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43 Cards in this Set

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What is starting dose for Amaryl?
1-2 mg q.d.
hyphenated amount
What is maintenance dose of Amaryl?
1-4 mg q.d.
What is maximum dose of Amaryl?
8 mg qd
What is hypoglycemic rate for Amaryl
0.9 to 1.7%
How is Amaryl excreted? (percentages)
Urine/kidneys - 60%
Feces - 40%
What are the three indications of Amaryl?
As an adjunct to diet and exercise:
1. monotherapy
2. combo therapy with metformin (glucophage)
3. combo therapy with insulin
Can for sulfonylureas cause weight gain?
What is the MOA of Amaryl?
Release of insulin from functioning pancreatic beta cells.

Increased sensitivity of peripheral tissues to insulin.

Decrease in hepatic glucose production.
What is dose for renally impaired patient on Amaryl?
1 mg
What are the available strengths of Amaryl?
1 mg
2 mg
4 mg

(2 and 4 mg strengths are sampled)
What is the drug class of Amaryl?
What is the generic name of Amaryl?
What are the contraindications to Amaryl?
Known sensitivity to the drug.

Diabetic ketoacidosis.
What is the effect of Amaryl on blood glucose?
2.0 percentage-point decrease in A1C vs placebo as monotherapy

28% reduction from baseline in FPG

40% reduction in 2-hour PPG
What is effect of Amaryl on first-phase insulin secretion?
Is Amaryl safe for renally impaired patients?
Yes, proven safety to a creatinine clearance of 9.4 mL/min.
What are the most common adverse reactions for Amaryl?
Dizziness - 1.7%
Asthenia - 1.6%
Headache - 1.5%
Nausea - 1.1%
The combination of Amaryl and what sensitizer have a synergistic effect?
Metformin (Glucophage)
What are the two major defects of type 2 diabetes mellitus?
Insulin resistance

Impaired insulin secretion
What is effect of Amaryl on weight and lipids?
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
What is the half-life of Amaryl?
9 hours
List some key points about Amaryl.
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
Amaryl restores what type of insulin secretion?
Endogenous insulin
Amaryl is unique in that it is the only sulfonylurea that improves both ________ and __________ insulin response
First and second phase

First phase = 1-3 min
Second phase = 60 min up to 2-3 hrs
List some examples of second-generation sulfonylureas
Amaryl, Glyburide (Diabeta, Micronase, Glynase), Glipizide (Glucotrol, Glucotrol XL)
What are the two defects of type 2 diabetes?
insulin resistence and insulin deficiency
Indications of metformin
monotherapy as adjunct to diet and exercise (first line therapy)

combination with SU

combination with insulin
Mechanism of action of metformin
Biguanide class exerts glucose-lowering effect by reducing hepatic glucose production, decreasing intestinal glucose absorption, and improving insulin sensitivity
Does metformin have any effect on insulin secretion by the pancreatic beta cells?
TZD's mechanism of action is what?
improve sensitivity of peripheral tissues (liver, muscle and adipose tissue) to insulin, but they do not target insulin secretion
What are the available TZD agents?

What are the indications for TZDs
Avandia - rosiglitazone
Actos - pioglitazone

adjunct to diet and exercise, monotherapy, combo with SU, metformin, or insulin.
What are the alpha-glucosidase inhibitors, their MOA, and indications?
acarbose - Precose
miglitol - Glyset

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

Indicated as monotherapy, combo with SU
What are the meglitinide analogs and MOA?
repaglinide and nateglinide

MOA - restore endogenous insulin secretion, but have short duration of action and must be taken with meals
What did the Sonnenberg trial study?
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
The Riddle study (listed in PI) compared combo therapy with Amaryl and insulin (70/30) vs placebo.

What was result?
Study showed less insulin was needed (38% less)
Describe the Schade study in relation to Amaryl use
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
What dose of Amaryl was most common for the Schade study?
1 to 6 mg
What does metformin have a warning against in its PI?
Lactic acidosis - must be used in caution in patients with renal disease and monitoring of liver function should be done
Metformin is contraindicated for:
Patients with renal disease or dysfunction.

Patients with CHF

Known hypersensitivity to drug

Acute or chronic metabolic acidosis, diabetic ketoacidosis
What are the primary AE's associated with metformin use?
Diarrhea (11.7%), nausea, vomiting, flatulence
What is starting and maximum dose of Glucophage XR (metformin)
starting - 500 mg in evening

max - 2000 mg
How is metformin excreted?
Unchanged in the urine
What was the objective, results, conclusions of the Korytkowski trial?
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