Version July 2025
Diabetes mellitus, type 2, treatment:
Note: May be used as an adjunctive agent or alternative monotherapy for patients in whom initial therapy with lifestyle intervention and metformin failed or who cannot take metformin. Meglitinides are associated with a greater risk of hypoglycemia than other noninsulin antidiabetic agents (Ref).
Initial:
HbA 1c <8%: Oral: 0.5 mg before each meal (up to 4 times/day).
HbA 1c ≥8%: Oral: 1 to 2 mg before each meal (up to 4 times/day).
Dosage adjustment: At intervals of ≥1 week, may double the dose with each meal until adequate glycemic control is achieved; usual maintenance dose: 0.5 to 1 mg before each meal (1.5 to 3 mg/day) (maximum: 4 mg/dose [16 mg/day]) (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Note: Although <2% of repaglinide is eliminated unchanged in the urine, Cmax is doubled and AUCs are tripled in patients with severe kidney impairment compared to those with normal kidney function, potentially due to a decrease in hepatic metabolism and clearance (Ref).
Altered kidney function:
CrCl ≥40 mL/minute: Oral: No dosage adjustment necessary (Ref).
CrCl <40 mL/minute: Oral: Initial: 0.5 mg once daily with largest meal; gradually increase to 0.5 mg before each meal (up to 4 times/day) (Ref). If response is inadequate, may further increase dose at intervals of ≥1 week by doubling the dose with each meal until adequate glycemic control is achieved, up to a maximum of 2 mg before each meal (up to 4 times/day) (Ref).
Hemodialysis, intermittent (thrice weekly): Not dialyzable (Ref):
Oral: Initial: 0.5 mg once daily with largest meal; gradually increase to 0.5 mg before each meal (up to 4 times/day) (Ref). If response is inadequate, may further increase dose at intervals of ≥1 week by doubling the dose with each meal until adequate glycemic control is achieved, up to a maximum of 2 mg before each meal (up to 4 times/day).
Peritoneal dialysis: Unlikely to be dialyzed (highly protein bound) (Ref):
Oral: Initial: 0.5 mg once daily with largest meal; gradually increase to 0.5 mg before each meal (up to 4 times/day) (Ref). If response is inadequate, may further increase dose at intervals of ≥1 week by doubling the dose with each meal until adequate glycemic control is achieved, up to a maximum of 2 mg before each meal (up to 4 times/day).
CRRT: Oral: Avoid use (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration): Oral: Avoid use (Ref).
There are no dosage adjustments provided in the manufacturer's labeling. Use with caution; consider longer intervals between dosage adjustments.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Central nervous system: Headache (9% to 11%)
Endocrine & metabolic: Hypoglycemia (16% to 31%)
Respiratory: Upper respiratory tract infection (10% to 16%)
1% to 10%:
Cardiovascular: Ischemia (4%), chest pain (2% to 3%)
Gastrointestinal: Diarrhea (4% to 5%), constipation (2% to 3%)
Genitourinary: Urinary tract infection (2% to 3%)
Hypersensitivity: Hypersensitivity reaction (1% to 2%)
Neuromuscular & skeletal: Back pain (5% to 6%), arthralgia (3% to 6%)
Respiratory: Sinusitis (3% to 6%), bronchitis (2% to 6%)
<1%, postmarketing, and/or case reports: Alopecia, anaphylactoid reaction, blurred vision (transient), cardiac arrhythmia, ECG abnormality, hemolytic anemia, hepatic insufficiency (severe), hepatitis, hypertension, increased liver enzymes, jaundice, leukopenia, myocardial infarction, palpitations, pancreatitis, Stevens-Johnson syndrome, thrombocytopenia, visual disturbance (transient)
Hypersensitivity to repaglinide or any component of the formulation; concurrent gemfibrozil therapy
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Severe hepatic impairment; concurrent use with clopidogrel; diabetic ketoacidosis, with or without coma; type 1 diabetes (insulin dependent)
Concerns related to adverse effects:
• Hypoglycemia: Severe hypoglycemia may occur; risk may be increased by changes in meal patterns, changes in physical activity levels, changes to coadministered medications, and concomitant use with other antidiabetic agents.
Disease-related concerns:
• Bariatric surgery:
– Altered absorption: Absorption may be altered given the anatomic and transit changes created by gastric bypass and sleeve gastrectomy surgery (Mingrone 2016; Mechanick 2020).
– Hypoglycemia: May increase the risk of hypoglycemia after gastric bypass, sleeve gastrectomy, and gastric band (Mechanick 2020). Insulin secretion and sensitivity may be partially or completely restored after these procedures (gastric bypass is most effective, followed by sleeve and, finally, band) (Korner 2009; Peterli 2012). First-phase insulin secretion and hepatic insulin sensitivity have been shown to be significantly improved in the immediate days after gastric bypass and sleeve gastrectomy. The restorative effects of these procedures on peripheral insulin sensitivity may occur later in the 3- to 12-month period after surgery. Where possible, the selection of antidiabetic agents without the potential for hypoglycemia is advised.
• Cardiovascular effects: Some studies suggest oral hypoglycemic drugs may be associated with increased cardiovascular events. Theoretically, repaglinide may also increase cardiovascular events, but there are no long-term studies assessing this concern. Use in combination with NPH insulin is not indicated; in two studies, reports of myocardial ischemia (6 events) in patients using repaglinide plus insulin have caused concern. Further evaluation is required to assess the safety of this combination.
• Hepatic impairment: Use with caution in patients with hepatic impairment; may be more susceptible to glucose-lowering effects.
• Renal impairment: Use with caution in patients with severe renal impairment; may be more susceptible to glucose-lowering effects.
Other warnings/precautions:
• Appropriate use: Not for use in patients with diabetic ketoacidosis or patients with type 1 diabetes mellitus.
• Hospitalized patients: Consider temporary discontinuation of noninsulin antidiabetic agents and initiation or continuation of insulin therapy during hospitalization (ADA 2023). In noncritically ill hospitalized patients, continued use of repaglinide may be considered if there are no contraindications, regular nutritional intake is expected, and blood glucose is well controlled; close monitoring and subsequent dosage adjustments are recommended (ADA/AACE [Moghissi 2009]; Bogun 2013; Inzucchi 2006).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Generic: 0.5 mg, 1 mg, 2 mg
Yes
Tablets (Repaglinide Oral)
0.5 mg (per each): $3.33 - $3.66
1 mg (per each): $3.66
2 mg (per each): $3.66
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, Oral:
GlucoNorm: 0.5 mg [DSC], 1 mg [DSC], 2 mg [DSC]
Generic: 0.5 mg, 1 mg, 2 mg
Oral: Administer within 30 minutes before meals; may be administered preprandially 2, 3, or 4 times/day in response to changes in meal pattern. If a meal is missed, do not administer next scheduled dose; if hypoglycemia occurs, reduce dose.
Diabetes mellitus, type 2, treatment: To improve glycemic control in adults with type 2 diabetes mellitus as an adjunct to diet and exercise.
Repaglinide may be confused with rasagiline
Prandin [multiple international markets] may be confused with Avandia brand name for rosiglitazone [US, Canada, and multiple international markets]
Prandin brand name for repaglinide [multiple international markets], but also brand name for deflazacort [South Korea]
Substrate of CYP2C8 (Major), CYP3A4 (Major), OATP1B1/1B3; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Aldesleukin: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Alpha-Lipoic Acid: May increase hypoglycemic effects of Antidiabetic Agents. Risk C: Monitor
Androgens: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Risk C: Monitor
Antidiabetic Agents: May increase hypoglycemic effects of Hypoglycemia-Associated Agents. Risk C: Monitor
Asciminib: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Belumosudil: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Avoid coadministration of belumosudil with these substrates of OATP1B1/1B3 for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the OATP1B1/1B3 substrate may be required. Risk D: Consider Therapy Modification
Beta-Blockers (Beta1 Selective): May increase adverse/toxic effects of Antidiabetic Agents. Specifically, beta-blockers may mask the hypoglycemic symptoms of antidiabetic agents. Risk C: Monitor
Beta-Blockers (Nonselective): May increase hypoglycemic effects of Antidiabetic Agents. Beta-Blockers (Nonselective) may increase adverse/toxic effects of Antidiabetic Agents. Specifically, beta-blockers may mask the hypoglycemic symptoms of antidiabetic agents. Risk C: Monitor
Bortezomib: May increase therapeutic effects of Antidiabetic Agents. Bortezomib may decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor
Bulevirtide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Coadministration of bulevirtide with OATP1B1/1B3 (also known as SLCO1B1/1B3) substrates should be avoided when possible. If used together, close clinical monitoring is recommended. Risk D: Consider Therapy Modification
Ceftobiprole Medocaril: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid
Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor
Clopidogrel: May increase serum concentration of Repaglinide. Management: Avoid use of clopidogrel and repaglinide if possible; if the combination must be used, limit total repaglinide daily dose to no more than 4 mg. This is contraindicated in some non-US labeling. Risk D: Consider Therapy Modification
CycloSPORINE (Systemic): May increase serum concentration of Repaglinide. Management: Limit the daily repaglinide dose to a maximum of 6 mg with concurrent use of cyclosporine, and monitor closely for increased repaglinide effects. Risk D: Consider Therapy Modification
CYP2C8 Inhibitors (Moderate): May increase serum concentration of Repaglinide. Risk C: Monitor
CYP2C8 Inhibitors (Strong): May increase serum concentration of Repaglinide. Risk X: Avoid
CYP2C8 Inhibitors (Weak): May increase serum concentration of Repaglinide. Risk C: Monitor
CYP3A4 Inducers (Moderate): May decrease serum concentration of Repaglinide. Risk C: Monitor
CYP3A4 Inducers (Strong): May decrease serum concentration of Repaglinide. Risk C: Monitor
CYP3A4 Inhibitors (Strong): May increase serum concentration of Repaglinide. Risk C: Monitor
Darolutamide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Dinutuximab Beta: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Direct Acting Antiviral Agents (HCV): May increase hypoglycemic effects of Antidiabetic Agents. Risk C: Monitor
Elexacaftor, Tezacaftor, and Ivacaftor: May increase serum concentration of Repaglinide. Risk C: Monitor
Elranatamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Eltrombopag: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Encorafenib: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Epcoritamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Erythromycin (Systemic): May increase serum concentration of Repaglinide. Risk C: Monitor
Etilefrine: May decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor
Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification
Glofitamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Glucagon-Like Peptide-1 Agonists: May increase hypoglycemic effects of Meglitinides. Management: Consider meglitinide dose reductions when used in combination with glucagon-like peptide-1 agonists, particularly when also used with basal insulin. Risk D: Consider Therapy Modification
Guanethidine: May increase hypoglycemic effects of Antidiabetic Agents. Risk C: Monitor
Herbal Products with Glucose Lowering Effects: May increase hypoglycemic effects of Hypoglycemia-Associated Agents. Risk C: Monitor
HMG-CoA Reductase Inhibitors (Statins): May increase serum concentration of Repaglinide. Risk C: Monitor
Hyperglycemia-Associated Agents: May decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor
Hypoglycemia-Associated Agents: Antidiabetic Agents may increase hypoglycemic effects of Hypoglycemia-Associated Agents. Risk C: Monitor
Hypoglycemia-Associated Agents: May increase hypoglycemic effects of Hypoglycemia-Associated Agents. Risk C: Monitor
Irbesartan: May increase serum concentration of Repaglinide. Risk C: Monitor
Lapatinib: May increase serum concentration of CYP2C8 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Leflunomide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Leniolisib: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid
Letermovir: May increase serum concentration of Repaglinide. Management: Monitor for increased repaglinide effects/toxicities (ie, hypoglycemia) if combined with letermovir. When letermovir is coadministered with cyclosporine, the use of repaglinide is not recommended. Risk C: Monitor
Linzagolix: May increase serum concentration of CYP2C8 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid
Lumacaftor and Ivacaftor: May decrease serum concentration of CYP2C8 Substrates (High Risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may increase serum concentration of CYP2C8 Substrates (High Risk with Inhibitors or Inducers). Risk C: Monitor
Maitake: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Risk C: Monitor
Monoamine Oxidase Inhibitors: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Risk C: Monitor
Mosunetuzumab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Pegvisomant: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Risk C: Monitor
Pretomanid: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Prothionamide: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Risk C: Monitor
Quinolones: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Quinolones may decrease therapeutic effects of Agents with Blood Glucose Lowering Effects. Specifically, if an agent is being used to treat diabetes, loss of blood sugar control may occur with quinolone use. Risk C: Monitor
Reproterol: May decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor
RifAMPin: May decrease serum concentration of Repaglinide. Risk C: Monitor
Ritodrine: May decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor
Salicylates: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Risk C: Monitor
Selective Serotonin Reuptake Inhibitor: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Risk C: Monitor
Spironolactone: May increase serum concentration of CYP2C8 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Talquetamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Tarlatamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Taurursodiol: May increase serum concentration of CYP2C8 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid
Teclistamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Teriflunomide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Thiazide and Thiazide-Like Diuretics: May decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor
Trofinetide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Avoid concurrent use with OATP1B1/1B3 substrates for which small changes in exposure may be associated with serious toxicities. Monitor for evidence of an altered response to any OATP1B1/1B3 substrate if used together with trofinetide. Risk D: Consider Therapy Modification
Tucatinib: May increase serum concentration of Repaglinide. Risk C: Monitor
Voclosporin: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
When given with food, the AUC of repaglinide is decreased. Taking medication without eating may cause hypoglycemia. Management: Administer within 30 minutes prior to a meal. If a meal is skipped, skip dose for that meal.
Repaglinide was shown to have a low potential to cross the placenta using an ex vivo perfusion model (Tertti 2011). Information describing the effects of repaglinide on pregnancy outcomes is limited.
Poorly controlled diabetes during pregnancy can be associated with an increased risk of adverse maternal and fetal outcomes, including diabetic ketoacidosis, preeclampsia, spontaneous abortion, preterm delivery, delivery complications, major malformations, stillbirth, and macrosomia. To prevent adverse outcomes, prior to conception and throughout pregnancy, maternal blood glucose and HbA1c should be kept as close to target goals as possible but without causing significant hypoglycemia (ADA 2023; Blumer 2013).
Agents other than repaglinide are currently recommended to treat diabetes mellitus in pregnancy (ADA 2023).
It is not known if repaglinide is present in breast milk.
Due to the potential for hypoglycemia in the breastfed infant, breastfeeding is not recommended by the manufacturer
Individualized medical nutrition therapy based on American Diabetes Association recommendations is an integral part of therapy.
Monitor fasting blood glucose (individualize frequency based on treatment regimen, hypoglycemia risk, and other patient-specific factors) (ADA 2023). During dose adjustment, fasting glucose can be used to determine response.
HbA1c: Monitor at least twice yearly in patients who have stable glycemic control and are meeting treatment goals; monitor quarterly in patients in whom treatment goals have not been met, or with therapy change. Note: In patients prone to glycemic variability (eg, patients with insulin deficiency), or in patients whose HbA1c is discordant with serum glucose levels or symptoms, consider evaluating HbA1c in combination with blood glucose levels and/or a glucose management indicator (ADA 2023; KDIGO 2020).
Recommendations for glycemic control in patients with diabetes:
Nonpregnant adults with diabetes (AACE [Samson 2023]; ADA 2023):
HbA1c: <7% (a more aggressive [<6.5%] or less aggressive [<8%] HbA1c goal may be targeted based on patient-specific characteristics). Note: In patients using a continuous glucose monitoring system, a goal of time in range >70% with time below range <4% is recommended and is similar to a goal HbA1c <7%.
Preprandial capillary blood glucose: 80 to 130 mg/dL (SI: 4.4 to 7.2 mmol/L) (more or less stringent goals may be appropriate based on patient-specific characteristics).
Peak postprandial capillary blood glucose (~1 to 2 hours after a meal): <180 mg/dL (SI: <10 mmol/L) (more or less stringent goals may be appropriate based on patient-specific characteristics).
Older adults (≥65 years of age) (ADA 2023):
Note: Consider less strict targets in patients who are using insulin and/or insulin secretagogues (sulfonylureas, meglitinides) (ES [LeRoith 2019]).
HbA1c: <7% to 7.5% (healthy); <8% (complex/intermediate health). Note: Individualization may be appropriate based on patient and caregiver preferences and/or presence of cognitive impairment. In patients with very complex or poor health (ie, limited remaining life expectancy), consider making therapy decisions based on avoidance of hypoglycemia and symptomatic hyperglycemia rather than HbA1c level.
Preprandial capillary blood glucose: 80 to 130 mg/dL (SI: 4.4 to 7.2 mmol/L) (healthy); 90 to 150 mg/dL (SI: 5 to 8.3 mmol/L) (complex/intermediate health); 100 to 180 mg/dL (SI: 5.6 to 10 mmol/L) (very complex/poor health).
Bedtime capillary blood glucose: 80 to 180 mg/dL (SI: 4.4 to 10 mmol/L) (healthy); 100 to 180 mg/dL (SI: 5.6 to 10 mmol/L) (complex/intermediate health); 110 to 200 mg/dL (SI: 6.1 to 11.1 mmol/L) (very complex/poor health).
Classification of hypoglycemia (ADA 2023):
Level 1: 54 to 70 mg/dL (SI: 3 to 3.9 mmol/L); hypoglycemia alert value; initiate fast-acting carbohydrate (eg, glucose) treatment.
Level 2: <54 mg/dL (SI: <3 mmol/L); threshold for neuroglycopenic symptoms; requires immediate action.
Level 3: Hypoglycemia associated with a severe event characterized by altered mental and/or physical status requiring assistance.
Nonsulfonylurea hypoglycemic agent which blocks ATP-dependent potassium channels, depolarizing the membrane and facilitating calcium entry through calcium channels. Increased intracellular calcium stimulates insulin release from the pancreatic beta cells. Repaglinide-induced insulin release is glucose-dependent.
Absorption: Complete
Distribution: Vd: 31 L
Protein binding, plasma: >98% to albumin
Metabolism: Hepatic via CYP3A4 and CYP2C8 isoenzymes and glucuronidation to inactive metabolites
Bioavailability: 56% ± 9%
Half-life elimination: ~1 hour
Time to peak, plasma: 1 hour
Excretion: Feces (~90%, <2% as unchanged drug); Urine (~8%, 0.1% as unchanged drug)
Altered kidney function: AUC and Cmax are increased in severe renal impairment.
Hepatic function impairment: Higher and more prolonged serum concentrations have been observed in patients with moderate to severe hepatic impairment.
