Drug Interaction Report

Repaglinide and Cyclosporine Injection: Interaction Details

A pharmacist-reviewed analysis of the Repaglinide and Cyclosporine Injection interaction: the documented clinical effects, severity rating, onset, mechanism, and management considerations, with cited references throughout.

AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature

Repaglinide

Prandin®
+

Cyclosporine Injection

Atopica Cequa Cyclavance Gengraf Modulis Neoral Optimmune Restasis
Dr. Brian Staiger, PharmD, BCPS
Medically reviewed by
Dr. Brian Staiger, PharmD, BCPS
Updated Aug 8, 2026
Editorial policy · Data sources
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Interaction severity
Moderate
Can be significant — usually manageable with monitoring.
How we grade severity & evidence

Severity levels

  • Contraindicated: These should generally not be used together.
  • Major: Potentially serious — often needs a change or close monitoring.
  • Moderate: Can be significant — usually manageable with monitoring.
  • Minor: Usually limited clinical impact.

Evidence grades

  • Established: Well documented — supported by controlled studies or strong clinical data.
  • Probable: Good supporting evidence, though not definitively proven.
  • Suspected: Some evidence suggests this interaction, but it is not well established.
  • Possible: Limited or conflicting evidence; the interaction may occur.
  • Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.

Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.

Of 65 documented Repaglinide interactions, 35 are rated moderate — including this one.
Onset
rapid
Evidence
established
Severity
Moderate

What happens

Increased repaglinide plasma concentrations

Interaction Deep Dive

In a randomized crossover study of 12 healthy volunteers, concurrent administration of repaglinide and cycloSPORINE significantly increased repaglinide exposure. However, no patient experienced symptomatic hypoglycemia2. If coadministration is necessary, limit repaglinide dose to no more than 6 mg/day and monitor blood glucose more frequently 1.

Why it happens (mechanism)

Inhibition of CYP3A4-mediated metabolism and OATP1B1-mediated hepatic uptake of repaglinide

Literature reports

1 report — tap to read

a) In a randomized crossover study, concurrent administration of cycloSPORINE and repaglinide resulted in significant elevations in repaglinide plasma concentrations. Healthy volunteers (N=12) were given either 100 mg oral cycloSPORINE or placebo at 8 p.m. on day 1 and at 8 a.m. on day 2. An hour after the second dose, a single oral dose of repaglinide 0.25 mg was administered. After 12 hours, Cmax and AUC of repaglinide were increased to 175% and 244% of the control values in the placebo phase, respectively. Tmax and t1/2 of repaglinide were not significantly affected. While one subject who had the greatest (5-fold) increase in repaglinide AUC also had the greatest increment of hypoglycemic effect, none of the subjects had symptomatic hypoglycemia. This was attributed to the low dosage of repaglinide and frequent food intake following repaglinide administration 2.

Common questions

Can I take Repaglinide and Cyclosporine Injection together?

Increased repaglinide plasma concentrations Always confirm with your pharmacist or prescriber before making any change.

How serious is the Repaglinide and Cyclosporine Injection interaction?

It is rated moderate. Can be significant — usually manageable with monitoring.

How quickly could this interaction happen?

The documented onset is "rapid". Effects can appear quickly, often within about 24 hours of combining the drugs.

How strong is the evidence for this interaction?

The evidence is graded "established". Well documented — supported by controlled studies or strong clinical data.

Questions for your pharmacist

  • Does my dose of Repaglinide or Cyclosporine Injection need adjusting while I take them together?
  • What symptoms should prompt me to call you or my prescriber right away?
  • Does the timing of my doses matter for this combination?
  • Is there anything you'd monitor while I'm on both?

References (2)

  1. Product Information: PRANDIN(R) oral tablets, repaglinide oral tablets. Novo Nordisk Inc. (per FDA), Plainsboro, NJ, 2017. DailyMed
  2. Kajosaari LI, Niemi M, Neuvonen M, et al: Cyclosporine markedly raises the plasma concentrations of repaglinide. Clin Pharmacol Ther 2005; 78(4):388-399. PubMed
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Repaglinide

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Cyclosporine Injection

Keep reading about Cyclosporine Injection

All Cyclosporine Injection interactions (545) Cyclosporine Injection drug information
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Beyond drug–drug

These medications also interact with supplements

Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:

Repaglinide + Activated Charcoal Siberian Cocklebur Acai African Wild Potato Agaricus Mushroom Agmatine Agrimony Alfalfa + 248 more

major · moderate · minor — check everything you take with our drug–supplement interaction checker.

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This information is for education, not a substitute for professional medical advice. Do not start, stop, or change any medication without talking to your pharmacist or prescriber.