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Pharmacology > GI Drugs > Flashcards

GI Drugs Flashcards

1
Q

What are 3 indications for PPIs

A
  1. Eradication H.Pylori
  2. Stomach Ulcers
  3. GORD
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2
Q

Explain mechanism if PPIs

A

Inhibit H+-K+ ATPase reducing gastric acid secretion

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3
Q

What are two common side effects of PPIs

A

Headache

GI disturbance

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4
Q

What infection may PPIs increase the risk of and why

A

PPIs increase pH - hence may increase c.difficile infection

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5
Q

What can prolonged treatment with PPIs result in

A

Hypomagnesaemia

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6
Q

What can hypomagnesaemia lead to

A

Tetany

Ventricular arythmias

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7
Q

What is a relative contraindication of PPIs and why

A

Osteoporosis - as PPIs shown to increase risk of fractures if used for long-time

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8
Q

What drug can omeprazole reduce the effectiveness of

A

Clopidogrel - due to decreasing its activation by CYP450

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9
Q

If an individual is on clopidogrel and needs a PPI what should they be prescribed

A

Lansoprazole

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10
Q

What time of day are PPIs best taken

A

Morning

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11
Q

If long-term use of PPI what should be checked at one-year

A

Serum Magnesium

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12
Q

Explain mechanism of H2 receptor antagonists and how it is different from PPIs

A

H-K+ ATPase in gastric pareital cells is stimulated by histamine from paracrine release. H2 receptor antagonists prevent this. However, mechanism can still be stimulated by other mechanisms.

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13
Q

What are 3 side-effects of H2 receptor antagonists

A

Dizziness
Headache
Diarrhoea

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14
Q

In which patients should the dose of ranitidine be reduced

A

Renal impairment

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15
Q

What is the spectrum of activity of cephalosporins

A

broad-spectrum

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16
Q

What activity due increasing generations of cephalosporins have

A

gram-negative activity including pseudomonas aeurginosa

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17
Q

What is the MOA of cephalosporins and carbapenams

A

B lactam ring.
Inhibit cross-linking of peptidoglycan and cell wall synthesis of bacteria - enabling water to enter via osmosis and lysis

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18
Q

What is a side effect of cephalosporins and carbapenams

A

GI disturbance, can cause C-difficle

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19
Q

Why should cephalosporins + carbapenams not be given to penicillin allergic patients

A

Due to similar structure, cross-reactivity can occur

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20
Q

What is the risk of prescribing carbapenam in high-doses or to renal impaired patients

A

Lead to neurological toxicity and seizures

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21
Q

What are 3 relative contraindications to cephalosporins + carbapenams

A
  1. Risk of c.difficile (cephalosporins)
  2. epilepsy (carbapenams)
  3. renal impairment - reduce dose
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22
Q

What is an absolute CI to cephalosporins + carbapenams

A

Anaphylactic response to penicillin

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23
Q

What drug can cephalosporins + carbapenams increase the effect of and how

A

Warfarin - due to reducing gut flora that process vitamin K

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24
Q

What drug may cephalosporins increase nephrotoxicity of

A

Aminoglycosides

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25
Q

What drug may carbapenams reduce efficacy of

A

Valproate

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26
Q

Name 3 quinolones

A

Ciprofloxacin
Levofloxacin
Moxifloxacin

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27
Q

What is the spectrum of activity of quinolones

A

Broad spectrum

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28
Q

Which organism is ciprofloxacin shown to have good activity against

A

Pseudomonas aeurginosa

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29
Q

What is the MOA of quinolones

A

Inhibit bacterial DNA synthesis (Bacteriacidal)

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30
Q

What is a problem with quinolones

A

Bacteria develop resistance quickly

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31
Q

Give 5 side effects of quinolones

A
  1. GI upset - diarrhoea, nausea
  2. Tendon inflammation and rupture
  3. Neurological effects - seizures and psychosis
  4. Hypersensitivity reactions
  5. Prolong QT
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32
Q

Which quinolone is worse for prolonging QT interval

A

Mexofloxacin

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33
Q

What antibiotics are most associated with C.difficle infection

A
  1. Cephalosporins

2. Ciprofloxacin

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34
Q

What are three relative contraindications for quinolones

A
  1. Children - can cause arthropathy
  2. Epilepsy - risk seizures
  3. QT prolongation
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35
Q

What reduces absorption of quinolones

A

Calcium

Antacids

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36
Q

What is the effect of ciprofloxacin in CYP450

A

Inhibits it

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37
Q

What drug does cirpfloxacin increase toxicity of

A

Theophylline

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38
Q

When quinolones are prescribed with what drug is there an increased risk of tendon-rupture

A

Prednisolone

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39
Q

When quinolones are prescribed with what drug is there an increased risk of seizures

A

NSAIDs

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40
Q

What drugs should quinolones not be prescribed with

A

Other drugs that prolong QT interval

41
Q

Name 3 corticosteroids

A

Dexamethasone
Hydrocortisone
Prednisolone

42
Q

What is the MOA of corticosteroids

A
  • Increase expression of anti-inflammatory genes. Reduce expression of pro-inflammatory genes
  • Bind to and directly inhibit eosinophils and monocytes
  • Also exhibit mineralocorticoid effects = increase retention of sodium and excretion of K+ - also leading to oedema
43
Q

What are the immune side effects of corticosteroids

A

Increase risk and severity of infection

44
Q

What are the 6 metabolic side effects of corticosteroids

A
  • Proximal muscle weakness (due to breakdown)
  • Skin thinning (striae)
  • Easy bruising
  • Diabetes
  • Osteoporosis
  • Gastritis
45
Q

What mood changes can corticosteroids cause

A

Insomnia
Confusion
Psychosis

46
Q

What side effects can occur due to the mineralocorticoid action of corticosteroids

A
  • HTN
  • hypokalaemia
  • Oedema
47
Q

What can happen if corticosteroids are stopped suddenly and why

A

Precipitates an addisonian crisis.
Exogenous corticosteroids reduces ACTH secretion - this leads to adrenal-cortical atrophy. Reducing cortisol release. Meaning if stopped suddenly, there will be a deficiency of cortisol.

48
Q

What are symptoms of chronic glucocorticoid deficiency

A

Lethargy
Weight loss
Arthalgia

49
Q

In which two groups of people should corticosteroids be produced with caution

A

Children - may suppress growth

Immunocompromised

50
Q

When used with which drug do corticosteroids increase risk of peptic ulcers and GI bleeds

A

NSAIDs

51
Q

When used with which drugs do glucocorticoids increase risk of hypokalaemia

A

B2-agonist
Thiazide diuretic
Loop diuretics
Theophylline

52
Q

What drugs reduce the efficacy of corticosteroids

A

CYP450 Inducers

53
Q

How do corticosteroids interact with vaccines

A

Corticosteroids reduce the efficacy of vaccines

54
Q

What time of day should once daily corticosteroids be taken and why

A

Morning - to mimmic circadian rhythm and prevent insomnia

55
Q

What monitoring may be ordered if someone is on long-term steroids

A

HbA1c - check for diabetes

DEXA - check for osteoporosis

56
Q

What are 3 indications of azathioprine

A
  • IBD
  • disease-modifying treatment in RA
  • given to individuals following organ-transplantation
57
Q

What type of drug is azathioprine

A

pro-drug

58
Q

What is a pro-drug

A

it is not metabolically active on it’s own but is converted to a metabolically active substance

59
Q

What is the main metabolite of azathioprine

A

6-metacaptopurine

60
Q

What is the mechanism of action of azathioprine

A

it inhibits the synthesis of purines. In particular guanine and adenosine - thereby inhibiting RNA formation.

61
Q

What does the metabolism of azathioprine depend on

A

Enzyme thiopurine methyltransferase (TPMT)

62
Q

What needs to be checked before giving azathioprine

A

Individuals TMPT levels

63
Q

What is the most serious risk associated with azathioprine

A

Bone marrow suppression

64
Q

What is a common side effect of azathioprine and how is this managed

A

Nausea: divide the daily dose

65
Q

What are 3 other risk factors of azathioprine

A
  • Veno-occlusive disease
  • Increased risk lymphoma
  • Hepatotoxicity
66
Q

What is an absolute contraindication to prescribing azathioprine

A

absent TPMT

67
Q

In what 2 conditions should dose of azathioprine be reduced

A
  1. Renal impairment

2. Hepatic impairment

68
Q

Explain relationship between azathioprine and pregnancy

A

Shown to be teratogenic in animal studies, unsure about humans.

Do not start in a pregnant women.
If a women is on azathioprine and gets pregnant if benefit outweighs risk, it may be continued

69
Q

When prescribed with which drugs does azathioprine increase risk of infection

A

Other immunosuppressants eg. corticosteroids

70
Q

what drugs should azathioprine not be prescribed with

A

Allopurinol. = Xanthine oxidase inhibitors as it reduces metabolism of azathioprine increasing risk of infection

71
Q

with which drugs is the risk of azathioprine causing leucopenia increased

A

Other myelosupressants such as trimethoprim

72
Q

What drug does azathioprine reduce efficacy of

A

Warfarin

73
Q

What monitoring is offered to patients on azathioprine

A

FBC is monitored weekly for the first 4W and then 3-monthly after that.

74
Q

Name 2 aminosalicylates

A

Sulfasalazine

Mesalazine

75
Q

What are the 2 indications for for aminosalicylates

A
  • IBD (mesalazine)

- RA (sulfasalazine)

76
Q

What is the MOA of aminosalicylates

A

the active ingratiate is 5-aminosalicylate which has anti-inflammatory and immunosuppressive effects

77
Q

What are the two most common side effects of aminosalicylates

A

Headache

GI disturbance: nausea and dyspepsia

78
Q

What are the 3 serious side effects of aminosalicylates

A

Thrombocytopenia
Leucopenia
Renal impairment

79
Q

What can aminocalicylates cause in men

A

Oligospermia

80
Q

Which individuals should NOT take aminosalicylates and why

A

Those with aspirin hypersensitivity. As these drugs are salicylates

81
Q

What drugs may mesalazine interact with and why

A

Mesalazine has a pH dependent coating for release. Therefore its absorption can be impacted by drugs that change pH such as PPIs and lactulose

82
Q

What should be monitored in patients on mesalazine

A

Renal Function

83
Q

What should be monitored in patients on sulfasalazine

A

FBC

LFTs

84
Q

Name two tetracyclines

A
  • Doxycycline

- Limecycline

85
Q

What is the spectrum of activity of tetracyclines

A

Broad-Spectrum

86
Q

What is the MOA of tetracyclines

A

Inhibits protein synthesis.

Binds to 30s RNA subunit. Inhibits tRNA binding mRNA and therefore is bacteriostatic

87
Q

What is an advantage of tetracyclines

A
  • Low probability of C.difficle

- Do not have a B-lactam ring and therefore low-risk of cross-reactivity in penicillin allergy.

88
Q

What are 5 tetracycline specific SEs

A
  1. Photosensitivity
  2. Oeseophageal irritation - ulceration, dysphagia
  3. Discolouration tooth enamel
  4. Intracranial HTN
  5. Hepatotoxicity
89
Q

What is the main problem with tetracyclines

A

bind to tooth and bone during foetal development, infancy and early-childhood

90
Q

What are 3 absolute CIs to tetracycline-use

A
  • Children under 12
  • Pregnant women
  • Breastfeeding
91
Q

What is a relative contraindication to tetracycline use and why

A

Renal impairment. Anti-anabolic effects of tetracyclines can increase urea

92
Q

What 3 drugs should tetracyclines not be given within 3h of and why

A

Calcium
Antacids
Iron
= as tetracyclines binds to divalent cations which may reduce it’s absorption

93
Q

What drug do tetracyclines enhance the effect of and how

A

Warfarin - due to killing vitamin K producing bacteria

94
Q

What are two anti motility drugs

A

Loperamide

Codeine phosphate

95
Q

What is loperamide used for

A

Used to control diarrhoea in IBS

96
Q

What is the mechanism of loperamide

A
  • It is a u-opioid receptor agonist that cannot cross into CNS
  • It increases non-peristaltic bowel contractions. But decreases peristaltic contractions.
  • This increases colonic transit time - that enables more time for water to be absorbed
97
Q

What are the main side effects of loperamide

A
  • Abdominal cramps
  • Flatulence
  • Constipation
98
Q

In which conditions should should loperamide not be given and why

A
  • UC and C.Difficle = as decreasing transit increases risk of toxic megacolon
  • Dysentry. As could be caused by EHEC. In EHEC infection, anti-motility agents have been shown to increase risk of haemolytic-uraemia syndrome (HUS).

Pharmacology (12 decks)

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