Small lipophilic molecules for example arachidonic acid, linoleic acid, prostaglandin 15d-PGJ2.
Primary physiological response to PPAR gamma activation is adipocyte differentiation.
PPARγ activity is associated with uptake into fat cells of circulating fatty acids as well as lipid storage shifts.
A & B
B & C
A & C
A, B & C
Thiozolidinediones/Thiozolidinediones currently available for treating patients with type II diabetes:
Troglitazone
Rosiglitazone
Pioglitazone
A & B
B & C
A & C
A, B & C
Cellular responses to PPARγ activation includes enhancement of responsiveness of tissue to insulin.
True
False
Rosiglitazone and pioglitazone:
Insulin sensitizers
Administration results in promoting insulin-mediated glucose uptake by about 40% range: 30%-50%) in type II diabetic patients
Both
Neither
Thiozolidinediones less likely to influence plasma triglyceride levels:
Rosiglitazone
Pioglitazone
Both equally likely to alter plasma triglyceride levels
Thiozolidinediones increase the expression of glucose transporters (GLUT 1 and GLUT 4).
True
False
Thiozolidinediones effect/effects:
Increased adiponectin
Reduced resistin release from the adipocytes
Reduced hepatic glucose output
Reduced free fatty acid plasma levels
A & B
B & C
A & C
D only
A, B, C & D
Rosiglitazone and pioglitazone:
May each be used as monotherapy
May each be combined with sulfonylureas, insulin, or metformin.
Both
Neither
Administration of biguanides (e.g. metformin) or thiozolidinediones (rosiglitazone and pioglitazone)
is likely to cause hypoglycemia.
True
False
Pioglitazone:
Exhibits PPARγ and some PPARα activity.
Absorbed within a couple hours of ingestion; however, food delays uptake.
Both
Neither
Pioglitazone is metabolized by the cytochrome P450 drug metabolizing system utilizing mainly CYP2C8 and CYP3A4 isoforms resulting in active metabolites.
True
Falls
Rosiglitazone:
Highly protein bound, rapidly absorbed.
Metabolized by the cytochrome P450 drug metabolizing system, especially utilizing CYP2C8 and CYP3A4, resulting in minimally active metabolites.
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Source Material:
Powers A D'Alessio D Chapters 47:
Endocrine Pancreas and Pharmacotherapy of Diabetes Mellitus and
Hypoglycemia in Goodman & Gilman's: The Pharmcological
Basis of Therapeutics, 13e, (Brunto LL Hilal-Dandan R Knollmann
BC, eds) McGraw-Hill Education, 2018.
Masharani U Diabetes
Mellitus (27-01) in Current Medical Diagnosis & Treatment (Papadakis
MA McPhee SJ Rabow MW McQuaid KR, eds) 61e McGraw Hill 2022.
Masharani U Kroon L
Chapter 41: Pancreatic Hormones & Glucose-Lowering Drugs
in Basic & Clinical Pharmacology (Katzung BG, Editor; Vanderah
TW, Associate editor) 15e McGraw Hill 2021.