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Mechanism of Drug Action (Drugs) > Diabetes mellitus and SLE (Drugs) > Flashcards

Diabetes mellitus and SLE (Drugs) Flashcards

1
Q

How can type I diabetes be treated?

A

Insulin

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2
Q

What are the types of insulin available?

A
  1. Fast-acting insulin
  2. Short-acting insulin
  3. Intermediate-acting insulin
  4. Long-acting insulin
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3
Q

What is an example of fast-acting insulin?

A

Insulin lispro

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4
Q

What is the mechanism of action of insulin lispro?

A
  • Swapping of Lys/Pro residue in C-terminus
  • Prevents oligomerisation of free insulin particles that causes deactivation
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5
Q

What is an example of short-acting insulin?

A

Unmodified insulin

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6
Q

What is an example of an intermdiate-acting insulin?

A

Neutral protamine hagedorn (NPH) insulin

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7
Q

What is the mechanism of action of NPH insulin?

A
  • Suspension of protamine and insulin
  • Causes formation of insoluble crystals of insulin and protamine that causes slow release of insulin
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8
Q

What are examples of long-acting insulin?

A
  1. Ultratard
  2. Glargine
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9
Q

What is the mechansm of action of ultratard?

A
  • Suspension of Zn2+ and insulin
  • Causes formation of insoluble Zn2+ and insulin crystals that release insulin slowly
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10
Q

What is the mechanism of action of glargine?

A
  • Amino acid changes to the α/β chain causes shift in isoelectric point
  • Causes aggregation of insulin particles once injected, reducing rate of absorption
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11
Q

How can type II diabetes be treated?

A
  1. Exercise and diet
  2. Metformin
  3. Sulphonylureas
  4. Meglitinides
  5. Thazolidinediones
  6. α-glucosidase inhibitors
  7. Incretin-related drugs
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12
Q

What is the mechanism of action of metformin?

A

Activation of AMPK receptors resulting in number of genetic changes leading to:

  1. ↓ Hepatic gluconeogenesis
  2. ↑ Glucose uptake by skeletal muscles
  3. ↓ Intestinal carbohydrate reabsorption
  4. ↓ Circulating levels of LDLs
  5. ↓ Appetite
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13
Q

What are the side effects of metformin?

A
  1. GI disturbalces
  2. Lactate acidosis
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14
Q

What is the mechanism of action of sulphonylureas?

A

Binds to SUR1 subunit of KATP in β-islet cells and causes closure, leading to increased release of insulin.

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15
Q

What are examples of sulphonylureas?

A
  1. Glibenclamide
  2. Glipizide
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16
Q

What are the side effects of sulphonylureas?

A
  • Hypoglycaemia
  • Increased appetite
  • Cardiovascular risk (due to inhibition of cardiac KATP)
17
Q

What is the mechanism of action of meglitinides?

A

Binds to SUR1 subunit of KATP in β-islet cells and causes closure, leading to increased release of insulin, but is much faster acting compared to sulphonylureas.

18
Q

What is an example of meglitinides?

A

Repaglinide

19
Q

What are the clinical uses of meglitinides and why?

A
  • Taken before meals
  • Fast-acting
20
Q

What is the mechanism of action of thiazolidinediones?

A

Activation of PPARγ and induction of changes that including:

  1. ↑ Lipogenesis
  2. ↑ Glucose/fatty acid uptake
  3. ↑ Expression of transporters including GLUT4
21
Q

What is an example of thazolidinediones?

A

Pioglitazone

22
Q

What are the side effects of thiazolidinediones?

A
  • Weight gain
  • Fluid retention (enhancement of amiloride-sensitive Na+ absorption)
23
Q

What are the clinical uses of thiazolidinediones and why?

A
  • GIven as an add-on to other drugs
  • Slow acting
24
Q

What is the mechanism of action of α-glucosidase inhibitors?

A

Inhibits breakdown of starch/disaccharides into glucose in the GI tract and reduces amount of glucose absorption.

25
Q

What is an example of an α-glucosidase inhibitor?

A

Acarbose

26
Q

What are the side effects of α-glucosidase inhibitors?

A
  1. Flatulence (accumulation of gas in GI tract)
  2. Diarrhoea
27
Q

What are the incretin-related drugs?

A
  1. Exenatide
  2. Sitagliptin
28
Q

What is the mechanism of action of exenatide?

A

Mimics glucose-reducing effects of GLP-1

29
Q

What is the mechanism of action of sitagliptin?

A

Inhibition of DPP-4, which breaks down GLP-1 and GIP, thus increasing levels of these incretins.

30
Q

What are the treatments for lupus?

A
  1. NSAIDs
  2. Hydroxychloroquine
  3. Corticosteroids
  4. Immunosuppressants
  5. Rituximab
  6. Belimumab
31
Q

What is the mechanism of action of hydrochloroquine in treating lupus?

A

Reduces inflammation probably by reducing interferon production.

32
Q

What is the mechanism of action of rituximab

A

Binds to CD20 on B cells, causing destruction.

33
Q

What is the mechanism of action of belimumab?

A

Sequesters BLyS and prevents it from stimulating B cell activity.

Mechanism of Drug Action (Drugs) (26 decks)

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