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Pharmacology Exam 5 > Anti-Diabetes > Flashcards

Flashcards in Anti-Diabetes Deck (37)
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1

Classification of Diabetes Mellitus

Type I-Insulin dependent (deficiency)
Type II-Insulin independent (resistance)

2

What diabetes can cause

major cause of heart disease and stroke; 7th leading cause of death in United States.

3

Macrovascular complications of diabetes

Coronary artery disease, cerebral vascular problem, peripheral vascular disease

4

Microvascular complications of diabetes

Nephropathy, retinopathy and neuropathy

5

Diagnostic Criteria for Diabetes

• Fasting plasma glucose (FPG)
• HbA1c level (also considering FPG results)
• Glucose level 2 hrs after a 75 g glucose load (less used)

6

Type I Diabetes

 Insulin dependent
 Juvenile onset
10%
 Inflammation of islets or antibodies to islet
 Prone to ketoacidosis
 HLA association
 No obesity
 Vascular complications*

7

Type II Diabetes

 NOT Insulin dependent  Maturity onset
90%
 Inability of insulin action  Not prone
 No association with HLA
 Obesity is a common risk factor  Vascular complications*

8

Model of insulin action on glucose transport in myocytes & adipocytes

Insulin binds to the α subunits of the insulin receptor and stimulates the tyrosine kinase activity of the β subunits. Glucose transport proteins are then activated and translocated from the cytoplasm to the cell membrane which stimulates glucose entry into the cell.

9

Long-acting therapy

`Glargine

10

Short-acting

Aspart/Lispro
Regular

11

Insulin management schedules:

2 or 3 meals (+/-PM) considerations; single or mixed insulin preps

12

Insulin Delivery Devices:

Syringes; Refillable/Prefilled Pens; Insulin Pumps

13

Complications of Insulin

Hypoglycemia: relieved by glucose (food intake; i.v. injection, etc.), ketoacidosis, insulin allergy, or lipodystrophy at injection site.

14

Pathophysiology of T2D

know how glucagon and insulin work

15

Sulfonylureas(SFUs):

Glyburide

16

Glyburide mode of action

Induce insulin release from pancreas (closing ATP-K+ channels)
Reduce serum glucagon levels
Potentiates action of insulin on its target tissues

17

Adverse drug reactions of glyburide

Severe hypoglycemia; weight gain, nausea, vomiting, hypersensitivity reactions

18

Indication for glyburide

T2D patients failed to achieve glycemic control with diet & life-style modifications; may be used in patients with kidney disease

19

Biguanides:

Metformin, generally 1st choice therapy

20

Metformin Mode of Action

↓ hepatic glucose production (HGP) (activates AMP-kinase)
↑ insulin action on peripheral muscle and fat tissues
Non-insulin-dependent effects, thus no hypoglycemia & no weight gain; No effect on release of growth hormone, glucagon.

21

Contraindications of Metformin

Contraindicated in patients with renal impairment, hepatic diseases, heart problems, acidosis, blood infection, etc.

22

Thiazolidinediones(TZDs)

Rosiglitazone and Pioglitazone

23

Mode of Action of rosiglitazone and pioglitazone

Agonists for nuclear peroxisome proliferator-activated receptor-γ (PPAR γ) & activate insulin responsive genes that regulate carbohydrate and lipid metabolism
Promote glucose uptake to muscles/fat & decrease HGP
Require insulin presence for action

24

Adverse drug reactions of rosiglitazone and pioglitazone

1st year liver function monitoring
Edema (fluid retention), weight gain
Rosiglitazone (FDA restricted access): risk of heart attack/MI;
Pioglitazone: common usage in the US

25

Indications and other considerations for rosiglitazone and pioglitazone

Good for overweight/obese patients;
Slow onset: 4-6 wks to affect blood glucose (may even take 3-4mos)

26

α-GlucosidaseInhibitors

Acarbose

27

Mode of action of acarbose

Delays carbohydrate digestion and slows glucose absorption in the gut
No effect on insulin release

28

Adverse drug reaction of acarbose

Dose related malabsorption, flatulence, nausea and diarrhea (No weight gain)

29

Newer Anti-Diabetics

Two main gut incretins:
GIP and GLP-1 (diminished in T2D post-meal)
Exenatide- IV
DPP-4 inhibitors (oral): sitagliptin
Both GLP-1 and GIP are rapidly inactivated by the enzyme dipeptidyl peptidase-4 (DPP-4).

30

Incretins

are a group of GI hormones that increase insulin release from the beta cells of the islets of Langerhans after eating. Incretin levels become elevated even before blood glucose levels. They also slow the rate of absorption of nutrients into the blood stream by reducing gastric emptying and may directly reduce food intake. They also inhibit glucagon release from the alpha cells of the Islets.