Diabetes Flashcards
Thiazolidinediones (gliatozones) bind avidly to peroxisome proliferator-activated receptor gamma in adipocytes to promote adipogenesis and fatty acid uptake in peripheral fat. By reducing circulating fatty acid concentrations and lipid availability in liver and muscle, the drug improves the patient’s sensitivity to insulin.
Side Effects: The most common side effects are upper respiratory infection, headache, muscle pain, weight gain, swelling, fluid retention, flatulence, anemia, and ovulation induction. Serious reactions may include new or worsening CHF, liver toxicity, diabetic macular edema, increased risk of bladder cancer and fractures (in female patients).
Biguanide (Metformin- Glucophage) decreases glucose production by the liver and increases tissue response to insulin. It inhibits glucose production in the liver, reduces glucose absorption in the gut, and sensitizes insulin receptors in target tissues to increase glucose reuptake in response to whatever insulin may be available.
Most common side effects include decreased appetite, nausea, and diarrhea. It decreases absorption of vitamin B12 and folic acid causing a deficiency which can contribute to peripheral neuropathy. Severe metabolic acidosis can occur with accumulation of metformin. A higher risk of this occuring happens to those diabetic patients with significant renal impairment.
Non-insulin Injectable drugs lower blood glucose by stimulating glucose-dependent insulin release, slowing gastric emptying, reducing appetite, and suppressing postprandial glucagon release.
The most common side effects are hypoglycemia (when combined with sulfonylurea or insulin dependant on the type of injectable used), GI symptoms (such as nausea, vomiting, and diarrhea), pancreatitis, injection site reactions such as irritation and pruritis. Postmarketing reports of hypersensitivity reactions including anaphylaxis and angioedema have also been noted. Exenatide should not be used by patients with severe renal impairment and used with caution in renal transplant recipients as it can cause renal impairment.
Second generation sulfonylureas(gliclazide, glipizide, and glimepiride) -Increase insulin secretion by pancreas and may increase tissue sensitivity to insulin
Headache, dizziness, Gastrointestinal side effects - nausea, heartburn, epigastric fullness, vomiting, diarrhea, constipation.
SGLT-2 inhibitors (Sodium-Glucose Cotransporter 2 inhibitors) like empagliflozin/Jardiance decrease reabsorption of glucose in the kidneys (hence increase glucose excretion via urine) and work by blocking SGLT-2 which is a transporter needed for glucose reabsorption.
AEs include UTIs, polyuria and yeast infections in female patients; another serious AE is hypotension secondary to dehydration (higher risk patients are older adults or patients taking diuretics)
“Meglitinides (Glinides), mostly ends in glinide
Nateglinide (Starlix), Repaglinide(Prandin,Gluco-
Norm) their mechanism of action is to promote
insulin secretion by the pancreas.”
“Common side effects include hypoglycemia, weight
gain, generally well tolerated. To avoid hypoglycemia
skip meal then skip a dose. Encourage patient
not to use in combination with insulin nor
sulfonylureas due to same MOA”
a-Glucosidase inhibitors (acarbose and miglitol). These medications act in the intestine to delay absorption of carbohydrates and reduce the rise in blood glucose after a meal. These medication inhibit a-glucosidase (an enzyme needed to break down carbohydrates into monosaccharides). They are indicated for type 2 diabetes together with diet modification and exercise. This medication can be used alone or in combination with insulin, metformin, or a sulfonylurea.
AEs include flatulence, cramps, abdominal distension, borborygmus, diarrhea, and possible anemia. When used in combination with insulin or a sulfonlyurea, there is a risk of hypoglycemia. When used long-term and high-dose, there is a risk of liver dysfunction.
Amylin Mimetic: Pramlintide. Pramlintide is a synthetic analog of amylin, a peptide hormone made in the pancreas and correleased with insulin. Pramlintide mimics the effects of amylin, reduces postprandial levels of glucose by delaying gastric emptying and suppressing glucagon secretion. Both act in the brain to increase the sense of satiety, helping to lower caloric intake.
Adverse Effect: Risk for severe hypoglycemia when combined with insulin, especially in patients with type 1 diabetes. Should not be given to patients who have hypoglycemia unawareness, poor adherence to insulin regimen, poor adherence to SMBG, or recurrent hypoglycemia needing assistance. Nausea occurs early in therapy, and is more common in patients with type 1. Injection site reaction may occur (redness, swelling, or itchining at the site).
DPP-4 Inhibitors (Gliptins)-they enhance the activity of incretins (by inhibiting their breakdown by DPP-4) and thereby increases insulin release, reduce glucagon release and decrease hepatic glucose production.
Adverse Effects: Pancreatitis, hypersensitivity reactions
“Dopamine Agonist: Bromocriptine (Cycloset)
Activates dopamine receptos in the central nervous system; how it improves glycemic control is unknown”
Adverse Effects: Orthostatic hypotension, Exacerbation of psychosis
GLP-1 receptor agonist (Exenatide) - Exenatidine is a GLP-1 receptor agonist released from the gut and acts to increase glucose-dependent insulin secretion from pancreatic beta cells, suppress glucagon secretion,delay gastric empyting, and reduce food intake
Adverse Effects: Hypoglycemia, nasuea, emesis, diarrhea and weight loss
DDP-4 inhibitors (Gliptins) work by inhibiting the breakdown of incretins by DPP-4, which allows for enhanced incretin activity. Gliptins can be used as monotherapy for glycemic control in type 2 diabetes or as add-on therapy to other oral agents.
Major adverse effects of Gliptins includes pancreatitis and hypersensitivity reactions. The FDA warns it may be associated with an increased risk of heart failure, particularly for patients with a history of heart or kidney disease. The FDA also warns that Gliptins may be associated with potentially severe and disabling joint pain.
