Rotations Rx - Endocrine Agents

Front 1

Endocrine Agents

Back 1

Endocrine Agents

Front 2

Hypolipidemics

Back 2

Hypolipidemics

Front 3

Hypolipidemics can be divided into 5 different categories. What are they?

Back 3

Statins,
Fibric Acid Derivatives,
Niacin,
Resins,
Cholesterol Absorption Inhibitors

Front 4

Statins (Atorva~, Prava~, Simva~, Fluva~, Lova~, Rosuva~)

1) What is the CU of statins?

2) MOA of statins?

3) AEs / CIs of statins?

Back 4

1) TX of choice for hypercholesterolemia in pts @ risk for CAD -->
Dec risk of MI & stroke
and dec CV mortality

Large dec LDL
Med dec TGs
Small inc HDL

2) Inhibs HMG-CoA reductase in liver -->
No chol synth in liver -->
Forces hepatocytes to upreg LDL receptors -->
Inc Hepatic LDL Catab
AND
Inc extraction of VLDL (LDL precursor) from circulation

3) AEs:
Inc transaminases (Liver);
Inc creatine kinase;
Symptomatic hepatitis;
Symptomatic myopathy (ask about leg cramps)

CIs:
Liver Dz;
CI'ed w/ concurrent use of gemfibrozil (inc risk myopathy)

Front 5

Fibric Acid Derivatives (Gemfibrozil)

1) CU of gemfibrozil?

2) MOA of gemfibrozil?

3) AEs / CIs of gemfibrozil?

4) 2 PK / PD points for gemfibrozil?

***NOTE:
-Fenofibrate is similar to gemfibrozil but causes great inc HDL
-Clofibrate is less well tolerated than gemfibrozil

Back 5

1) Hypertriglyceridemia!!

Large dec TGs
Med inc HDL
Small dec TC and LDL

2) Binds nuclear transcription regulator PPAR-alpha -->
Inc LPL -->
Dec TGs by dec'ing VLDL and apo-CIII

3) AEs:
GI distress;
rash;
myopathy;
gallstones

CI:
Hepatic dysfnctn;
Renal dysfnctn

4) Potentiates effects of warfarin and sulfonylureas like Glyburide

Front 6

Niacin (B3)

1) CU of Niacin?

2) MOA of Niacin?

3) AEs / CIs?

Back 6

1) Hypercholesterolemia w/ concomitant inc TGs;
Low HDL

2) Inhibs Hormone Sensitive Lipase in adipose -->
Dec lipolysis of TGs -->
Dec FA to liver -->
Dec hepatic synth of TGs

Dec peripheral LP lipase --> Dec TGs

Large dec TGs
Med inc HDL
Medium dec TC and LDL

3) AEs:
Flushing that can be prevented by taking ASA before;
Pruritus;
GI distress, glucose intolerance, inc Transaminases, Hyperuricemia, Gout, Amblyopia

Front 7

Resins (Cholestyramine)

1) CU of Cholestyramine?

2) MOA of Cholestyramine?

3) AEs and CIs of Cholestyramine?

Back 7

1) 2nd line (behind statins) for Hypercholesterolemia

Large Nothing
Medium dec in TC and LDL
Small inc HDL and TGs

2) Binds bile acids in intestine -->
Inhibits enterohepatic circulation of bile acids -->
Inc excretion of bile acids -->
Inc conversion of cholesterol into bile acids in liver -->
Upregulation and subsequent inc clearance of LDL from plasma

3) AEs:
Bloating and other GI

CIs:
Hypertriglyceridemia

***Other resins include: Colestipol & Colsevelam

Front 8

Cholesterol Absorption Inhibitors (Ezetimibe)

1) CU of Ezetimibe?

2) MOA of Ezetimibe?

3) AEs / CIs of Ezetimibe?

Back 8

1) w/ a statin for hypercholesterolemia

Dec TC and LDL

2) Inhibs intestinal cholesterol absorption in jejunum

3) AEs:
URIs;
slight inc risk of transaminitis when given w/ statin

Front 9

Hypoglycemics

Back 9

Hypoglycemics

Front 10

What are the 7 classes of hypoglycemics?

Back 10

Insulin
Sulfonylureas
Meglitinides
GLP-1 Analogs
Biguanides
TZDs
alpha-glucosidase inhibitors

Front 11

Insulin

1) What is the CU of insulin

2) MOA of insulin?

3) AEs / CI's of Insulin?

***NOTE:
Pramlintide is an amylin analog. Amylin is a peptide hormone co-secreted w/ insulin from pancreas -->
Dec Gastric emptying and Inhib Glucagon secretion.

Back 11

1) Glucose CTL in diabetics:
Req'd in Type I,
Used in Type II if glucose cannot be well CTL'ed w/ oral agents

w/ Glucose for life-threatening hyperkalemia

2)
-Liver:
Stims Glycogenesis;
Inhibs Glycogenolysis;
Inhibs Gluconeogenesis

-Muscle:
Glucose and K uptake

-Adipose:
Stims glucose uptake into adipocytes

3) Hypoglycemia

Front 12

Sulfonylureas (Glyburide)

1) CU of Sulfonylureas?

2) MOA of Sulfonylureas?

3) AEs & CIs of Sulfonylureas?

Back 12

1) T II DM if glucose cannot be CTL'ed w/ diet and metformin

2) Blocks K+ channels on pancreatic beta cell -->
Dec K+ Efflux -->
Inc IC K+ -->
Depolarization of pancreatic beta-cell -->
Ca Influx -->
Insulin Release

3) Hypoglycemia

Front 13

Meglitinides (Starlix)

1) CU of Meglitinides?

2) MOA of Meglitinides?

3) AEs / CIs of Meglitinides?

Back 13

1) TII DM (3rd Line)

2) Same as Sulfonylureas EXCEPT has a more rapid onset and a shorter duration

3) Hypoglycemia

Front 14

GLP-1 Analog (Glucagon-like Peptide 1 Analog) (Exenatide)

1) CU of GLP-1 Analog?

2) MOA of GLP-1 Analog?

3) AEs / CIs of GLP-1 Analog?

Back 14

1) TII DM if can't CTL glucose w/ diet and metformin

2) Binds GLP-1 receptors on pancreatic beta cells -->
Stim Adenylate Cyclase -->
Inc cAMP -->
Inc Insulin Synthesis Secretion

3) -Hypoglycemia if given concurrentlyw/ a Sulfonylurea
-Nausea

Front 15

BIguanides (Metformin)

1) CU of Biguanides?

2) MOA of Biguanides?

3) AEs / CIs of Biguanides?

Back 15

1) 1st line Tx for TII DM

2) Inhibs hepatic gluconeogenesis

3) GI Upset

Front 16

TZDs (Rosiglitazone)

1) CU of TZDs?

2) MOA of TZDs?

3) AEs / CIs of TZDs?

Back 16

1) TII DM (If no glucose CTL w/ diet and metformin)

2) Binds PPAR-gamma -->
Cells are more sensitized insulin

3) Hepatotoxic

Front 17

alpha-glucosidase Inhibitors (Acarbose)

1) CU of alpha-glucosidase Inhibitors?

2) MOA of alpha-glucosidase Inhibitors?

3) AEs / CIs of alpha-glucosidase inhibitors?

Back 17

1) TII DM (3rd Line)

2) Inhibs metab of carbohydrates

3) ABD Pain