Meglitinides / Glinides (Short Acting Prandial Insulin Releasers)

Introduction :

• Non  sulphonylurea  moiety  of  Glibenclamide Contains Benzamido Group
• Used in Type 2 Diabetes
• Prandial Insulin Releasers
• Two Agents – Repaglinide  & Nateglinide Introduced in 1998 & 2001 respectively.

Mode Of Action:

• Bind To Benzamido site on sulphonylurea receptor SUR 1 in plasma membrane of islet B-cells.
• Closure of K+ATP channel
• Membrane  depolarization
• Opens  Voltage  dependent L-type calcium Channels
• Insulin release by exocitosis

Pharmacokinetics:

Repaglinide (0.5-4 mg) 

Max - 16 mg 

Peak – 1 hr

Duration of Action :  4-6 hr

Elimination in Bile(90%)

Nateglinide (60-180mg)

Max – 540 mg

Duration of Action : 3-5 hr

Elimination in Urine (80%)

Indications & Contraindications :

• Non pharmacological measure failed to control
• Those who exhibit post-Prandial hyperglycemia with near normal fasting glycemia( 15-30 Min before meals )
• Individuals with irregular lifestyles(missed meals)
• Elderly patients(less hypoglycemia)
• Where  other agents contraindicated ( Mod renal impairment with metformin & sulphonylurea  can not be used)
• Combination with metformin or thiazolidinediones.

Efficacy :

• Reduce post Prandial Hyperglycemia
• Small reduction in fasting hyperglycemia
• HbA1C  reduction – 0.5-1.5%

Adverse Effects :

• Hypoglycemia
• Sensitivity reactions
• Weight  gain when monotherapy

Common Brand Names:

Repaglinide :

Eurepa (0.5-1-2)

Novonorm (0.5-1-2)

Regan (0.5-1-2)

Nateglinide:

Glinate

Natiz

Natelide

Natstar