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
What drug may carbapenams reduce efficacy of
Valproate
26
Name 3 quinolones
Ciprofloxacin Levofloxacin Moxifloxacin
27
What is the spectrum of activity of quinolones
Broad spectrum
28
Which organism is ciprofloxacin shown to have good activity against
Pseudomonas aeurginosa
29
What is the MOA of quinolones
Inhibit bacterial DNA synthesis (Bacteriacidal)
30
What is a problem with quinolones
Bacteria develop resistance quickly
31
Give 5 side effects of quinolones
1. GI upset - diarrhoea, nausea 2. Tendon inflammation and rupture 3. Neurological effects - seizures and psychosis 4. Hypersensitivity reactions 5. Prolong QT
32
Which quinolone is worse for prolonging QT interval
Mexofloxacin
33
What antibiotics are most associated with C.difficle infection
1. Cephalosporins | 2. Ciprofloxacin
34
What are three relative contraindications for quinolones
1. Children - can cause arthropathy 2. Epilepsy - risk seizures 3. QT prolongation
35
What reduces absorption of quinolones
Calcium | Antacids
36
What is the effect of ciprofloxacin in CYP450
Inhibits it
37
What drug does cirpfloxacin increase toxicity of
Theophylline
38
When quinolones are prescribed with what drug is there an increased risk of tendon-rupture
Prednisolone
39
When quinolones are prescribed with what drug is there an increased risk of seizures
NSAIDs
40
What drugs should quinolones not be prescribed with
Other drugs that prolong QT interval
41
Name 3 corticosteroids
Dexamethasone Hydrocortisone Prednisolone
42
What is the MOA of corticosteroids
- 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
What are the immune side effects of corticosteroids
Increase risk and severity of infection
44
What are the 6 metabolic side effects of corticosteroids
- Proximal muscle weakness (due to breakdown) - Skin thinning (striae) - Easy bruising - Diabetes - Osteoporosis - Gastritis
45
What mood changes can corticosteroids cause
Insomnia Confusion Psychosis
46
What side effects can occur due to the mineralocorticoid action of corticosteroids
- HTN - hypokalaemia - Oedema
47
What can happen if corticosteroids are stopped suddenly and why
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
What are symptoms of chronic glucocorticoid deficiency
Lethargy Weight loss Arthalgia
49
In which two groups of people should corticosteroids be produced with caution
Children - may suppress growth | Immunocompromised
50
When used with which drug do corticosteroids increase risk of peptic ulcers and GI bleeds
NSAIDs
51
When used with which drugs do glucocorticoids increase risk of hypokalaemia
B2-agonist Thiazide diuretic Loop diuretics Theophylline
52
What drugs reduce the efficacy of corticosteroids
CYP450 Inducers
53
How do corticosteroids interact with vaccines
Corticosteroids reduce the efficacy of vaccines
54
What time of day should once daily corticosteroids be taken and why
Morning - to mimmic circadian rhythm and prevent insomnia
55
What monitoring may be ordered if someone is on long-term steroids
HbA1c - check for diabetes | DEXA - check for osteoporosis
56
What are 3 indications of azathioprine
- IBD - disease-modifying treatment in RA - given to individuals following organ-transplantation
57
What type of drug is azathioprine
pro-drug
58
What is a pro-drug
it is not metabolically active on it's own but is converted to a metabolically active substance
59
What is the main metabolite of azathioprine
6-metacaptopurine
60
What is the mechanism of action of azathioprine
it inhibits the synthesis of purines. In particular guanine and adenosine - thereby inhibiting RNA formation.
61
What does the metabolism of azathioprine depend on
Enzyme thiopurine methyltransferase (TPMT)
62
What needs to be checked before giving azathioprine
Individuals TMPT levels
63
What is the most serious risk associated with azathioprine
Bone marrow suppression
64
What is a common side effect of azathioprine and how is this managed
Nausea: divide the daily dose
65
What are 3 other risk factors of azathioprine
- Veno-occlusive disease - Increased risk lymphoma - Hepatotoxicity
66
What is an absolute contraindication to prescribing azathioprine
absent TPMT
67
In what 2 conditions should dose of azathioprine be reduced
1. Renal impairment | 2. Hepatic impairment
68
Explain relationship between azathioprine and pregnancy
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
When prescribed with which drugs does azathioprine increase risk of infection
Other immunosuppressants eg. corticosteroids
70
what drugs should azathioprine not be prescribed with
Allopurinol. = Xanthine oxidase inhibitors as it reduces metabolism of azathioprine increasing risk of infection
71
with which drugs is the risk of azathioprine causing leucopenia increased
Other myelosupressants such as trimethoprim
72
What drug does azathioprine reduce efficacy of
Warfarin
73
What monitoring is offered to patients on azathioprine
FBC is monitored weekly for the first 4W and then 3-monthly after that.
74
Name 2 aminosalicylates
Sulfasalazine | Mesalazine
75
What are the 2 indications for for aminosalicylates
- IBD (mesalazine) | - RA (sulfasalazine)
76
What is the MOA of aminosalicylates
the active ingratiate is 5-aminosalicylate which has anti-inflammatory and immunosuppressive effects
77
What are the two most common side effects of aminosalicylates
Headache GI disturbance: nausea and dyspepsia
78
What are the 3 serious side effects of aminosalicylates
Thrombocytopenia Leucopenia Renal impairment
79
What can aminocalicylates cause in men
Oligospermia
80
Which individuals should NOT take aminosalicylates and why
Those with aspirin hypersensitivity. As these drugs are salicylates
81
What drugs may mesalazine interact with and why
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
What should be monitored in patients on mesalazine
Renal Function
83
What should be monitored in patients on sulfasalazine
FBC | LFTs
84
Name two tetracyclines
- Doxycycline | - Limecycline
85
What is the spectrum of activity of tetracyclines
Broad-Spectrum
86
What is the MOA of tetracyclines
Inhibits protein synthesis. | Binds to 30s RNA subunit. Inhibits tRNA binding mRNA and therefore is bacteriostatic
87
What is an advantage of tetracyclines
- Low probability of C.difficle | - Do not have a B-lactam ring and therefore low-risk of cross-reactivity in penicillin allergy.
88
What are 5 tetracycline specific SEs
1. Photosensitivity 2. Oeseophageal irritation - ulceration, dysphagia 3. Discolouration tooth enamel 4. Intracranial HTN 5. Hepatotoxicity
89
What is the main problem with tetracyclines
bind to tooth and bone during foetal development, infancy and early-childhood
90
What are 3 absolute CIs to tetracycline-use
- Children under 12 - Pregnant women - Breastfeeding
91
What is a relative contraindication to tetracycline use and why
Renal impairment. Anti-anabolic effects of tetracyclines can increase urea
92
What 3 drugs should tetracyclines not be given within 3h of and why
Calcium Antacids Iron = as tetracyclines binds to divalent cations which may reduce it's absorption
93
What drug do tetracyclines enhance the effect of and how
Warfarin - due to killing vitamin K producing bacteria
94
What are two anti motility drugs
Loperamide | Codeine phosphate
95
What is loperamide used for
Used to control diarrhoea in IBS
96
What is the mechanism of loperamide
- 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
What are the main side effects of loperamide
- Abdominal cramps - Flatulence - Constipation
98
In which conditions should should loperamide not be given and why
- 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).