Amaryl - Quiz

Front 1

What is starting dose for Amaryl?

Back 1

1-2 mg q.d.

Hint 1

hyphenated amount

Front 2

What is maintenance dose of Amaryl?

Back 2

1-4 mg q.d.

Hint 2

hyphenated

Front 3

What is maximum dose of Amaryl?

Back 3

8 mg qd

Front 4

What is hypoglycemic rate for Amaryl

Back 4

0.9 to 1.7%

Front 5

How is Amaryl excreted? (percentages)

Back 5

Urine/kidneys - 60%
Feces - 40%

Front 6

What are the three indications of Amaryl?

Back 6

As an adjunct to diet and exercise:
1. monotherapy
2. combo therapy with metformin (glucophage)
3. combo therapy with insulin

Front 7

Can for sulfonylureas cause weight gain?

Back 7

Yes

Front 8

What is the MOA of Amaryl?

Back 8

Release of insulin from functioning pancreatic beta cells.

Increased sensitivity of peripheral tissues to insulin.

Decrease in hepatic glucose production.

Front 9

What is dose for renally impaired patient on Amaryl?

Back 9

1 mg

Front 10

What are the available strengths of Amaryl?

Back 10

1 mg
2 mg
4 mg

(2 and 4 mg strengths are sampled)

Front 11

What is the drug class of Amaryl?

Back 11

Sufonylurea

Front 12

What is the generic name of Amaryl?

Back 12

Glimiperide

Front 13

What are the contraindications to Amaryl?

Back 13

Known sensitivity to the drug.

Diabetic ketoacidosis.

Front 14

What is the effect of Amaryl on blood glucose?

Back 14

2.0 percentage-point decrease in A1C vs placebo as monotherapy

28% reduction from baseline in FPG

40% reduction in 2-hour PPG

Front 15

What is effect of Amaryl on first-phase insulin secretion?

Back 15

55%

Front 16

Is Amaryl safe for renally impaired patients?

Back 16

Yes, proven safety to a creatinine clearance of 9.4 mL/min.

Front 17

What are the most common adverse reactions for Amaryl?

Back 17

Dizziness - 1.7%
Asthenia - 1.6%
Headache - 1.5%
Nausea - 1.1%

Front 18

The combination of Amaryl and what sensitizer have a synergistic effect?

Back 18

Metformin (Glucophage)

Front 19

What are the two major defects of type 2 diabetes mellitus?

Back 19

Insulin resistance

Impaired insulin secretion

Front 20

What is effect of Amaryl on weight and lipids?

Back 20

Weight neutral - 6.67 pound reduction over 18 months

Lipid neutral - no deleterious changes in lipoprotein, 11.99 reduction in total cholesterol, 8.12 reduction from baseline LDL

Front 21

What is the half-life of Amaryl?

Back 21

9 hours

Front 22

List some key points about Amaryl.

Back 22

1. Significant A1C reductions through FBG and PPG
2. Glucose mediated response
3. Low incidence of hypoglycemia
4. Synergistic effect in combo with metformin
5. Flexible, once-daily dosing
6. Safe in renally impaired patients

Front 23

Amaryl restores what type of insulin secretion?

Back 23

Endogenous insulin

Front 24

Amaryl is unique in that it is the only sulfonylurea that improves both ________ and __________ insulin response

Back 24

First and second phase

First phase = 1-3 min
Second phase = 60 min up to 2-3 hrs

Front 25

List some examples of second-generation sulfonylureas

Back 25

Amaryl, Glyburide (Diabeta, Micronase, Glynase), Glipizide (Glucotrol, Glucotrol XL)

Front 26

What are the two defects of type 2 diabetes?

Back 26

insulin resistence and insulin deficiency

Front 27

Indications of metformin

Back 27

monotherapy as adjunct to diet and exercise (first line therapy)

combination with SU

combination with insulin

Front 28

Mechanism of action of metformin

Back 28

Biguanide class exerts glucose-lowering effect by reducing hepatic glucose production, decreasing intestinal glucose absorption, and improving insulin sensitivity

Front 29

Does metformin have any effect on insulin secretion by the pancreatic beta cells?

Back 29

no

Front 30

TZD's mechanism of action is what?

Back 30

improve sensitivity of peripheral tissues (liver, muscle and adipose tissue) to insulin, but they do not target insulin secretion

Front 31

What are the available TZD agents?

What are the indications for TZDs

Back 31

Avandia - rosiglitazone
Actos - pioglitazone

adjunct to diet and exercise, monotherapy, combo with SU, metformin, or insulin.

Front 32

What are the alpha-glucosidase inhibitors, their MOA, and indications?

Back 32

acarbose - Precose
miglitol - Glyset

MOA - delay glucose absorption in the GI tract, do not enhance insulin secretion

Indicated as monotherapy, combo with SU

Front 33

What are the meglitinide analogs and MOA?

Back 33

repaglinide and nateglinide

MOA - restore endogenous insulin secretion, but have short duration of action and must be taken with meals

Front 34

What did the Sonnenberg trial study?

Back 34

Evaluated 3 mg bid to 6 mg qd with Amaryl for efficacy.

Proved Amaryl helps correct deficiencies in body's physiologic response to meals.

Studied safety profile, with low rate of hypoglycemia

Front 35

The Riddle study (listed in PI) compared combo therapy with Amaryl and insulin (70/30) vs placebo.

What was result?

Back 35

Study showed less insulin was needed (38% less)

Front 36

Describe the Schade study in relation to Amaryl use

Back 36

Amaryl vs placebo (249 patients)

Studied safety, efficacy, and dosing

Efficacy - reduced A1C from 9.1 to 6.7, fasting down by 46 mg/dL, and PPG down by 72 mg/dL. 69% achieved tight control

Safety - safe for renally impaired, low incidence of hypo

Dosing - Half life of 9 hours, convenient once daily dosing for increased compliance

Front 37

What dose of Amaryl was most common for the Schade study?

Back 37

1 to 6 mg

Front 38

What does metformin have a warning against in its PI?

Back 38

Lactic acidosis - must be used in caution in patients with renal disease and monitoring of liver function should be done

Front 39

Metformin is contraindicated for:

Back 39

Patients with renal disease or dysfunction.

Patients with CHF

Known hypersensitivity to drug

Acute or chronic metabolic acidosis, diabetic ketoacidosis

Front 40

What are the primary AE's associated with metformin use?

Back 40

Diarrhea (11.7%), nausea, vomiting, flatulence

Front 41

What is starting and maximum dose of Glucophage XR (metformin)

Back 41

starting - 500 mg in evening

max - 2000 mg

Front 42

How is metformin excreted?

Back 42

Unchanged in the urine

Front 43

What was the objective, results, conclusions of the Korytkowski trial?

Back 43

Objective - study effect of Amaryl on insulin sensitivity and secretion in type 2 diabetics (did not prove improved sensitivity)

Conclusion - No improved sensitivity, observed improvement in first and second phase insulin secretion