Nateglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to β cells of the pancreas to stimulate insulin release. Nateglinide is an amino acid derivative that induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal.
Mechanism of Action of Nateglinide
Nateglinide activity is dependent on the presence of functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, nateglinide has no effect on insulin release in the absence of glucose. Rather, it potentiates the effect of extracellular glucose on ATP-sensitive potassium channel and has little effect on insulin levels between meals and overnight. As such, nateglinide is more effective at reducing postprandial blood glucose levels than fasting blood glucose levels and requires a longer duration of therapy (approximately one month) before decreases in fasting blood glucose are observed. The insulinotropic effects of nateglinide are highest at intermediate glucose levels (3 to 10 mmol/L) and it does not increase insulin release already stimulated by high glucose concentrations (greater than 15 mmol/L). Nateglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.
Indications of Nateglinide
- Type 2 Diabetes Mellitus
- Treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
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For the treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
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Combination therapy with metformin in type 2 diabetic patients inadequately controlled despite a maximally tolerated dose of metformin alone.
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Combination therapy with metformin in type 2 diabetic patients inadequately controlled despite a maximally tolerated dose of metformin alone
Contra-Indications of Nateglinide
- Low blood sugar
- Pituitary hormone deficiency
- Decreased function of the adrenal gland
- Inadequate vitamin B12
- Excess body acid
- Extreme loss of body water
- The habit of drinking too much alcohol
- Alcohol intoxication
- Heart attack
- Suddenly serious symptoms of heart failure
- Liver problems
- Recent operation
- Fever
- Shock
- Severe vomiting
- Severe diarrhea
- Serious lack of oxygen in the blood
- Weakened patient
- Injury
- Sepsis syndrome
- X-Ray Study with intravenous iodine contrast agent
- Kidney disease with a likely reduction in kidney function
- Acute inflammation of the pancreas
- Chronic inflammation of the pancreas
- Moderate to Severe kidney impairment.
Dosage of Nateglinide
Strengths: 60 mg; 120 mg
Diabetes Type 2
- Initial dose: 120 mg orally 3 times a day before meals
- Maintenance dose: 60 to 120 mg orally 3 times a day before meals
Side Effects of Nateglinide
Most common
- Abdominal or stomach discomfort
- increased urination.
- low blood pressure,
- difficult, burning, or painful urination
- increased potassium blood levels (hyperkalemia),
- low blood sugar (hypoglycemia), and
- diarrhea
- Cough
- runny or stuffy nose
- sore throat
- symptoms of weakness, muscle pain (myalgia)
- upper respiratory tract infection
- low blood sugar (hypoglycemia)
- abdominal pain (GI complaints), lactic acidosis (rare)
- low blood levels of vitamin B-12
- nausea,vomiting
- chest discomfort
- chills, dizziness
- bloating/abdominal distention
- constipation
- heartburn
More common
- Abdominal or stomach discomfort
- a cough or hoarseness
- decreased appetite
- diarrhea
- fast or shallow breathing
- fever or chills
- the general feeling of discomfort
- lower back or side pain
- muscle pain or cramping
- painful or difficult urination
Less common
- Abnormal stools
- bad, unusual, or unpleasant (after) taste
- change in taste
- difficulty with moving
- discoloration of the fingernails or toenails
- flu-like symptoms
- joint pain
- rash
- a runny nose
- sneezing
- stuffy nose
- swollen joints
Drug Interactions of Nateglinide
Canagliflozin may interact with following drugs, supplements & may decrease the efficacy of the drug
- androgens (e.g., methyltestosterone, nandrolone, testosterone)
- angiotensin-converting enzyme inhibitors (ACEIs; captopril, ramipril)
- angiotensin receptor blockers (ARBs; e.g., candesartan, irbesartan, losartan)
- antipsychotic medications (e.g., chlorpromazine, haloperidol, olanzapine,
- birth control pills
- bupropion
- atorvastatin
- atypical antipsychotics (e.g., aripiprazole, clozapine, olanzapine; quetiapine, risperidone)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- barbiturates (e.g., pentobarbital, phenobarbital)
- cyclosporine
- lanreotide
- levodopa
- mifepristone
- corticosteroids (e.g., dexamethasone, prednisone)
- diabetic drugs (e.g., glyburide, insulin, repaglinide, sitagliptin)
- diuretics (e.g., furosemide, hydrochlorothiazide)
- HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
- phenytoin
- quinolone antibiotics (e.g., levofloxacin, moxifloxacin)
- selective serotonin reuptake inhibitors (SSRIs; citalopram, fluoxetine, sertraline paroxetine,
- trimethoprim
- sulfonamide antibiotics (“sulfas”; e.g., sulfisoxazole, sulfamethoxazole)
Pregnancy & Lactation of Nateglinide
FDA Pregnancy Category C
Pregnancy
This medication should not be used during pregnancy. If you think you may be pregnant or if you become pregnant while taking this medication, contact your doctor immediately.
Lactation
It is not known if nateglinide passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.
References
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