nateglinide

Action and Spectrum

Actions and Spectrum: 

Actions: 

• Stimulates insulin secretion: nateglinide works by binding to the ATP-sensitive potassium channels on the beta cells of the pancreas, leading to an increase in insulin secretion. 
• Rapid onset of action: nateglinide is rapidly absorbed and reaches peak plasma concentrations within 1 hour of administration. 
• Short duration of action: The effects of nateglinide typically last for 2-4 hours, making it useful for controlling postprandial (after-meal) blood sugar levels. 

Spectrum: 

• Monotherapy: nateglinide can be used as a monotherapy in people with type 2 diabetes who are unable to control their blood sugar levels through diet and exercise alone. 
• Combination therapy: nateglinide can also be used in combination with other medications for diabetes management, such as metformin or thiazolidinediones. 
• Limited efficacy: While nateglinide can be effective in controlling postprandial blood sugar levels, it may not be as effective in reducing fasting blood sugar levels or HbA1c levels (a measure of average blood sugar levels over the past 2-3 months) compared to other medications such as metformin or sulfonylureas. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Increased uric acid 

Dizziness 

Weight gain 

Hypoglycemia 

Arthropathy 

Flu-like syndrome 

Frequency not defined 

Nausea 

Diarrhea 

Black Box Warning

There is no blackbox warning for this drug 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity: nateglinide should not be used in people who have a known hypersensitivity to the drug or its components. 
• Type 1 diabetes: nateglinide is not recommended for people with type 1 diabetes. 
• Diabetic ketoacidosis: nateglinide should not be used in people with diabetic ketoacidosis (a serious complication of diabetes characterized by high levels of ketones in the blood). 

Cautions: 

• Liver impairment: nateglinide is metabolized in the liver, so it should be used with caution in people with liver impairment. 
• Renal impairment: nateglinide is primarily excreted in the urine, so it should be used with caution in people with renal impairment. 
• Pregnancy and breastfeeding: The safety of nateglinide in pregnancy and breastfeeding has not been established, so it should be used with caution in these populations. 
• Hypoglycemia: Like all medications used to treat diabetes, nateglinide can cause hypoglycemia (low blood sugar), particularly when used in combination with other medications. People taking nateglinide should be advised on how to recognize and treat hypoglycemia. 
• Drug interactions: nateglinide can interact with certain medications, such as gemfibrozil and rifampin, so it is important to inform your healthcare provider of all medications you are taking. 

Pregnancy / Lactation

Pregnancy consideration:  

Category B 

Breastfeeding warnings:  

No data is available about the excretion of nateglinide in breastmilk. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

nateglinide is an oral medication used to control blood sugar levels in people with type 2 diabetes. It belongs to a class of drugs called meglitinides, which work by stimulating the pancreas to release insulin in response to a meal. 

nateglinide works by binding to ATP-sensitive potassium channels on the beta cells of the pancreas. This binding leads to the closure of these channels, which results in the depolarization of the cell membrane and the subsequent opening of voltage-gated calcium channels. This influx of calcium causes the release of insulin from the beta cells. 

nateglinide has a rapid onset of action, with peak levels reached within one hour of administration. Its effects are short-lived, with the drug being metabolized and eliminated within four hours. As a result, nateglinide is typically taken before meals to help control postprandial glucose levels. 

nateglinide is generally well-tolerated, with the most common side effects being hypoglycemia (low blood sugar), headache, and upper respiratory tract infections. It should not be used in people with type 1 diabetes or diabetic ketoacidosis, and caution should be exercised in people with liver or kidney disease. 

Pharmacodynamics: 

The pharmacodynamics of nateglinide is related to its mechanism of action in the body. nateglinide belongs to the class of drugs called meglitinides, which stimulate the release of insulin from the pancreas in response to a meal. 

When nateglinide is taken orally, it is rapidly absorbed from the gastrointestinal tract and reaches peak blood concentrations within 1 hour. nateglinide binds to ATP-sensitive potassium channels on the beta cells of the pancreas, which leads to the depolarization of the cell membrane and the subsequent opening of voltage-gated calcium channels. This influx of calcium causes the release of insulin from the beta cells. 

The insulin released by nateglinide is in response to a meal, and its effects are short-lived, typically lasting for about 4 hours. This makes nateglinide particularly useful in controlling postprandial (after-meal) blood sugar levels in people with type 2 diabetes. 

nateglinide has been shown to improve glycemic control in people with type 2 diabetes, as measured by reductions in hemoglobin A1c (HbA1c), fasting plasma glucose, and postprandial glucose levels. The drug has also been shown to reduce the risk of cardiovascular events in people with diabetes, although the mechanisms underlying this effect are not fully understood. 

Pharmacokinetics: 

The pharmacokinetics of nateglinide describe the way the drug is absorbed, distributed, metabolized, and eliminated from the body. 

Absorption 

nateglinide is rapidly absorbed from the gastrointestinal tract after oral administration, with peak plasma concentrations achieved within 1 hour of dosing. Food does not significantly affect the absorption of nateglinide. 

Distribution 

nateglinide is extensively distributed throughout the body, with a volume of distribution of approximately 10 L/kg. The drug is highly bound to plasma proteins, primarily to albumin. 

Metabolism 

nateglinide is extensively metabolized in the liver by CYP2C9 and CYP3A4 enzymes to form metabolites that are inactive or have minimal activity. The metabolites are then excreted in the urine or feces. 

Elimination and Excretion 

nateglinide has a relatively short half-life of about 1-2 hours, and the drug and its metabolites are primarily eliminated by the kidneys. Approximately 83% of the administered dose is excreted in the urine, and the remainder is excreted in the feces. 

Special Populations: In people with renal or hepatic impairment, the pharmacokinetics of nateglinide may be altered, and dosage adjustments may be necessary. 

Adminstartion

Administration: 

nateglinide is an oral medication that is typically taken just before meals to help control postprandial (after-meal) blood sugar levels in people with type 2 diabetes. 

The recommended starting dose of nateglinide is usually 120 mg taken orally three times daily, 1 to 30 minutes before meals. The maximum recommended daily dose of nateglinide is 360 mg. 

nateglinide should be taken with meals to help prevent hypoglycemia (low blood sugar) and to maximize its glucose-lowering effect. If a meal is skipped, the corresponding dose of nateglinide should also be skipped to avoid hypoglycemia. 

nateglinide should be stored at room temperature, protected from light and moisture, and kept out of reach of children. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: nateglinide 

Pronounced: Na-te-GLYE-nide 

Why do we use nateglinide? 

nateglinide is used to control blood sugar levels in people with type 2 diabetes. It is particularly effective in controlling postprandial (after-meal) blood sugar levels. When a person with type 2 diabetes eats a meal, their body may not produce enough insulin or use insulin effectively to lower their blood sugar levels. nateglinide helps to stimulate the release of insulin from the pancreas in response to a meal, which helps to lower blood sugar levels. 

nateglinide is particularly useful for people with type 2 diabetes who experience significant increases in blood sugar levels after meals, as it can help to prevent postprandial hyperglycemia (high blood sugar). The short duration of action of nateglinide means that it does not cause a prolonged lowering of blood sugar levels, which can increase the risk of hypoglycemia (low blood sugar).