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75 Cards in this Set
- Front
- Back
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what type of receptor does insulin act on?
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tyrosine kinase
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what does insulin's activation of the tyrosine kinase receptor lead to?
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phosphorylation of the receptor and then phosphorylation of 5 insulin receptor substrates
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what happens downstream to tyrosine kinase receptor activation?
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PI 3-kinase activates PKC and Akt which are responsible for anabolic actions
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what is responsible for mitogenesis and cell proliferation?
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Shc/IRS binding and activating Grb-2/SOS
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what pump does insulin stimulate?
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Na+/K+ ATPase to stimulate K+ influx
can be used to rapidly reduce K+ levels |
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what type of nervous system will stimulate insulin secretion?
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parasympathetic
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what type of nervous system will inhibit insulin secretion?
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sympathetic stimulation
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how does glucose depolarize the insulin secreting cell?
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an increase in the ATP/ADP ratio
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how does an increase in the ATP/ADP ratio lead insulin release?
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by partially depolarizing the cell, voltage-gated Ca++ channels open up and increased Ca2+ leads to release from insulin containing granules
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what is lispro?
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a rapid acting insulin
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what is aspart?
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a rapid-acting insulin
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what is gluslisine?
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a rapid-acting insulin
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how fast and how long do rapid-acting insulins work?
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onset in 10-15mins
work for 3-5 hours |
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what do modifications to rapid-acting insulin affect?
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do not affect binding, half-life, or immunogenicity
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what is novolin?
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a short-acting insulin
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what is humulin?
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a short acting insulin
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what is velosulin?
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a short acting insulin
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what insulin is identical to human insulin?
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short acting
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how fast and how long do short acting insulins work?
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actin in 2-3hours, last 5-8
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in terms of monomers, dimers, and hexamers, which is the fastest and slowest?
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hexamers are slowest
monomers are fastest |
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what breaks down into hexamers, dimers, and monomers?
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short-acting insulin
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how are short acting insulins administered?
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IV
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when should short-acting insulins be administered?
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30-45mins before meal time
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what is NPH insulin?
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an intermediate acting insulin
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what is humulin/novolin?
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intermediate acting insulins
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what are intermediate acting insulins mixed with?
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protamine
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how fast and how long do intermediate acting insulins work?
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2-5 hours; last for 4-12 hours
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what is usually mixed with short or rapid acting insulin?
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intermediate acting insulin
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what is a peakless insulin?
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long acting/glargine
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what is glargine?
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a long acting insulin
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how fast/how long does glargine work?
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4-6 hours/ last 11-24 hours
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what should not be mixed with other insulin preps because it must be kept acidic?
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glargine
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what is detemir?
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a long acting insulin
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how fast/how long does detemir work?
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1-2 hours/lasts 24+ hours
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what are glipizide and glimepiride?
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sulfonylureas insulin secreatgogues
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What is the MOA of glipizide and glimepiride?
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they cause hypoglycemia by stimilating the release of insulin by binding to the SUR1 subunit of the K+ channel
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what do gilpizide and glimepiride do for peripheral insulin sensitivity?
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increase it
decrease Hb1Ac by 1.5-2% |
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what are gilpizide and glimepiride used for?
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conrtol hyperglycemia in 2DM
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what does administration of gilipizide and glimepiride require?
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dietary restrictions
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who is gilipizde and glimepiride contraindicated in? (3)
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1DM
hepatic/renal insufficiency pregnancy |
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what can glimipiride and glipizide cause secondarily?
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beta cell burnout leading to decreased insulin release
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what is an important adverse effect of glimipiride and glipizide?
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weight gain (4kg)
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what are repaglinide and nateglinide?
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insulin secretagauges belonging to the meglitidine class
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what is the MOA of repaglinide and nateglinide?
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close the ATP-dependent K+ channel causing depolarization, influx of Ca++, and insulin release
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what are repaglinide and nateglinide used for?
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preprandially because their levels peak in 1 hour
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what are repaglinide and nateglinide used in combination with?
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insulin sensitizers
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what is an adverse side effect of repaglinide and nateglinide?
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hepatic/renal insufficency
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what is metformin?
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an insulin sensitizer
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what is metformin the first line drug for?
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to reduce A1C by 1.5-2%
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what is the MOA of metformin? (2)
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decreases hepatic glucose and GI uptake
increased insulin actions in muscle and fat |
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who is metformin contraindicated in?
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any condition that predisposes to lactic acidosis (renal/hepatic dysfunction, heart failure)
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what is an important side effect of metformin?
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N/V, abd pain, flatulence
should be titrated |
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what is pioglitazone?
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an insulin sensitizer
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what is the MOA of pioglitazone?
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agonist for nuclear peroxisome proliferator-activated receptor
activates insulin responsive genes that regulate lipid and carb metabolism |
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what does pioglitazone require for activity?
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insulin
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what are 2 serious side effects of pioglitazone?
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liver problems
anemia, weight gain, plasma volume expansion possibly leading to heart failure |
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what are acarbose and miglitol?
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alpha-glucosidase inhibitors
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what is the MOA of acarbose and miglitol?
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competitively inhibit enzymes involved in glucose metabolism, primarily alpha-glucosidease in the liver which slows the absorption of carbs
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what drug has no direct insulin release and therefore won't cause hypoglycemia?
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acarbose and miglitol
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what is an adverse side effect of acarbose and miglitol?
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dose-related malabsorption of carbs
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what can sulfonyureas be combined with? (3)
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metformin
pioglitazone (TZD) all 3 together |
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what can metformin be combined with? (3)
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sulfonyureas
pioglitazone (TZD) all 3 together |
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what types of combinations are not recommendations? (3)
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2 types of insulin secretagogues
SUs in 1DM SU with insulin |
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what is amylin?
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a protein co-secreted with insulin
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what does amylin do? (3)
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delays gastric emptying
inhibits glucagon secretion synergistic with insulin |
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what is pramintide?
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a synthetic analog of amylin that modulates post-prandial glucose levels
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what is exenatide?
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a glucagon like peptide analog
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what does exenatide do?
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stimulates the GLP-1 receptor to cause an increase in insulin expression
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what is exenatide dependent of?
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glucose
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what is exenatide a mimetic of?
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incretin
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what is an unusual effect of exenatide?
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weight loss
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what is sitaglipin?
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a dipeptidal peptidase-IV inhibitor
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how does sitaglipin work?
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it inhibits DPP-IV, preventing the degradation of GLP-1 and other GLP-1 like molecules
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what does sitaglipin stimulate?
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glucose depdendent insulin secretion
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what is an adverse effect of sitaglipitin?
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dose adjustment in renal patients
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