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Doctor, Patient and Disease Lectures > New Diabetic Drugs for diabetes > Flashcards

New Diabetic Drugs for diabetes Flashcards

1
Q

How do you manage hyperglycaemia conservatively. (2)

A

Diet.

Exercise.

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2
Q

How do you manage hyperglycaemia medically. (6)

A 
Biguanide. 
Sulphonylureas. 
Insulin sensitisers (thiozolidinediones)
Insulin. 
Incretins.
Gliptins.
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3
Q

Give an example of a biguanide.

A

Metformin.

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4
Q

Give and example of a sulphonylurea.

A

Gliclazide.

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5
Q

Give an example of a thiozolidinediones.

A

Rosiglitazone.

Pioglitazone.

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6
Q

Give an example of an incretin.

A

GLP-1

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7
Q

Give an example of a gliptin.

A

Dipeptidyl peptidase 4 inhibitors (DPP4 inhibitors)

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8
Q

How do you use insulin in diabetes. (2)

A 
Long acting (depot) insulin. (eg insulin zinc suspension).
Short acting (eg normal soluble insulin) with each meal.
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9
Q

Give two examples of short acting insulins.

A

Insulatard.

Actrapid.

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10
Q

What problem is there with administering soluble natural insulin to diabetics.

A

When soluble natural insulin is given subcutaneously, it forms a hexamer under the skin, delaying release.

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11
Q

What must you do if you are using soluble natural insulin as a short acting insulin.

A

Inject it 30mins before a meal.

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12
Q

What are two examples of insulin analogues.

A

Lispro.

Aspart.

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13
Q

How does lispro differ from natural insulin.

A

It replaces a proline with a lysine at position 28

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14
Q

How does aspart differ from natural insulin.

A

It replaces the proline to aspartate at position 28

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15
Q

What benefit is there to using lispro or aspart instead of natural insulin before means.

A

They are very fast acting, so the patient can eat immediately after injecting.

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16
Q

What is the purpose of long acting insulin analogues.

A

Different alterations in the insulin molecule to try and attain a plateau like concentration over time.

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17
Q

What is insulin glargine.

A

A long acting insulin that seems to give the least variation in plasma insulin levels for 24h after injection.

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18
Q

How many insulin gargine injections do you need/day.

A

One per 24h period.

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19
Q

What is the structure of insulin detemir.

A

14C fatty acid chain attached to B29.

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20
Q

How long does it take for the effects of insulin detemir to come on.

A

It has a delayed onset of 7h.

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21
Q

What are the main advantages of using insulin to control DM.

A

Can give the best control of HbA1c when combined with diet and exercise.
No side effects compared to the others.

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22
Q

What is a side effect of metformin.

A

Diarrhoea.

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23
Q

What are the side effects of thiozolidinediones. (2)

A

Rarely hepatic.

Osteoporosis.

24
Q

Which thiozolidinediones has been withdrawn from the market. Why.

A

Rosiglitazone has been withdrawn from the market over a link to fluid retention and increased risk of heart failure.

25
Q

What are the disadvantages of insulin. (5)

A

If you drive HGM, you cannot work.
Hypoglycaemia common even with good control.
Weight gain common.
Huge doses required.

26
Q

Which insulin is exempt from not allowing you to work with HGM.

A

Exenatide.

27
Q

Why do you gain weight with insulin treatment.

A

Glycosuria is stopped, saving many calories.

Increasing your appetite, and improving your well being.

28
Q

Where is GLP-1 and GIP released from.

A

GI tract.

29
Q

What two hormones does the pancreas release.

A

Insulin.

Glucagon.

30
Q

What cells release insulin.

A

Beta cells in the pancreas.

31
Q

What cells release glucagon.

A

Alpha cells in the pancreas.

32
Q

What effect does GLP-1 and GIP have on the pancreas (2)

A

Decrease glucagon.

Increases insulin.

33
Q

Insulin ______ peripheral glucose uptake.

A

Increases.

34
Q

Increased insulin and ______glucagon ______hepatic glucose output.

A

Decreased.

Reduce.

35
Q

What is the incretin effefct.

A

You get a much more intense insulin response if you administer glucose orally, than if you administer it intravenously.

36
Q

What effects (besides insulin control) does GLP-1 have. (2)

A

Reduces gastric emptying.

Increases hypothalamic satiety.

37
Q

What is interesting about the venom produced by the gila monster.

A

It produces a venom called exendin 4, which is very similar to GLP-1 (an incretin!)

38
Q

What venom is produced by the gila monster.

A

Exendin 4.

39
Q

What is the difference between endogenous GLP-1 and exendin 4 from gila monsters.

A

Exendin 4 is similar in structure to GLP-1, but has a longer half life.

40
Q

What is exenatide a synthetic version of.

A

Exendin 4.

41
Q

What is the main function of exenatide. (4)

A

To increase hypothalamic satiety.
Stimulates insulin secretion.
Slows gastric emptying.
Inhibits insulin production by the liver.

42
Q

What is the action of the DPP-4 enzyme.

A

To rapidly degrade incretins.

43
Q

Give two examples of gliptins.

A

Vildagliptin.

Sitagliptin.

44
Q

Where is the SGLT2 and SGLT1 cotransporter located.

A

In the proximal tubule of the kidney nephron.

45
Q

What is the function of SGLT1/2.

A

To reabsorb glucose in the proximal tubule of the kidney.

46
Q

What volume of plasma is filtered by the kidney in a day.

A

180L

47
Q

What volume of glucose is filtered by the kidney in a day.

A

180g

48
Q

How much glucose is reabsorbed by the kidney every day.

A

160-180g

49
Q

How much glucose is excreted by the kidney every day.

A

Minimal.

50
Q

What is the renal threshold.

A

It is the ‘tipping point’ at which the reabsorptive capacity of SGLT2 is exceeded, and urinary glucose excretion in increased.

51
Q

What happens to SGLT2 in T2DM.

A

Increased expression, causing more absorption of glucose.

52
Q

What happens to the adaptive increase in renal threshold in response to hyperglycaemia in T2DM.

A

It becomes maladaptive, reinforcing raised glucose levels.

53
Q

What is the renal threshold increased to in people with T2DM.

A

14mmol/L

54
Q

What is the purpose of an SGLT2 inhibitor in treating T2DM.

A

It lowers the inappropriately elevated renal threshold for glucose in T2DM, increasing glucose excretion.

55
Q

Give an example of an SGLT2 inhibitor.

A

Canagliflozin.

56
Q

What are some common side effects of canagliflozin (>1% (8)

A 
Constipation.
Thirst.
Nausea. 
Polyuria (increased volume)  or pollakiuria (increased frequency).
UTIs.
Balanitis or balanoposthitis. 
Increased haematocrit.
57
Q

What are some very common side effects of canagliflozin. (>10%) (2)

A 
Hypoglycaemia when used in combination with insulin or sulphonylurea. 
Vulvovaginal candidiasis (thrush).

Doctor, Patient and Disease Lectures (36 decks)

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