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Inflammation block > Pharmacology of T2DM > Flashcards

Pharmacology of T2DM Flashcards

1
Q

List the drugs used to treat T2DM

A
  • Biguanides
  • Sulphonyureas
  • Thiazolidinediones
  • Meglitinides
  • Incretins
  • Dipeptidylpeptidase 4 ( DPP4) inhibitors
  • alpha-glucosidase inhibitors
  • Sodium glucose transporter 2 (SGLT2) inhibitors
  • Amylin analogues
  • Insulin
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2
Q

What is an example of a biguanide

A

Metformin

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3
Q

Outline the characteristics of biguanides

A
  • Don’t affect the release of insulin,glucagon,GH,cortisol,somatostatin
  • May act through AMPK
  • Increase AMP levels
  • Inhibit adenylate cyclase/activate AMPK
  • mTOR (mammalian target for rampamyacin)
  • inhibition of glycerophosphate dehydrogenase
  • decrease hepatic gluconeogenesis
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4
Q

Outline the pharmacology of metformin including how it decreases BG levels

A

-absorbed from the small intestine
-Half life=3 hours
-Not bound to plasma protein,excreted unchanged in urine
Decrease blood glucose concentration by:
-decreased hepatic glucose production
-potentiate insulin action on muscle & adipose tissue
-stimulation of glycolysis in tissues,stimulate glucose uptake
-decrease carbohydrate absorption
-stimulate lactate production
-inhibit expression of genes involved in gluconeogenesis

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5
Q

What are the benefits of biguanides

A

-Doesn’t cause hypoglycaemia
-Reduced microvascular complications
-Doesn’t stimulate appetite
-Doesn’t cause weight gain
It is therefore the drug of choice in obese patients who fail with diet alone

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6
Q

What are the side effects of biguanides

A
  • diarrhoea
  • nausea
  • metallic taste
  • rare lactate acidosis
  • decreases intestinal absorption of folate& vitamin B12
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7
Q

What can biguanides be given with?

A

-sulphonylureas, thiazolidenediones, incretins, DPP4 inhibitors, SGLT2 inhibitors and/or insulin, but sulphonylureas, thiazolidenediones and insulin DO cause hypoglycaemia

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8
Q

Which GLUT channel is present in the beta cells of the pancreas?

A

GLUT2

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9
Q

What acute effects do sulphonylureas have?

A
  • Increase insulin release
  • Increase plasma insulin concentration
  • Decrease hepatic clearance of insulin
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10
Q

What chronic effects do sulphonylureas have?

A

-No acute increase in insulin release but decreased plasma glucose conc still remains
-Chronic hyperglycaemia decreases insulin release
-Down regulation of sulphonylurea receptor
-Largely protein bound (90-99%)
drug interactions =
-NSAIDs, MAO inhibitors, some antibiotics etc

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11
Q

What are the characteristics of sulphonylureas?

A

-Excreted in urine, enhanced effect in elderly & renal disease
-1st gen= long half life< 24hours
-2nd gen=short half life(7-10hours)
100x more potent
lasts for 16-24hours
less interactions

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12
Q

What are the side effects of sulphonylureas

A
  • Main adverse effect is hypoglycaemia
  • Neuroglycopenia
  • Confusion & coma( take oral glucose; if severe give iv glucose/glucagon/adrenaline)
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13
Q

Outline the characteristics of Meglitinides

A
  • Half life= 1 hour
  • More rapid, less sustained release, less potent that sulphonylureas, less hypoglycaemia
  • Take just before meal
  • Close K+ ATP channels on Beta cells
  • Share 2 binding sites with sulphonylureas but have their own distinct binding site
  • More selective for Beta cells than cardiac/vascular K+ ATP channels
  • can be used as monotherapy
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14
Q

Give egs of Meglitinides

A
  • Repaglinide (Prandin)

- Nateglinide( Stalix)

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15
Q

Give egs of thiazolidenediones(glitazones) and their associated adverse side effects

A
  • Troglitazone; liver toxicity
  • Rosiglitazone; cardiovascular problems
  • Pioglitazone; risk bladder cancer
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16
Q

Outline the characteristics of thiazolidenediones(glitazones)

A

selective agonists for:

  • PPARgamma (nuclear peroxisome proliferator-activated receptor gamma)
  • PPARgamma combines with RXR(Retinoid X receptor)

-Found in adipose tissue,muscle & liver

  • protein bound
  • half life=7 hours ; active metabolite half life=24 hours
  • Takes 6-12 weeks for max effect to develop
  • Give with metformin or other hypoglycaemic drugs
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17
Q

Outline the mechanism of action of thiazolidenediones(glitazones)

A
  • Activates insulin responsive genes that control CHO & lipid metabolism
  • Needs insulin to be effective
  • Reduces insulin resistance in peripheral tissues
  • Reduces glucose production by liver
  • Increases glucose uptake in muscle& adipose tissue potentiates actions of insulin
  • Increase adipocyte number & lipogenesis
18
Q

What are the side effects of thiazolidenediones(glitazones)

A

-weight gain (1-4kg) due to increased differentiation of adipocytes, fluid retention by stimulating amiloride sensitive Na+ absorption

19
Q

What are incretins? Give examples.

A
  • Compound stimulates insulin release
  • GIP: glucose-dependent insulinotrophic peptide or gastric inhibitory peptide K cells in duodenum
  • GLP1: glucagon-like peptide 1 L cells in distal ileum
20
Q

What are the actions of incretins?

A
  • Acts on incretin receptor (GLP-1 receptor)
  • Stimulates insulin release
  • Suppresses glucagon secretion
  • Reduces appetite& body weight
  • Slows gastric emptying
  • Stimulated beta cell number
21
Q

Give examples of incretins (GLP-1 analogues)

A 
Byetta
Bydureon
Victoza(liraglutide)
Lyxumia(lixisenatide)
Eperzan(albiglutide)
Trulicity(dulaglutide)
Ozempic (semaglutide)
22
Q

What are serine protease dipeptidyl peptidase 4 (DPP4) inhibitors?

A
  • breakdown natural incretins

- Gliptins DPP4 inhibitors

23
Q

What are the benefits of DPP4 inhibitors

A
  • No effect on weight

- No hypoglycaemia

24
Q

List some serine protease dipeptidyl peptidase 4 (DPP4) inhibitors

A
  • Sitagliptin(Januvia)
  • Vildagliptin(galvus)
  • Saxagliptin(onglyza)
  • Linagliptin(tradjenta)
25
Q

What is a possible side effect of serine protease dipeptidyl peptidase 4 (DPP4) inhibitors

A

-increase in incidence of some cancers

26
Q

What are eg’s of alpha-glucosidase inhibitors?

A

Acarbose & Miglitol

27
Q

Outline the characteristics of alpha-glucosidase inhibitors

A
  • Inhibits intestinal brush border alpha-glucosidase
  • Reduces postprandial increase in blood glucose levels
  • effective in IDDM& NIDDM (Type 1 &2)
  • poorly adsorbed
28
Q

What is the benefit of alpha-glucosidase inhibitors?

A

-Don’t cause hypoglycaemia

29
Q

What are the potential side effects of alpha-glucosidase inhibitors?

A

faltulence & diarrhoea

30
Q

What is the function of sodium glucose transporter 2 (SGLT2)inhibitors?

A
  • inhibit glucose re-uptake in the kidney

- give up to 10% excretion of calorie intake

31
Q

Give eg’s of SGLT2 inhibitors

A
  • dapagliflozin (Forxiga)
  • canaglifozin(Invokana-SGLT2 &SGLT1)
  • empaglifozin (Jardiance)
32
Q

Outline the characteristics of amylin analogues

A
  • Amylin(37aa) main component of pancreatic amyloid related to calcitonin/CGRP
  • Decreases gastric emptying
  • Inhibits glucagon release
  • Promotes satiety
  • Related to Beta-amyloid & can form aggregates
33
Q

What is Pramlintide; what’s the benefit of it

A

-analogue of human amylin with pro replacement as in rat amylin,
BENEFIT=does not aggregate

34
Q

How should amylin analogues be taken?

A

Adjunct for both type 1 & type 2

35
Q

Which medication controls appetite

A
  • Incretins

- Amylin

36
Q

Which medication reduces glucose reabsorption

A

-SGLT2 inhibitors

37
Q

Which medications increases glucose uptake & utilization?

A
  • Thiazolidinediones

- Metformin

38
Q

Which medications reduces lipotoxicity

A
  • Thiazolidinediones

- Salcylates

39
Q

Which medications reduces hepatic glucose output

A
  • Metformin

- Thiazolidinediones

40
Q

Which medications reduce blood glucose levels via the GI tract

A
  • Incretins
  • alpha glucosidase inhibitors
  • Amylin
  • Bile acid sequestrant
41
Q

Outline various treatments for obesity

A
  • Monoamine uptake inhibitor
  • Cannabinoid CB1antagonist
  • Lipase inhibitor
  • Belviq 5HT2c agonist
  • Qsymia
  • Contrave
  • Saxenda GLP-1 agonist

Inflammation block (27 decks)

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