Diabetes Flashcards
Features of regular insulin
physiologic levels of zinc, no protein
readily soluble and rapidly absorbed
onset 1/2 to 1 hour, peak in 2-4h duration of 5-8h
Can be given IV
Features of isophane insulin
insulin complexed with the protein protamine at neutral pH (NPH)
Onset 1-2h peak 6-12h duration 18-24h
Cannot be used IV
Therapeutic use of regular insulin
for pre-meal use, short duration
Therapeutic use of isophane insulin
between meal use, often combined with regular insulin at meal times
Rapid and short acting insulin analog
Insulin Lispro
What are the therapeutic considerations for insulin lispro
does not dimerize so acts more quickly and has shorter duration. This means that timing for meals is less important and there is less chance of hypoglycemia after meals/missed meals
Slow and short acting insulin analog
Insulin glargine
Features that reduce solubility of insulin glargine
formulated with zinc and at acidic pH slows absorption
Dosing of insulin glargine
sub cutaneous once daily
Considerations for injecting rapid and slow insulin analogs
can be used together, but not mixed before injection
Inhaled insulin
Afrezza
What is the treatment for severe hypoglycemia where the patient is unconscious
glucagon
What is the only novel diabetes drug on the market
Pramlintidine
MOA of pramlintidine
analog of amylin, peptide hormone release from beta cells along with insulin, which decreases liver glucose production
What is the advantage with pramlintidine
decreases gastric emptying and reduces weight gain
Therapeutic use/dosing of pramlintidine
only given in combination with normal insulin injected sub
What is the prototype sulfonylureas (SUs)
Glimepiride
What is the MOA of glimepiride
block the ATP sensitive channel in islet cells, which leads to calcium dependent release of insulin. Increases insulin release
Dosing for glimepiride
once daily
Metabolism of glimepiride
metabolized by liver and excreted by kidney, contraindicated in liver and kidney disease
What is the MOA of meglitinides
similar to SUs, not very effective
What is the prototype for biguanides
metformin
What is the MOA of metformin
activates AMP-K, increases glucose uptake in liver, does not alter insulin level, so no risk of hypoglycemia
Pharmacokinetics of metformin
2-4 times per day orally, excreted unmetabolized by kidneys, contraindicated in patients with kidney disease
Advantages of metformin
does not cause hypoglycemia or weight gain
Adverse effects of metformin
Inhibits lactate metabolism, can cause lactic acidosis, especially in patients with impaired liver function
Unpleasant GI effects
Prototype drugs of Reducers of GI glucose
Acarbose
MOA of acarbose
microbial sugars that inhibit sugar metabolism in the gut
dosing of acarbose
immediately before meals, always used with other agents
Side effects of acarbose
can caused hypoglycemia when in combination with other agents, not on its own
Adverse GI effects (farts), especially in combination with metformin
Prototype thiazolidinediones
Pioglitazone
MOA of Pioglitazone
increases PPAR-gamma activity, increases transcription of insulin responsive genes
- decreases gluconeogenesis
- increase glucose uptake in muscle and adipocytes
Pharmokinetics of pioglitazone
orally effective, taken with food
metabolized by liver, excreted in feces
Adverse effects of piogliatazone
hepatotoxicity, cardiovascular
