Search
glimepiride (Amaryl)
Tradename: Amaryl. 2nd generation sulfonylurea. Molecular formula: C24H34N4O5S
Indications:
- treatment of diabetes mellitus type-2
Advantages: (over 1st generation sulfonylurea)
1) insulin-sensitizing effect
2) favorable ratio between endogenous insulin secretion & blood glucose decrease
3) lesser drop in blood glucose during exercise
Contraindications:
- not recommended for pregnant or nursing mothers or children
Dosage: 1-4 mg PO QD.
Pharmacokinetics:
- metabolized in the liver by cyt P450 2C9
Adverse effects:
1) hypoglycemia
- among nursing home residents, new use of glimepiride results in higher rates of severe hypoglycemia vs amother glipizide or glyburide [5]
2) asthenia
3) dizziness
4) headache
5) nausea
6) no increase in cardiovascular risk [4]
Drug interactions:
1) glimepiride is potentiated by highly protein-bound agents
a) NSAIDs
b) sulfonamides
c) chloramphenicol
d) coumadin
e) probenecid
f) MAO inhibitors
g) beta blockers
2) potential interactions with other cyt P450-metabolized agents
a) phenytoin
b) diclofenac
c) ibuprofen
d) naproxen
e) mefenamic acid
3) any drug which inhibits cyt P450 2C9 can increase glimepiride levels
4) any drug which induces cyt P450 2C9 can diminish glimepiride levels
Laboratory:
- glimepiride in serum/plasma
- glimepiride in urine
Mechanism of action:
- may increase plasma levels of adiponectin, which increases insulin sensitivity
Interactions
drug interactions
drug adverse effects (more general classes)
monitor with sulfonylureas
Related
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
General
sulfonylurea
Properties
SIZE: MW = 490.6 G/M
MISC-INFO: elimination route LIVER
1/2life 9 HOURS
pregnancy-category ?
safety in lactation ?
Database Correlations
PUBCHEM cid=3476
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#: 220233
(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: 12547850
- Riddle MC
A Verdict for Glimepiride: Effective and Not Guilty of Cardiovascular Harm.
Diabetes Care 2019 Dec; 42(12): 2161-2163
PMID: 31748210
https://care.diabetesjournals.org/content/42/12/2161
- 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: 36495141
https://agsjournals.onlinelibrary.wiley.com/doi/abs/10.1111/jgs.18160
Component-of
glimepiride/pioglitazone (Duetact)
glimepiride/rosiglitazone (Avandaryl)