B5 The pharmacological basis of therapy Flashcards

1
Q

Do antacids provide a cure?

A

no but they provide relief

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2
Q

Give examples of antacids

A

sodium bicarbonate
magnesium hydroxide
aluminium hydroxide

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3
Q

How to alginates work?

A

alginic acid combine with saliva and forms a viscous foam, this floats on the gastric contents forming a raft which protects the oesophagus during reflux

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4
Q

Why not use atropine?

A

suppresses acid production but has antimuscarinic side effects

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5
Q

What are examples of H2 receptor antagonists?

A

cimetidine
ranitidine
famotidine

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6
Q

Are H2 receptor antagonist drugs for long term or short term use and what class are the low and high doses?

A

short term
low-OTC
high-POM

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7
Q

What does maximum response equal?

A

efficacy of drug

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8
Q

What does EC50 equal?

A

concentration of agonist giving 50% of maximal response- potency

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9
Q

What are on the x & y axis of a competitive receptor antagonism graph?

A

x- log conc of agonist

y- pharmacological response

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10
Q

How to antagonists work?

A

they bind at the same site as the agonist & so reduce action of agonist by competition

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11
Q

How can completion from an antagonist be overcome?

A

increase conc of agonist

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12
Q

What is antagonist affinity a measure of?

A

how well the drug binds to a receptor

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13
Q

What is the affinity constant Ka measured in?

A

molar^-1

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14
Q

What is Kd or 1/Ka?

A

dissociation constant, is the conc at which the drug occupies half the receptor population

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15
Q

Will a high affinity drug have a high or low Kd?

A

low

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16
Q

What does pA2=?

A

-logKd

17
Q

What does high PA2 mean for affinity?

A

high affinity

18
Q

What are the benefits of H2RAs?

A

reduce gastric acid secretion

provide symptomatic relief

19
Q

What are H1 receptor antagonists?

A

antihistamines

20
Q

Why is cimetidine not chosen over ranitidine?

A

cimetidine inhibits cytochrome P450 & therefore the metabolism of other drugs, whereas ranitidine does not interact this way

21
Q

What drugs does cimetidine interact with?

A

oral anticoagulants
phenytoin
carbamazepine
tricyclic antidepressants

22
Q

What are examples of PPIs?

A

omeprazole, pantoprazole, lansoprazole

23
Q

How to PPIs work?

A

activated by acidic pH, enter body, passes to parietal cells, pKa means activated at lower pH, localised action

24
Q

What are possible ADRs of PPIs?

A

inhibit H+ secretion by > 90%, leads to achlorhydria (absence of HCl)
increase risk of campylobacter infection (food poisoning)

25
Q

What is rebound acid hyper secretion?

A

following the cessation of H2RAs or PPIs, increase in acid release, increase in dyspepsia symptoms

26
Q

How can you mange rebound acid hyper secretion?

A

with antacids

27
Q

Give an example of a prostaglandin analogue?

A

misoprostol

28
Q

How do prostaglandin analogues work?

A

agonist at PG receptor, suppress acid release and promote cytoprotection

29
Q

What can prostaglandin analogues cause?

A

uterine contraction, cause miscarriage, abortion

30
Q

How to pro kinetic drugs work?

A

cause gastric emptying, movement of gastric contents from stomach to duodenum

31
Q

What are two examples of pro kinetic drugs and how do they work?

A

domperidone- increased closure of oesophageal sphincter and one lower sphincter
metoclopramide- act locally to increase gastric motility and emptying

32
Q

What is the most effective treatment for long term cure of ulcers?

A

H.pylori eradication

33
Q

What is TRIPLE THERAPY and how does it work?

A

involves an antibiotic, 2 from either; clarithromycin, amoxicillin, metronidazole plus PPI and/ or H2 antagonist
triple therapy lasts for one week then PPI alone