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Flashcards in Pharmacology Deck (94)
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1
Q

What are exocrine glands?

A

Have ducts

2
Q

What do the ducts of endocrine glands secrete?

A

Hormones

3
Q

Which endocrine glands creates ACTH?

A

Anterior pituitary

4
Q

What does ACTH stand for?

A

Adrenocorticotropic hormone

5
Q

Where synthesises cortisol from ACTH?

A

Adrenal cortex

6
Q

Where are the adrenal glands?

A

Superior to the kidneys

7
Q

What 3 endocrine glands are in the brain?

A

Pineal
Hypothalamus
Pituitary

8
Q

What is the differences in endocrine glands in males and females?

A

Testes in males

Ovaries (& placenta) in females.

9
Q

What is autocrine signalling?

A

When a cell secretes a hormone which is taken up and acted upon by the same cell

10
Q

What is paracine signalling?

A

When a cell secretes a hormone which is taken up by neighbouring cells

11
Q

What is endocrine signalling?

A

When a cell secretes a hormone which is taken into the blood supply and distributed to many cells around the body

12
Q

What are the 3 classes of hormones?

A

Proteins and peptides
Steroids
Tyrosine and tryptophan

13
Q

Give an example of a peptide hormone

A

Insulin

Oxytocin

14
Q

Give an example of a steroid type hormone

A

Cortisol

Testosterone

15
Q

Give an example of a tyrosine type hormone

A

Adrenaline
thyroid hormone
Melatonin

16
Q

Describe the storage of amino acids

A

Pre-synthesised stored in vesicles

17
Q

When are amino acids released?

A

released in response to stimuli by Ca2+ exocytosis

18
Q

Where are amines released into?

A

Free plasma

19
Q

Where are precursors for peptides synthesised?

A

Ribosomes on RER

20
Q

How are peptide precursors coverted to mature hormones?

A

Convertase enzymes using proteolytic steps

21
Q

What influx needs to happen for the release of peptides into the plasma?

A

Ca++ influx

22
Q

Where are steroids stored?

A

They aren’t!

Synthesised and secreted upon demand.

23
Q

What converts cholesterol to steroids?

A

pregnenolones

24
Q

Are steroids hydrophobic or hydrophillic?

A

Hydrophobic

25
Q

Are steroids in free or bound plasma?

A

Mostly bound to plasma proteins.

Remember only FREE steroids are biologically active

26
Q

What do carrier proteins do?

A

Increase amound of steroids and thyroxine transported in blood and prevent excretion by stopping filtration at the kidney

27
Q

Which carrier protein binds cortisol?

A

Cortisol binding globulin (CBG)

28
Q

What does thyroxine binding globulin bind?

A

T4 thyroxine.

some T3

29
Q

Name two general carrier proteins

A

Albumin

Transthyretin

30
Q

Why do proteins and peptides not need carrier proteins?

A

Soluble in plasma so don’t need carrier proteins for transport

31
Q

What is the feedback system re hormones?

A

Negative feedback

32
Q

Which part of the is at the top of the feedback loop ?

A

Hypothalamus

33
Q

What does the hypothalamus do?

A

Secretes corticotropin releasing hormone

34
Q

What does the release of corticotropin hormone do?

A

Stimulates the anterior pituitary to secrete ACTH

35
Q

What does the release of ACTH stimulates?

A

Adrenal cortex secretes cortisol

36
Q

What is the half life of steroids and thyroid hormones?

A

Hours to days

37
Q

What kind of receptors are the cell surface receptors?

A

G protein coupled.

Specifically Gs, Gi or Gq.

38
Q

Intracellularly, what are the different kinds of nuclear receptors?

A

Class 1, 2 and hybrid

39
Q

What interacts with the hybrid nuclear receptors?

A

thyroid hormone

40
Q

Where are class 1 receptors found?

A

Cytoplasm, bound to inhibitory heat shock proteins.

41
Q

What activates class 1 nuclear receptors?

A

Steroid hormones

42
Q

What activates class 2 nuclear receptors?

A

Lipids

43
Q

Where are class 2 nuclear receptors found?

A

In the nucleus

44
Q

Which protein activates protein kinase A?

A

cAMP

45
Q

What does protein kinase A do?

A

Phosphorylates target proteins and therefore gives effects

46
Q

What is needed for cAMP to be synthesised?

A

ATP and adenylyl cyclase

47
Q

What can stop cAMP from being formed?

A

Gi receptors, encouraged by melatonin

48
Q

What encourages formation of cAMP?

A

Gs, encouraged by adrenaline, glucagon

49
Q

What does prolactin do?

A

Produces breastmilk

50
Q

Which hormone can be described as a chronic stress hormone?

A

Cortisol

51
Q

Which is the acute stress hormone?

A

Adrenaline

52
Q

When should cortisol levels be tested?

A

9AM due to diurnal variation this is when they are highest

53
Q

What condition develops if cortisol levels are too high?

A

Cushing’s syndrome

54
Q

Which hormone uses receptor kinases?

A

Insulin

55
Q

What needs to occur for cellular effects to take place when insulin is being signalled?

A

Needs to be phosphorylated

56
Q

Which hormone is signalled via a nuclear receptor class 1?

A

Steroid hormones

57
Q

Where is the class 1 receptor in steroid signalling?

A

Either cytoplasm or nucleus

58
Q

When steroids combine with an intercellular receptor what do they produce?

A

Heat shock producing proteins

59
Q

What does the receptor steroid complex do?

A

Moves to the nucleus and forms a dimer.

60
Q

Give an example of a biguanide

A

Metformin.

Only one!

61
Q

What is the risk in using metformin in a patient with existing renal dysfunction?

A

Metformin is renally excreted so may not be excreted well if kidneys damaged and may build up and cause further damage.

62
Q

Give two examples of sulphonylureas

A

Glicazide

Glimeparide

63
Q

What effect can sulphonylureas have on weight

A

Can cause weight gain

64
Q

What class of drug does pioglitazone belong to?

A

Thiazolidinediones (also called PPAR gamma agonists)

65
Q

What affect does pioglitazone have on weight?

A

Gain weight.

66
Q

When should pioglitazone not be prescribed?

A

heart failure

bladder cancer

67
Q

What is the max dose of metformin possible?

A

1g BD

68
Q

What affect does metformin have on weight?

A

Neutral.

Possible reduction

69
Q

When can metformin cause hypoglycaemia?

A

Does not cause hypos when used as monotherapy

70
Q

Can metformin be used in pregnancy and lactation?

A

Yes

71
Q

What other conditions can benefit from metformin?

A

Gestational DM
PCOS
NAFLD

72
Q

What are common side effects of metformin?

A

Anorexia, nausea, v&d, abdo pain

73
Q

What vitamins does metformin interfere with?

A

B12 and folic acid

74
Q

When should metformin be discontinued?

A

If eGFR

75
Q

What is the mechanism of action of sulphonylureas?

A

Binds to K+ channel and speeds up its release of K, ultimately releasing insulin

76
Q

What are the adverse effects with sulphonylureas?

A

Hypoglycaemia
weight gain
Avoid in renal/liver failure

77
Q

Give two examples of sulphonylureas

A

Gliclazide

Glipazide

78
Q

Is gliclazide safe to use in pregnancy?

A

No. Causes hypoglycaemia

79
Q

What is the mechanism of action of pioglitazone?

A

Lipophilic so binds to PPARgamma in adipose easily and changed DNA to make glucose more readily absorbed

80
Q

What are the side effects of pioglitazone?

A

weight gain

Fluid retention

81
Q

How do DPP4 and incretin analogues inhibitors work?

A

Decrease the total blood glucose by decreasing glucagon from pancreatic alpha cells.

82
Q

What is extenatide an example of?

A

Incretin analogue

83
Q

How do incretin analogues work?

A

Binds to GLP1 receptor that increases [cAMP]. Increases insulin secretion and suppresses glucagon secretion.

84
Q

How is extenatide administered?

A

Subcutaneously BD

85
Q

Where does GLP-1 come from?

A

L cells

86
Q

Where does GIP come from?

A

K cells

87
Q

What are the benefits of using a GLP1 antagonists (incretins)?

A

No hypoglycaemia

Reduces appetite

88
Q

What is an example of a DPP4 inhibitor?

A

Vildagliptin, Linagliptin

89
Q

What are the benefits of using a DPP4 inhibitor?

A

No hypoglycaemia

weight neutral

90
Q

How do SGLT2 inhibitors work?

A

Block the reabsorption of glucose into the prox. tubule of kidney so more excretion of glucose

91
Q

What are the benefits of SGLT” inihibs?

A

weight loss

Little risk of hypoglycaemia

92
Q

What is an example of SGLT2?

A

Dapagliflozin

93
Q

What is the disadvantage of SGLT2 inhibs?

A

Thrush

Increase in urine infection

94
Q

What is a possible dangerous side effect of Exenatide?

A

?pancreatitis/ pancreatic cancer