Lecture 91 - Pancreatic Hormones & Anti_DM Drugs Flashcards
Insulin binds to its receptor — then what happens?
Insulin binds to alpha subunit Beta - tyrosine kinase domain Forms Tetramer; auto-phosph of Beta Domains Phosphorylation cascade Effects: GLUT 4 Channel inserted in cell membrane -- increased glucose uptake increased protein synthesis increased TG storage
Insulin Receptor is internalized and degraded
treatment regimen for T1DM
insulin analogs
what are the fast acting insulin analogs
what are the longer acting insulin analogs
Ultra short Acting - - Lispro, Aspart, Glulisine -
Long Acting
Glargine –
Detemir
complications of insulin analog use
hypoglycemia –
Insulin allergy – (eg if from pork)
lipodystrophy at injection site
what are the sulfonylureas
Mechanism of Sulfonylurea
Glimepiride, Glipizide, Glyburide
blocks the K+ channel in beta cells; depolarization; VGCC –> Insulin secretion
what is the sulfa-moeity free version of sulfonylureas
how else does it differ?
Sulfa Free= Meglitinides- Repaglinide (Prandin):
Weaker affinity and dissociates quickly
side effects of Sulfonylrurea
hypoglycemia
what classes of drugs are considered “hypoglycemic”,
which are “anti-hyperglycemia”
hypoglycemic – Insulin analogs and sulfonyl ureas – will drive down serum glucose no matter what
Metformin (Biguanides) – antihypergylcemic – drops blood glucose only in the setting of hyperglycemia
effects of metformin
Increased glycolysis;
Increased insulin sensitivity; reduces insulin resistance;
reduced GNG in the Liver;
Lowing of Glucose absorption in the Gut.
lowers Glucagon levels
side effects of metformin
contraindications:
other indications:
N/V/D/pain; anorexia
contra: renal, hepatic disease, alcoholism,
other indications: Insulin resistance in obese patients, PCOS, Prevention of DM in pre-DM, Getastational DM
name 2 Thiazolidinediones (TZD)
mechanism
Pioglitzone, Rosiglitazone
Mechanism: binds to PPAR-gamma nuclear transcription regulator
Genes involved with glucose and lipid metabolism
side effects and more serious complication of TZD use that has gotten in banned in Europe
Side effects: weight gain, edema, hepatotoxicity (P450s/drug interactions)
Bladder Cancer
alpha glucosidase inhibitors:
name 2
mechansim
Acarbose and miglitol –
Competitive Inhibition of Intestinal Alpha Glucosidase; therefore not breaking down starches to monosaccharides, therefore cannot absorp
side effect of glucosidase inhibitors
if pt becomes hypoglycemic on TZDs, how do you manage it?
Flatulence, Diarrhea, Abd pain
If patient is taking these drugs and have hypoglycemic episode; have to give monosaccharrides
Incretin based therapies can only be used in ___DM
t2DM bc they require pre-existing insulin
