Diabetic Medications Flashcards
What pancreatic islet cell are damaged in diabetes?
B cells that secrete insulin
a pancreatic cells secrete?
Glucagon
What are the actions of insulin?
- Lowers BG level
- Regulates fat metabolism
- Regulates protein metabolism
- Increases K+ uptake into the cells
When is Type I DM usually diagnosed?
Usually diagnosed in early childhood to early adulthood
What is the cause of Type I DM?
Caused by autoimmune destruction of the B cells of the pancreas, absolute deficiency of insulin (B islet cells)
What HgbA1c is diagnostic for diabetes?
> 6.5
What are some complications associated with DM?
Retinopathy
Nephropathy
Neuropathy
CV complications
Gastroparesis, Autonomic insufficiency
What are the therapeutic goals of giving insulin?
- To replicate normal physiologic insulin secretion
- To replace basal insulin (overnight, fasting and between meals)
- To provide bolus at meal time
What are the rapid acting insulins?
- Insulin aspart (Novolog)
- Insulin lispro (Humalog)
- Insulin glulisine (Adidra)
What is the MOA of rapid acting insulins?
- Acts as natural insulin: facilitates glucose transport into cells, inhibit glycogenolysis and gluconeogensis, regulate fat and protein metabolism, increase K+ uptake in cells
What is the PK of rapid acting insulins?
- SubQ w/in 15 minute of a meal, or IV administration
- Onset 10-30 minutes, peak effects seen 30-90 minutes, effective up to 1-5 hours
What are the uses of rapid acting insulins?
- Rapid-acting insulins
- Admin to mimic mealtime release of insulin and to control postprandial glucose
- Fast correction of elv glucose
- Usually used in combo with longer acting insulin
What are the side effects of insulin?
Weight gain, Somogyi effect, Dawn phenomenon, hypogycemia
HA, tachycardia, vertigo, anxiety, confusion, diaphoresis, lipodystrophy, hypersensitivity
What are the regular short acting insulins?
Humulin R and Novolin R
What is the use of regular short acting insulin?
- Short acting insulin
- Admin to mimic mealtime release of insulin and to control postprandial glucose
- Fast correction of elevated glucose
- Usually used in combo with longer acting insulin
What is the Somogyi effect?
If the blood sugar level drops too low in the early morning hours, hormones (such as growth hormone, cortisol, and catecholamines) are released. These help reverse the low blood sugar level but may lead to blood sugar levels that are higher than normal in the morning.
What is the MOA of regular short acting insulin?
Acts as a natural insulin: facilitates glucose transport into cells, inhibits glycogenolysis and gluconeogensis, regulate fat and protein metabolism, increase K+ uptake in cells
What is the PK of regular short acting insulin?
- SubQ, 30 minutes before meal, or IV admin (emergency)
- Onset, 30 minutes- 5 hours, peak 2-3 hours, effective up to 8-12 hours
What type of insulin is NPH Insulin Isophane (Humulin N)?
An intermediate acting insulin
What are the uses for NPH Insulin Isophane (Humulin N)?
- Intermediate acting insulin
- Basal (fasting) control in type 1 or 2 diabetes
- Usually given along with rapid or short acting insulin for mealtime control
- DO NOT use when rapid glucose lowering is needed
What is the MOA of NPH Insulin Isophane (Humulin N)?
Acts as a natural insulin: facilitates glucose transport into cells, inhibits glycogenolysis and gluconeogenesis, regulate fat and protein metabolism, increase K+ uptake in cells
What is the PK of NPH Insulin Isophane (Humulin N)?
- SubQ admin only
- Onset 4-12 hours, peak 5.5 hours, effective up to 18-24 hours
What are the long-acting insulins?
Insulin detemir (Levemir) and Insulin Glargine (Lantus)
What are the uses of Insulin Determir and Insulin Glargine (long-acting insulins)?
- Long acting insulin
- Basal (fasting) control in type 1 and 2 diabetes
What is the MOA of long-acting insulins?
Acts as a natural insulin: facilitates glucose transport into cells, inhibits glycogenolysis and gluconeogenesis, regulate fat and protein metabolism, increase K+ uptake in cells
What is the PK for Insulin detemir (Levemir)?
- SubQ admin ONLY, twice daily dosing
- Onset 1-2 hours, peak 6-8 hours, effective up to 24 hours
What is the PK for Insulin glargine (Lantus)?
- SubQ admin ONLY, once daily dosing
- Onset 1-1.5 hours, peak 4 hours, effective up to 24 hours
What is the MOA of GLP-1 agonists?
GLP-1 receptor agonists –> promote insulin secretion, enhance satiety, decrease postprandial glucagon secretion, promote beta cell proliferation
What drugs are GLP-1 agonists?
Exenatide
Liraglutide
Dulaglutide
What is the PK of the GLP-1 agonists?
SubQ admin
Liraglutide: long half-life, once daily dosing
Exenatide: shorter half-life, twice daily dosing, eliminated by glomerular filtration
What are the side effects of GLP-1 agonists?
N/V, diarrhea, constipation, possible pancreatitis
Exenatide: contra in severe renal impairment
What are the Sulfonylureas?
Glyburide
Glipizide
Glimepiride
What are the use of Sulfonylureas?
Treatment of patients who have type 2 DM that is not controlled with diet
What is the MOA of Sulfonylureas?
Block ATP-sensitive K+ channels –> depolorization, Ca2+ influx, and insulin release
- Increase insulin sensitivity
What is the PK of Sulfonylureas?
- Oral admin
- 18-24 hours DOA
- Hepatic metabolism
What are the side effects of Sulfonylureas?
Weight gain, hyperinsulinemia, hypoglycemia
Sulfonylureas are contraindicated in who?
Sulfa allergy
Pregnancy
Sulfonylureas should be used in caution in whom?
Hepatic and renal insufficiency, geriatric patients
What are the meglitinides?
Repaglinide
Natelinide
What are the uses of meglitinides?
- Postprandial glucose regulators
- Used infrequently
- Should not be used with Sulfonylureas
What is the MOA of the meglitinides?
Bind to distinct sites on B cells, closing ATP-sensitive K+ channels and causing insulin release
What is the PK of meglitinidenes?
Oral admin prior to a meal
What are the side effects of meglitinedenes?
Lower incidence of weight gain and hypoglycemia than sulfonylureas
Meglitinedenes should be used in caution in what cohort?
Hepatic impairment
