Diabetes Pharm Flashcards
Unusual/future insulin therapies (2)
- pancreatic/islet cell transplant
- Inhaled insulin
Type 1 diabetic is hungry and hasn’t taken any insulin. How long must he wait after taking rapid-acting insulin?
Inject rapid-acting insulin 10 minutes before eating.
rapid acting: 10 min onset of action
Insulin side effects:
-systemic (4)
- hypoglycemia
- insulin allergy
- insulin edema (peripheral edema 1st few week of taking insulin)
- weight gain (insulin is anabolic)
also, atherosclerosis and cancer risk are theoretic side effects at high does
Describe example of 2 shot insulin regimen for T2DM
70/30 insulin SQ qAM
70/30 insulin SQ qPM
Standard diabetic goals with insulin therapy:
- fasting glucose
- post-prandial glucose 2 hours after meal
- A1C
- 70-130 mg%
- <180 mg%
- <7%
Sulfonylureas
- drug names (3)
- mech of action
- side effects
Glyburide, glimepiride, glipizide
Mech: binds to K+ channel on beta islet cell, closing it. This depolarizes the cell, causing Ca+ influx and therefore release of insulin.
-side effects: hypoglycemia. Disulfuram-like reaction in older 1st gen drugs.
SGTP-2 inhibitors
- drug name
- mech
- side effects (2)
Sodium-glucose transport protein inhibitor
- Canaglifozin
- Inhibits the transport proteins that reabsorb glucose in the kidney, resulting in increased glucose urinary loss
- side effects:
1. yeast infections (b/c of glucose in bladder)
2. dehydration (osmotic diuresis)
very new drug
Short acting insulin
- drug name
- bonus: brand names
- Regular insulin
- Humulin R, Novolin R
Which 3 diabetes drug classes are the most effective at lowering A1C
-what is their average A1C decrease effect?
- biguanides (metformin)
- sulfonylureas (glipizide, glyburide, glimepiride)
- glitazones (pioglitazone, rosiglitazone)
- All lower A1C by average 1.5 %
Long acting insulin
- drug names (2)
- bonus: brand names
- Glargine (Lantus)
- Detemir (Levemir)
Pirate says “Glaar” and has long-lasting “Debts”
GLP-1 analogues
- drug names (2)
- mech
- side effects
- exenatide, liraglutide
- mimic GLP-1 (glucagon-like peptide), which is secreted in response to eating to stimulate insulin release
- side effects: pancreatitis, nausea/vomting
Treating T2DM: it’s common to Rx a combination of 2 drugs
- Why is this?
- example combos
Rx combo of A) drug that increases insulin and B) drug that increases insulin sensitivity
A) sulfonylurea
insulin
GLP-1 analog/DPP-4 inhibitor
B) metformin
glitazone
Describe example of basal-bolus insulin regimen in T1DM pt with insulin pump
-what type of insulin does pump have?
Pump has rapid-acting insulin so it’s easy to adjust onset/duration
You see an insulin vial with cloudy, not clear liquid
-what is it
NPH Insulin
- it’s a cloudy, colloidal suspension
- Pt must mix it before injecting
Intermediate acting insulin:
- drug name
- bonus: brand names
- NPH
- Humulin N, Novolin N
Which insulins can be used IV, which are SubQ?
Only regular insulin can be used IV.
Everything can be used SubQ
Insulin side effects
-local to injection site (2)
Local to SubQ sites:
- lipoatrophy
- lipohypertrophy (insulin is anabolic for fat)
This is why you rotate injection sites
Insulin categories (4)
-also list the specific insulin analog names
- rapid acting
- lispro, aspart - short acting
- regular - intermediate acting
- NPH - long acting
- glargine, detemir
DPP-4 inhibitors
- drug name
- mech
- Sitagliptin
- blocks protease that degrades GLP-1, prolonging GLP-1 action of stimulating insulin release
Intermediate acting insulin
- onset
- peak
- duration
NPH insulin
O: 1-2 hrs
P: 4-12 hrs
D: 18-26 hrs
Describe example of basal-bolus insulin regimen in T1DM
Glargine SQ at bedtime
Aspart SQ TID pre-meal 10 minutes
Long acting insulin, Detemir
- onset
- peak
- duration
Detemir
O: 4 hrs
P: 6-14 hrs
D: 24 hrs
Rapid acting insulin:
- drug names (3)
- bonus: brand names
- lispro (humalog)
- aspart (novolog)
- glulisine (apidra)
Short acting insulin
- onset
- peak
- duration
Regular insulin
O: 30 min
P: 2-5 hr
D: 6-8 hrs
How are insulin analogs different chemically from regular insulin?
Insulin analogs have changes in the amino acid sequence to alter timing/duration of action
Which insulin has no peak time of action?
Glargine (Lantus) long acting
Onset: 4-6 hrs
Duration 24-36 hrs
Short acting insulin:
- onset
- peak
- duration
lispro, aspart, glulisine
O: 10 min
P: 45 min
D: 2 h
Glitazones (thiazolidinediones)
- drug names (2)
- mech
- major side effects (3)
- rosiglitazone, pioglitazone
- increase insulin sensitivity in peripheral target tissues. Binds PPAR-gamma nuclear transcription regulator to increase GLUT4 in tissues.
- side effects:
1. hepatotoxicity
2. weight gain
3. edema
Why is rapid-acting insulin better than regular insulin for a meal?
- quicker onset of action prevents immediate hyperglycemia (10 min vs 30 min)
- shorter duration prevents postprandial hypoglycemia (2 hrs vs 6-8 hrs)
Long acting insulin, Glargine
- onset
- peak
- duration
Glargine
O: 4-6 hrs
P: none
D: 24-36 hrs
What is a side of insulin that can occur during the first few weeks of starting insulin?
Insulin Edema–peripheral edema occurs only in pts that just started insulin
Describe example of 3-shot insulin regimen for T2DM
-why would pt prefer this instead of 2-shot regimen?
NPH and Regular SQ qAM
Regular SQ qPM
NPH SQ bedtime
-Injecting NPH later at bedtime allows insulin to be effective at breakfast time
You diagnose a pt with T2DM and he also has renal insufficiency. What drug to avoid?
Metformin (biguanide)
-risk of fatal lactic acidosis in pts with renal insufficiency
Name the classes of diabetes drugs (not including insulin):
(7)
Sulfonylureas
Biguanides
Glitazones (thiazolidinediones)
alpha-Glucosidase inhibitors
GLP-1 analogues
DPP-4 inhibitors
SGTP-2 inhibitors
Which diabetic drug class is the only one without hypoglycemia side effect?
Biguanides (metformin)
-it decreases gluconeogenesis
Insulin premixed:
which drugs are in the mixture?
- 70/30
- 50/50
- 75/25
intermediate mixed with short/rapid acting
- NPH/reg
2 NPH/reg
- NPH/lispro
Alpha-glucosidase inhibitors
- drug name
- mech
- side effects
- acarbose
- inhibits intestinal brush-border enzymes that break down carbs, resulting in partial malabsorption of carbs.
- side effects: bloating, gas, diarrhea–from bacterial fermentation of carbs
Insulin detemir
-how does it achieve long-acting ability?
Detemir self-associates (binds to itself) in the SubQ injection site and also binds to albumin in the bloodstream
Biguanides
- drug name
- mech
- side effects (2)
- metformin
- decreases liver gluconeogenesis (liver is more sensitive to insulin)
1. GI effects (abdominal discomfort, diarrhea)–common
2. Lactic acidosis–rare, fatal. Don’t prescribe to pts with renal insufficiency
Insulin glargine
-how does it achieve long-acting ability?
Glargine is soluble at pH4 but poorly soluble at pH7. Thus, when injected subQ, it precipitates in the interstitial fluid and slowly mobilizes from the depot site.
Rapid-acting insulin
-how do they achieve rapid-acting ability?
Insulin has a tendency to form hexamers in solution. Breakdown takes time.
Rapid-acting insulin more rapidly forms monomers from hexamers
