Endocrine Pharm Flashcards
What is insulin?
- Hormone synthesized by beta cells of pancreas within islets of langerhans
- Proinsulin = insulin precursor
Categories of insulin
- Rapid Acting
- Short Acting
- Intermediate Duration
- Long Duration
Rapid Acting Insulin
- Lispro
- Onset 10-20 minutes
- Give if incredibly hyperglycemic
- Need to take RIGHT before eating (tray is in the room)
- Peaks in 30 min - 2.5 hours and lasts 3-6 hours
- Varies based on absorption because given SC
- Commonly used with meals
Short Acting Insulin
- Regular insulin
- Onset 30-60 min
- Peak 1-5 hours
- Lasts 6-10 hours
- Should take with meals but not as quickly as rapid acting
- Also helps with hyperkalemia
Intermediate Duration Insulin
- NPH
- Works in 1-2 hours
- Peaks 6-14 hours
- Lasts 16-24 hours
- Mimic what pancreas would be doing constantly
Long Duration Insulin
- Glargine
- No peak
- Mimic what pancreas would be doing constantly
- Steady
- Works in 70 minutes
- Lasts 24 hours
- Nice because don’t have to take so many times each day
What is a common insulin regimen?
Intermediate/long acting and rapid/short acting around meal times
Mixing Insulins
- Often use short acting and longer acting simultaneously
- NPH is compatible with regular, lisper, apart, glulisine
- Draw up short acting first
Administration of Insulin
- SC injections:
- Syringe and needle, pen injectors, jet injectors, subcutaneous pumps
Side effects of insulin
- Hypoglycemia
- Hypokalemia
- Allergic rxn: irritation around injection site
Treatment of Hypoglycemia
- IV: Dextrose 50% injection
- IM: Glucagon breaks down glycogen to glucose, works in 10-15 min
Metformin (Biguanide)
- Often initial drug of choice for Type 2 DM
- MOA: inhibits glucose production in liver, reduces glucose absorption in gut, sensitizes insulin receptors in target tissues
- DOES NOT STIMULATE INSULIN RELEASE (would not cause hypoglycemia)
- Slowly absorbed from small intestines
- Excreted unchanged in kidneys
- Most common side effects: GI (decreased appetite, n and d)
- Start with low dose and titrate to tolerate effects
- 3-5% of patients will stop using bc GI effects
Toxicity and Cautions of Metformin
- Inhibit mitochondrial oxidation of lactic acid = can lead to lacticacidosis (rare but life threatening)
- Caution in patients with poor renal function bc increased risk of lacticacidosis
- Contraindicated within 48 hours of IV contrast admin
Sulfonylureas
- First oral anti diabetic available
- MOA: stimulate release of insulin from pancreatic islets (will not work if pancreas doesn’t work)
- Can be used in combination with metformin
2 Generations of Sulfonylureas
- First gen: uncommon, not seen anymore
- Second gen: Glipizide = immediate and sustained release
AE of Sulfonylureas
- Hypoglycemia: because causes release of insulin from pancreas
- Really eliminated: can be a problem if we have a kidney problem
- Reduce dose in elderly
- Avoid in pregnancy: can cause hypoglycemia in fetus upon birth
Thiazolidinediones
- MOA: reduces insulin resistance and decreases glucose production by activating PPAR gamma enzyme
- Usually used in combination with other agents
- Prototype: Pioglitazone
Pioglitazone
- Metabolism: CYP2C8 = drug interactions
- AE: most common are resp tract infection, headache, sinusitis, myalgia
- Most important AE: fluid retention (worry about this in heart failure), hypoglycemia
Meglitinides
- MOA: stimulate insulin release
- Prototype: Repaglinide
- If don’t respond to sulfonylurea then won’t respond to this
- Metabolized by liver with VERY short half life (important because must give frequently)
- AE: hypoglycemia
- Rapidly absorbed from GI tract so have to eat within 30 minutes
Incretin Hormes
- Glucagon-like peptide-1 (GLP-1) and GIP
- Secreted following meal ingestion
- DPP-4 enzyme inactivates GLP-1 and GIP
- GLP-1 and GIP facilitate release of insulin from B cell in pancreas and prevent glucagon release from liver
Gliptins: DPP-4 Inhibitors
- Cause GLP-1 and GIP to go to pancreas
- Stimulate insulin release and block glucagon release
- Prototype: Sitagliptin
- AE: Upper resp infection, headache, inflammation in nose and throat
- Serious AE: Hypoglycemia, pancreatitis, hypersensitivity reactions (anaphylaxis and SJS)
Incretin Mimetics
- Prototype: Liraglutide
- MOA: analog of human GLP-1 that causes direct activation of GLP-1 Receptors
- Can be used alone or with other things (watch with sulfonylurea to avoid hypoglycemia)
- Administered via SQ injection
- AE: dose-related GI effects and rare cases of pancreatitis