Diabetes Flashcards
Drugs used to treat diabetes
○ Biguanides/Metformin
○ Sulfonylureas
○ Thiazolidinediones (TZDs)
○ Dipeptidyl peptidase-4 (DDP-4) inhibitors
○ Glucagon-like peptide-1 (GLP-1) agonist
○ Sodium-glucose cotransporter-2 (SLGT-2) inhibitors
○ Insulin
Biguanides example
Agents: Metformin (Glucophage™)
○ Immediate Release Formulation
○ Extended Release Formulation
Biguanides MOA
Decreases hepatic glucose production, decreased intestinal
glucose absorption, and increases insulin sensitivity and peripheral glucose uptake and
utilization
Biguanides preferred
Preferred initial agent for type 2 diabetes
Biguanides efficacy
Efficacy: Decreases A1C approximately 1-1.5%
Biguanides SE
○ GI Upset (diarrhea, nausea, upset stomach, flatulence)
○ B12 and other vitamin deficiencies
Biguanides do what to avoid SE
take with food
Biguanides Serious side effects
○ Lactic Acidosis
Biguanides Monitoring
○ Side effects (mainly GI)
○ Renal Function
○ Lactic Acidosis
○ A1C, Fasting and 2-hour PP Blood glucose
Biguanides Contraindications
○ eGFR <30mL/min
Sulfonylureas - agents
glipizide (Glucotrol™), glimepiride (Amaryl™), and glyburide (Glynase™)
Sulfonylureas - MOA
: Stimulates insulin secretion from functioning beta cells in the
pancreas, especially in response to a meal; may also increase insulin sensitivity and lower
hepatic glucose production
Sulfonylureas - Efficacy
○ Hypoglycemia
○ Weight gain
Sulfonylureas - Common side effects
○ Hypoglycemia - Avoid in elderly patients for fall risk
Sulfonylureas - Serious side effects
○ Hypoglycemia!
○ A1C, blood glucose
Sulfonylureas monitoring
○ Avoid in patients with G6PD deficiency
○ Glimepiride - Avoid in the elderly
Sulfonylureas - place in therapy
○ Really fallen out of favor given newer agents with better benefits
○ Used when cost is a major issue (uninsured/underinsured)
Sulfonylureas administration
○ Take with food for ER products and just before (30ish minutes) before a meal for IR products
○ ER tablets should not be crushed/chewed
Sulfonylureas - Pearls
Inexpensive and generally well covered
Biguanides - place in therapy
○ First line for management of Type 2 Diabetes
○ Should be continued for as long as possible
Biguanides administartion
○ Take with food to reduce GI upset
Biguanides - pearls
○ ER formulation less likely to cause GI upset
○ Osmotic ER formulation is rarely covered by insurance
○ Take with food
Thiazolidinediones (TZDs) - Agents
pioglitazone (Actos™) and rosiglitazone (Avandia™)
Thiazolidinediones (TZDs)
- MOA
: increases insulin-dependent glucose disposal and decreases
hepatic glucose output by decreasing insulin resistance in the periphery and in the liver
Thiazolidinediones (TZDs)
Efficacay
Decreases A1C approximately 1-1.5%
Thiazolidinediones (TZDs)
SE
○ Edema
○ Weight Gain
○ Headache
Thiazolidinediones (TZDs)
- Seriously SE
Heart Failure
○ LFT elevations
Thiazolidinediones (TZDs)
Monitoring
○ LFTs prior to therapy
○ Signs/symptoms of heart failure
○ A1C, blood glucose
Thiazolidinediones (TZDs)
- Precautions
History of heart failure
○ Severe edema
○ Generally not recommended with renal impairment - fluid retention
Thiazolidinediones (TZDs)
Place in Therapy
Used less often, generally third line agent after metformin and another agent
○ Generally used when cost is a concern
Thiazolidinediones (TZDs)
Administration
Can take with or without food
Thiazolidinediones (TZDs)
Pearles
Avoid with patients with history of heart failure
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Agents
Agents: sitagliptin (Januvia™), linagliptin (Tradjenta™), alogliptin (Nesina™), saxagliptin
(Onglyza™)
○ The “gliptins”
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- MOA
protects glucose-dependent insulinotropic polypeptide (GIP) and
glucagon-like peptide (GLP-1) from inactivation by DPP-4, thereby enhancing their
actions; Increases insulin release and decreases glucagon levels in the circulation in a
glucose-dependent manner
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Efficacy
Decreases A1C approximately 0.5-1%
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Common Side Effects
○ Headache
○ Nasopharyngitis
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Serious Side Effects
Pancreatitis
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Monitoring
○ Renal Function
■ Dosing Adjustments: sitagliptin, saxagliptin, alogliptin
○ A1C, Blood glucose
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Contraindications
○ Concomitant use of sulfonylurea
○ Heart Failure
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Place in Therpay
○ More rarely used but sometimes used as a 3rd line option
○ Similar mechanism of action to GLP-1 agonists, so generally not used in combination with these
agents
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Administration
○ Take with or without food
Dipeptidyl Peptidase-4 Inhibitors (DPP-4
Inhibitors)
- Pearls
Becoming increasingly well covered
