- August 19, 2022
- Newsletter
- 617-430-5616
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Brand Name :
Glynase, Diabeta, Glynase PresTab
Synonyms :
glyburide
Class :
Antidiabetics, Sulfonylureas
Brand Name :
Glynase, Diabeta, Glynase PresTab
Synonyms :
glyburide
Class :
Antidiabetics, Sulfonylureas
Dosage forms & Strengths
Tablet
1.25mg
2.5mg
5mg
Micronized Tablet
1.5mg
3mg
5mg
6mg
If CrCl<50 ml/min, use the medicine cautiously
In the case of severe hepatic impairment, avoid the medication
:
Regular tablets-
Initially, 2.5 to 5 mg orally each day
Maintenance dose- 1.25-20 mg orally each day or every 12 hours
Do not exceed 20 mg/day
For a dose of more than 10 mg/day, consider administration every 12 hours
Micronized tablets-
Initially, 1.5-3 mg orally each day
Maintenance dose- 0.75-12 mg orally each day
Do not exceed more than 12 mg/day
Patients at risk towards hypoglycemia-
Initially 0.75 mg orally each day
Transfer of insulin therapy to glyburide-
Insulin<20 units, discontinue it and start over glyburide: 2.5-5 mg/day and 1.5-3 mg/day for regular and micronized tablets respectively
Insulin 20-40 units, discontinue it and start over glyburide: 5 mg/day and 3 mg/day for regular and micronized tablets respectively
Insulin >40 units, decrease its dose and start over glyburide: 5 mg/day and 3 mg/day for regular and micronized tablets respectively
Based on patients’ response, increase the dose of glyburide by 1.25-2.5 mg and 0.75-1.5 mg/day for regular and micronized tablets respectively
Not recommended for pediatrics
Dosage forms & Strengths
Tablet
1.25mg
2.5mg
5mg
Micronized Tablet
1.5mg
3mg
5mg
6mg
may decrease the therapeutic effect of corticosteroids
may enhance the anticoagulant effect
may enhance the anticoagulant effect
may enhance the anticoagulant effect
may enhance the anticoagulant effect
may enhance the anticoagulant effect
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect when combined with antidiabetic agents
beta-Blockers may enhance the hypoglycemic effect of sulfonylureas
beta-Blockers may enhance the hypoglycemic effect of sulfonylureas
beta-Blockers may enhance the hypoglycemic effect of sulfonylureas
beta-Blockers may enhance the hypoglycemic effect of sulfonylureas
beta-Blockers may enhance the hypoglycemic effect of sulfonylureas
may increase the hypoglycaemic effect
may increase the hypoglycaemic effect
may increase the hypoglycaemic effect
may increase the hypoglycaemic effect
may increase the hypoglycaemic effect
may enhance the serum concentration of CYP2C9 inhibitors
may increase the hypoglycemic effect of quinolones
may diminish the therapeutic effect of antidiabetic agents
may diminish the therapeutic effect of antidiabetic agents
may diminish the therapeutic effect of antidiabetic agents
may diminish the therapeutic effect of antidiabetic agents
choline magnesium trisalicylate
may enhance the hypoglycemic effect
may increase the hypoglycemic effect of beta blockers
may increase the hypoglycemic effect of beta blockers
may increase the hypoglycaemic effect of beta blockers
may diminish the therapeutic effect of thiazide and thiazide like diuretics
lisinopril/hydrochlorothiazide
may enhance the serum concentration of thiazide and thiazide like diuretics
methyldopa/hydrochlorothiazide
may diminish the therapeutic effect of thiazide and thiazide like diuretics
may increase the hypoglycemic effect of direct-acting viral agents
may increase the hypoglycemic effect of direct-acting antiviral agents
may enhance the hypoglycemic effect of beta blockers
may enhance the hypoglycemic effect of beta blockers
may increase the effect of antidiabetic agents
may increase the effect of antidiabetic agents
may increase the effect of antidiabetic agents
may increase the effect of antidiabetic agents
may increase the effect of antidiabetic agents
may increase the effect of antidiabetic agents
may enhance the effect of sulfonylureas
may enhance the effect of sulfonylureas
may enhance the effect of sulfonylureas
may enhance the effect of sulfonylureas
may enhance the effect of sulfonylureas
may enhance the effect of sulfonylureas
may increase the hypoglycemic effect of salicylates
may increase the hypoglycemic effect of hypoglycemia-associated agents
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
relugolix/estradiol/norethindrone
may enhance the hypoglycemic effect
relugolix/estradiol/norethindrone
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may enhance the hypoglycemic effect
may diminish the therapeutic effect
may diminish the therapeutic effect
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect when combined with antidiabetic agents
may decrease the therapeutic effect of Hyperglycemia-Associated Agents
antidiabetic agents may have a reduced therapeutic effect when used together with ritodrine
may have an increased hypoglycemic effect when combined with antidiabetic agents
may have an increased hypoglycemic effect when combined with antidiabetic agents
may have an increased hypoglycemic effect when combined with antidiabetic agents
estrogens esterified/methyltestosterone
may increase the hypoglycemic effect of androgens
drospirenone/ethinyl estradiol/levomefolate
may decrease the therapeutic effect of Hyperglycemia-Associated Agents
dipeptidyl peptidase-IV inhibitors increase the effect of hypoglycemia of sulfonylureas
dipeptidyl peptidase-IV inhibitors increase the effect of hypoglycemia of sulfonylureas
Actions and Spectrum:
Actions:
Spectrum:
glibenclamide has a broad spectrum of activity and is effective in managing blood glucose levels in individuals with type 2 diabetes mellitus. It is typically used with other medications, such as metformin, which has a different mechanism of action, to achieve better blood sugar control.
Frequency not defined
Angioedema
Rash
Urticaria
Pruritis
Heartburn
Photosensitivity
Vasculitis
Nocturia
Hyponatremia
Hemolytic anemia
Agranulocytosis
Thrombocytopenia
Pancytopenia
Paresthesia
Blurred vision
Myalgia
Hypoglycemia
Minor diuretic effect
Erythema
Dermatitis
Weight gain
Contraindication/Caution:
Contraindications:
Precautions:
Pregnancy consideration:
Category C
Breastfeeding warnings:
No data is available about the excretion of glibenclamide in breast milk. Avoid using in lactating women.
Pregnancy category:
Pharmacology:
glibenclamide, also known as glyburide, is a sulfonylurea medication used to treat type 2 diabetes mellitus. It works by stimulating the release of insulin from the beta cells in the pancreas, thereby helping to lower blood glucose levels.
The mechanism of action of glibenclamide involves binding to specific receptors on the beta cells known as sulfonylurea receptors (SURs). This binding leads to the closure of ATP-sensitive potassium (KATP) channels, which depolarizes the cell membrane and triggers the opening of voltage-dependent calcium (Ca2+) channels. This influx of calcium triggers the release of insulin from the beta cells.
glibenclamide has a rapid onset of action, with peak effects occurring within 2-4 hours of administration. The medication is metabolized in the liver and excreted in the urine.
In addition to its effects on insulin release, glibenclamide may also have other effects on glucose metabolism, including increasing insulin sensitivity in peripheral tissues and decreasing hepatic glucose production.
glibenclamide is typically used in combination with lifestyle modifications such as diet and exercise to help manage type 2 diabetes. It is available in immediate-release tablets and should be taken with food to help prevent gastrointestinal side effects such as nausea and upset stomach.
Pharmacodynamics:
glibenclamide, also known as glyburide, is a sulfonylurea medication used to treat type 2 diabetes mellitus. It works by stimulating the release of insulin from the beta cells in the pancreas, thereby helping to lower blood glucose levels.
The mechanism of action of glibenclamide involves binding to specific receptors on the beta cells known as sulfonylurea receptors (SURs). This binding leads to the closure of ATP-sensitive potassium (KATP) channels, which depolarizes the cell membrane and triggers the opening of voltage-dependent calcium (Ca2+) channels. This influx of calcium triggers the release of insulin from the beta cells.
glibenclamide has a rapid onset of action, with peak effects occurring within 2-4 hours of administration. The medication has a short duration of action, and its effects typically last for 12-24 hours, depending on the dosage.
Pharmacokinetics:
Absorption
The bioavailability is variable, depending on the oral dosage form
Onset of action takes place 15-60 min after a single dose
Duration of action is less than 24 hours
The volume of distribution is 9-10 L
Peak serum concentration is achieved in 2-4 hours (adults)
Distribution
The protein bound is 99%
Metabolism
The drug is metabolized extensively in the liver to less-active metabolites
The metabolites formed are 4-trans-hydroxyglyburide and 3-cis-hydroxyglyburide (active)
Elimination and Excretion
The half-life is 10 hours (for DiaBeta) and 4 hours (for Glynase, PresTab)
The drug is excreted 50% in the Urine and 50% in the feces
Administration:
glibenclamide, also known as glyburide, is an oral medication used to treat type 2 diabetes mellitus. The medication is usually taken once or twice daily, with the dosage and timing determined by the healthcare provider based on the individual’s blood glucose levels and response to treatment.
glibenclamide is available in immediate-release tablets and should be taken with food to help prevent gastrointestinal side effects such as nausea and upset stomach. The immediate-release tablets are typically taken 30 minutes before a meal.
The dosage of glibenclamide will depend on several factors, including the individual’s blood glucose levels, kidney function, and response to the medication. It’s important to take glibenclamide as directed by your healthcare provider to ensure that you get the maximum benefit from the medication.
Missing a dose of glibenclamide can lead to high blood glucose levels, and taking too much glibenclamide can cause low blood glucose levels, also known as hypoglycemia. If you miss a dose, take it as soon as you remember, unless it’s almost time for your next dose. In that case, skip the missed dose and continue with your regular dosing schedule. Don’t take a double dose to make up for a missed dose.
Patient information leaflet
Generic Name: glibenclamide
Pronounced: gli-ben-clay-mide
Why do we use glibenclamide?
glibenclamide, or glyburide in the United States, is an oral medication for treating type 2 diabetes mellitus. It belongs to the class of medications known as sulfonylureas, which stimulate insulin release from the beta cells in the pancreas.
glibenclamide is used to help lower blood glucose levels in people with type 2 diabetes who cannot control their blood sugar levels with diet and exercise alone. It is typically prescribed along with lifestyle modifications such as diet and exercise, and it may also be used in combination with other medications for diabetes management.
Like other sulfonylureas, glibenclamide binds to specific receptors on the beta cells in the pancreas known as sulfonylurea receptors (SURs). This binding leads to the closure of ATP-sensitive potassium (KATP) channels, which depolarizes the cell membrane and triggers the opening of voltage-dependent calcium (Ca2+) channels. This influx of calcium triggers the release of insulin from the beta cells.
By increasing insulin release, glibenclamide helps to lower blood glucose levels in people with type 2 diabetes. It is generally considered effective and safe when used appropriately and as directed by a healthcare provider.