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171 Cards in this Set

  • Front
  • Back
What are 2 major functions of the endocrine system?
1. communicate
2. maintain homeostasis
Name 2 hormones secreted by the pancreas.
1. glucagon
2. insulin
Which pancreatic cells secrete glucagon?
alpha cells
What does glucagon do?
increases the hepatic glucose output .:. increases blood glucose concentration
Which pancreatic cells secrete insulin?
beta cells
What is the function of insulin?
promote the uptake, utilization, and storage of glucose .:. lowers blood glucose concentration
What are 2 ways that insulin is normally secreted?
1. BASALLY in small amounts between meals and overnight
2. BOLUSES in response to food; activated by an increased concentration of carbs in the gut
What percent of insulin is secreted by the pancreas as basal? As bolus?
basal: 50%

bolus: 50%
Is our insulin level ever 0?
no
When do boluses of insulin build up in the plasma?
about 30 min- 2 hour after you eat
Define basal insulin and describe the frequency of its release.
The natural amount of insulin in the body; small amounts are released by the pancreas every 24 hours
What is the basal insulin rate of secretion in adults?
adults secrete about 1 unit of insulin/hr, regardless of food intake
What are 4 other names for bolus insulin?
1. premeal
2. mealtime
3. prandial
4. nutritional insulin
What is the purpose of bolus insulin?
It is used to limit postprandial hyperglycemia by stimulating glucose uptake in the peripheral tissue
In response to food, the amount of insulin secretion increases or decreases?
increases
What determines the resting membrane potential in beta cells?
ATP-sensitive K+ channels
How does glucose enter beta cells?
via the membrane transporter GLUT-2
What happens when intracellular glucose blocks the ATP-sensitive K+ channels?
membrane depolarization and the opening of Ca++ channels
What does the Ca++ influx from glucose blackage of the ATP-sensitve K+ channels induce?
insulin secretion
What is diabetes mellitus?
a syndrome that develops when insulin secretion or activity are not sufficient to maintain normal blood glucose levels
What is another term for Type I diabetes?
IDDM: Insulin dependent diabetes mellitus
Who usually gets Type I diabetes?
kids
How does one develop Type I diabetes?
altered immune function; usually viral destruction of beta cells
What does Type I diabetes therapy require?
always requires insulin replacement
What is another term for Type II diabetes?
adult onset aka noninsulin dependent diabetes mellitus

*now many kids are developing this
What is the physiologic cause of Type II diabetes?
the body produces insulin, but not enough
How do you treat Type II diabetes?
1. oral antidiabetic medicines
2. diet

*may be given insulin, usually after trying multiple meds
Define hypoglycemia.
A pathologic state produced by a lower than normal amount of sugar (glucose) in the blood
Define hyperglycemia.
A condition in which an excessive amount of glucose is in the blood
List 8 types of medications for diabetes mellitus.
1. insulin
2. sulfonylureas
3. meglitinides
4. biguanides
5. alpha-glucosidase inhibitors
6. thiazolidinediones
7. incretin mimetics
8. amylin analogues
What is animal insulin?
Preparations of insulin available from either beef or pork pancreas
Why is animal insulin no longer used?
people got allergic reactions
How do scientists produce human insulin?
through recombinant DNA techniques (with E. coli or yeast vectors)
Why do we prefer recombinant human insulin over animal insulin?
Less likely to have resistance, allergic reactions, or antibodies against it
What type of molecule is insulin?
a peptide hormone
Can insulin be administered orally?
no
What is the half-life of natural circulating insulin?
a few minutes
Why does natural insulin have such a short half-life?
due to rapid removal by liver and kidneys
What are 4 classes of insulin preparations?
1. rapid acting
2. short acting
3. intermediate acting
4. long acting
How are ALL insulin preparations administered?
subQ
What is another name for short acting insulin? What is another way that it can be administered?
Regular insulin

IV
Why should you alternate injection sites?
To prevent lipohypertrophy (if this occurs, insulin won't be absorbed in the body)
If you have a patient that is taking insulin, but is still hypoglycemic, what could you assume?
that the patient is not rotating sites
What are 3 examples of rapid acting insulin preparations?
1. Humalog (lispro)
2. Novolog (aspart)
3. Apidra
What is the onset of rapid acting insulin?
quick
When do rapids acting insulin preparations peak?
30 minutes - 3 hrs
What is the duration of action of rapid acting insulin?
1 - 5 hours
When should you administer rapid acting insulin?
IMMEDIATELY before a meal
What does rapid acting insulin mimic?
endogenous insulin molecules
Why is rapid acting insulin easy to use?
because you can coordinate it with meals
What is another name for short acting insulin?
regular insulin
Give an example of short acting insulin.
Regular (Humulin R)
What is the onset of short acting insulin?
30 min-60 min
When is the peak of short acting insulin?
2-4 hours
What is the duration of action of short acting insulin?
8-12 hours
When should you administer short acting insulin?
30-45 min before meals
Can short acting insulin be administered via IV?
yes
Why does short acting insulin have a shorter duration of action?
because giving the drug by the IV route has a shorter duration of action than when it's given by subQ
What is the onset of immediate acting drugs?
1 - 1.5 hours
What is the duration of action of immediate acting drugs?
12 - 16 hours
What does intermediate acting insulin look like?
appears cloudy (the only insulin preparation that isn't clear)
What is an example of intermediate acting insulin?
NPH (humulin N)
Can intermediate acting insulin be used for emergency IV use?
no
What usually fills the contents of an insulin pen?
long acting insulin + regular acting insulin in 1 combination
How do you draw a combo?
-Draw up the regular first (always want the clear liquid in the syringe first)
-then draw up NPH
The intermediate acting insulin preparations vary on durations. How do you decide which to give to a patient?
depends on the patient's need
What is the onset of long acting insulin preparations?
1-2 hours
What is the peak for long acting insulin preparations?
-6-8 hours for LEVEMIR (DETEMIR)

-NONE for GLARGINE
What is the duration of action for long acting agents?
24 hours

*usually administered once daily
What are 2 examples of long acting insulin preparations?
1. Lantus (glargine)
2. Levemir (detemir)
When is Lantus (glargine) usually given?
at bed time
Does Lantus have a peak?
no
What is a key benefit of Lantus?
doesn't cause hypoglycemia because it has no peak

(in other drugs, if a patient is given too much meds [above the peak] the patient may develop hypoglycemia)
What does the FORM OF INSULIN ADMINISTERED determine?
1. onset of action
2. peak action
3. duration of action

**which one you give depends on the patient's needs
What is rapid/short acting insulin used for?
1. covers meal intake
2. used for elevated glucose levels after a meal
What is intermediate/long acting insulin used for?
used for basal insulin needs
What is intermediate/long acting insulin NOT used for?
not intended to cover meal
Name a combination product.
Novolin or Humulin 70/30
What is contained in Novolin or Humulin 70/30?
70% NPH (intermediate)
30% regular insulin (short)
What are the benefits of administering a combination product?
1. longer coverage
2. decrease the number of injections (usually 2x/day dosing)
How do you administer combination products?
pen or vial
What do you base the insulin dose on? What units should you use in insulin dosing?
total body weight

units
Which trends should you observe in insulin dosing?
1. hypoglycemia
2. hyperglycemia

**often you undergo trial and error dosing
**monitor the patient with blood glucose monitors
What is the ONLY insulin that can be administered via IV?
regular insulin
What insulins can be administered SubQ?
ALL
Rank the SubQ areas for insulin injection.
Abdomen>buttocks>arm/leg
What 3 factors increase insulin absorption?
1. exercise
2. rubbing
3. heat

**all accelerate insulin absorption
Name 3 types of insulin administration mechanisms.
1. portable pen injectors (if patient on short + intermediate)
2. infusion pump
3. vial & syringe
What are portable pen injectors?
cartridges of insulin and replaceable needles
Name 3 pros of portable pen injectors for insulin.
1. more accurate dosing mechanisms (turn end to measure the amount of units)
2. faster/easier than conventional syringes
3. improved patient compliance (easier for kids too)
What is an insulin infusion pump?
pump connected to an indwelling subcutaneous catheter to deliver short acting (regular) insulin

**needle is in the skin
Which patients typically use an insulin infusion pump?
Type I patients
What are the pros and cons of using an insulin infusion pump?
PRO:
-reduced glycemic variability

CON:
-not always practical for routine use (may be useful in special circumstances)
Should you refridgerate vials of insulin that are not in use?
yes
How long might USED insulin be kept at room temperature?
up to 28 days
How should you store insulin?
away from direct heat or light
Before drawing or injecting insulin, what should you visually inspect?
1. shouldn't be cloudy
2. look for particulate matter
Name 3 adverse effects associated with insulin. (*) the most common.
1. hypoglycemia (*)
2. Insulin allergy (rare now, was common with pork or beef)
3. lipohypertrophy (lump under the skin caused by accumulation of extra fat from frequent injections at the same site)
What are signs and symptoms of hypoglycemia?
1. tachycardia
2. confusion (from low blood glucose)
3. vertigo
4. diaphoresis
How should you treat mild hypoglycemia in a patient that is conscious and able to swallow?
1. simple sugar or glucose should be administered
2. give OJ, hard candy, sugar packets, or glucose tablets/gels
What is severe hypoglycemia characterized by?
unconsciousness or stupor
To decrease the severity of severe hypoglycemia, what should you do?
1. give 20-50 mL of 50% dextrose by the IV route
2. 1 mg glucagon either SubQ or IV
What should you always do before injecting a patient with insulin?
Always check blood glucose level
Should you shake insulin vials?
No, gently roll
How should your insulin injection site look?
free of scarring or bruising

**ask patient where they prefer it (they usually know best)
the remaining drugs are for type II
the remaining drugs are for type II
What are 2 divisions of sulfonylureas?
1. first generation
2. second generation
Name the 3 first generation sulfonylureas.
1. chlorpropamide (diabinese)
2. tolbutamide (orinase)
3. tolazamide (tobinase)
Name the 3 second generation sulfonylureas.
1. glyburide (DiaBeta, Micronase, Glynase Pres Tab)
2. Glipizide (Glucotrol, Glucotrol XL)
3. Glimepiride (Amaryl)
What must you be able to produce in order for sulfonylureas to work?
insulin
What is the MOA of sulfonylureas?
1. sulfonylureas bind to the beta cell receptor
2. closing the K+ channels
3. causing a Ca++ influx
4. depolarization
5. insulin release
What are the primary and secondary effects of sulfonylureas?
Primary: increase secretion of insulin from beta cells of the pancreas

Secondary: increase insulin receptor sensitivity and decrease hepatic glucose output
How are sulfonylureas absorbed?
rapidly through the GI
How are sulfonylureas metabolized?
90-100% hepatic metabolism
What is an exception to typical sulfonylurea metabolism?
Glyburide

50% hepatic metabolism
50% renally excreted
What is the duration of action of sulfonylureas?
approx 24 hr (1/day dosing)
What cautions should you take when administering sulfonylureas?
1. hepatic and/or renal disease
2. elderly (kidney function decreases)
3. patients with a "sulfa" allergy
What should you tell the patients who are taking drugs with sulfa moieties?
wear sunscreen because sulfa drugs increase sun sensitivity
What are the adverse effects for sulfonylureas? (*) the primary)
1. hypoglycemia (*)
2. dermatologic reactions (rash, photosensitivity, hypersensitivity)
3. GI disturbances (N/V/abnormal liver function tests)
4. weight GAIN
(not ideal, we want them to lose weight)
Name 2 Meglitinides.
1. Repaglinide (prandin)
2. nateglinide (starlix)
What is the MOA of Meglitinides?
increase secretion of insulin from beta cells by the same pathway as sulfonylureas
How are Meglitinides and sulfonylureas similar? different?
structurally related, but Meglitinides does not contain a sulfa moiety-->ideal for patients with allergies to sulfonylureas
What is the onset of action for Meglitinides?
15 minutes
What is the duration of action of Meglitinides?
<4 hours
Where are Meglitinides metabolized?
CYP 3A4 and CYP 2C9
What are potential advantages of Meglitinides?
1. rapid onset and shorter duration of action
2. ideal for elderly
3. may be useful in patients who skip meals or eat sporadically
What are 2 adverse effects associated with Meglitinides?
1. hypoglycemia
2. weight gain
Give an example of a biguanide.
Metformin (glucophage)
Which are prescribed more often, biguanides or sulfonylureas/meglitinides?
biguanides
What is the biguanide MOA?
1. decreased hepatic glucose output
2. increased peripheral glucose uptake and utilization

**alter the glucose without altering the insulin!
What are biguanide advantages?
1. does NOT cause hypoglycemia because it doesn't effect insulin release
2. causes weight loss
Are biguanides metabolized through the liver?
no
How are biguanides eliminated?
100% excreted through the kidney
Adverse effects associated with biguanides?
1. GI: D
2. lactic acidosis (increase lactate production in the body) **monitor patients because they could go into anaerobic metabolism!
What must you test first before administering a biguanide?
creatinine levels
What creatinine levels indicate renal impairment in men and women?
do NOT give a biguanide if:

M: >/= 1.5 mg/dL
F: >/= 1.4 mg/dL
Why shouldn't you give someone a biguanide who has hepatic impairment?
may have decreased ability to eliminate lactid acid (and increase the likelihood of lactic acidosis)
What do biguanides interact with? Why?
iodinated contrast materials

they are both renally excreted (must stop metformin 24hr before to 48 hr after administering iodine materials)
Name 2 alpha-glucosidase inhibitors.
1. acarbose (precose)
2. miglitol (glyset)
What is alpha glucosidase?
an enzyme in the gut that helps with the ingestion of carbs and causes an increase in blood glucose
What is the MOA of alpha-glucosidase inhibitors?
potent competitive inhibitor of brush border alpha glucosidases necessary for the breakdown of complex carbs (causes a decrease in glucose)
What are 2 alpha-glucosidase inhibitors pros?
1. won't alter actual insulin
2. doesn't cause hypoglycemia*
Where are alpha-glucosidase inhibitors absorbed?
poorly in gut
What is the onset of action of alpha-glucosidase inhibitors?
6 hours
Where are alpha-glucosidase inhibitors metabolized?
by intestinal bacteria

*be careful in patient with a GI disorder
Adverse effects associated with alpha-glucosidase inhibitors?
1. abdominal pain, flatulence, diarrhea
2. acarbose (hepatotoxicity at very high doses)
What conditions are CI for alpha-glucosidase inhibitors?
patients with significant GI disorders
Name 2 thiazolidinediones.
1. rosiglitazone (avandia)
2. pioglitazone (actos)
What is the MOA of thiazolidinediones?
binds to the nuclear steroid hormone receptor and promotes glucose uptake into skeletal and muscle/adipose tissue
Do thiazolidinediones cause hypoglycemia?
no
Where are thiazolidinediones metabolized?
extensively by the liver through the CYP 450
What are the adverse effects associated with thiazolidinediones?
1. hepatotoxicity
2. edema (worse if combined with insulin)
Why should you be careful administering thiazolidinediones to CHF patients?
worsens accumulation of water in their body
What are incretins?
intestional hormones that are released in response to glucose
What is GLP-1?
glucose-like peptide-1
What is GLP-1 rapidly degraded by?
DPP-4=dipeptidyl peptidase-4
When is GLP-1 released?
in relation to when you eat

(GLP-1 rapidly rises within minutes of food ingestion)
What are the 4 actions of GLP-1?
1. enhancement of glucose-dependent insulin secretion on beta cells
2. suppression of glucagon secretion of alpha cells
3. slows the rate of gastric emptying
4. reduces appetite
Give an example of an incretin mimetic.
Exenatide (Byetta)
What is the function of Exenatide?
GLP-1 agonist
How/how often do you administer exenatide?
pre-filled pens for subcutaneous injection administered 2x/day
Name 4 adverse effects with the increten mimetic, Exenatide.
1. Hypoglycemia (esp. in combo with sulfonylureas-->additive)
2. N/D
3. Headache
4. Pancreatitis
Name 2 DPP4 Inhibitors.
1. Sitagliptin (Januvia)
2. Saxagliptin (Onglyza)
What is the MOA for DPP4 Inhibitors?
Inhibit DPP-4 enzyme that is responsible for the breakdown of incretin GLP-1
How/how often do you administer DPP-4 inhibitors?
orally 1x/day
What are the adverse effects associated with DPP4-Inhibitors?
gew GI effects

*NO evidence of hypoglycemia
*since it's a new drug, we're still looking out for side effects
Give an example of an amylin analogue.
Pramlintide (Symlin)
What is the MOA for Pramlintide?
1. slows gastric emptying
2. suppresses glucagon secretion
3. decreases glucose output by the liver
Which patients are indicated for a Pramlintide prescription?
Both Type I and Type II patients who have failed other meds
How/when should you administer the amylin analogue Pramlintide?
SubQ injection

PRIOR to meals
What are the adverse effects associated with Pramlintide?
1. severe hypoglycemia (for an unknown reason, since the drug doesn't alter insulin concentration)
2. GI disturbance: N/V