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Primary Pharmacology > Endocrine Pharmacology > Flashcards

Endocrine Pharmacology Flashcards

1
Q

Structure of insulin receptor
Mechanism of action

A

2 alpha and 2 beta subunits linked by disulphide bridges to form cylinder
Alpha subunits extracellular forming insulin binding site
Beta subunits span membrane and have intracellular tyrosine kinase activity
Alpha subunit inhibits tk activity until bound to insulin
Tk acts on insulin receptor substrate 1 triggering a chain reaction
Binding of insulin to alpha also causes formation of transmembrane tunnel allowing glucose entry to cell

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2
Q

How does an insulin receptor stop functioning

A

Internalised with recycling of receptor and insulin degraded in lysosomes

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3
Q

Amount of energy in 1L 5% dextrose

A

840kj/L

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4
Q

Where is glucagon formed in physiology

A

A cells in the pancreas and in upper gi tract

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5
Q

Half life of iV insulin

A

5 mins

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6
Q

Onset, peak and duration of short acting sc insulin in hrs

A

0.5-1, 2-4, 8

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7
Q

Onset, peak and duration of intermediate acting sc insulin in hrs

A

1-2, 4-12, 12-24

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8
Q

Onset, peak and duration of long acting sc insulin in hrs

A

2-4, 24-40, 36

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9
Q

How is the duration of action of insulin increased

A

By addition of zinc or protamine forming complexes with intermediate duration or both forming long duration

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10
Q

How many aa differences do bovine and porcine insulin have vs human

A

Bovine 3
Porcine 1

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11
Q

What is the disadvantage of porcine or bovine insulin over human

A

Non native sequences may be antigenic causing insulin resistance and immunoreactivity

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12
Q

How is human insulin synthesised

A

Bacteria
Enzymatic modification of porcine

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13
Q

Examples of sulphonylureas
Mechanism

A

Gliclazide, glipizide, tolbutamide
Augment endogenous insulin secretion from existing B cells - bind to receptors and increase sensitivity of the cells to glucose. Decreased K permeability so depolarisation, influx of ca and secretion of insulin.

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14
Q

Metabolism of sulphonylureas

A

Hepatic forming active metabolites excreted in urine

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15
Q

Effect of sulphonylureas in pregnancy

A

Cross placenta causing hypoglycaemia in newborn

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16
Q

Proteins binding of sulphonylureas

A

Highly protein bound thus displaced by eg aspirin

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17
Q

Example of biguanide
Mechanism

A

Metformin
Decrease hepatic gluconeogenesis
Increase insulin mediated peripheral glucose uptake
Do this by increasing sensitive of target tissues to insulin

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18
Q

Metaboism and protien binding of metformin

A

Excreted unchanged in urine
Not protine bound

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19
Q

Examples of thiazolidinediones
Mechanism

A

Piaglitazone, rosiglitazone
Sensitise target tissue to insulin
Mainly work in adipose tissues

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20
Q

Examples of meglitinied analogues
How do they work

A

Nateglinide
Inhibit atp dependant k channels in B cells stimulating insulin release

21
Q

Examples of sglt2 inhibitors

A

Dapagliflozin, empagliflozin
Inhibit sglt2 stopping glucose reabsorption in urine

22
Q

Side effects of sglt2 inhibitors

A

Diabetic ketoacidosis
Urine infections
Dehydration

23
Q

Example of a dpp4 inhibitor
How do they work

A

Sitagliptin
Block dpp4 resulting in more incretin which increases insulin only when it is needed and reduce the amount of glucose from liver when it is not needed

24
Q

Example of glp1 analogue
Mechanism

A

Exanatide
Mimic incretin producing more insulin only when needed and reducing hepatic glucose production when not needed

25
Q

Perioperative management of non insulin diabetic meds

A

Meglitinide - omit on day when fasting (hypo risk)
Sluphonylureas - omit mane, if pm surgery omit pm dose too (hypo risk)
Sglt 2 inhibitors - omit on day (DKA risk)
All others inc metformin take as normal

26
Q

What treatment should be used for a hypothyroid coma (thyroid replacement) why

A

t3 - faster onset than t4

27
Q

How does carbimazole work
How long to take effect
Big side effect

A

Blocks organification of iodine
3-4 weeks
Agranulocytosis

28
Q

Which steroid treatment is naturally occurring

A

Hydrocortisone (cortisol)

29
Q

Disadvantage of hydrocortisone over prednisolone

A

Higher mineralocorticoid effect so more fluid retention

30
Q

Prednisolone glucocorticoid and mineralocorticoid effect vs hydrocortisone

A

G 4
M 0.25

31
Q

Dexamethasone gluco and mineralocorticoid effect vs hydrocortisone

A

25
0

32
Q

Fludrocortisone gluco and mineralocorticoid effect vs hydrocortisone

A

10
300

33
Q

How are glucocorticoids transported in blood

A

Corticosteroid binding globulin
Low capacity so easily saturated when large volumes of steroids used

34
Q

Structure of oxytocin
What is the name of the pharmacological preparation, why

A

Octopeptide
Syntocinon as it is synthetic

35
Q

Why does oxytocin cause uterine contraction

A

Binds causing increased k permeability making cell more excitable

36
Q

How does uterine sensitivity to oxytocin change over pregnancy

A

Minimal at start to maximal at term

37
Q

Action of ergometine

A

Stimulates 5Ht receptors causing uterine contraction and slight vascular smooth muscle contraction

38
Q

Side effects of ergometrine

A

Hypertension
Vomiting - stimulates d2 receptors
Headache and blurred vision lasting several days

39
Q

Metabolism ergometrin

A

Liver excreted into bile

40
Q

What is carboprost
Side effects

A

A prostaglandin
Comiting, Bronchospasm, flushing, diarrhoea

41
Q

Dose of ergometrine and carboprost

A

Ergometrine 250-500mcg
Carboprost 250mcg

42
Q

Structure of vasopressin

A

Octopeptide

43
Q

Half life of vasopressin

A

10minutes

44
Q

Clinical effects of vasopressin and receptor

A

V1a - vasoconstriction
V2 - water reabsorption in collecting duct,

increased hepatic glycogenolysis, encourages platelet aggregation

V1b - triggers acth-rh release

45
Q

Use of despmopressin
Comparison to vasopressin

A

Dx and Tx of diabetes insipidus
Strong antiduretic activity (12x vasopressin) but fraction of vasoconstriction activity

46
Q

What is terlipressin
Route of administration

A

Prodrug for vaspressin
IV

47
Q

What is demeclocycline

A

A vasopressin antagonist used in inappropriate vasopressin secretion

48
Q

Examples of vasopressin receptor antagonists
Uses

A

Conivaptan, lixivaptan, tolvaptan
Use in heart failure and hyponatraemia where water loss is desired

49
Q

Duration of action hydrocortisone;

A

8 hrs

Primary Pharmacology (18 decks)

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