Glimepiride side effects and drug information

Glimepiride is a drug that is intended to be used for patients with type 2 diabetes. It is administered orally and works best if combined with exercise and diet as it will help improve blood sugar control in adults.

Trade NameAmaryl
FormulaC24H34N4O5S
Molar mass490.617 g/mol
CAS ID93479-97-1
MetabolismComplete Liver (1st stage through CYP2C9)

Important Information

This medication should not be used by people who are allergic to sulfa drugs and those who have diabetic ketoacidosis.

Side Effects

Glimepiride may cause some potential side effects that can range from the common ones to the rare types.  

Some of its most common side effects include the following:

  • Hypoglycemia
  • Leukopenia
  • Dizziness
  • Thrombocytopenia
  • Vomiting
  • Kidney enzyme deficiency reactions
  • Weight gain
  • Weakness
  • Headache
  • Pancytopenia
  • Nausea
  • Elevation of enzyme levels
  • Decreased immunity
  • Low sodium levels
  • Allergic skin reaction
  • Diarrhea
  • Pain in the gastrointestinal area
  • Cholestasis
  • Aplastic anemia

Though very rare, it has the possibility of causing jaundice as a side effect of the drug.

Post Marketing Side Effects:

  • Serious hypersensitivity reactions
  • Hemolytic anemia
  • Liver impairment that may lead to liver failure
  • Blistering skin lesions
  • Sensitivity to light
  • Allergic inflammation of the blood vessels
  • Leukopenia
  • Reduced immunity
  • Aplastic anemia
  • Pancytopenia
  • Thrombocytopenia
  • Hepatic porphyria
  • Hyponatremia
  • Distortion of taste
  • Alopecia

Dosage and Administration

The data on Glimepiride’s dosage and administration are based on the average doses only, but dosages may vary according to the patient’s condition and response to the medication.

Usual Adult Dose for Type 2 Diabetes:

The usual initial dose given for an adult is about 1 to 2mg, and the dosage may be adjusted and increased no more than the interval of every 1 to 2 weeks, depending on the glycemic response of the patient. The maximum dosage allowed is 8mg daily.

Comments:

Glimepiride should be administered along with the patient’s breakfast or the first main meal of the day.

People who are at an increased risk for hypoglycemia should have an initial dose of 1mg through oral administration once a day.

For patients who will be shifting to this medication from a longer half-life sulfonylurea, close monitoring for about 1 to 2 weeks must be done to check if there are overlapping side effects.

Usual Geriatric Dose for Type 2 Diabetes:

For the initial dosage of the elderly, give 1mg once a day through oral administration, then adjust the dosage slowly along with close monitoring.

Usual Pediatric Dose for Type 2 Diabetes:

This drug is not advised for younger patients as it may cause unfavorable reactions on their body weight and may result in hypoglycemia.

Renal Dose Adjustments:

The initial dosage for this kind of treatment is 1mg through oral administration, then maybe adjusted later on but with close monitoring of the patient.

Liver Dose Adjustments:

For this type of treatment, usage of this drug must be used with great caution.

Drug Interaction

Glimepiride may cause some interactions; it is important that you should always consult with your health care provider first before making any changes to your dosage, or before starting or stopping the use of this drug.  

This medication has at least 146 moderate interactions with other medicines, and about 89 mild interactions with other drugs.

Glimepiride may cause some serious interactions with:

  • Ethanol
  • Aminolevulinic acid
  • Methyl aminolevulinate
  • Ivacaftor/ lumacaftor

Warnings and Precautions

Warnings:

Before taking this product, read the label first and consult your doctor if it is safe for you, and keep in mind the following:

  • If you are allergic to Glimepiride or any of its components, do not take Amaryl.
  • Make sure to always keep this product out of children’s reach
  • In case of overdose, seek medical help immediately or contact the poison control center.

Contraindications:

This medication may not work well with conditions such as:

  • Type 1 diabetes
  • Complicated gestational diabetes mellitus
  • Hypersensitivity
  • Diabetic ketoacidosis either with or without coma

Cautions:

Glimepiride must be used with great caution by people with conditions that include:

  • Those who are at an increased risk of having low blood sugar 
  • Those who are debilitated, underweight or malnourished, and the elderly
  • Those who are under stress because of surgery, trauma, fever, or infection. If the patient is exposed to stress, it is advised that insulin must be used instead of this drug.
  • Those with liver or kidney issues
  • Those who are pregnant
  • Those who are breastfeeding
  • Those who are at a high risk of experiencing cardiovascular mortality
  • Those who are allergic to other sulfonamide derivatives
  • Those who have issues with fluid retention as it may lead to heart failure

When used along with sulfonylurea agents, it may cause damage to the red blood cells. And when used in combination with insulin, there may be a higher risk of experiencing other cardiovascular effects.  

This medication may also increase the risk of having ischemic cardiovascular reactions, and may cause fluid build-up in the eye as well. Using Glimepiride should be used with caution as it may cause reactions such as weight gain, anemia, and dose-related edema, increased incidence of bone fracture, severe allergic reactions, rapid swelling, or Stevens-Johnson syndrome. If the latter happens, stop taking this drug and use an alternative treatment.

Overdose and Contraindications

The use of Glimepiride may result in unfavorable reactions if the patient has hypersensitivity to this drug or any of its components. It also interacts with other drugs that contain sulfonamides.  

Though information on allergenic cross-sensitivity for the drugs in this classification is not enough, because of similarity in nature of their chemical structure and pharmacologic reactions, possibilities of cross-sensitivity cannot be rejected.

For Canadian labeling, other additional contraindications that are not on the US labels are added. Additions include pregnancy, breastfeeding, Type 1 diabetes, severe renal or hepatic impairment, and diabetes ketoacidosis that comes with or without coma.

Clinical Pharmacology

Glimepiride encourages the release of insulin from the pancreatic beta cells as well as lessens the glucose output that’s coming from the liver. This drug increases insulin sensitivity in peripheral target areas.

Its absorption rate is 100%, and it is expected to take effect about 2 to 3 hours after intake. This drug is mostly excreted through urine with 60 to 90% as M1 and M2 metabolites, and also through feces but with only 40 to 70% as M1 and M2 metabolites.