glimepiride (Amaryl)
Jump to navigation
Jump to search
Introduction
Tradename: Amaryl. 2nd generation sulfonylurea. Molecular formula: C24H34N4O5S
Indications
- treatment of diabetes mellitus type-2
Contraindications
- not recommended for pregnant or nursing mothers or children
Advantages
(over 1st generation sulfonylurea)
- insulin-sensitizing effect
- favorable ratio between endogenous insulin secretion & blood glucose decrease
- lesser drop in blood glucose during exercise
Dosage
Pharmacokinetics
- metabolized in the liver by cyt P450 2C9
elimination via liver
1/2life = 9 hours
Adverse effects
- hypoglycemia
- among nursing home residents, new use of glimepiride results in higher rates of severe hypoglycemia vs amother glipizide or glyburide[5]
- asthenia
- dizziness
- headache
- nausea
- no increase in cardiovascular risk[4]
Drug interactions
- glimepiride is potentiated by highly protein-bound agents
- potential interactions with other cyt P450-metabolized agents
- any drug which inhibits cyt P450 2C9 can increase glimepiride levels
- any drug which induces cyt P450 2C9 can diminish glimepiride levels
- drug interaction(s) of sulfonylureas with warfarin
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of fluroquinolones with sulfonylureas
- drug interaction(s) of macrolides with sulfonylureas
- drug interaction(s) of salicylates with sulfonylureas
- drug interaction(s) of gliptins with sulfonylureas
- drug interaction(s) of fluoroquinolones with hypoglycemic agents
Laboratory
Mechanism of action
- may increase plasma levels of adiponectin, which increases insulin sensitivity
More general terms
Additional terms
- cytochrome P450 2C9; cytochrome P450 BP-1; cytochrome P450 MP-4; S-mephenytoin-4-hydroxylase; limonene 6-monooxygenase; limonene 7-monooxygenase (CYP2C9, CYP2C10)
- Periscope trial
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Tsunekawa T, Hayashi T, Suzuki Y, Matsui-Hirai H, Kano H, Fukatsu A, Nomura N, Miyazaki A, Iguchi A. Plasma adiponectin plays an important role in improving insulin resistance with glimepiride in elderly type 2 diabetic subjects. Diabetes Care. 2003 Feb;26(2):285-9. PMID: https://www.ncbi.nlm.nih.gov/pubmed/12547850
- ↑ 4.0 4.1 Riddle MC A Verdict for Glimepiride: Effective and Not Guilty of Cardiovascular Harm. Diabetes Care 2019 Dec; 42(12): 2161-2163 PMID: https://www.ncbi.nlm.nih.gov/pubmed/31748210 https://care.diabetesjournals.org/content/42/12/2161
- ↑ 5.0 5.1 Zullo AR Comparative safety of sulfonylureas among U.S. nursing home residents. J Am Geriatr Soc. 2023 Apr;71(4):1047-1057. Epub 2022 Dec 10. PMID: https://www.ncbi.nlm.nih.gov/pubmed/36495141 https://agsjournals.onlinelibrary.wiley.com/doi/abs/10.1111/jgs.18160