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Principles of Therapy > Theme 8 - Endocrine Pharmacology > Flashcards

Theme 8 - Endocrine Pharmacology Flashcards

1
Q

Name the 3 hormones of the pancreas

A

insulin
glucagon
somatostatin

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2
Q

What are the metabolic effects of glucagon?

A

Stimulates gluconeogenesis and glycogenolysis

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3
Q

What effect does glucagon have on blood glucose?

A

increases blood glucose levels

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4
Q

Which 5 processes does insulin inhibit?

A 
gluconeogenesis
glycogenolysis
lipolysis
ketogenesis
proteolysis
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5
Q

Which 5 processes does insulin stimulate?

A
  • glucose uptake in muscles and tissues
  • glycolysis
  • glycogen synthesis
  • protein synthesis
  • uptake of ions
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6
Q

What effect does insulin have on blood glucose?

A

decreases blood glucose levels

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7
Q

Describe the mechanism of action by which insulin is released by the b-cells of the pancreas.

A
  • K+ channels in beta-cells are regulated by intracellular ATP
  • When blood glucose increases, more glucose enters beta-cells and intracellular ATP increases and closes K+ channels
  • Depolarisation of beta-cells initiates influx of Ca2+ ions through voltage- sensitive Ca2+ channels
  • This process triggers insulin release
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8
Q

Describe the structure of an insulin receptor

A

Membrane spanning glycoprotein with 2 alpha subunits

and 2x beta subunits covalently bonded by disulphide bonds

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9
Q

What is the action of an insulin receptor?

A

Insulin binds to a subunit, the insulin-receptor complex enters the cell and produces metabolic effects.

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10
Q

Name 3 rapid acting insulins

A

insulin lispro, insulin aspart, insulin glulisine

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11
Q

Name a short acting insulin

A

regular insulin

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12
Q

Name an intermediate acting insulin

A

NPH insulin (isophane insulin)

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13
Q

Name 2 long-acting insulins

A

insulin glargine and insulin detemir

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14
Q

What is premixed biphasic insulins a combination of?

A

Combination of prandial & basal insulin, premixed in defined ratios: 30% rapid/short-acting and 70% intermediate-acting

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15
Q

What is the onset and duration of action of premixed biphasic insulins?

A 
Rapid onset (due to rapid/short acting insulin)
Prolonged duration of action (due to intermediate-acting insulin)
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16
Q

Which insulin types are prandial?

A

rapid and short acting

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17
Q

Which insulin types are basal?

A

intermediate and long-acting

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18
Q

Discuss the chain of reactions that is initiated after binding of insulin to its receptor.

A
  • Insulin-receptor complex enters the cell, where the insulin is destroyed by lysosomal enzymes.
  • The internalisation of the insulin-receptor complex underlies the down regulation of receptors that is
    produced by high levels of insulin.
  • The binding of insulin to the receptors
    activates the tyrosine kinase activity of the β-subunit and initiates a complex chain of reactions that lead to the effects of insulin.
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19
Q

What is the main form of treatment for type 1 diabetes?(and why?)

A

insulin therapy: Insulin is administered because there is no beta-cell function

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20
Q

What are the treatment options for type 2 diabetes? (and why)

A 
Diet, exercise and oral antidiabetics or
Insulin injections (if no response to above): There is some beta-cell function or Insulin resistance, so the main aim is to increase insulin secretion and sensitivity and increase glucose loss.
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21
Q

List the 7 oral antidiabetics

A
  • Biguanides
  • Sulfonylureas
  • Thiazolidinediones
  • Dipeptidyl peptidase 4 (DPP-4) inhibitors
  • Glucagon like peptide 1 (GLP-1) receptor agonists
  • Sodium-glucose co-transporter 2 (SGLT2) inhibitors
  • Alpha-glucosidase inhibitors
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22
Q

Name a Biguanide

A

Metformin

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23
Q

Which 3 organs/tissues do Biguanides effect?

A

intestine, liver, skeletal muscle

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24
Q

What effect do Biguanides have on the intestines?

A

decreases glucose absorption

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25
Q

What effect do Biguanides have on the liver?

A

Decreases gluconeogenesis
Increases fatty acid oxidation
Increases lactate production

26
Q

What effect do Biguanides have on skeletal muscle?

A

Decreases glucose uptake and utilisation

27
Q

What is the main adverse effect of Biguanides?

A

GIT disturbances (diarrhoea, nausea, anorexia)

28
Q

Name 3 Sulfonylureas

A

Gliclazide
Glimepiride
Glibenclamide

29
Q

What is the mechanism of action of Sulfonylureas? (3)

A

Stimulate secretion of insulin by β-cells, decrease serum glucagon levels, increase affinity of insulin to receptors for the hormone

30
Q

What do Sulfonylureas need to function?

A

functioning β-cells

31
Q

What is the main adverse effect of Sulfonylureas?

A

hypoglycaemia

32
Q

Name a Thiazolidinedione

A

Pioglitazone (it is the only one available as the rest have been withdrawn due to adverse effects)

33
Q

What is the mechanism of action of Thiazolidinediones? (3)

A
  • Increase sensitivity to insulin (decrease insulin resistance)
  • Selective agonist (PPAR-gamma)
  • Increase transcription of insulin-sensitive genes
34
Q

What do Thiazolidinediones need to function?

A

circulating insulin

35
Q

What is the main adverse effect of Thiazolidinedione?

A

fluid retention

heart failure (reason why most drugs were withdrawn)

36
Q

Name 3 DPP-4 inhibitors

A

Sitagliptin
Vildagliptin
Saxagliptin

37
Q

What is the mechanism of action of DPP-4 inhibitors?

A

Inhibits DPP-4 enzymes (inactivates incretins) in order to prevent a decrease in incretins

38
Q

What are the incretins and what do they do?

A

GLP-1, GIP: Promotes insulin release and inhibits glucagon secretion

39
Q

What is the main adverse effect of DPP-4 inhibitors?

A

GIT disturbances

40
Q

Name 2 GLP-1 receptor agonists

A

Exenatide

Liraglutide

41
Q

What is the mechanism of action of GLP-1 receptor agonists?

A
  • Increases the secretion of GLP-1 from pancreatic beta cells
  • Retards gastric emptying
  • Suppresses glucagon secretion
42
Q

What do GLP-1 receptor agonists need to function?

A

Must be administered subcutaneously, and require beta-cell functioning

43
Q

What is the main adverse effect of GLP-1 receptor agonists?

A

GIT disturbances

44
Q

Name 3 SGLT2 inhibitors

A

Dapagliflozin
Empagliflozin
Canagliflozin

45
Q

What is the mechanism of action of SGLT2-inhibitors?

A

suppress SGLT2 action and increase urinary glucose excretion

46
Q

What is the function of SGLT2?

A

Responsible for reabsorption of glucose in renal distal tubules

47
Q

Wha is the main adverse effect of SGLT2-inhibitors?

A

UTI/Fungal genital infections

48
Q

Name an alpha-glucosidase inhibitor

A

Acarbose

49
Q

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

A

Inhibits intestinal alpha-glucosidase, which delays the digestion of starch and sucrose and decreases absorption, which leads to a decreased post- prandial plasma glucose.

50
Q

What is the main adverse effect of alpha-glucosidase inhibitors?

A

GIT disturbances

51
Q

What are the main uses of glucagon in pharm (not as a hormone)? (5)

A 
hypoglycaemia
beta-blocker
calcium channel blocker
tricyclic antidepressant overdose
relaxes the GIT for radiographic examinations
52
Q

What is the mechanism of action of glucagon? (5 steps)

A
  1. One signal molecule binds to G-protein linked receptor and activates the G-protein
  2. G-protein turns on adenylyl cyclase (amplifier enzyme)
  3. Andenylyl cyclase turns ATP into cyclic AMP
  4. cAMP activates protein kinase A
  5. Protein kinase A phosphorylates other proteins which leads to a cellular response
53
Q

What is the mechanism of action of corticosteroids?

A

Involved in the regulation of genes that in
turn induce specific mRNA synthesis which leads to the synthesis of specific proteins. They occupy a cytosolic receptor which after activation in the nucleus
of the cell, acts on DNA transcription.

54
Q

What is the main glucocorticoid?

A

cortisol

55
Q

Name 2 short-acting glucocorticoids

A

Hydrocortisone

Cortisone

56
Q

Name 3 intermediate-acting glucocorticoids

A

Prednisolone
Prednisone
Methylprednisolone

57
Q

Name 2 long-acting glucocorticoids

A

Dexamethasone

Betamethasone

58
Q

Name a mineralocorticoid as a steroid drug

A

fludrocortisone

general mineralocorticoid (steriod)= aldosterone

59
Q

What are the 2 groups of corticosteroids?

A

glucocorticoids and mineralocorticoid

60
Q

What is the main clinical use of corticosteroids? (5)

A
  • Suppression of the immune system by organ transplants.
  • Anti-inflammatory properties
  • Treatment of allergic symptoms and signs such as eczema and asthma.
  • In anaphylactic shock.
  • Replacement therapy in cases of adrenal cortex insufficiency.
61
Q

Name 6 inhaled corticosteroids

A 
Beclomethasone
Budesonide
Ciclesonide
Fluticasone
Mometasone
Triamcinalone
62
Q

What are inhaled corticosteroids used for?

A

Bronchospasm
Seasonal rhinitis
Perrenial rhinitis

(Rhinitis is a condition that typically involves nasal obstruction or congestion, runny nose or post-nasal drip, itchy nose, and/or sneezing)

Principles of Therapy (10 decks)

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