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Diabetes Mellitus Medications
Name the drugs, mechanism of action, and side effects of each class
7
Medical
Professional
05/21/2012

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Term
Sulfonylureas
Definition
Glipizide (Glucotrol), Glyburide (DiBeta), and glimepiride (Amaryl)

Increase insulin secretion from pancrease.

Higher risk for hypoglycemia, rare cross allergy to sulfas, can cause photosynthesis, and are generally less effective after 5 years due to decreased pancreatic functioning. Causes 6-10 pound weight gain.
Term
Biguanides
Definition
Metformin (glucophage)

1. Reduces glucose production from lactic acid in the liver.
2. Reduces intestinal absorption of glucose.
3. Sensitizes cells to insulin

Rare lactic acidosis (reduced metabolism of lactic acid), hard on the kidneys - monitor creatinine and do not use with renal impairment, common GI side effects which usually improve over time(start low go slow), virtually no hypoglycemic risk as solo therapy.
Term
Thiazolidinediones
Definition
pioglitazone (Actos), Rosiglitazone (Avandia) increases insulin sensitivity in muscle, fat, and body cells by working as an agonist to the PPAR-gama receptors which regulate fatty-acid storage and glucose metabolism in proportion to insulin amounts. Additionally, reduces inflammation in the cardiovascular system and decreases glucose production from liver. Not used very often due to risks with cardiac disease. Increased risk of bone fractures and CHF. Use with insulin or nitrates not recommended if patient has cardiovascular risk factors. Long-term use may be associated with bladder cancer. Causes 1-5 pound weight gain.
Term
Incretin mimetics
Definition
exenatide (Byetta), liraglutide (Victoza)

Slows gastric emptying which often reduces appetite and causes weight loss, stimulates insulin production in response to increased blood glucose.

Nausea and vomiting (usually improves over time), contraindicated with gastroparesis. OK to give as an add on with insulin glargine (peakless basal 24hour insulin)
Term
Meglitinides
Definition

repaglinide (Prandin) Stimulate pancreatic insulin secretion. It works much like the sulfonylureas, but it is short acting and used to control postprandial (after meal) blood sugars. Side effects include weight gain of 4-5 pounds, Hypoglycemia, abdominal pain, diarrhea, headaches, and increased upper resp. infection risk.

This is metabolized by CYP-450 3A4. It is contraindicated with gemfibrozil (lopid- a fibric acid derivative).

Term
DPP-4 inhibitors
Definition
sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta) Inhibits DPP-4 (When a carbohydrate is ingested, the L-cells in the intestine release incretins (GLP-1) to stimulate insulin release and lower glucose production from the liver. DPP-4 breaks down the incretin to prevent hypoglycemia). Well tolerated, weight neutral, low hypoglycemic risk. Monitor patient for pancreatitis.
Term
Alpha-glucosidase inhibitors
Definition

acarbose (Precose) and miglitol (Glyset) Delay intestinal carbohydrate absorption by blocking alpha-glucosidase from breaking down starches in the stomach and portions of the intestine. This helps to reduce postprandial (after meals) blood sugars.  It doesn't affect insulin sensitivity or secretion.

Taken at beginning of meal, the starches do eventually get broken down by bacteria in the intestine producing tremendous gas and GI upset side effects. Avoid use with inflammatory bowel or impaired renal function.

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