Repaglinide Potency Greatly Increased When Combined
With Gemfibrozil
If the combination is used, repaglinide dosage should
be greatly reduced and blood glucose concentrations
carefully monitored. Gemfibrozil raised the plasma
concentration of repaglinide by 5.5-15.0 times and
prolonged its half-life from 1.3 to 3.7 hours.
A potentially hazardous interaction between gemfibrozil,
a fibrate, and repaglinide, an oral hypoglycemic
agent, has been found by Finnish specialists.
Gemfibrozil, especially in combination with itraconazole,
greatly increased and prolonged the blood glucose-lowering
effect of repaglinide, they found. Repaglinide thus
became a long-acting and stronger anti-diabetic.
Clinicians should avoid using the two medications
together, the specialists warned. If the combination
is necessary, repaglinide dosage should be greatly
reduced and blood glucose concentrations carefully
monitored.
The specialists, clinical pharmacologists at Helsinki
University Central Hospital, Finland, studied possible
interactions of gemfibrozil, itraconazole and their
combination with repaglinide in a randomised crossover
study.
They enrolled 12 healthy volunteers who were given
either gemfibrozil 600 mg., itraconazole 100 mg.
(first dose 200 mg.), gemfibrozil and itraconazole
together or placebo, all twice daily for 3 days.
On the third day, the volunteers took a 0.25 mg.
dose of repaglinide.
Plasma drug and blood glucose concentrations were
followed for 7 hours and serum insulin and C-peptide
concentrations for 3 hours post-dose.
Gemfibrozil raised the area under the plasma concentration-time
curve of repaglinide by 5.5-15.0 times and prolonged
its half-life from 1.3 to 3.7 hours.
Itraconazole alone raised repaglinide's area under
the plasma concentration-time curve by 1.1-1.9 times.
But, the gemfibrozil-itraconazole combination raised
it by 12.9-24.7 times and prolonged repaglinide's
half-life to 6.1 hours.
Gemfibrozil increased plasma repaglinide concentration
at 7 hours by 28.6 times. The gemfibrozil-itraconazole
combination increased plasma repaglinide concentration
at 7 hours by 70.4 times. Diabetes Care 2003;26:
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