Antidiabetic Agents Flashcards

1
Q
What are the functions of all the Key cell types of the endocrine pancreas?
Alpha
Beta
Delta
G
F
A
Alpha: Glucagon
Beta: Insulin
Delta: Somatostatin
G: Gastrin
F: Pancretic Polypeptide
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2
Q

What positively regulates Insulin release?

A
GLucose (subs)
Amino Acids (subs)
Incretins (horm)
Epi/B2- Adrenergic Stim (horm)
Vagus Stim (neuro)
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3
Q

What negatively regulates Insulin release?

A

NE/alpha 2 Adrenergic stim (neuro)

Amylin (horm)

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4
Q

What are the receptors on the Beta Cell that stimulate Insulin release?

A

Glucose dn reg.
ATP Sensitive K+ Channel
leads to voltage dependant Ca++ Channel opening

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5
Q

How does insulin work on the adipose and skeletal muscle cells?

A

GLUT 4 translocation

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6
Q

What actions does insulin have on metabolic pathways?

A

(+)FA, glycogen, Protein synth

(-) Beta Ox, Glycogenolysis, Glycolysis, Protein catabolism

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7
Q

What is the main mediatior of T1DM onset?

A

Autoimmune destruction of Beta Cells

Genetic Predisposition

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8
Q

What are the precursors of Full blown T2DM?

A
Insulin resistance and insulin secretory defect
Genetic Pre-disposition
Obesity
Nutrition
Physical Activity
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9
Q

What are the Signs and Symptoms of T1DM?

A
Polyuria
Thirst
Blurred Vision
Weight Loss/Polyphagia
Weakness/Dizziness
Paresthesia
Dec. LOC can be rapid or gradual onset
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10
Q

How do we diagnose diabetes clinically?

A

Glucose Challenge

High Blood Glucose after a meal.

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11
Q

What is the most common type of administration of Insulin?

A

Sub Cutaneous Injection

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12
Q

What is the theraputic goal of Insulin therapy?

A

Maintain blood glucose concentrations between 90 and 120 mg/dL.

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13
Q

Waht are the kinetic considerations of Insulin administration?

A

Diffusion into peripheral tissues is greater than with intrinsically derived insulin.

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14
Q

How is insulin kinetics altered?

A

Changing the AA sequence to make it stick together for a longer or shorter amount of time.

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15
Q

What are key features of Rapid acting insulin?

A

AA alteration in C terminal of B peptide Prevents insulin complex formation Duration of 3-5 hrs

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16
Q

What are key features of Short acting insulin?

A

Identical to human insulin 4-12 hrs

17
Q

What are key features of Intermediate acting insulin?

A

Protaimine Insulin complex

10-20 hrs

18
Q

What are key features of Long acting insulin?

A

AA changes make it precipitate at a more neutral pH
12-20 hrs
Myristic acid added to inc duration to 22-24 hrs

19
Q

What are examples of Rapid acting Insulin?

A

Lispro
Aspart
Glulisine
Inhaled insulin

20
Q

When do you want to use short acting insulin?

A

In response to a meal.

21
Q

What are examples of Intermediate acting Insulin?

A

NPH

22
Q

What are examples of Long acting Insulin?

A

Glargine

Detemir

23
Q

What is the most common adverse effect to insulin?

A
Hypoglycemia is most common. 
Hypersensitivity(rare)
Resistance (rare)
Lipohypertrophy
Lipoatrophy
24
Q

How is Lipohypertrophy avoided?

A

Inject insulin at a different place each time.

25
Q

When is glucagon therapy used?

A

Use if pt can’t take in glucose by mouth(unconcious)

26
Q

What are the key points of Metformin use?

A

1st line agent
Doesn’t prduce hypoglycemia
Not dependant on B cell function

27
Q

What is the MOA of Metformin?

A

Dec. Hepatic Glucose output
Increase peripheral glucose utilization
Activation of hepatic enzyme AMP-activated protein kinase

28
Q

What are the Adverse effects of Metformin?

A

GI disturbances

Vit B12 deficiency

29
Q

What is the MOA of Sulfonylureas and Meglitinides?

A

Inhibition of ATP-sensitive potassium channel of B cell, insulin release

30
Q

What are the Contraindications of the Glucosidase inhibitors?

A

Those with GI diseases bc: Inhibits brush border glucosidase enzyme and subsequent absorption of glucose

31
Q

What is the MOA of Thiazolidinediones?

A

Dec peripheral resistance by activating peroxisome proliferator-activated receptor
Effect on glucagon metabolism/insulin signaling

32
Q

What are the AA of Thiazolidinediones?

A

Peripheral edema, weight gain, hepato tox,
Bone Fractures
Hypoglycemia

33
Q

What is the MOA of Amylinomimetics?

A

Inhibits glucagon release
Inhibits gastric emptying
Anoretic effect.

34
Q

What is the MOA of Incretins?

A

Insulin secretion

otherwise the same as the amylinomimetics

35
Q

What is the MOA of DPP inhibitors?

A

inhibit incretin degradation.