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Endocrine > drug notes: incretin drugs > Flashcards

drug notes: incretin drugs Flashcards

1
Q

what is an OGTT?

A

oral glucose tolerance test

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2
Q

what is the incretin effect?

A

-if same amount of glucose is administered orally and on a separate occasion through IV then there will always be more insulin produced the time it has been given orally, suggesting there must be a substance in the gut which acts to increase insulin in the beta cell

(these substances in the gut are called incretins)

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3
Q

True or False

Incretin effect is lost later on in T2DM

A

False- incretin effect is lost earlier on in T2DM

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4
Q

what are the two incretins?

A

GIP

GLP-1

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5
Q

what cells secrete GIP?

A

K cells

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6
Q

what cells secrete GLP-1?

A

L cells

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7
Q

what enzyme breaks down GIP and GLP-1?

A

DPP-IV

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8
Q

what is the half life like for GIP and GLP-1?

A

very short half life

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9
Q

what are GIP and GLP-1 broken down into and what clears then?

A

they are broken down by DPP-IV into inactive metabolites and then cleared by the kidneys

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10
Q

how do incretins amplify insulin secretion?

A

-GLP-1 binds to receptot on pancreatic beta cell which increases cAMP and amplifies the release of insulin

however this cannot be done unless the regular triggering for insulin has occured

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11
Q

what pathway do incretins affect?

A

the amplifying pathway

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12
Q

what affect does increase in cAMP from incretins have on beta pancreatic cell?

A
  • close KATP channel (PKA)
  • modulate calcium currents (PKA)
  • directly on insulin secretory mechanism
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13
Q

what affect does GLP-1 have?

A
  • increase insulin secretion
  • decreases glucagon secretion
  • increases insulin biosynthesis
  • increases beta cell proliferation
  • decreases beta cell apoptosis
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14
Q

whats another name for DPP4 inhibitors?

A

gliptins

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15
Q

what is the mechanism of action of DPP4 inhibitors (aka Gliptins)?

A

they inhibit DPP4 and so increase the half life of GIP and GLP-1, increasing incretin effect

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16
Q

what do DPP4q (gliptins have in common with sulphonylureas?

A

they are insulin secretagogues

17
Q

can DPP4is cause hypoglycaemia?

A

no due to incretin being glucose dependant

18
Q

what affect to DPP4i have on weight?

A

no effect

19
Q

what are side effects of DPP4i?

A
  • generally very well tolerated
  • increased risk in pancreatitis
  • some signal for increased HF hospitalisation
20
Q

are DPP4i’s expensive?

A

yes very!!

21
Q

what is the mechanism of action of GLP-1RA?

A
  • they are GLP-1 like molecules modified to avoid breakdown by DPP4. They act directly on the GLP-1 receptor.
  • they act to promote insulin secretion (insulin secretagogues) in a glucose dependant mechanism and lower glucagon
  • act in other tissues especially hypothalamus to reduce apetite and intestines to reduce gastric emptying
22
Q

are GLP-1RA expensive?

A

yes very!

23
Q

what are side effects of GLP-1RA?

A
  • nausea and vomiting (often improves after 6 weeks)
  • small increase in gallstones
  • small increase in pancreatitis
24
Q

what effect does GLP-1RA have on CV health?

A

improves!

25
Q

when would GLP-1RA be given?

A
  • second line to metformin and high risk cardiovascular disease such as patients who have had a heart attack) (patient will be on metformin and GLP-1RA)
  • if a patient has heart failure or chronic kidney disease and SGLT2i are contraindicated then give GLP-1RA second line the metformin!
26
Q

what should be given to a patient with T2B with no prior disease, CVD, HF or CKD, have already tried metformin and needs to minimize hypoglycaemia?

A

DPP-4i
GLP-1RA
SGLT2i
TZD

27
Q

what should be given to a patient with T2B with no prior disease, CVD, HF or CKD, have already tried metformin and needs to lose weight?

A

GLP-1RA really good for weight loss

-SGLT2i

Endocrine (53 decks)

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