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Pharmacology & Therapeutics > Pharmacology of Diabetes > Flashcards

Pharmacology of Diabetes Flashcards

Metformin Dipeptidyl-peptidase 4 (DPP) inhibitors Sulphonylurea Sodium glucose co-transporter (SGLT2) inhibitors

1
Q

What is metformin used for?

A
  • Glycemic control in type 2 diabetes mellitus
  • For insulin resistance in polycystic ovary syndrome (PCOS)
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2
Q

What is the primary drug target of metformin?

A
  • 5’-AMP-activated protein kinase (AMPK)
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3
Q

What is the drug target type of metformin?

A
  • Enzyme antagonist
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4
Q

What is the location of action of metformin?

A
  • Hepatocyte mitochondria (Therapeutic effects)
  • Gastrointestinal mitochondira (Adverse effects)
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5
Q

What are the mechanism of action of metformin?

A
  • Metformin is uptaken into the hepatocytes by organic cation transporter-1 (OCT1)
  • Metformin inhibits mitochondrial complex I → preventing the production of mitochondrial ATP → increase cytoplasmic ADP:ATP & AMP:ATP ratios
  • These changes activate 5’-AMP-activated protein kinase (AMPK), an enzyme that plays an important role in the regulation of glucose metabolism
  • Increases in AMP:ATP ratio inhibit fructose-1,6-bisphosphatase enzyme → inhibition of gluconeogenesis
  • Increases in AMP:ATP ratio inhibit fructose-1,6-bisphosphatase enzyme → inhibition of adenylate cyclase & decreasing the production of cyclic adenosine monophosphate (cAMP)
  • Activated AMPK phosphorylates two isoforms of acetyl-CoA carboxylase enzyme → inhibiting fat synthesis → fat oxidation → reducing hepatic lipid stores & increasing liver sensitivity to insulin
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7
Q

What are the main adverse effects of metformin (1)?

A
  • GI side effects (Abdominal pain / Decreased appetite / Diarrhoea / Vomiting)
    • Presence of OCT-1 in the gastrointestinal tract
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8
Q

When is metformin most effective?

A
  • Most effective in the presence of endogenous insulin, so it’s most effective with some residual functioning pancreatic islet cells
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9
Q

What is DPP-4 inhibitors used for?

A
  • Management of type 2 diabetes mellitus
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10
Q

What is the primary drug target of DPP-4 inhibitors?

A
  • Dipeptidyl peptidase-4
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11
Q

What is the drug target type of DPP-4 inhibitors?

A
  • Enzyme antagonist
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12
Q

What is the mechanism of action of DPP-4 inhibitors?

A
  • DPP-4 inhibitor inhibit DDP-4
  • Decrease in metabolism of incretins (GLP-1) in the plasma
  • Increase in GLP-1
  • Increase in insulin when needed
  • Decrease glucagon when not needed & slow down digestion and appetite
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13
Q

What is the location of action of DPP-4 inhibitors?

A
  • Vascular endothelium
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15
Q

What are the main adverse effects of DPP-4 inhibitors (2)?

A
  • Upper respiratory tract infections (headache / runny nose / sore throat)
  • Serious allergic reaction (less common)
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16
Q

When is DPP-4 inhibitors most effective?

A
  • Most effective in the presence of endogenous insulin, so it’s most effective with some residual functioning pancreatic islet cells
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17
Q

What is the benefit of DPP-4 inhibitors over the other antidiabetic drugs?

A
  • It does not appear to cause weight gain
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18
Q

What is sulfonylurea used for?

A
  • Management of type 2 diabetes mellitus
19
Q

What is the primary drug target of sulfonylurea?

A
  • ATP-sensitive potassium channel (KATP)
20
Q

What is the mechanism of action of sulfonylurea?

A
  • Inhibit KATP
  • Leads to depolarisation of membrane
  • Ca2+ influx
  • Increase in insulin vesicle exocytosis
21
Q

What is the drug target type of sulfonylurea?

A
  • Ion channel antagonist
22
Q

What is the location of action of sulfonylurea?

A
  • Pancreatic beta cell
24
Q

What are the main adverse effects of sulfonylurea (2)?

A
  • Weight gain
  • Hypoglycaemia
25
Q

What are sodium glucose co-transporter (SGLT2) inhibitors used for?

A
  • Management of type 1 diabetes mellitus
26
Q

What is the mechanism of action of SGLT2 inhibitors?

A
  • Inhibits SGLT2
  • Decrease glucose reabsorption
  • Increase urine glucose secretion
27
Q

What is the primary drug target of SGLT2 inhibitors?

A
  • Sodium glucose co-trasporter (SGLT2)
28
Q

What is the drug target type of SGLT2 inhibitors?

A
  • Transport protein antagonists
29
Q

What is the location of action SGLT2 inhibitors?

A
  • Proximal convoluted tubule
31
Q

What are the main adverse effects of SGLT2 inhibitors (5)?

A
  • Uro-genital infection due to increased glucose load
  • Slight decraese in bone formation
  • Can worsen diabetic ketoacidosis
  • Weight loss
  • Decrease in BP

Pharmacology & Therapeutics (11 decks)

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