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Nateglinide

Meglitinide (D-phenylalanine derivative) prandial insulin secretagogue · Antidiabetic

START
120 mg PO TID, 1–30 min before main meals (60 mg if near goal); omit if meal skipped
TYPICAL MAX
360 mg/day (120 mg pre-meal ×3)
STOP IF
Recurrent/severe hypoglycaemia, severe hepatic impairment, hypersensitivity
WATCH
Postprandial glucose/HbA1c, hypoglycaemia (meal-dose matching), hepatic enzymes; counsel skip-dose-if-skip-meal
CDSCO approvedSchedule HATC A10BX03
Dose laddermg/d
60start120titrate360max/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo specific adjustment; usual dosing15CAUTIONLimited data — u…90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
18minONSET1hPEAK1.5h4hDURATION
ONSET
18min · insulin-release onset
PEAK
1h · Cmax
1.5h · plasma t½
DURATION
4h · prandial effect
EXCRETION
Hepatic CYP2C9; ~83% renal metabolites
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Avoid — insulin preferred in pregnancy
FDA category + note
Top interactionssee all 12
  • CinoxacinSevereDatabaseDDInter
  • CiprofloxacinSevereDatabaseDDInter
  • DelafloxacinSevereDatabaseDDInter
  • EnoxacinSevereDatabaseDDInter
Available in India

10 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Rapid, short-acting closure of pancreatic beta-cell ATP-sensitive K+ channels → glucose-dependent prandial insulin release; faster on/off than sulfonylureas (targets postprandial glucose, lower interprandial hypoglycaemia).

Indications

Type 2 diabetes mellitus — postprandial glucose control (monotherapy or with metformin/TZD)

Dosing

Adult
120 mg PO three times daily, 1–30 minutes before main meals (60 mg if near HbA1c goal). Skip dose if a meal is skipped.
Pediatric
Not established.
Renal adjustment
No adjustment (active metabolites minor; caution in severe — limited data, accumulation of weak metabolites).
Hepatic adjustment
Mild–moderate: no adjustment. Severe: caution/avoid.
Geriatric
No specific adjustment; hypoglycaemia awareness.
Max dose
360 mg/day (120 mg before each of 3 meals)

Pharmacokinetics

Onset
~15–20 min
Peak effect
~1 h
Duration
~4 h (short — prandial)
Half-life
~1.5 h
Bioavailability
~73%
Protein binding
~98%
Metabolism
Hepatic CYP2C9 (major) and CYP3A4
Excretion
Renal (~83% metabolites) and faecal

Contraindications

  • Type 1 diabetes / diabetic ketoacidosis
  • Severe hepatic impairment
  • Hypersensitivity to nateglinide

Side effects

Common
Hypoglycaemia (less interprandial than sulfonylureas)Weight gain (modest)Upper respiratory symptomsDizziness
Serious
  • Severe hypoglycaemia (esp. with potentiating drugs/missed-meal mismatch)
  • Hypersensitivity reactions
  • Hepatic enzyme elevation (rare)

Pregnancy & lactation

Pregnancy

Avoid — insulin preferred in pregnancy

Lactation

Avoid (excreted in animal milk)

Drug interactions

Cinoxacin
Severe
Database

Drug interaction classified as: antagonism

Source: DDInter

Ciprofloxacin
Severe
Database

Drug interaction classified as: antagonism

Source: DDInter

Delafloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Enoxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Gatifloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Gemfibrozil
Severe
Database

CYP2C9 inhibition → raised nateglinide → hypoglycaemia (less marked than with repaglinide but caution)

Monitor glucose closely; consider alternative

Source: Kimi deep-research + Cla

Gemifloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Grepafloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Levofloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Lomefloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Moxifloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Nalidixic Acid
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Ask House about Nateglinide

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19