation risk is L3 (Moderately Safe).
Infant Risk:
Potential for hypoglycemia in the breastfed infant. Monitor infant for signs of hypoglycemia.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Not recommended for use in children.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly 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 short-acting insulin secretagogue, ideal for patients with prominent postprandial hyperglycemia and relatively well-controlled fasting glucose.
- It should be taken immediately before meals (1-30 minutes prior) to match its rapid onset of action with the mealtime glucose surge.
- If a meal is skipped, the dose for that meal should also be skipped to avoid hypoglycemia.
- Less likely to cause weight gain compared to sulfonylureas.
- Lower risk of hypoglycemia compared to sulfonylureas, especially if taken correctly with meals.
- Consider starting with 60 mg TID for patients with HbA1c close to target or those prone to hypoglycemia.
- Not recommended as monotherapy for patients with very high HbA1c (e.g., >9%) as it may not provide sufficient glycemic control.
Alternative Therapies
- Repaglinide (another meglitinide)
- Sulfonylureas (e.g., Glipizide, Glyburide, Glimepiride)
- DPP-4 inhibitors (e.g., Sitagliptin, Saxagliptin)
- GLP-1 receptor agonists (e.g., Liraglutide, Semaglutide)
- SGLT2 inhibitors (e.g., Canagliflozin, Dapagliflozin)
- Thiazolidinediones (e.g., Pioglitazone, Rosiglitazone)
- Insulin therapy
Cost & Coverage
Average Cost:
Check current pricing (varies) per 30 tablets
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 is essential to contact your doctor promptly. 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 detailed information about the overdose, including the medication taken, the amount, and the time it occurred.