PHARM EXAM 4: Antidiabetic Medications Oral Agents

Insulin Secretagogues drugs

• Sulfonylureas

• Meglitinides

Insulin Secretagogues what do they do

Both stimulate release of insulin from the pancreas

Insulin Secretagogues: meglitinides is

significantly faster and shorter acting

Sulfonylureas drug

Second generation Agents:

• Glipizide (Glucotrol), Glyburide (DiaBeta, Micronase, Glynase), Glimepride (Amary

Sulfonylureas: MOA

stimulates the release of insulin from the pancreas

Sulfonylureas: duration

12-24 hours

Sulfonylureas: use

type 2 diabetes

Sulfonylureas: adverse effects

hypoglycemia; weight gain

Sulfonylureas nursing consideration

• Contraindicated in pregnancy

• Caution with renal and hepatic disease (increased risk of hypoglycemia)

• Caution with alcohol & beta blockers

Meglitinides (Glinides): drug

Agents: Repaglinide (Prandin), Nateglinide (Starlix)

Meglitinides: MOA

stimulates the release of insulin from the pancreas

Meglitinides duration

Peak one hour; duration four hours

Meglitinides: use

type 2 diabetes

Meglitinides: adverse effects

hypoglycemia (lower risk than with sulfonylureas),

weight gain

Meglitinides: nursing considerations

• Dosing must always be followed by a meal

• Caution with liver dysfunction

Oral Agents Promoting Incretin Effects drugs

Incretin Mimetics: Glucagon-like peptide-1 (GLP-1) receptor agonists

Incretin Promotors: Dipeptidyl peptidase – IV (DPP – 4) inhibitors

what are two important incretin hormones secreted by the gut in response to eating

Glucagon-like peptide-1 (GLP-1)

Glucose-dependent insulinotropic polypeptide (GIP)

Glucagon-like peptide-1 (GLP-1)

Stimulates the glucose-dependent release of insulin, inhibits the postprandial release of glucagon,

• (so basically makes body believe that glucose in secreted so the insulin will be secreted but in reality no glucose was secreted just the insulin which is good in diabetes because it is helping blood sugar go down)

slows gastric emptying, and suppresses appetit

what is Glucagon-like peptide-1 (GLP-1) rapidly inactivated by

enzyme dipeptidyl peptidase- IV (DPP-IV)

Glucose-dependent insulinotropic polypeptide (GIP)

• Stimulates the glucose-dependent release of insulin

• Promotes beta cell proliferation

• increases insulin

Glucose-dependent insulinotropic polypeptide (GIP) is inactivated by

DPP-IV as well

Oral Glucagon-Like Peptide 1 (GLP-1) Receptor Agonist: drug

Agents: Semaglutide (Rybelsus)

Oral Glucagon-Like Peptide 1 (GLP-1) Receptor Agonist: MOA

stimulates glucose-dependent release of insulin, inhibits postprandial glucagon release, slows gastric emptying and promotes satiety

Oral Glucagon-Like Peptide 1 (GLP-1) Receptor Agonist: use

Oral adjuvant therapy for type 2 diabetes in patients taking metformin or other oral agents.

Oral Glucagon-Like Peptide 1 (GLP-1) Receptor Agonist: adverse effects

GI common (N/V/abdominal pain), risk of pancreatitis and some thyroid cancers. Contraindicated in some thyroid and related cancers (MTC, MEN).

Oral Glucagon-Like Peptide 1 (GLP-1) Receptor Agonist: nursing consideration

take 1x/day, 30 minutes before the first food of the day. Taken with meals reduces absorption. Excess hypoglycemia when used with insulin or sulfonylureas

Dipeptidyl Peptidase – IV (DPP – 4) Inhibitors (Gliptins): drugs

Sitagliptin (Januvia), saxagliptin (Onglyza), alogliptin (Nesina), linagliptin (Tradjenta)

Dipeptidyl Peptidase – IV (DPP – 4) Inhibitors (Gliptins): MOA

enhances the action of incretin hormones (secrete insulin) by inhibiting dipeptidyl pepsidase – IV (DPP – 4) an enzyme that inactivates incretin

Dipeptidyl Peptidase – IV (DPP – 4) Inhibitors (Gliptins): use

type 2 diabetes with other drugs

Dipeptidyl Peptidase – IV (DPP – 4) Inhibitors (Gliptins): adverse effects

nasal inflammation, upper respiratory infection, risk of pancreatitis, headache

Dipeptidyl Peptidase – IV (DPP – 4) Inhibitors (Gliptins): nursing consideration

If pancreatitis occurs the drug should be permanently discontinued.

Other Oral Agents

• Biguanides

• Sodium-Glucose Co-Transporter 2 (SGLTs) Inhibitors

• Thiazolidinediones (Glitazones or TZDs)

• Alpha-Glucosidase Inhibitors

• None of these independently pose a significant risk of hypoglycemia

Biguanide drugs

Metformin (Glucophage, Fortamet, Glumetza, Riomet)

Biguanide MOA

suppression of hepatic glucose production (primary mechanism), enhances glucose uptake and utilization by muscle (insulin enhancer), decreases glucose absorption in the gut (slightly)

Biguanide use

type 2 diabetes; PCOS (off label)

Biguanide: adverse effects

GI disturbances (nausea, diarrhea, satiety) are common, lactic acidosis (rare but potentially fatal)

Biguanide: nursing considerations

hold with IV dye studies; contraindicated in renal insufficiency; caution in heart failure; avoid alcohol; can cause B-12 and folate deficiencies

Sodium-Glucose Co-Transporter 2 (SGLT2) Inhibitors (Flozin’s): drugs

Canagliflozin (Invokana), dapagliflozin (Farxiga), empagliflozin (Jardiance)

Sodium-Glucose Co-Transporter 2 (SGLT2) Inhibitors (Flozin’s): MOA

blocks the action of SGLT2. SGLT2 works in the kidney to reabsorb glucose. Blocking SGLT2 results in more glucose being excreted in the urine.

Sodium-Glucose Co-Transporter 2 (SGLT2) Inhibitors (Flozin’s): use

type 2 diabetes; cardiovascular and renal protective, reduce heart failure risk

Sodium-Glucose Co-Transporter 2 (SGLT2) Inhibitors (Flozin’s): adverse effects

UTI and yeast infections. Can lead to plasma volume depletion. because peeing and secreting more

Sodium-Glucose Co-Transporter 2 (SGLT2) Inhibitors (Flozin’s): nursing considerations

can cause postural hypotension in elderly due to increased urination reducing plasma volume. Reduces blood sugar independent of insulin.

Thiazolidinediones (Glitazones or TZDs): drugs

Pioglitazone (Actos); Rosiglitazone (Avandia) only available under restricted access

Thiazolidinediones (Glitazones or TZDs): MOA

reduces insulin resistance of fat & muscle, may decrease glucose production

Thiazolidinediones (Glitazones or TZDs): use

type 2 diabetes

Thiazolidinediones (Glitazones or TZDs): adverse effects

edema, URI, sinusitis, myalgia; HF due to fluid retention greatest concer

Thiazolidinediones (Glitazones or TZDs): nursing consideration

instruct patients to report signs of HF; weight gain; possible hepatotoxicity - monitor ALT levels; increased risk of bone fractures in women; contraindicated in bladder cancer.

• why we dont really use these drugs

Alpha-glucosidase inhibitors: drugs

Acarbose (Precose), Miglitol (Glycet)

Alpha-glucosidase inhibitors: MOA

inhibits alpha-glucosidase which breaks down complex carbohydrates. Delays intestinal absorption of carbohydrates, reducing postprandial hyperglycemia (because more of it is going straight thru rather than being broken down and disgested)

Alpha-glucosidase inhibitors: use

type 2 diabetes, limited effectiveness

Alpha-glucosidase inhibitors: adverse effects

GI disturbances common - abdominal pain, diarrhea etc. Liver dysfunction with high dose acarbose therapy; monitor liver function.

Alpha-glucosidase inhibitors: nursing considerations

contraindicated with some GI disease. If patient becomes hypoglycemic must use glucose (not sucrose) to treat

most patients with type 2 diabetes require

multiple medications.

what oral drug is the most commonly used

metformin

diabetes combination products are

more convenient and improve compliance