Affiliation:
1. University of Charleston, School of Pharmacy, Charleston, WV, USA
Abstract
This chapter is a comprehensive account of diabetes and the medicinal
chemistry of antidiabetic drugs. It provides the mechanism of disease progression and
drug action and detailed structure-activity relationships (SAR) of antidiabetic drugs to
give the knowledge base for pharmacists. After studying this chapter, students will be
able to:
• Discuss the epidemiology and etiology of diabetes.
• Describe the clinical features of diabetes and differentiate between type I and type II
diabetes.
• Discuss various risk factors and corresponding mechanisms responsible for the
development of diabetes.• Review biosynthesis of insulin, its metabolic outcomes, regulation of insulin
secretion, and insulin signaling.• Explain in detail the pathophysiologic mechanisms responsible for the clinical
features of diabetes.
• Evaluate the clinical role of natural human insulin and commercially available other
insulin products and discuss its mechanism of action, pharmacokinetics, adverse
effects, motor complications, drug interactions, contraindications, and precautions.
• Discuss the mechanism of action, pharmacokinetics, adverse effects, motor
complications, drug interactions, contraindications, and precautions for each class of
antidiabetic drugs listed below.
o Sulfonylureas: tolbutamide (Orinase®
), tolazamide (Tolinase®
), chlorpropamide
(Diabinese®
), and acetohexamide (Dymelor®
), glyburide (Diabeta®
), glipizide
(Glucotrol®
), and glimepiride (Amaryl®
).
o Meglitinides: repaglinide (Prandin®
), nateglinide (Starlix®
).
o Biguanides: metformin (Glucophage®
, Glucophage XR).o Peroxisome proliferator activated receptor (PPAR) agonists/Thiazolidinediones:
pioglitazone (Actos®
), rosiglitazone (Avandia®
).o Alpha glucosidase inhibitors: acarbose (Precose®
).
o Glucagon-like peptide-1 (GLP-1) agonists: dulaglutide (Trulicity®
), exenatide
(Bydureon®
, Byetta®
), liraglutide (Victoza®
), lixisenatide (Adlyxin®
), semalgutide
(Ozempic®
, Rybelsus®
).
o Dipeptidyl peptidase-4 (DPP-4) inhibitors: alogliptin (Nesina®
), linagliptin
(Tradjenta®
), saxagliptin (Onglyza®
), sitagliptin (Januvia®
).o Amylin agonist: pramlintide (Symlin®
).o Sodium-glucose cotransporter-2 (SGLT2) inhibitors: empagliflozin (Jardiance®
),
canagliflozin (Invokana®
), dapagliflozin (Farxiga®
), ertugliflozin (Steglatro®
).
o Miscellaneous agents.
Publisher
BENTHAM SCIENCE PUBLISHERS
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