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Repaglinide 1 mg Tablet, 500-count — NDC 57237-158-05 (Billing 57237-0158-05)

by Rising Pharma Holdings, Inc. · 500 TABLET in 1 BOTTLE

This is a package of 500 tablets of Repaglinide 1 mg Tablet from Rising Pharma Holdings, Inc., marketed since Jan 2014 and currently FDA-listed.

NDC 57237-0158-05
🏷️ FDA NDC (as labeled) 57237-158-05 billing pads the product segment with a zero
This package
Contains500-count Pack sizes2 compare ↓
Also priced by: Part D plans $0.1282/unit — full pricing hub ↓
Product page 57237-0158-01 Also comes in: 100 tablets 57237-158-01
Rx only Generic On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 57237-158-05
Product NDC 57237-158
11-digit billing NDC 57237015805
RxCUI 200256, 200257, 200258
UNII 668Z8C33LU
UPC 0357237157015, 0357237158012, 0357237159019
Application # ANDA203820
SPL Set ID d7673e22-0dbb-4395-ad60-943d249203a1
Established class (EPC) Glinide
Mechanism of action Potassium Channel Antagonists
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2014-01-22
Route ORAL
Dosage form TABLET
Substance REPAGLINIDE
TE code (Orange Book) AB · RLD · RS

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GPI-14 27280060000320
GPI class Repaglinide
GCN Seq No 038907
GCN 26312
HICL code 017915
Ingredient (HICL) Repaglinide
HIC1 code C
Therapeutic class — broad (HIC1) Electrolyte Balance/Metabolism/Nutrition
HIC2 code C4
Therapeutic class — intermediate (HIC2) Antihyperglycemics
HIC3 code C4K
Therapeutic class — specific (HIC3) Antihyperglycemic, Insulin-Release Stimulant Type
AHFS code 68:20.16.00
AHFS class Meglitinides
FDB label name REPAGLINIDE 1 MG TABLET
FDB brand name Repaglinide
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 038907
  • GCN: 26312
  • GPI-14 (Medi-Span): 27280060000320
  • HICL (First Databank): 017915
  • AHFS class code: 68:20.16.00
  • RxCUI (RxNorm): 200256
Why two NDCs? The FDA registers this code as 57237-158-05 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 57237-0158-05. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

RxNorm drug class

This medicine belongs to the Glinide class.

Pharmacologic class Glinide
Drug family (ATC) Other blood glucose lowering drugs, excl. insulins
How it works Potassium Channel Antagonists
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

Clinical

Label name REPAGLINIDE 1 MG TABLET Ingredient Repaglinide
📗 Our plain-language guide HelloPharmacist
  • It helps adults with type 2 diabetes lower blood sugar, alongside diet and exercise. It is not for type 1 diabetes or diabetic ketoacidosis.
  • Take it within 30 minutes before a meal. If you skip a meal, skip that dose too, which lowers your risk of low blood sugar. Follow your prescriber's directions on how many times a...
  • Low blood sugar is the most common. Others include cold-like infections, headache, sinus problems, joint or back pain, nausea and diarrhea. Call your doctor if lows happen often or...
  • Treat low blood sugar right away as your doctor has taught you, and check your glucose. Your doctor may lower your dose. Severe lows with confusion or seizure are an emergency.
📖 Read our full Repaglinide guide →
1
Nutrient depletion considerations

Repaglinide may be associated with lower levels of 1 nutrient — worth a chat with your pharmacist, not a cause for alarm.

🧪 Full Repaglinide nutrient depletion report →
An association is not a deficiency. Educational only — don't start or stop anything without professional guidance.
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $0.1282 $64.10 / 500 tablets
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Packaging — all sizes for this product

Package NDCDescription Per unit Per pack Marketing startMarketing endStatus
57237-0158-01 57237-158-01 Main listing 100 TABLET in 1 BOTTLE $0.0987 / ea $9.87 2014-01-22 — Active
57237-0158-05 You're viewing this 500 TABLET in 1 BOTTLE — — 2014-01-22 — Active

You're viewing the largest of 2 pack sizes for this product.

This pack shows little to no recent Medicaid volume — the 100 tablets pack carries most fills. See all packs ↓

Pack size FAQ

What quantity is in this package?
This is a 500-count package — 500 tablet in 1 bottle.
How does this package differ from NDC 57237-0158-01?
Both are Repaglinide 1 mg Tablet — the drug itself is identical. This page's package is the 500-count one, while NDC 57237-0158-01 is the 100 tablets package.
What NDC number is used to bill for this package of Repaglinide 1 mg Tablet?
Use the 11-digit billing form listed in the identifiers section of this page. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Repaglinide 1 mg 33342-0249-11 Macleods 100 tablets $0.099 AB Availability likely —
Repaglinide 1 mg 60687-0560-21 American 30 tablets $0.099 AB Availability likely —
Repaglinide 1 mg 62135-0947-90 Chartwell 90 tablets $0.099 AB Availability likely —
Repaglinide 1 mg 65862-0671-01 Aurobindo 100 tablets $0.099 — Availability likely —
Repaglinide 1 mg 72603-0811-01 NorthStar 100 tablets $0.099 AB Availability likely —
Repaglinide 1 mgthis 57237-0158-05 Rising 500 tablets — AB FDA listed —
Repaglinide 1 mg 72162-2558-01 Bryant 100 tablets — AB FDA listed —
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2014
On the market since
Jan 2014
📍
2026
Currently FDA-listed
12 years listed
🔓
·
Generic on the market
this product is a generic
✅This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

Loading inactive ingredients from the official FDA label in the background. No external source is being called by this page request.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerRising Pharma Holdings, Inc.
Application holderAUROBINDO PHARMA LTD
FDA applicationANDA203820 (ANDA)
Labeler code57237
First marketedJan 2014
Product typeHuman Prescription Drug
Portfolio525 products on file
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📋 Description 💬 Information for Patients 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Package Label / Principal Display Panel
🎯 Indications and Usage 90 words ▾

1 INDICATIONS AND USAGE Repaglinide tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitation of Use: Repaglinide tablets should not be used in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis. Repaglinide tablets are a glinide indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

(1) Limitation of Use : Not for treatment of type 1 diabetes mellitus or diabetic ketoacidosis (1)

⏱️ Dosage and Administration ~2 min read ▾

2 DOSAGE AND ADMINISTRATION The recommended starting dose is 0.5 mg orally before each meal if HbA1c is less than 8%; and 1 or 2 mg orally before each meal if HbA1c is 8% or greater. (2.1) The recommended dose range is 0.5 mg to 4 mg before meals, with a maximum daily dose of 16 mg. (2.1) The patient’s dose should be doubled up to 4 mg with each meal until satisfactory glycemic control is achieved.

At least one week should elapse to assess response after each dose adjustment. (2.1) Instruct patients to skip the dose of repaglinide tablets if a meal is skipped. In patients who experience hypoglycemia, the dose of repaglinide tablets should be reduced.

(2.1 ; 5.1) Instruct patients to take repaglinide tablets within 30 minutes before meals. (2.1) In patients with severe renal impairment (CrCl = 20 to 40 mL/min), recommended starting dose is 0.5 mg orally before each meal. (2.2) Dose modifications are required when used concominantly with some medications.

(2.3 , 7)

2.1Recommended Dosage and Administration The recommended starting dose for patients whose HbA 1c is less than 8% is 0.5 mg orally before each meal. For patients whose HbA 1c is 8% or greater the starting dose is 1 mg or 2 mg orally before each meal. The recommended dose range is 0.5 mg to 4 mg before meals, with a maximum daily dose of 16 mg.

The patient’s dose should be doubled up to 4 mg with each meal until satisfactory glycemic control is achieved. At least one week should elapse to assess response after each dose adjustment. Instruct patients to take repaglinide tablets within 30 minutes before meals.

Repaglinide tablets may be dosed 2, 3, or 4 times a day in response to changes in the patient’s meal pattern. In patients who skip meals, instruct patients to skip the scheduled dose of repaglinide tablets to reduce the risk of hypoglycemia. In patients who experience hypoglycemia, the dose of repaglinide tablets should be reduced [see Warnings and Precautions (5.1) ] .

2.2Patients with Severe Renal Impairment In patients with severe renal impairment (CrCl = 20 to 40 mL/min) initiate repaglinide tablets 0.5 mg orally before each meal. Gradually titrate the dose, if needed to achieve glycemic control.

2.3Dose Modifications for Drug Interactions Dosage adjustments are recommended in patients taking concomitant strong CYP3A4 or CYP2C8 inhibitors or strong CYP3A4 or CYP2C8 inducers [see Drug Interactions (7) , Clinical Pharmacology (12.3) ] . Concomitant use with gemfibrozil is contraindicated [see Contraindications (4) ] . Avoid concomitant use of repaglinide tablets with clopidogrel.

If concomitant use cannot be avoided, initiate repaglinide tablets at 0.5 mg before each meal and do not exceed a total daily dose of 4 mg [see Drug Interactions (7) , Clinical Pharmacology (12.3) ] . Do not exceed a total daily dose of 6 mg of repaglinide tablets in patients receiving cyclosporine [see Drug Interactions (7) , Clinical Pharmacology (12.3) ] .

💊 Dosage Forms and Strengths 85 words ▾

3 DOSAGE FORMS AND STRENGTHS Repaglinide tablets USP, 0.5 mg are white to off white, round, biconvex uncoated tablets, debossed with ‘H’ on one side and ‘10’ on other side. Repaglinide tablets USP, 1 mg are yellow colored, round, biconvex uncoated tablets, debossed with ‘H’ on one side and ‘11’ on other side. Repaglinide tablets USP, 2 mg are peach colored, mottled round, biconvex uncoated tablets, debossed with ‘H’ on one side and ‘12’ on other side.

Tablets: 0.5 mg, 1 mg, 2 mg (3)

⛔ Contraindications 40 words ▾

4 CONTRAINDICATIONS Repaglinide tablets are contraindicated in patients with: Concomitant use of gemfibrozil [see Drug Interactions (7) ] Known hypersensitivity to repaglinide or any inactive ingredients Concomitant use with gemfibrozil (4) Known hypersensitivity to repaglinide or any inactive ingredients (4)

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS Hypoglycemia : Repaglinide may cause hypoglycemia. Skip the scheduled dose of repaglinide if a meal is skipped to reduce the risk of hypoglycemia. Reduce the dose of repaglinide if hypoglycemia occurs.

(5.1) Serious Cardiovascular Adverse Reactions with Concomitant NPH-insulin : Repaglinide is not indicated for use in combination with NPH-insulin. (5.2) Macrovascular outcomes : There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with repaglinide. (5.3)

5.1Hypoglycemia All glinides, including repaglinide, can cause hypoglycemia [see Adverse Reactions (6.1) ] . Severe hypoglycemia can cause seizures, may be life-threatening, or cause death. Hypoglycemia can impair concentration ability and reaction time; this may place an individual and others at risk in situations where these abilities are important (e.g., driving or operating other machinery).

Hypoglycemia can happen suddenly and symptoms may differ in each individual and change over time in the same individual. Symptomatic awareness of hypoglycemia may be less pronounced in patients with longstanding diabetes, in patients with diabetic nerve disease, in patients using medications that block the sympathetic nervous system (e.g., beta-blockers) [see Drug Interactions (7) ] , or in patients who experience recurrent hypoglycemia. Factors which may increase the risk of hypoglycemia include changes in meal pattern (e.g., macronutrient content), changes in level of physical activity, changes to co-administered medication [see Drug Interactions (7) ] , and concomitant use with other antidiabetic agents.

Patients with renal or hepatic impairment may be at higher risk of hypoglycemia [see Use in Specific Populations (8.6 , 8.7) ] . Patients should administer repaglinide before meals and be instructed to skip the dose of repaglinide if a meal is skipped. In patients who experience hypoglycemia, the dose of repaglinide should be reduced [see Dosage and Administration (2.1) ] .

Patients and caregivers must be educated to recognize and manage hypoglycemia. Self-monitoring of blood glucose plays an essential role in the prevention and management of hypoglycemia. In patients at higher risk for hypoglycemia and patients who have reduced symptomatic awareness of hypoglycemia, increased frequency of blood glucose monitoring is recommended.

5.2Serious Cardiovascular Adverse Reactions with Concomitant Use with NPH-insulin Across seven controlled trials, there were six serious adverse events of myocardial ischemia in patients treated with repaglinide plus NPH-insulin from two studies, and one event in patients using insulin formulations alone from another study [See Adverse Reactions (6.1) ] . Repaglinide is not indicated for use in combination with NPH-insulin.

5.3Macrovascular Outcomes There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with repaglinide.

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following serious adverse reaction is also described elsewhere in the labeling: Hypoglycemia [see Warnings and Precautions (5.1) ] The most common adverse reactions (5% or greater incidence) among patients treated with repaglinide were: hypoglycemia, upper respiratory infection, headache, sinusitis, arthralgia, nausea, diarrhea, and back pain. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Rising Health, LLC at 1-833-395-6928 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying designs, the adverse reaction rates reported in one clinical trial may not be easily compared to those rates reported in another clinical trial, and may not reflect the rates actually observed in clinical practice. Repaglinide has been administered to 2931 individuals during clinical trials. Approximately 1500 of these individuals with type 2 diabetes have been treated for at least 3 months, 1000 for at least 6 months, and 800 for at least 1 year.

The majority of these individuals (1228) received repaglinide in one of five 1-year, active-controlled trials. Over one year, 13% of repaglinide patients were discontinued due to adverse reactions. The most common adverse reactions leading to withdrawal were hyperglycemia, hypoglycemia, and related symptoms.

Table 1 lists the common adverse reactions for repaglinide patients compared to placebo in trials 12 to 24 weeks duration. Table 1: Adverse Reactions (%) occurring ≥ 2% in Repaglinide Treated Patients from Pool of 12 to 24 Week Placebo Controlled Trials* *See trial descriptions in Clinical Trials (14) Repaglinide N=352 Placebo N=108 Upper Respiratory Infection Headache Sinusitis Arthralgia Nausea Diarrhea Back Pain Rhinitis Constipation Vomiting Paresthesia Chest pain Bronchitis Dyspepsia Urinary tract infection Tooth disorder Allergy 16 11 6 6 5 5 5 3 3 3 3 3 2 2 2 2 2 8 10 2 3 5 2 4 3 2 3 3 1 1 2 1 0 0 Hypoglycemia In clinical trials with repaglinide, hypoglycemia is the most commonly observed adverse reaction.

Mild or moderate hypoglycemia occurred in 31% of repaglinide treated patients and 7% of placebo treated patients [see Warnings and Precautions (5.1) ] . Hypoglycemia was reported in 16% of 1228 repaglinide patients, 20% of 417 glyburide patients, and 19% of 81 glipizide patients in 1-year controlled trials. Of repaglinide-treated patients with symptomatic hypoglycemia, none developed coma or required hospitalization.

In a 24-week placebo controlled trial, patients who were naïve to oral hypoglycemic agent therapy and patients with a HbA 1c below 8% at baseline had a higher frequency of hypoglycemia. Weight Gain There was no average gain in body weight when patients previously treated with oral hypoglycemic agents were switched to repaglinide. The average weight gain in patients treated with repaglinide and not previously treated with sulfonylurea drugs was 3.3%.

Cardiovascular Events The incidence of total serious cardiovascular adverse events, including ischemia, was higher for repaglinide (51/1228 or 4%) than for sulfonylurea drugs (13/498 or 3%) in controlled comparator clinical trials. Table 2: Summary of Serious Cardiovascular Events in Trials Comparing Repaglinide to Sulfonylureas (% of total patients with events) *: glyburide and glipizide Repaglinide SU* Total Exposed Serious CV Events Cardiac Ischemic Events Deaths due to CV Events 1228 4% 2% 0.5% 498 3% 2% 0.4% Seven controlled clinical trials included repaglinide combination therapy with NPH-insulin (n=431), insulin formulations alone (n=388) or other combinations (sulfonylurea plus NPH-insulin or repaglinide plus metformin) (n=120).

There were six serious adverse events of myocardial ischemia in patients treated with repaglinide plus NPH-insulin from two studies, and one event in patients using insulin formulations alone from another study [see Warnings and Precautions (5.3) ] . Combination Therapy with Thiazolidinedione… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~2 min read ▾

7 DRUG INTERACTIONS Clinically Important Drug Interactions with Repaglinide Table 3 includes a list of drugs with clinically important drug interactions when administered concomitantly with repaglinide and instructions for preventing or managing them. Table 3: Clinically Important Drug Interactions with Repaglinide Gemfibrozil Clinical Impact: Gemfibrozil significantly increased repaglinide exposures by 8.1 fold [see Clinical Pharmacology (12.3) ] Intervention: Do not administer repaglinide to patients receiving gemfibrozil [see Contraindications (4) ] .

Clopidogrel Clinical Impact: Clopidogrel increased repaglinide exposures by 3.9 to 5.1 fold [see Clinical Pharmacology (12.3) ] Intervention: Avoid concomitant use of repaglinide with clopidogrel. If concomitant use cannot be avoided, initiate repaglinide at 0.5 mg before each meal and do not exceed a total daily dose of 4 mg [see DOSAGE AND ADMINISTRATION (2.3) ] . Increased frequency of glucose monitoring may be required during concomitant use.

Cyclosporine Clinical Impact: Cyclosporine increased low dose repaglinide exposures by 2.5 fold [see Clinical Pharmacology (12.3) ] Intervention: Daily maximum repaglinide dose should be limited to 6 mg, and increased frequency of glucose monitoring may be required when repaglinide is co-administered with cyclosporine. CYP2C8 and CYP3A4 Inhibitors Intervention: Repaglinide dose reductions and increased frequency of glucose monitoring may be required when co­-administered. Examples: Drugs that are known to inhibit CYP3A4 include antifungal agents (ketoconazole, itraconazole) and antibacterial agents (clarithromycin, erythromycin).

Drugs that are known to inhibit CYP2C8 include trimethoprim, gemfibrozil, montelukast, deferasirox, and clopidiogrel. CYP2C8 and CYP3A4 Inducers Intervention: Repaglinide dose increases and increased frequency of glucose monitoring may be required when co-­administered. Examples: Drugs that induce the CYP3A4 and/or 2C8 enzyme systems include rifampin, barbiturates, and carbamezapine Drugs That May Increase the Risk of Hypoglycemia Intervention: Repaglinide dose reductions and increased frequency of glucose monitoring may be required when co-­administered.

Examples: Antidiabetic agents, ACE inhibitors, angiotensin II receptor blocking agents, disopyramide, fibrates, fluoxetine, monoamine oxidase inhibitors, nonsteroidal anti-inflammatory agents (NSAIDs), pentoxifylline, pramlintide, propoxyphene, salicylates, somatostatin analogs (e.g., octreotide), and sulfonamide antibiotics Drugs That May Decrease the Blood Glucose Lowering Effect of Repaglinide Intervention: Repaglinide dose increases and increased frequency of glucose monitoring may be required when co-­administered.

Examples: Atypical antipsychotics (e.g., olanzapine and clozapine), calcium channel antagonists, corticosteroids, danazol, diuretics, estrogens, glucagon, isoniazid, niacin, oral contraceptives, phenothiazines, progestogens (e.g., in oral contraceptives), protease inhibitors, somatropin, sympathomimetic agents (e.g., albuterol, epinephrine, terbutaline), and thyroid hormones. Drugs That May Blunt Signs and Symptoms of Hypoglycemia Intervention: Increased frequency of glucose monitoring may be required when repaglinide is co-administered with these drugs.

Examples: beta-blockers, clonidine, guanethidine, and reserpine Clopidogrel : Avoid concomitant use; if used concomitantly initiate at 0.5 mg before each meal and limit total daily dose to 4 mg (7) Cyclosporine : Limit daily dose of repaglinide to 6 mg and increase frequency of glucose monitoring when co-administered (7) CYP2C8 and CYP3A4 Inhibitors and Drugs That May Increase the Risk of Hypoglycemia : Co-administration may require repaglinide dose reductions and increased frequency of glucose monitoring (7) CYP2C8 and CYP3A4 Inducers and Drugs That May Decrease the Blood Glucose Lowering Effect of Repaglinide : Co-administration may require repaglinide dose increases and increased frequency… [Excerpted — this section continues on DailyMed.]

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Lactation: Repaglinide is not recommended when breastfeeding (8.2)

8.1Pregnancy Risk Summary Limited available data from case reports and case series with repaglinide use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy (see Clinical Considerations) . Teratogenicity was not observed in rats and rabbits administered repaglinide during organogenesis at approximately 60 and 1 times the maximum daily clinical dose, based on body surface area.

No adverse developmental effects were observed in offspring of rats administered repaglinide during late gestation and lactation at approximately 4 times the maximum daily clinical dose (see Data). The estimated background risk of major birth defects is 6 to 10% in women with pre-gestational diabetes with a HbA1c>7 and has been reported to be as high as 20 to 25% in women with a HbA1c>10. The estimated background risk of miscarriage for the indicated population is unknown.

In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, and delivery complications. Poorly controlled diabetes increases the fetal risk for major birth defects, stillbirth and macrosomia related morbidity.

Data Animal Data Repaglinide was not teratogenic in rats or rabbits at doses 60 times (rats) and approximately 1 times (rabbit) clinical exposure (on a mg/m 2 basis) when administered during the period of organogenesis. Offspring of rat dams exposed to repaglinide at ≥22 times clinical exposure on a mg/m 2 basis during days 17 to 22 of gestation and during lactation were less viable and developed skeletal deformations consisting of shortening, thickening, and bending of the humerus during the postnatal period. This effect was not seen at doses up to 4 times clinical exposure (on a mg/m 2 basis).

8.2Lactation Risk Summary There are no data on the presence of repaglinide in human milk, the effects on the breastfeeding infant, or the effects on milk production. The drug is present in animal milk. When a drug is present in animal milk, it is likely that the drug will be present in human milk (see Data) .

Because of the potential for hypoglycemia in breastfed infants, repaglinide is not recommended for use when breastfeeding. Data In rat reproduction studies, measurable levels of repaglinide were detected in the breast milk of the dams and lowered blood glucose levels were observed in the pups. Cross fostering studies indicated that skeletal changes [see Use in Specific Populations (8.1) ] could be induced in control pups nursed by treated dams, although this occurred to a lesser degree than those pups treated in utero .

8.4Pediatric Use Safety and effectiveness have not been established in pediatric patients.

8.5Geriatric Use In clinical studies of 24 weeks or greater duration, 415 patients were over 65 years of age and no patients were greater than 75 years of age. In one-year, active-controlled trials, no differences were seen in effectiveness or adverse events between these subjects and those less than 65. There was no increase in frequency or severity of hypoglycemia in older subjects, but greater sensitivity of some older individuals to repaglinide therapy cannot be ruled out.

8.6Renal Impairment Pharmacokinetic studies of repaglinide were conducted in patients with mild to moderate renal function impairment (CrCl = 40 to 80 mL/min), and severe renal function impairment (CrCl = 20 to 40 mL/min). Initial dose adjustment is not required in patients with mild to mode… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~2 min read ▾

8.1Pregnancy Risk Summary Limited available data from case reports and case series with repaglinide use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy (see Clinical Considerations) . Teratogenicity was not observed in rats and rabbits administered repaglinide during organogenesis at approximately 60 and 1 times the maximum daily clinical dose, based on body surface area.

No adverse developmental effects were observed in offspring of rats administered repaglinide during late gestation and lactation at approximately 4 times the maximum daily clinical dose (see Data). The estimated background risk of major birth defects is 6 to 10% in women with pre-gestational diabetes with a HbA1c>7 and has been reported to be as high as 20 to 25% in women with a HbA1c>10. The estimated background risk of miscarriage for the indicated population is unknown.

In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, and delivery complications. Poorly controlled diabetes increases the fetal risk for major birth defects, stillbirth and macrosomia related morbidity.

Data Animal Data Repaglinide was not teratogenic in rats or rabbits at doses 60 times (rats) and approximately 1 times (rabbit) clinical exposure (on a mg/m 2 basis) when administered during the period of organogenesis. Offspring of rat dams exposed to repaglinide at ≥22 times clinical exposure on a mg/m 2 basis during days 17 to 22 of gestation and during lactation were less viable and developed skeletal deformations consisting of shortening, thickening, and bending of the humerus during the postnatal period. This effect was not seen at doses up to 4 times clinical exposure (on a mg/m 2 basis).

🧒 Pediatric Use 13 words ▾

8.4Pediatric Use Safety and effectiveness have not been established in pediatric patients.

🧓 Geriatric Use 78 words ▾

8.5Geriatric Use In clinical studies of 24 weeks or greater duration, 415 patients were over 65 years of age and no patients were greater than 75 years of age. In one-year, active-controlled trials, no differences were seen in effectiveness or adverse events between these subjects and those less than 65. There was no increase in frequency or severity of hypoglycemia in older subjects, but greater sensitivity of some older individuals to repaglinide therapy cannot be ruled out.

🆘 Overdosage 92 words ▾

10 OVERDOSAGE Severe hypoglycemic reactions with coma, seizure, or other neurological impairment may occur and constitute medical emergencies requiring immediate hospitalization. Hypoglycemic symptoms without loss of consciousness or neurologic findings should be treated aggressively with oral glucose and adjustments in drug dosage and/or meal patterns. Close monitoring may continue until the physician is assured that the patient is out of danger.

Patients should be closely monitored for a minimum of 24 to 48 hours, since hypoglycemia may recur after apparent clinical recovery. There is no evidence that repaglinide is dialyzable using hemodialysis.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Repaglinide lowers blood glucose levels by stimulating the release of insulin from the pancreas. This action is dependent upon functioning beta (ß) cells in the pancreatic islets. Insulin release is glucose-dependent and diminishes at low glucose concentrations.

Repaglinide closes ATP-dependent potassium channels in the ß-cell membrane by binding at characterizable sites. This potassium channel blockade depolarizes the ß-cell, which leads to an opening of calcium channels. The resulting increased calcium influx induces insulin secretion.

The ion channel mechanism is highly tissue selective with low affinity for heart and skeletal muscle.

12.2Pharmacodynamics A four-week, double-blind, placebo-controlled dose-response trial was conducted in 138 patients with type 2 diabetes using doses ranging from 0.25 (not an approved dose) to 4 mg taken with each of three meals. Repaglinide therapy resulted in dose-proportional glucose lowering over the full dose range. Plasma insulin levels increased after meals and reverted toward baseline before the next meal.

Most of the fasting blood glucose-lowering effect was demonstrated within 1 to 2 weeks. In a double-blind, placebo-controlled, 3-month dose titration study, repaglinide or placebo doses for each patient were increased weekly from 0.25 mg (not an approved dose) through 0.5, 1, and 2 mg, to a maximum of 4 mg, until a fasting plasma glucose (FPG) level <160 mg/dL was achieved or the maximum dose reached. The dose that achieved the targeted control or the maximum dose was continued to end of study.

FPG and 2-hour post-prandial glucose (PPG) increased in patients receiving placebo and decreased in patients treated with repaglinide. Differences between the repaglinide- and placebo-treated groups were -61 mg/dL (FPG) and -104 mg/dL (PPG) (Table 4). Table 4: Repaglinide vs Placebo Mean Change from Baseline after 3 Months of Treatment *:p< 0.05 for between group difference Repaglinide Placebo N 66 33 Fasting Plasma Glucose (mg/dL) Baseline Change from baseline (at last visit) Post Prandial Glucose (mg/dL) Baseline Change from baseline (at last visit) 220.2 -31.0 * 261.7 -47.6 * 215.3 30.3 245.2

56.5The dosing of repaglinide relative to meal-related insulin release was studied in three trials including 58 patients. Glycemic control was maintained during a period in which the meal and dosing pattern was varied (2, 3 or 4 meals per day; before meals x 2, 3, or 4) compared with a period of 3 regular meals and 3 doses per day (before meals x 3). Blood glucose-lowering effect did not differ when repaglinide was administered at the start of a meal, 15 minutes before, or 30 minutes before the meal.

12.3Pharmacokinetics 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 Tables 5 and 6. These data indicate that repaglinide did not accumulate in serum. Clearance of oral repaglinide did not change over the 0.5 to 4 mg dose range, indicating a linear relationship between dose and plasma drug levels.

Table 5: Pharmacokinetic Parameters for Repaglinide in Healthy Subjects CL = total body clearance Vss = volume of distribution at steady state AbsBio = absolute bioavailability Parameter CL (based on i.v.) 38 ± 16 L/hr Vss (based on i.v.) 31 ± 12 L AbsBio 56 ± 9% Table 6: Pharmacokinetic Parameters for Repaglinide in Patients with Type 2 Diabetes* *dosed preprandially with three meals Pharmacokinetic Parameter Dose (mg) AUC 0-24 hr (ng/mL*hr) Mean (SD) C max0-5 hr (ng/mL) Mean (SD) 0.5 68.9 (154.4) 9.8 (10.2) 1 125.8 (129.8) 18.3 (9.1) 2 152.4 (89.60) 26.0 (13.0) 4 447.4 (211.3) 65.8 (30.1) T max0-5 hr Means (SD) T½ Means (Ind Range) 0.5 to 4 1.0 to 1.4 (0.3 to 0.5) hr 1.0 to 1.4 (0.4 to 8.0) hr Absorption After oral administration, repaglinide is completely absorbe… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 94 words ▾

12.1Mechanism of Action Repaglinide lowers blood glucose levels by stimulating the release of insulin from the pancreas. This action is dependent upon functioning beta (ß) cells in the pancreatic islets. Insulin release is glucose-dependent and diminishes at low glucose concentrations.

Repaglinide closes ATP-dependent potassium channels in the ß-cell membrane by binding at characterizable sites. This potassium channel blockade depolarizes the ß-cell, which leads to an opening of calcium channels. The resulting increased calcium influx induces insulin secretion.

The ion channel mechanism is highly tissue selective with low affinity for heart and skeletal muscle.

📦 How Supplied / Storage and Handling 134 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Repaglinide Tablets USP, 0.5 mg are white to off white, round, biconvex uncoated tablets, debossed with ‘H’ on one side and ‘10’ on other side. Bottles of 100 NDC 57237-157-01 Bottles of 500 NDC 57237-157-05 Repaglinide Tablets USP, 1 mg are yellow colored, round, biconvex uncoated tablets, debossed with ‘H’ on one side and ‘11’ on other side. Bottles of 100 NDC 57237-158-01 Bottles of 500 NDC 57237-158-05 Repaglinide Tablets USP, 2 mg are peach colored, mottled round, biconvex uncoated tablets, debossed with ‘H’ on one side and ‘12’ on other side.

Bottles of 100 NDC 57237-159-01 Bottles of 500 NDC 57237-159-05 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Keep bottles tightly closed.

Dispense in tight containers with safety closures.

📋 Description 121 words ▾

11 DESCRIPTION Repaglinide is an oral blood glucose-lowering drug of the glinide class. Repaglinide, S(+)2-ethoxy-4(2((3-methyl-1-(2-(1-piperidinyl) phenyl)-butyl) amino)-2-oxoethyl) benzoic acid, is chemically unrelated to the oral sulfonylurea insulin secretagogues. Structural Formula of Repaglinide Repaglinide USP is a white to off-white solid with molecular formula C 27 H 36 N 2 O 4 and a molecular weight of 452.6.

Repaglinide tablets, USP contain 0.5 mg, 1 mg, or 2 mg of repaglinide USP. In addition, each tablet contains the following inactive ingredients: anhydrous dibasic calcium phosphate, corn starch, glycerol, magnesium stearate, meglumine, microcrystalline cellulose, polacrillin potassium, poloxamer, and povidone. In addition, the 1 mg tablet contains ferric oxide (Sicovit Yellow 10) and 2 mg tablet contains ferric oxide (Sicovit Red 30).

Chemical Structure

💬 Information for Patients 150 words ▾

17 PATIENT COUNSELING INFORMATION Hypoglycemia Inform patients that repaglinide tablets can cause hypoglycemia and instruct patients and their caregivers on self-management procedures including glucose monitoring and management of hypoglycemia. Inform patients that their ability to concentrate and react may be impaired as a result of hypoglycemia. In patients at higher risk for hypoglycemia and patients who have reduced symptomatic awareness of hypoglycemia, increased frequency of blood glucose monitoring is recommended [see Warnings and Precautions (5.1) ] .

Administration Instruct patients to take repaglinide tablet within 30 minutes before meals. Instruct patients to skip their dose of repaglinide tablet when a meal is skipped. [see Dosage and Administration (2) ] . Drug Interactions Discuss potential drug interactions with patients and inform them of potential drug-drug interactions with repaglinide tablets. [see Drug Interactions (7) ] .

Distributed by: Rising Health, LLC Saddle Brook, NJ 07663 Made in India Code: TS/DRUGS/19/1993 Revised: 07/2021

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics 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 Tables 5 and 6. These data indicate that repaglinide did not accumulate in serum. Clearance of oral repaglinide did not change over the 0.5 to 4 mg dose range, indicating a linear relationship between dose and plasma drug levels.

Table 5: Pharmacokinetic Parameters for Repaglinide in Healthy Subjects CL = total body clearance Vss = volume of distribution at steady state AbsBio = absolute bioavailability Parameter CL (based on i.v.) 38 ± 16 L/hr Vss (based on i.v.) 31 ± 12 L AbsBio 56 ± 9% Table 6: Pharmacokinetic Parameters for Repaglinide in Patients with Type 2 Diabetes* *dosed preprandially with three meals Pharmacokinetic Parameter Dose (mg) AUC 0-24 hr (ng/mL*hr) Mean (SD) C max0-5 hr (ng/mL) Mean (SD) 0.5 68.9 (154.4) 9.8 (10.2) 1 125.8 (129.8) 18.3 (9.1) 2 152.4 (89.60) 26.0 (13.0) 4 447.4 (211.3) 65.8 (30.1) T max0-5 hr Means (SD) T½ Means (Ind Range) 0.5 to 4 1.0 to 1.4 (0.3 to 0.5) hr 1.0 to 1.4 (0.4 to 8.0) hr Absorption After oral administration, repaglinide is completely absorbed from the gastrointestinal tract.

After single and multiple oral doses in healthy subjects or in patients, peak plasma drug levels (C max ) occur within 1 hour (T max ). Repaglinide is eliminated from the blood stream with a half-life of approximately 1 hour. The mean absolute bioavailability is 56%.

When repaglinide was given with food, the mean T max was not changed, but the mean C max and AUC (area under the time/plasma concentration curve) were decreased 20% and 12.4%, respectively. Distribution After intravenous (IV) dosing in healthy subjects, the volume of distribution at steady state (V ss ) was 31 L, and the total body clearance (CL) was 38 L/h. Protein binding and binding to human serum albumin was greater than 98%.

Metabolism and Elimination Repaglinide is completely metabolized by oxidative biotransformation and direct conjugation with glucuronic acid after either an IV or oral dose. The major metabolites are an oxidized dicarboxylic acid (M2), the aromatic amine (M1), and the acyl glucuronide (M7). The cytochrome P-450 enzyme system, specifically 2C8 and 3A4, have been shown to be involved in the N-dealkylation of repaglinide to M2 and the further oxidation to M1.

Metabolites do not contribute to the glucose-lowering effect of repaglinide. Within 96 hours after dosing with 14 C-repaglinide as a single, oral dose, approximately 90% of the radiolabel was recovered in the feces and approximately 8% in the urine. Only 0.1% of the dose is cleared in the urine as parent compound.

The major metabolite (M2) accounted for 60% of the administered dose. Less than 2% of parent drug was recovered in feces. Repaglinide appears to be a substrate for active hepatic uptake transporter (organic anion transporting protein OATP1B1).

Variability of Exposure Repaglinide AUC after multiple doses of 0.25 to 4 mg with each meal varies over a wide range. The intra-individual and inter- individual coefficients of variation were 36% and 69%, respectively. AUC over the therapeutic dose range included 69 to 1005 ng/mL*hr, but AUC exposure up to 5417 ng/mL*hr was reached in dose escalation studies without apparent adverse consequences.

Specific Populations Geriatric Healthy volunteers were treated with a regimen of 2 mg repaglinide taken before each of 3 meals. There were no significant differences in repaglinide pharmacokinetics between the group of patients <65 years of age and a comparably sized group of patients ≥65 years of age [see Use in Specific Populations (8.5) ] . Gender A comparison of pharmacokinetics in males and females showed the AUC over the 0.5 mg to 4 mg dose range to be 15% to 70% higher in females with type 2 diabetes.

This difference was not reflected in the frequency of h… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacodynamics ~1 min read ▾

12.2Pharmacodynamics A four-week, double-blind, placebo-controlled dose-response trial was conducted in 138 patients with type 2 diabetes using doses ranging from 0.25 (not an approved dose) to 4 mg taken with each of three meals. Repaglinide therapy resulted in dose-proportional glucose lowering over the full dose range. Plasma insulin levels increased after meals and reverted toward baseline before the next meal.

Most of the fasting blood glucose-lowering effect was demonstrated within 1 to 2 weeks. In a double-blind, placebo-controlled, 3-month dose titration study, repaglinide or placebo doses for each patient were increased weekly from 0.25 mg (not an approved dose) through 0.5, 1, and 2 mg, to a maximum of 4 mg, until a fasting plasma glucose (FPG) level <160 mg/dL was achieved or the maximum dose reached. The dose that achieved the targeted control or the maximum dose was continued to end of study.

FPG and 2-hour post-prandial glucose (PPG) increased in patients receiving placebo and decreased in patients treated with repaglinide. Differences between the repaglinide- and placebo-treated groups were -61 mg/dL (FPG) and -104 mg/dL (PPG) (Table 4). Table 4: Repaglinide vs Placebo Mean Change from Baseline after 3 Months of Treatment *:p< 0.05 for between group difference Repaglinide Placebo N 66 33 Fasting Plasma Glucose (mg/dL) Baseline Change from baseline (at last visit) Post Prandial Glucose (mg/dL) Baseline Change from baseline (at last visit) 220.2 -31.0 * 261.7 -47.6 * 215.3 30.3 245.2

56.5The dosing of repaglinide relative to meal-related insulin release was studied in three trials including 58 patients. Glycemic control was maintained during a period in which the meal and dosing pattern was varied (2, 3 or 4 meals per day; before meals x 2, 3, or 4) compared with a period of 3 regular meals and 3 doses per day (before meals x 3). Blood glucose-lowering effect did not differ when repaglinide was administered at the start of a meal, 15 minutes before, or 30 minutes before the meal.

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES

14.1Monotherapy Trials A double-blind, placebo-controlled trial was carried out in 362 patients treated for 24 weeks. HbA 1c for the repaglinide-treated groups (1 and 4 mg groups combined) at the end of the study was decreased compared to the placebo-treated group in treatment naïve patients and in patients previously treated with oral hypoglycemic agents by 2.1% and 1.7%, respectively. In this fixed-dose trial, patients who were treatment naïve to oral hypoglycemic agent therapy and patients with a HbA 1c below 8% at baseline showed greater blood glucose-lowering.

14.2Combination Trials Repaglinide in Combination With Metformin Repaglinide was studied in combination with metformin in 83 patients not satisfactorily controlled on exercise, diet, and metformin alone. Repaglinide dosage was titrated for 4 to 8 weeks, followed by a 3-month maintenance period. Combination therapy with repaglinide and metformin resulted in statistically significant improvement in HbA 1c and fasting plasma glucose (FPG) compared to repaglinide or metformin monotherapy (Table 8).

In this study where metformin dosage was kept constant, the combination therapy of repaglinide and metformin showed dose-sparing effects with respect to repaglinide. The improvement in HbA 1c and FPG of the combination group was achieved at a lower daily repaglinide dosage than in the repaglinide monotherapy group (Table 8). Table 8: Repaglinide in Combination with Metformin: Mean Change from Baseline after 4 to 5 Months of Treatment 1 1 : based on intent-to-treat analysis ∗ : p< 0.05, for pairwise comparisons with repaglinide and metformin monotherapy. # : p< 0.05, for pairwise comparison with metformin.

Repaglinide Monotherapy Repaglinide Combination Therapy with Metformin Metformin Monotherapy N 28 27 27 Median Final Dose (mg/day) 12 6 (Repaglinide) 1500 (metformin) 1500 HbA 1c (%) Baseline 8.6 8.3

8.6Change from baseline -0.38 -1.41 * -0.33 Fasting Plasma Glucose (mg/dL) Baseline 174 184 194 Change from baseline 8.8 -39.2 ∗ -4.5 Weight (kg) Baseline 87 93 91 Change from baseline 3.0 2.4 # -0.90 Repaglinide in Combination With Pioglitazone A combination therapy regimen of repaglinide and pioglitazone (N=123) was compared to repaglinide alone (N=61) and pioglitazone alone (N=62) in a 24-week trial that enrolled 246 patients previously treated with sulfonylurea or metformin monotherapy (HbA 1c > 7.0%). repaglinide dosage was titrated during the first 12 weeks, followed by a 12-week maintenance period.

Combination therapy resulted in statistically significant improvement in HbA 1c and FPG compared to monotherapy (Figure 1). The changes from baseline for completers in FPG (mg/dL) and HbA 1c (%), respectively were: -39.8 mg/dL and -0.1% for repaglinide, -35.3 mg/dL and -0.1% for pioglitazone and -92.4 mg/dL and -1.9% for the combination. In this study where pioglitazone dosage was kept constant, the combination therapy group showed dose-sparing effects with respect to repaglinide (see Figure 1 Legend).

The improvement in HbA 1c and FPG of the combination group was achieved at a lower daily repaglinide dosage than in the repaglinide monotherapy group. Figure 1: Repaglinide in Combination with Pioglitazone: HbA 1c Values LEGEND: HbA 1c values by study week for patients who completed study (combination, N = 101; repaglinide, N = 35, pioglitazone, N = 26). Subjects with FPG above 270 mg/dL were withdrawn from the study.

Pioglitazone dose: fixed at 30 mg/day; repaglinide median final dose: 6 mg/day for combination and 10 mg/day for monotherapy. Repaglinide in Combination With Rosiglitazone A combination therapy regimen of repaglinide and rosiglitazone was compared to monotherapy with either agent alone in a 24-week trial that enrolled 252 patients previously treated with sulfonylurea or metformin (HbA 1c > 7.0%). Combination therapy resulted in statistically significant improvement in HbA 1c and FPG compared to monotherapy (Table 9 below).

The glycemic effects… [Excerpted — this section continues on DailyMed.]

🧪 Nonclinical Toxicology ~1 min read ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility In a 104-week carcinogenicity study in rats at doses up to 120 mg/kg/day, which is approximately 90 times clinical exposure on a mg/m 2 basis, the incidences of benign adenomas of the thyroid and liver were increased in male rats. No evidence of carcinogenicity was found in female rats. The higher incidences of thyroid and liver tumors in male rats were not seen at lower dose of 30 mg/kg/day and 60 mg/kg/day respectively (which are over 20 and 45 times, respectively, clinical exposures on a mg/m 2 basis).

In a 104-week carcinogenicity study in mice at doses up to 500 mg/kg/day, no evidence of carcinogenicity was found in mice (which is approximately 187 times clinical exposure on a mg/m 2 basis). Repaglinide was non-genotoxic in a battery of in vivo and in vitro studies: Bacterial mutagenesis (Ames test), in vitro forward cell mutation assay in V79 cells (HGPRT), in vitro chromosomal aberration assay in human lymphocytes, unscheduled and replicating DNA synthesis in rat liver, and in vivo mouse and rat micronucleus tests.

In a rat fertility study, repaglinide was administered to male and female rats at doses up to 300 and 80 mg/kg/day, respectively. No adverse effects on fertility were observed (which are over 60 times clinical exposure on a mg/m 2 basis).

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 219 words ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility In a 104-week carcinogenicity study in rats at doses up to 120 mg/kg/day, which is approximately 90 times clinical exposure on a mg/m 2 basis, the incidences of benign adenomas of the thyroid and liver were increased in male rats. No evidence of carcinogenicity was found in female rats. The higher incidences of thyroid and liver tumors in male rats were not seen at lower dose of 30 mg/kg/day and 60 mg/kg/day respectively (which are over 20 and 45 times, respectively, clinical exposures on a mg/m 2 basis).

In a 104-week carcinogenicity study in mice at doses up to 500 mg/kg/day, no evidence of carcinogenicity was found in mice (which is approximately 187 times clinical exposure on a mg/m 2 basis). Repaglinide was non-genotoxic in a battery of in vivo and in vitro studies: Bacterial mutagenesis (Ames test), in vitro forward cell mutation assay in V79 cells (HGPRT), in vitro chromosomal aberration assay in human lymphocytes, unscheduled and replicating DNA synthesis in rat liver, and in vivo mouse and rat micronucleus tests.

In a rat fertility study, repaglinide was administered to male and female rats at doses up to 300 and 80 mg/kg/day, respectively. No adverse effects on fertility were observed (which are over 60 times clinical exposure on a mg/m 2 basis).

📄 Package Label / Principal Display Panel 209 words ▾

PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 0.5 mg (100 Tablets Bottle Label) Rising ® NDC 57237-157-01 Repaglinide Tablets, USP 0.5 mg 100 Tablets Rx only PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 0.5 mg (100 Tablet Bottle)

PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 0.5 mg (100 Tablets Carton Label) Rising ® NDC 57237-157-01 Repaglinide Tablets, USP 0.5 mg 100 Tablets Rx only PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 0.5 mg (100 Tablets Carton Label)

PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 1 mg (100 Tablets Bottle Label) Rising ® NDC 57237-158-01 Repaglinide Tablets, USP 1 mg 100 Tablets Rx only PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 1 mg (100 Tablets Bottle Label)

PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 1 mg (100 Tablets Carton Label) Rising ® NDC 57237-158-01 Repaglinide Tablets, USP 1 mg 100 Tablets Rx only PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 1 mg (100 Tablets Carton Label)

PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 2 mg (100 Tablets Bottle Label) Rising ® NDC 57237-159-01 Repaglinide Tablets, USP 2 mg 100 Tablets Rx only PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 2 mg (100 Tablets Bottle Label)

PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 2 mg (100 Tablets Carton Label) Rising ® NDC 57237-159-01 Repaglinide Tablets, USP 2 mg 100 Tablets Rx only PACKAGE LABEL-PRINCIPAL DISPLAY PANEL - 2 mg (100 Tablets Carton Label)

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

Medicaid utilization by pack size

Medicaid (SDUD) totals over the four most recent reported quarters for every package size of this drug — handy when a specific package (e.g. a starter/titration pack) carries little or no Medicaid volume on its own.
100 tablets57237-0158-01 7,561 Rx · $159,701
500 tablets this page57237-0158-05 No Medicaid data
Drug total (last 4 qtrs): 7,561 Rx · 825,480 units · $159,701 gross reimbursed
Tap a pack size to open its page. Source: CMS State Drug Utilization Data, last 4 quarters.

Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Repaglinide — the program that covers self-administered drugs. 4 manufacturers.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Repaglinide. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$2.79M
Claims incl. refills
92.9K
Beneficiaries
63.8K
Spend / beneficiary
$43.71
Spend / claim
$30.00
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Repaglinide — the ingredient across all brands.

Top reported reactions

Hypoglycaemia794
Acute Kidney Injury558
Drug Interaction433
Diarrhoea384
Lactic Acidosis368
Dyspnoea287
Nausea266

Age at onset

Neonate3
Child1
Adolescent1
Adult363
Elderly925

Reporter sex

7,418 reports
Male · 54%
Female · 46%
Unknown · 0%

Serious outcomes

Hospitalization4,450
Life-threatening805
Death708
Disabling150
Reports over time (by year) — tap or hover for the count & year
2019 2021 2023 2026 739 0
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos — Not published for this NDC No photo available yet for this listing.
Inactive ingredients (structured) — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available.
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by Rising Pharma Holdings, Inc.. Listing status can change — the directory data on this page refreshes weekly.
Does this product come in other package sizes?
Yes — the FDA directory lists 1 other package presentation of this same product, including 100 tablets (57237-0158-01). Each has its own NDC and its own page — see the package list near the top of this page.
Who lists this product with the FDA?
Rising Pharma Holdings, Inc. is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.
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For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.