cyp3a4 inducers prandin

Dosage adjustments are recommended in patients taking concomitant strong CYP3A4 or CYP2C8 inhibitors or strong CYP3A4 or CYP2C8 inducers [see Drug Interactions (7.1), Clinical Pharmacology (12.3)]. The most common adverse events leading to withdrawal were hyperglycemia, hypoglycemia, and related symptoms (see PRECAUTIONS). PRANDIN is a glinide indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. 117853-overview Examples: Drugs that induce the CYP3A4 and/or 2C8 enzyme systems include rifampin, barbiturates, and carbamezapine. Mean weight change associated with combination therapy was greater than that of Prandin monotherapy.Distribution: After intravenous (IV) dosing in healthy subjects, the volume of distribution at steady state (Vss) was 31 L, and the total body clearance (CL) was 38 L/h. Hypoglycemia was reported in 16% of 1228 Prandin patients, 20% of 417 glyburide patients, and 19% of 81 glipizide patients. Repaglinide is metabolized by CYP2C8 and to a lesser extent by CYP3A4.

provider for the most current information.The recipient will receive more details and instructions to access this offer.By clicking send, you acknowledge that you have permission to email the recipient with this information.The recipient will receive more details and instructions to access this offer.By clicking send, you acknowledge that you have permission to email the recipient with this information. Hepatic insufficiency may cause elevated repaglinide blood levels and may diminish gluconeogenic capacity, both of which increase the risk of serious hypoglycemia. No comparable cases in the monotherapy treatment groups were reported.Mean change in weight from baseline was +4.9 kg for Prandin-thiazolidinedione therapy.


In addition, an increase in repaglinide plasma levels was observed in a study that evaluated the co-administration of Prandin with trimethoprim and Prandin with deferasirox, both cytochrome P-450 enzyme 2C8 inhibitors. Drugs that are known to inhibit CYP2C8 include agents like trimethoprim, gemfibrozil and montelukast. Diseases & Conditions When such drugs are withdrawn from a patient receiving oral blood glucose lowering agents, the patient should be observed closely for loss of glycemic control.Certain drugs tend to produce hyperglycemia and may lead to loss of glycemic control. The relevance of these findings to humans is unclear. Contact the applicable plan See CLINICAL PHARMACOLOGY section, Drug-Drug Interactions.Repaglinide appears to be a substrate for active hepatic uptake transporter (organic anion transporting protein OATP1B1). Drugs that inhibit OATP1B1 (e.g. The comparator drugs in these 1‑year trials were oral sulfonylurea drugs (SU) including glyburide and glipizide. When such drugs are administered to a patient receiving oral blood glucose‑lowering agents, the patient should be observed closely for hypoglycemia. and formulary information changes. Less than 2% of parent drug was recovered in feces.Pharmacokinetic Parameters: The pharmacokinetic parameters of repaglinide obtained from a single-dose, crossover study in healthy subjects and from a multiple dose, parallel, dose-proportionality (0.5, 1, 2 and 4 mg) study in patients with type 2 diabetes are summarized in the following table:These data indicate that repaglinide did not accumulate in serum. Patients with impaired liver function may be exposed to higher concentrations of repaglinide and its associated metabolites than would patients with normal liver function receiving usual doses. The effect may be very significant if both enzymes are inhibited at the same time resulting in a substantial increase in repaglinide plasma concentrations. 2001 CYP2C8 and CYP3A4 Inducers: Intervention: PRANDIN dose increases and increased frequency of glucose monitoring may be required when co-administered. When these drugs are administered to a patient receiving oral blood glucose lowering agents, the patient should be observed for loss of glycemic control.