Endocrine

Insulin

released from beta cells of the islets of Langerhans, used for glucose uptake by the liver and transported into skeletal muscle and adipose tissue

glucagon

released from alpha cells of the islets of Langerhans in the pancreas to break down glycogen and release glucose into the blood stream

How does the liver increase glycogen synthesis?

Increases enzyme activity that converts glucose to glycogen, inhibits glycogenolysis, and increases the synthesis and storage of triglycerides and formation of VLDL

How does insulin impact the muscle and adipose tissue

recruits GLUT4 transporters to the plasma membrane and promotes synthesis

What is the pharmacologic treatment for diabetes besides insulin?

oral antidiabetic drugs, incretin mimetic, amylinomimetic

What are biguanides?

most common oral antidiabetic, often used as first line to reduce hepatic gluconeogenesis and insulin resistance via GLUT-4 transporters

True or false: biguanides (metformin) causes hypoglycemia and weight gain

false: metformin does not do these

What are sulfonylureas?

antidiabetic med that stimulates release of insulin from functioning pancreatic beta cells

Examples of sulfonylureas (antidiabetics)

glipizide (glucotrol), glyburide (micronase, DiaBeta)

What are the concerns of sulfonylureas (antidiabetic)?

hypoglycemia in the malnourished older adult or those with liver problems, weight gain

Meglitinides have a similar therapeutic effect to sulfonylureas (antidiabetic), what are the advantages?

reduced risk of hypoglycemia, less weight gain

What are thiazolidinediones (TZDs)?

increases muscle, liver, and adipose tissue sensitivity to insulin

Examples of thiazolidinediones (TZDs)

rosiglitazone (avandia), pioglitazone (actos)

What are the concerns with thiazolidinediones (TZDs)?

weight gain, fluid retention

What is an advantage of thiazolidinediones?

improvement in lipid profile

What are alpha-glucosidase inhibitors?

inhibit the enzyme alpha-glucosidase which is responsible for carbohydrate breakdown to glucose in order to be absorbed into bloodstream

Where do alpha-glucosidase inhibitors act in the body?

intestine

What are some examples of alpha-glucosidase inhibitors?

acarbose (precose), miglitol (glyset)

What are the concerns with alpha glucosidase inhibitors?

GI symptoms due to fermentation of unabsorbed carbohydrates by bacteria in the colon, hypoglycemia if administered with other things

True or false: when alpha glucosidase inhibitors are administered alone, there is a risk of hypoglycemia

false: there is only a risk if administered with other things

What are dipeptidyl peptidase-IV inhibitors?

glucagon-like peptide-1 (GLP 1) is released by endocrine cells in small intestine and increases insulin release, slows gastric emptying, inhibit glucagon secretion and produce sense of satiety

What is the therapeutic effect of dipeptidyl peptidase-IV inhibitors?

inhibits dipeptidyl peptidase-IV, the enzyme responsible for breakdown of glucagon-like peptide (GLP-1)

What is the concern with dipeptidyl peptidase-IV inhibitors?

GI distress

Examples of dipeptidyl peptidase-IV inhibitors

sitagliptin (januvia) and saxagliptin (onglyza)

What are sodium-glucose co-transports?

co-transporter that is located in the proximal nephron in kidney that reabsorbs majority of glucose that is filtered

What are sodium-glucose co-transport 2 inhibitors?

inhibit co-transporter to increase the excretion of glucose in the urine to lower blood glucose levels

Examples of sodium-glucose co-transporter 2 inhibitors

canaglifozin (invokana), dapagliflozin (farxiga), empaglifozin (jardiance)

What are the concerns with SLGT2 inhibitors?

acute kidney injury, hypotension

What is the advantage with SLGT2 inhibitors?

possible reduction in weight and blood pressure without hypoglycemia

What is the therapeutic effect of incretin mimetic?

exerts similar effects as GLP-1

Example of incretin mimetic

exenatide (byetta)

How is incretin mimetic administered and why is it important?

injection because an oral or IV form would degrade too quickly

What are the concerns with incretin mimetics?

nausea/vomiting, hypoglycemia if administered with sulfonylurea

What are amylinomimetics?

synthetic analog of amylin, which prolongs gastric emptying and reduces glucagon secretion after a meal

example of amylinomimetic

pramlintide (symlin)

W\hat is the concern with amylinomimetic?

if administered with insulin, insulin dose must be reduced to avoid hypoglycemia

How is dosing expressed for insulin and how is it adminstered?

units, IV or insulin pump

What is the purpose of ultra-rapid acting insulin?

therapeutic effect is to dissolve rapidly at site of administration to lower blood sugar immediately before meals

Examples of ultra-rapid acting insulin

insulin lispro (humalog), insulin aspart (novolog), insulin glulisine (apidra)

What is the onset of action for ultra-rapid insulin?

5 minutes, peak action is 1 hour, lasts for 3-5 hours

true or false: rapid acting insulin is the same as regular insulin

true

What is the therapeutic effect of rapid acting insulin?

lower blood sugar 1+ hours before a meal

What is the onset of action for rapid-acting insulin?

onset action is 30 minutes, peak is 2 hours, lasts for 6-8 hours

Examples of rapid-acting insulin

humulin R, nobolin R

What is the purpose of an NPH insulin (intermediate acting)?

slows absorption of insulin, is added to regular insulin

What is the onset of action for intermediate acting insulin?

onset is 1-4 hours, peak is 6-12, duration is 14-24 hours

Examples of intermediate-acting insulin

humulin N, novolin N

What is the onset of action of long-acting insulin?

onset is 4-6 hours, peak is 8-20, duration is up to 36 hours

Examples of long-acting insulin

insulin glargine (lantus), insulin detemir (levemir)

What are the general adverse effects of insulin?

hypoglycemia, weight changes, seizures, dizziness, visual disturbance

true or false: Exercise improves insulin sensitivity

true: it stimulates GLUT-4 transporters in muscle and improves glycogen storage

What are statins?

HMG-CoA reductase inhibitors that competitively inhibit the process for biosynthesis of cholesterol in the liver

Side effects of statins

liver abnormalities, muscle pain, food/drug interactions (grapefruit), GI disturbance

What is ezetimibe?

LDL lowering agent that helps avoid large doses of statins

What is the therapeutic effect of ezetimibe?

cholesterol absorption inhibitor in the intestine, impairs dietary and biliary cholesterol absorption

How are hypothyroid conditions managed?

synthetic T4 levothyroxine

What is the first line of therapy for osteoporosis?

oral bisphosphonates that inhibit osteoclast recruitment

Examples of oral bisphosphonates for osteoporosis

alendronate, risedronate

Side effects of oral bisphosphonates

esophagitis, nausea, abdominal pain, osteonecrosis of the jaw