Glimepiride

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Glimepiride chemical structure
Glimepiride
Systematic (IUPAC) name
3-ethyl-N,N-bis (3-ethyl-4-methyl-2-oxo-5H-pyrrol-2-yl)- 4-methyl-2-oxo-5H-pyrrole-1- carboxamide
Identifiers
CAS number 93479-97-1
ATC code A10BB12
PubChem 3476
DrugBank APRD00381
Chemical data
Formula C24H34N4O5S
Mol. weight 490.617 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding >99.5%
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic drug. It is marketed as Amaryl® by Aventis.

Contents

[edit] Description

Glimepiride is the first III generation sulphonyl urea it is a very potent sulphonyl urea with long duration of action.

[edit] Mechanism of Action

Glimepiride distinctly lower the blood glucose level by both defects of NIDDM, by stimulating pancreatic beta cells to produce more insulin and induced increased activity of peripheral insulin intra cellular receptor.

[edit] Clinical Pharmacology

With Glimepiride GI absorption is complete with no interference of meals. Significant absorption of glimepiride was seen within one hour, and distributed through out the body, bound to the plasma protein to an extended of 99.5% and it is metabolised by oxidative biotransformation and 60% is excreted in the urine, and remaining is excreted in the faeces.

[edit] Indications

Type 2 diabetes (or) NIDDM

[edit] Dosage

There is no fixed dosage regimen for the management of diabetes mellitus with GLI, in general the dosage of GLI should be lowest which is sufficient to achieve the desired metabolic control. Starting dose : 1-2mg OD Maintenance :1-4mg OD Maximum recommended dose : 8mg OD

[edit] Contra-Indication

Hypersensitivity to glimepiride other sulphonyl urea.

[edit] Drug Interactions

With NSAIDs like Salicylates, Sulphoamides, Chlorampenizol coumarin and probencid may potentiate the hypoglycemic action of glimepride. Thiazides, other diuretic, phothiazides, thyroid products, oral contraceptives, phenytoin tend to produce hyperglycemic.

[edit] Special Precautions

In the initial weeks of treatment the risk of hypoglycemia, may be increased and necessities especially careful monitoring.

[edit] Adverse Effects

GI disturbance, rarely thrombopenia , leucopenia, haemolytic anaemia, occasionally allergic.


Oral antidiabetic drugs (A10B) edit
Biguanides: Metformin
Sulfonylureas: Chlorpropamide, glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide
Alpha-glucosidase inhibitor: Acarbose, Miglitol
Thiazolidinediones (TZD): Pioglitazone, Rosiglitazone, Troglitazone
Meglitinides: Nateglinide, Repaglinide, Mitiglinide
Dipeptidyl peptidase-4 (DPP-4) inhibitors: Saxagliptin, Sitagliptin, Vildagliptin