Block 32 Pharm Flashcards
1
Q
Antacids and alginates examples
A
- Magnesium trisilicate
- Aluminium/magnesium mixtures (Maalox) - Alginates
2
Q
what are antacids and alginates used for?
A
dyspepsia, GORD
3
Q
Mag trisillicate mechanism?
A
-antacid
- inc pH of gastric juicr via neutrilisation
4
Q
CI of magnesium triscillicate?
A
Hypophosphataemia
5
Q
mag tricillicate interactions?
A
- amlodepine
- nifedipine
- verapamil
6
Q
mag trisillicate side effects?
A
- diarrhoea
- nephrolithiasis (long term use)
7
Q
Co-magaldrox (Maalox) mechanism?
A
- mix of mag hydroxide and al hydroxide
- neutralises acid
8
Q
Co-magaldrox indications?
A
dyspepsia
9
Q
Co-magaldrox side effects?
A
constipation and diarrhoea
10
Q
Co-magaldrox and renal impairment?
A
There is a risk of accumulation and aluminium toxicity with antacids containing aluminium salts
11
Q
alginates mechanism?
A
- reacts w gastric acid to form a raft of alginic acid gel
- raft had a neutral pH
- acts as a barrier to impede reflux
12
Q
CI of alginic acid?
A
- intestinal obstruction
- where excessive water loss likely (e.g. fever, diarrhoea, vomiting, high room temperature)
13
Q
alginates and renal impairment?
A
avoid - risk of hypernatremia
14
Q
alginic acid (gaviscon) side effects?
A
- ankle swelling
- constipation
15
Q
H2-receptor antagonists?
A
rantidine
16
Q
rantidine indications?
A
dyspepsia, GORD, peptic ulceration, prophylaxis of NSAID associated peptic ulceration
17
Q
cautions with H2 receptor antagonits like ranitidine?
A
signs and symptoms of gastric cancer can be masked
18
Q
ranitidine side effects?
A
- bone marrow depression
- nephritis
- acute pancreatitis
- dyskinesia
19
Q
ranitidine mechanism?
A
- normally after a meal, gastrin -> histamine release -> H2 activation -> acid secretopm
- ranitidine blocks H2 receptors on gastric parietal cells -> less acid produced
20
Q
PPIs?
A
- Lansoprazole
- Omeprazole
21
Q
PPIs mechanism?
A
- inhition of the H+/K+/ATPase pump
- inhibition of acid production
22
Q
PPIs and H pylori eradication?
A
- PUD associated w H pylori infection
- acid inhibition in H pylori eradication therapy raises gastric pH discouraging growth of H pylori
- PPI inhibit urease enzyme
23
Q
PPIs indications?
A
- dyspepsia
- GORD
- oesophagitis
- peptic ulceration
- prophylaxis of NSAID associated peptic ulceration
- H. pylori eradication
24
Q
cautions of PPIs?
A
- risk of fractures - high doses in the elderly
- C diff infection risk
- masking gastric cancer symptoms
- B12 abs reduced w long term use
- osteoporosis risk
25
side effects of all PPIs?
- abd pain
- constipation
- diarrhoea
- headache
- skin reactions
26
Opiate based anti-motility agents =
codeine
27
indications of codiene?
- diarrhoea
- short term pain relief
- dry cough
28
CI of codeine and all opiods?
- ARD
- comatose
- raised ICP
- risk of paralytic ileus
29
CI for codeine?
- active UC
- ab associated colitis
- children under 18
- known ultra-rapid codeine metabolisers
30
codeine interactions?
- buprenorphine
- clozapine
- naltrexone
- fluoxetine
31
side effects of codeine?
- arrhythmias
- constipation
- hallucinations
- nausea and vomiting on initiation
- urinary retention
32
Non-opiate based anti-motility agents =
loperamide
33
codeine mechanism?
- mu opiod receptors agonism
- g protein response
- hyperpolarisation of nociceptive neurons -> impaired pain transmission
34
loperamide mechanism?
- used for diarrhoea
- mu opiod agonist on the circ and longitudinal intestinal muscle
- inhibits release of ACh and prostaglandins -> reducing peristalsis -> inc intestinal transit time
35
loperamide indications?
- diarrhoea - acute and chronic
- faceal incontinence
36
loperamide CI?
- Active UC
- ab assoc colitis
- abd distension
37
loperamide interactions?
- clozapine
38
cautions of loperamide?
children under 12
39
side effects of loperamide?
- GI disorders
- headache
- nausea
40
Aminosalicylates?
- e.g. mesalazine
- IBD
41
mesalazine mechanism?
- induce and maintains remission
- inhibition of nuclear factor kappa B and blocks production of pro-inflamm cytokines
- blocks COX pathways - less leukotrienes
42
mesalazine CI?
- blood clotting abn
43
side effects of aminosalicyclates?
- cough
- fever
- leucopenia
- proteinuria
-*** pancreaTitis ****
- **** agranulocytosis****
- ****peripheral neuropathy****
44
corticosteroids?
Hydrocortisone,Prednisolone, Budesonide
45
corticosteroids indications?
IBD - Crohs earlier than UC
46
corticosteroids mechanism?
- neutrophil apoptosis
- inhibits phospholipase A2, and NF-Kappa B
- promote anti-inflammatory genes like IL10
47
CI for all corticosteroids?
- avoid live viruses
- systemic infection
48
steroids side effects?
- cushings syndrome
- psychotic disorder
- hirtutism
- HTN
- osteoporosis
- peptic ulcer
- inc weight
49
steroids and adrenal suppression?
During prolonged therapy with corticosteroids, particularly with systemic use, adrenal atrophy develops and can persist for years after stopping. Abrupt withdrawal after a prolonged period can lead to acute adrenal insufficiency, hypotension, or death
50
Immunosuppressants =
azathioprine -> Crohns
51
azathioprine mechanism?
- IS
- Purine synthesis inhibition
- inhibition of B and T cells
52
azathioprine Cl?
Reduced TPMT activity
53
azathioprine interactions?
- allopurinol
- BCG vaccine
- captopril
- HZ vaccine
- ACEi
- trimethoprim
54
azathioprine side effects?
- bone marrow depression
- leucopenia
- pancreatitos
- inc infection risk
- thrombocytopenia
55
pre-treament screening for azathioprine?
- TPMT activity
- increased risk of myelosuppression with reduced TPMT activoty
56
azathioprine monitoring?
- FBC weekly for first 4 weeks
- then at least every 3 months
- for risk of myelosuppression
57
cytokine inhibitors?
- Infliximab
- Adalimumab
58
cytokine inhibitors Ix?
Crohns
59
infliximab mechanism?
- binds to TNF-a
-> Downregulation of IL1 and IL6
60
adalimumab mechanism?
- TNF-a inhibition
61
CI of infliximab/ adalimumab?
moderate/ severe HF, severe infections
62
infliximab interactions?
- BCG vaccine
- cholera vaccine
- MMR vaccine
- HZ vaccine
- influenza vaccine
63
side effects of infliximab?
- alopecia
- arrhythmias
- hypotension/ hTN
- neutropenia
- vasodilation
- sepsis
64
pre-Tx screening w infliximab/ adalimumab?
TB
65
adalimumab side effects?
- agranulocytosis
- anx
- haemorrhage
- leucopenia, neutropenia, thrombocytopenia
66
adalimumab is assoc w ?
infections, sometimes severe, including tuberculosis, septicaemia, and hepatitis B reactivation.
67
Metronidazole & Vancomycin are used for
C diff assoc diarrhoea - colitis
68
metronizadole mechanism?
- high activity against anaerobic bacteria and protozoa
69
metronidazole interactions?
- disulfiram
- fluorouracil
- lithium
- warfarin
70
side effects of metronidazole - IV?
- Vomiting
- metallic taste
- nausea
- dry mouth
- vomiting
71
rare side effects w metronidazole
- panc
- agranulocytosis
- peripheral neuropathy
- cerebellar syndrome
72
metronidazole mechanism?
- nucleic acid synthesis inhibition
- anaerobic bacteria
73
vancomycin mechanism?
- prevens crosslinkage of peptidoglycan subunits
- prevents cell wall formation
- glycopeptide ab
74
cautions of vancomycin?
Systemic absorption may be enhanced in patients with inflammatory disorders of the intestinal mucosa or with Clostridioides difficile-induced pseudomembranous colitis (increased risk of adverse reactions)
75
side effects of vancomycin?
- agran
- eosinophilia
- hypersensitivity
- renal failure
76
Antiprotozoal agent e.g.
metronidazole
77
anti-fungal agents?
- Nystatin
-Fluconazole
78
nystatin mechanism?
- forms channels in the membrane
- changes membrane permeability
- affinity for ergosterol
79
nystatin indications?
- oral candidasis
80
nystatin side effects?
- abd distress
- angioedema
- face oedema
- SJS
81
fluconazole mechanism?
- selective inhibitor of P450 dependent enzyme lansterol 14-a demethylase
- this enzyme converts lanosterol to ergosterol, which is necessary for fungal cell wall synthesis
82
fluconazole Ix?
- candidasis
83
CI of fluconazole?
acute porphyrias
84
cautions of fluconazole?
Susceptibility to QT interval prolongation
85
interactions of fluconazole?
- alc
- amiodarone -> hepatotoxicity
- amphotericin B
- apiprazole
- atorvostatin
- bendroflumethaizide
86
side effects of fluconazole?
- GI discomf
- diarrhoea
- headache
- skin reactions
- agranulocytosis
- QT prolongation
- torsades
87
other antispasmodics?
Mebeverine & Peppermint oil
88
IBS drugs?
- Mebeverine
- Peppermint oil
- Hyoscine (Buscopan)
89
hyoscine mechanism?
- muscarinic receptor antagonism
- anticholinergic effect
- relaxes/ spasmolytic effect on SM
90
Safety info for hyoscine?
- risk of serious adverse effects
- including tachycardia, hypotension, and anaphylaxis
91
CI for all antimuscarinics?
- closed angle glaucoma
- GI obstruction
- MG
- paralytic ileus
- pyloric stenosis
- severe UC
- significant bladder outflow obstruction
- toxic megacolon; urinary retention
92
Interactions of hyoscine?
clozapine
93
side effects of all antimuscarinics?
- const
- dry mouth
- flushing
- dyspepsia
- tachycardia
- urinary retention
94
mebeverine?
- antispasmodic
- anticholinergic
- relaxes SM
95
Mebeverine CI?
paralytic ileus
96
side effects of mebeverine?
- angioedema
- face oedema
- skin reactions
97
peppermint oil mechanism?
- contains L-menthol
- blocks CC in SM -> antispasmodic effect
- reduces calcium influx
98
side effects for peppermint oil?
- bradycardia
- GI discomfort
- reflux
- tremor
- paraesthesia
99
what are the laxatives?
- Methylcellulose
- Ispaghula husk
- Senna Lactulose
- Sodium picosulphate
100
methylcellulose mechanism?
- bulk forming laxative
- inc water content of stool
- Methylcellulose absorbs water in the gastrointestinal lumen thereby increasing the bulk of the stool.
- This leads to distension and stimulation of peristalsis
101
isphalga husk mechanism?
- bulk forming
- increasing faecal mass which stimulates peristalsis
102
CI of isphalga husk?
- faceal impaction
- intestinal obstruction
- undiagnosed rectal bleeding
- reduced gut motility
103
cautions w isphalga husk?
- adequate fluid intake to avoid oesophageal or intestinal obstruction
104
side effects of ispaghula husk?
- abd distension
- bronchospasm
- conjunctivitis
105
senna mechanism?
- stimulant laxative
- stimulates peristalsis thereby increasing the motility of the large intestine.
106
senna CI?
- atony
- intestinal obs
- undiagnosed abd pain
107
side effects of senna?
- albuminuria
- fluid imbalance
- GI discomfort
- haematuria
- **pseudomelanosis coli**
108
prolonged/ excessive senna use can cause?
hypokalaemia
109
lactulose indications?
- constipation
- hepatic encephalopathy
110
lactulose CI?
- galactosaemia
- GI obstruction
- GI perf
111
side effects of lactulose?
- diarrhoea
- flatulence
- nausea
- vomiting
- abd pain
112
lactulose mechanism?
- osmotic laxative
- causes retention of water through osmosis leading to softer easier to pass stool
113
Sodium picosulphate mechanism?
- stimulant laxative
- inhibits abs of water and electrolytes and increases their secretion into intestinal lumen to form an active metabolite which acts directly on colonic mucosa to stimulate peristalsis
114
CI of Sodium picosulphate?
intestinal obst
115
side effects of Sodium picosulphate
- diarrhoea
- GI discomfory
116
summary of the laxatives?
- methylcellulose and ispaghula husk: BF
- senna: faecal softner
- lactulose: osmotic
- Sodium picosulphate: stimulant
117
Local anaesthetics =
- Lidocaine
- Bupivacaine
- used for suturing
118
lidocaine CI?
all grades of AV block, severe myocardial depression
119
SE of lidocaine?
- AV block
- cardiac arrest
- hypotension
- methaemglovinaemia
120
lidocaine mechanism?
- blocks sodium channels
- preventing nerve depolarisation
121
bupivacaine mechanism?
- sodium channel blocker
122
CI of bupivacaine?
- Bier's block
- injection into inflamed tissues
123
SE of bupivacaine?
- arrythmias
- dizziness
- hTN
- parasthesia
- neurotoxicity
124
IV anaesthetics?
- Etomidate
- Ketamine
- Propofol
- Thiopental
125
What are IV anaesthetics used forr?
Rapid induction of anaesthesia, total intravenous anaesthesia, prolonged sedation
126
etomidate mechanism?
- short acting IV
- binds to GABA-A increasing duration of time
- post inhib effect of GABA is prolonged
127
etomidate cautions?
- acute circ failure
- adrenal insufficiency
- hypovolaemia
- cardiovascular disease
128
etomidate - adrenal insufficiency?
- suppresses adrenocortical function
- should not be used for maintenance of anaesthesia
129
SE of etomidate?
- hypotension
- resp disorders
- vascular pain
- adrenal insufficiency
130
Ketamine mechanism?
- rapid acting GA
- NMDA antagonist used for induction of anaesthesia
131
ketamine CI?
- HTN
- pre-eclampsia
- raised ICP
- stroke
132
side effects of ketamine?
- anx
- hallucination
- nystagmus
- vomiting
133
which anaesthetic can cause cystitis haemorrhagic?
ketamine
134
reducing hallucinations with ketamine?
Incidence of hallucinations can be reduced by premedicaton with a benzodiazepine (such as midazolam).
135
Propofol mechanism?
- positive modulation of the inhibitory function of GABA-A
136
propofol indications?
- induction and maintenance of anaesthesia
137
cautions of propofol?
- shock
- cardiac impairment
- hypovolaemia
- raised ICP
138
SE of propofol?
- apnoea
- arrhythmias
- hypotension
- nausea and vomiting
139
what else can occur w propofol?
- pulm oedema
- urine discoloration
- pancreatitis
140
Thiopental mechanism?
- barbituate
- binds to CI- ionophore at GABA receptor, enhancing effect of GABA
141
thiopental SE?
- decreased cardiac contractility
- arrhythmia
- circ collapse
- resp disorders
142
IV opiods during anaesthesia?
- Fentanyl
- Remifentanil
143
use of iV opiods during anaesthesia?
Reduction in the dose requirement of anaesthetic agents, sedation and respiratory depression during assisted ventilation in intensive care
144
fentanyl Mx?
- mu opiod receptor agonist
- hyperpolarises cell and inhibits nerve activity
145
CI of fentanyl?
opiod naive ppts
146
SE of fentanyl?
- apnoea
- HTN
- muscle rigidity
- resp disorders
147
Remifentanil mechanism?
µ-opioid agonist with rapid onset and peak effect, and short duration of action.
148
CI of remifentanil?
analgesia in conscious patients
149
remifentanil SE?
- Apnoea
- hypotension
- muscle rigidity
150
remifentanil metabolism?
In contrast to other opioids which are metabolised in the liver, remifentanil undergoes rapid metabolism by plasma esterases; it has short duration of action which is independent of dose and duration of infusion
151
inhalation anaesthetics =
- Desflurane
- Halothane
- Isoflurane
- Nitrous oxide
- Sevoflurane
152
Desflurane indications?
indication and maintenance of anaesthesia
153
CI of all volatile halogenated anaesthetics?
Susceptibility to malignant hyperthermia
154
side effects of all volatile halogenated anaesthethics?
- agitation
- chills
- resp disorders
- cough
155
SE of desflurance/
coagulation disorders, conjunctivitis
156
desflurane mechanism?
- agonises GABA-A and glycine receptors
- antagonises glutamate receptors
157
Halothane mechanism?
- binds to potassium channels in cholinergic neurons
- binds to NMDA and calcium channels causing hyperpolarisation
158
SE of halothane?
- hepatotoxicity
- resp depression
- irreg HB
159
Isoflurane SE?
- Carboxyhaemoglobinaemia
- delirium
- cognitive impairment
160
isoflurane mechansim?
- binds to GAB receptor, glutamate receptor and glycine receptor
161
nitrous oxide cautions?
- presence of intercranial air after head injury or trapped air after underwater dive
- pneumothorax
162
NO interacts w
methotrexate
163
SE of NO?
- Abd distension
- agranulocytosis
- parasthesia
- subcaute combined cord degeneration
164
NO mechanism?
- induces opiod release in the brain stem
- activates descending nociceptive process
165
sevoflurane mechanism?
- GABA and glycine receptors
- inhibt excitatory activity by blocking nictonic ACh, serotonin and glutamate receptors
166
uses of the inhalational anaesthetics?
Induction and maintenance of anaesthesia
167
sevoflurane CI?
Susceptibility to QT-interval prolongation
168
Sevoflurane SE?
- Drowsiness
- fever
- hypothermia
169
Depolarising neuromuscular-blocking drugs
suxamethonium (succinylcholine)
170
use of suxamethonium?
Endotracheal intubation, muscle relaxation during surgery or on the ICU
171
suxamethonium mechanism?
- mimicks ACh at NM junction
- but bc its hydrolsed much slower than ACh, depolarisation is prolonged leading to NM blockade
172
CI of suxamethonium?
- hyperkalaemia
- low plasma cholinesterase activity - including severe liver dsisease
- malignant hyperthermia
173
suxamethonium interacts w
steroids - fludrocortisone, hydrocortisone, pred, beclomethasone
174
SE of suxamethonium?
- arrythymias
- bradycardia
- involuntary muscle contractions
- myogloburia
175
Competitive N2 receptor antagonists (non-depolarising blockers)
- Atracurium
- Cisatracurium
- Mivacurium
- Pancuronium
- Rocuronium
- Vecuronium
176
atracurium uses?
NM blockade
177
cautions for all non depolarising NM blocking drugs?
- burns
- CV disease
- fluid dist
- MG
178
Atracurium interacts w?
steroids
179
SE of all ND NM blocking drugs?
- flushing
- hypotension
180
atraucrium and other non depolarising NM blockers mechanism?
- competes w ACh for binding sites
181
competitive N2 antagonists (ND NM blockers) are used for...
Endotracheal intubation, muscle relaxation during surgery or on the ICU
182
acetylcholineesterase inhibitors =
- Edrophonium
- Neostigmine
- Pyridostigmine
183
edrophonium, neostigmine and pyridostigmine mechanism?
- prolong ACh action
- by inhibiting acetylcholineesterase action
184
AChE inhibitors are used to treat
- MG, and to
- reverse non depolarising (competitive) NM blockade - neostigmine
185
CI of all anticholinesterases?
- intestinal or urinary obs
186
side effects of all anticholinesterases?
- abd cramps
- diarrhoea
- hypersalivation
- nausea and vomiting
187
Reversal of musle relaxants used during general anaesthesia =
neostigmine
188
to test the therapeutic response to AChE inhibitors in myasthenia gravis =
edrophonium
189
drug used for MG =
Pyridostigmine
190
