Oral medications

Question 1

Sulfonylureas MOA

Answer 1

Insulin secretagogues

Increase BASAL and MEAL-stimulated (PRANDIAL ) insulin secretion

Question 2

3 Sulfonylureas used:

Answer 2

Glyburide, Glimeperide, Glipizide

Question 3

which SU has less hypoglycemia in elderyly?

Answer 3

Glimeperide

Question 4

Why would SU not work?

Answer 4

1) if beta cells burnt out. 2) if TYPE 1

Question 5

SU ADR: TOP 2 and other

Answer 5

1) HYPOGLYCEMIA 2) WEIGHT GAIN

Other: GI, skin rashes, hepatic changes (rare)

Question 6

SU contraindications:

Answer 6

1) known hypersensitivity to the drug or it’s inactive ingredients
2) Type 1 Diabetes
3) Diabetic ketoacidosis, with or without coma

Question 7

Meglitinides/Phenylalanines

Answer 7

Mechanism of action:
Insulin secretagogues
( similar to SU)

Major difference is that these dosed three or four times a day and that means they are very rapid acting. You take right before you eat.
Rapid acting insulin secretagogoes.

Question 8

Name the 2 meglitnides

Answer 8

1) Rapaglinide and 2) Nateglinide

Question 9

Biguanide class has one drug

Answer 9

Metformin

Question 10

Metformin action?

4

Answer 10

Improves insulin sensitivity by reducing insulin
resistance:
Decreases hepatic glucose production
(primary action)
Increases skeletal muscle glucose uptake
(secondary action)
Decreases intestinal absorption of glucose
(minor effect)

Question 11

METFORMIN DOSING (common questions)

1) w/ or w/o meals?
2) what dose to start at?
3) how often do you increase dose?
4) MAX dose?
5) how often is IR given? how often ER?

Answer 11

1) Take with meals
2) Start with small dose (500 mg) for less GI problems
3) Increase dose at weekly intervals (or longer)
4) Maximum dose: =
2000 mg (effective)
2550 mg/day (FDA-approved)
Given 2 to 3 times a day (immediate release)
Once a day extended release products (Glucophage XR) available

Question 12

Metformin advantages: 6 of them.

Answer 12

1) may aid weight loss or weight maintenance
2) Improves plasma lipids
3) Decreased triglycerides
4) Decreased LDL-cholesterol
5) Lowers insulin levels (indirect effect)
6) Usually does not cause hypoglycemia

Question 13

Metformin concerns: 3

serum creatinine cutoff: 1) men? 2) for women?

Answer 13

1) ADRs:
• GI-related complaints (nausea, vomiting, diarrhea ) - give ca carbonate to decrease diarrehea
• Unpleasant or metallic taste

2) Lactic acidosis is a serious, rare event
3) Reduction in serum vitamin B12

serum creatinine cut offs: is 1.5 for men and 1.4 for women!!!!!!!!!!!know this number.

Question 14

Metformin: Contraindications

Answer 14

Avoid/Cautious use in:
Pregnancy or lactation
Congestive heart failure
Hepatic dysfunction
History of alcohol abuse or binge drinking
Tissue hypoxia (e.g., acute MI, dye tests)
Renal dysfunction
Serum creatinine >1.5 mg/dL in men
Serum creatinine >1.4 mg/dL in women)
Age >80 years (without adequate renal function or creatinine clearance)

Question 15

Thiazolidinediones

Answer 15

Directly reduces insulin resistance byactivating PPAR-gamma nuclear receptors
• Increase glucose uptake in skeletal muscle and fat cells
• Lower hepatic glucose output

Question 16

TZD drugs

Answer 16

1) Pioglitazone 2) Rosiglitazone

Question 17

TZD

1) how much A1C reduction?
2) how long till decrease in blood glc?
3) maximum glucose lowering effects in how long?
4) how long will effects last?

Answer 17

1) Usual reduction in A1C of 1.5% - 2.5%
2) Decreases in blood glucose can be seen within 2-4 weeks
3) Maximum glucose lowering effects may take up to 12 weeks
4) Demonstrated perseverance of effect for up to 1-2 years

Question 18

TZD ADR

Answer 18

1) Weight gain of 1-6 kg, which is dose dependent and varies with the type of agent used in combination therapy
2) Peripheral edema, which tends to be dose dependent, more common in patients treated concomitantly with insulin, and may cause dyspenia and potentiate heart failure
3) Macular edema
4) Increased incidence of bone fractures

Question 19

TZD BBW

Answer 19

1) CHF. Can cause or exacerbate. Signs of it would be excessive weight gain, edema, dypnea

Question 20

alpha-Glucosidase Inhibitors MOA

Answer 20

Mechanism of action:
Inhibit membrane-bound alpha-glucosidase enzymes in small intestine
Decrease glucose absorption from intestine, reducing postprandial hyperglycemia

Question 21

alpha-glucosidase inhibtors agents (2)

annoying adr?

Answer 21

1) Acarbose (Precose)
2) Miglitol (Glyset)

adr: FLATULENCE

Question 22

NON diabetes drugs used in diabetes?

2

Answer 22

1) Bile Acid Sequestrants
Colesevelam (Welchol) is approved for treatment of type 2 diabetes
Lowers LDL Cholesterol
Lowers A1C by about 0.5%

2) Bromocriptine (Cycloset)
Acts on CNS to improve insulin resistance and glucose tolerance – resets neuroendocrine rhythms