Gemfibrozil
Contraindicated
Database
CYP2C8 inhibition → massive repaglinide rise, severe hypoglycaemia
Absolute contraindication — do not co-administer
Source: Kimi deep-research + Cla
Drug reference
Repaglinide
Meglitinide (non-sulfonylurea insulin secretagogue) · Antidiabetic
START
Confirm type 2 diabetes. Verify not type 1 or DKA. Counsel on taking WITH meals (within 30 min before eating) and SKIPPING dose if meal skipped. Baseline LFTs.
TYPICAL MAX
4mg per meal (16mg/day). Hypoglycemia is dose-limiting. In elderly, start 0.5mg and titrate slowly.
STOP IF
Severe or recurrent hypoglycemia, hepatotoxicity (LFTs >3x ULN), severe hypersensitivity, pregnancy.
WATCH
Blood glucose monitoring before meals. HbA1c every 3 months. Hypoglycemia risk increases with missed/delayed meals, alcohol, exercise, renal impairment, and hepatic impairment. Weight gain (~2-3kg) is common. Flexible dosing allows patients to skip doses when meals are skipped—advantage over sulfonylureas.
CDSCO approvedSchedule HATC A10BX02
KDIGO 2024 + manufacturer label
- ONSET
- 30min · Insulin secretion within 30 min
- PEAK
- 45min · Tmax 0.5-1 hour
- t½
- 1h · t½ ~1 hour
- DURATION
- 5h · 4-6 hours (prandial)
EXCRETION
Fecal as metabolites (~90%)
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Not recommended in pregnancy—insulin is preferred for glycemic control. Animal data show no teratogenicity at therapeutic doses.
FDA category + note
Top interactionssee all 12 →
- GemfibrozilContraindicatedDatabaseKimi deep-research + Cla
- CinoxacinSevereDatabaseDDInter
- CiprofloxacinSevereDatabaseDDInter
- ClopidogrelSevereDatabaseDDInter
Available in India
65 branded formulations. Look up specific brands in the Drugs workspace.
Mechanism
Blocks ATP-sensitive potassium (KATP) channels on pancreatic beta-cell membranes, causing membrane depolarization, calcium influx, and insulin secretion. Rapid onset and short duration—stimulates prandial insulin secretion. Closes KATP channels at a different binding site than sulfonylureas.
Indications
Type 2 diabetes mellitus (prandial glucose lowering)Combination with metformin when monotherapy inadequate
Dosing
- Adult
- 0.5-4mg PO taken 0-30 minutes before each meal (TID). Start 0.5-1mg before meals if HbA1c <8%; start 1-2mg if HbA1c ≥8%. Titrate by 1mg per meal every 1-2 weeks. Max 4mg per meal (16mg/day). Skip dose if meal skipped.
- Pediatric
- Not established in children.
- Renal adjustment
- No adjustment needed (hepatically metabolized); preferred over sulfonylureas in renal impairment.
- Hepatic adjustment
- Mild-moderate: use caution; start at 0.5mg. Severe: contraindicated.
- Geriatric
- Start 0.5mg before meals; increased hypoglycemia risk; monitor glucose closely.
- Max dose
- 4mg per meal; 16mg/day
Pharmacokinetics
Onset
Rapid; insulin secretion within 30 minutes
Peak effect
Tmax 0.5-1 hour; peak insulin at 1 hour; peak glucose lowering at 1-2 hours
Duration
4-6 hours (short-acting; covers prandial glucose only)
Half-life
~1 hour (very short; enables flexible meal timing)
Bioavailability
~56%
Protein binding
>98% (albumin)
Metabolism
Extensive hepatic via CYP2C8 (major) and CYP3A4 to inactive metabolites
Excretion
~90% fecal (metabolites); ~8% renal (metabolites); <1% unchanged in urine
Contraindications
- Type 1 diabetes mellitus
- Diabetic ketoacidosis
- Severe hepatic impairment
- Hypersensitivity to repaglinide
- Concomitant gemfibrozil (markedly increases repaglinide levels)
Side effects
Common
Hypoglycemia (most common—dose and meal-timing dependent)Upper respiratory infectionHeadacheNauseaDiarrheaBack painArthralgia
Serious
- Severe hypoglycemia (can cause seizures, coma, death)
- Hepatotoxicity (elevated LFTs)
- Severe hypersensitivity
- Cardiovascular events (controversial—meglitinides may have less CV benefit than other agents)
- Pancreatitis (rare)
Pregnancy & lactation
Pregnancy
Not recommended in pregnancy—insulin is preferred for glycemic control. Animal data show no teratogenicity at therapeutic doses.
Lactation
Excretion in breast milk unknown; not recommended during breastfeeding.
Drug interactions
Cinoxacin
Severe
Database
Drug interaction classified as: antagonism
Source: DDInter
Ciprofloxacin
Severe
Database
Drug interaction classified as: antagonism.
Source: DDInter
Clopidogrel
Severe
Database
Drug interactions with repaglinide, potentially increasing its concentration and effect.
Monitor for altered effects of repaglinide if coadministration is necessary.
Source: DDInter
Cyclosporine
Severe
Database
Potentiation of repaglinide's action, increasing risk of hypoglycemia.
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
Gemifloxacin
Severe
Database
Clinical effect not specified
Source: DDInter
Grepafloxacin
Severe
Database
Clinical effect not specified
Source: DDInter
Levofloxacin
Severe
Database
.
Source: DDInter
Lomefloxacin
Severe
Database
Clinical effect not specified
Source: DDInter
Related guidelines
Ask House about Repaglinide
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