Glimepiride

Glimepiride(Amaryl) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.Target: DPP4Glimepiride (Hoe 490) is a new sulfonylurea. After oral administration of Hoe 490 to rabbits, blood glucose was lowered 3.5 times more than after glibenclamide (HB 419) and after intravenous administration, 2.5 times more [1]. glimepiride decreased extracellular Aβ40 and Aβ42 levels. glimepiride may serve as a promising drug for the treatment of AD associated with diabetes [2]. glimepiride was generally associated with lower risk of hypoglycemia and less weight gain compared to other sulfonylureas. Glimepiride use may be safer in patients with cardiovascular disease because of its lack of detrimental effects on ischemic preconditioning [3].Clinical indications: Non-insulin dependent diabetesToxicity: Severe hypoglycemic reactions with coma; seizure or other neurological impairment.

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

[1]. Geisen, K., Special pharmacology of the new sulfonylurea glimepiride. Arzneimittelforschung, 1988. 38(8): p. 1120-30.

[2]. Liu, F., et al., Glimepiride attenuates Abeta production via suppressing BACE1 activity in cortical neurons. Neurosci Lett, 2013. 557 Pt B: p. 90-4.

[3]. Basit, A., M. Riaz, and A. Fawwad, Glimepiride: evidence-based facts, trends, and observations (GIFTS). [corrected]. Vasc Health Risk Manag, 2012. 8: p. 463-72.

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

MOLECULAR FORMULA :

C24-H34-N4-O5-S

MOLECULAR WEIGHT :

490.68

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD - Lethal dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>10 gm/kg

TOXIC EFFECTS :

Liver - other changes

REFERENCE :

ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 43,547,1993

TYPE OF TEST :

LD - Lethal dose

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>3950 mg/kg

TOXIC EFFECTS :

Liver - other changes

REFERENCE :

ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 43,547,1993

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Unreported

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>10 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

DIFREZ Diabetes Frontier. (Medikaru Rebyusha, Yoshida Bldg., 1-7-3 Hirano-machi, Chuo-ku, Osaka, 541, Japan) V.1- 1990- Volume(issue)/page/year: 3,565,1992

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Unreported

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

>10 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

DIFREZ Diabetes Frontier. (Medikaru Rebyusha, Yoshida Bldg., 1-7-3 Hirano-machi, Chuo-ku, Osaka, 541, Japan) V.1- 1990- Volume(issue)/page/year: 3,565,1992 ** REPRODUCTIVE DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

DOSE :

254 ug/kg

SEX/DURATION :

female 7-18 day(s) after conception

TOXIC EFFECTS :

Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - abortion Reproductive - Fertility - other measures of fertility

REFERENCE :

KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,1477,1993