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PR3152 Pharmacology and Biopharmaceutics > Diabetic Agents > Flashcards

Diabetic Agents Flashcards

1
Q

Describe the mode of action of metformin

A

Inhibit gluconeogenesis in liver activates AMP-activated kinase

Also enhance tissue sensitivity to insulin allowing greater glucose uptake of tissues

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2
Q

Name the clinical benefits of metformin

A

Low risk of hyperinsulinemia and hypoglycemia

Weight loss

Improves lipids

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3
Q

How is Metformin absorbed?

A

Orally

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4
Q

How is Metformin distributed?

A

Rapid distribution

Minimal plasma protein binding

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5
Q

Is Metformin metabolized?

A

No

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6
Q

How is Metformin excreted?

A

Unchanged in the urine

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7
Q

What are some of the adverse effects associated with Metformin?

A

Diarrhea
Vomiting
Indigestion
Anorexia
Increase risk of B12 malabsorption

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8
Q

What are some patients that are contraindicated for use of Metformin?

A

Those with renal problems

Risk of lactic acidosis

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9
Q

Describe the mode of action of glipizide

A

Bind to SU receptor on proteins and inhibit K ATP channel mediated K efflux

This triggers calcium dependent exocytosis of insulin granules from pancreatic beta cells

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10
Q

What is a criteria for those who intend to start on glipizide?

A

Functional beta cells

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11
Q

How is glipizide absorbed? What is a special consideration to advice patients?

A

Oral

Need to be taken before food as absorption can be delayed with food

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12
Q

How is the distribution like for glipizide?

A

Bind extensively to plasma proteins

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13
Q

Why is glipizide preferred among the other sulphonylureas?

A

Lower risk of hypoglycemia

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14
Q

What are the adverse effects of glipizide?

A

Hypoglycemia

Weight gain

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15
Q

How is glipizide metabolized?

A

By the liver via hydroxylation

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16
Q

How is glipizide eliminated?

A

<10% excreted unchanged in urine and feces

17
Q

Why are the elderly more susceptible to hypoglycemia upon taking glipizide?

A

Poorer renal and liver function

18
Q

Describe the mode of action of Sitagliptin

A

Binds and inhibit DPP-4 enzymes which are responsible for degrading GLP-1

Therefore, prolongs action of endogenous insulin and suppresses alpha-cell mediated glucagon release.

Inhibits hepatic glucose production

Also can stimulate beta cells and increase glucose-stimulated insulin release.
Thus, decreasing blood glucose

19
Q

How is Sitgliptin absorbed?

A

Orally

20
Q

How is sitagliptin metabolized and excreted?

A

Metabolized by low hepatic metabolism and excreted in urine

21
Q

What are the adverse effects of Sitagliptin?

A

GI disturbances
Flu like symptoms
Skin reaction

22
Q

What are some contraindications to the use of Sitagliptin?

A

History of pancreatitis

Renal insufficiency

23
Q

Describe the mode of action of Liraglutide

A

Acts as a GLP-1 receptor agonist by activating GLP-1 receptors on pancreas

Activates adenyl cyclase

Increase cAMP and PKA

Therefore causing a cascade:
1. Increase insulin secretion
2. Decrease glucagon released
3. Delayed gastric emptying
4. Decreases appetite

24
Q

What is a clinical benefit of GLP-1 agonist?

A

Insulin secretion will subside as blood glucose decrease and achieve euglycemia

25
Q

How is liraglutide absorbed?

A

SC injection

26
Q

How is liraglutide distributed?

A

Extended plasma protein binding due to C16 fatty acid binding to plasma proteins

27
Q

How is liraglutide excreted?

A

Mostly already removed by proteolysis

Some removed by faeces and urine

28
Q

What is the advantages and disadvantages of using GLP-1 agonist?

A

Advantages: Encourages weight loss; Lesser risk of CVD death, non fatal MI and HF

Disadvantages: Expensive, possible ADR include acute pancreatitis, dyspepsia and N/V

29
Q

What is the mode of action of empagliflozin?

A

Inhibition of SGLT2 causes decrease renal reabsorption of filtered glucose.

Increased excretion of urinary glucose and decrease renal threshold of glucose

30
Q

What are the clinical benefits of using empagliflozin?

A

Decreases risk of major cardiac event

Decrease risk of worsening end point renal failure

31
Q

What is the ADME of empagliflozin?

A

A: Oral
D: Highly plasma protein bound
M: Metabolized in liver via glucuronidation
E: Feces and urine

32
Q

What are some of the adverse effects of empagliflozin?

A

UTI
Increased urination
Female genital mycotic infection
Diabetic ketoacidosis

PR3152 Pharmacology and Biopharmaceutics (6 decks)

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