Diabetic Medications Flashcards
Rapid-acting Insulins uses
- Insulin Lispro
- Insulin Aspart
- Insulin Glulisine
Uses: mimic prandial release of insulin; usually given with longer acting insuling to assure proper glucose control
Given SC 15 minutes before a meal; also can be IV
Short-acting Insulin
- Regular Insulin (soluble crystalline zinc insulin)
30 minutes before a meal usually SC (IV in emergencies)
Intermediate-acting Insulins
- Neutral Protamine Hagedorn (also called Isophane insulin)
Uses: for basal control
Only given by SC and usually given along with rapid or short acting insuling for mealtime control
Long-acting Insulins
- Insulin Glargine
- Insulin Detemir
- Insulin Degludec
No peak
What are the drugs that cause hypoglycemia?
- Ethanol
- B-blockers
- Salicylates
Drugs that cause Hyperglycemia
- Epinephrine
- Glucocorticoids
- Atypical antipsychotics
- HIV protease inhibitors
- Phenytoin
- Clonidine
- Ca2+-channel blockers
- Diuretics
What are the non-insulin antidiabetic agents?
- Insulin Secretagogues - Sulfonylureas and Meglitinides
- Biguanides
- Thiazolidinediones (TZDs)
- alpha-Glucosidase Inhibitors
- Incretin Analogs
- Amylin Analogs
- Bile-Acid Sequestrants
- SGLT2 Inhibitors
Sulfonylureas MOA, use, AE
- Chlorpropamide - 1st generation; more AE so CI in elderly and hyperemic flush with alcohol; apparent SIADH
- Glyburide (Glibenclamide) - hypoglycemia 20-30%
- Glipizide - hypoglycemia 10-15%; short half life
- Glimepiride - hypoglycemia 9-14%
MOA: stimulate release from B cells by binding to SUR1 subunit and block ATP-sensitive K+ channel in B cell membrane
Uses: effective at reducing fasting plamsa glucose (FPG) and HbA1C
AE: hypoglycemia, weight gain
Meglitinides MOA, use, AE
- Repaglinide
- Nateglinide
MOA: stimulate insuline relase by binding to SUR1 and inhibiting ATP-sensitive K+ channel
Uses: not as effective as sulfonylureas in reducing FPG and HbA1C
AE: hypoglycemia (less risk in Nateglinide), weight gain
Biguanides MOA, Uses, AE, CI
- Metformin
MOA: activation of AMP-activated protein kinase (AMPK) > reduces glucose levels primarily by reducing gene expression of gluconeogenesis enzymes > improvement of glycemic control > insulin concentration decline; increases insulin mediated glucose utilization in muscle and liver
Uses: equivalent to sulfonylureas in reducing FPG and HbA1C but no hypoglycemia, reduces plasma TG by 10-15%, decreased body weight
AE: GI (anorexia, N/V, abd discomfort, diarrhea), long term > B12 deficiency, small risk of potentially fatal lactic acidosis
CI: pts with renal disease, hepatic disease, hypoxia, or alcoholism
Thiazolidinediones (TZDs)
- Pioglitazone - better effects on lipids
- Rosiglitazone
MOA: agonist of peroxisome proliferator-activated receptor-gamma (PPAR-g) which is intracellular recptors in muscle, fat, liver; slow onset over weeks or months
Uses: decrease insulin resistance, promote glucose uptake/utilization in adipose tissue, less effect in decreasing FPG/HbA1C
AE: fluid retention, weight gain, edema, cause/exacerbate CHF
CI: class III/IV heart failure; need LFTs
alpha-Glucosidase Inhibitors
- Acarbose
MOA: competitive inhibitor of intestinal alpha-glucosidases > reduces postprandial digestion of starch and disaccharides > decreases postprandial hyperglycemia and hyperinsulinemia
Uses: modest drop in FPG and HbA1C levels
AE: flatulence, diarrhea, abd pain, reversible hepatic enzyme elevation (periodical LFTs)
CI: IBS or any condition worsened by gas/distention
Incretin Analogs
- Exenatide - analog of glucagon-like-polypeptide 1 (GLP-1)
MOA: full agonist at human GLP-1 receptors
Uses: enhances glucose-dependent insulin secretions, suppresses postprandial glucagon release, slows gastric emptying, decreases appetite, may stimulate B-cell proliferation
AE: N/V/D, acute pancreatits
CI: gastroparesis
Inhibitors of DDP-IV MOA, AE
- Sitagliptin
MOA: increases circulating GLP-1 and insulin levels
AE: pancreatitis, hypersensitivity reactions (urticaria, angioedema, anaphylaxis, and skin reactions like Stevens-Johnson syndrome
Amylin Analogs MOA
- Pramlintide
MOA: peptide co-secreted with insulin from pancreatic B-cells and inhibits food intake, gastric emptying, and glucagon secretions