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1
Q

What are examples of PPIs?

A

Omeprazole

Lansoprazole

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2
Q

When are PPIs indicated?

A
  • Dyspepsia (uninvestigated 4w only)
  • Peptic ulceration (H. pylori eradication or prophylaxis of NSAIDs)
  • Zollinger-Ellison syndrome
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3
Q

What is the MOA of PPIs?

A

Reduces gastric acid secretion
Inhibits H+/K+-ATPase
Gastric parietal cell
Blocks final stage of HCL secretion

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4
Q

What are important side effects of PPIs?

A
  • May mask gastric cancer
  • Increased risk of fractures in elderly (1y use)
  • May increase c.diff infection
  • Hyponatraemia risk
  • Hypomagnesium risk
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5
Q

What are examples of H2RA?

A

Ranitidine

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6
Q

When are H2RAs indicated?

A
  • Dyspepsia (uninvestigated 4w only)
  • Peptic ulceration (H. pylori eradication or prophylaxis of NSAIDs)
  • Zollinger-Ellison syndrome
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7
Q

What should be noted for H2RAs?

A

Resurgence in use following concern of reduced antiplatelet action in px using clopidogrel

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8
Q

What is the MOA for H2RA?

A

Competitive inhibitor of histamine
At parietal cell H2 receptor
Suppresses normal secretion of HCl and meal stimulated secretion of acid

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9
Q

What are side effects of H2RA?

A

Half dose if eGFR <50ml/min // 1.73m2

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10
Q

What are examples of lipase inhibitors?

A

Oristat

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11
Q

When are lipase inhibitors indicated?

A

Adjunct to diet for weight loss if BMI >30kg.m2 or >28kg.m2 if other CVD risk factor

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12
Q

What should be noted for lipase inhibitors?

A

Continue only beyond 12w if weight loss >5% of baseline

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13
Q

What is the MOA of lipase inhibitors?

A

Reduced absorption of dietary fat

Inhibits pancreatic lipase

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14
Q

What are side effects of lipase inhibitors?

A

Abdominal discomfort
Lose, oily stools
Increased risk of UTIs

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15
Q

What are examples of systemic and topical corticosteroids

A

Hydrocortisone
Prednisolone
Beclometasone
Budesonide

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16
Q

When are S/T corticosteroids indicated?

A

Acute diffuse IBD

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17
Q

What is the MOA for S/T corticosteroids?

A

Inhibition of leukocyte infiltration by receptor binding

Interference of inflammatory mediators

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18
Q

What are side effects of corticosteroids?

A 
Adrenal axis suppression 
Immunosuppression 
Catabolic, hyperglycaemic metabolic state
Osteoporosis 
Hypomania and psychosis
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19
Q

What are examples of aminosalicylates?

A

Mesalazine

Sulfasalazine

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20
Q

When are aminosalicylates indicated?

A

Acute diffuse IBD

Maintenance of remission of IBD

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21
Q

What is the MOA of aminosalicylates?

A

Metabolised in gut to 5-aminosalicylic acid
Antioxidant - possibly traps free radicals
Decreases inflammation locally by blocking COX and inhibiting PGs in colon

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22
Q

What are examples of antispasmodics?

A

Peppermint oil

Buscopan

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23
Q

When are antispasmodics indicated?

A

Relief of abdominal colic in IBS

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24
Q

What is the MOA of antispasmodic drugs?

A

Uncertain

GI L-type calcium channels inhibition

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25
What are side effects of antispasmodics?
Local irritant
26
What are examples of osmotic laxatives?
Lactulose
27
When are osmotic laxatives indicated?
Treatment or prevention of constipation
28
What is the MOA of osmotic laxatives?
Semi synthetic disaccharide not absorbed in GI tract Increases amount of water in LB: Drawing or retaining fluid Produces osmotic diarrhoea Low faecal diarrhoea and discourages proliferation of ammonia producing organisms
29
What are side effects of osmotic laxatives?
Nausea Vomiting Abdominal discomfort
30
What are examples of stimulant laxatives?
Senna
31
When are stimulant laxatives indicated?
Treatment and prevention of constipation
32
What is the MOA of stimulant laxatives?
Directly stimulates myenteric plexus | Increased peristalsis and defecation
33
What are side effects of stimulant laxatives?
Abdominal cramps | Risk of hypoglycaemia with prolonged use
34
What are examples of anti-platelet drugs?
Aspirin | Clopidogrel
35
When is aspirin indicated?
CVD secondary prevention Transient Ischaemic attack (with dipyridamole) Acute stroke (14 days) ACS
36
What is the MOA of aspirin?
Irreversible COX inhibition Suppresses PGs and thromboxanes synthesis Reduces platelet aggregation
37
What are side effects of aspirin?
``` GI ulceration and irritation Bleeding Nephrotoxicity Hypertension Reye's syndrome ```
38
What is the link between aspirin and Reye's syndrome?
Aspirin not to be used in children under 16yo | Unless for Kawasaki disease
39
When is clopidogrel indicated?
NSTEMI MI | Stroke (after 14 days of aspirin)
40
What is the MOA of aspirin?
Prodrug | Inhibits ADP dependent activation of GP1b/IIa receptor
41
What are the side effects of clopidogrel?
Dyspepsia Bleeding Diarrhoea
42
What are examples of ACEi?
Ramipril
43
When are ACEi indicated?
Hypertension (<55yo and not AfroC) Heart failure Nephropathy
44
What is the MOA of ramipril?
Competes with Ang I for ACE | Blocks conversion of AngI --> Ang II
45
What are the side effects of ramipril?
AKI if concurrent dehydration or NSAID use or if pre-existing renal artery stenosis Cough (10%) Angioedema risk
46
What are examples of Ang II receptor antagonist?
Lorsartan Candarsartan Valsartan
47
When are Ang II RA indicated?
Hypertension (<55yo and not AfroC) | Heart failure
48
What are the Ang II RA drugs used in heart failure?
Candasartan Lorsartan Valsartan
49
What is the MOA of Ang II RA?
Reduced Ang II vasoconstriction | Direct and competitive inhibition of AT1 and 2
50
What are side effects of Ang II RA?
AKI if concurrent dehydration or NSAID use or if pre-existing renal artery stenosis Angioedema risk
51
What are examples of calcium channel blockers?
Amlodipine (dihydropiridine)
52
When are calcium channel blockers indicated?
Hypertension (>55 or AfroC) | Angina
53
What is the MOA of calcium channel blockers?
Vasodilation by L type Ca channel inhibition | Inhibits vascular smooth muscle cells contraction
54
What are side effects of calcium channel blockers?
Post venual dilation | Constipation
55
What are examples of thiazide like diuretics?
Indapamide
56
When are thiazide like diuretics indicated?
Hypertension (>55yo or AfroC)
57
What is the MOA of thiazide like diuretics?
Inhibits Cl- reabsorption at DCT via Na-Cl co-transporter
58
What are side effects of thiazide like diuretics?
Hyponatraemia Hypokalaemia Erectile dysfunction Gout
59
What are examples of B adrenoreceptor blockers?
Bisoprolol | Propranolol
60
When are BB indicated?
``` Angina Heart failure Arryhythmia Anxiety (propranolol) Symptomatic relief for hyperthyroidism (propranolol) ```
61
What is the MOA of BB?
Competitive antagonist of of catecholamines for binding at B adrenergic receptors
62
What is special about propranolol?
Lipid soluble | Penetrates CNS
63
What are side effects of BB?
Bronchospasm Peripheral ischaemia Erectile dysfunction
64
What are examples of statins?
Atorvastatin | Simvastatin
65
When are statins indicated?
Primary or secondary CVD prevention
66
What is the MOA of statins?
Hydrolysed to active metabolite Competes HMG-CoA for HMG-CoA reductase Reduces enzyme and quantity of mevalonic acid (cholsterol precursor)
67
What are side effects of statins?
Hyperglycaemia Muscle toxicity (Raised CK, myopathy or rhabdomyolysis) This is increased in elderly or hypothyroidism Hepatotoxicity
68
What are examples of exogenous nitric oxide donors?
GTN spray | Isosorbide mononitrate
69
When are exogenous nitric oxide donors indicated?
Prophylaxis and treatment of angina
70
What is the MOA of exogenous nitric oxide donors?
Converted to nitric oxide Activates guanylate cyclase Stimulates cGMP to cause vasodilation Through protein kinase dependent phosphorylations in VSMC Results in dephosphorylation of myosin light chain fibre
71
What are side effects of exogenous nitric oxide donors?
Headache Postural hypotension Rapid tolerance
72
What needs to be ensured when using exogenous nitric oxide donors?
4-12 hours nitrate free period required daily to prevent loss of efficacy
73
What are examples of rate limiting calcium channel blockers?
Diltiazem | Verapamil
74
When are rate limiting calcium channel blockers indicated?
Narrow complex tachycardia Angina Hypertension
75
What is the MOA of rate limiting calcium channel blockers?
AVN conduction delay | Inhibits L type calcium channels
76
What are the side effects of rate limiting calcium channel blockers?
Risk of heart block - AVOID CONCURRENT BB USE Negatively inotropic Constipation
77
What are examples of antianginals?
Nicorandil (K) Ivabradine (K) Ranolazine (Na)
78
When are antianginals indicated?
Angina | 2nd line if cannot tolerate BB or CCBs
79
What is the MOA of Nicorandil?
Combines Katp channel activation with NO donor | K+ channel!
80
What is the MOA of Ivabradine?
Sinus node Kf channel blocker | HCN
81
What is the MOA of Ranolazine?
Uncertain Sodium channel blocker Myocyte metabolic substrate utilisation
82
What are the side effects of Nicorandil?
Rectal bleeding | Flushing
83
What are the side effects of Ivabradine?
Bradycardia Heart block AF
84
What are the side effects of Ranolozine?
QT prolongation
85
What are examples of loop diuretics?
Furosemide | Bumetanide
86
When are loop diuretics indicated?
Symptomatic relief of pulmonary oedema | Peripheral oedema in HF or cirrhosis
87
What are the MOA of loop diuretics?
Inhibit Na+/K+?Cl- symporter within ascending LOH
88
What are the side effects of loop diuretics?
``` Hypotension Hypokalaemia Hyponatraemia Ototoxicity (toxic to the ear) Nephrotoxicity ```
89
When are aldosterone antagonists indicated?
``` Primary hyperaldosteronism Secondary hyperaldosteronism - Heart failure - Cirrhosis - Nephrotic syndrome PCOS ```
90
What are examples of aldosterone antagonists?
Eplerenone | Spironolactone
91
What is the MOA of aldosterone antagonist?
Antagonist of intracellular mineralocorticoid receptor
92
What are side effects of aldosterone antagonist?
Hyperkalaemia Hyponatraemia Hepatotoxicity Gynaecomastia
93
What are examples of parental anticoagulants?
Heparin LMWH (Enoxaparin) Fondaparinux
94
When are parental anticoagulants indicated?
Prophylaxis and treatment of venous thromboembolism | Treatment of ACS (LMWH and fondaparinux)
95
What is the MOA of parental anticoagulants?
Factor Xa inhibition
96
What is the MOA of heparin?
Factor Xa inhibition | Thrombin inhibitor
97
How is Heparin administered?
IV
98
How is LMWH administered?
SC
99
How is Fondaparinux administered?
SC
100
What are side effects of parental anticoagulants?
Bleeding Purpurea (ITP) Heparin induced thrombocytopenia (HIT)
101
What are examples of oral anticoagulants?
``` Warfarin Novel oral anticoagulants - Apixaban - Dabigatran - Rivaroxaban ```
102
When are oral anticoagulants indicated?
Prophylaxis and treatment of venous thromboembolism | Prevention of stroke and systemic emboli in AF
103
What is the MOA of Warfarin?
Inhibits VKOR | Inhibits synthesis of FII, VII, IV and X
104
What is the MOA of the DOACs?
Inhibit FXa
105
What are the side effects of oral anticoagulants?
Haemorrhage Purpura (purple toes) Skin necrosis
106
When is adrenaline indicated?
``` Cardiac arrest (1/10,000) Anaphylaxtic shock (1/100) ```
107
What is the MOA of adrenaline?
Beta > alpha adrenergic receptor agonist
108
What are the side effects of adrenaline?
Tachycardia MI Hypertension Decreased placental blood flow
109
When is adenosine indicated?
Paroxysmal AVNRT / AVRT | Diagnosis of tachydysarrhythmias
110
What is the MOA of adenosine?
AV node conduction block Short duration due to 8-10s half life Increased if on dipyridamole or theophylline
111
What are the side effect of adenosine?
Arrhythmia Angina Headache Flushing
112
When is Amiodarone indicated?
Treatment of narrow and broad complex tachycardias AF Atrial flutter
113
What is the MOA of amiodarone?
Class I-IV Vaugh Williams effects | Half life of 90 days
114
What are side effects of amiodarone?
``` Hepatotoxicity Pulmonary toxicity Hyper/Hypo thyroidism Grey skin Corneal deposits Multiple interactions ```
115
When is digoxin indicated?
Rate control in AF | HF
116
What is the MOA of digoxin?
Positive inotropic action and negative chronotropic action Increase cytosolic calcium inhibition of Na+/K+?ATPase pump And increased vagal tone
117
What are side effects of digoxin?
Narrow therapeutic index GI disturbance Yellow vision Dysarrhythmias
118
What are examples of fibrinolytic drugs?
Alteplase | Streptokinase
119
When are fibrinolytic drugs indicated?
Acute STEMI Acute ischaemic stroke Compromised PE
120
What is the MOA of fibrinolytic drugs?
Activate plasminogen to plasmin | Degrades fibrin clot
121
What are the side effects of fibrinolytic drugs?
Haemorrhage | High risk of mortality or morbidity in intracranial bleeds
122
What are examples of short acting inhaled Beta 2 agonists?
Salbutamol
123
What are examples of long acting Beta 2 agonists?
Salmeterol
124
When are Beta 2 agonists indicated?
Asthma COPD Premature labour
125
How is salbutamol used?
IV as tocolytic agent (anti-contraction)
126
What is the MOA of beta 2 agonists?
Specific beta 2 agonist | Causes bronchodilation through smooth muscle relaxation
127
What are important side effects of beta 2 agonists?
Tremor Headache Hypokalaemia
128
What are examples of antimuscarinic bronchodilators?
Ipratropium | Tiotropium
129
When are antimuscarinic bronchodilators indicated?
Asthma | COPD
130
What is the MOA of antimuscarinic bronchodilators?
Inhibit M1-3 muscarinic receptors | Causes bronchodilation through smooth muscle relaxation
131
What are side effects of antimuscarinic bronchodilators?
Dry mouth | GI upset
132
What are examples of inhaled corticosteroids?
Beclometasone | Fluticasone
133
When are corticosteroids indicated?
Asthma | COPD
134
What is the MOA of inhaled corticosteroids?
Binds with highly affinity to specific cytoplasmic receptors Produce inhibition of leukocytes infiltration Interference in function of mediators and suppression of humoral immune responses
135
What are the side effects of inhaled corticosteroids?
Paroxysmal bronchoconstriction Oral thrush Adrenal suppression risk Potential risk of reduced growth velocity in children Increased risk of pneumonia in COPD patients
136
When is Theophylline indicated?
Asthma | COPD
137
What is the MOA of Theophylline?
Inhibits cAMP degradation | Causes bronchodilation through smooth muscle relaxation
138
What are the side effects of Theophylline?
``` Narrow therapeutic index GI upset Tachycardia Headache Convulsions Hypokalaemia Hyperglycaemia ```
139
When is oxygen indicated?
Treatment of hypoxaemia | Palliation of dyspnoea
140
What is the MOA of oxygen?
Final electron acceptor in cellular metabolism
141
What is to note with oxygen?
Contraindicated in paraquat poisoning | Risk of free radical generation
142
What are side effects of oxygen?
Loss of hypoxic drive causing type II respiratory failure
143
What are examples of antihistamines?
Chlorphenamine | Loratadine
144
When are antihistamines indicated?
Symptomatic relief of allergies | Emergency treatment of anaphylaxis (chlorphenamine)
145
What is the MOA of antihistamines?
Inhibition of H1 receptors
146
What are the side effects of antihistamines?
Sedation, enhanced with alcohol Dysarrhythmias Antimuscarinic effects
147
What are examples of opioid analgesics?
Codeine Morphine Methadone Pethidine
148
When are opioid analgesics indicated?
``` Moderate pain - codeine Severe pain - morphine Treatment of opioid dependence - methadone Obstetric pain relief - pethidine Biliary colic - pethidine ```
149
Why is pethidine used in obstetrics?
Decreased risk of neonatal respiratory suppression
150
What is the MOA of opioid analgesics?
Opioid receptor agonist Codeine metabolised to morphine by CYP2D6 2D6 is under genetic control, may cause apparent lack of efficacy in individuals
151
What is the difference between methadone and morphine?
Methadone is less sedating than morphine | Methadone has a longer half life
152
What are side effects of opioid analgesics?
``` Sedation or coma Respiratory depression Constipation QT prolongation (methadone) Hyperprolactinaemia ```
153
What are examples of antiemetic drugs?
Antihistamines - Cyclizine or promethazine in pregnancy Phenothiazines - metodopramide 5HT3 antagonists - Ondanestrone
154
When are antiemetics indicated?
Post-operative nausea and vomiting Treatment or prophylaxis of chemotherapy or radiotherapy nausea and vomiting Treatment of migraine associated nausea and vomiting (metoclopramide) Treatment of motion sickness (cyclizine)
155
What is the MOA of antiemetics?
Antagonist to receptors represent in CTZ Dopamine and muscarinic receptors 5HT receptors are present within GI tract too
156
What are side effects of antihistamines (as antiemetics)?
Sedation | Other antimuscarinic effects
157
What are the side effects of metochlorpramide (phenothiazine)?
Risk of occulo-gyric crisis | Extra pyramidal features
158
What are side effects of 5HT3 antagonists (as antiemetics)?
Constipation | Flushing
159
What are examples of anti-epileptic drugs?
Sodium valporate Carbamazepine Lamotrigine
160
When are anti-epileptic drugs indicated?
``` Focal seizures (carbamazepine and lamotrigine) Generalised seizures (sodium valporate or lamotrigine) ```
161
What is the MOA of anti-epileptic Carbamazepine?
Voltage operated sodium ion channel inhibitor Strong hepatic enzyme inducer Reduces half life from 30h-15h
162
What is the MOA of anti-epileptic Sodium valporate?
Sodium and calcium ion channel blocker | Increases GABA in the CNS
163
What is the MOA of anti-epileptic lamotrigine?
Potent sodium channel blocker
164
What are side effects of anti-epileptic Carbamazepine?
Sedation Ataxia Leukopenia Hepatotoxicity
165
What are side effects of anti-epileptic Sodium valporate?
Alopecia Weight gain Teratogenic
166
What are side effects of anti-epileptic lamotrigine?
Sedation | Rash and dizziness
167
What is to be noted about anti-epileptic lamotrigine?
Valporate may increase plasma concentration of lamotrigine to toxic concentrations
168
What are examples of antimigraine drugs?
Sumatriptan
169
When are antimigraine drugs indicated?
Treatment of acute migraine or cluster headache
170
What is the MOA of antimigraine drugs?
5HT1 receptor agonist
171
When should antimigraine drugs be avoided?
Avoid if previous CVA or TIA or hypertension
172
What are side effects of antimigraine drugs?
Vasoconstriction Sedation Dyshythmias Raynaud's
173
What are drugs used in Parkinsonism?
- Levodopa + peripheral dopa-decarboxylase inhibitor (co-beneldopa) - Ropinirole --Dopamine receptor agonists - Monoamine Oxidase B inhibitors (Selegiline)
174
What is the MOA of Levodopa?
Dopamine precursor | Given with peripheral dopa-decarboxylase inhibitor to minimise peripheral side effects
175
What is the MOA of Ropinirole?
Direct acting dopamine receptor agonist
176
What is the MOA of Monoamine oxidase B inhibitor / Selegiline?
Increase availability of dopamine in CNS | May also reduce the end of dose effects in advanced Parkinson's
177
What are side effects of levodopa?
Psychosis and dementia Postural hypotension Dysrhythmias Dry mouth
178
What are side effects of Ropinirole?
Impulse disorders such as pathological gambling, binge eating and hypersexuality Confusion Hallucinations
179
What are side effects of Selegiline?
Ulcers Hypotensions Sedation Confusion
180
What are drugs used for dementia?
Acetylcholinesterase inhibitors | Glutamate receptor antagonists
181
What are examples of Acetylcholinesterase inhibitors?
Donepezil Galantamine Rivastigmine
182
What are examples of Glutamate receptor antagonists?
Memantine
183
When are Acetylcholinersterase inhibitors indicated?
Mild to moderate dementia | Rivastigmine is licensed for dementia in Parkinson's
184
When is memantine indicated?
Moderate to severe dementia
185
What is the MOA of acetylcholinesterase inhibitors?
Increase in ACh through reversible inhibition of enzyme degradation
186
How else does Rivistagmine act?
Non competitive agonist
187
How else does Galantamine act?
Nicotinic receptor agonist
188
What are side effects of acetylcholinesterase inhibitors?
``` Cholinergic effects Syncope Hallucinations Aggression Incontinence Heart block Seizures ```
189
What are the side effects of Memantine?
``` Hypertension Heart failure Thrombosis Psychosis Suicidal intent ```
190
What are examples of anxiolytics?
Diazepam | Lorazepam
191
When are anxiolytics indicated?
Acute alcohol withdrawal Acute drug induced dystonic reactions Status epilepticus Short term use in anxiety or insomnia
192
What is the MOA of anxiolytics?
BZD act on GABAa receptors | Facilitate opening of GABA-activated chloride channels
193
What are the side effects of anxiolytics?
``` Drowsiness Confusion Ataxia Dependence Paradoxical aggression ```
194
What is to note with the side effects of anxiolytics?
Side effects may be enhanced with alcohol
195
What are antipsychotics used?
1st generation - typical | 2nd generation - atypical
196
What are examples of 1st generation antipsychotics?
Haloperidol
197
What are examples of 2nd generation antipsychotics?
Olanzapine | Clozapine
198
When are antipsychotics indicated?
Treatment of schizophrenia or psychosis | Haloperidol may be used to manage aggression in organic brain disorders
199
What is MOA of typical antipsychotics?
Dopamine D2 receptor antagonists | Non selective so there are no extrapyramidal side effects
200
What is the MOA of atypical antipsychotics?
Antagonises D1, D2, D4, 5HT2 and H1 and muscarinic receptors
201
What are side effects of antipsychotics?
Extra pyramidal features Hypotension QT prolongation (ECG requires prior to treatment)
202
What are extrapyramidal side effects?
Parkinsonism Dystonia Akathesis Tardive dyskinesia
203
What are side effects of atypical antipsychotics?
Hyperlipidaemia Glucose intolerance Weight gain Bone marrow suppression -- especially clozapine
204
What are drugs used for bipolar disorder or mania?
Lithium salts
205
When are lithium salts indicated?
Treatment and prophylaxis of mania or bipolar disorder
206
What is the MOA of lithium salts?
Lithium ions permeate voltage gated sodium ion channels Accumulate within the cytosol Effect several intracellular signalling pathways and cAMP production
207
What are the side effects of lithium salts?
``` Narrow therapeutic index GI disturbance QT prolongation AV block Tremor Cognitive impairment Extrapyramidal features Seizures Thyroid abnormalities Renal impairment - beware of concurrent ACEi, NSAIDs or diuretics ```
208
What are examples of SSRIs
Fluoxetine | Citalopram
209
When are SSRIs indicated?
Depressive illness Panic disorders (citalopram) Bulimia (fluoxetine) OCD (fluoxetine)
210
What is the MOA of SSRIs?
Increase synaptic concentration of 5-hydroxytrytaphan through inhibition of re-uptake transporter
211
What are the side effects of SSRIs?
Hyponatraemia (especially in the elderly) Risk of serotonin syndrome with other seretonergic drugs Risk of suicidal idealisation in children
212
What are examples of TCAs?
Amitriptyline
213
When are TCAs indicated?
NO LONGER RECOMMENDED FOR DEPRESSION DUE TO TOXICITY IN OVERDOSE Unlicensed use in neuropathic pain and migraine prophylaxis
214
What is the MOA of TCAs?
Muscarinic and voltage gated sodium ion channel antagonist Increases 5HT and catecholamine concentrations in CNS Inhibits re-uptake transporters
215
What are the side effects of TCAs?
Antichol ?
216
What are examples of Beta -lactams ?
``` PENICILLINS Amoxicillin Amoxicillin + clavulanic acid (co amoxiclav) Benzylpenicillin (Pen G) Flucloxacillin ```
217
When are beta lactams indicated?
Gram + and Gram - organisms
218
When is amoxicillin indicated?
Oral infections Lyme disease Anthrax and H.pylori eradication
219
When is Co-amoxiclav indicated?
``` Active against beta lactamase producing organisms LRTIs Joint or bone infections Animal bites GU infections ```
220
What is the MOA of beta lactam antibiotics?
Interferes with synthesis of bacterial cell wall peptidoglycan After attachment to penicillin-binding proteins on bacteria Inhibits transpeptidation enzyme that cross links peptide chain attached to backbone of peptidoglycan
221
What is to be noted about Benzylpenicillin?
Not effective orally
222
What is to be noted about Clavulanate?
Competitively and irreversibly inhibits wide variety of beta lactamases produced by certain bacteria Makes drug more potent
223
What is to be noted about Flucloxacillin?
Stable against hydrolysis by variety of beta lactamases | Including penicillinases and cephalosporinases and extended spectrum beta lactamases
224
What are side effects of beta lactams?
GI disturbance Type I and IV hypersensitivity reactions Cholestatic jaundice associated with co-amoxiclav use
225
What are examples of quinolones?
Ciprofloxacin
226
When are Quinolones indicated?
``` Gram + and - bacteria Pseudomonas Chlamydia Gonorrhoea Typhoid ```
227
What is the MOA of quinolones?
Bacteriocidal | Inhibition of bacterial DNA enzyme topoisomerases II (DNA gyrase) and IV
228
What are side effects of quinolones?
``` Tendon rupture (elderly) Decreased seizure threshold Peripheral neuropathy Hypoglycaemia High c.diff risk ```
229
What are examples of cephalosporins?
Cefotaxime
230
When are cephalosporins indicated?
``` Septicaemia Pneumonias Biliary tract infections Meningitis Epiglottitis Gonorrhoea ```
231
What is MOA of cephalosporins?
Inhibition of cell wall synthesis via affinity for penicillin - binding proteins (PBPs) Displays resistance to penicillinases Makes it useful to treat infections resistant to penicillin derivatives (also cefuroxime)
232
What are side effects of cephalosporins?
10% cross over hypersensitivity risk of penicillin allergic | High C.diff risk
233
What are examples of Macrolide antiobiotics?
Clarithromycin
234
When are macrolide antibiotics indicated?
Similar antimicrobial spectrum to penicillin and atypical pneumonias and campyobacter
235
What is MOA of macrolide antibiotics?
Protein synthesis inhibitor Reversibly binds to 50 S subunit of bacterial ribosomes or near "P" or donor site Binding of tRNA to donor site blocked
236
What are side effects of macrolides?
QT prolongation | Steven Johnson Syndrome / Toxic Epidermal Necrosis
237
What are examples of aminoglycosides?
Gentamicin
238
When are aminoglycosides indicated?
Septicaemia secondary to gram - and some +
239
What is MOA of aminoglycosides?
Protein synthesis inhibition Irreversibly binds to specific 30 S subunit proteins and 16S rRNA Leads to interference with initiation complex Misreading of mRNA so incorrect amino acids are inserted into polypeptide
240
What are side effects of aminoglycosides?
Narrow therapeutic index Nephrotoxicity Irreversible ototoxicity
241
When is nitrofurantoin indicated?
UTIs
242
What is the MOA of nitrofurantoin?
Inhibits bacterial acetyl-coenzyme A Interferes with organism's carb metabolism Can disrupt bacterial cell wall formation
243
What are side effects of nitrofurantoin?
Pulmonary fibrosis Retroperitoneal fibrosis Peripheral neuropathy
244
When is trimethoprim indicated?
UTIs Bronchitis PCP (pneumocytosis pneumonia)
245
What is MOA of trimethoprim?
Bacterial dihydrofolate reductase inhibitor | Reduces folate metabolism
246
What are side effects of trimethoprim?
Hyperkalaemia
247
What are examples of glycopeptides?
Vancomycin
248
When are glycopeptides indicated?
Gram + cocci | C.diff oral
249
What is MOA of glycopeptides?
Glycopeptide antibiotic which acts by inhibiting cell wall synthesis
250
What are side effects of glycopeptides?
Nephrotoxic Ototoxic Red man syndrome
251
When is metronidazole indicated?
Anaerobic infections Protozoal infections H.pylori infection Crohn's disease
252
What is MOA of metronidazole?
Reduced metronidazole disrupts DNAs helical structure Inhibits bacterial nucleic acid synthesis Results in bacterial cell death
253
What are side effects of metronidazole?
Disulfram like reaction with alcohol
254
When are anti-tuberculosis medications used?
Ethambutol Isoniazid Pyrazinamide Rifampicin
255
When is ethambutol indicated?
Mycobacterium infection
256
What is MOA of ethambutol?
Inhibits transfer of mycolic acids into cell wall of tubercle bacillus
257
What are side effects of ethambutol?
Optic neuritis | Red/Green colour blindness
258
When is isoniazid indicated?
Mycobacterium infection
259
What is MOA of isoniazid?
Prodrug | Once inactivated, inhibits synthesis of mycolic acids
260
When is pyrazinamide indicated?
Mycobacterium infection
261
What is the MOA of pyrazinamide?
Mechanism unclear Metabolite (pyrazinoic acid) may lower intrabacterial pH To level that could inactivate vital target enzyme
262
What are the side effects of pyrazinamide?
Hepatotoxicity | Anaemia
263
What are side effects of isoniazid?
Slow acetylators at increased risk Peripheral neuropathy Hepatotoxicity
264
When is Rifampicin indicated?
Mycobacterium infection
265
What is MOA of rifampicin?
Inhibits DNA dependent RNA polymerase activity in bacillus
266
What are side effects of rifampicin?
Orange/ red body fluids | Hepatotoxicity
267
What is Fluconazole?
Anti-fungal
268
When is Fluconazole indicated?
Candidiasis - local or systemic
269
What is the MOA of fluconazole?
Inhibits fungal cytochrome P450 3A enzyme and Lanosine 14a demethylase Prevents conversion of lanosterol to ergosterol in fungal cell membrane
270
What are side effects of fluconazole?
Hepatotoxicity QT prolongation SJS/ TEN
271
What are the types of insulin?
``` Short acting (soluble) Intermediate (Isophane) Long acting (Insulin glargine or detemir) ```
272
When is insulin indicated?
Diabetes mellitus DKA Treatment of hyperkalaemia
273
What is the MOA of insulin?
Binds to insulin receptor Heterotetrameric protein consisting of 2 extracellular alpha units and 2 transmembrane beta units Binding of insulin causes: 1. Increased glucose uptake by muscle and adipose tissue through activation of glucose uptake channels 2. Increased anabolism - protein synthesis and fat synthesis
274
What are side effects of insulin?
Hypoglycaemia Weight gain Lipid atrophy at injection sites
275
What are examples of sulfonylureas?
Gliclazide
276
When are sulfonylureas indicated?
T2DM
277
What is MOA of sulfonylureas?
Binds to beta cell sulfonyl urea receptor (SUR1) Blocks ATP sensitive potassium channels Closure causes depolarisation and calmodulin activation Exocytosis of insulin containing secretory granules
278
What are side effects of sulfonylureas?
GI disturbance Weight gain Hypoglycaemia Hepatotoxicity (rare)
279
When is metformin indicated?
T2DM | PCOS
280
What is the MOA for metformin?
Decreases hepatic GNG | Inhibits hepatic mitochondrial glycerophosphate dehydrogenase
281
What are the side effects of metformin?
GI disturbance | Risk of lactic acidosis
282
When is the risk of lactic acidosis increased (from metformin)?
>65yo Renal impairment Iodine contrast HF
283
What are examples of SGLT2 inhibitors?
Canaglifozin | Dapaglifozin
284
When are SGLT2 inhibitors indicated?
T2DM monotherapy if metformin intolerant | In combination with other drugs for T2DM (except poglitazone)
285
What is MOA of SGLT2 inhibitors?
Reversible inhibition of renal PCT sodium glucose cotransporter 2
286
What are side effects of SGLT2 inhibitors?
UTI risk Hypoglycaemia DKA risk
287
What are examples of GLP-1 agonists?
Exenatide
288
When are GLP-1s indicated?
Second line treatment of T2DM in combination with other agents in px whom insulin therapy would be problematic BMI >35 or occupational reason to avoid insulin
289
What is MOA of GLP-1s?
Increased insulin secretion and decreased gastric emptying
290
What are side effects of GLP-1s?
Dyspepsia Hypoglycaemia Pancreatitis
291
What are examples of DPP-4 inhibitors?
Saxagliptin | Sitagliptin
292
When are DPP-4s inhibitors indicated?
T2DM monotherapy if metformin intolerant | In combination with other drugs for T2DM
293
What is MOA of DPP-4 inhibitors?
Inhibit DPP-4 to increase half life of endogenous gliptins | Increases insulin secretion and suppresses glucagon secretion
294
What are side effects of DPP-4 inhibitors?
``` GI upset Oedema Hypoglycaemia Abnormal lipids and increased triglycerides Pancreatitis ```
295
What are examples of glucocorticoids?
Hydrocortisone Prednisolone Dexamethasone
296
When are glucocorticoids indicated?
Replacement therapy in adrenal insufficiently or Addison's disease Immunosuppressive therapy Anti-inflammatory In combination with chemotherapy
297
What is MOA of glucocorticoids?
Binds with high affinity to specific cytoplasmic receptors Inhibition of leukocyte infiltration at site of inflammation Interference in function of mediators of inflammatory response and suppression of humoral immune responses
298
What are side effects of glucocorticoids?
``` Hypertension Oedema Hyperglycaemia Osteoporosis Cushing's syndrome Insomnia Psychosis Adrenal insufficiency risk up to 1y after withdrawal ```
299
What are examples of thyroid hormones?
Levothyroxine
300
When is levothyroxine indicated?
Hypothyroidism
301
What is the MOA of levothyroxine?
Converted to tri-idothyronine (T3) Binds to nuclear receptor proteins Affects transcription and production of specific proteins
302
What are side effects of levothyroxine?
``` Excessive dose may cause: Tachycardia Angina Tremor Heat intolerance Weakness Hair loss ```
303
What are antithyroid drugs?
Carbimazole
304
When is carbimazole indicated?
Hyperthyroidism
305
What is MOA of carbimazole?
Inhibits thyroxine iodination of tyrosyl residues in thyroglobulin Via inhibition of thyroperoxidase H2O2 complex
306
What are side effects of carbimazole?
Risk of neutropenia or agranulocytosis | Hypothyroidism if excessive dosing
307
What is important with px on carbimazole?
``` Px must be advised to immediately report any sx of: Fever Sore throat Bruising Mouth ulcers ```
308
What are examples of prostaglandins?
Misoprostol | Dinoprostone
309
When is Misoprostol indicated?
Medical termination of pregnancy | Labour induction in foetal death in utero
310
When is Dinoprostone indicated?
Induction of labour
311
What is the MOA of prostaglandins?
Exogenous prostaglandins ripens cervix
312
What are side effects of prostaglandins?
``` GI upset Severe uterine contractions Hypertension Bronchospasm Low APGAR scores ```
313
What are examples of oxytocin and ergometrine?
Symtometrine
314
When are oxytocin and ergometrine indicated?
Prevention and treatment of PPH
315
What is MOA of ergometrine?
Causes vasoconstriction via 5HT2 and 5HT1D receptors
316
What is MOA of oxytocin?
Increases uterine contractions | Can be used alone to induce or augment labour
317
What are side effects of oxytocin and ergometrine?
``` Dysrhythmias Hypertension Chest pain Pulmonary oedema Myocardial infarction Excessive uterine contractions ```
318
What are examples of the COCP?
Ethinylestradiol + Norethisterone
319
When is COCP indicated?
Contraception | Menstrual symptoms
320
What is the MOA of the ethinylestradiol?
Inhibits secretion of FSH via negative feedback on APG | Suppresses development of ovarian follicle
321
What is MOA of Norethisterone?
Inhibits secretion of LH and prevents ovulation | Makes cervical mucus less suitable for passage of sperm
322
What are side effects of COCP?
``` Risk of venous thromboembolism disease Hypertension Risk of stroke Liver impairment Increased risk of breast and cervical cancers ```
323
When is COCP contraindicated?
History of migraines History or family history of blood clots Oestrogen sensitivity - including cancer
324
What are examples of POP?
Norethisterone
325
When is POP indicated?
Contraception
326
What are side effects of POP?
Menstrual irregularities | Increased breast cancer risk
327
What are examples of anti-oestrogens?
Tamoxifen
328
When is Tamoxifen indicated?
ER positive breast cancer | Anovulatory infertility
329
What is MOA of Tamoxifen?
Selective oestrogen receptor modulator (SERM) Competes with endogenous oestrogens for oestrogen receptors Inhibits transcription of oestrogen responsive genes
330
What are side effects of Tamoxifen?
Increased endometrial changes Flushes PV bleeding
331
What are examples of bisphosphonates?
Alendronic acid
332
When are bisphosphonates indicated?
Treatment of osteoporosis | Prevention and treatment of steroid induced osteoporosis
333
What is MOA of bisphosphonates?
Osteoclast inhibitors | Slow rate of bone turnover
334
What are side effects of bisphosphonates?
``` Osteophagitis Dyspepsia GI upset Atypical femoral fractures Osteonecrosis of jaw ```
335
What are examples of NSAIDs?
Ibuprofen | Naproxen
336
When are NSAIDs indicated?
Pain relief in MSK disorders Post-operative analgesia Fever in children
337
What is MOA of NSAIDs?
Reduced pain and inflammation by reversibly inactivating COX Suppressing the production of prostaglandins
338
What is side effects of NSAIDs?
``` GI haemorrhage Hypertension HF AKI Asthma Increased risk of cardiovascular events ```
339
When is paracetamol indicated?
Mild to moderate pain relief | Treatment of pyrexia
340
What is the MOA of paracetamol?
COX inhibitor | Minimal anti-inflammatory
341
What are side effects of of paracetamol?
Hepatotoxicity
342
When is Allopurinol indicated?
Prophylaxis of gout Prophylaxis of renal stones Prophylaxis of post chemotherapy hyperuricaemia
343
What is MOA of allopurinol?
Reduces synthesis of uric acid Competitive inhibition of Xanthine oxidase Some inhibition of de novo purine synthesis Converted to alloxanthine by xanthine oxidase Metabolite remains in tissue for long time Is effective non-competitve inhibitor of enzyme So produces most therapeutic effect
344
What are side effects of allopurinol?
Risk of xanthioprine toxicity if concurrent use | Rash - WITHDRAW therapy if occurs due to SJS/TEN
345
When is colchicine indicated?
Treatment of acute gout Short term prophylaxis of gout during initiation of allopurinol (1month) Treatment of Familial Mediterranean syndrome
346
What is MOA of colchicine?
Inhibition of neutrophil-beta tubulin polymerisation | Prevents neutrophil activation, migration and degranulation
347
What are side effects of Colchicine?
GI disturbance
348
What are disease modifying agents used in rheumatoid disorders (DMARDs)?
Methotrexate
349
When is methotrexate indicated?
Rheumatoid arthritis Crohn's disease Oncology
350
What is MOA of methotrexate?
Immunomodulator Inhibits tetrahydrofolate dehydrogenase Prevents formation of tetrahydrofolate necessary for synthesis of thymidylate (essential DNA component)
351
What is to be noted about methotrexate?
Administered WEEKLY
352
What are side effects of methotrexate?
Bone marrow suppression Hepatotoxicity Pulmonary toxicity Plasma concentration increased by NSAIDs - toxicity risk
353
When is atropine indicated?
Cycloplegia | Anterior uveitis
354
What is MOA of atropine?
Antimuscarinic (antocholinergic) competitive antagonist of muscarinic acetylcholine receptors
355
What are side effects of of atropine?
Dilated pupil | Loss of accommodation
356
When is pilocarpine indicated?
Primary angle closure glaucoma
357
What is MOA of pilocarpine?
Tertiary amine muscarinic agonist | Opens drainage channels to trabecular network
358
What are side effects of pilocarpine?
Pin point pupils | Red sclera
359
When is Timolol indicated?
Reduce intra-ophthalmic pressure in primary angle closure glaucoma
360
What is MOA of Timolol?
Non selective beta blocker
361
What are side effects of Timolol?
Risk of bronchospasm | Risk of bradycardia
362
When is tropicamide indicated?
Aid fundoscopy
363
What is MOA of tropicamide?
Muscarinic (M4) antagonist Blocks response to iris sphincter muscle to iris and ciliary muscles to cholinergic stimulation Produces dilation of pupil and paralysis of ciliary muscles
364
What are examples of topical corticosteroids?
Mild - hydrocortisone Moderate - Betnovate Potent - Beclomethasone
365
When are topical corticosteroids indicated?
Treatment of inflammatory conditions: Eczema Dermatitis
366
What is MOA of topical corticosteroids?
Binds with high affinity to specific cytoplasmic receptors Provides inhibition of leukocyte infiltration at site of inflammation Interference in function of mediators of response and suppression of humoral immune responses
367
What are side effects of topical corticosteroids?
Potent steroids may be absorbed though skin --> systemic side effects Can have similar effects to glucocorticoids
368
When is activated charcoal indicated?
Reduction of absorption of poisons
369
What is MOA of activated charcoal?
Absorbs several drugs and toxins | Due to high surface area: volume
370
What is activated charcoal NOT effective for?
Toxic alcohols Heavy metals Hydrocarbons
371
What are side effects of activated charcoal?
Chemical pneumonitis risk
372
When should activated charcoal NOT be used?
When risk of aspiration
373
When is N-acetylcysteine indicated?
Treatment of paracetamol poisoning (hepatotoxicity)
374
What is MOA of NAC?
Restores hepatic concentrations of glutathione in early stages Affects other stages later
375
What are side effects of NAC?
GI disturbance | Anaphylactoid reactions - especially if low paracetamol concentrations
376
When is Naloxone indicated?
Treatment of opioid overdose
377
What is MOA of Naloxone?
Competitive antagonist at opioid receptors Binds at mu, delta and kappa Strongest binding is to mu
378
What are side effects of naloxone?
Risk of precipitating opioid withdrawal
379
What is to note about Naloxone?
Shorter half life than opioids of abuse | An infusion may be required

Core Formulary (11 decks)

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