What is repaglinide used for?

Contents

Prandin

SIDE EFFECTS

The following serious adverse reaction is also described elsewhere in the labeling: Hypoglycemia

Clinical 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.

PRANDIN 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 PRANDIN in one of five 1-year, active-controlled trials. Over one year, 13% of PRANDIN 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 PRANDIN patients compared to placebo in trials 12 to 24 weeks duration.

Table 1: Adverse Reactions (%) occurring ≥ 2% in PRANDIN Treated Patients from Pool of 12 to 24 Week Placebo Controlled Trials*

PRANDIN
N=352
Placebo
N=108
Upper Respiratory Infection 16 8
Headache 11 10
Sinusitis 6 2
Arthralgia 6 3
Nausea 5 5
Diarrhea 5 2
Back Pain 5 4
Rhinitis 3 3
Constipation 3 2
Vomiting 3 3
Paresthesia 3 3
Chest pain 3 1
Bronchitis 2 1
Dyspepsia 2 2
Urinary tract infection 2 1
Tooth disorder 2 0
Allergy 2 0
*See trial descriptions in Clinical Trials

Hypoglycemia

In clinical trials with PRANDIN, hypoglycemia is the most commonly observed adverse reaction. Mild or moderate hypoglycemia occurred in 31% of PRANDIN treated patients and 7% of placebo treated patients .

Combination Therapy With Thiazolidinediones

During 24-week treatment clinical trials of PRANDIN-rosiglitazone or PRANDIN-pioglitazone combination therapy (a total of 250 patients in combination therapy), hypoglycemia (blood glucose < 50 mg/dL) occurred in 7% of patients in combination therapy compared to 7% for PRANDIN monotherapy, and 2% for thiazolidinedione monotherapy.

Peripheral Edema And Heart Failure

Peripheral edema was reported in 12 out of 250 (4.8%) PRANDIN-thiazolidinedione combination therapy patients and 3 out of 124 (2.4%) thiazolidinedione monotherapy patients, with no cases reported in these trials for PRANDIN monotherapy. There were reports in 2 of 250 patients (0.8%) treated with PRANDIN-thiazolidinedione therapy of episodes of edema with congestive heart failure. Both patients had a prior history of coronary artery disease and recovered after treatment with diuretic agents. No comparable cases in the monotherapy treatment groups were reported.

Weight Gain

Mean weight increases associated with combination, PRANDIN and pioglitazone therapy were 5.5 kg, 0.3 kg, and 2.0 kg respectively. Mean weight increases associated with combination, PRANDIN and rosiglitazone therapy were 4.5 kg, 1.3 kg, and 3.3 kg respectively.

Infrequent Adverse Events (<1% of Patients)

Less common adverse clinical or laboratory events observed in clinical trials included elevated liver enzymes, thrombocytopenia, leukopenia, and anaphylactoid reactions.

Postmarketing Experience

The following additional adverse reactions have been identified during post approval use of PRANDIN. Because these reactions are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or a causal relationship to drug exposure.

  • Alopecia
  • Hemolytic anemia
  • Pancreatitis
  • Stevens-JohnsonSyndrome
  • Severe hepatic dysfunction including jaundice and hepatitis

Read the entire FDA prescribing information for Prandin (Repaglinide)

repaglinide (oral) (Prandin)

What should I discuss with my healthcare provider before taking repaglinide (Prandin)?

You should not use repaglinide if you are allergic to it, or if you have:

  • severe liver disease;
  • diabetic ketoacidosis (call your doctor for treatment with insulin); or
  • if you also take gemfibrozil.

To make sure repaglinide is safe for you, tell your doctor if you have:

  • liver disease; or
  • if you also take metformin or other diabetes medicines.

Follow your doctor’s instructions about using this medicine if you are pregnant. Blood sugar control is very important during pregnancy, and your dose needs may be different during each trimester.

It is not known whether repaglinide passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.

Repaglinide is not approved for use by anyone younger than 18 years old.

How should I take repaglinide (Prandin)?

Follow all directions on your prescription label. Your doctor may occasionally change your dose. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Repaglinide is usually taken 2 to 4 times daily, within 30 minutes before eating a meal. Follow your doctor’s instructions. If you skip a meal, do not take your dose of repaglinide. Wait until your next meal.

Your blood sugar will need to be checked often, and you may need other blood tests at your doctor’s office.

Low blood sugar (hypoglycemia) can happen to everyone who has diabetes. Symptoms include headache, hunger, sweating, irritability, dizziness, nausea, fast heart rate, and feeling anxious or shaky. To quickly treat low blood sugar, always keep a fast-acting source of sugar with you such as fruit juice, hard candy, crackers, raisins, or non-diet soda.

Your doctor can prescribe a glucagon emergency injection kit to use in case you have severe hypoglycemia and cannot eat or drink. Be sure your family and close friends know how to give you this injection in an emergency.

Blood sugar levels can be affected by stress, illness, surgery, exercise, alcohol use, or skipping meals. Ask your doctor before changing your dose or medication schedule.

Repaglinide is only part of a treatment program that may also include diet, exercise, weight control, blood sugar testing, and special medical care. Follow your doctor’s instructions very closely.

Store repaglinide at room temperature away from moisture and heat.

QUESTION

______________ is another term for type 2 diabetes. See Answer

ACT Repaglinide

How does this medication work? What will it do for me?

Repaglinide belongs to the class of medications called antidiabetes agents. It is an oral hypoglycemic (lowering of blood sugar) medication used by people with type 2 diabetes, along with proper diet and exercise, for the control of blood sugar. It is used when diet, exercise, and weight reduction alone have not been found to control blood sugar well enough.

Repaglinide may also be used in combination with metformin or rosiglitazone, two other medications that lower blood sugar, when medication (in addition to diet, exercise, and weight reduction) does not control blood sugar well enough on its own. Repaglinide helps to control blood sugar by increasing the amount of insulin released by the pancreas.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

0.5 mg
Each white-to-off-white, round biconvex tablet with “RA05” on one side and a symbol on the other, contains repaglinide 0.5 mg. Nonmedicinal ingredients: calcium hydrogen phosphate, croscarmellose sodium, glycerol, iron oxide yellow, magnesium stearate, maize starch, meglumine, microcrystalline cellulose, poloxamer, and povidone.

1 mg
Each yellow, round, biconvex tablet with “RA1” on one side and a symbol on the other, contains repaglinide 1 mg. Nonmedicinal ingredients: calcium hydrogen phosphate, croscarmellose sodium, glycerol, magnesium stearate, maize starch, meglumine, microcrystalline cellulose, poloxamer, and povidone.

2 mg
Each pink, round, biconvex tablet with “RA2” on one side and a symbol on the other, contains repaglinide 2 mg. Nonmedicinal ingredients: calcium hydrogen phosphate, croscarmellose sodium, glycerol, iron oxide red, magnesium stearate, maize starch, meglumine, microcrystalline cellulose, poloxamer, and povidone.

How should I use this medication?

The usual dose of repaglinide is based on response to the medication, but is usually started at 0.5 mg. It can be taken either immediately before a meal or up to 30 minutes before a meal. The dose is increased by your doctor based on your response to the medication. The maximum daily dose is 16 mg. Repaglinide may be used along with other medications that reduce blood sugar if one medication is not enough to reduce blood sugar levels to the desired range.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones given here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor. If you miss a dose of this medication, skip the missed dose and continue with your regular schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not take this medication if you:

  • are allergic to repaglinide or any ingredients of this medication
  • are taking the medication gemfibrozil
  • are taking the medication clopidogrel
  • have diabetic ketoacidosis with or without coma (this condition should be treated with insulin)
  • have severe liver disease
  • have type 1 diabetes

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • abdominal pain
  • back pain
  • constipation
  • diarrhea
  • dizziness
  • fatigue
  • headache
  • joint pain
  • nausea
  • vomiting

Although most of the side effects listed below don’t happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • bloody or cloudy urine
  • burning, painful, or difficult urination
  • chills
  • cough
  • fever
  • low blood sugar, including:
    • anxious feeling
    • behavioural change similar to being drunk
    • blurred vision
    • cold sweats
    • confusion
    • cool pale skin
    • difficulty thinking
    • drowsiness
    • excessive hunger
    • fast heartbeat
    • headache
    • nausea
    • nervousness
    • nightmares
    • restless sleep
    • shakiness
    • slurred speech
    • unusual tiredness or weakness
  • runny or stuffy nose
  • shortness of breath
  • signs of liver damage:
    • abdominal pain
    • dark urine
    • fatigue
    • fever
    • loss of appetite
    • yellow skin or eyes
  • sinus congestion with pain
  • sneezing
  • sore throat
  • vision changes
  • wheezing

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • chest pain
  • convulsions (seizures)
  • fast or irregular heartbeat
  • signs of an allergic reaction, e.g.:
    • difficulty breathing
    • hives
    • swelling of the face or throat
  • signs of bleeding, e.g.:
    • bleeding gums
    • blood in the urine
    • dark tarry stools
    • easy bruising
    • nosebleeds
    • vomiting blood
  • unconsciousness

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

HEALTH CANADA ADVISORY

July 31, 2015

Health Canada has issued new restrictions concerning the use of gluconorm (repaglinide). To read the full Health Canada Advisory, visit Health Canada’s web site at www.hc-sc.gc.ca.

Blood sugar control: If you are exposed to extra stress such as fever, trauma, infection, or surgery, your blood sugar control may vary. Monitor your blood sugar carefully and call the doctor if any important changes occur in your control.

Hypoglycemia (low blood sugar): Hypoglycemia (low blood sugar) can occur when taking repaglinide. If you experience low blood sugar (e.g., headache, drowsiness, weakness, dizziness, confusion, irritability, hunger, fast heartbeat, sweating, and feeling jittery) while taking this medication, contact your doctor.

Kidney function: If you have decreased kidney function, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: Reduced liver function may cause higher levels of repaglinide in the body and increase the risk for low blood sugar levels (hypoglycemia). Make sure you report all your medical conditions to your doctor(s). People with severe liver disease should not take repaglinide.

Missed or delayed meals: This medication acts by promoting the secretion of insulin and should be taken before meals. If a meal is skipped or delayed, the dosing of repaglinide should be skipped or delayed as well.

Pregnancy: This medication should not be used during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known whether repaglinide passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: This safety and effectiveness of using this medication have not been established for children.

What other drugs could interact with this medication?

There may be an interaction between repaglinide and any of the following:

  • abiraterone
  • ACE inhibitors (e.g., ramipril, lisinopril)
  • anti-psychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzepine, quetiapine, risperidone)
  • barbiturates (e.g., phenobarbital)
  • beta-blockers (e.g., propranolol, metoprolol)
  • birth control pills
  • boceprevir
  • bosentan
  • calcium channel blockers (e.g., nifedipine, verapamil)
  • carbamazepine
  • celecoxib
  • clopidogrel
  • corticosteroids (e.g., dexamethasone, prednisone)
  • cyclosporine
  • dabrafenib
  • danazol
  • deferasirox
  • other diabetes medications (e.g., chlorpropamide, glipizide, glyburide, insulin, metformin, nateglinide, rosiglitazone, sitagliptin)
  • diuretics (e.g., furosemide, hydrochlorothiazide)
  • eltrombopag
  • enzalutamide
  • estrogens
  • gemfibrozil
  • HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs; e.g., delaviridine, efavirenz, etravirine, nevirapine)
  • HIV protease inhibitors (e.g., darunavir, indinavir, lopinavir, saquinavir, tipranavir)
  • irbesartan
  • isoniazid
  • itraconazole
  • ketoconazole
  • losartan
  • macrolide antibiotics (e.g., clarithromycin, erythromycin)
  • monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
  • nefazodone
  • nicotinic acid
  • nonsteroidal anti-inflammatory drugs (e.g., ibuprofen, naproxen)
  • octreotide
  • phenytoin
  • primidone
  • progesterone
  • quinine
  • quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
  • rifabutin
  • rifampin
  • rifapentine
  • ritonavir
  • St. John’s wort
  • salicylates (e.g., ASA)
  • selective serotonin reuptake inhibitors (SSRI; e.g., fluoxetine, paroxetine, sertraline)
  • stiripentol
  • sulfonamides (e.g., sulfamethoxazole)
  • tacrolimus
  • tamoxifen
  • testosterone
  • trimethoprim

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than the ones listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications that you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

All material copyright MediResource Inc. 1996 – 2020. Terms and conditions of use. The contents herein are for informational purposes only. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Source: www.medbroadcast.com/drug/getdrug/ACT-Repaglinide

Generic Name: repaglinide (oral) (re PAG li nide)
Brand Names: Prandin

Medically reviewed by Drugs.com. Last updated on Jun 24, 2019.

  • Overview
  • Side Effects
  • Dosage
  • Professional
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What is Prandin?

Prandin (repaglinide) is an oral diabetes medicine that helps control blood sugar levels by causing the pancreas to produce insulin.

Prandin is used together with diet and exercise to improve blood sugar control in adults with type 2 diabetes mellitus. This medicine is not for treating type 1 diabetes.

Important information

You should not use Prandin if you have type 1 diabetes, severe liver disease, or diabetic ketoacidosis.

You should not use Prandin together with gemfibrozil (Lopid) or NPH insulin (such as isophane insulin).

Prandin is only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely. Changing any of these factors can affect your blood sugar levels.

Before taking this medicine

You should not use Prandin if you are allergic to repaglinide, or if you have:

  • severe liver disease;

  • diabetic ketoacidosis (call your doctor for treatment with insulin); or

  • if you also take gemfibrozil.

To make sure Prandin is safe for you, tell your doctor if you have:

  • liver disease; or

  • if you also take metformin or other diabetes medicines.

Follow your doctor’s instructions about using Prandin if you are pregnant. Blood sugar control is very important during pregnancy, and your dose needs may be different during each trimester.

It is not known whether repaglinide passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.

Prandin is not approved for use by anyone younger than 18 years old.

How should I take Prandin?

Take Prandin exactly as prescribed by your doctor. Follow all directions on your prescription label. Your doctor may occasionally change your dose. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Prandin is usually taken 2 to 4 times daily, within 30 minutes before eating a meal. Follow your doctor’s instructions. If you skip a meal, do not take your dose of Prandin. Wait until your next meal.

Your blood sugar will need to be checked often, and you may need other blood tests at your doctor’s office.

Low blood sugar (hypoglycemia) can happen to everyone who has diabetes. Symptoms include headache, hunger, sweating, irritability, dizziness, nausea, fast heart rate, and feeling anxious or shaky. To quickly treat low blood sugar, always keep a fast-acting source of sugar with you such as fruit juice, hard candy, crackers, raisins, or non-diet soda.

Your doctor can prescribe a glucagon emergency injection kit to use in case you have severe hypoglycemia and cannot eat or drink. Be sure your family and close friends know how to give you this injection in an emergency.

Blood sugar levels can be affected by stress, illness, surgery, exercise, alcohol use, or skipping meals. Ask your doctor before changing your dose or medication schedule.

Prandin is only part of a treatment program that may also include diet, exercise, weight control, blood sugar testing, and special medical care. Follow your doctor’s instructions very closely.

Store at room temperature away from moisture and heat.

Prandin dosing information

Usual Adult Dose for Diabetes Type 2:

Individualize therapy:
Dose preprandially 2, 3, or 4 times a day
-For patients not previously treated with antidiabetic agents or whose glycosylated hemoglobin (HbA1c) is less than 8%:
Initial dose: 0.5 mg orally with each meal
-For patients previously treated with antidiabetic agents or whose HbA1c is 8% or higher:
Initial dose: 1 or 2 mg orally with each meal
Dose Adjustments: Based upon blood glucose response, double the preprandial dose up to a maximum meal time dose of 4 mg until satisfactory glycemic response is achieved; allow at least 1 week to assess response after each dose adjustment.
Recommended Dose Range: 0.5 to 4 mg orally with each meal
Maximum Daily Dose: 16 mg per day

-Fasting blood glucose concentrations are generally used to adjust doses, however, postprandial glucose levels may be used in patients whose pre-meal blood glucose levels are satisfactory but whose overall glycemic control (HbA1c) is inadequate.
-When hypoglycemia occurs in patients taking this drug in combination with a thiazolidinedione or metformin, the dose of this drug should be reduced.
Use: As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

What happens if I miss a dose?

Take the missed dose as soon as you remember, but only if you are getting ready to eat a meal. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. A repaglinide overdose can cause life-threatening hypoglycemia.

Symptoms of severe hypoglycemia include extreme weakness, blurred vision, sweating, trouble speaking, tremors, stomach pain, confusion, and seizure (convulsions).

What should I avoid while taking Prandin?

Avoid drinking alcohol. It lowers blood sugar and may interfere with your diabetes treatment.

Prandin side effects

Get emergency medical help if you have signs of an allergic reaction to Prandin: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • severe pain in your upper stomach spreading to your back, nausea and vomiting, fast heart rate;

  • pale or yellowed skin, dark colored urine, fever, confusion or weakness; or

  • severe skin reaction – fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Common Prandin side effects may include:

  • low blood sugar;

  • nausea, diarrhea;

  • headache, back pain;

  • joint pain; or

  • cold symptoms such as stuffy nose, sneezing, sore throat.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Prandin?

Many other medicines that can increase or decrease the effects of repaglinide n lowering your blood sugar. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Prandin only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Copyright 1996-2020 Cerner Multum, Inc. Version: 9.01.

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  • Diabetes, Type 2

Repaglinide

Repaglinide is the generic name of the brand-name drug Prandin.

It’s used to treat people with type 2 diabetes who can’t manage their condition by diet and exercise alone.

When you have type 2 diabetes, your body doesn’t make or use the hormone insulin normally, so it can’t control the amount of sugar, or glucose, in the blood.

Repaglinide is a meglitinide antidiabetic. It helps the body regulate sugar in the blood by encouraging the pancreas to release insulin.

Taking repaglinide, along with adopting a healthy lifestyle, can decrease your risk of developing the serious or life-threatening complications of type 2 diabetes.

These may include cardiovascular diseases, such as heart attack, stroke, and problems related to blood circulation; nerve damage; kidney disease; or eye conditions.

The Food and Drug Administration (FDA) approved repaglinide in 1997. It’s manufactured by Novo Nordisk.

Repaglinide Warnings

You shouldn’t take repaglinide if you have type 1 diabetes (the body doesn’t produce any insulin) or diabetic ketoacidosis (a dangerous condition that can occur if high blood sugar is untreated).

Before taking this medicine, tell your doctor if you have or have ever had:

  • Liver disease
  • Kidney disease
  • Adrenal or pituitary problems

Don’t take repaglinide if you are also taking NPH insulin or gemfibrozil (Lopid).

Tell your healthcare providers that you’re taking repaglinide before having any type of surgery, including a dental procedure.

Repaglinide should be used with caution in elderly people because they may be more sensitive to it.

Don’t give this medicine to a child or anyone under 18 years old. Safety and effectiveness of repaglinide in kids hasn’t been established.

Repaglinide may cause changes in your blood sugar.

You should know the symptoms of high (hyperglycemic) or low (hypoglycemic) blood-sugar episodes and be prepared to treat them.

Low blood sugar is a common side effect of repaglinide.

Symptoms can include headache, hunger, weakness, sweating, tremor or severe shaking, irritability, or trouble concentrating.

Drinking orange juice or eating a hard candy or glucose tablet can bring up blood sugar levels.

Tell your physician if you experience an illness, fever, injury, or unusual stress while taking repaglinide, because these can change your blood sugar and the dosage you need.

Repaglinide controls diabetes, but it doesn’t cure it. Continue to take it even if you feel well. Don’t stop it without talking to your doctor.

Your doctor will probably want to frequently check your glucose levels while you are taking repaglinide.

Always wear a diabetic ID bracelet to be sure you get proper treatment in case of an emergency.

Pregnancy and Repaglinide

This medicine is an FDA Pregnancy Category C drug, which means harm to an unborn baby can’t be ruled out.

Tell your doctor if you’re pregnant or plan to become pregnant while taking repaglinide.

Your physician may recommend insulin during pregnancy to ensure that your blood sugar is well-controlled.

It’s also not known if repaglinide is found in breast milk. Don’t breastfeed while taking this medicine without talking to your doctor first.

Prandin is a drug which is taken before meals and acts quickly to help keep blood glucose levels from rising too high after meals.

The drug belongs to a group of diabetes medications known as prandial glucose regulators (or meglitinides) and has been available since gaining approval for use in 1997.

About Prandin

  • Trade name: Prandin
  • Generic name: Repaglinide
  • Drug class: Prandial glucose regulators / Meglitinides
  • Manufacturer: Novo Nordisk

Mechanism of action

Prandin stimulates the release of insulin by beta cells in the pancreas The stimulation of insulin producing cells by the drug tends to be more immediate and lasts for a shorter period than drugs in the sulphonylureas class of drugs.

By triggering more insulin to be released by the pancreas, Prandin helps to lower blood glucose levels but the increased release of insulin may raise blood pressure levels and promote weight gain.

Prandin should be taken in combination with a healthy diet and regular physical activity.

Who is Prandin suitable for?

Prandin is suitable for people with type 2 diabetes if lifestyle changes have not brought blood glucose levels under sufficient control.

Prandin may be taken on its own (monotherapy) or in combination with metformin or another diabetes drug (dual therapy).

Who should not take repaglinide?

Repaglinide is not suitable for people with type 1 diabetes, an autoimmune form of diabetes. Ensure your doctor knows if you have any of the following conditions:

  • If you are pregnant, planning a pregnancy or breastfeeding
  • If you are taking any supplements which can lower blood glucose levels
  • If you have kidney or liver damage

How to take repaglinide

Repaglinide is available in tablet form and is best taken 15 minutes before having a main meal but can be taken at any point within 30 minutes prior to starting a main meal.

If you miss a dose, wait until before your next main meal to resume your treatment.

What to do if you take an overdose

An overdose of repaglinide could cause blood glucose levels to go too low. Be aware of the symptoms of hypoglycemia and treat low blood glucose with fast acting carbohydrate if a hypo occurs.

Call your health team immediately for advice if you have taken an overdose.

Side effects

Side effects of taking Prandin may include one or more of the following:

  • Low blood glucose levels (hypoglycemia)
  • Abdominal pains
  • Diarrhoea

Rarer side effects may include:

  • Cardiovascular problems
  • Eyesight problems
  • Liver problems

Please note that the list provided here is not exhaustive. A complete list of adverse effects is included in the patient information leaflet provided with the medication.

Long term safety

Drugs which stimulate insulin, referred to as insulin secretagogues, have been associated with higher risks of cardiovascular disease (including heart attacks and stroke) compared with metformin A 20 year Danish study, however, showed that repaglinide presented a lower risk than a number of other insulin secretagogues and had a similar cardiovascular risk to metformin.

Whilst studies have shown evidence that some insulin secretagogues are associated with an increased rate of death of the insulin producing cells in the pancreas ( beta cells ), prandial glucose regulators, such as repaglinide and nateglinide, have not been associated with an increase in the rate of beta cell death.

Generic Name: repaglinide (oral) (re PAG li nide)
Brand Name: Prandin

Medically reviewed by Drugs.com on Aug 27, 2019 – Written by Cerner Multum

  • Overview
  • Side Effects
  • Dosage
  • Professional
  • Interactions
  • More

What is repaglinide?

Repaglinide is an oral diabetes medicine that helps control blood sugar levels by causing the pancreas to produce insulin.

Repaglinide is used together with diet and exercise to improve blood sugar control in adults with type 2 diabetes mellitus. repaglinide is not for treating type 1 diabetes.

Repaglinide may also be used for purposes not listed in this medication guide.

Important Information

You should not use repaglinide if you have type 1 diabetes, severe liver disease, or diabetic ketoacidosis.

You should not use repaglinide together with gemfibrozil (Lopid) or NPH insulin (such as isophane insulin).

You should not use repaglinide if you are allergic to it, or if you have:

  • severe liver disease;

  • diabetic ketoacidosis (call your doctor for treatment with insulin); or

  • if you also take gemfibrozil.

To make sure repaglinide is safe for you, tell your doctor if you have:

  • liver disease; or

  • if you also take metformin or other diabetes medicines.

Follow your doctor’s instructions about using repaglinide if you are pregnant. Blood sugar control is very important during pregnancy, and your dose needs may be different during each trimester.

It is not known whether repaglinide passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.

Repaglinide is not approved for use by anyone younger than 18 years old.

What should I avoid while taking repaglinide?

Avoid drinking alcohol. It lowers blood sugar and may interfere with your diabetes treatment.

More about repaglinide

  • Side Effects
  • During Pregnancy or Breastfeeding
  • Dosage Information
  • Drug Images
  • Drug Interactions
  • Pricing & Coupons
  • En Español
  • 9 Reviews
  • Drug class: meglitinides
  • Repaglinide
  • Repaglinide (Advanced Reading)

Other brands: Prandin

  • Repaglinide (AHFS Monograph)
  • … +2 more
  • Diabetes, Type 2

What is Repaglinide?

Your doctor will want to check your progress at regular visits, especially during the first few weeks you take this medicine. Blood and urine tests may be needed to check for unwanted effects.

Do not take gemfibrozil (Lopid®) while you are taking this medicine. Using these medicines together may cause unwanted effects.

It is very important to follow carefully any instructions from your health care team about:

  • Alcohol—Drinking alcohol may cause severe low blood sugar. Discuss this with your health care team.
  • Other medicines—Do not take other medicines during the time you are taking repaglinide unless they have been discussed with your doctor. This especially includes nonprescription medicines such as aspirin, and medicines for appetite control, asthma, colds, cough, hay fever, or sinus problems.
  • Counseling—Other family members need to learn how to prevent side effects or help with side effects if they occur. Also, patients with diabetes may need special counseling about diabetes medicine dosing changes that might occur because of lifestyle changes, such as changes in exercise and diet. Furthermore, counseling on contraception and pregnancy may be needed because of the problems that can occur in patients with diabetes during pregnancy.
  • Travel—Keep a recent prescription and your medical history with you. Be prepared for an emergency as you would normally. Make allowances for changing time zones and keep your meal times as close as possible to your usual meal times.

In case of emergency—There may be a time when you need emergency help for a problem caused by your diabetes. You need to be prepared for these emergencies. It is a good idea to wear a medical identification (ID) bracelet or neck chain at all times. Also, carry an ID card in your wallet or purse that says that you have diabetes and a list of all of your medicines.

This medicine may cause hypoglycemia (low blood sugar). This is more common when this medicine is taken together with certain medicines. Low blood sugar must be treated before it causes you to pass out (unconsciousness). People feel different symptoms of low blood sugar. It is important that you learn which symptoms you usually have so you can treat it quickly. Talk to your doctor about the best way to treat low blood sugar.

Hyperglycemia (high blood sugar) may occur if you do not take enough or skip a dose of your medicine, overeat or do not follow your meal plan, have a fever or infection, or do not exercise as much as usual. High blood sugar can be very serious and must be treated right away. It is important that you learn which symptoms you have in order to treat it quickly. Talk to your doctor about the best way to treat high blood sugar.

This medicine may make you dizzy or drowsy. Avoid driving, using machines, or doing anything else that could be dangerous until you know how this medicine affects you.

Identification

Are you a new drug developer? Contact us to learn more about our customized products and solutions. Stay in the know! As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages. #DrugBankUpdates Name Repaglinide Accession Number DB00912 (APRD00439) Type Small Molecule Groups Approved, Investigational Description

Repaglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to β cells of the pancreas to stimulate insulin release. Repaglinide induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal. Approximately one month of therapy is required before a decrease in fasting blood glucose is seen. Meglitnides may have a neutral effect on weight or cause a slight increase in weight. The average weight gain caused by meglitinides appears to be lower than that caused by sulfonylureas and insulin and appears to occur only in those naïve to oral antidiabetic agents. Due to their mechanism of action, meglitinides may cause hypoglycemia although the risk is thought to be lower than that of sulfonylureas since their action is dependent on the presence of glucose. In addition to reducing postprandial and fasting blood glucose, meglitnides have been shown to decrease glycosylated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Meglitinides appear to be more effective at lowering postprandial blood glucose than metformin, sulfonylureas and thiazolidinediones. Repaglinide is extensively metabolized in the liver and excreted in bile. Repaglinide metabolites do not possess appreciable hypoglycemic activity. Approximately 90% of a single orally administered dose is eliminated in feces and 8% in urine.

Structure 3D Download Similar Structures

Structure for Repaglinide (DB00912)

× Close Synonyms

  • Repaglinida
  • Repaglinide
  • Repaglinidum

External IDs AG-EE 388 ZW / AG-EE 623 ZW / AG-EE-623ZW Product Images Prescription Products

Name Dosage Strength Route Labeller Marketing Start Marketing End
Unlock Additional Data
Act Repaglinide Tablet Oral Actavis Pharma Company 2010-10-18 Not applicable Canada
Act Repaglinide Tablet Oral Actavis Pharma Company 2010-10-18 Not applicable Canada
Act Repaglinide Tablet Oral Actavis Pharma Company 2010-10-18 Not applicable Canada
Gluconorm 0.5mg Tablet Oral Novo Nordisk 1999-06-21 Not applicable Canada
Gluconorm 1.0mg Tablet Oral Novo Nordisk 1999-06-21 Not applicable Canada
Gluconorm 2.0mg Tablet Oral Novo Nordisk 1999-06-21 Not applicable Canada
Novonorm Tablet 2 mg Oral Novo Nordisk 1998-08-17 Not applicable EU
Novonorm Tablet 0.5 mg Oral Novo Nordisk 1998-08-17 Not applicable EU
Novonorm Tablet 1 mg Oral Novo Nordisk 1998-08-17 Not applicable EU
Novonorm Tablet 1 mg Oral Novo Nordisk 1998-08-17 Not applicable EU

Additional Data Available

  • Application Number Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products

Name Dosage Strength Route Labeller Marketing Start Marketing End
Unlock Additional Data
Apo-repaglinide Tablet Oral Apotex Corporation 2012-10-16 Not applicable Canada
Apo-repaglinide Tablet Oral Apotex Corporation 2012-10-16 Not applicable Canada
Apo-repaglinide Tablet Oral Apotex Corporation 2012-10-16 Not applicable Canada
Auro-repaglinide Tablet Oral Auro Pharma Inc 2014-04-30 Not applicable Canada
Auro-repaglinide Tablet Oral Auro Pharma Inc 2014-04-30 Not applicable Canada
Auro-repaglinide Tablet Oral Auro Pharma Inc 2014-04-30 Not applicable Canada
Enyglid Tablet 1 mg Oral Krka, D.D., Novo Mesto 2009-10-14 Not applicable EU
Enyglid Tablet 2 mg Oral Krka, D.D., Novo Mesto 2009-10-14 Not applicable EU
Enyglid Tablet 2 mg Oral Krka, D.D., Novo Mesto 2009-10-14 Not applicable EU
Enyglid Tablet 0.5 mg Oral Krka, D.D., Novo Mesto 2009-10-14 Not applicable EU

Additional Data Available

  • Application Number Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code Product Code

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Mixture Products

Name Ingredients Dosage Route Labeller Marketing Start Marketing End
Prandimet Repaglinide (2 mg/1) + Metformin hydrochloride (500 mg/1) Tablet Oral Novo Nordisk 2009-01-15 2017-05-31 US
Prandimet Repaglinide (1 mg/1) + Metformin hydrochloride (500 mg/1) Tablet Oral Novo Nordisk 2009-01-16 2017-05-31 US
Repaglinide and Metformin Hydrochloride Repaglinide (2 mg/1) + Metformin hydrochloride (500 mg/1) Tablet Oral Lupin Pharmaceuticals 2015-12-10 Not applicable US
Repaglinide and Metformin Hydrochloride Repaglinide (1 mg/1) + Metformin hydrochloride (500 mg/1) Tablet Oral Lupin Pharmaceuticals 2015-12-10 Not applicable US

International/Other Brands GlucoNorm (Novo Nordisk) / Surepost Categories UNII 668Z8C33LU CAS number 135062-02-1 Weight Average: 452.5857
Monoisotopic: 452.26750765 Chemical Formula C27H36N2O4 InChI Key FAEKWTJYAYMJKF-QHCPKHFHSA-N InChI InChI=1S/C27H36N2O4/c1-4-33-25-17-20(12-13-22(25)27(31)32)18-26(30)28-23(16-19(2)3)21-10-6-7-11-24(21)29-14-8-5-9-15-29/h6-7,10-13,17,19,23H,4-5,8-9,14-16,18H2,1-3H3,(H,28,30)(H,31,32)/t23-/m0/s1 IUPAC Name 2-ethoxy-4-({butyl]carbamoyl}methyl)benzoic acid SMILES CCOC1=C(C=CC(CC(=O)N(CC(C)C)C2=CC=CC=C2N2CCCCC2)=C1)C(O)=O

Pharmacology

Indication

As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Associated Conditions

  • Type 2 Diabetes Mellitus

Pharmacodynamics

Insulin secretion by pancreatic β cells is partly controlled by cellular membrane potential. Membrane potential is regulated through an inverse relationship between the activity of cell membrane ATP-sensitive potassium channels (ABCC8) and extracellular glucose concentrations. Extracellular glucose enters the cell via GLUT2 (SLC2A2) transporters. Once inside the cell, glucose is metabolized to produce ATP. High concentrations of ATP inhibit ATP-sensitive potassium channels causing membrane depolarization. When extracellular glucose concentrations are low, ATP-sensitive potassium channels open causing membrane repolarization. High glucose concentrations cause ATP-sensitive potassium channels to close resulting in membrane depolarization and opening of L-type calcium channels. The influx of calcium ions stimulates calcium-dependent exocytosis of insulin granules. Repaglinide increases insulin release by inhibiting ATP-sensitive potassium channels in a glucose-dependent manner.

Mechanism of action

Repaglinide activity is dependent on the presence functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, repaglinide has no effect on insulin release in the absence of glucose. Rather, it potentiates the effect of extracellular glucose on ATP-sensitive potassium channel and has little effect on insulin levels between meals and overnight. As such, repaglinide is more effective at reducing postprandial blood glucose levels than fasting blood glucose levels and requires a longer duration of therapy (approximately one month) before decreases in fasting blood glucose are observed. The insulinotropic effects of repaglinide are highest at intermediate glucose levels (3 to 10 mmol/L) and it does not increase insulin release already stimulated by high glucose concentrations (greater than 15 mmol/L). Repaglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.

Target Actions Organism
AATP-binding cassette sub-family C member 8 inhibitor Humans
UPeroxisome proliferator-activated receptor gamma agonist Humans

Unlock Additional Data Additional Data Available Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more Absorption

Rapidly and completely absorbed following oral administration. Peak plasma concentrations are observed within 1 hour (range 0.5-1.4 hours). The absolute bioavailability is approximately 56%. Maximal biological effect is observed within 3-3.5 hours and plasma insulin levels remain elevated for 4-6 hours. When a single 2 mg dose of repaglinide is given to healthy subjects, the area under the curve (AUC) is 18.0 – 18.7 (ng/mL/h)^3.

Volume of distribution

31 L following IV administration in healthy individuals

Protein binding

>98% (e.g. to to albumin and α1-acid glycoprotein)

Metabolism

Repaglinide is rapidly metabolized via oxidation and dealkylation by cytochrome P450 3A4 and 2C9 to form the major dicarboxylic acid derivative (M2). Further oxidation produces the aromatic amine derivative (M1). Glucuronidation of the carboxylic acid group of repaglinide yields an acyl glucuronide (M7). Several other unidentified metabolites have been detected. Repaglinide metabolites to not possess appreciable hypoglycemic activity.

  • Repaglinide hydroxyrepaglinide
  • Repaglinide repaglinide aromatic amine

Route of elimination

90% eliminated in feces (<2% as unchanged drug), 8% in urine (0.1% as unchanged drug)

Half life

1 hour

Clearance

33-38 L/hour following IV administration

Toxicity

LD50 >1 g/kg (rat) (W. Grell)

Affected organisms

  • Humans and other mammals

Pathways

Pathway Category
Repaglinide Action Pathway Drug action

Pharmacogenomic Effects/ADRs Not Available

Interactions

Drug Interactions This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

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  • Approved
  • Vet approved
  • Nutraceutical
  • Illicit
  • Withdrawn
  • Investigational
  • Experimental
Drug Interaction
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(R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Repaglinide.
(S)-Warfarin The metabolism of (S)-Warfarin can be decreased when combined with Repaglinide.
2,4-thiazolidinedione The risk or severity of hypoglycemia can be increased when Repaglinide is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinoline The therapeutic efficacy of Repaglinide can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
6-Deoxyerythronolide B The serum concentration of Repaglinide can be increased when it is combined with 6-Deoxyerythronolide B.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Repaglinide.
Abatacept The metabolism of Repaglinide can be increased when combined with Abatacept.
Abiraterone The metabolism of Repaglinide can be decreased when combined with Abiraterone.
Acarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Repaglinide.
Acebutolol The therapeutic efficacy of Repaglinide can be increased when used in combination with Acebutolol.

Additional Data Available

  • Extended Description Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level Evidence Level

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Food Interactions

  • Take up to 30 minutes before meals.
  • When taken with a high-fat meal, AUC and Cmax decreases.

Synthesis Reference US20040102477 General References External Links Human Metabolome Database HMDB0015048 KEGG Drug D00594 KEGG Compound C07670 PubChem Compound 65981 PubChem Substance 46508150 ChemSpider 59377 BindingDB 50153520 ChEBI 8805 ChEMBL CHEMBL1272 Therapeutic Targets Database DAP000133 PharmGKB PA451234 HET BJX RxList RxList Drug Page Drugs.com Drugs.com Drug Page PDRhealth PDRhealth Drug Page Wikipedia Repaglinide ATC Codes A10BD14 — Metformin and repaglinide

  • A10BD — Combinations of oral blood glucose lowering drugs
  • A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
  • A10 — DRUGS USED IN DIABETES
  • A — ALIMENTARY TRACT AND METABOLISM

A10BX02 — Repaglinide

  • A10BX — Other blood glucose lowering drugs, excl. insulins
  • A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
  • A10 — DRUGS USED IN DIABETES
  • A — ALIMENTARY TRACT AND METABOLISM

AHFS Codes

  • 68:20.16 — Meglitinides

PDB Entries 6jb1 / 6jb3 / 6pz9 FDA label (175 KB) MSDS (57.3 KB)

Clinical Trials

Clinical Trials

Phase Status Purpose Conditions Count
1 Active Not Recruiting Treatment Advanced Solid Tumors / Lymphoma, Large B-Cell, Diffuse (DLBCL) / Mantle Cell Lymphoma (MCL) / Marginal Zone Lymphoma / Primary Mediastinal Lymphoma 1
1 Completed Basic Science Drug Drug Interaction (DDI) / Healthy Volunteers 1
1 Completed Basic Science Healthy Volunteers / Pharmacokinetics of Caffeine / Pharmacokinetics of Repaglinide 1
1 Completed Treatment Diabetes / Healthy Volunteers 1
1 Completed Treatment Diabetes / Type 2 Diabetes Mellitus 2
1 Completed Treatment Drug Drug Interaction (DDI) 1
1 Completed Treatment Healthy Adult Subjects 1
1 Completed Treatment Healthy Volunteers 1
1 Completed Treatment Parkinson’s Disease (PD) 1
1 Completed Treatment Type 2 Diabetes Mellitus 1
2 Completed Treatment Type 2 Diabetes Mellitus 1
3 Completed Prevention Atherosclerosis / Cardiovascular Heart Disease / Coronary Heart Disease (CHD) / Diabetes Mellitus / High Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus 1
3 Completed Treatment Cystic Fibrosis (CF) / Diabetes Mellitus 2
3 Completed Treatment Diabetes / Type 2 Diabetes Mellitus 2
4 Active Not Recruiting Treatment Type 2 Diabetes Mellitus 1
4 Completed Treatment Diabetes Mellitus 1
4 Completed Treatment Diabetes / Type 2 Diabetes Mellitus 10
4 Completed Treatment Type 2 Diabetes Mellitus 5
4 Terminated Treatment Diabetes / Type 2 Diabetes Mellitus 1
4 Unknown Status Treatment Type 2 Diabetes Mellitus 1
Not Available Completed Not Available Cystic Fibrosis Related Diabetes / Pancreatic Insufficiency 1
Not Available Completed Not Available Diabetes / Type 2 Diabetes Mellitus 6
Not Available Completed Not Available Type 2 Diabetes Mellitus 3
Not Available Completed Treatment Diabetes 1
Not Available Unknown Status Not Available Type 2 Diabetes Mellitus 1
Not Available Withdrawn Treatment Diabetes 1

Pharmacoeconomics

Manufacturers

  • Novo nordisk inc
  • Novo Nordisk Inc.

Packagers

  • Boehringer Ingelheim Ltd.
  • Cardinal Health
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Novo Nordisk Inc.
  • Recipharm AB

Dosage forms

Form Route Strength
Tablet Oral 0.5 mg
Tablet Oral 1 mg
Tablet Oral 2 mg
Tablet Oral
Tablet Oral
Tablet Oral 0.5 mg/1
Tablet Oral 1 mg/1mg
Tablet Oral 1 mg/1
Tablet Oral 2 mg/1mg
Tablet Oral 2 mg/1

Prices

Unit description Cost Unit
Prandin 1 mg tablet 2.48USD tablet
Prandin 0.5 mg tablet 2.47USD tablet
Prandin 2 mg tablet 2.33USD tablet
Gluconorm 2 mg Tablet 0.34USD tablet
Gluconorm 1 mg Tablet 0.32USD tablet
Gluconorm 0.5 mg Tablet 0.31USD tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only. Patents

Patent Number Pediatric Extension Approved Expires (estimated)
Unlock Additional Data
US6677358 No 2004-01-13 2018-06-12 US
CA2111851 No 2002-02-26 2011-06-21 Canada

Additional Data Available

  • Filed On Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State Solid Experimental Properties

Property Value Source
melting point (°C) 130-131 °C Not Available
logP 5.9 Not Available

Predicted Properties

Property Value Source
Water Solubility 0.00294 mg/mL ALOGPS
logP 5.05 ALOGPS
logP 3.95 ChemAxon
logS -5.2 ALOGPS
pKa (Strongest Acidic) 3.68 ChemAxon
pKa (Strongest Basic) 4.82 ChemAxon
Physiological Charge -1 ChemAxon
Hydrogen Acceptor Count 5 ChemAxon
Hydrogen Donor Count 2 ChemAxon
Polar Surface Area 78.87 Å2 ChemAxon
Rotatable Bond Count 10 ChemAxon
Refractivity 131.83 m3·mol-1 ChemAxon
Polarizability 51.49 Å3 ChemAxon
Number of Rings 3 ChemAxon
Bioavailability 1 ChemAxon
Rule of Five Yes ChemAxon
Ghose Filter No ChemAxon
Veber’s Rule No ChemAxon
MDDR-like Rule Yes ChemAxon

Predicted ADMET features

Property Value Probability
Human Intestinal Absorption + 0.9172
Blood Brain Barrier 0.7101
Caco-2 permeable 0.5891
P-glycoprotein substrate Substrate 0.8145
P-glycoprotein inhibitor I Inhibitor 0.6044
P-glycoprotein inhibitor II Inhibitor 0.6868
Renal organic cation transporter Non-inhibitor 0.849
CYP450 2C9 substrate Non-substrate 0.8288
CYP450 2D6 substrate Non-substrate 0.9117
CYP450 3A4 substrate Substrate 0.7019
CYP450 1A2 substrate Non-inhibitor 0.9206
CYP450 2C9 inhibitor Non-inhibitor 0.907
CYP450 2D6 inhibitor Non-inhibitor 0.9231
CYP450 2C19 inhibitor Non-inhibitor 0.9026
CYP450 3A4 inhibitor Non-inhibitor 0.9264
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8682
Ames test Non AMES toxic 0.8136
Carcinogenicity Non-carcinogens 0.8004
Biodegradation Not ready biodegradable 0.919
Rat acute toxicity 2.4497 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9605
hERG inhibition (predictor II) Non-inhibitor 0.5272

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST) Not Available Spectra

Taxonomy

Description This compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group. Kingdom Organic compounds Super Class Organoheterocyclic compounds Class Piperidines Sub Class Phenylpiperidines Direct Parent Phenylpiperidines Alternative Parents Phenylacetamides / Benzoic acids / Aniline and substituted anilines / Benzoyl derivatives / Dialkylarylamines / Phenol ethers / Phenoxy compounds / Alkyl aryl ethers / Amino acids / Secondary carboxylic acid amidesCarboxylic acids / Monocarboxylic acids and derivatives / Azacyclic compounds / Hydrocarbon derivatives / Carbonyl compounds / Organic oxides / Organopnictogen compounds show 7 more Substituents Phenylpiperidine / Phenylacetamide / Benzoic acid or derivatives / Benzoic acid / Phenoxy compound / Benzoyl / Phenol ether / Tertiary aliphatic/aromatic amine / Dialkylarylamine / Aniline or substituted anilinesAlkyl aryl ether / Benzenoid / Monocyclic benzene moiety / Amino acid / Tertiary amine / Carboxamide group / Amino acid or derivatives / Secondary carboxylic acid amide / Monocarboxylic acid or derivatives / Ether / Carboxylic acid / Carboxylic acid derivative / Azacycle / Organonitrogen compound / Hydrocarbon derivative / Carbonyl group / Amine / Organic oxide / Organopnictogen compound / Organooxygen compound / Organic oxygen compound / Organic nitrogen compound / Aromatic heteromonocyclic compound show 23 more Molecular Framework Aromatic heteromonocyclic compounds External Descriptors piperidines (CHEBI:8805)

Targets

Kind Protein Organism Humans Pharmacological action Yes Actions Inhibitor General Function Sulfonylurea receptor activity Specific Function Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release. Gene Name ABCC8 Uniprot ID Q09428 Uniprot Name ATP-binding cassette sub-family C member 8 Molecular Weight 176990.36 Da Kind Protein Organism Humans Pharmacological action Unknown Actions Agonist General Function Zinc ion binding Specific Function Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE… Gene Name PPARG Uniprot ID P37231 Uniprot Name Peroxisome proliferator-activated receptor gamma Molecular Weight 57619.58 Da

  1. Scarsi M, Podvinec M, Roth A, Hug H, Kersten S, Albrecht H, Schwede T, Meyer UA, Rucker C: Sulfonylureas and glinides exhibit peroxisome proliferator-activated receptor gamma activity: a combined virtual screening and biological assay approach. Mol Pharmacol. 2007 Feb;71(2):398-406. Epub 2006 Nov 2.

Enzymes

Kind Protein Organism Humans Pharmacological action Unknown Actions Substrate General Function Vitamin d3 25-hydroxylase activity Specific Function Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react… Gene Name CYP3A4 Uniprot ID P08684 Uniprot Name Cytochrome P450 3A4 Molecular Weight 57342.67 Da Kind Protein Organism Humans Pharmacological action Unknown Actions Substrate General Function Steroid hydroxylase activity Specific Function Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un… Gene Name CYP2C8 Uniprot ID P10632 Uniprot Name Cytochrome P450 2C8 Molecular Weight 55824.275 Da

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1.
  2. Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT: CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol. 2003 Sep;56(3):305-14.
  3. Flockhart Table of Drug Interactions

Carriers

Details1. Serum albumin Kind Protein Organism Humans Pharmacological action Unknown General Function Toxic substance binding Specific Function Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid… Gene Name ALB Uniprot ID P02768 Uniprot Name Serum albumin Molecular Weight 69365.94 Da

Transporters

Kind Protein Organism Humans Pharmacological action Unknown Actions Substrate General Function Sodium-independent organic anion transmembrane transporter activity Specific Function Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland… Gene Name SLCO1B1 Uniprot ID Q9Y6L6 Uniprot Name Solute carrier organic anion transporter family member 1B1 Molecular Weight 76447.99 Da Kind Protein Organism Humans Pharmacological action No Actions Substrate General Function Transporter activity Specific Function Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes. Gene Name ABCB11 Uniprot ID O95342 Uniprot Name Bile salt export pump Molecular Weight 146405.83 Da ×Unlock Data

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Drug created on June 13, 2005 07:24 / Updated on February 02, 2020 00:22

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