Pharm
Nateglinide
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Nateglinide
, Starlix
See Also
Meglitinide
Repaglinide
Second Generation Sulfonylurea
Type II Diabetes Medications
Indications
Early
Type II Diabetes Mellitus
Oral Agent
Elevated postprandial
Glucose
Consider if only used intermittently for pre-meal
Hyperglycemia
Contraindications
Sulfa
Hypersensitivity
Chronic Kidney Disease
Stage 5 (eGFR <15 ml/min)
Mechanism
Insulin
secretogogue
Benzoic acid derived from
Sulfonylurea
s
Directly stimulates pancreatic beta cells (Similar to
Sulfonylurea
s)
Binds different sites from
Sulfonylurea
s (
Sulfonylurea
Receptors 1, 1A and 1B)
Closes ATP sensitive K+ channels
Results in
Insulin
secretion
Effects
Predominately effects postprandial
Glucose
Faster oral absorption and onset than
Sulfonylurea
s
Shorter duration of binding and shorter effect than
Sulfonylurea
s
Medications
Nateglinide (Starlix): 60 mg, 120 mg
Dosing
Gene
ral
Take only before meals, especially before the largest meal (and skip if
Fastin
g)
Adults (not FDA approved in children)
Take 60 to 120 mg orally before meals, from 1 to 3 times daily
Typical dosing is 120 mg
However, may use 60 mg dose if patient near glycemic control goals
Pharmacokinetics
Renal excretion
Hepatic metabolism (
CYP3A4
,
CYP2C9
)
Adverse Effects
Hypoglycemia
(lower risk than
Sulfonylurea
s)
Safety
Pregnancy Category C
Unknown safety in
Lactation
Efficacy
Lowers
HBA1C
by 0.5 to 1%
Of the
Meglitinide
s, Nateglinide is significantly weaker than
Repaglinide
(
Prandin
)
Advantages in comparison to
Sulfonylurea
s
Low risk of
Hypoglycemia
(2.4%) than
Sulfonylurea
s
Effect depends on
Ambien
t
Blood Glucose
levels
No significant gastrointestinal side effects
Minimal weight gain
No lab monitoring required
No significant
Drug Interaction
s
No
Lactic Acidosis
No adjustments needed (other than per meal)
No adjustment in
Congestive Heart Failure
No adjustment for age
No adjustment in
Renal Insufficiency
Disadvantages in comparison to
Sulfonylurea
s
Two to three times as expensive as
Sulfonylurea
s
Resources
Nateglinide (DailyMed)
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=88698921-cd8f-4d41-96e6-ff671913c5c3
References
Luna (2001) Am Fam Physician 63(9):1747-56 [PubMed]
Luna (1999) Prim Care 26:895-915 [PubMed]
Vaughan (2024) Am Fam Physician 109(4): 333-42 [PubMed]
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