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Nateglinide; Uses, Dosage, Side Effects, Interactions

Nateglinide is a phenylalanine derivative of the meglitinide class of agents with hypoglycemic activity. Nateglinide, compared to repaglinide, binds with a higher affinity to the SUR1 subunit and with a faster onset of action and a shorter duration of action. This agent is metabolized by the cytochrome P450 isoenzyme CYP2C9, and, to a lesser extent, by CYP3A4. The parent drug and metabolites are mainly excreted in the urine and its half-life is about 1.5 hours. Nateglinide is an oral hypoglycemic agent and amino acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Nateglinide has been linked to rare instances of clinically apparent acute liver injury.

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.

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Indications of Nateglinide

Type 2 Diabetes Mellitus
Treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
For the treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
Combination therapy with metformin in type 2 diabetic patients inadequately controlled despite a maximally tolerated dose of metformin alone.
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

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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.