Formulary
Repaglinide: Indications, Dosing, Side Effects and Interactions
Repaglinide stimulates insulin secretion.
MedNext Academy | 3 min read
Repaglinide: Indications, Dosing, Side Effects and Interactions
Repaglinide stimulates insulin secretion.
Drug action
Repaglinide stimulates insulin secretion.
Indications and dose
**Type 2 diabetes mellitus (as monotherapy or in combination with metformin when metformin alone inadequate)**
- **Adult** (By Mouth): Initially 500 micrograms (max. per dose 4 mg), adjusted according to response, dose to be taken within 30 minutes before main meals and adjusted at intervals of 1-2 weeks; maximum 16 mg per day.
**Type 2 diabetes mellitus (as monotherapy or in combination with metformin when metformin alone inadequate), if transferring from another oral antidiabetic drug**
- **Adult** (By Mouth): Initially 1 mg (max. per dose 4 mg), adjusted according to response, dose to be taken within 30 minutes before main meals and adjusted at intervals of 1-2 weeks; maximum 16 mg per day.
Cautions
Debilitated patients; elderly (no information available); malnourished patients Cautions, further information Manufacturer advises patients exposed to stress (including fever, trauma, infection or surgery) may require treatment interruption and temporary replacement with insulin to maintain glycaemic control.
Contraindications
Ketoacidosis
Side effects
Common or very common Abdominal pain; diarrhoea; hypoglycaemia Rare or very rare Cardiovascular disease; constipation; hepatic function abnormal; vasculitis; vision disorders; vomiting Frequency not known Acute coronary syndrome; hypoglycaemic coma; nausea; skin reactions
Interactions
**Severe interactions:**
- Co-administration of trimethoprim (160 mg twice daily), a moderate CYP2C8 inhibitor, and repaglinide (a single dose of 0.25 mg) increased the repaglinide AUC, Cmax and t (1.6-fold, 1.4-fold and...
- No significant effect on the glucose level in healthy volunteers was observed.
- A small, significant decrease in blood glucose values was observed.
- Co-administration of cimetidine, nifedipine, oestrogen, or simvastatin with repaglinide, all CYP3A4 substrates, did not significantly alter the pharmacokinetic parameters of repaglinide.
**Other interactions (33):**
- A number of medicinal products are known to influence repaglinide metabolism.
- Possible interactions should therefore be taken into account by the physician: In vitro data indicate that repaglinide is metabolised predominantly by CYP2C8, but also by CYP3A4.Clinical data in...
- Consequently metabolism, and by that clearance of repaglinide, may be altered by drugs which influence these cytochrome P-450 enzymes via inhibition or induction.
- Special care should be taken when both inhibitors of CYP2C8 and 3A4 are coadministered simultaneously with repaglinide.
- Based on in vitro data, repaglinide appears to be a substrate for active hepatic uptake (organic anion transporting protein OATP1B1).
- Substances that inhibit OATP1B1 may likewise have the potential to increase plasma concentrations of repaglinide, as has been shown for ciclosporin (see below).
Pregnancy
Avoid.
Breast feeding
Avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises avoid in severe impairment (risk of increased exposure).
Renal impairment
Use with caution. M
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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