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Core Formulary > Drugs > Flashcards

Drugs Flashcards

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
Q

What are side effects of antispasmodics?

A

Local irritant

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26
Q

What are examples of osmotic laxatives?

A

Lactulose

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27
Q

When are osmotic laxatives indicated?

A

Treatment or prevention of constipation

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28
Q

What is the MOA of osmotic laxatives?

A

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

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29
Q

What are side effects of osmotic laxatives?

A

Nausea
Vomiting
Abdominal discomfort

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30
Q

What are examples of stimulant laxatives?

A

Senna

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31
Q

When are stimulant laxatives indicated?

A

Treatment and prevention of constipation

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32
Q

What is the MOA of stimulant laxatives?

A

Directly stimulates myenteric plexus

Increased peristalsis and defecation

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33
Q

What are side effects of stimulant laxatives?

A

Abdominal cramps

Risk of hypoglycaemia with prolonged use

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34
Q

What are examples of anti-platelet drugs?

A

Aspirin

Clopidogrel

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35
Q

When is aspirin indicated?

A

CVD secondary prevention
Transient Ischaemic attack (with dipyridamole)
Acute stroke (14 days)
ACS

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36
Q

What is the MOA of aspirin?

A

Irreversible COX inhibition
Suppresses PGs and thromboxanes synthesis
Reduces platelet aggregation

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37
Q

What are side effects of aspirin?

A 
GI ulceration and irritation 
Bleeding 
Nephrotoxicity 
Hypertension 
Reye's syndrome
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38
Q

What is the link between aspirin and Reye’s syndrome?

A

Aspirin not to be used in children under 16yo

Unless for Kawasaki disease

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39
Q

When is clopidogrel indicated?

A

NSTEMI MI

Stroke (after 14 days of aspirin)

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40
Q

What is the MOA of aspirin?

A

Prodrug

Inhibits ADP dependent activation of GP1b/IIa receptor

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41
Q

What are the side effects of clopidogrel?

A

Dyspepsia
Bleeding
Diarrhoea

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42
Q

What are examples of ACEi?

A

Ramipril

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43
Q

When are ACEi indicated?

A

Hypertension (<55yo and not AfroC)
Heart failure
Nephropathy

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44
Q

What is the MOA of ramipril?

A

Competes with Ang I for ACE

Blocks conversion of AngI –> Ang II

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45
Q

What are the side effects of ramipril?

A

AKI if concurrent dehydration or NSAID use or if pre-existing renal artery stenosis
Cough (10%)
Angioedema risk

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46
Q

What are examples of Ang II receptor antagonist?

A

Lorsartan
Candarsartan
Valsartan

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47
Q

When are Ang II RA indicated?

A

Hypertension (<55yo and not AfroC)

Heart failure

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48
Q

What are the Ang II RA drugs used in heart failure?

A

Candasartan
Lorsartan
Valsartan

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49
Q

What is the MOA of Ang II RA?

A

Reduced Ang II vasoconstriction

Direct and competitive inhibition of AT1 and 2

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50
Q

What are side effects of Ang II RA?

A

AKI if concurrent dehydration or NSAID use or if pre-existing renal artery stenosis
Angioedema risk

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51
Q

What are examples of calcium channel blockers?

A

Amlodipine (dihydropiridine)

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52
Q

When are calcium channel blockers indicated?

A

Hypertension (>55 or AfroC)

Angina

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53
Q

What is the MOA of calcium channel blockers?

A

Vasodilation by L type Ca channel inhibition

Inhibits vascular smooth muscle cells contraction

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54
Q

What are side effects of calcium channel blockers?

A

Post venual dilation

Constipation

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55
Q

What are examples of thiazide like diuretics?

A

Indapamide

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56
Q

When are thiazide like diuretics indicated?

A

Hypertension (>55yo or AfroC)

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57
Q

What is the MOA of thiazide like diuretics?

A

Inhibits Cl- reabsorption at DCT via Na-Cl co-transporter

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58
Q

What are side effects of thiazide like diuretics?

A

Hyponatraemia
Hypokalaemia
Erectile dysfunction
Gout

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59
Q

What are examples of B adrenoreceptor blockers?

A

Bisoprolol

Propranolol

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60
Q

When are BB indicated?

A 
Angina 
Heart failure
Arryhythmia 
Anxiety (propranolol)
Symptomatic relief for hyperthyroidism (propranolol)
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61
Q

What is the MOA of BB?

A

Competitive antagonist of of catecholamines for binding at B adrenergic receptors

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62
Q

What is special about propranolol?

A

Lipid soluble

Penetrates CNS

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63
Q

What are side effects of BB?

A

Bronchospasm
Peripheral ischaemia
Erectile dysfunction

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64
Q

What are examples of statins?

A

Atorvastatin

Simvastatin

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65
Q

When are statins indicated?

A

Primary or secondary CVD prevention

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66
Q

What is the MOA of statins?

A

Hydrolysed to active metabolite
Competes HMG-CoA for HMG-CoA reductase
Reduces enzyme and quantity of mevalonic acid (cholsterol precursor)

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67
Q

What are side effects of statins?

A

Hyperglycaemia
Muscle toxicity (Raised CK, myopathy or rhabdomyolysis)
This is increased in elderly or hypothyroidism
Hepatotoxicity

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68
Q

What are examples of exogenous nitric oxide donors?

A

GTN spray

Isosorbide mononitrate

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69
Q

When are exogenous nitric oxide donors indicated?

A

Prophylaxis and treatment of angina

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70
Q

What is the MOA of exogenous nitric oxide donors?

A

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

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71
Q

What are side effects of exogenous nitric oxide donors?

A

Headache
Postural hypotension
Rapid tolerance

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72
Q

What needs to be ensured when using exogenous nitric oxide donors?

A

4-12 hours nitrate free period required daily to prevent loss of efficacy

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73
Q

What are examples of rate limiting calcium channel blockers?

A

Diltiazem

Verapamil

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74
Q

When are rate limiting calcium channel blockers indicated?

A

Narrow complex tachycardia
Angina
Hypertension

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75
Q

What is the MOA of rate limiting calcium channel blockers?

A

AVN conduction delay

Inhibits L type calcium channels

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76
Q

What are the side effects of rate limiting calcium channel blockers?

A

Risk of heart block - AVOID CONCURRENT BB USE
Negatively inotropic
Constipation

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77
Q

What are examples of antianginals?

A

Nicorandil (K)
Ivabradine (K)
Ranolazine (Na)

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78
Q

When are antianginals indicated?

A

Angina

2nd line if cannot tolerate BB or CCBs

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79
Q

What is the MOA of Nicorandil?

A

Combines Katp channel activation with NO donor

K+ channel!

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80
Q

What is the MOA of Ivabradine?

A

Sinus node Kf channel blocker

HCN

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81
Q

What is the MOA of Ranolazine?

A

Uncertain
Sodium channel blocker
Myocyte metabolic substrate utilisation

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82
Q

What are the side effects of Nicorandil?

A

Rectal bleeding

Flushing

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83
Q

What are the side effects of Ivabradine?

A

Bradycardia
Heart block
AF

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84
Q

What are the side effects of Ranolozine?

A

QT prolongation

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85
Q

What are examples of loop diuretics?

A

Furosemide

Bumetanide

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86
Q

When are loop diuretics indicated?

A

Symptomatic relief of pulmonary oedema

Peripheral oedema in HF or cirrhosis

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87
Q

What are the MOA of loop diuretics?

A

Inhibit Na+/K+?Cl- symporter within ascending LOH

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88
Q

What are the side effects of loop diuretics?

A 
Hypotension 
Hypokalaemia 
Hyponatraemia 
Ototoxicity (toxic to the ear)
Nephrotoxicity
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89
Q

When are aldosterone antagonists indicated?

A 
Primary hyperaldosteronism 
Secondary hyperaldosteronism 
- Heart failure
- Cirrhosis 
- Nephrotic syndrome
PCOS
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90
Q

What are examples of aldosterone antagonists?

A

Eplerenone

Spironolactone

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91
Q

What is the MOA of aldosterone antagonist?

A

Antagonist of intracellular mineralocorticoid receptor

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92
Q

What are side effects of aldosterone antagonist?

A

Hyperkalaemia
Hyponatraemia
Hepatotoxicity
Gynaecomastia

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93
Q

What are examples of parental anticoagulants?

A

Heparin
LMWH (Enoxaparin)
Fondaparinux

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94
Q

When are parental anticoagulants indicated?

A

Prophylaxis and treatment of venous thromboembolism

Treatment of ACS (LMWH and fondaparinux)

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95
Q

What is the MOA of parental anticoagulants?

A

Factor Xa inhibition

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96
Q

What is the MOA of heparin?

A

Factor Xa inhibition

Thrombin inhibitor

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97
Q

How is Heparin administered?

A

IV

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98
Q

How is LMWH administered?

A

SC

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99
Q

How is Fondaparinux administered?

A

SC

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100
Q

What are side effects of parental anticoagulants?

A

Bleeding
Purpurea (ITP)
Heparin induced thrombocytopenia (HIT)

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101
Q

What are examples of oral anticoagulants?

A 
Warfarin 
Novel oral anticoagulants
- Apixaban 
- Dabigatran 
- Rivaroxaban
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102
Q

When are oral anticoagulants indicated?

A

Prophylaxis and treatment of venous thromboembolism

Prevention of stroke and systemic emboli in AF

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103
Q

What is the MOA of Warfarin?

A

Inhibits VKOR

Inhibits synthesis of FII, VII, IV and X

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104
Q

What is the MOA of the DOACs?

A

Inhibit FXa

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105
Q

What are the side effects of oral anticoagulants?

A

Haemorrhage
Purpura (purple toes)
Skin necrosis

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106
Q

When is adrenaline indicated?

A 
Cardiac arrest (1/10,000)
Anaphylaxtic shock (1/100)
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107
Q

What is the MOA of adrenaline?

A

Beta > alpha adrenergic receptor agonist

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108
Q

What are the side effects of adrenaline?

A

Tachycardia
MI
Hypertension
Decreased placental blood flow

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109
Q

When is adenosine indicated?

A

Paroxysmal AVNRT / AVRT

Diagnosis of tachydysarrhythmias

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110
Q

What is the MOA of adenosine?

A

AV node conduction block
Short duration due to 8-10s half life
Increased if on dipyridamole or theophylline

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111
Q

What are the side effect of adenosine?

A

Arrhythmia
Angina
Headache
Flushing

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112
Q

When is Amiodarone indicated?

A

Treatment of narrow and broad complex tachycardias
AF
Atrial flutter

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113
Q

What is the MOA of amiodarone?

A

Class I-IV Vaugh Williams effects

Half life of 90 days

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114
Q

What are side effects of amiodarone?

A 
Hepatotoxicity
Pulmonary toxicity 
Hyper/Hypo thyroidism
Grey skin 
Corneal deposits
Multiple interactions
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115
Q

When is digoxin indicated?

A

Rate control in AF

HF

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116
Q

What is the MOA of digoxin?

A

Positive inotropic action and negative chronotropic action
Increase cytosolic calcium inhibition of Na+/K+?ATPase pump
And increased vagal tone

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117
Q

What are side effects of digoxin?

A

Narrow therapeutic index
GI disturbance
Yellow vision
Dysarrhythmias

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118
Q

What are examples of fibrinolytic drugs?

A

Alteplase

Streptokinase

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119
Q

When are fibrinolytic drugs indicated?

A

Acute STEMI
Acute ischaemic stroke
Compromised PE

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120
Q

What is the MOA of fibrinolytic drugs?

A

Activate plasminogen to plasmin

Degrades fibrin clot

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121
Q

What are the side effects of fibrinolytic drugs?

A

Haemorrhage

High risk of mortality or morbidity in intracranial bleeds

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122
Q

What are examples of short acting inhaled Beta 2 agonists?

A

Salbutamol

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123
Q

What are examples of long acting Beta 2 agonists?

A

Salmeterol

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124
Q

When are Beta 2 agonists indicated?

A

Asthma
COPD
Premature labour

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125
Q

How is salbutamol used?

A

IV as tocolytic agent (anti-contraction)

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126
Q

What is the MOA of beta 2 agonists?

A

Specific beta 2 agonist

Causes bronchodilation through smooth muscle relaxation

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127
Q

What are important side effects of beta 2 agonists?

A

Tremor
Headache
Hypokalaemia

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128
Q

What are examples of antimuscarinic bronchodilators?

A

Ipratropium

Tiotropium

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129
Q

When are antimuscarinic bronchodilators indicated?

A

Asthma

COPD

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130
Q

What is the MOA of antimuscarinic bronchodilators?

A

Inhibit M1-3 muscarinic receptors

Causes bronchodilation through smooth muscle relaxation

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131
Q

What are side effects of antimuscarinic bronchodilators?

A

Dry mouth

GI upset

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132
Q

What are examples of inhaled corticosteroids?

A

Beclometasone

Fluticasone

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133
Q

When are corticosteroids indicated?

A

Asthma

COPD

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134
Q

What is the MOA of inhaled corticosteroids?

A

Binds with highly affinity to specific cytoplasmic receptors
Produce inhibition of leukocytes infiltration
Interference in function of mediators and suppression of humoral immune responses

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135
Q

What are the side effects of inhaled corticosteroids?

A

Paroxysmal bronchoconstriction
Oral thrush
Adrenal suppression risk
Potential risk of reduced growth velocity in children
Increased risk of pneumonia in COPD patients

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136
Q

When is Theophylline indicated?

A

Asthma

COPD

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137
Q

What is the MOA of Theophylline?

A

Inhibits cAMP degradation

Causes bronchodilation through smooth muscle relaxation

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138
Q

What are the side effects of Theophylline?

A 
Narrow therapeutic index
GI upset
Tachycardia 
Headache 
Convulsions 
Hypokalaemia 
Hyperglycaemia
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139
Q

When is oxygen indicated?

A

Treatment of hypoxaemia

Palliation of dyspnoea

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140
Q

What is the MOA of oxygen?

A

Final electron acceptor in cellular metabolism

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141
Q

What is to note with oxygen?

A

Contraindicated in paraquat poisoning

Risk of free radical generation

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142
Q

What are side effects of oxygen?

A

Loss of hypoxic drive causing type II respiratory failure

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143
Q

What are examples of antihistamines?

A

Chlorphenamine

Loratadine

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144
Q

When are antihistamines indicated?

A

Symptomatic relief of allergies

Emergency treatment of anaphylaxis (chlorphenamine)

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145
Q

What is the MOA of antihistamines?

A

Inhibition of H1 receptors

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146
Q

What are the side effects of antihistamines?

A

Sedation, enhanced with alcohol
Dysarrhythmias
Antimuscarinic effects

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147
Q

What are examples of opioid analgesics?

A

Codeine
Morphine
Methadone
Pethidine

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148
Q

When are opioid analgesics indicated?

A 
Moderate pain - codeine 
Severe pain - morphine 
Treatment of opioid dependence - methadone 
Obstetric pain relief - pethidine 
Biliary colic - pethidine
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149
Q

Why is pethidine used in obstetrics?

A

Decreased risk of neonatal respiratory suppression

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150
Q

What is the MOA of opioid analgesics?

A

Opioid receptor agonist
Codeine metabolised to morphine by CYP2D6
2D6 is under genetic control, may cause apparent lack of efficacy in individuals

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151
Q

What is the difference between methadone and morphine?

A

Methadone is less sedating than morphine

Methadone has a longer half life

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152
Q

What are side effects of opioid analgesics?

A 
Sedation or coma 
Respiratory depression 
Constipation 
QT prolongation (methadone)
Hyperprolactinaemia
153
Q

What are examples of antiemetic drugs?

A

Antihistamines - Cyclizine or promethazine in pregnancy
Phenothiazines - metodopramide
5HT3 antagonists - Ondanestrone

154
Q

When are antiemetics indicated?

A

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
Q

What is the MOA of antiemetics?

A

Antagonist to receptors represent in CTZ
Dopamine and muscarinic receptors
5HT receptors are present within GI tract too

156
Q

What are side effects of antihistamines (as antiemetics)?

A

Sedation

Other antimuscarinic effects

157
Q

What are the side effects of metochlorpramide (phenothiazine)?

A

Risk of occulo-gyric crisis

Extra pyramidal features

158
Q

What are side effects of 5HT3 antagonists (as antiemetics)?

A

Constipation

Flushing

159
Q

What are examples of anti-epileptic drugs?

A

Sodium valporate
Carbamazepine
Lamotrigine

160
Q

When are anti-epileptic drugs indicated?

A 
Focal seizures (carbamazepine and lamotrigine)
Generalised seizures (sodium valporate or lamotrigine)
161
Q

What is the MOA of anti-epileptic Carbamazepine?

A

Voltage operated sodium ion channel inhibitor
Strong hepatic enzyme inducer
Reduces half life from 30h-15h

162
Q

What is the MOA of anti-epileptic Sodium valporate?

A

Sodium and calcium ion channel blocker

Increases GABA in the CNS

163
Q

What is the MOA of anti-epileptic lamotrigine?

A

Potent sodium channel blocker

164
Q

What are side effects of anti-epileptic Carbamazepine?

A

Sedation
Ataxia
Leukopenia
Hepatotoxicity

165
Q

What are side effects of anti-epileptic Sodium valporate?

A

Alopecia
Weight gain
Teratogenic

166
Q

What are side effects of anti-epileptic lamotrigine?

A

Sedation

Rash and dizziness

167
Q

What is to be noted about anti-epileptic lamotrigine?

A

Valporate may increase plasma concentration of lamotrigine to toxic concentrations

168
Q

What are examples of antimigraine drugs?

A

Sumatriptan

169
Q

When are antimigraine drugs indicated?

A

Treatment of acute migraine or cluster headache

170
Q

What is the MOA of antimigraine drugs?

A

5HT1 receptor agonist

171
Q

When should antimigraine drugs be avoided?

A

Avoid if previous CVA or TIA or hypertension

172
Q

What are side effects of antimigraine drugs?

A

Vasoconstriction
Sedation
Dyshythmias
Raynaud’s

173
Q

What are drugs used in Parkinsonism?

A
  • Levodopa + peripheral dopa-decarboxylase inhibitor (co-beneldopa)
  • Ropinirole –Dopamine receptor agonists
  • Monoamine Oxidase B inhibitors (Selegiline)
174
Q

What is the MOA of Levodopa?

A

Dopamine precursor

Given with peripheral dopa-decarboxylase inhibitor to minimise peripheral side effects

175
Q

What is the MOA of Ropinirole?

A

Direct acting dopamine receptor agonist

176
Q

What is the MOA of Monoamine oxidase B inhibitor / Selegiline?

A

Increase availability of dopamine in CNS

May also reduce the end of dose effects in advanced Parkinson’s

177
Q

What are side effects of levodopa?

A

Psychosis and dementia
Postural hypotension
Dysrhythmias
Dry mouth

178
Q

What are side effects of Ropinirole?

A

Impulse disorders such as pathological gambling, binge eating and hypersexuality
Confusion
Hallucinations

179
Q

What are side effects of Selegiline?

A

Ulcers
Hypotensions
Sedation
Confusion

180
Q

What are drugs used for dementia?

A

Acetylcholinesterase inhibitors

Glutamate receptor antagonists

181
Q

What are examples of Acetylcholinesterase inhibitors?

A

Donepezil
Galantamine
Rivastigmine

182
Q

What are examples of Glutamate receptor antagonists?

A

Memantine

183
Q

When are Acetylcholinersterase inhibitors indicated?

A

Mild to moderate dementia

Rivastigmine is licensed for dementia in Parkinson’s

184
Q

When is memantine indicated?

A

Moderate to severe dementia

185
Q

What is the MOA of acetylcholinesterase inhibitors?

A

Increase in ACh through reversible inhibition of enzyme degradation

186
Q

How else does Rivistagmine act?

A

Non competitive agonist

187
Q

How else does Galantamine act?

A

Nicotinic receptor agonist

188
Q

What are side effects of acetylcholinesterase inhibitors?

A 
Cholinergic effects
Syncope
Hallucinations 
Aggression 
Incontinence 
Heart block 
Seizures
189
Q

What are the side effects of Memantine?

A 
Hypertension 
Heart failure 
Thrombosis 
Psychosis 
Suicidal intent
190
Q

What are examples of anxiolytics?

A

Diazepam

Lorazepam

191
Q

When are anxiolytics indicated?

A

Acute alcohol withdrawal
Acute drug induced dystonic reactions
Status epilepticus
Short term use in anxiety or insomnia

192
Q

What is the MOA of anxiolytics?

A

BZD act on GABAa receptors

Facilitate opening of GABA-activated chloride channels

193
Q

What are the side effects of anxiolytics?

A 
Drowsiness
Confusion 
Ataxia 
Dependence 
Paradoxical aggression
194
Q

What is to note with the side effects of anxiolytics?

A

Side effects may be enhanced with alcohol

195
Q

What are antipsychotics used?

A

1st generation - typical

2nd generation - atypical

196
Q

What are examples of 1st generation antipsychotics?

A

Haloperidol

197
Q

What are examples of 2nd generation antipsychotics?

A

Olanzapine

Clozapine

198
Q

When are antipsychotics indicated?

A

Treatment of schizophrenia or psychosis

Haloperidol may be used to manage aggression in organic brain disorders

199
Q

What is MOA of typical antipsychotics?

A

Dopamine D2 receptor antagonists

Non selective so there are no extrapyramidal side effects

200
Q

What is the MOA of atypical antipsychotics?

A

Antagonises D1, D2, D4, 5HT2 and H1 and muscarinic receptors

201
Q

What are side effects of antipsychotics?

A

Extra pyramidal features
Hypotension
QT prolongation (ECG requires prior to treatment)

202
Q

What are extrapyramidal side effects?

A

Parkinsonism
Dystonia
Akathesis
Tardive dyskinesia

203
Q

What are side effects of atypical antipsychotics?

A

Hyperlipidaemia
Glucose intolerance
Weight gain
Bone marrow suppression – especially clozapine

204
Q

What are drugs used for bipolar disorder or mania?

A

Lithium salts

205
Q

When are lithium salts indicated?

A

Treatment and prophylaxis of mania or bipolar disorder

206
Q

What is the MOA of lithium salts?

A

Lithium ions permeate voltage gated sodium ion channels
Accumulate within the cytosol
Effect several intracellular signalling pathways and cAMP production

207
Q

What are the side effects of lithium salts?

A 
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
Q

What are examples of SSRIs

A

Fluoxetine

Citalopram

209
Q

When are SSRIs indicated?

A

Depressive illness
Panic disorders (citalopram)
Bulimia (fluoxetine)
OCD (fluoxetine)

210
Q

What is the MOA of SSRIs?

A

Increase synaptic concentration of 5-hydroxytrytaphan through inhibition of re-uptake transporter

211
Q

What are the side effects of SSRIs?

A

Hyponatraemia (especially in the elderly)
Risk of serotonin syndrome with other seretonergic drugs
Risk of suicidal idealisation in children

212
Q

What are examples of TCAs?

A

Amitriptyline

213
Q

When are TCAs indicated?

A

NO LONGER RECOMMENDED FOR DEPRESSION DUE TO TOXICITY IN OVERDOSE

Unlicensed use in neuropathic pain and migraine prophylaxis

214
Q

What is the MOA of TCAs?

A

Muscarinic and voltage gated sodium ion channel antagonist
Increases 5HT and catecholamine concentrations in CNS
Inhibits re-uptake transporters

215
Q

What are the side effects of TCAs?

A

Antichol ?

216
Q

What are examples of Beta -lactams ?

A 
PENICILLINS 
Amoxicillin 
Amoxicillin + clavulanic acid (co amoxiclav)
Benzylpenicillin (Pen G)
Flucloxacillin
217
Q

When are beta lactams indicated?

A

Gram + and Gram - organisms

218
Q

When is amoxicillin indicated?

A

Oral infections
Lyme disease
Anthrax and H.pylori eradication

219
Q

When is Co-amoxiclav indicated?

A 
Active against beta lactamase producing organisms
LRTIs
Joint or bone infections
Animal bites
GU infections
220
Q

What is the MOA of beta lactam antibiotics?

A

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
Q

What is to be noted about Benzylpenicillin?

A

Not effective orally

222
Q

What is to be noted about Clavulanate?

A

Competitively and irreversibly inhibits wide variety of beta lactamases produced by certain bacteria
Makes drug more potent

223
Q

What is to be noted about Flucloxacillin?

A

Stable against hydrolysis by variety of beta lactamases

Including penicillinases and cephalosporinases and extended spectrum beta lactamases

224
Q

What are side effects of beta lactams?

A

GI disturbance
Type I and IV hypersensitivity reactions
Cholestatic jaundice associated with co-amoxiclav use

225
Q

What are examples of quinolones?

A

Ciprofloxacin

226
Q

When are Quinolones indicated?

A 
Gram + and - bacteria 
Pseudomonas
Chlamydia 
Gonorrhoea 
Typhoid
227
Q

What is the MOA of quinolones?

A

Bacteriocidal

Inhibition of bacterial DNA enzyme topoisomerases II (DNA gyrase) and IV

228
Q

What are side effects of quinolones?

A 
Tendon rupture (elderly)
Decreased seizure threshold 
Peripheral neuropathy 
Hypoglycaemia 
High c.diff risk
229
Q

What are examples of cephalosporins?

A

Cefotaxime

230
Q

When are cephalosporins indicated?

A 
Septicaemia 
Pneumonias 
Biliary tract infections
Meningitis 
Epiglottitis 
Gonorrhoea
231
Q

What is MOA of cephalosporins?

A

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
Q

What are side effects of cephalosporins?

A

10% cross over hypersensitivity risk of penicillin allergic

High C.diff risk

233
Q

What are examples of Macrolide antiobiotics?

A

Clarithromycin

234
Q

When are macrolide antibiotics indicated?

A

Similar antimicrobial spectrum to penicillin and atypical pneumonias and campyobacter

235
Q

What is MOA of macrolide antibiotics?

A

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
Q

What are side effects of macrolides?

A

QT prolongation

Steven Johnson Syndrome / Toxic Epidermal Necrosis

237
Q

What are examples of aminoglycosides?

A

Gentamicin

238
Q

When are aminoglycosides indicated?

A

Septicaemia secondary to gram - and some +

239
Q

What is MOA of aminoglycosides?

A

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
Q

What are side effects of aminoglycosides?

A

Narrow therapeutic index
Nephrotoxicity
Irreversible ototoxicity

241
Q

When is nitrofurantoin indicated?

A

UTIs

242
Q

What is the MOA of nitrofurantoin?

A

Inhibits bacterial acetyl-coenzyme A
Interferes with organism’s carb metabolism
Can disrupt bacterial cell wall formation

243
Q

What are side effects of nitrofurantoin?

A

Pulmonary fibrosis
Retroperitoneal fibrosis
Peripheral neuropathy

244
Q

When is trimethoprim indicated?

A

UTIs
Bronchitis
PCP (pneumocytosis pneumonia)

245
Q

What is MOA of trimethoprim?

A

Bacterial dihydrofolate reductase inhibitor

Reduces folate metabolism

246
Q

What are side effects of trimethoprim?

A

Hyperkalaemia

247
Q

What are examples of glycopeptides?

A

Vancomycin

248
Q

When are glycopeptides indicated?

A

Gram + cocci

C.diff oral

249
Q

What is MOA of glycopeptides?

A

Glycopeptide antibiotic which acts by inhibiting cell wall synthesis

250
Q

What are side effects of glycopeptides?

A

Nephrotoxic
Ototoxic
Red man syndrome

251
Q

When is metronidazole indicated?

A

Anaerobic infections
Protozoal infections
H.pylori infection
Crohn’s disease

252
Q

What is MOA of metronidazole?

A

Reduced metronidazole disrupts DNAs helical structure
Inhibits bacterial nucleic acid synthesis
Results in bacterial cell death

253
Q

What are side effects of metronidazole?

A

Disulfram like reaction with alcohol

254
Q

When are anti-tuberculosis medications used?

A

Ethambutol
Isoniazid
Pyrazinamide
Rifampicin

255
Q

When is ethambutol indicated?

A

Mycobacterium infection

256
Q

What is MOA of ethambutol?

A

Inhibits transfer of mycolic acids into cell wall of tubercle bacillus

257
Q

What are side effects of ethambutol?

A

Optic neuritis

Red/Green colour blindness

258
Q

When is isoniazid indicated?

A

Mycobacterium infection

259
Q

What is MOA of isoniazid?

A

Prodrug

Once inactivated, inhibits synthesis of mycolic acids

260
Q

When is pyrazinamide indicated?

A

Mycobacterium infection

261
Q

What is the MOA of pyrazinamide?

A

Mechanism unclear
Metabolite (pyrazinoic acid) may lower intrabacterial pH
To level that could inactivate vital target enzyme

262
Q

What are the side effects of pyrazinamide?

A

Hepatotoxicity

Anaemia

263
Q

What are side effects of isoniazid?

A

Slow acetylators at increased risk
Peripheral neuropathy
Hepatotoxicity

264
Q

When is Rifampicin indicated?

A

Mycobacterium infection

265
Q

What is MOA of rifampicin?

A

Inhibits DNA dependent RNA polymerase activity in bacillus

266
Q

What are side effects of rifampicin?

A

Orange/ red body fluids

Hepatotoxicity

267
Q

What is Fluconazole?

A

Anti-fungal

268
Q

When is Fluconazole indicated?

A

Candidiasis - local or systemic

269
Q

What is the MOA of fluconazole?

A

Inhibits fungal cytochrome P450 3A enzyme and Lanosine 14a demethylase
Prevents conversion of lanosterol to ergosterol in fungal cell membrane

270
Q

What are side effects of fluconazole?

A

Hepatotoxicity
QT prolongation
SJS/ TEN

271
Q

What are the types of insulin?

A 
Short acting (soluble)
Intermediate (Isophane)
Long acting (Insulin glargine or detemir)
272
Q

When is insulin indicated?

A

Diabetes mellitus
DKA
Treatment of hyperkalaemia

273
Q

What is the MOA of insulin?

A

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
Q

What are side effects of insulin?

A

Hypoglycaemia
Weight gain
Lipid atrophy at injection sites

275
Q

What are examples of sulfonylureas?

A

Gliclazide

276
Q

When are sulfonylureas indicated?

A

T2DM

277
Q

What is MOA of sulfonylureas?

A

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
Q

What are side effects of sulfonylureas?

A

GI disturbance
Weight gain
Hypoglycaemia
Hepatotoxicity (rare)

279
Q

When is metformin indicated?

A

T2DM

PCOS

280
Q

What is the MOA for metformin?

A

Decreases hepatic GNG

Inhibits hepatic mitochondrial glycerophosphate dehydrogenase

281
Q

What are the side effects of metformin?

A

GI disturbance

Risk of lactic acidosis

282
Q

When is the risk of lactic acidosis increased (from metformin)?

A

> 65yo
Renal impairment
Iodine contrast
HF

283
Q

What are examples of SGLT2 inhibitors?

A

Canaglifozin

Dapaglifozin

284
Q

When are SGLT2 inhibitors indicated?

A

T2DM monotherapy if metformin intolerant

In combination with other drugs for T2DM (except poglitazone)

285
Q

What is MOA of SGLT2 inhibitors?

A

Reversible inhibition of renal PCT sodium glucose cotransporter 2

286
Q

What are side effects of SGLT2 inhibitors?

A

UTI risk
Hypoglycaemia
DKA risk

287
Q

What are examples of GLP-1 agonists?

A

Exenatide

288
Q

When are GLP-1s indicated?

A

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
Q

What is MOA of GLP-1s?

A

Increased insulin secretion and decreased gastric emptying

290
Q

What are side effects of GLP-1s?

A

Dyspepsia
Hypoglycaemia
Pancreatitis

291
Q

What are examples of DPP-4 inhibitors?

A

Saxagliptin

Sitagliptin

292
Q

When are DPP-4s inhibitors indicated?

A

T2DM monotherapy if metformin intolerant

In combination with other drugs for T2DM

293
Q

What is MOA of DPP-4 inhibitors?

A

Inhibit DPP-4 to increase half life of endogenous gliptins

Increases insulin secretion and suppresses glucagon secretion

294
Q

What are side effects of DPP-4 inhibitors?

A 
GI upset 
Oedema 
Hypoglycaemia 
Abnormal lipids and increased triglycerides
Pancreatitis
295
Q

What are examples of glucocorticoids?

A

Hydrocortisone
Prednisolone
Dexamethasone

296
Q

When are glucocorticoids indicated?

A

Replacement therapy in adrenal insufficiently or Addison’s disease
Immunosuppressive therapy
Anti-inflammatory
In combination with chemotherapy

297
Q

What is MOA of glucocorticoids?

A

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
Q

What are side effects of glucocorticoids?

A 
Hypertension 
Oedema 
Hyperglycaemia 
Osteoporosis 
Cushing's syndrome 
Insomnia 
Psychosis 
Adrenal insufficiency risk up to 1y after withdrawal
299
Q

What are examples of thyroid hormones?

A

Levothyroxine

300
Q

When is levothyroxine indicated?

A

Hypothyroidism

301
Q

What is the MOA of levothyroxine?

A

Converted to tri-idothyronine (T3)
Binds to nuclear receptor proteins
Affects transcription and production of specific proteins

302
Q

What are side effects of levothyroxine?

A 
Excessive dose may cause:
Tachycardia
Angina 
Tremor 
Heat intolerance 
Weakness 
Hair loss
303
Q

What are antithyroid drugs?

A

Carbimazole

304
Q

When is carbimazole indicated?

A

Hyperthyroidism

305
Q

What is MOA of carbimazole?

A

Inhibits thyroxine iodination of tyrosyl residues in thyroglobulin
Via inhibition of thyroperoxidase H2O2 complex

306
Q

What are side effects of carbimazole?

A

Risk of neutropenia or agranulocytosis

Hypothyroidism if excessive dosing

307
Q

What is important with px on carbimazole?

A 
Px must be advised to immediately report any sx of:
Fever
Sore throat 
Bruising 
Mouth ulcers
308
Q

What are examples of prostaglandins?

A

Misoprostol

Dinoprostone

309
Q

When is Misoprostol indicated?

A

Medical termination of pregnancy

Labour induction in foetal death in utero

310
Q

When is Dinoprostone indicated?

A

Induction of labour

311
Q

What is the MOA of prostaglandins?

A

Exogenous prostaglandins ripens cervix

312
Q

What are side effects of prostaglandins?

A 
GI upset
Severe uterine contractions 
Hypertension 
Bronchospasm 
Low APGAR scores
313
Q

What are examples of oxytocin and ergometrine?

A

Symtometrine

314
Q

When are oxytocin and ergometrine indicated?

A

Prevention and treatment of PPH

315
Q

What is MOA of ergometrine?

A

Causes vasoconstriction via 5HT2 and 5HT1D receptors

316
Q

What is MOA of oxytocin?

A

Increases uterine contractions

Can be used alone to induce or augment labour

317
Q

What are side effects of oxytocin and ergometrine?

A 
Dysrhythmias 
Hypertension 
Chest pain 
Pulmonary oedema 
Myocardial infarction 
Excessive uterine contractions
318
Q

What are examples of the COCP?

A

Ethinylestradiol + Norethisterone

319
Q

When is COCP indicated?

A

Contraception

Menstrual symptoms

320
Q

What is the MOA of the ethinylestradiol?

A

Inhibits secretion of FSH via negative feedback on APG

Suppresses development of ovarian follicle

321
Q

What is MOA of Norethisterone?

A

Inhibits secretion of LH and prevents ovulation

Makes cervical mucus less suitable for passage of sperm

322
Q

What are side effects of COCP?

A 
Risk of venous thromboembolism disease
Hypertension 
Risk of stroke
Liver impairment 
Increased risk of breast and cervical cancers
323
Q

When is COCP contraindicated?

A

History of migraines
History or family history of blood clots
Oestrogen sensitivity - including cancer

324
Q

What are examples of POP?

A

Norethisterone

325
Q

When is POP indicated?

A

Contraception

326
Q

What are side effects of POP?

A

Menstrual irregularities

Increased breast cancer risk

327
Q

What are examples of anti-oestrogens?

A

Tamoxifen

328
Q

When is Tamoxifen indicated?

A

ER positive breast cancer

Anovulatory infertility

329
Q

What is MOA of Tamoxifen?

A

Selective oestrogen receptor modulator (SERM)
Competes with endogenous oestrogens for oestrogen receptors
Inhibits transcription of oestrogen responsive genes

330
Q

What are side effects of Tamoxifen?

A

Increased endometrial changes
Flushes
PV bleeding

331
Q

What are examples of bisphosphonates?

A

Alendronic acid

332
Q

When are bisphosphonates indicated?

A

Treatment of osteoporosis

Prevention and treatment of steroid induced osteoporosis

333
Q

What is MOA of bisphosphonates?

A

Osteoclast inhibitors

Slow rate of bone turnover

334
Q

What are side effects of bisphosphonates?

A 
Osteophagitis 
Dyspepsia 
GI upset
Atypical femoral fractures 
Osteonecrosis of jaw
335
Q

What are examples of NSAIDs?

A

Ibuprofen

Naproxen

336
Q

When are NSAIDs indicated?

A

Pain relief in MSK disorders
Post-operative analgesia
Fever in children

337
Q

What is MOA of NSAIDs?

A

Reduced pain and inflammation by reversibly inactivating COX
Suppressing the production of prostaglandins

338
Q

What is side effects of NSAIDs?

A 
GI haemorrhage 
Hypertension 
HF
AKI
Asthma
Increased risk of cardiovascular events
339
Q

When is paracetamol indicated?

A

Mild to moderate pain relief

Treatment of pyrexia

340
Q

What is the MOA of paracetamol?

A

COX inhibitor

Minimal anti-inflammatory

341
Q

What are side effects of of paracetamol?

A

Hepatotoxicity

342
Q

When is Allopurinol indicated?

A

Prophylaxis of gout
Prophylaxis of renal stones
Prophylaxis of post chemotherapy hyperuricaemia

343
Q

What is MOA of allopurinol?

A

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
Q

What are side effects of allopurinol?

A

Risk of xanthioprine toxicity if concurrent use

Rash - WITHDRAW therapy if occurs due to SJS/TEN

345
Q

When is colchicine indicated?

A

Treatment of acute gout
Short term prophylaxis of gout during initiation of allopurinol (1month)
Treatment of Familial Mediterranean syndrome

346
Q

What is MOA of colchicine?

A

Inhibition of neutrophil-beta tubulin polymerisation

Prevents neutrophil activation, migration and degranulation

347
Q

What are side effects of Colchicine?

A

GI disturbance

348
Q

What are disease modifying agents used in rheumatoid disorders (DMARDs)?

A

Methotrexate

349
Q

When is methotrexate indicated?

A

Rheumatoid arthritis
Crohn’s disease
Oncology

350
Q

What is MOA of methotrexate?

A

Immunomodulator
Inhibits tetrahydrofolate dehydrogenase
Prevents formation of tetrahydrofolate necessary for synthesis of thymidylate (essential DNA component)

351
Q

What is to be noted about methotrexate?

A

Administered WEEKLY

352
Q

What are side effects of methotrexate?

A

Bone marrow suppression
Hepatotoxicity
Pulmonary toxicity

Plasma concentration increased by NSAIDs - toxicity risk

353
Q

When is atropine indicated?

A

Cycloplegia

Anterior uveitis

354
Q

What is MOA of atropine?

A

Antimuscarinic (antocholinergic) competitive antagonist of muscarinic acetylcholine receptors

355
Q

What are side effects of of atropine?

A

Dilated pupil

Loss of accommodation

356
Q

When is pilocarpine indicated?

A

Primary angle closure glaucoma

357
Q

What is MOA of pilocarpine?

A

Tertiary amine muscarinic agonist

Opens drainage channels to trabecular network

358
Q

What are side effects of pilocarpine?

A

Pin point pupils

Red sclera

359
Q

When is Timolol indicated?

A

Reduce intra-ophthalmic pressure in primary angle closure glaucoma

360
Q

What is MOA of Timolol?

A

Non selective beta blocker

361
Q

What are side effects of Timolol?

A

Risk of bronchospasm

Risk of bradycardia

362
Q

When is tropicamide indicated?

A

Aid fundoscopy

363
Q

What is MOA of tropicamide?

A

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
Q

What are examples of topical corticosteroids?

A

Mild - hydrocortisone
Moderate - Betnovate
Potent - Beclomethasone

365
Q

When are topical corticosteroids indicated?

A

Treatment of inflammatory conditions:
Eczema
Dermatitis

366
Q

What is MOA of topical corticosteroids?

A

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
Q

What are side effects of topical corticosteroids?

A

Potent steroids may be absorbed though skin –> systemic side effects

Can have similar effects to glucocorticoids

368
Q

When is activated charcoal indicated?

A

Reduction of absorption of poisons

369
Q

What is MOA of activated charcoal?

A

Absorbs several drugs and toxins

Due to high surface area: volume

370
Q

What is activated charcoal NOT effective for?

A

Toxic alcohols
Heavy metals
Hydrocarbons

371
Q

What are side effects of activated charcoal?

A

Chemical pneumonitis risk

372
Q

When should activated charcoal NOT be used?

A

When risk of aspiration

373
Q

When is N-acetylcysteine indicated?

A

Treatment of paracetamol poisoning (hepatotoxicity)

374
Q

What is MOA of NAC?

A

Restores hepatic concentrations of glutathione in early stages
Affects other stages later

375
Q

What are side effects of NAC?

A

GI disturbance

Anaphylactoid reactions - especially if low paracetamol concentrations

376
Q

When is Naloxone indicated?

A

Treatment of opioid overdose

377
Q

What is MOA of Naloxone?

A

Competitive antagonist at opioid receptors
Binds at mu, delta and kappa
Strongest binding is to mu

378
Q

What are side effects of naloxone?

A

Risk of precipitating opioid withdrawal

379
Q

What is to note about Naloxone?

A

Shorter half life than opioids of abuse

An infusion may be required

Core Formulary (11 decks)

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