Glyburide Side Effects
Glyburide, also known as Glibenclamide is an oral blood glucose lowering medication which belongs to a class of drugs called Sulfonylureas which are used for treatment of type 2 diabetes mellitus (T2DM).
Glyburide is sold under the brand names Micronase, PresTab, DiaBeta and Glynase.
According to the US Food and Drug Administration (FDA), Glyburide is used as an adjunct to exercises and diet for treatment of type 2 diabetes mellitus (T2DM), or non-insulin dependent diabetes mellitus (NIDDM). T2DM or NIDDM is a subtype of diabetes mellitus (DM) which usually affects adults more than children. NIDDM is characterized by loss of weight, polyuria (frequent urination), polyphagia (increased hunger), polydipsia (excessive thirst) and paresthesia (tingling and numbness sensation in the hands and or legs).
Glyburide is available in the form of 1¼ mg, 2½ mg and 5 mg tablets. For treatment of type 2 DM in adult patients, Glyburide is usually started in a dose of 2.5 mg daily, given with the first main meal, or breakfast. The dose may be increased if needed to a maximum daily dose of 20 mg.
Safety and effectiveness of Glyburide in young children have not been established yet.
The most commonly reported Glyburide side effects include nausea, abdominal discomfort, heart burn, diarrhea, weight gain, blurring of vision, skin rash, headache and drowsiness.
In 1966, Glyburide was developed in a cooperative study between Hoechst and Boehringer Mannheim. As of 2003, in the United States, Glyburide was the most popular sulfonylurea.
Glyburide is also available in combination with metformin (oral blood glucose lowering drug) under the brand names Glibomet and Glucovance.
Black Box Warnings: Black box warnings for this drug are currently not available.
Common Glyburide Side Effects
Gastrointestinal Tract (GIT):
- Heart burn
- Dyspepsia (stomach upset or indigestion)
- Abnormal liver function tests, such as elevated ALT (Alanine aminotransferase) and AST (Aspartate aminotransferase)
- Hypoglycemia (low blood glucose level)
- Fluctuation in blood glucose levels
- Increased appetite
- Weight gain
- Blurring of vision
- Photosensitivity (oversensitivity of eyes to light)
- Myalgia (muscle pain)
- Arthralgia (joint pain)
Other Common Glyburide Side Effects
- Central Nervous System (CNS): drowsiness and headache
- Allergic reactions, such as skin rash, itching, or urticarial,
Serious Glyburide Side Effects
Gastrointestinal Tract (GIT):
- Pancreatitis (inflammation of the pancreas which may be life-threatening)
- Hepatitis (inflammation of the liver, which may progress to liver failure)
- Cholestatic jaundice (yellowness of the skin, mucous membranes and whites of the eyes due to accumulation of certain pigments in the blood)
- Syndrome of inappropriate antidiuretic hormone hypersecretion (SIADH, endocrine disorder caused by excessive secretion of antidiuretic hormone and characterized by retention of water and decreased sodium level in the blood. –
- Brain swelling and coma may occur if the condition is left untreated)
- Aplastic anemia (serious disorder characterized by failure of the bone marrow to produce sufficient new cells to replenish blood cells)
- Hemolytic anemia (type of anemia caused by premature break down of red blood cells “RBCs”)
- Pancytopenia (reduction in the number of red blood cells, white blood cells and platelets)
- Thrombocytopenia (reduction in the number of platelets which may lead to spontaneous internal, or external bleeding if left untreated)
- Leukopenia (reduction in the number of white blood cells which may lead to recurrent infections if left untreated)
- Agranulocytosis (reduction in the number of granulocytes which may lead to suppression of immune system if left untreated)
Other Serious Glyburide Side Effects:
- Hyponatremia (decreased sodium level in the blood)
- Disulfiram-like reaction (drowsiness, headache and garlic or metallic taste in the mouth)
Glyburide Contraindications, Cautions, and Drug Interactions:
It is contraindicated for people who have any of the following disorders to take Glyburide:
- Known hypersensitivity or allergy to Glyburide
- Type 1 diabetes mellitus (T1DM), or insulin-dependent diabetes mellitus (IDDM). T1DM, or IDDM is a subtype of diabetes mellitus (DM) which usually affects children more than adults
- Diabetic ketoacidosis (DKA, a life-threatening complication of diabetes mellitus characterized by nausea, vomiting, high blood glucose level, drowsiness and disturbed consciousness)
- Creatinine clearance (CrCl) less than 50 mL/minute
Glyburide should be used with caution in people who have any of the following disorders:
- Known hypersensitivity or allergy to Sulphonamides
- Severe impairment of kidney function
- Severe impairment of liver function
- Severe heart diseases
- Severe infection or injury
- Thyroid gland diseases
- Adrenal gland insufficiency (medical disorder in which the adrenal glands, located above the kidneys, do not produce sufficient amounts of steroid hormones)
- Autonomic neuropathy (nerve disorder that affects involuntary body functions, such as blood pressure, heart rate, digestion and respiration)
- Glucose-6-phosphate dehydrogenase (G6PD) deficiency
Caution should be exercised when Glyburide is used in elderly or debilitated patients.
It is contraindicated to use Glyburide at the same time with any of the following medications:
- Bosentan (Tracleer)
- Ritonavir (Norvir)
- Tipranavir (Aptivus)
It is better to avoid using Glyburide with any of the following medications at the same time:
- Ethanol (drinking alcohol, pure alcohol, grain alcohol or ethyl alcohol)
- Medications for mental diseases, like atypical antipsychotics, such as Abilify, Zyprexa, or Clozaril
- Angiotensin-converting enzyme inhibitors (ACEIs), such as captopril, enalapril, or lisinopril
- Non-steroidal anti-inflammatory drugs (NSAIDs), such as Baclofen (Lioresal) and Naproxen (Midol, Aleve, Naprosyn, or Wal-Proxen)
- Female hormones, such as progestins, estrogens, or birth control pills
- Male hormones, such as androgens, or anabolic steroids
- Quinolone antibiotics, such as ofloxacin, ciprofloxacin, or levofloxacin
- Diuretics (water pills)
- Topical aminolevulinic acid (Levulan Kerastick)
- Nateglinide (Starlix)
- Acarbose (Precose)
- Aloe gel
- Aprepitant (Emend, Emend 3-Day)
- Atazanavir (Reyataz)
The aforementioned Glyburide Contraindications, Cautions, and Drug Interactions are examples of the most ones. For a complete list see the manufacturer’s prescriber guidelines, and for specific concerns consult your physician or pharmacist.
Glyburide works by stimulating pancreatic islet beta cells to release insulin. Insulin lowers blood glucose levels and controls diabetes mellitus (DM). In addition to its blood glucose lowering effect, Glyburide produces a mild diuresis by increasing renal free water clearance. Glyburide is metabolized through the liver. An enzyme called 2C9, which belongs to a group of enzymes collectively known as cytochrome P450 (CYP 450), plays a major role in Glyburide metabolism. The plasma half-life of the drug is about 10 hours. Glyburide is excreted in the urine and bile, about 50% by each route. This dual excretory pathway is different from that of other Sulfonylureas, which are excreted mainly in the urine.
Pregnancy and Lactation:
Glyburide is categorized by the US Food and Drug Administration (FDA) as a pregnancy class C medication, meaning that it may be unsafe for pregnant women to take Glyburide. Studies have been performed in rabbits and rats and have revealed no evidence of harm to the fetus or impaired fertility due to Glyburide. However, studied in pregnant women are not adequate. Because animal studies are not always predictive of human response, women who are or who may be pregnant should consult their health care professionals before taking Glyburide.
Recent data suggests that abnormal blood glucose levels during pregnancy are associated with a higher risk of congenital fetal malformations. Many experts prefer to use insulin to maintain blood glucose levels as close to normal as possible during pregnancy.
It is unknown whether Glyburide in excreted in human milk. Using the drug during breast feeding may lead to decreased blood glucose levels (hypoglycemia) in nursing infants. Breast feeding women should seek a professional medical advice before taking Glyburide.
Overdose of Glyburide can produce mild hypoglycemic symptoms, such as weakness, anxiety, irritability, sweating, confusion and nausea. Mild hypoglycemia should be treated aggressively with oral glucose. Severe hypoglycemia with coma, convulsions or other neurological impairment may occur and require immediate hospitalization. If hypoglycemic coma is suspected or diagnosed, rapid intravenous injection of concentrated (50%) glucose solution should be given immediately. Patients should be closely monitored for at least 24 to 48 hours because hypoglycemia may recur after apparent recovery.