Anti-hyperglycemics Flashcards

1
Q

Anti-hyperglycemics

A

Insulin replacements (Lispro, Regular, NPH, Glargine), Inhibitors of CHO absorption, Insulin secretagogues, Insulin sensitizers, Insulin releasers, Na-glucose cotransporter 2 inhibs

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2
Q

What are the rapid insulin preparations

A

Lispro, Aspart, Glulisine

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3
Q

What is the short acting insuline preparation?

A

Regular (human)

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4
Q

What is the intermediate insulin preparation?

A

NPH (neutral protamine hagadorn)

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5
Q

What are the long-acting insulin preparations?

A

Glargine, Detimir

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6
Q

What are the CHO absorption inhibitors?

A

Acarbose, Miglitol

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7
Q

Acarbose, Miglitol (CHO absorption) - MoA

A

alpha-glucosidase inhibitor prevents cleavage of disaccharides to monosaccharides

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8
Q

Acarbose, Miglitol (CHO absorption) - adverse effects

A

GI side effects include flatulence (80%), diarrhea (27%) and nausea (8%) . Titrating the dose of drug slowly reduces GI side effects.

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9
Q

What are the insulin secretagogues?

A

Sulfonylureas
Repaglinide
Nateglinide

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10
Q

Sulfonylureas - MoA

A

Blocks potassium channel. Cell becomes more positive and depolarizes. Calcium enters cell and causes a release of insulin granules

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11
Q

What are the sulfonylureas?

A

1st generation - chlorpropamide

2nd generation - Glyburide, Glimeperide, Glipizide

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12
Q

Sulfonylureas - adverse effects

A

Hypoglycemia and weight gain

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13
Q

Sulfonylureas - Contraindications

A

Type 1 Diabetes
Pregnancy
Lactation
Significant Renal and/or hepatic insufficiency

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14
Q

Insulin Secretagogues -Meglitinides (Repaglinide, Nateglinide)

A

Same mechanism of action as sulfonylureas but needs glucose to work.

Metabolized by liver, so watch out for liver failure

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15
Q

Insulin Sensitizers

A

Biguanides, Thiazolidinediones

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16
Q

Biguanides example

A

Metformin

17
Q

Metformin (Biguanide) - MoA

A

Decr. Mitochondrial ATP production

Net: decr. hepatic glucose production and incr. glucose uptake in muscle and adipose

Incr. expression or activity of glycolytic enzymes and Glut-4

Can reduce plasma glucose by 25% and decrease Hb A1C by 1-2%. Also lowers TG levels

18
Q

Metformin - adverse effect

A

metabolic acidosis with non-compliance

19
Q

Metformin - contraindication

A

Not used if receiving contrast
Not used with acidosis
Not used with renal failure (>1.5 men and 1.4 women)

20
Q

Thiazolidinediones (insulin sensitizers) example

A

Pioglitazone

21
Q

Pioglitazone - MoA

A

Activate nuclear receptors - peroxisome proliferator-activator receptors (PPAR-y)

Stimulates fat synthesis and decreases free fatty acids.

Increases insulin sensitivity

22
Q

Pioglitazone - adverse rxns

A

Can worsen or cause heart failure. Also causes edema and a decrease in hematocrit

23
Q

New Classes - Amylin, Pramlintide - MoA

A

suppresses inappropriate postprandial
glucagon secretion

delays gastric emptying
suppress appetite.

24
Q

New Classes - Incretin - Glucagon-like peptide (GLP) - MoA

A
  • increases Beta cell number
  • enhances insulin release
  • Inhibits glucagon secretion
  • delays gastric emptying
  • suppress appetite, weight loss
25
Q

GLP-1 agonists (2)

A

Exenatide, Liraglutide

26
Q

DPP-4 inhibitors (4)

A

Sitagliptin, Linagliptin, Alogliptin, Saxagliptin

27
Q

DPP-4 inhibitors - MoA

A

Blocks enzyme that degrades incretin (GLP-1) called dipeptidl peptidase-4

28
Q

Sodium Glucose co-transporter inhibitors (2)

A

Canagliflozin

Dapagliflozin

29
Q

Sodium-Glucose co-transporter inhibitor - MoA

A

Inhibits the sodium-glucose co-transporter 2 in the kidney leads to an increase in urine glucose and a decrease in blood glucose

30
Q

Sodium-glucose co-transporter inhibitor - contraindication

A

Renal insufficiency
Hypotension
Hyperkalemia

31
Q

Hyperglycemics

A
Glucagon
Diazoxide (opens K channels in beta cells and prolongs open state, hyperpolarizes cell)