Diabetes Drugs: Part Of Exam 3

Question 1

Insulin functions

Answer 1

It stimulates carbohydrate metabolism in skeletal and cardiac muscle and in adipose tissue by facilitating the transport of glucose into these cells. In the liver, insulin facilitates the phosphorylation of glucose to glucose-6-phosphate, which is then converted to glycogen for storage. By causing glucose to be stored in the liver as glycogen, insulin keeps the kidney free of glucose. It stimulates lipogenesis and inhibits lipolysis and the release of fatty acids from adipose cells. insulin stimulates protein synthesis and promotes the intracellular shift of potassium and magnesium into the cells.

Question 2

Rapid-acting Insulin

Answer 2

Most rapid onset of action (5 to 15 minutes)
Peak: 1 to 2 hours
Duration: 3 to 5 hours
Patient must eat a meal after injection.
Insulin lispro (Humalog)
Similar action to endogenous insulin
Insulin aspart (NovoLog)
Insulin glulisine (Apidra)
May be given subcutaneously (SUBQ) or via continuous SUBQ infusion pump (but not intravenously [IV])

Question 3

Afrezza

Answer 3

Rapid-acting insulin that is inhaled
Peak of 12 to 15 minutes
Short duration of action of 2 to 3 hours
Administered within 20 minutes before each meal
Must be given in conjunction with long-acting insulins or oral diabetic agents (for type 2 DM)
Side effects: hypoglycemia, cough, and throat pain
Contraindicated: smokers and those with chronic lung diseases
Black box warning regarding the risk of acute bronchospasms

Question 4

Short-Acting Insulins

Answer 4

Regular insulin (Humulin R)
Routes of administration: IV bolus, IV infusion, intramuscular (IM), SUBQ
SUBQ route:
Onset: 30 to 60 minutes
—Peak: 2.5 hours
—Duration: 6 to 10 hours
IV route:
—Immediate onset
—Duration: 2 to 6 hours

Question 5

Intermediate-Acting Insulins

Answer 5

Insulin isophane suspension (also called NPH)
Cloudy appearance
Often combined with regular insulin
Onset—1 to 2 hours
Peak—4 to 8 hours
Duration—10 to 18 hours

Question 6

Long-Acting Insulins

Answer 6

Insulin glargine (Lantus)
Clear, colorless solution
Constant level of insulin in the body
Usually dosed once daily
Can be dosed every 12 hours
Referred to as basal insulin
Onset: 1 to 2 hours
Peak: none
Duration: 24 hours
Toujeo is insulin glargine that is available as a more concentrated, U-300, form.

Question 7

Insulin detemir (Levemir)

Answer 7

Long acting
Duration of action is dose dependent.
Lower doses require twice-daily dosing.
Higher doses may be given once daily.

Question 8

Insulin glargine (Lantus or Basaglar)

Answer 8

Long acting
Biosimilar insulin
U100

is unique in that it provides a constant level of insulin in the body. This enhances its safety, because blood levels do not rise and fall as with other insulins. Sometimes referred to as a basal insulin

Question 9

Insulin degludec (Tresiba)

Answer 9

Ultra long acting
Once daily
U100 or U200

Question 10

Metformin

Answer 10

Metformin is currently the only drug classified as a biguanide. Metformin works by decreasing glucose production by the liver. It may also decrease intestinal absorption of glucose and improve insulin receptor sensitivity. Unlike sulfonylureas, metformin does not stimulate insulin secretion and therefore is not associated with weight gain and significant hypoglycemia when used alone.

Question 11

Biguanides (Metformin): Adverse Effects

Answer 11

Primarily affects gastrointestinal (GI) tract: abdominal bloating, nausea, cramping, diarrhea, feeling of fullness
May also cause metallic taste, reduced vitamin B12 levels
Lactic acidosis is rare but lethal if it occurs.
Contraindicated in renal or hepatic disease
Does not cause hypoglycemia

Question 12

Non-Insulin Antidiabetic Drugs: Sulfonylureas

Answer 12

Second generation: glimepiride (Amaryl), glipizide (Glucotrol), glyburide (DiaBeta)
Stimulate insulin secretion from the beta cells of the pancreas, thus increasing insulin levels
Beta cell function must be present.
Improve sensitivity to insulin in tissues
Result in lower blood glucose level
Adverse effects: hypoglycemia, hematologic effects, nausea, epigastric fullness, heartburn, many others

Question 13

Non-Insulin Antidiabetic Drugs: Glinides

Answer 13

Repaglinide (Prandin), nateglinide (Starlix)
Indication: type 2 DM
Action similar to sulfonylureas
Increase insulin secretion from the pancreas
Adverse effects: hypoglycema, weight gain

Question 14

Non-Insulin Antidiabetic Drugs:Thiazolidinediones (Glitazones)

Answer 14

Thiazolidinediones (glitazones)
Pioglitazone (Actos)
Rosiglitazone (Avandia)
—Only available through specialized manufacturer programs
Insulin-sensitizing drugs= increasing sensitivity of insulin receptors
Indication: type 2 DM
MOA:
—Decrease insulin resistance
—“Insulin sensitizing drugs”
—Increase glucose uptake and use in skeletal muscle
—Inhibit glucose and triglyceride production in the liver
Adverse effects: contraindicated in heart failure patients because can exacerbate HF

Question 15

Non-Insulin Antidiabetic Drugs: Alpha-Glucosidase Inhibitors

Answer 15

Acarbose (Precose), miglitol (Glyset)
Indication: type 2 DM
Contraindications: certain bowel disorders
MOA: Reversibly inhibit the enzyme alpha glucosidase in the small intestine
Result in delayed absorption of glucose
Must be taken with meals to prevent excessive postprandial blood glucose elevations (with the “first bite” of a meal)
Adverse effects: Flatulence, diarrhea, abdominal pain

Question 16

DPP-IV Inhibitors Adverse Effects

Answer 16

Upper respiratory tract infection, headache, and diarrhea
Hypoglycemia can occur and is more common if used in conjunction with a sulfonylurea.
Possible pancreatitis

Question 17

Amylin Agonist

Answer 17

Pramlintide (Symlin)
—Mimics the natural hormone amylin
—Slows gastric emptying
—Suppresses glucagon secretion, reducing hepatic glucose output
—Centrally modulates appetite and satiety
—Used when other drugs have not achieved adequate glucose control
—SUBQ injection

Question 18

Amylin Agonist Indications

Answer 18

Patients with Type 1 or Type 2 diabetes who receive mealtime insulin and who have failed to achieve optimal glycemic control with insulin
Contraindication: gastroparesis
The patient’s usual insulin dose usually needs to be reduced by 50%
Give 1 hour before other oral medications as it can delay oral absorption of other drugs.

Question 19

Non-Insulin Antidiabetic Drugs: Sodium Glucose Cotransporter Inhibitors (SGLT2 Inhibitors)

Answer 19

Inhibition of SGLT2 leads to a decrease in blood glucose caused by an increase in renal glucose excretion.
SGLT2 inhibitors: new class of oral drugs for the treatment of type 2 DM
Canagliflozin (Invokana), dapagliflozin (Farxiga), and empagliflozin (Jardiance), ertugliflozin (Steglatro) and others in development
Action: work independently of insulin to prevent glucose reabsorption from the glomerular filtrate, resulting in a reduced renal threshold for glucose and glycosuria

Question 20

SGLT2 Inhibitors
Adverse effects

Answer 20

Genital yeast infections
Urinary tract infections
Increased urination
Hypotension,
Hypovolemia
Hyperkalemia
Possible ketoacidosis, acute kidney injury
2018 FDA warning: necrotizing fasciitis of the perineum (Fournier’s gangrene)