Repaglinide: The Side Effects Of A Postprandial Blood Glucose Regulator
blog detail banner

Drug Side Effects

Side Effects of Postprandial Blood Glucose Regulators (Repaglinide)

Nov 25, 2016

What Is Repaglinide?

Repaglinide is a meglitinide class drug that is used to lower blood glucose in the treatment of T2D. It is administered orally. Postprandial Blood Glucose Regulators (Glinides) are chemicals that stimulate the beta cells in the pancreas to produce more insulin. Glinides, or postprandial (meaning “after meal”) glucose regulators, are usually taken half an hour before food. This helps to increase the amount of insulin available to escort the glucose produced after meals into the cells. Thus, it prevents the build-up of sugar in the blood.

Glinides are often prescribed to patients who need drugs to stimulate their pancreas to produce more insulin (such as sulfonylureas) but have an allergy to sulfa drugs.

Mechanism of Action

Repaglinide lowers blood glucose levels by triggering the release of insulin from the pancreas. They can only act in the presence of functioning beta cells present in the pancreatic islets. The insulin mediated by Repaglinide is glucose-dependent and diminishes as glucose levels get lower.

How Should This Medicine Be Used?

Repaglinide is available as a tablet to be taken orally. The doses should be taken before meals – any time from 30 minutes before a meal to just before the meal. Repaglinides work only when you consume food. So, if you miss a meal, you need to miss the dose of repaglinide as well. Conversely, if you eat an additional meal, you will need to take an additional dose of repaglinide. Depending on how you respond, your healthcare provider may or may not, gradually, increase your dose. Follow the instructions written on your prescription label carefully. Also, ask your healthcare practitioner or pharmacist to explain any part you do not understand. Take repaglinide exactly as directed, do not take higher or lower amounts of any dosage. Preferably, stick to the dosage directed to you by your healthcare practitioner / the package label / patient information leaflet.

You need to continue taking repaglinide even if you feel well. Do not stop taking repaglinide without talking to your healthcare practitioner.

Most Prescribed Names In This Category of Drugs Include

  • Prandin
  • Starlix Rapamon
  • Regan
  • Glinate 120
  • Nebicard
  • Natiz 60

Postprandial Blood Glucose Regulators (Repaglinide) Side Effects

The common side effects of Repaglinide are:

  • Digestive issues – Including diarrhea, constipation and abdominal pain.
  • Low blood sugar – Can cause shaking, palpitations, dizziness, extreme hunger, fuzzy vision, fainting, etc.
  • Allergic reactions – Including a stuffy nose, cold-like symptoms, etc.
  • Cardiovascular issues – Including palpitations, a racing heart and other heart-related issues.

The reason these side effects occur are also explained in detail below. Equally important, but often ignored, are the side effects that come from long term usage of this medication. They are caused due to vital nutrients being taken away from the body.

Digestive Issues

The most common Repaglinide side effects involve the digestive tract. You could face diarrhea, constipation, nausea or abdominal pain.

Low Blood Sugar or Hypoglycemia

Low Blood Sugar is a common side-effect of Postprandial Blood Glucose Regulators

Low Blood Sugar is a common side-effect of Postprandial Blood Glucose Regulators

Glinides belong to a class of drugs known as secretagogues. They enhance the secretion of insulin in the blood stream, just before food. They act fast, so sugar levels can drop rapidly when you take them. Hypoglycemia could manifest in shaking, palpitations, dizziness, extreme hunger and tiredness. It is a common long-term effect of glinide usage.

Allergic Reactions

Some allergic skin reactions and symptoms, such as a runny or stuffy nose, sneezing and sore throat, could also occur. Liver problems caused due to allergic reactions are uncommon in this category, but occur nonetheless.

How Can You Deal With These Side Effects Successfully?

If you face any of these adverse effects, you should inform your healthcare practitioner immediately. This is especially true for those having a liver condition. The only short-term solution that may exist is to change your drug and that is a decision your healthcare practitioner can help you with. You should also maintain a postprandial blood sugar level chart to monitor your glucose levels. This will point out deviations and help you gauge the efficacy of your anti-diabetic medication.

Should You Be Using Glinides Over The Long Term?

Generally, glinides are prescribed to those diabetics who are allergic to sulfonylureas. However, research shows that due to hypoglycemia, they can cause adverse effects too. Patients who use glinides for a long period may suffer from other health complications, as a result of vital nutrients being removed from the body.

Side Effects Of Long Term Use of Repaglinide (Glinides)

CoQ10 depletion is a major cause of the side effects experienced due to the usage of Repaglinide. Here is a list of common symptoms that you might experience if you’ve been taking Repaglinide (or glinides) for a long time:

Tiredness

Does a regular day at the office makes you feel more tired than usual? It could be due to the depletion of Coenzyme Q10. CoQ10 is involved in the energy production for muscles and the depletion of this important coenzyme can cause fatigue, tiredness and lethargy.

Digestive Issues

Have stomach ache, nausea and constipation been plaguing you recently? Your drug could be the cause of that. Glinides are known to deplete CoQ10, which is an important coenzyme in the digestive process as well. Gingivitis or gum problems could also occur due to CoQ10 depletion.

Cardiac Trouble and Muscle Pain

Unexplained muscle pain could, also, be due to CoQ10 depletion. CoQ10 is one of the most important nutrients in the body since it is used as a coenzyme for energy production. Being the most demanding muscle in the body, an energy crunch hits the heart hard. A lack of CoQ10 can cause high blood pressure, angina and serious conditions, like congestive heart failure.

What You Can Do About It

Replenishing your body’s stock of vital nutrients can help you cope with some of these nutrient-depletion symptoms. These dietary supplements are safe, however, it’s advisable to involve your medical practitioner, especially if you’re on prescription medications.

What May Help (Per Day)

CoQ10: 30-200 mcg

Research shows that supplementing can help you mitigate risks and protect your body from the side effects associated with using prescription drugs.

What Are The Special Precautions You Should Follow?

Before taking Repaglinide,

  • Inform your healthcare practitioner and pharmacist about being allergic to repaglinide or any other drugs.
  • Inform your healthcare practitioner if you are taking gemfibrozil (sold as Lopid). Your doctor will, most probably, advise you to not take repaglinide if you are already on this medication.
  • Inform your healthcare practitioner and pharmacist about all the prescription and non-prescription medications, vitamins, nutritional supplements and herbal products you are taking or plan to take.

Be sure to mention  the following, if you have been / will be using them:

  • Acetophenazine (Tindal)
  • Aspirin
  • Blood pressure medicines
  • Carbamazepine (Tegretol)
  • Chloramphenicol (Chloromycetin)
  • Chlorpromazine (Thorazine)
  • Corticosteroids
  •  Diuretics (water pills)
  • Drugs for arthritis
  • Erythromycin
  • Troglitazone (Rezulin)
  • Estrogens
  • Fluphenazine (Prolixin)
  • Isoniazid (Rifamate)
  • Ketoconazole (Nizoral)
  • Mesoridazine (Serentil)
  • Oral contraceptives
  • Perphenazine (Trilafon)
  • Phenelzine (Nardil)
  • Phenobarbital (Luminal)
  • Phenytoin (Dilantin)
  • Probenecid (Benemid)
  • Prochlorperazine (Compazine)
  • Promazine (Sparine)
  • Promethazine (Phenergan)
  • Rifampin (Rifadin, Rimactane)
  • Thioridazine (Mellaril)
  • Tranylcypromine (Parnate)
  • Trifluoperazine (Stelazine)
  • Triflupromazine (Vesprin)
  • Trimeprazine (Temaril)
  • Vitamins or warfarin (Coumadin)

Your doctor may need to change your Repaglinide dosage, or monitor you carefully for side effects, when you use it in along with the above mentioned medications. Also, inform your healthcare practitioner, if you:

  • Have or have ever had liver or kidney disease.
  • Have been told you have Type 1 diabetes mellitus.
  • Are pregnant, plan to become pregnant or are breast-feeding. If you become pregnant while taking repaglinide, call your doctor.
  • Are going to undergo surgery, including dental surgery, and let the doctor (or dentist) know that you are taking repaglinide.

What Should You Do If You Forget A Dose?

If you have just begun to have a meal, take the missed dose as soon as you remember it. However, if you have finished eating, skip the missed dose and continue dosing as per your regular schedule. Do not take a double dose to compensate for the missed one.

What You Should Know About The Storage And Disposal Of This Medication

  • Store this medication in the bottle you got it in, with the lid tightly closed and the bottle out of the reach of children.
  • Store it at 20-25 ̊C (68-77 ̊F), that is, at room temperature.
  • Protect the bottles from moisture.

Dietary Considerations While Medicating

Make sure you follow all the exercise and dietary recommendations made by your healthcare practitioner or dietitian. It is very important to follow a healthy diet.

Alcohol may bring down your blood sugar level. Ask your healthcare practitioner about the effects of consuming alcoholic beverages while you are taking Repaglinide.

What Are The Ingredients In Repaglinide Tablets?

Repaglinide tablets contain 1 or 2 mg of Repaglinide, along with the inactive ingredients (also termed as excipients). Generally, these excipients are dicalcium phosphate (anhydrous), microcrystalline cellulose, corn starch, meglumine, croscarmellose sodium, povidone, poloxamer, magnesium stearate and colloidal silicon dioxide. The 1 and 2 mg tablets contain iron oxides (yellow and red, respectively) as coloring agents.

Drug Interactions

Gemfibrozil and Itraconazole:

Co-administration of gemfibrozil (600 mg), or itraconazole, or both, with a single dose (0.25 mg) of Repaglinide resulted in an increase in the concentration of Repaglinide in blood plasma, with respect to time.

Fenofibrate:

When fenofibrate is co-administered with a single dose (0.25 mg) of Repaglinide, the repaglinide concentration in blood plasma remains unchanged.

Ketoconazole

Co-administration of ketoconazole and a single (2 mg) dose of Repaglinide resulted in an increase in Repaglinide concentration in blood plasma remains unchanged. (Does not make sense)

Who Should Not Take Repaglinide?

Do not take Repaglinide if –

  • You are allergic to it, or to any of the other substances present in it.
  • You have Type 1 diabetes.
  • The acid level in your blood is on the higher side (diabetic ketoacidosis).
  • If you have a severe liver disease.
  • If you are consuming gemfibrozil (a medicine that is used to lower fat levels in the blood).

Lab Test Considerations

Responses to all diabetic therapies should be monitored by periodic measurements of fasting blood glucose and hemoglobin levels. The goal is to decrease them and bring them towards the normal range.

During dose adjustment, fasting glucose can be used to determine the therapeutic response. Thereafter, both, glucose and hemoglobin, should be monitored. Hemoglobin may, especially, be useful for evaluating long-term sugar control. Post-meal glucose level testing may be clinically helpful in patients whose pre-meal blood glucose levels are satisfactory, but whose overall glycemic control (HbA1c) is inadequate.

Parting Thoughts

Remember, the biggest weapon in the fight against diabetes is KNOWLEDGE.

A positive mental attitude, also, plays a key role in fighting diabetes. Diabetes is a dietary disorder which can be reversed through a healthy, balanced diet and healthy lifestyle choices. Dietary supplements can be of additional help by reducing the side effects of prescription anti-diabetic medication. They protect the body from long-term health complications as well. Intermittent fasting, exercise, yoga, meditation and losing weight can also have tremendous benefits.

Nachiket Rajadhyaksha
Nachiket holds a first class degree in Pharmacy and is passionate about writing. He believes that subject experts must simplify medical concepts to make them interesting and accessible to everyone.

References:

1.Drug-Induced Nutrient Depletion Handbook: Ross Pelton, James B. LaValle, Ernest B. Hawkins, Daniel L.Krinsky , 2nd Edition. Supplement Your Prescription: Hyla Cass, M.D.