Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Endocrinology > drugs used in the treatment of type 2 diabetes mellitus > Flashcards

drugs used in the treatment of type 2 diabetes mellitus Flashcards

1
Q

Why do we even need to treat hyperglycaemia?

A

For every decrease of 10 mmol/mol in HbA1c you reduce the risk of microvascular complications by 25%/

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Treatment of T2DM

A

1st line= metformin
2nd line= dual therapy with METFORMIN PLUS A sulfonylurea or pioglitazone or GLP-1 agent or SGLT-2 inhibitor
3rd line= triple therapy
4th line= insulin therapy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What class of drug does metformin belong to?

A

Metformin is a biguanide.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is the mechanism of action of metformin?

A
  • reduces hepatic gluconeogenesis by stimulating AMP-activated protein (AMPK)
  • increases glucose uptake and utilisation by skeletal muscle by increasing insulin signalling
  • reduces carbohydrat absorption
  • increases fatty acid metabolism
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

desirable affects of metformin

A
  • reduces HbA1c by 15-20mmol/mol
  • does not cause hypoglycaemia when used as a mono therapy
  • reduces microvascular and macrovascualr complication
  • causes weight loss
  • reduces triglycerides and LDL
  • safe to use in pregnancy and used to treat polycystic ovarian syndrome
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

adverse affects of metformin

A
  • GI side affects can occur in up to 25% of people, but only 5% cannot tolerate the drug because of nausea, vomiting, diarrhoea and taste disturbances
  • lactic acidosis is a rare side effect but can occur so should not be used in people with significant renal or hepatic disease
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

use of metformin in renal disease

A

metformin dose should be halved when EGFR is between 30-45 ml/min and when EGFR falls to 30ml/min metformin should be stooped completely

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

prescribing metformin

A

start with 500mg od or bd ad slowly titrate up to the maximum dose of 1g bd to reduce the risk of GI intolerance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

examples of sulfonylureas

A

gliclazide, glibenclamide, glimepiride

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

mechanism of action of sulfonylureas

A
  • displaces the binding of ADP-Mg2+ from the SUR1 subunit which closes the KATP channel causing depolarisation and subsequent insulin release
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

desirable affects of sulfonylureas

A
  • works quicker than metformin
  • reduces HbA1c by 15-20mmol.mol
  • reduces risk of microvascular complications
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

adverse affects of sulfonylureas

A
  • hypoglycaemia due to excessive insulin secretion even when blood glucose levels are low, more common in elderly, alcoholics and those with chronic kidney and liver disease
  • weight gain due to the anabolic affect of insulin which is increased, increase in appetite and urinary loss of glucose decreased
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

prescribing a sulfonylurea

A
  • only used first line where metformin is contra-indicated, mostly used second line with metformin
  • should be avoided in the frail elderly, severely obese, and not safe in pregnancy
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

which sulfonylurea is safe in pregnancy

A

glibenclamide as it does not cross the placenta

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

only example of thiazolidinediones

A

pioglitazone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

mechanism of action of pioglitazone

A

exogenous agonist of PPAR- GAMMA
- PPAR gamma associated with retinoid receptor X (RXR) to form a complex which acts as a transcription factor that binds to DNA to promote the expression of genes encoding several proteins involves in insulin signalling and lipid metabolism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

desirable affects of pioglitazone

A
  • reduces HbA1c by 15-20mmol/mol by increasing insulin sensitivity
  • does not cause hypoglycaemia
  • promotes fatty acid uptake and storage in adipocytes rather than in skeletal muscle and liver
18
Q

adverse affects of pioglitazone

A
  • increases the risk of hip fractures by 20% per year of use therefor should not be used in those over 65
  • causes fluid retention as they promote sodium reabsorption in the kidneys so is contra-indicated in people with heart failure
19
Q

whats the downside of pioglitazone

A

it does not reduce the risk of microvascular or macrovascular complications

20
Q

prescribing pioglitazone

A

15-45mg od not really used as much anymore due to newer better agents

21
Q

What is the incretin affect?

A

The incretin affect is the affect which describes how insulin responds to oral glucose greater than the insulin response which will be elicited in response to IV gludoce/

22
Q

the ingestion of food

A

stimulus the release of glucagon like peptide 1 (GLP-1) AND glucose dependant insulinotropic peptide (GIP) from enteroendocrine cells in the small intestine (K cells in the duodenum, L cells in the ileum)

23
Q

GLP-1 and GIP then

A

enter the portal blood and enhance insulin release from pancreatic beta cells and delay gastric emptying which enhances glucose uptake and utilisation

24
Q

GLP-1 also

A

decreases glucagon release from pancreatic alpha cells causing decreased production of glucose

25
Q

both of these actions

A

decrease blood glucose

26
Q

incretin analogues known as

A

GLP-1 AGONISTS

27
Q

List examles of GLP-1 Agonists>

A

exenatide and liraglutide

28
Q

mechanism of action of GLP-1 AGONISTS

A

bind as agonist to GPCR GLP-1 receptors that increase intra-cellular cAMP concentration in pancreatic beta cells to stimulate insulin expression and excretion

29
Q

desirable affects of GLP-1 agonists

A
  • promotes insulin secretion but will not cause hypoglycaemia
  • surpasses secretion of glucagon
  • delayed gastric emptying causes early satiety
  • acts on hypothalamus to reduce apetite
30
Q

What are the adverse affects of GLP-1 Agonists and GIP[

A
  • they have to be injected

- increases risk of acute pancreatitis

31
Q

the action of GLP-1 and GIP is

A

very rapidly terminated by the enzyme dipeptidyl peptidase-4 (DPP-4)

32
Q

examples of DPP-4 inhibitors

A

saxalgliptin, vildagliptin, linagliptin, alogliptin

33
Q

mechanism of action

A

gliptins competitively inhibit DPP-4 prolonging the action of endogenous GLP-1 and GIP and increasing plasma insulin

34
Q

desirable affects

A
  • promotes insulin secretion from pancreas without hypoglycaemia
  • surpasses glucagon
35
Q

adverse affects

A
  • they’re not potent at all because they only work on the endogenous GLP-1 AND GIP but in type 2 diabetes the levels of there 2 enzymes in already low so inhibiting there breakdown doesn’t have a massive affects on HbA1c levels
  • may increase risk of acute pancreatitis
36
Q

examples of SGLT-2 inhibitors

A

dapagliflozin, empagliflozin, canagliflozin

37
Q

mechanism of action of SGLT-2 inhibitors

A

selectively blocks the SGLT-2 transported in the proximal tubule of the kidney by blocking the reabsorption of glucose directly causes glucosuria

38
Q

desirable affects of SGLT-2 inhibitors

A
  • reduces blood glucose but unlikely to cause hypoglycaemia

- causes wight loss for the first 3-4 weeks

39
Q

adverse affects

A
  • increased incidence of though and urinary tract infections
40
Q

anyone who has type 2 diabetes and has had a myocardial infarction should be given

A

empagliflozin independent of there HbA1c levels as it reduces the risk of cardiovascular death

41
Q

Who can you not use SGLT-2 in?

A

You cannot use SGLT-2 inhibit

Endocrinology (15 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions