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Pharmacology > 50+ Drugs > Flashcards

50+ Drugs Flashcards

1
Q

What are the indications for the use of aspirin?

A

Secondary prevention of thrombotic events

Pain relief

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2
Q

What is the mechanism of action of aspirin?

A

Irreversible inactivation of cyclooxyrgenase COX enzyme
This reduces platelet thromboxane production and endothelial prostaglandin production
Reduced thromboxane production reduces platelet aggregation and thrombus formation
Reduced prostaglandin synthesis decreases nociceptive sensitisation and inflammation

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3
Q

What are the side effects of aspirin?

A 
Bleeding 
Peptic ulceration
Angiooedema
Broncospasm
Reye's syndrome
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4
Q

The pharmacokinetics of aspirin may be non-linear with overdose T/F?

A

True

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5
Q

What drug might be prescribed alongside aspirin?

A

Proton pump inhibitor

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6
Q

To which class of drugs does aspirin belong?

A

Anti platelet

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7
Q

What are the side effects of clopidogrel?

A

Bleeding
Abdominal pain
Diarrhoea

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8
Q

When should clopidogrel be avoided?

A

Liver failure

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9
Q

What are the side effects of tissue plasminogen activators?

A

Bleeding

Allergic reaction /angiooedema

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10
Q

Which tissue plasminogen activator is given as a single bolus?

A

Tenecteplase

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11
Q

Which tissue plasminogen activator is given as a bolus and infusion?

A

Alteplase

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12
Q

Which anticoagulant is used in haemodialysis?

A

Heparin

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13
Q

What are the side effects of heparins?

A

Bleeding
Heparin induced thrombocytopenia
Osteoporosis

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14
Q

Unfractionated heparinshave complex pharmacokinetics. What is the practical relevance of this?

A

Heparins require therapeutic drug monitoring

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15
Q

How is therapeutic drug monitoring of unfractionated heparin conducted?

A

APTT

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16
Q

How can the anticoagulant effect of heparin be reversed?

A

Protamine

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17
Q

Unfractionated heparin has a shorter duration of action than low molecular weight heparin. T/F?

A

True

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18
Q

What are the side effects of warfarin?

A

Bleeding
Warfarin necrosis
Osteoporosis

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19
Q

How is therapeutic drug monitoring of warfarin conducted?

A

INR

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20
Q

What over the counter drug should patients on warfarin be advised not to use?

A

Aspirin

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21
Q

What are the side effects of dabigatran?

A

Bleeding

Dyspepsia

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22
Q

What are the side effects of rivaroxaban and apixaban?

A

Bleeding

Nausea

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23
Q

What are the indications of rivaroxaban?

A

Prophylaxis of vTE (especially if post-op)
Thromboprofylaxis in non-valvular AF
Treatment of VTE

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24
Q

What enzyme system metabolises rivaroxaban and apixaban but not dabigatran?

A

CYP450

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25
Q

What are the indications of apixaban?

A

Prophylaxis of VTE following hip/knee replacement surgery

Thromboprophylaxis in non-valvular AF

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26
Q

Give examples of cardio selective beta blockers?

A

Bisoprolol

Atenolol

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27
Q

What is the mechanism of action of cardio selective beta blockers?

A

Cardioselective beta 1 adrenoreceptor antagonists. Inhibit sympathetic stimulation of the heart and renal vasculature, Blockade of the SA node reduces heart rate, blockade of receptors in the myocardium depress cardiac contractility and blockage of beta-1 adrenoreceptors in renal tissues inhibits the release of renin

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28
Q

What are the indications for bisoprolol/atenolol?

A

Hypertension
Angina
Rate control in AF
Bisoprolol is used as part of supportive therapy for mild/moderate heart failure

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29
Q

What are the side effects of cardiac selective beta blockers?

A 
Bradycardia
Hypotension
Bronchospasm
Fatigue
Cold extremities
Sleep disturbances
Loss of hypoglycaemic awareness
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30
Q

In what patients should cardiac selective and non-cardioselective beta blockers be avoided?

A

Asthma / COPD due to risk of bronchospasm

History of frequent hypoglycaemia

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31
Q

Why should beta blockers and rate-limiting calcium channel blockers not be combined in anti-hypertensive therapy?

A

Risk of heart block

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32
Q

Give examples of rate-limiting calcium channel blockers?

A

Verapamil

Diltiazem

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33
Q

Give examples of non-cardioselective beta blockers?

A

Propranolol

Carvedilol

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34
Q

What is the mechanism of action of propranolol?

A

Non-cardioselective beta one adrenoreceptor antagonist

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35
Q

What is the mechanism of action of carvedilol?

A

Non-selective beta one, beta two and alpha one adrenergic receptor antagonist

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36
Q

What are the indications for the use of non-cardioselective beta blockers?

A 
Hypertension
Angina
Anxiety
Migraine prophylaxis
Post MI prophylaxis
Carvedilol may be sued as part of supportive therapy for mild/moderate heart failure
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37
Q

What are the side effects of non-cardioselective beta blockers?

A 
Bradycardia
Hypotension
Bronchospasm
Fatigue
Cold extremities
Sleep disturbances
Loss of hypoglycaemic awareness
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38
Q

In what patients should non-cardioselective beta blockers be cautioned?

A

Diabetics due to risk of deranged carbohydrate metabolism

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39
Q

Why should propranolol be avoided in liver impairment?

A

It is lipid soluble and is predominantly cleared by the liver

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40
Q

Give examples of ACE inhibitors?

A

Ramipril
Enalapril
Lisinopril
Perindopril

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41
Q

What are the indications for ACE inhibitors?

A

Hypertension
Heart failure
Nephropathy
Prevention of cardiovascular events in high risk patients

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42
Q

What are the side effects of ACE inhibitors?

A 
Dry cough
Hypotension
Hyperkalaemia
Renal impairment
Angiooedema
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43
Q

Why is a blood test requires at 1-2 weeks after starting ACE inhibitors?

A

To check electrolyte balance

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44
Q

In which patients are adverse drug reactions with ACE inhibitors most common?

A 
High dose diuretic therapy
Hypovolaemia
Hyponatraemia
Hypotension
Unstable heart failure
Renovascular disease
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45
Q

Give examples of nitrates

A

Isosorbide mononitrate

glyceryl trinitrate

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46
Q

Describe the mechanism of action of nitrates?

A

Converted to nitric oxide which is a potent vasodilator. These are cardioselective and act predominantly on coronary blood vessels, enhancing flow of blood to ischaemic areas of the myocardium. Additionally, nitrates reduce myocardial oxygen consumption by reducing cardiac preload and after load

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47
Q

What are the indications for the use of nitrates?

A

Angina

Severe hypertension

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48
Q

What are the side effects of nitrates?

A

Headache
Postural hypotension
Tachycardia

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49
Q

Tolerance to nitrates develops with long term use. How can this be avoided?

A

Patients should have a daily nitrate free period

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50
Q

How is isosorbide mononitrate administered?

A

Orally

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51
Q

How is glyceryl trinitrate administered?

A

Sublingual spray/tablet

IV

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52
Q

Give examples of rate limiting calcium channel blockers.

A

Verapamil

Dilitiazem

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53
Q

What is the mechanism of action of rate limiting calcium channel blockers

A

Prevents cellular entry of calcium by blocking l-type calcium channels. Myocardial and smooth muscle contractility is depressed and cardiac contractility is reduced, These dilate coronary blood vessels to reduce afterload. Antidysrythmic actions due to prolonged AV node conduction to depress the heart rate

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54
Q

What are the indications for rate limiting calcium channel blockers?

A

Supraventricular arrythmias
Treatment of angina
Hypertension

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55
Q

What are the side effects of verapamil?

A 
Constipation
Flushing
Headache
Dizziness
Hypotension
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56
Q

What are the side effects of diltiazem?

A 
GI disturbances
Bradycardia
Peripheral oedema
Dizziness
Headache
Hypotension
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57
Q

When are rate limiting calcium channel blockers contraindicated and avoided?

A

Contraindicated - heart failure, left ventricular dysfunction
Avoid - bradycardia, hypotension

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58
Q

Give examples of non rate-limiting calcium channel blockers?

A

Amlodipine
Nifedipine
Felodipine

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59
Q

Describe the mechanism of action of non rate-limiting calcium channel blockers?

A

Prevents cellular entry of calcium by blocking l-type calcium channels
Myocardial and smooth muscle contractility is depressed. Dilate coronary blood vessels and reduce after load. Do not lower heart rate

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60
Q

What are the indications for the use of non-rate limiting calcium channel blockers?

A

Hypertension

Treatment of angina

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61
Q

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

A 
Ankle oedema
Abdominal pain / nausea
Palpitations
Flushing
Headache
Dizziness
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62
Q

When should non rate limiting calcium channel blockers be avoided?

A

Cardiogenic shock
Unstable angina
significant aortic stenosis

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63
Q

What makes ankle swelling with calcium channel blockers worse?

A

Hot weather

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64
Q

Give examples of HMG CoA reductase inhibitors?

A

Simvastatin
Atorvastatin
Pravastatin

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65
Q

Describe the mechanism of action of statins?

A

Completely inhibits HMG CoA reductase - the rate limiting enzyme in the mevalonate pathway of cholesterol synthesis. Increases LDL receptor expression on the surface of hepatocytes. Increases hepatic uptake of cholesterol, reducing plasma cholesterol levels, Reduces development of atherosclerotic plaques

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66
Q

What are the indications of HMG CoA reductase inhibitors?

A

Familial hypercholesterolaemia

prevention of cardiovascular events in high risk patients

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67
Q

What are the side effects of HMG CoA reductase inhibitors?

A

Myalgia
Myopathy and rhabdomyolysis
GI disturbances
Liver abnormalities - deranged LFTs

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68
Q

What side effects of HMG CoA reductase inhibitors are dose related?

A

Myalgia

Rhabdomyolysis

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69
Q

Give an example of a cardiac glycoside?

A

Digoxin

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70
Q

Describe the mechanism of action of digoxin?

A

Increases vagal parasympathetic activity and inhibits the NA/K pump causing intracellular build up of sodium. In an effort to remove NA, Ca is brought into the cell by the action of Na/Ca exchangers. The build-up of Ca is responsible for the increased force of contraction of the heart and reduced rate of conduction through the AV node

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71
Q

What are the indications for cardiac glycosides (digoxin)?

A

Heart failure

Rate control in AF

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72
Q

What are the side effects of digoxin?

A

Nausea
Vomiting
Diarrhoea
Confusion

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73
Q

What can be used to treat life threatening digoxin overdose?

A

Digoxin specific antibody

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74
Q

What are the major determinants for safe digoxin dosage?

A

Renal function
Age
Heart Disease

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75
Q

Digoxin has a narrow therapeutic index. T/F?

A

True

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76
Q

Give an example of an anti-arrhythmic drug?

A

Amiodarone

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77
Q

Describe the mechanism of action of amiodarone?

A

Amiodarone blocks cardiac potassium channels, prolonging depolarisation of the cardiac action potential. It restores regular sinus rhythm and slows AV node conduction

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78
Q

What are the indications of amiodarone?

A

Supraventricular / ventricular arrhythmias

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79
Q

What are the side effects of amiodarone?

A 
Photosensitivity skin reactions
Hypersensitivity reactions
Hyper/hypothyroidism
Pulmonary fibrosis
corneal deposits
neurological disturbances
GI disturbances / hepatitis
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80
Q

How long can it take to achieve steady state amuodarone plasma concentrations?

A

Weeks to months

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81
Q

What monitoring blood tests are required during amiodarone treatment?

A

TFTs before treatment, every six months and if symptomatic

LFTs

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82
Q

Give examples of penicillins?

A

Flucloxacillin
Amoxicillin
Benzylpenicillin
Penicillin V

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83
Q

Describe the mechanism of action of penicillins?

A

Attaches to penicillin-binding proteins on forming bacterial cell walls which inhibits the transpeptidase enzyme which cross-links the bacterial cell wall. Failure to cross-link causes bacterial cell autolysis.

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84
Q

What are the indications for flucloxacillin?

A

Soft tissue infection
Staphylococcal endocarditis
Otitis externa

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85
Q

What are the indications of amoxicillin?

A

Non-severe community acquired pneumonia

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86
Q

What are the side effects of penicillins?

A

Diarrhoea
Vomiting
Liver Function Impairment
Hypersensitivity reactions

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87
Q

What is amoxicillin often combined with to prevent resistance?

A

Clavulinic acid - a beta lactase inhibitor

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88
Q

Give examples of cephalosporins?

A

Ceftriaxone

Cephalexin

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89
Q

What is the mechanism of action of cephalosporins?

A

Attaches to penicillin binding proteins on forming bacterial cell walls, inhibits transpeptidase enzyme which cross links the bacterial cell wall. Failure to cross link induces bacterial cell autolysis

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90
Q

Cephalosporins are less susceptible to beta lactamases than penicillins. T/F?

A

True

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91
Q

What are the indications for cephalosporins?

A

Serious infection - sepsis, pneumonia, meningitis

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92
Q

What are the side effects of cephalosporins?

A

Hypersensitivity reactions
Antibiotic associated c.difficile
Liver function impairment

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93
Q

How are cephalosporins secreted?

A

Renal excretion

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94
Q

Give an example of a glycopeptide?

A

Vancomycin

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95
Q

Describe the mechanism of action of vancomycin?

A

Bactericidal, inhibiting cell wall synthesis in gram positive bacteria

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96
Q

What are the indications for vancomycin?

A

Severe gram positive infections
MRSA infection
Severe c.difficile infection

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97
Q

What are the side effects of vancomycin?

A 
Fever
Rash
Local phlebitis at site of infection
Nephrotoxicity
Ptottoxicity
Blood disorders - neutriopenia
Anaphylactoid reaction - red man syndrome - if infusion rate is too fast
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98
Q

Vancomycin requires therapeutic drug monitoring. T/F?

A

True

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99
Q

How can vancomycin be administered?

A

Continuous intravenous infusion or a pulsed infusion regimen

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100
Q

Describe the mechanism of action of gentamicin

A

Binds to the 30s ribosomal subunit to inhibit protein synthesis and induce prolonged post-antibiotic bacteriostatic effect, There is additional bactericidal action on the cell wall in high doses

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101
Q

What are the indications for gentamicin?

A

Gram negative infections (biliary tract infection, pyelonephritis, hospital acquired pneumonia
Severe gram positive infections (soft tissue infections and endocarditis)

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102
Q

What are the side effects of gentamicin?

A

Nephrotoxicity

Ototoxicity

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103
Q

What are the indications for the use of quinolones?

A 
Gram negative bacterial infection
Respiratory tract infection
Upper UTI
Peritoneal infection
Gonorrhoea
Prostatitis
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104
Q

What are the side effects of quinolones?

A

GI toxicity
QT prolongation
C.difficile infection
Tendonitis

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105
Q

What are the indications for macrolides?

A

Atypical organisms causing pneumonia / severe community acquired pneumonia
Mild/moderate skin and soft tissue infection
otitis media
Lyme disease
helicobacter pylori eradication therapy
severe campylobacter infection

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106
Q

What are the indications for the use of trimethoprim?

A

First line for uncomplicated UTI
Acute or chronic bronchitis
Pneumocystis pneumnia

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107
Q

What is the mechanism of action of acyclovir?

A

A guanosine derivative, converted to triphosphate by infected cells, it then inhibits DNA polymerase, terminating the nucleotide chain and inhibiting viral DNA replication

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108
Q

What are the indications of acyclovir?

A

Herpes simples infection

Varicella zoster infection

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109
Q

To what class of drug does acyclovir belong?

A

Anti viral

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110
Q

What are the side effects of aciclovir?

A

Nausea
Vomiting
Local inflammation at infusion site if given IV

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111
Q

How can acyclovir be administered?

A

Oral
IV
Topical

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112
Q

Acyclovir penetrates well into the CSF. T/F?

A

True

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113
Q

Describe the mechanism of action of short and long acting beta adrenergic bronchodilators?

A

Relaxes bronchial smooth muscle, inducing bronchodilator. Inhibits pro-inflammatory cytokine release from mast cells and TNF-alpha release from monocytes to reduce airway inflammation. Stimulates cilia action which increases mucous clearance

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114
Q

What are the indications of short and long acting beta 2 adrenoreceptor agonists?

A

Asthma

COPD

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115
Q

What are the side effects of short and long acting beta 2 adrenoreceptor agonists?

A

Tremor
Tachycardia/cardiac dysryhtmia
Headache
Sleep disturbances

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116
Q

Long acting beta 2 adrenoreceptor agonists can be used in rapidly deteriorating asthma. T/F?

A

False - they have too slow an onset for this so short acting beta 2 agonists should be used instead

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117
Q

Give examples of anti-muscarinic bronchodilators?

A

Tiotropuim

Ipratropium bromide

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118
Q

Describe the mechanism of action of anti muscarinic bronchodilators?

A

Muscarinic receptor M3 antagonists produce bronchodilators effects. It reduces mucous secretion and may increase bronchial mucous clearance by stimulating cilia

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119
Q

What are the indications for anti-muscarinic bronchodilators?

A

Asthma
COPD
Rhinitis

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120
Q

What are the side effects of anti-muscarinic bronchodilators?

A

Dry mouth
Cough
Constipation

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121
Q

Why should nebuliser ipratropium bromide always be administered via a mouth piece?

A

To minimise the risk of acute angle closure glaucoma

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122
Q

Give an example of an inhaled corticosteroid?

A

Beclomethasone

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123
Q

Describe the mechanism of action of inhaled corticosteroids?

A

Anti-inflammatory effect on airways
Decrease formation of pro-inflammatory cytokines
Up-regulates beta 2 adrenoreceptors in airways

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124
Q

What are the indications for inhaled corticosteroids?

A

COPD

Asthma

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125
Q

What are the side effects of inhaled corticosteroids?

A

oral candidiasis
adrenal suppression
osteoporosis

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126
Q

All patients on inhaled corticosteroids need to carry a steroid user card. T/F?

A

False - only those on high dose ICS

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127
Q

Give examples of antihistamines?

A

Chlorpheniramine
Desloratidine
Fexofenadine
Hydroxyzine

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128
Q

Describe the mechanism of action of antihistamines?

A

H1 receptor antagonist

Inhibits histamine mediated contraction and vasodilation of the bronchial smooth muscle

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129
Q

What are the indications for antihistamines?

A

Anaphylaxis
Hay fever
Urticaria
Sedation

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130
Q

What are the side effects of antihistamines?

A

Drowsiness

Tinnitus

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131
Q

How do antihistamines cause sedation?

A

Central nervous system H1 antagonism

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132
Q

What are the implications of the sedative effects on antihistamines for patients?

A

Can’t drive or operate heavy machinery

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133
Q

Describe the mechanism of action of levodopa?

A

Pro-drug which crosses the BBB and is converted to dopamine. This increases stratal dopaminergic neurotransmission

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134
Q

What is the indication for the use of levodopa?

A

Parkinson’s disease

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135
Q

What are the side effects of levodopa?

A 
Dyskinesia
Compulsive disorders
Hallucinations
Nausea
GI upset
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136
Q

What is co-administered with levodopa to reduce the side effects?

A

Dopamine decarboxylase inhibitor or COMT inhibitor

137
Q

Give examples of dopamine agonists?

A 
Apomorphine
Pramipexole
Bromocriptine
Pergolide
Rotigotine
138
Q

Describe the mechanism of action fo dopamine agonists?

A

Stimulate post synaptic dopamine receptors
Apomorphine is non selective for D1 and D2
Prampipexole is selective for D3 receptor

139
Q

What is the indication for the use of dopamine agonists?

A

Parkinson’s disease

140
Q

What are the side effects of apomorphine?

A

Pain at site of injection, nausea, vomiting

141
Q

What are the side effects of pramipexole?

A

Hallucinations
Nausea
Drowsiness
Involuntary movement

142
Q

How is apomorphine administered?

A

Parenterally

143
Q

Give an example of a catechol-o-methyl transferaseinhibitor?

A

Entacapone

144
Q

What is the mechanism of action of entacapone?

A

Prevents peripheral breakdown of levodopa by inhibiting COMT, therefore more levodopa reaches the brain

145
Q

What is the indication for entacapone?

A

Parkinson’s disease in conjunction with L-DOPA and dopamine decaroxylase inhibitor

146
Q

What are the side effects of entacapone?

A 
Dyskinesia
Nausea
Abdominal pain
Vomiting 
Dry mouth
Dizziness
147
Q

Describe the mechanism of action of carbamazepine?

A

Voltage gated sodium channel blocker on the pre-synaptic membrane
Blocks the sodium influx
reduces neuronal excitability and decreases the action potential

148
Q

What are the indications for the use of carbamezepine?

A

Epilepsy
Trigeminal neuralgia
Neuropathic pain

149
Q

What are the side effects of carbamazepine?

A 
Dizzziness
Dry mouth
Ataxia
Fatugue
Headache
Dipolopia
Blurred vision
Hyponatraemia
Stevens Johnsons syndrome
150
Q

What food can significantly increase serum levels of carbamazepine?

A

Grapefruit

151
Q

Give examples of voltage gated sodium channel antagonists used as anti-epileptics?

A

Carbamezepine

Lamotrigrine

152
Q

Give examples of voltage gated potassium channel agonists used as anti-epileptics?

A

Retigabine

153
Q

Give an example of a SV2A vesicle antagonist used as an anti-epileptic drug?

A

Levetiracetam

154
Q

Give examples of voltage gated calcium channel antagonists used as anti-epileptics?

A

Pregabalin

Gabapentin

155
Q

Give examples of GABA metabolism inhibitors used as anti-epileptic drugs?

A

Valproate

Vigabatrin

156
Q

Give examples of GABA transporter antagonists used as anti-epileptic drugs?

A

Tiagabine

157
Q

Give examples of GABA receptor agonists used as anti-epileptic drugs?

A

Benzzodiazepines

158
Q

Describe the mechanism of action of sodium valproate?

A

Weak sodium ion channel blocker
Inhibitor of GABA degrading enzymes
Increased GABA stops action potentials

159
Q

What are the indications of sodium valproate?

A

Epilepsy
Bipolar disorder
Depression

160
Q

What are the side effects of sodium valproate?

A 
Nausea
Diarrhoea
Gastric irritation
Weight gain
Hyponatraemia
Behavioural disturbances
Confusion
Stevens Johnson syndrome
161
Q

What blood test must be conducted before and during the initial 6 months of sodium valproate therapy?

A

LFTs

162
Q

Describe the mechanism of action of phenytoin?

A

Acts as a voltage gated sodium channel blocker on the pre-synaptic neuronal membrane
Limits action potential transmission to limit spread of seizure activity

163
Q

What are the indications for phenytoin?

A

Epilepsy

Trigeminal neuralgia

164
Q

What are the side effects of phenytoin?

A 
Insomnia
Headache
Rash
Constipation
Vomiting 
Gingival hyperplasia
Liver damage
Steven Johnson syndrome
Thrombocytopenia
165
Q

Phenytoin has a narrow therapeutic index. T/F?

A

True

166
Q

What information is important for patients on phenytoin to know?

A

Avoid alcohol
Take with food to reduce irritaition
Do not take calcium, aluminium, magnesium or iron supplements within 2 hours of ingestion

167
Q

Describe the mechanism of action of lamotrigine?

A

Varied mechanism of action
Inhibits voltage gated sodium channels and/or calcium channels
Acts on pre-synaptic neuronal membrane
Reduces action potential and excitatory signals

168
Q

What are the indications for lamotrigine?

A

Epilepsy

Depressive episodes associated with bipolar disorder

169
Q

What are the side effects of lamotrigrine?

A 
Nausea
Vomiting
Diarrhoea
Tremor
Insomnia
Blurred vision
Aggression
Skin reactions- Steven Johnson syndrome and toxic epidermal necrolysis
170
Q

What will cause the half-life of lamotrigine to double?

A

Chronic renal impairment

171
Q

What is the mechanism of action of levetiracetam?

A

SV2A is a synaptic vesicle protein required for neurotransmitter release which is blocked by levetiracetam to induce an anti-epileptic effect

172
Q

What is the indication for levetiracetam?

A

Epilepsy

173
Q

What are the side effects of levetiracetam?

A 
Headache
Fatigue
Anxiety
Irritability
Drowsiness
Constipation
174
Q

Cytochrome p450 is not involved in the metabolism of levetiracetam. T/F?

A

True

175
Q

Give examples of selective serotonin reuptake inhibitors?

A 
Citalopram
Fluoxetine
Paroxetine
Escotalopram
Sertraline
176
Q

Describe the mechanism of action of SSRIs?

A

Inhibitition of reuptake of serotonin at the serotonin reuptake pump of the synaptic cleft in the CNS. Increases serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors

177
Q

What are the indications of SSRIs?

A

Depression
Obsessive compulsive disorder
Bulimia

178
Q

What are the side effects of SSRIs?

A 
Dry mouth
Nausea
Insomnia
Anxiety
Decreased libido
Seizures
Dyskinesia
179
Q

Why do SSRIs have fewer side effects than tricyclic antidepressants?

A

They bind with less affinity to histamine, acetylcholine and norepinephrine receptors

180
Q

Give examples of tricyclic antidepressants?

A

Amitriptyline
Imipramine
Doxepin

181
Q

Describe the mechanism of action of tricyclic antidepressants?

A

Block the reuptake of monoamines by binding to the monoamine pump at the pre-synaptic cleft which reduces the rupture or norepinephrine and/or serotonin

182
Q

What are the indications of tricyclic antidepressants?

A

Depression
Panic disorders
Neuropathic pain

183
Q

What are the side effects of tricyclic antidepressants?

A 
Sedation
Postural hypotension
Tachycardia
Urinary retention
Dry mouth
Blurred vision
Diplopia
184
Q

What can occur with overdose of tricyclic antidepressants?

A

Seizures

Cardiac arrhythmias

185
Q

Give examples of first generation antipsychotics?

A

Haloperidol

Chlorpromazine

186
Q

Give examples of atypical anti-psychotics?

A

Olanzapine

Clozapine

187
Q

Describe the mechanism of action of anti-psychotics?

A

Block dopamine receptors, Action on mesolimic and nigrostriatal parts of the brain. Also have anti-histaminergic and anti-cholinergic effects. Reduce positive symptoms of schizophrenia

188
Q

What are the indications of anti-psychotics?

A 
Schizzophrenia
Mania
Delusions/hallucinations
Bahvioural problems
Haloperidol is an anti-emetic
189
Q

What are the side effects of anti-psychotics?

A 
Sedation
Postural hypotension
Tachycardia
Urinary retention
Dry mouth
Blurry vision
190
Q

Give examples of benzodiazepines?

A

Diazepam
Lorazepam
Midazolam

191
Q

Describe the mechanism of action of benzodiazepines?

A

Increases GABA affinity for GABA receptor
GABA binding to receptor increases chloride flow through chloride channels
Hyperpolarisation occurs - reducing activity of limbic, thalamic and hypothalamic areas of the bran

192
Q

What are the indications for benzodiazepines?

A

Anxiety
Epilepsy
Muscle spasm
Alcohol withdrawal

193
Q

What are the side effects of benzodiazepines?

A

Sedation
Ataxia
Altered mental status
Insomnia

194
Q

How can diazepam be administered?

A

Oral
Rectal
Parenteral

195
Q

How can lorazepam by administered?

A

Oral

Parenteral

196
Q

Which benzodiazepine is used most often in patients with liver failure?

A

Lorazepam as it accumulates less with long term use

197
Q

Give an example of a short acting benzodiazepine?

A

Midazolam

198
Q

Give examples of glucocorticoids which can be given orally?

A

Prednisolone
Hydrocortisone
Dexamethasone

199
Q

Give examples of glucocorticoids which can be given topically?

A

Hydrocortisone
Betamethasone
Clobetasone

200
Q

Give examples of glucocorticoids which can be given parenterally?

A

Methylprednisolone
Hydrocortisone
Triamcinolone

201
Q

Describe the mechanism of action of glucocorticoids?

A

Bind to glucocorticoid receptors causing up regulation of a variety of anti-inflammatory mediators and down regulation of pro-inflammatory mediators. Also increase gluconeogenesis and some glucocorticoids have mineralocorticoid activity

202
Q

What are the indications for these of glucocorticoids?

A

Replacement therapy in adrenal insufficiency
Post transplant immunosupression
Treatment of exacerbations of inflammatory conditions(e.g. eczema, RA, IBD)
Acute asthma

203
Q

What are the side effects of glucocorticoids?

A 
Sleep disturbance
Modd disturbance
Hyperglycaemia
Immunodeficiency
Easy bruising
Moon faces
Increased abdominal fat
Glaucoma
Striae
Hypertension
Gastric irritation
204
Q

What information is it important for patients on glucocorticoids to know?

A

Avoid alcohol and caffeine
Take with food to avoid gastric irritation
Don’t stop suddenly
Always inform doctors that they are on steroids and carry a steroid card
Double dose when ill

205
Q

Give an example of a corticosteroid which has predominant glucocorticoid activity and low mineralocorticoid activity?

A

Prednisolone, gbetamethasone, dexamethasone

206
Q

Give examples of corticosteroids which show much glucocorticoid and mineralocorticoid activity?

A

Hydrocortisone

Fludrocortisone

207
Q

Give examples of anti-TNF agents?

A

Etanercept
Infliximab
Adalimumab

208
Q

Describe the mechanism of action of anti-TNF agents?

A

Anti TNF-alpha and beta. Blocks its interactions with TNF cell receptors
TNF alpha and beta produced from macrophages and T cells
Stimulates cytokines IL1/8/6. Reduces inflammation

209
Q

What is the indication for anti-TNF agents?

A

RA
Psoriatic arthritis
Ankylosing spondylitis
Juvenile arthritis

210
Q

What are the side effects of anti-TNF agents?

A

Injection site reactions
Flu-Like symptoms(fever, headache, runny nose)
Immune deficiency

211
Q

Give examples of immunosupressants

A

Methotrexate
Azathioprine
Mercaptopurine

212
Q

Describe the mechanism of action of azathioprine?

A

Blocks purine synthesis mainly in lymphocytes

213
Q

Describe the mechanism of action of methotrexate?

A

Stops the action of the enzyme dihydrofolate needed for the production. of DNA

214
Q

What are the indications for. the use of immunosuppressants?

A

Post transplantation immunosuppression
inflammatory bowel disease
renal vasculitis
paediatric leukaemia (methotrexate)

215
Q

What are the side effects of immunosuppressants?

A 
Bone marrow suppression
Risk of infection
Nephrotoxicity
Hepatotoxicity
Seizures
GI upset
Mucosal ulceration
Alopecia
216
Q

Immunosuppressants cross the blood brain barrier. T/F?

A

False

217
Q

Which patients are more prone to azathioprine and mercaptopurine related marrow suppression?

A

Patients with low levels of thiopurine and methyltransferase

218
Q

Give examples of PPIs

A

Omeprazole
Lansoprazole
Pantoprazole

219
Q

Describe the mechanism of action of PPIs?

A

Bind to H/K ATPase pump on gastric parietal cells

Reduces HCl production and hence reduces gastric acidity

220
Q

What are the indications for the use of PPIs?

A 
Peptic ulcers
GORD
H.pylori infection
prophylaxis in patients on long term NSAIDs
Zollinger Ellison syndrome
221
Q

What are the side effects of PPIs?

A 
Nausea
Vomiting
Insomnia
Vertigo
Headaches
222
Q

Which PPI is an. inhibitor of CYP450?

A

Omeprazole

223
Q

What information is it important for patients on PPIs to know?

A

Avoid alcohol

take 30-60 mins before food

224
Q

Give examples of. H2 receptor antagonists?

A

Ranitidine
Cimetidine
Famotidine
Nizatifine

225
Q

Describe the mechanism of action of H2 receptor antagonists?

A

Histamine binds to H2 receptors on. gastric parietal cells stimulating gastric acid secretion
H2 antagonists inhibit this by reduced cAMP and hence reducing the activity of H/K ATPase

226
Q

What are the indications for the use of H2 receptor antagonists?

A

Peptic ulcer
GORD
Zollinger Ellison. syndrome

227
Q

What are the side effects of H2 receptor antagonists?

A 
Headache
Dizziness
Diarrhoea
Reduced B12 absorption
Gynaecomastia
228
Q

Which H2 receptor antagonist. is. an inhibitor of CYP450?

A

Cimetidine

229
Q

Give examples of laxatives

A

Lactulose

Senaa

230
Q

Describe the mechanism of action of lactulose?

A

Reduces water reabsorption in the. intestine - pulls water into the bowel to promote distension and movement

231
Q

Describe the mechanism of action of Senna?

A

Stimulant/irritant agent

232
Q

What are the indications for. the use of laxatives?

A

Constipation
pregnancy
prophylaxis in opiate analgesic use

233
Q

What are the side effects of laxatives?

A

Dehydration
salt loss
abdominal cramps
fatigue

234
Q

Why is Senna recommended for short term use only?

A

Risk organ failure with long term use or abuse

235
Q

What are. the four broad types of laxatives?

A

Bulk producing. agents (lactulose)
Stool softeners
Simulant or irritant (senna)
Hydrating agents (milk of magnesia)

236
Q

Give an example of an anti-emetic?

A

Cyclizine

237
Q

Describe the mechanism of action of cyclizine?

A

histamine. H1 receptor antagonist, acts on. vomiting centre. in. the medullary region. Also has mild anticholinergic and antimuscarinic effects

238
Q

What are the indications for the use of anti-emetics?

A

Nausea and vomiting
Motion sickness
Vertigo and dizziness
Prophylaxis alongside chemotherapy and opiate. analgesic use

239
Q

What are the side effects of anti-emetics?

A

Headache
Sedation
Diarrhoea

240
Q

What are the five broad types of anti-emetic?

A 
Anticholinergics
Antihistamine
Serotonin antagonist
Phenothiazine
Motility stimulants
241
Q

Give an example of an anticholinergic antiemetic?

A

Hyoscine. hydrobromide

242
Q

Give an example of a serotonin antagonist antiemetic?

A

Ondansetron

243
Q

Give an example of a phenothiazine antiemetic?

A

Prochlorperazine

244
Q

Give an example of a motility stimulant antiemetic?

A

Metoclorpramide

245
Q

Describe the mechanism of action of metclopramide?

A

Dopamine D2 receptor antagonist, raises activity in the chemoreceptor. trigger zone and increases gastric emptying and intestinal transit. Reduces oesophageal reflux

246
Q

What are the indications for the use of metclopramide?

A

Nausea
Vomiting
To increase gastric emptying

247
Q

What are the side effects of metclopramide?

A 
Dystonia
Confusion
Dizziness
Diarrhoea
Parkinsonism with long term use
248
Q

How can metclopramide be administered?

A

Oral

Parenterally

249
Q

Describe the mechanism of action of prochlorperazine?

A

Anti-psychotic drug which is used as an anti-emetic. Dopamine D2 receptor antagonist causes increases dopamine turnover

250
Q

What. are the indications for the. use of prochlorperazine?

A

Nausea
Vomiting
Adjunct in some psychotic disorders

251
Q

What are the side effects of prochlorperazine?

A

Dry mouth
Tachycardia
restlessness
drowsiness

252
Q

Give examples of thiazide diuretics?

A

Bendroflumethazide
Indapamide
Chlortalidone

253
Q

Describe the. mechanism of action of thiazide diuretics?

A

Inhibit sodium/chloride transporters at the distal convulsed tubule and collecting duct
Increases sodium, chloride and water excretion

254
Q

What are the indications of thiazide diuretics?

A

Hypertension

Oedema of cardiac/renal/hepatic/iatrogenic origin

255
Q

What are the side effects of thiazide diuretics?

A 
Hypokalaemia
Hypomagnesaemia
Hyponatraemia
Hypercalcaeia
Hyperuricaemia
Reduced glucose tolerance
Hypersensitivity reactions
256
Q

What drug reduces. the efficacy of thiazide diuretics?

A

NSAIDs

257
Q

Give examples of loop diuretics?

A

Furosemide
Bumetanide
Torasemide

258
Q

Describe the mechanism of action of loop diuretics?

A

Na/Cl/K symporter antagonists

Act on the thick ascending loop of Henley to increase the secretion of sodium, potassium, chloride and water

259
Q

What are the indications of loop diuretics?

A 
Hypertension
Hyperkalaemia
Heart failure
Cirrhosis of the liver
Nephrotic syndrome
260
Q

What are the side effects of loop diuretics?

A

Hypokalaemia, hypovolaemia, hyperuricaemia
Metabolic acidosis
Abdominal pain
Ototoxicity

261
Q

Give an example of a long acting insulin

A

Glargine

262
Q

Describe the mechanism of action of insulin

A

Insulin increases cellular uptake of glucose. It stimulates glycogenesis, encourages DNA synthesis and promotes release of growth hormone.

263
Q

Give an example of a short acting insulin

A

Novorapid

264
Q

Give an example of a fast-acting intermediate-acting mix insulin

A

Humalog mix

265
Q

What are the indications for insulin?

A

T1DM
T2DM
Hyperkalaemia (in conjunction with dextrose)

266
Q

What are the side effects of insulin?

A

Hypoglycaemia - sweats, shakes, tachycardia, headache, weakness, fatigue
Oedema
Injection site reactions

267
Q

What type of insulin can be given IV?

A

Short acting e.g. act rapid

268
Q

Describe the time to reach circulation, peak and duration of action of rapid acting insulin?

A

Reaches circulation within 15 mins after injection
peaks 30 to 90 mins later
lasts for up to 5 hours

269
Q

Describe the time to reach circulation, peak and duration of action of short acting insulin?

A

Reaches circulation 30 mins after injection
peaks 2-4 hours later
lasts for up 4-8 hours

270
Q

Describe the time to reach circulation, peak and duration of action of intermediate acting insulin?

A

Reaches circulation 2-6 hours after injection
peaks 4-14 hours later
lasts for up 20 hours

271
Q

Describe the time to reach circulation, peak and duration of action of long acting insulin?

A

Reaches circulation 6-14 hours after injection
minimal peak
lasts for up 24 hours

272
Q

Give examples of sulphonylureas

A

Gliclazide

Glimepiride

273
Q

Describe the mechanism of action of sulphonylureas?

A

Stimulates beta cells in the pancreas to produce more insulin. Increases cellular glucose uptake and glycogenesis and reduces gluconeogenesis

274
Q

What is the duration of action of Gliclazide?

A

~12 hours

275
Q

What is the indication for the use of sulphonylureas?

A

T2DM

276
Q

What are the side effects of sulphonylureas?

A 
Hypoglycaemia
Rashes
Nausea
Vomiting
Stomach pain
Indigestion
Weight gain
277
Q

Give an example of a long acting sulphonylurea?

A

Glimepiride

278
Q

Give and example of a biguanide?

A

Metformin

279
Q

Describe the mechanism of action of biguanides

A

Increase the activity of AMP-dependent protein kinase (AMPL) which inhibits gluconeogenesis and reduces insulin resistance

280
Q

What are the indications for the use of metformin?

A

T2DM

Metabolic and reproductive abnormalities associated with PCOS

281
Q

What are the side effects of metformin?

A 
Diarrhoea
Nausea
Vomiting
Taste disturbances
Lack of appetite
Risk of lactic acidosis with illness and renal failure
282
Q

When should metformin not be used?

A

Pregnancy

Renal failure

283
Q

Give examples of GLP1 agonists

A

Exanatide

Liraglutide

284
Q

Describe the mechanism of action of GLP1 agonists

A

GLP-1 is a hormone which is release after meals to increase insulin secretion. GLP1 agonists act on GLP1 receptors to increase insulin secretion, decrease glucagon secretion and reduce hunger

285
Q

What are the indications for the use of GLP1 agonists?

A

T2DM (in association with excess weight)

286
Q

What are the side effects of GLP1 agonists?

A

Hypoglycaemia
Nausea
Vomiting
Diarrhoea

287
Q

How is GLP1 administered?

A

Bi-daily injections

288
Q

What is the mechanism of action of levothyroxine?

A

Thyroxine increases. the metabolic rate of all tissues in the body, Levothyroxine is a synthetically prepared T4 which is converted to T3 in the liver and kidney. It maintains brain function, food metabolism and body temperature

289
Q

What are the indications for the use of levothyroxine?

A

Hypothyroidism

Chronic lymphocytic thyroiditis

290
Q

What are the side effects of levothyroxine?

A 
Chest pain
Coma
Diarrhoea
Tachycardia
Itching
Muscle cramps
291
Q

How long after starting levothyroxine should TFTs be checked?

A

6 weeks

292
Q

Give examples of anti-thyroid drugs?

A

Carbimazole

Propylthiouracil

293
Q

Describe the mechanism of action of anti-thyroid drugs

A

Reduces activity of peroxidase enzyme required for the production of thyroid hormones and may also reduce peripheral conversion fo T4 to. T3

294
Q

What are the indications for the use of anti-thyroid drugs?

A

Hyperthyroidism
Thyrotoxicosis
Preparing patients for thyroid surgery

295
Q

What. are the side effects of anti-thyroid drugs?

A

Rash
Sore throat
Agranulocytosis

296
Q

Carbimazole is a prodrug. T/F?

A

True

297
Q

Why can carbimazole not be used in pregnancy?

A

It can cross the placenta

298
Q

What drug is usually co-prescribed with anti-thyroid agents?

A

Beta blockers

299
Q

Give examples of bisphosphonates?

A

Aledronate

Ibandronate

300
Q

Describe the mechanism of action of bisphosphonates

A

Inhibits osteoclast bone resorption

No effect on bone formation

301
Q

What are the indications for bisphosphonates?

A

Post menopausal osteoporosis
Reduces risk of vertebral and hip fractures
Paget’s disease of bone

302
Q

What are the side effects of bisphosphonates?

A 
Abdominal pain
Dyspepsia
Acid regurgitation
Dysphagia
Headache
303
Q

Give examples of the oral contraceptive pill

A

Microgynon (combined)

Cerazette (progesterone only)

304
Q

Describe the mechanism of action of the oral contraceptive pill

A

Acts on female reproductive tract, the mammary glands, hypothalamus and. pituitary gland. Reduces the production of gonadotropin releasing hormone
Blunts LH surge. that stimulates ovulation

305
Q

Describe the indications for the oral contraceptive pill

A

Contraception
Menopausal and postmenopausal. disorders
Polycystic ovarian syndrome

306
Q

Describe the side effects of the oral contraceptive pill

A

Mood swings
Headache
Breast tenderness
Increased risk of breast and ovarian cancer
Increased risk of venous thromboembolic disease

307
Q

What drugs can worsen the efficacy of the oral contraceptive pill?

A

Antibiotics

Some enzyme inducers

308
Q

What information is it important for the patient to know when on the oral contraceptive pill?

A

Important to take the tablet at the same time everyday

Use alternative forms of contraception when taking concurrent antibiotics or enzyme inducers

309
Q

Describe the mechanism of action of codeine, oxycodone and morphine?

A

Acts on mu, kappa and delta on presynaptic neutrons, this gives numerous effects that increase nociceptive thresholds throughout the central and peripheral nervous system

310
Q

What are the indications for the use fo codeine?

A

Mild to moderate pain
Persistent dry cough
Diarrhoea

311
Q

What. are the side effects of codeine?

A 
Nausea
Vomiting
Constipation
Biliary spasm
Headache on withdrawal
312
Q

Why are some people resistant to codeine’s analgesic properties?

A

10% of the population lack the demthylating enzyme which converts codeine to morphine

313
Q

Codeine can be taken with paracetamol. T/F?

A

True

314
Q

What are the indications for the use of morphine?

A

Acute severe pain - MI
Acute pulmonary oedema
Chronic pain

315
Q

What are the side effects of morphine?

A 
Nausea
Vomiting
Abdominal pain
Constipation
Respiratory depression
Sedation
316
Q

What can happen with accumulation of morphine?

A

Respiratory and CNS. depression

317
Q

What drug is morphine often co-administered with?

A

Anti-emetic

318
Q

What are the indications for the use. of oxycodone?

A

Moderate to severe pain relief in cancer patients
Postoperative pain
Severe pain

319
Q

What are the side effects of oxycodone?

A

Nausea
Vomiting
Abdominal pain
Constipation

320
Q

Give examples of non-selective NSAIDs?

A

Ibuprofen

Diclofenac

321
Q

Describe the mechanism of action of non-selective NSAIDs

A

Non-selective inhibits of COX (1+2) enzymes, decreasing key inflammatory mediator prostaglandins from being synthesised which reduces pain, inflammation and swelling

322
Q

Describe the indications of non-selective NSAIDs

A

Mild to moderate. pain relief
Rheumatic disorders - RA, OA
Fever

323
Q

What. are the side effects of non-selective NSAIDs?

A 
Gastric and duodenal. ulceration
Nausea
Diarrhoea
Increased risk of thrombotic events
Renal impairment
Hyperkalaemia
324
Q

Why should NSAIDs be avoided in pregnancy?

A

Risk of closure of foetal. ductus arterioles in utero and pulmonary hypertension in the newborn

325
Q

In elderly patients what drug is usually co-prescribed with. non-selective NSAIDs?

A

PPIs

326
Q

Give an example of a selective NSAID

A

Celecoxib

327
Q

Describe the mechanism of action of selective NSAIDs

A

Selective inhibitor of COX2, decreasing key inflammatory mediator prostaglandins from being synthesised. This reduces pain, inflammation and swelling

328
Q

GI side effects of NSAIDs are mediate by COX2. T/F?

A

False - they are mediated by COX1

329
Q

What are the indications fo the use of selective NSAIDs?

A

Pain and inflammation in OA, RA, ankylosing spondylitis

330
Q

What are the side effects of selective NSAIDs?

A 
Gastric and duodenal ulceration
Nausea
Diarrhoea
Renal impairment
Hyperkalaemia
331
Q

There is a higher risk of. cardiovascular events with selective compared to non-selective NSAIDs. T/F?

A

True

332
Q

Describe the mechanism of action of paracetamol?

A

Weak COX inhibitor with selectivity for brain COX. It therefore lacks peripheral anti-inflammatory actions but is useful in increasing the threshold for nociceptive activation by inhibiting prostaglandin synthesis and its effects centrally

333
Q

What are the indications for the use of paracetamol?

A

Mild to moderate pain relief

Fever

334
Q

What are the side effects of paracetamol?

A

Rash

Blood disorders

335
Q

Give an example of a xanthine oxidase inhibitor?

A

Allopurinol

336
Q

Describe the mechanism of action fo allopurinol?

A

Reduces synthesis of uric acid by competitively inhibiting xanthine oxidase, this reduces serum uric acid level

337
Q

Describe the indications for the use of xanthine oxidase inhibitors

A

Prophylaxis of. gout
Prophylaxis of calcium oxalate renal stone
Hyperuricaemia associated with cancer chemotherapy

338
Q

What are the side effects of xanthine oxidase inhibitors?

A

Rash
Hypersensitivity
GI disturbance
Neutropenia

339
Q

Why should xanthine oxidase inhibitors not be used to treat acute attacks of gout?

A

They can exacerbate the inflammation

Pharmacology (3 decks)

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