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Principles of Therapy > Theme 8 - Endocrine Pharmacology > Flashcards

Theme 8 - Endocrine Pharmacology Flashcards

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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
What effect do Biguanides have on the liver?
Decreases gluconeogenesis Increases fatty acid oxidation Increases lactate production
26
What effect do Biguanides have on skeletal muscle?
Decreases glucose uptake and utilisation
27
What is the main adverse effect of Biguanides?
GIT disturbances (diarrhoea, nausea, anorexia)
28
Name 3 Sulfonylureas
Gliclazide Glimepiride Glibenclamide
29
What is the mechanism of action of Sulfonylureas? (3)
Stimulate secretion of insulin by β-cells, decrease serum glucagon levels, increase affinity of insulin to receptors for the hormone
30
What do Sulfonylureas need to function?
functioning β-cells
31
What is the main adverse effect of Sulfonylureas?
hypoglycaemia
32
Name a Thiazolidinedione
Pioglitazone (it is the only one available as the rest have been withdrawn due to adverse effects)
33
What is the mechanism of action of Thiazolidinediones? (3)
- Increase sensitivity to insulin (decrease insulin resistance) - Selective agonist (PPAR-gamma) - Increase transcription of insulin-sensitive genes
34
What do Thiazolidinediones need to function?
circulating insulin
35
What is the main adverse effect of Thiazolidinedione?
fluid retention heart failure (reason why most drugs were withdrawn)
36
Name 3 DPP-4 inhibitors
Sitagliptin Vildagliptin Saxagliptin
37
What is the mechanism of action of DPP-4 inhibitors?
Inhibits DPP-4 enzymes (inactivates incretins) in order to prevent a decrease in incretins
38
What are the incretins and what do they do?
GLP-1, GIP: Promotes insulin release and inhibits glucagon secretion
39
What is the main adverse effect of DPP-4 inhibitors?
GIT disturbances
40
Name 2 GLP-1 receptor agonists
Exenatide | Liraglutide
41
What is the mechanism of action of GLP-1 receptor agonists?
- Increases the secretion of GLP-1 from pancreatic beta cells - Retards gastric emptying - Suppresses glucagon secretion
42
What do GLP-1 receptor agonists need to function?
Must be administered subcutaneously, and require beta-cell functioning
43
What is the main adverse effect of GLP-1 receptor agonists?
GIT disturbances
44
Name 3 SGLT2 inhibitors
Dapagliflozin Empagliflozin Canagliflozin
45
What is the mechanism of action of SGLT2-inhibitors?
suppress SGLT2 action and increase urinary glucose excretion
46
What is the function of SGLT2?
Responsible for reabsorption of glucose in renal distal tubules
47
Wha is the main adverse effect of SGLT2-inhibitors?
UTI/Fungal genital infections
48
Name an alpha-glucosidase inhibitor
Acarbose
49
What is the mechanism of action of alpha-glucosidase inhibitors?
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
What is the main adverse effect of alpha-glucosidase inhibitors?
GIT disturbances
51
What are the main uses of glucagon in pharm (not as a hormone)? (5)
``` hypoglycaemia beta-blocker calcium channel blocker tricyclic antidepressant overdose relaxes the GIT for radiographic examinations ```
52
What is the mechanism of action of glucagon? (5 steps)
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
What is the mechanism of action of corticosteroids?
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
What is the main glucocorticoid?
cortisol
55
Name 2 short-acting glucocorticoids
Hydrocortisone | Cortisone
56
Name 3 intermediate-acting glucocorticoids
Prednisolone Prednisone Methylprednisolone
57
Name 2 long-acting glucocorticoids
Dexamethasone | Betamethasone
58
Name a mineralocorticoid as a steroid drug
fludrocortisone general mineralocorticoid (steriod)= aldosterone
59
What are the 2 groups of corticosteroids?
glucocorticoids and mineralocorticoid
60
What is the main clinical use of corticosteroids? (5)
- 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
Name 6 inhaled corticosteroids
``` Beclomethasone Budesonide Ciclesonide Fluticasone Mometasone Triamcinalone ```
62
What are inhaled corticosteroids used for?
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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