- March 15, 2022
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Brand Name :
Amaryl
Synonyms :
glimepiride
Class :
Antidiabetics, Sulfonylureas
Dosage Forms & Strengths
Tablet
1 mg
2 mg
4 mg
Dosage Forms & Strengths
Safety and efficacy not determined
Refer to adult dosing
It may diminish the serum concentration when combined with colesevelam
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect of Sodium-Glucose Cotransporter 2 Inhibitors
Dipeptidyl Peptidase-IV Inhibitors: they may increase the hypoglycemic effect of sulfonylureas
Dipeptidyl Peptidase-IV Inhibitors: they may increase the hypoglycemic effect of sulfonylureas
may increase the therapeutic efficacy of each other when combined
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased risk of hypoglycemia when combined with glimepiride
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 anticoagulant effect
may enhance the anticoagulant effect
may enhance the anticoagulant effect
may enhance the anticoagulant effect
may enhance the anticoagulant effect
It may enhance the toxicity when combined with mipomersen
It may enhance the effect when combined with cannabidiol by diminishing metabolism
It may enhance toxicity when combined with cholic acid by diminishing the elimination
it may diminish the metabolism when combined with azelastine
It may enhance the effect when combined with lixisenatide by pharmacodynamic synergism
Combining glimepiride with pranlukast may cause a reduction in the glimepiride’s metabolism
When halometasone is used together with glimepiride, this leads to elevated risk or seriousness of hyperglycemia
may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
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 decrease the therapeutic effect
may decrease the therapeutic effect
may decrease the therapeutic effect
may decrease the therapeutic effect
it increases the effect of hypoglycemia of antidiabetic agents
may enhance the serum concentration of CYP2C9 inhibitors
may enhance the hypoglycemic effect of agents with blood glucose lowering effects
may enhance the hypoglycemic effect of agents with blood glucose lowering effects
may enhance the hypoglycemic effect of agents with blood glucose lowering effects
may enhance the hypoglycemic effect of agents with blood glucose lowering effects
may enhance the hypoglycemic effect of agents with blood glucose lowering effects
may increase the hypoglycemic effect of beta blockers
may enhance the hypoglycemic effect of beta blockers
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 hypoglycemic effect
may enhance the hypoglycemic effect
It may intensify the hypoglycemic effect of sulfonylureas
It has the potential to amplify the hypoglycemic impact of sulfonylureas
may have an increased adverse/toxic effect when combined with alcohol
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
lansoprazole, amoxicillin, and clarithromycin
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
bismuth subcitrate, metronidazole and tetracycline
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
may have an increased hypoglycemic effect when combined with sulfonylureas
dipeptidyl peptidase-IV inhibitors increase the effect of hypoglycemia of sulfonylureas
dipeptidyl peptidase-IV inhibitors increase the effect of hypoglycemia of sulfonylureas
colesevelam has the potential to reduce the levels of serum in glimepiride
Actions and Spectrum:
glimepiride works by attaching to the ATP-sensitive potassium channels on the surface of pancreatic beta cells and causing them to close. The cell membrane depolarizes as a result of this closure, which leads to the release of insulin.
glimepiride’s effect range is rather small; therefore, its main effects are on insulin and blood sugar levels. Other areas of metabolism or body processes are not significantly impacted. I
t is crucial to remember that glimepiride might result in hypoglycaemia (low blood sugar) as an adverse reaction, thus it must be taken carefully and with a doctor’s supervision.
Frequency Defined
1-10%
Headache (1.5%)
Asthenia (1.6%)
Nausea (1.1%)
Dizziness (1.7%)
>10%
Hypoglycemia (4-20%)
<1%
Pruritus
Urticaria
Allergic skin reactions
Erythema
Morbilliform or maculopapular eruptions
Diarrhea
Vomiting
Agranulocytosis
Gastrointestinal pain
Anemia
Elevation of liver enzyme levels
Hepatic porphyria reactions
Leukopenia
Pancytopenia
Thrombocytopenia, hemolytic
Disulfiram-like reactions
Hyponatremia
Aplastic anemia
Cholestasis
Jaundice (rare)
Post marketing reports
Hemolytic anemia in patients with and without G6PD deficiency
Hepatic impairment (e.g., jaundice, cholestasis), as well as hepatitis, which may progress to liver failure
Serious hypersensitivity reactions, including angioedema, anaphylaxis, and Stevens- Johnson Syndrome
Aplastic anemia, pancytopenia, Leukopenia, and agranulocytosis
Hyponatremia and SIADH, most often in patients on other medications or increase release of antidiuretic hormone or have medical conditions known to cause hyponatremia
Porphyria cutanea tarda, photosensitivity reactions and allergic vasculitis
Dysgeusia
Alopecia
Thrombocytopenia (including severe cases with platelet count <10,000/mcL) and thrombocytopenic purpura
Hepatic porphyria reactions and disulfiram-like reactions
Black Box Warning
According to the glimepiride black box warning, significant hypoglycaemia (low blood sugar) may occur, which can result in a coma or even death.
When glimepiride is used with certain other drugs, such as insulin or other sulfonylureas, or in those with kidney or liver disease, hypoglycaemia is more likely to happen.
The warning also advises against using glimepiride in people with type 1 diabetes or diabetic ketoacidosis as the drug is ineffective in these situations.
Contraindication/Caution:
Contraindication:
Caution:
Pregnancy warnings:
Pregnancy category: N/A
Lactation: Excretion into human milk is unknown
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology
A second-generation sulfonylurea anti-diabetic medication called glimepiride increases the amount of insulin that the pancreatic beta cells secrete. It blocks the ATP-sensitive potassium channels (KATP) via binding to the sulfonylurea receptor (SUR) on the surface of pancreatic beta cells, which causes the membrane to depolarize and release insulin.
Pharmacodynamics
glimepiride’s effects on the pancreatic beta cells boost insulin production, which lowers blood glucose levels in people with type 2 diabetes mellitus. In reaction to glimepiride, the pancreatic beta cells produce insulin in a glucose-dependent way. As a result, the medication only promotes insulin release when blood glucose levels are high, assisting in the prevention of hypoglycemia.
Pharmacokinetics
Absorption
Orally given glimepiride is quickly absorbed from the digestive tract. Almost 100% of the medication’s dosage is absorbed into the circulation, which indicates that the drug has a high bioavailability. To promote the best absorption, glimepiride should be taken with the first substantial meal of the day.
Distribution
More than 99% of glimepiride is protein-bound to serum albumin. It has a substantial volume of distribution, which suggests that it is dispersed among the tissues of the body.
Metabolism
The cytochrome P450 enzyme system, CYP2C9, largely metabolizes glimepiride in the liver. The inactive hydroxy derivative is the main metabolite. The carboxyl derivative and the cyclohexyl hydroxy methyl derivative are two further minor metabolites.
Elimination and excretion
glimepiride and its byproducts are eliminated in the feces (40%) and urine (60%) respectively. The medicine has an elimination half-life of around 5 to 9 hours, and total elimination happens 4 to 5 days following the last dose.
Administration:
glimepiride pills are taken orally to provide the medication. To achieve the best absorption, it is normally taken once daily with the first large meal of the day.
The pills should not be chewed, crushed, or broken and should be consumed whole with a glass of water. glimepiride dose is tailored to the patient’s glycaemic control and should be progressively increased to reach the desired blood glucose level.
Patient information leaflet
Generic Name: glimepiride
Why do we use glimepiride?
glimepiride is used to treat type 2 diabetes mellitus, a disease where the body has trouble using insulin properly and has high blood sugar levels as a result. By encouraging the secretion of insulin from the pancreas, the medication is used to assist in lowering blood glucose levels.
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