Page 783 - Basic _ Clinical Pharmacology ( PDFDrive )

CHAPTER 41 Pancreatic Hormones & Antidiabetic Drugs 769

Mechanism of Clinical Pharmacokinetics,
Subclass, Drug Action Effects Applications Toxicities, Interactions
GLUCAGON-LIKE POLYPEPTIDE-1 (GLP-1) RECEPTOR AGONISTS
• Exenatide, liraglutide, Analogs of GLP-1: Bind Reduce post-meal glucose Type 2 diabetes, Parenteral (SC) • Toxicity: Nausea,
albiglutide, dulaglutide to GLP-1 receptors excursions: Increase glucose- liraglutide only: headache, vomiting, anorexia, mild
mediated insulin release, obesity weight loss, pancreatitis, C-cell
lower glucagon levels, slow tumors in rodents
gastric emptying, decrease
appetite
DIPEPTIDYL PEPTIDASE-4 (DPP-4) INHIBITORS
• Sitagliptin, saxagliptin, Block degradation of Reduces post-meal glucose Type 2 diabetes Oral • half-life ~12 h • 24-h duration
linagliptin, alogliptin, GLP-1, raise circulating excursions: Increases of action • Toxicity: Rhinitis, upper
vildagliptin 1 GLP-1 levels glucose-mediated insulin respiratory infections, headaches,
release, lowers glucagon pancreatitis, rare allergic reactions
levels, slows gastric
emptying, decreases
appetite
SODIUM-GLUCOSE CO-TRANSPORTER 2 (SGLT2) INHIBITORS
• Canagliflozin, dapagliflozin, Block renal glucose Increase glucosuria, lower Type 2 diabetes Oral • half-life ~10–14 h • Toxicity:
empagliflozin resorption plasma glucose levels Genital and urinary tract infections,
polyuria, pruritus, thirst, osmotic
diuresis, constipation
ISLET AMYLOID POLYPEPETIDE ANALOG
• Pramlintide Analog of amylin: Binds Reduces post-meal glucose Type 1 and type 2 Parenteral (SC) • rapid onset
to amylin receptors excursions: Lowers glucagon diabetes • half-life ~48 min • Toxicity: Nausea,
levels, slows gastric anorexia, hypoglycemia, headache
emptying, decreases
appetite

BILE ACID SEQUESTRANT
• Colesevelam hydrochloride Bile acid binder: Lowers Reduces glucose levels Type 2 diabetes Oral • 24-h duration of action
glucose through • Toxicity: Constipation, indigestion,
unknown mechanisms flatulence

DOPAMINE AGONIST
• Bromocriptine D 2 receptor agonist: Reduces glucose levels Type 2 diabetes Oral • 24-h action • Toxicity: Nausea,
Lowers glucose through vomiting, dizziness, headache
unknown mechanism
1 Not available in United States.