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Repaglinide;Uses, Dosage, Side Effects, Drug Interactions

Repaglinide is a nonsulfonylurea insulin secretagogue belonging to the melgitinide class with hypoglycemic activity. Repaglinide is rapidly absorbed and has a rapid onset and short duration of action. This agent is metabolized in the liver by CYP2C8 and CYP3A4 and its metabolites are excreted in the bile. Repaglinide has a half-life of one hour.

Repaglinide is a benzoic acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Repaglinide has been linked to rare instances of clinically apparent acute liver injury.

Repaglinide 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. Repaglinide 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 Repaglinide

Repaglinide activity is dependent on the presence of functioning β cells and glucose. In contrast to sulfonylurea insulin secretagogues, repaglinide 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, repaglinide 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 repaglinide 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). Repaglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.

Indications of Repaglinide

Type 2 Diabetes Mellitus
Repaglinide is an oral medication used in addition to diet and exercise for blood sugar control in type 2 diabetes mellitus
As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Repaglinide is indicated in adults with type 2 diabetes mellitus whose hyperglycemia can no longer be controlled satisfactorily by diet, weight reduction and exercise. Repaglinide is also indicated in combination with metformin in adults with type 2 diabetes mellitus who are not satisfactorily controlled on metformin alone.
Treatment should be initiated as an adjunct to diet and exercise to lower the blood glucose in relation to meals.
Repaglinide is indicated in adults with type 2 diabetes mellitus whose hyperglycemia can no longer be controlled satisfactorily by diet, weight reduction and exercise. Repaglinide is also indicated in combination with metformin in adults with type 2 diabetes mellitus who are not satisfactorily controlled on metformin alone.
Treatment should be initiated as an adjunct to diet and exercise to lower the blood glucose in relation to meals.
Repaglinide is indicated in adults with type 2 diabetes mellitus whose hyperglycemia can no longer be controlled satisfactorily by diet, weight reduction and exercise.
Repaglinide is also indicated in combination with metformin in adults with type 2 diabetes mellitus who are not satisfactorily controlled on metformin alone.
Treatment should be initiated as an adjunct to diet and exercise to lower the blood glucose in relation to meals.
Repaglinide is indicated in patients with type 2 diabetes (Non-Insulin-Dependent Diabetes Mellitus (NIDDM)) whose hyperglycemia can no longer be controlled satisfactorily by diet, weight reduction and exercise. Repaglinide is also indicated in combination with metformin in type 2 diabetes patients who are not satisfactorily controlled on metformin alone.
Treatment should be initiated as an adjunct to diet and exercise to lower the blood glucose in relation to meals.
Repaglinide is a short-acting oral secretagogue. It is indicated for adults with type 2 diabetes mellitus whose hyperglycemia can no longer be controlled satisfactorily by diet, weight reduction and exercise. Repaglinide is also indicated in combination with metformin in adults with type 2 diabetes mellitus who are not satisfactorily controlled on metformin alone. Treatment should be initiated as an adjunct to diet and exercise to lower the blood glucose in relation to meals.

Contra-Indications of Repaglinide

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

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Dosage of Repaglinide

Strengths: 0.5 mg; 1 mg; 2 mg

Diabetes Type 2

Individualize therapy:

Dose preprandially 2, 3, or 4 times a day

For patients not previously treated with antidiabetic agents or whose glycosylated hemoglobin (HbA1c) is less than 8%

Initial dose: 0.5 mg orally with each meal

For patients previously treated with antidiabetic agents or whose HbA1c is 8% or higher

Initial dose: 1 or 2 mg orally with each meal

Dose Adjustments

Based upon blood glucose response, double the preprandial dose up to a maximum mealtime dose of 4 mg until a satisfactory glycemic response is achieved; allow at least 1 week to assess response after each dose adjustment.
Recommended Dose Range: 0.5 to 4 mg orally with each meal
Maximum Daily Dose: 16 mg per day

Side Effects of Repaglinide

Most common

Abdominal or stomach discomfort
increased urination.
low blood pressure,
difficult, burning, or painful urination
discharge with a strong odor from the penis
increased potassium blood levels (hyperkalemia),
low blood sugar (hypoglycemia), and
diarrhea
gas (flatulence)
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

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Drug Interactions of Repaglinide

Repaglinide may interact with following drugs, supplements & may decrease the efficacy of the drug

angiotensin-converting enzyme inhibitors (ACEIs; captopril, ramipril)
angiotensin receptor blockers (ARBs; e.g., candesartan, irbesartan, losartan)
angiotensin-converting enzyme inhibitors (ACEIs; captopril, enalapril, ramipril)
antipsychotic medications (e.g., chlorpromazine, haloperidol, olanzapine,
birth control pills
bupropion
atypical antipsychotics (e.g., aripiprazole, clozapine, olanzapine; quetiapine, risperidone)
“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
barbiturates (e.g., pentobarbital, phenobarbital)
crizotinib
cyclosporine
lanreotide
levodopa
mifepristone
corticosteroids (e.g., dexamethasone, prednisone)
diabetic drugs (e.g., glyburide, insulin, repaglinide, sitagliptin)
digoxin
diuretics (e.g., furosemide, hydrochlorothiazide)
HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
iodinated contrast material
phenytoin
quinolone antibiotics (e.g., levofloxacin, moxifloxacin)
selective serotonin reuptake inhibitors (SSRIs; citalopram, fluoxetine, sertraline paroxetine,
trimethoprim
sulfonamide antibiotics (“sulfas”; e.g., sulfisoxazole, sulfamethoxazole)
tacrolimus
teriflunomide
vorinostat
verapamil
sulfonamides (e.g., sulfamethoxazole)
tacrolimus
tamoxifen
testosterone
trimethoprim

Pregnancy & Lactation of Repaglinide

FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Lactations

It is not known whether repaglinide 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.