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Phase 3 > 50 Drugs > Flashcards

50 Drugs Flashcards

1
Q

State the class of drugs to which Aspirin belongs

A

Anti-Platelet

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2
Q

Describe the MOA of Aspirin

A

Irreversible inactivation of Cyclooxygenase enzyme This reduces production of Platelet Thromboxane (TXA2) and Endothelial Prostaglandin (PGI2) Reduced TXA2 production reduces platelet aggregation and thrombus formation Reduced prostaglandin synthesis decreases nociceptive sensation and inflammation

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3
Q

State indications for Aspirin

A

Secondary prevention of thrombotic events Pain relief

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4
Q

State side effects of Aspirin

A

Bleeding Peptic Ulcer Disease Angiooedema Bronchospasm Reye’s Syndrome

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5
Q

Describe important pharmacokinetic features of Aspirin

A

Half life increases with very large doses (therefore pharmacokinetics may be non-linear in overdose)

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6
Q

State some important pieces of patient information that should be given alongside Aspirin

A

May be advisable to take PPI with long term aspirin Avoid OTC preparations containing aspirin Not to be take by children under 16

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7
Q

State the class of drugs to which Clopidogrel belongs

A

Anti-Platelet

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8
Q

Describe the MOA of Clopidogrel

A

Irreversibly blocks the ADP receptor on platelet cell membranes Therefore prevents formation of the GPIIb/IIIa complex, required for platelet aggregation Decreased thrombus formation

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9
Q

State indications for Clopidogrel

A

Secondary prevention of thrombotic events

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10
Q

State side effects of Clopidogrel

A

Abdominal Pain Diarrhoea Bleeding

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11
Q

Describe important pharmacokinetic/pharmacodynamic features of Clopidogrel

A

Should be avoided in patients with liver failure

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12
Q

State some important pieces of patient information that should be given alongside Clopidogrel

A

Patients may be advised to stop clopidogrel before surgical procedures Patients should not stop clopidogrel without consulting their doctor if they have an arterial stent in-situ

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13
Q

Give examples of Recombinant Tissue Plasminogen Activators

A

Tenecteplase Alteplase

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14
Q

Describe the MOA of Recombinant Tissue Plasminogen Activators

A

Catalyses conversion of plasminogen to plasmin to promote fibrin clot lysis

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15
Q

State indications for the use of Recombinant Tissue Plasminogen Activators

A

Acute Ischaemic Stroke (within 4.5 hours) Myocardial Infarction (within 12 hours) Massive Pulmonary Embolism

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16
Q

State side effects of Recombinant Tissue Plasminogen Activators

A

Bleeding Allergy Angiooedema

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17
Q

Describe important pharmacokinetic/pharmacodynamic features of Recombinant Tissue Plasminogen Activators

A

Alteplase is given as a bolus-infusion regimen Tenecteplase is given as a single bolus Interacts with other blood thinners (anticoagulants/antiplatelets)

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18
Q

State some important pieces of patient information that should be given alongside Recombinant Tissue Plasminogen Activators

A

Patient should be made aware of the risk benefit ratio which should include reference to bleeding complications

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19
Q

Describe the MOA of Unfractioned Heparin

A

Unfractioned Heparin enhances the action of Antithrombin III, which inhibits thrombin

It also inhibits multiple other components of the coagulation cascade to have an anticoagulant effect

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20
Q

State the indications for Unfractioned Heparin

A

Treatment and Prophylaxis of Thromboembolic Disease

Renal Dialysis (Haemodialysis)

Treatment of Acute Coronary Syndrome

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21
Q

State the side effects of Unfractioned Heparin

A

Bleeding

Heparin-Induced Thrombocytopaenia

Osteoporosis

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22
Q

State important pharmacokinetic/pharmacodynamic features of Unfractioned Heparin

A

Administered by continuous IV infusion or subcutaneous injection

Complex kinetics - non-linear relationship between dose/half life and effect

Requires Therapeutic Dose Monitoring (TDM)

Anticoagulant effect can be reversed by Protamine

Shorter duration of action than LMW Heparin

Used in preference to LMW Heparin in selected patients due to shorter duration of action and reversibility (e.g. peri-operatively)

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23
Q

State some important pieces of patient information that should be given with Unfractioned Heparin

A

Risk of bleeding

Requires regular blood monitoring

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24
Q

Describe the MOA of LMW Heparin

A

LMW Heparin enhances the action of Antithrombin III, which inhibits thrombin

It also inhibits multiple other components of the coagulation cascade to have an anticoagulant effect

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25
Q

State the indications for LMW Heparin

A

Treatment and Prophylaxis of Thromboembolic Disease

Renal Dialysis (Haemodialysis)

Treatment of Acute Coronary Syndrome

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26
Q

State the side effects of LMW Heparin

A

Bleeding

Heparin-Induced Thrombocytopaenia

Osteoporosis

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27
Q

Describe important pharmacokinetic/pharmacodynamic features of LMW Heparin

A

Administered by subcutaneous injection

More predictable dose-response relationship than Unfractionated Heparin

2-4 times longer plasma half life than Unfractionated Heparin

Mostly renal clearance, therefore half life may be elevated in patients with renal failure so dose adjustment may be needed

Regular TDM not needed

Less readily reversed with Protamine than Unfractionated Heparin

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28
Q

State some important pieces of patient information that should be given with LMW Heparin

A

Risk of Bleeding

Requires Injection

May need regular monitoring in prolonged therapy (FBC to check for thrombocytopaenia)

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29
Q

To which class of drugs does Warfarin belong?

A

Vitamin K Antagonists

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30
Q

Describe the MOA of Warfarin

A

Inhibits Vitamin K epoxide reductase

Prevents recycling of Vitamin K to reduced form after carboxylation of coagulation factors II, VII, IX and X

Therefore, prevents thrombus formation

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31
Q

State indications for Warfarin

A

Treatment of Venous Thromboembolism

Thromboprophylaxis in AF/Metallic Heart Valves/Cardiomyopathy

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32
Q

State side effects of Warfarin

A

Bleeding (risk increases with increasing INR)

Warfarin Necrosis

Osteoporosis

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33
Q

Describe important pharmacokinetic/pharmacodynamic features of Warfarin

A

Numerous drug/food interactions

Reversed by Vitamin K

Polymorphisms in key metabolising enzymes (VKORC1 and CYP2C9)

Needs therapeutic dose monitoring and monitored loading regimen

Monitored with INR and dose adjusted depending on indication

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34
Q

State some important pieces of patient information that should be given with Warfarin

A

Need for compliance and attendance for monitoring

Care needed with alcohol

Must inform doctor before starting new drugs

Should avoid OTC preparations including aspirin

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35
Q

To which class of drugs does Dabigatran belong?

A

Direct Thrombin Inhibitors

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36
Q

Describe the MOA of Dabigatran

A

Direct thrombin inhibitor that prevents conversion of fibrinogen to fibrin

Thus prevents thrombus formation

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37
Q

State indications for Dabigatran

A

Prophylaxis of Venous Thromboembolism (especially post-operative)

Thromboprophylaxis in Non-Valvular AF

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38
Q

State side effects of Dabigatran

A

Bleeding

Dyspepsia

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39
Q

Describe important pharmacodynamic/pharmacokinetic features of Dabigatran

A

Rapid onset of action

No food and few drug interactions

Not metabolised by CYP450

No need for therapeutic monitoring

No available antidote

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40
Q

State some important pieces of patient information that should be given with Dabigatran

A

Risk of bleeding

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41
Q

To which class of drugs does Rivaroxaban belong?

A

Factor Xa Inhibitors

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42
Q

Describe the MOA of Rivaroxaban

A

Inhibits conversion of prothrombin to thrombin, thereby reducing thrombin concentrations in the blood

This inhibits formation of fibrin clots

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43
Q

State indications for Rivaroxaban

A

Prophylaxis of Venous Thromboembolism (especially post-operatively)

Thromboprophylaxis in Non-Valvular AF

Treatment fo Venous Thromboembolism

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44
Q

State side effects of Rivaroxaban

A

Nausea

Bleeding

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45
Q

Describe important pharmacodynamic/pharmacokinetic features of Rivaroxaban

A

Predictable drug interactions (metabolised by CYP450 and CYP3A4)

No need for therapeutic monitoring

Currently no available antidote

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46
Q

Describe important pieces of patient information that should be given with Rivaroxaban

A

Risk of bleeding

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47
Q

To which class of drugs does Apixaban belong?

A

Factor Xa Antagonists

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48
Q

Describe the MOA of Apixaban

A

Inhibits conversion of prothrombin to thrombin, thereby reducing concentration of thrombin in the blood

This inhibits formation of fibrin clots

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49
Q

State indications for Apixaban

A

Prophylaxis of Venous Thromboembolism Following Hip or Knee Replacement Surgery

Thromboprophylaxis in Non-Valvular AF

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50
Q

State side effects of Apixaban

A

Nausea

Bleeding

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51
Q

Describe important pharmacodynamic/pharmacokinetic features of Apixaban

A

Predictable Drug Interactions (metabolised by CYP450 and subtrate for p glycoprotein)

75% is metabolised by the liver, the rest is renally excreted

No need for therapeutic monitoring

Currently no available antidote

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52
Q

Describe important pieces of patient information that should be given with Apixaban

A

Risk of bleeding

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53
Q

Give examples of drugs in the class of ‘Cardioselective Beta Blockers’

A

Atenolol

Bisoprolol

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54
Q

Describe the MOA of Cardioselective Beta Blockers

A

e.g. Atenolol and Bisoprolol

Preferentially block Beta-1-Adrenoceptors in cardiac and renal tissue

Inhibits sympathetic stimulation of heart and renal vasculature

Blockage of the sino-atrial node reduces heart rate (negative chronotropic effect) and blockage of receptors in the myocardium depresses cardiac contractility (negative inotropic effect)

Additionally, blockade of beta-1 adrenoceptors in renal tissue inhibits the release of renin, depressing the vasoconstrictive effects of the renin-angiotensin-aldosterone system

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55
Q

State indications for the use of Cardioselective Beta Blockers such as Atenolol and Bisoprolol

A

Hypertension

Angina

Rate Control in AF

(Bisoprolol may be used as supportive therapy in mild-moderate Heart Failure)

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56
Q

State side effects of Cardioselective Beta Blockers such as Atenolol and Bisoprolol

A

Bradycardia

Hypotension

Bronchospasm

Fatigue

Cold Extremities

Sleep Disturbance

Loss of Hypoglycaemic Awareness

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57
Q

Describe important pharmacodynamic/pharmacokinetic features of Cardioselective Beta Blockers such as Atenolol and Bisoprolol

A

Avoid higher doses and use with caution in patients with COPD/Asthma due to risk of bronchospasm

Avoid in patients with a history of frequent hypoglycaemia

Do not combine with Rate Limiting Ca2+ Channel Blockers in anti-hypertensive therapy due to risk of heart block

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58
Q

Describe important pieces of patient information that should be given with Cardioselective Beta Blockers such as Atenolol and Bisoprolol

A

Compliance is important as patients may stop the drug as they don’t feel physically better - but should be reminded that HTN is asymptomatic but dangerous and needs to be controlled

Fatigue and cold extremities are common side effects

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59
Q

Give examples of Non-Cardioselective Beta Blockers

A

Propranolol

Carvedilol

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60
Q

Describe the MOA of Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol

A

Propranolol - Non-Cardioselective Beta-1-Adrenoceptor Agonist

Carvedilol - Non-Selective Beta-1, Beta-2 and Alpha-1-Adrenergic Receptor Antagonistic Effects

Inhibits sympathetic activity in the heart and vascular smooth muscle

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61
Q

State indications for Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol

A

Hypertension

Anxiety

Angina

Migraine Prophylaxis

Post-MI Prophylaxis

(Carvedilol may be used as supportive therapy for mild-moderate heart failure)

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62
Q

State side effects of Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol

A

Bradycardia

Hypotension

Bronchospasm

Fatigue

Cold Extremities

Sleep Disturbances

Loss of Hypoglycaemic Awareness

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63
Q

Describe important pharmacodynamic/pharmacokinetic features of Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol

A

Caution in diabetic patients due to risk of deranged carbohydrate metabolism

Avoid in patients with Asthma/COPD due to risk of bronchospasm

Do not combine with Rate Limiting Ca2+ Channel Blockers (Verapamil/Diltiazem) in anti-hypertensive therapy

Propranolol is lipid-soluble and predominantly cleared by the liver, therefore, should be avoided in liver impairment and abrupt withdrawal should be avoided due to risk of liver impairment

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64
Q

Describe important pieces of patient information that should be given with Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol

A

Nightmares and sleep disturbances may occur

Compliance is important as patients may stop drugs if they do not feel a physical benefit but should be reminded that HTN is asymptomatic but dangerous and needs to be controlled

Fatigue and cold extremities are common side effects

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65
Q

Give examples of ACE Inhibitors

A

Ramipril

Enalapril

Lisinopril

Perindopril

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66
Q

Describe the MOA of ACE Inhibitors

A

Inhibits conversion of AngI to AngII (a potent vasoconstrictor)

This subsequently inhibits aldosterone release from the adrenal cortex, depressing renal sodium and fluid retention to decrease blood volume

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67
Q

State indications of ACE Inhibitors

A

Hypertension

Heart Failure

Nephropathy

Prevention of CV Events in High Risk Patients

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68
Q

State side effects of ACE Inhibitors

A

Dry Cough

Hypotension

Hyperkalaemia

Renal Impairment

Angiodema

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69
Q

Describe important pharmacodynamic/pharmacokinetic features of ACE Inhibitors

A

Adverse drug reactions are higher in patients with:

High Dose Diuretics

Hypovolaemia

Hyponatraemia

Hypotension

Unstable Heart Failure

Renovascular Disease

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70
Q

Describe important pieces of information that should be given with ACE Inhibitors

A

Blood test require at 1-2 weeks to check electrolyte balance

Dry cough is a common (10%) side effect

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71
Q

Give examples of Nitrates

A

Isosorbide Mononitrate

Glyceryl Trinitrate (GTN)

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72
Q

Describe the MOA of Nitrates

A

Converted to Nitric Oxide (NO), a potent vasodilator

Cardioselective, acting mainly on coronary blood vessels to enhance blood flow to ischaemic areas of the myocardium

Also reduces myocardial oxygen demand by reducing cardiac afterload and preload

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73
Q

State indications for Nitrates

A

Treatment of Angina

Severe HTN (IV GTN may be used)

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74
Q

State side effects of Nitrates

A

Headaches

Postural Hypotension

Dizziness

Tachycardia

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75
Q

Describe important pharmacodynamic/pharmacokinetic features of Nitrates

A

Tolerance develops with long-term use

In order to avoid tolerance, patients should have a daily nitrate-free period

Isosorbide Mononitrate: Oral, Longer Duration of Action than GTN

GTN: Rapidly inactivated by first pass metabolism, Sublingual Spray/Tablet only or IV

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76
Q

Describe important pieces of patient information that should be given with Nitrates

A

Headache is a common initial side effect but incidence decreases with long term use

GTN should be taken before activity that brings on angina

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77
Q

Give two examples of Rate Limiting Calcium Channel Blockers

A

Verapamil

Diltiazem

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78
Q

Describe the MOA of Rate Limiting Calcium Channel Blockers

A

Prevent cellular entry of Ca2+ by blocking L-type calcium channels

Myocardial and Smooth muscle contractility is depressed

Cardiac contractility will be reduced

Dilate coronary blood vessels and reduce afterload

Antidysrhythmic actions due to prolonged atrioventricular node conduction – depresses heart rate

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79
Q

State indications for Rate Limiting Calcium Channel Blockers

A

Supraventricular Arrhythmias

Angina

Hypertension

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80
Q

State side effects of Rate Limiting Calcium Channel Blockers

A

Verapamil - Constipation, Flushing, Headache, Dizziness, Hypotension

Diltiazem - GI Disturbances, Bradycardia, Peripheral Oedema, Dizziness, Headache, Hypotension

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81
Q

Describe important pharmacodynamic/pharmacokinetic features of Rate Limiting Calcium Channel Blockers

A

Contra-indicated in heart failure and LV dysfunction due to potent negative inotropy

Avoid in bradycardia and hypotension

Do not use with beta-blockers

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82
Q

Describe important pieces of patient information that should be given with Rate Limiting Calcium Channel Blockers

A

Constipation is a common side effect with Verapamil

Ankle swelling is a common side effect with Diltiazem, hot weather making it worse

Compliance is important – Patients may stop Calcium-channel blockers if they do not feel any better

Remind them that hypertension is asymptomatic but nonetheless a dangerous risk factor that needs controlled

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83
Q

Give examples of Non-Rate Limiting Calcium Channel Blockers

A

Amlodipine

Nifedipine

Felodipine

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84
Q

Describe the MOA of Non-Rate Limiting Calcium Channel Blockers

A

Prevent cellular entry of Ca2+ by blocking L-type calcium channels

Myocardial and smooth muscle contractility depressed – these drugs mainly affect smooth muscle

Dilate coronary blood vessels and reduce afterload

These drugs do not lower heart rate (heart rate may increase)

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85
Q

State indications for Non-Rate Limiting Calcium Channel Blockers

A

Hypertension

Angina

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86
Q

State side effects of Non-Rate Limiting Calcium Channel Blockers

A

Ankle Oedema

Nausea

Abdominal Pain

Palpitations

Headaches

Dizziness

Flushing

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87
Q

Describe important pharmacodynamic/pharmacokinetic features of Non-Rate Limiting Calcium Channel Blockers

A

Avoid in:

Cardiogenic Shock, Unstable Angina, Significant Aortic Stenosis

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88
Q

Describe important pieces of patient information that should be given with Non-Rate Limiting Calcium Channel Blockers

A

Compliance is important – Patients may stop Calcium Channel Blockers if they do not feel any better

Remind them that hypertension is asymptomatic but nonetheless a dangerous risk factor that needs controlled

Ankle swelling is a common side effect, hot weather making it worse

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89
Q

Give examples of HMG CoA-Reductase Inhibitors

A

Atorvastatin

Simvastatin

Pravastatin

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90
Q

Describe the MOA of HMG CoA-Reductase Inhibitors

A

Competitively inhibits HMG CoA Reductase; the rate-determining enzyme in the mevalonate pathway synthesis of cholesterol

This causes an increase in LDL-receptor expression, on the surface of hepatocytes

Increases hepatic uptake of cholesterol, reducing plasma cholesterol levels

Reduces development of athersclerotic plaques

Statins may have additional pleotropic effects

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91
Q

State indications for HMG CoA-Reductase Inhibitors

A

Familial Hypercholesterolaemia

Prevention of CV Events in High-Risk Patients

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92
Q

State side effects of HMG CoA-Reductase Inhibitors

A

Myalgia

Myopathy and Rhabdomyolysis

GI Disturbances

LFT Derangement

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93
Q

Describe important pharmacodynamic/pharmacokinetic features of HMG CoA-Reductase Inhibitors

A

Myalgia and Rhabdomyolysis are dose-related, so begin with a low dose especially in patients with previous side effects

Hypothyroidism should be corrected before assessing need for Statin use

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94
Q

Describe important pieces of patient information that should be given with HMG CoA-Reductase Inhibitors

A

Report any unexplained muscle pains to their GP, who will check a creatine kinase blood level

Diarrhoea and abdominal pain may be present initially

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95
Q

To which class of drug does Digoxin belong?

A

Cardiac Glycosides

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96
Q

Describe the MOA of Digoxin

A

Increases vagal parasympathetic activity and inhibits the Na+/K+ pump, causing a buildup of Na+ intracellularly

In an effort to remove Na+, more Ca2+ is brought into the cell by the action of Na+/Ca2+ exchangers

The buildup of Ca2+ is responsible for the increased force of contraction and reduced rate of conduction through the AV node

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97
Q

State indications for Digoxin

A

Heart Failure

Rate Control in AF

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98
Q

Describe side effects of Digoxin

A

Nausea

Vomiting

Diarrhoea

Confusion

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99
Q

Describe important pharmacodynamic/pharmacokinetic features of Digoxin

A

Digoxin has a narrow therapeutic index

Symptoms of digoxin toxicity are similar to effects of clinical deterioration

Additionally, the plasma-concentration is not a reliable indicator of toxicity

Digoxin-specific antibody fragments are used for life-threatening digoxin overdose

Digoxin has a long half-life and maintenance doses may only be required once-daily

Renal function, age and heart disease are major determinants for safe digoxin dosage

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100
Q

Describe important pieces of patient information that should be given with Digoxin

A

Risk of Toxicity

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101
Q

State the class of drug to which Amiodarone belongs

A

Anti-Arrhythmics

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102
Q

Describe the MOA of Amiodarone

A

Amiodarone blocks cardiac K+ channels, prolonging repolarization of the cardiac action potential to restore regular sinus rhythm

It also slows atrioventricular nodal conduction

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103
Q

State indications for Amiodarone

A

Supraventricular/Ventricular Arrhythmias

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104
Q

State 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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105
Q

Describe important pharmacodynamic/pharmacokinetic features of Amiodarone

A

Very long half-life, once daily dosing, can take weeks-months to achieve steady-state amiodarone-plasma concentrations

Thyroid function tests should be performed before treatment and every six months, or where symptomatic

LFTs should be taken during treatment

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106
Q

Describe important pieces of patient information that should be given with Amiodarone

A

Requires good compliance and attendance for monitoring blood tests

Avoid exposure to the sun, wear protective clothing and sunscreen

Report presence of rash after use (hypersensitivity risk)

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107
Q

Give examples of drugs in the Penicillins class

A

Flucloxacillin

Amoxicillin

Benzylpenicillin

Penicillin V

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108
Q

Describe the MOA of Penicillins

A

Attaches to penicillin-binding-proteins on forming bacterial cell walls

This inhibits the transpeptidase enzyme which cross-links the bacterial cell wall

Failure to cross-link induces bacterial cell autolysis

Amoxicillin provides some amount of gram-negative cover in addition to gram-positive

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109
Q

State indications for Penicillins

A

Different drugs in the class have different indications due to having different spectrums of cover

Flucloxacillin provides Staph. Aureus cover whereas Amoxicillin does not

Flucloxacillin: Soft Tissue Infection, Staphylococcal Endocarditis, Otitis Externa

Amoxicillin: Non-Severe CAP

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110
Q

State side effects of Penicillins

A

Diarrhoea

Vomiting

Impaired Liver Function

Hypersensitivity Reaction

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111
Q

Describe important pharmacodynamic/pharmacokinetic features of Penicillins

A

Good Oral Absorption

Flucloxacillin: Beta-Lactamase Stable/Insensitive

Amoxicillin: Beta-Lactamase Susceptible (often combined with Claculinic Acid, a beta-lactamase inhibitor)

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112
Q

Describe important pieces of patient information that should be given with Penicillins

A

Return if symptoms persist after the course of antibiotics, may be infected with resistant organism

Diarrhoea is a common side effect

Report any incidence of a rash after use – risk of hypersensitivity reactions

To overcome resistance in bacteria that secrete Beta-lactamase, a Beta-lactamase inhibitor is given with the penicillin.

An example is Clavulonic Acid, when combined with amoxicillin, it forms co-amoxiclav.

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113
Q

Give two example of Cephalosporin antibiotics

A

Ceftriaxone

Cephalexin

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114
Q

Describe the MOA of Cephalosporins

A

Attaches to penicillin-binding-proteins on forming bacterial cell walls

This inhibits the transpeptidase enzyme which cross-links the bacterial cell wall

Failure to cross-link induces bacterial cell autolysis

Less susceptible to beta-lactamases than penicillins

Both Gram +ve and -ve Cover

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115
Q

State indications for Cephalosporins

A

Serious Infection: Septicaemia, Pneumonia, Meningitis

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116
Q

State side effects of Cephalosporins

A

Hypersensitivity Reactions

Antibiotics Associated C. Diff

Impaired Liver Function

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117
Q

Describe important pharmacodynamic/pharmacokinetic features of Cephalosporins

A

Renal Excretion

Longer Half-Life, Needs to be given once daily

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118
Q

Describe important pieces of patient information that should be given with Cephalosporins

A

Diarrhoea is a common side effect

Report any incidence of a rash after use – risk of hypersensitivity reactions

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119
Q

To which class of drug does Vancomycin belong?

A

Glycopeptide Antibiotic

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120
Q

Describe the MOA of Vancomycin

A

Bactericidal, inhibiting cell-wall synthesis in Gram +ve bacteria

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121
Q

State indications for Vancomycin

A

Severe Gram +ve Infections

MRSA

Severe C. Diff

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122
Q

State side effects of Vancomycin

A

Fever

Rash

Local Phlebitis at Injection Site

Nephrotoxicity

Ototoxicity

Blood Disorders, inc. Neutropenia

Anaphylactoid Reaction (Red Many Syndrome is Infusion Rate Too Fast)

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123
Q

Describe important pharmacodynamic/pharmacokinetic features of Vancomycin

A

Can either be given as a continuous intravenous infusion or as a pulsed infusion regimen

Long duration of action, can be given every 12 hours

Therapeutic drug-monitoring should be undertaken as Vancomycin has a narrow therapeutic range

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124
Q

Describe important pieces of patient information that should be given with Vancomycin

A

Risk of kidney damage

Patients should report any changes in hearing

Regular blood tests required for monitoring

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125
Q

State the class of drug to which Gentamicin belongs

A

Aminoglycosides

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126
Q

Describe the MOA of Gentamicin

A

Binds to 30s ribosomal subunit, inhibiting protein synthesis, inducing a prolonged post-antibiotic bacteriostatic effect

Additionally, bactericidal action on bacterial cell wall results in rapid killing early in dosing interval and is prominent at high doses

Also provides a synergistic effect when used alongside other antibiotics (such as flucloxacillin or vancomycin in gram-positive infections)

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127
Q

State indications for Gentamicin

A

Severe Gram -ve Infection (e.g. Biliary Tract Infection, Pyelonephritis, Hospital Acquired Pneumonia)

Some Gram +ve Infections (e.g. Soft Tissue Infection and Endocarditis)

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128
Q

State side effects of Gentamicin

A

Nephrotoxicity

Ototoxicity

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129
Q

Describe important pharmacodynamic/pharmacokinetic features of Gentamicin

A

Give high initial dose to take advantage of rapid killing

Leave long dosing interval to minimise toxicity

Measure trough level to ensure gentamicin is not accumulating and only prescribe further doses once this is confirmed

Try to limit use to approximately 3 days to minimise risk of side-effects

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130
Q

Describe important pieces of patient information that should be given with Gentamicin

A

Ask patients to report any change to their hearing

Risk of kidney damage so monitoring of drug levels and renal function tests are required

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131
Q

State the class of drug to which Ciprofloxacin belongs

A

Quinolone

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132
Q

Describe the MOA of Ciprofloxacin

A

Interferes with bacterial DNA replication and repair

Broad spectrum bactericidal antibiotic, provides both Gram +ve and -ve cover

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133
Q

State indications for Ciprofloxacin

A

Gram -ve Bacterial Infection

Respiratory Tract Infection

Upper UTI

Peritoneal Infection

Gonorrhoea

Prostatitis

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134
Q

State side effects of Ciprofloxacin

A

GI Toxicity

QT Segment Prolongation

C. Diff Infection

Tendonitis

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135
Q

Describe important pieces of patient information that should be given with Ciprofloxacin

A

Risk of diarrhoea after use

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136
Q

Give two examples of Macrolide antibiotics

A

Clarithromycin

Erythromycin

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137
Q

Describe the MOA of Macrolide antibiotics

A

Binds to 50s ribosomal subunit

Inhibits bacterial protein synthesis

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138
Q

State indications for Macrolide antibiotics

A

Atypical Organisms Causing Pneumonia

Severe CAP

Severe Campylobacter Infection

Mild-Moderate Skin and Soft Tissue Infection

Otitis Media

Lyme Disease

H.Pylori Eradication Therapy

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139
Q

State side effects of Macrolide antibiotics

A

Diarrhoea

Vomiting

QT Segment Prolongation

Ototoxicity

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140
Q

Describe important pharmacodynamic/pharmacokinetic features of Macrolide antibiotics

A

Uses hepatic enzyme Cytochrome P450 pathway

Can interact with all drugs using this pathway, especially Simvastatin, Atorvastatin and Warfarin

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141
Q

Describe important pieces of patient information that should be given with Macrolide antibiotics

A

Risk of Diarrhoea

Senses of smell and taste may be disturbed during therapy

Tooth and tongue discolouration may occur during therapy

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142
Q

State the class of drug to which Trimethoprim belongs

A

Inhibitor of Folate Synthesis

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143
Q

Describe the MOA of Trimethoprim

A

Inhibits folate metabolism pathway and leads to impaired nucleotide synthesis

Therefore interferes with bacterial DNA replication

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144
Q

State indications for Trimethoprim

A

1st Line Antibiotic in Uncomplicated UTI

Acute/Chronic Bronchitis

Pneumocystis Pneumonia

Good Range of Gram +ve and -ve Cover

Some MRSA Cover

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145
Q

State side effects of Trimethoprim

A

Elevated Serum Creatinine

Hyperkalaemia

Depressed Haematopoiesis

Rash

GI Disturbance

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146
Q

Describe important pharmacodynamic/pharmacokinetic features of Trimethoprim

A

Penetrates well into the prostate, suitable for men with uncomplicated UTI

Avoid in the first trimester of pregnancy

Resistant organisms are a major problem in clinical use

Hyperkalaemia is more common in patients with impaired renal function

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147
Q

Describe important pieces of patient information that should be given with Trimethoprim

A

Blood tests required in those at risk of hyperkalaemia

Return to the doctor if symptoms do not clear after trimethoprim course, resistance does occur

Rash and GI disturbances are common adverse reactions

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148
Q

State the class of drug to which Aciclovir belongs

A

Anti-Virals

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149
Q

Describe the MOA of Aciclovir

A

A guanosine derivative converted to triphosphate by infected host cells

Aciclovir triphosphate then inhibits DNA polymerase, terminating the nucleotide chain and inhibiting viral DNA replication

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150
Q

State indications for Aciclovir

A

Herpes SImplex Infection

Varicella Zoster Infection

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151
Q

State side effects of Aciclovir

A

Nausea

Vomiting

Local Inflammation at Infusion Site (IV Only)

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152
Q

Describe important pharmacodynamic/pharmacokinetic features of Aciclovir

A

Can be given orally, intravenously or topically

Penetrates well into the CSF with CSF concentrations being 50% concentration of that of plasma

Excreted by the kidneys so dose adjustment is needed in renal impairment

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153
Q

Describe important pieces of patient information that should be given Aciclovir

A

Multiple/repeat doses may be required in immunosuppressed patients

Type of infection or recurrent infections may prompt HIV infection

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154
Q

State the class of drug to which Salbutamol belongs

A

Beta-Adrenergic Bronchodilators

(Short-Acting)

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155
Q

Describe the MOA of Salbutamol

A

Short-acting Beta-2 adrenoceptor agonists (SABA)

Relaxes bronchial smooth muscle, inducing bronchodilation

Inhibit pro-inflammatory cytokine release from mast cells and TNF-α release from monocytes, reducing airway inflammation

Increase mucus clearance from the airways by stimulating cilia action

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156
Q

State indications for Salbutamol

A

Asthma

COPD

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157
Q

State side effects of Salbutamol

A

Tremor

Tachycardia

Cardiac Dysrhythmia

Headache

Sleep Disturbance

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158
Q

Describe important pharmacodynamic/pharmacokinetic features of Salbutamol

A

Only a small percentage of inhaled drug reaches target in the airways (a spacer may improve delivery)

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159
Q

Describe important pieces of patient information that should be given with Salbutamol

A

Check inhaler technique, review the need for spacer / nebuliser

In exercise-induced-asthma, a dose immediately before exercise can reduce incidence of symptoms

If required more than once daily, treatment needs reviewed

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160
Q

State the class of drug to which Salmeterol belongs

A

Beta-Adrenergic Bronchodilators

(Long-Acting)

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161
Q

Describe the MOA of Salmeterol

A

Long-acting Beta-2 adrenoceptor agonist (LABA)

Relaxes bronchial smooth muscle, inducing bronchodilation

Inhibit pro-inflammatory cytokine release from mast cells and TNF-α release from monocytes, reducing airway inflammation

Increase mucus clearance from the airways by stimulating cilia action

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162
Q

State indications for Salmeterol

A

Asthma

COPD

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163
Q

State side effects of Salmeterol

A

Tremor

Tachycardia

Cardiac Dysrhythmia

Headache

Sleep Disturbance

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164
Q

Describe important pharmacodynamic/pharmacokinetic features of features of Salmeterol

A

Not to be commenced in patients with rapidly deteriorating asthma due to slower onset of action than SABAs

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165
Q

Describe important pieces of patient information that should be given with Salmeterol

A

Report any deterioration in symptoms following initiation of LABA

Do not exceed stated dose

Seek medical advice when stated dose fails to control symptoms

166
Q

Give two examples of Anti-Muscarinic Bronchodilators

A

Tiotropium

Ipratropium Bromide

167
Q

Describe the MOA of Anti-Muscarinic Bronchodilators

A

Muscarinic receptor (M3) antagonists producing bronchodilatory effects

Reduces mucus secretion and may increase bronchial mucus clearance by stimulating cilia

168
Q

State indications for Anti-Muscarinic Bronchodilators

A

Asthma

COPD

Rhinitis

169
Q

State side effects of Anti-Muscarinic Bronchodilators

A

Dry Mouth

Cough

Constipation

170
Q

Describe important pharmacodynamic/pharmacokinetic features of Anti-Muscarinic Bronchodilators

A

Inhaled and poorly absorbed into the circulation – unable to affect systemic muscarinic/cholinergic receptors

Nebulised Ipratropium Bromide should always be administered via a mouthpiece to minimize the risk of acute angle closure glaucoma

171
Q

Describe important pieces of patient information that should be given with Anti-Muscarinic Bronchodilators

A

Good inhaler technique improves efficacy

Cough may arise

172
Q

State the class of drug to which Beclomethasone belongs

A

Inhaled Corticosteroids

173
Q

Describe the MOA of Beclomethasone

A

Anti-inflammatory effect on the airways

Decreases formation of pro-inflammatory cytokines

Up-regulates Beta-2 Adrenoceptor in airways

174
Q

State indications for Beclomethasone

A

Asthma

COPD

175
Q

State side effects of Beclomethasone

A

Oral Candidiasis (Thrush)

Adrenal Suppression

Osteoporosis

176
Q

Describe important pharmacodynamic/pharmacokinetic features of Beclomethasone

A

Takes several weeks to months for full effect of therapy

Spacer devices can reduce risk of thrush and improve drug delivery

177
Q

Describe important pieces of patient information that should be given with Beclomethasone

A

If on higher doses, should carry a steroid card

Increase dose during periods of illness

178
Q

Give example of Anti-Histamine (H1 Receptor Antagonist) drugs

A

Chlorpheniramine

Desloratidine

Fexofenadine

Hydroxyzine

179
Q

Describe the MOA of Anti-Histamines

A

H1 Receptor Antagonists

Inhibit histamine-mediated contraction and vasodilation of the bronchial smooth muscle

180
Q

State indications for Anti-Histamines

A

Anaphylaxis

Hay Fever

Urticaria

Sedation

181
Q

State side effects of Anti-Histamines

A

Drowsiness

Tinnitus

182
Q

Describe important pharmacodynamic/pharmacokinetic features of Anti-Histamines

A

Renally excreted

Sedation arises from CNS H1 antagonism (second generation H1 antagonists do not cross BBB in therapeutic doses)

183
Q

Describe important pieces of patient information that should be given with Anti-Histamines

A

Do not operate heavy machinery

Do not drive

184
Q

Describe the MOA of Levodopa

A

Pro-drug (dopamine precursor)

Crosses the BBB and is converted to dopamine

Striatal dopaminergic neurotransmission is increased

185
Q

State the indications for Levodopa

A

Parkinson’s Disease

186
Q

State side effects of Levodopa

A

Dyskinesia

Compulsive Disorders

Hallucinations

Nausea

GI Upset

187
Q

Describe important pharmacodynamic/pharmacokinetic features of Levodopa

A

Converted to dopamine in the peripheries (which can cause motor side effects)

Given with a dopamine decarboxylase inhibitor or COMT inhibitor to reduce these effects

Short half-life of 50 to 90 minutes

Rapidly absorbed from the proximal small intestine via the large neutral amino acid (LNAA) transport carrier system

188
Q

Describe important pieces of patient information that should be given with Levodopa

A

Dyskinesia is common

Reduced efficacy over time

Avoid abrupt withdrawal

189
Q

Give examples of Dopamine Agonists

A

Apomorphine

Pramipexole

Bromocriptine

Pergolide

Rotigotine

190
Q

Describe the MOA of Dopamine Agonists

A

Stimulate post-synaptic dopamine receptors

Apomorphine: Non-Selective D1 and D2 Dopamine subfamily of receptors

Pramipexole: Selective D3 Receptor

191
Q

State indications for Dopamine Agonists

A

Parkinson’s Disease

192
Q

State side effects of Dopamine Agonists

A

Apomorphine: Pain at Injection Site, Nausea and Vomiting

Pramipexole: Hallucinations, Nausea, Drowsiness, Involuntary Movements

193
Q

Describe important pharmacodynamic/pharmacokinetic features of Dopamine Agonists

A

Have reduced efficacy over time

Apomorphine: Highly emetic (hence limited use), short half-life (40mins), must be given by injection

Pramipexole: Cimetidine increases its toxicity, long half-life (8hrs)

194
Q

Describe important pieces of patient information that should be given with Dopamine Agonists

A

Apomorphine can only be injected

Dopamine Agonists are weaker than L-Dopa so treatment may need to be modified in time

195
Q

State the class of drug to which Entacapone belongs

A

Catechol-o-methyl Transferase (COMT) Inhibitor

196
Q

Describe the MOA of Entacapone

A

Prevents peripheral breakdown of levodopa by inhibiting COMT (COMT converts L-Dopa into 3-OMD which does not cross the BBB)

Therefore, more levodopa reaches the brain

197
Q

State indications for Entacapone

A

Parkinson’s Disease

In conjuncion with L-Dopa and Dopamine Decarboxylase Inhibitors

198
Q

State side effects of Entacapone

A

Dyskinesia

Nausea

Abdominal Pain

Vomiting

Dry Mouth

Dizziness

199
Q

Describe important pharmacodynamic/pharmacokinetic features of Entacapone

A

Rapidly absorbed

L-Dopa dose may need to be reduced by 10-30% when given with Entacapone

200
Q

Describe important pieces of patient information that should be given with Entacapone

A

Urine may turn brown, this is normal

Could become lightheaded/dizzy while doing daily activities

Avoid abrupt withdrawal

201
Q

State the class of drug to which Carbamazepine belongs

A

Anti-Epileptic

202
Q

Describe the MOA of Carbamazepine

A

Voltage-gated Na+ channel blocker on the pre-synaptic membrane

Blocks the Na+ influx, reduces neuronal excitability and decreases the action potential

203
Q

State indications for Carbamazepine

A

Epilepsy

Trigeminal Neuralgia

Neuropathic Pain

204
Q

State side effects of Carbamazepine

A

Dizziness

Dry Mouth

Ataxia

Fatigue

Headache

Diplopia

Blurred Vision

Hyponatraemia

Stevens-Johnson Syndrome (Rare)

205
Q

Describe important pharmacodynamic/pharmacokinetic features of Carbamazepine

A

Response to the drug can be variable

Enzyme inducer of cytochrome P450 (induces metabolism of itself)

Interactions with other anti-convulsants

A transporter (RALBP1) can confer drug resistance

Grapefruit can significantly increase serum levels (bioavailability) of the drug

HLA-B 1502 allele raises the risk for SJS, avoid in these patients

206
Q

Describe important pieces of patient information that should be given with Carbamazepine

A

Avoid alcohol

Avoid grapefruit

207
Q

State the class of drug to which Sodium Valproate belongs

A

Anti-Epileptic

208
Q

Describe the MOA of Sodium Valproate

A

Weak sodium ion channel blocker

Inhibitor of GABA degrading enzymes

Increased GABA stops action potential

209
Q

State indications for Sodium Valproate

A

Epilepsy

Bipolar Disorder

Depression

210
Q

State side effects of Sodium Valproate

A

Nausea

Diarrhoea

Gastric Irritation

Weight Gain

Hyponatraemia

Behavioural Disturbance

Confusion

Stevens-Johnson Syndrome (Rare)

211
Q

Describe important pharmacodynamic/pharmacokinetic features of Sodium Valproate

A

Enzyme inhibitor of cytochrome P450

Rapidly absorbed from GI tract - Varies with formulation administered (liquid, solid or powder) and when administered (post-prandial or fasting)

Can cause interactions with other anti-epileptic drugs

212
Q

Describe important pieces of patient information that should be given with Sodium Valproate

A

Avoid alcohol

Take with food

Do not take with milk

LFTs must be monitored before and during the initial 6 months

VERY teratogenic, should not be given to women of child-bearing potential unless other options have been exhausted and effective contraception must be used

213
Q

State the class of drug to which Phenytoin belongs

A

Anti-Epileptics

214
Q

Describe the MOA of Phenytoin

A

Acts as a voltage-gated Na+ channel blocker on the pre-synaptic neuronal membrane

Limits action potential transmission

Hence limits spread of seizure activity

215
Q

State indications for Phenytoin

A

Epilepsy (incl. Status Epilepticus)

Trigeminal Neuralgia

216
Q

State side effects of Phenytoin

A

Insomnia

Headache

Rash

Constipation

Vomiting

Gingival Hyperplasia

Liver Damage

Stevens-Johnson Syndrome

Leucopenia

Thrombocytopenia

217
Q

Describe important pharmacodynamic/pharmacokinetic features of Phenytoin

A

Enzyme inducer of cytochrome P450

Can cause interactions with other anti-epileptic drugs

Narrow therapeutic index

Relationship between dose and plasma concentration in non-linear

218
Q

Describe important pieces of patient information that should be given with Phenytoin

A

Avoid alcohol

Do not take calcium, aluminium, magnesium or iron supplements within 2 hours of ingestion

Take with food to reduce irritation

219
Q

State the class of drug to which Lamotrigine belongs

A

Anti-Epileptic

220
Q

Describe the MOA of Lamotrigine

A

Varied MOA

Inhibits voltage-gated Na+ channels and/or Ca2+ channels

Acts on pre-synaptic neuronal membrane

Reduces action potential and excitatory signals

221
Q

State indications for Lamotrigine

A

Epilepsy (Focal and Generalised Seizures)

Depressive Disorders associated with Bipolar Disorder

222
Q

State side effects of Lamotrigine

A

Nausea

Vomiting

Diarrhoea

Tremor

Insomnia

Blurred Vision

Aggression

Skin Reactions (incl. Stevens-Johnson Syndrome and Toxic Epidermal Necrolysis)

223
Q

Describe important pharmacodynamic/pharmacokinetic features of Lamotrigine

A

Half-life doubles in chronic renal impairment so dose adjustment is required

224
Q

Describe important pieces of patient information that should be given with Lamotrigine

A

Take without regard to meals

Seeks medical advice if any rash or signs/symptoms of hypersensitivity

225
Q

State the class of drug to which Levetiracetam

A

Anti-Epileptic

226
Q

Describe the MOA of Levetiracetam

A

SV2A is a synaptic vesicle protein required for neurotransmitter release

Levetiracetam blocks this and reduces neurotransmitter release

Induces an anti-epileptic effect

227
Q

State indications for Levetiracetam

A

Epilepsy

228
Q

State side effects of Levetiracetam

A

Headache

Fatigue

Anxiety

Irritability

Drowsiness

Constipation

229
Q

Describe important pharmacodynamic/pharmacokinetic features of Levetiracetam

A

Rapidly and almost completely absorbed after oral administration (99%)

Food does not affect bioavailability

Cytochrome P450 is not involved in its metabolism

230
Q

Describe important pieces of patient information that should be given with Levetiracetam

A

May affect ability to drive or operate machinery

Not recommended during pregnancy or breast feeding

231
Q

Give examples of Selective Serotonin Reuptake Inhibitors (SSRIs)

A

Citalopram

Fluoxetine

Paroxetine

Escitalopram

Sertraline

232
Q

Describe the MOA of SSRIs

A

Inhibition 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

233
Q

State indications for SSRIs

A

Depression

Bulimia

Obsessive Compulsive Disorder

234
Q

State side effects of SSRIs

A

Dry Mouth

Nausea

Insomnia

Anxiety

Decreased Libido

Seizures

Dyskinesia

235
Q

Describe important pharmacodynamic/pharmacokinetic features of SSRIs

A

SSRIs bind with less affinity to histamine, acetylcholine and noradrenaline receptors than TCAs leading to fewer side effects

Less dangerous in overdose than TCAs

236
Q

Describe important pieces of patient information that should be given with SSRIs

A

Be wary with alcohol, toxicity is possible

Improvement in depressive symptoms may take several weeks to occur

Abrupt discontinuation of SSRIs may cause withdrawal symptoms (fatigue, tremor, sweating)

237
Q

Give examples of Tricyclic Antidepressants (TCAs)

A

Amitriptyline

Imipramine

Doxepin

238
Q

Describe the MOA of TCAs

A

Stops the reuptake of monoamines

Binds to monoamine pump at pre-synaptic cleft

The reduced reuptake of noradrenaline and/or serotonin combats depression

239
Q

State indications for TCAs

A

Depression

Panic Disorders

Neuropathic Pain

240
Q

State side effects of TCAs

A

Sedation (anti-histaminergic effects)

Postural Hypotension, Tachycardia (anti-adrenergic effects)

Urinary Retention, Dry Mouth, Blurred Vision, Diplopia (anti-cholinergic effects)

241
Q

Describe important pharmacodynamic/pharmacokinetic features of TCAs

A

Blocks histamine H1 receptors, alpha1 adrenergic receptors and muscarinic receptors which accounts for their sedative, hypotensive and anti-cholinergic effects

Well absorbed orally

First pass effect from the liver

242
Q

Describe important pieces of patient information that should be given with TCAs

A

Reduction in depressive symptoms may take several weeks to appear

TCA overdose can be serious and cause seizures and cardiac arrythmias

243
Q

Give examples of Anti-Psychotic drugs

A

1st Generation (Act non-selectively on D1-like and D2-like receptors): Haloperidol or Chlorpromazine

Atypical (Varying effects on dopamine and serotonin receptors): Olanzapine or Clozapine

244
Q

Describe the MOA of Anti-Psychotics

A

Block dopamine receptors

Action on mesolimbic and nigrostriatal parts of brain

Also have anti-histaminergic and anti-cholinergic effects

These effects reduce positive symptoms of schizophrenia and can cause sedation and provide anti-emetic activity

245
Q

State indications for Anti-Psychotics

A

Schizophrenia

Mania

Delusions

Hallucinations

Behavioural Problems

Anti-Emetic (Haloperidol)

246
Q

State side effects of Anti-Psychotics

A

Sedation (anti-histaminergic effect)

Postural Hypotension, Tachycardia (anti-adrenergic effect)

Urinary Retention, Dry Mouth, Blurry Vision (anti-cholinergic effect)

247
Q

Describe important pharmacodynamic/pharmacokinetic features of Anti-Psychotics

A

Has effects on numerous receptor symptoms within the CNS

248
Q

Describe important pieces of patient information that should be given with Anti-Psychotics

A

Symptoms may not always disappear while on medication

Dosage may have to be increased if no improvement is made after a few weeks

249
Q

Give examples of Benzodiazepines

A

Diazepam

Lorazepam

Midazolam

250
Q

Describe the MOA 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 brain

251
Q

State indications for Benzodiazepines

A

Anxiety

Epilepsy

Muscle Spasm

Alcohol Withdrawal

252
Q

State side effects of Benzodiazepines

A

Sedation

Ataxia

Altered Mental State

Insomnia

253
Q

Describe important pharmacodynamic/pharmacokinetic features of Benzodiazepines

A

Diazepam is a long-acting benzo with active metabolites so can accumulate in long-term use and in patients with liver failure. It can be given orally, rectally or parenterally

Lorazepam accumulates less with long-term use or in patients with liver failure so is preferred in this setting. It cannot be given rectally

Midazolam is a potent and short-acting benzo typically given parenterally although buccal preparations exist

254
Q

Describe important pieces of patient information that should be given with Benzodiazepines

A

Monitor breathing and report if severe breathlessness or palpitations

Only prescribed for short terms due to risk of addiction

255
Q

Give examples (three each) of oral, topical and parenteral glucocorticoids

A

Oral - Prednisolone, Hydrocortisone, Dexamethasone

Topical - Hydrocortisone, Betamethasone, Clobetasone

Parenteral - Methylprednisolone, Hydrocortisone, Triamcinolone

256
Q

Describe the MOA of glucocorticoids

A

Bind to glucocorticoid receptors

Causes up-regulation of a variety of anti-inflammatory mediators and down-regulation of pro-inflammatory mediators

Provides immunosuppression

Also have metabolic effects including increasing gluconeogenesis and some may have a little mineralocorticoid activity

257
Q

State indications for glucocorticoids

A

Replacement in Adrenal Insufficiency

Post-Transplant Immunosuppression

Treatment of Exacerbation of Various Inflammatory Conditions (incl. Eczema, RA, IBD and MS)

Treatment of Acute Exacerbation of Asthma

258
Q

State side effects of glucocorticoids

A

Sleep Disturbance

Mood Disturbance/Psychosis

Hyperglycaemia

Immunodeficiency

Easy Bruising

Moon-Faced

Increased Abdominal Fat

Glaucoma

Striae

Hypertension

Gastric Irritation

259
Q

Describe important pharmacodynamic/pharmacokinetic features of glucocorticoids

A

Variety of different preparations are available

Drugs have differing degrees of glucocorticoid and mineralocorticoid activity

260
Q

Describe important pieces of patient information that should be given with glucocorticoids

A

Avoid Alcohol and Caffeine

Take with food to avoid gastric irritation

Don’t stop abruptly

Allway tell doctor if on prednisolone

Carry steroid card

Take a higher dose when ill

261
Q

State the relative glucocorticoid/mineralocorticoid activity of Prednisolone, Betamethasone, Hydrocortisone, Dexamethasone and Fludrocortisone

A

Prednisolone: Predominantly G, Low M

Betamethasone: Potent G, No M

Hydrocortisone: Good G and M

Dexamethasone: Potent G, Minimal or No M

Fludrocortisone: Mild-Moderate G, Potent M

262
Q

Give three examples of Anti-TNF Agents

A

Etanercept (Receptor Fusion Protein)

Infliximab (Monoclonal Antibody)

Adalimumab (Monoclonal Antibody)

263
Q

Describe the MOA of Anti-TNF Agents

A

Anti-TNF-Alpha and Anti-TNF-Beta

Blocks its interactions with TNF cell receptors

TNF Alpha and Beta are produced by macrophages and T-Cells

TNF stimulates cytokines including IL-1, 6 and 8

Therefore they reduce inflammation

264
Q

State indications for Anti-TNF Agents

A

Rheumatoid Arthritis

Psoriatic Arthritis

Ankylosing Spondylitis

Juvenile Arthritis

265
Q

State side effects of Anti-TNF Agents

A

Injection Site Reactions

Flu-Like Symptoms (Fever, Headache, Runny Nose)

Immune Deficiency (Particular risk of Legionella and Listeria and reactivation of TB)

266
Q

Describe important pharmacodynamic/pharmacokinetic features of Anti-TNF Agents

A

Given parenterally by subcutaneous injection

267
Q

Describe important pieces of patient information that should be given with Anti-TNF Agents

A

Maintain good hygiene and report symptoms of infection early

268
Q

Give examples of Immunosuppressant drugs

A

Methotrexate

Azathioprine

Mercaptopurine

269
Q

Describe the MOA of immunosuppressants

A

Disrupt DNA synthesis

Azathioprine: Blocks purine synthesis mainly in lymphocytes

Methotrexate: Stops the action of the enzyme dihydrofolate needed for production of DNA

270
Q

State indications for immunosuppressant drugs

A

Post Transplantation Immunosuppression

Inflammatory Bowel Disease

Renal Vasculitis

Paediatric Leukaemia (Methotrexate)

271
Q

State side effects of immunosuppressant drugs

A

Bone Marrow Suppression (Leucopenia)

Risk of Infection

Nephrotoxicity

Hepatotoxicity

Seizures

GI Upset

Mucosal Ulceration

Alopecia

272
Q

Describe important pharmacodynamic/pharmacokinetic features of immunosuppressant drugs

A

Does not cross the BBB

Undergo hepatic metabolism

Oral absorption is dose-dependent

Patients with low levels of thiopurine methyltransferase activity are more prone to azathioprine and mercaptopurine related marrow suppression

273
Q

Describe important pieces of patient information that should be given with immunosuppressant drugs

A

Limit caffeine intake

Take without regard to meals

274
Q

Give examples of Proton Pump Inhibitors

A

Omeprazole

Lansoprazole

Pantoprazole

275
Q

Describe the MOA of PPIs

A

Bind to H/K ATPase pump on gastric parietal cells

Reduces HCl production and hence reduces gastric acidity

276
Q

State indications for PPIs

A

Peptic Ulcers

Gastro-Oesophageal Reflux Disease

H. Pylori Infection

Prophylaxis in Patiens Receiving Long Term NSAIDs

277
Q

State side effects of PPIs

A

Nausea

Vomiting

Insomnia

Vertigo

Headaches

278
Q

Describe important pharmacodynamic/pharmacokinetic features of PPIs

A

Omeprazole is an inhibitor of cytochrome P450 enzymes

279
Q

Describe important pieces of patient information that should be given with PPIs

A

Avoid alcohol

Take 30-60 minutes before food

280
Q

Give examples of H2 receptor antagonists

A

Ranitidine

Cimetidine

Famotidine

Nizatidine

281
Q

Describe the MOA of H2 receptor antagonists

A

Histamine binds to H2 receptors on gastric parietal cells stimulating gastric acid secretion

Drugs antagonise the effect of histamine at these H2 receptors

Reduced cAMP and hence reduced activity of H/K ATPase pump

282
Q

State indications for H2 receptor antagonists

A

Peptic Ulcer

Gastro-Oesophagal Reflux Disease

Zollinger-Ellison Syndrome

283
Q

State side effects of H2 receptor antagonists

A

Headache

Dizziness

Diarrhoea

Reduced B12 Absorption

Gynaecomastia

284
Q

Describe important pharmacodynamic/pharmacokinetic features of H2 receptor antagonists

A

Cimetidine is an inhibitor of cytochrome P450 enzymes

285
Q

Describe important pieces of patient information that should be given with H2 receptor antagonists

A

Avoid a high protein diet

Take without regard to meals

286
Q

Give examples of Laxatives

A

Lactulose

Senna

287
Q

Describe the MOA of Laxatives

A

Bulk Producing Agent (e.g. Lactulose) - Reduces water reabsorption in the intestine, pulling water into the bowel and thus promotes distention and movement

Stimulant/Irritant (e.g. Senna) - Acts on intestinal mucosa to alter water and electrolyte secretion

Stool Softeners - Add more water and fat into the stool

Hydrating Agents (e.g. Milk of Magnesia) - Intestines hold more water

288
Q

State indications for Laxatives

A

Constipation

Pregnancy

Prophylaxis in Opiate Analgesic Use

289
Q

State side effects of Laxatives

A

Dehydration

Salt Loss

Abdominal Cramps

Fatigue

290
Q

Describe important pharmacodynamic/pharmacokinetic features of Laxatives

A

Lactulose - Consists of the monosaccharides fructose and galactose. Breakdown of this in the intestine by colonic bacteria increases osmotic pressure

Senna - Recommended for short-term use only due to risk of organ failure with long term use or abuse

291
Q

Describe important pieces of patient information that should be given with Laxatives

A

Take liberally without regard to meals

292
Q

To which class of drug does Cyclizine belong?

A

Anti-Emetic

293
Q

Describe the MOA of Cyclizine

A

H1 Histamine Receptor Antagonist

Acts on vomiting centre in the medullary region

Mild anti-cholinergic and anti-muscarinic effects

294
Q

State indications for Cyclizine

A

Nausea and Vomiting

Motion Sickness

Vertigo and Dizziness

Prophylaxis alongisde chemotherapy and opiate analgesic use

295
Q

State side effects of Cyclizine

A

Headache

Sedation

Diarrhoea

296
Q

Describe important pharmacodynamic/pharmacokinetic features of Cyclizine

A

Can also be a central nervous system depressant

297
Q

Describe important pieces of patient information that should be given with Cyclizine

A

Avoid alcohol

Food may reduce irritation

Take without regard to meals

298
Q

To which class of drug does Metoclopramide belong?

A

Anti-Emetic

299
Q

Describe the MOA of Metoclopramide

A

Dopamine D2 receptor antagonist

Raises activity in the chemoreceptor trigger zone, reducing input from afferent visceral nerves

Also increases gastric emptying and intestinal transit

Reduces oesophageal reflux

300
Q

State indications for Metoclopramide

A

Nausea

Vomiting

To increase gastric emptying

301
Q

State side effects of Metoclopramide

A

Dystonia (due to dopamine antagonism)

Confusion

Dizziness

Diarrhoea

Parkinsonism with long-term use

302
Q

Describe important pharmacodynamic/pharmacokinetic features of Metoclopramide

A

Can be given orally/parenterally

Dystonic reactions and movement disorders are more common at the extremes of age so caution is needed in these groups

303
Q

Describe important pieces of patient information that should be given with Metoclopramide

A

Avoid alcohol

Take 30 minutes before food

304
Q

To which class of drug does Prochlorperazine belong?

A

Anti-Emetic

305
Q

Describe the MOA of Prochlorperazine

A

Penothiazine anti-psychotic drug that is also used as an anti-emetic

Dopamine D2 receptor antagonist

Causes increased dopamine turnover (in mesolimbic and chemoreceptor trigger zone)

306
Q

State indications for Prochlorperazine

A

Nausea

Vomiting

Adjunct in some psychotic disorders

307
Q

State side effects of Prochlorperazine

A

Dry mouth

Tachycardia

Restlessness

Drowsiness

308
Q

Describe important pharmacodynamic/pharmacokinetic features of Prochlorperazine

A

Anti-cholinergic and alpha-adrenergic receptors antagonism occurs leading to sedation, muscle relaxation and hypotension

The dose differs substantially when given parenterally

309
Q

Describe important pieces of patient information that should be given with Prochlorperazine

A

Avoid alcohol and caffeine

Take with food and a full glass of water

310
Q

Give examples of Thiazide Diuretics

A

Bendroflumethiazide

Indapamide

Chlortalidone

311
Q

Describe the MOA of Thiazide Diuretics

A

Inhibit Na/Cl transporter at the distal convoluted tubule and collecting duct

Increases Na/Cl and water excretion

312
Q

State indications for Thiazide Diuretics

A

Hypertension

Oedema of Cardiac/Renal/Hepatic/Iatrogenic Origin

313
Q

State side effects of Thiazide Diuretics

A

Hypokalaemia

Hypomagnesaemia

Hyponatraemia

Hypercalcaemia

Hyperuricaemia

Reduced Glucose Tolerance

Hypersensitivity Reactions - Rashes, Pneumonitis

314
Q

Describe important pharmacodynamic/pharmacokinetic features of Thiazide Diuretics

A

Produces diuresis quickly within 1-2 hours

NSAIDs reduce efficacy of thiazide diuretics

Urinary symptoms are less common with the lower dose used for the treatment of hypertension

315
Q

Describe important pieces of patient information that should be given with Thiazide Diuretics

A

Urinary frequency usually not affected

Report if sudden rash

Make aware of risk of electrolyte imbalance

316
Q

Give examples of Loop Diuretics

A

Furosemide

Bumetanide

Torasemide

317
Q

Describe the MOA of Loop Diuretics

A

Na/Cl/K Symporter Antagonists

Act on the thick ascending loop of henle

Increase secretion of Na/K/Cl and water

318
Q

State indications for Loop Diuretics

A

Hypertension

Hyperkalaemia

Heart Failure

Cirrhosis of the Liver (Fluid Retention)

Nephrotic Syndrome

319
Q

State side effects of Loop Diuretics

A

Hypokalaemia

hypovolaemia

Hyperuricaemia

Metabolic Acidosis

Abdominal Pain

Ototoxicity

320
Q

Describe important pharmacodynamic/pharmacokinetic features of Loop Diuretics

A

60% absorbed in patients with normal renal function

Renal and hepatic excretion - increased half-life for patients with renal or hepatic disease

321
Q

Describe important pieces of patient information that should be given with Loop Diuretics

A

Avoid alcohol excess

Urinary frequency increases

322
Q

Describe the different insulin preparations available

A

Rapid Acting (e.g. Novorapid) - Reaches circulation within 15 minutes after injection, peaks 30 to 90 minutes later and lasts for up to 5 hours

Short Acting - Reaches circulation 30 minutes after injection, peaks 2 to 4 hours later and lasts up to 4-8 hours

Intermediate Acting - Reaches circulation in 2-6 hours and peaks 4-14 hours later and lasts for up to 20 hours

Long Acting (e.g. Glargine) - Reaches circulation in 6 to 14 hours with a minimal peak and lasts for up to 24 hours

323
Q

Describe the MOA of Insulin

A

Increases cellular uptake of glucose

Stimulates glycogenesis, encourages DNA synthesis and promotes release of growth hormone

324
Q

State indications for Insulin

A

Type 1 Diabetes Mellitus

Type 2 Diabetes Mellitus

Hyperkalemia (in conjunction with Dextrose)

325
Q

State side effects of Insulin

A

Hypoglycaemia

Sweats, Shakes, Tachycardia, Headache, Weakness, Fatigue (typically signs of hypoglycaemia)

Oedema

Injection Site Reactions

326
Q

Describe important pharmacodynamic/pharmacokinetic features of Insulin

A

Patients are given varying types of insulin combinations based on their activities and preferences

Given subcutaneously and short-acting (actrapid) can be given IV

327
Q

Describe important pieces of patient information that should be given with Insulin

A

Only in the form of an injection

Compliance is very important

Never skip a meal when on insulin

328
Q

Give two examples of Sulphonylureas

A

Gliclazide

Glimepiride

329
Q

Describe the MOA of Sulphonylureas

A

Stimulates beta cells of the pancreas to produce more insulin

Increase cellular glucose uptake and glycogenesis while reducing gluconeogenesis

330
Q

State indications for Sulphonylureas

A

Type 2 Diabetes Mellitus

331
Q

State side effects of Sulphonylureas

A

Hypoglycaemia

Rashes

Nausea

Vomiting

Stomach Pain

Indigestion

Weight Gain

332
Q

Describe important pharmacodynamic/pharmacokinetic features of Sulphonylureas

A

Renally excreted so accumulates in renal failure

Gliclazide is short-acting (12 hours)

Glimepiride is long-acting

333
Q

Describe important pieces of patient information that should be given with Sulphonylureas

A

Compliance is important

Maintain constant diet

Avoid alcohol

334
Q

To which class of drug does Metformin belong?

A

Biguanides

335
Q

Describe the MOA of Metformin

A

Increases the activity of AMP-Dependent Protein Kinase (AMPK)

This inhibits gluconeogenesis and reduces insulin resistance

336
Q

State indications for Metformin

A

Type 2 Diabetes Mellitus

Metabolic/Reproductive Abnormalities Associated with Polycystic Ovarian Syndrome

337
Q

State side effects of Metformin

A

Diarrhoea

Nausea

Vomiting

Taste Disturbance

Lack of Appetite

Risk of LActic Acidosis in Patients with Renal Failure

338
Q

Describe important pharmacodynamic/pharmacokinetic features of Metformin

A

Not recommended in pregnancy

Not recommended in renal failure if eGFR<30

Absorption reduces when taken with food

339
Q

Describe important pieces of patient information that should be given with Metformin

A

Take them at the same time everyday

Avoid alcohol

Does not increase weight

340
Q

Give examples of GLP-1 Agonists

A

Exanatide

Liraglutide

(Glucagon Like Peptide)

341
Q

Describe the MOA of GLP-1 Agonists

A

GLP-1 is a hormone that is released after meals to increase insulin secretion

Therefore GLP-1 agonists increase insulin secretion while decreasing glucagon secretion and reducing hunger

342
Q

State indications for GLP-1 Agonists

A

Type 2 Diabetes Mellitus + Excess Weight

343
Q

State side effects of GLP-1 Agonists

A

Hypoglycaemia

Nausea

Vomiting

Diarrhoea

344
Q

Describe important pharmacodynamic/pharmacokinetic features of GLP-1 Agonists

A

It can lower glucose alone, but when given in conjunction with metformin, sulphonylureas and/or insulin it can improve glucose control

Renally excreted so dos adjustment needed in renal failure

345
Q

Describe important pieces of patient information that should be given with GLP-1 Agonists

A

Only given as injections

Twice a day

346
Q

To which class of drug does Levothyroxine belong?

A

Synthetic Thyroid Hormone

347
Q

Describe the MOA of Levothyroxine

A

Thyroxine increases the metabolic rate of all tissues in the body

Synthetically prepared levo-isomer of thyroxine

Acts like T4 and gets converted to T3 in the liver and kidney

Maintains brain function, food metabolism and body temperature among other effects

348
Q

State indications for Levothyroxine

A

Hypothyroidism

Chronic Lymphocytic Thyroiditis

349
Q

State side effects of Levothyroxine

A

Chest Pain

Coma

Diarrhoea

Tachycardia

Itching

Muscle Cramps

(If dosing is correct, side effects are unusual)

350
Q

Describe important pharmacodynamic/pharmacokinetic features of Levothyroxine

A

Primarily eliminated by the kidneys

IV formulations available

Long half-life (6-7 days) so thyroid function should be rechecked 6 weeks after a dose adjustment

351
Q

Describe important pieces of patient information that should be given with Levothyroxine

A

Take 30-60 minutes before breakfast

352
Q

Give examples of Anti-Thyroid Thionamides

A

Carbimazole

Propylthiouracil

353
Q

Describe the MOA of Anti-Thyroid Thionamides

A

Reduces activity of peroxidase enzyme (required for the production of thyroid hormones)

May also reduce peripheral conversion of T4 to T3

Carbimazole is a pro-drug

354
Q

State indications for Anti-Thyroid Thionamides

A

Hyperthyroidism

Thyrotoxicosis

Preparing Patients for Thyroid Surgery

355
Q

State side effects of Anti-Thyroid Thionamides

A

Rash

Agranulocytosis

Sore Throat

356
Q

Describe important pharmacodynamic/pharmacokinetic features of Anti-Thyroid Thionamides

A

Carbimazole is rapidly metabolised to thiamazole, meaning peak plasma concentration occurs after one hour

It crosses the placenta and can be found in breast milk

The effect of anti-thyroid drugs can take several weeks to occur so are usually prescribed alongside a beta blocker to reduce symptoms of hyperthyroidism

357
Q

Describe important pieces of patient information that should be given with Anti-Thyroid Thionamides

A

Compliance is important

Regular blood checks will be needed to monitor treatment response and renal and hepatic function and full blood counts

358
Q

Give examples of Bisphosphonates

A

Alendronate (Alendronic Acid)

Ibandronate

Risedronate

Zalendronate (Zalendronic Acid)

359
Q

Describe the MOA of Bisphosphonates

A

Inhibits osteoclast bone resorption

No effect on bone formation

Little effect on bone density but large effect on fracture risk

360
Q

State indications for Bisphosphonates

A

Osteoporosis

Paget’s Disease of the Bone

361
Q

State side effects of Bisphosphonates

A

Abdominal Pain

Dyspepsia

Acid Regurgitation

Dysphagia

Headache

Avascular Necrosis of the Jaw (Rare but important)

Atypical Femoral Fracture (Rare but important)

362
Q

Describe important pharmacodynamic/pharmacokinetic features of Bisphosphonates

A

Bioavailability reduces with breakfast (with coffee or orange juice)

363
Q

Describe important pieces of patient information that should be given with Bisphosphonates

A

Avoid caffeine

Administer 30 minutes before or after food or drink and remain upright for at least 30 minutes afterwards

Most are given once weekly, some can be given daily and some by 6-monthly IV infusion

364
Q

Give examples of the Oral Contraceptive Pill (OCP)

A

Microgynon (Combined)

Cerazette (Progestogen Only)

365
Q

Describe the MOA of the OCP

A

A progestin (synthetic form of progesterone) along with an oestrogen (combined oral contraceptive pill) or a progestin alone (progestogen only pill)

Acts on female reproductive tract, the mammary glands, hypothalamus and the pituitary gland

Reduces the production of Gonadotrophin Releasing Hormone (GnRH)

Blunts the LH surge that stimulates ovulation

366
Q

State indications for the OCP

A

Contraception

Menopausal and Postmenopausal Disorders

Polycyctsic Ovarian Syndrome

367
Q

State side effects of the OCP

A

Mood Swings

Headache

Breast Tenderness

Increased Risk of Breast and Ovarian Cancer

Increased Risk of Venous Thromboembolic Disease

368
Q

Describe important pharmacodynamic/pharmacokinetic features of the OCP

A

Antibiotics and some enzyme inducers (e.g. St John’s Wort) can reduce efficacy

369
Q

Describe important pieces of patient information that should be given with the OCP

A

Take at the same time everyday - compliance is critical for efficacy

Take with food

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

370
Q

State the class of drug to which Codeine belongs

A

Opiate

371
Q

Describe the MOA of Codeine

A

Opioid receptor agonist; acts on mu, kappa and delta receptors on presynaptic neurons

This gives numerous effects that increase nociceptive thresholds throughout the central and peripheral nervous system

372
Q

State indications for Codeine

A

Mild to Moderate Pain

Persistent Dry Cough

Diarrhoea

373
Q

State side effects of Codeine

A

Nausea

Vomiting

Constipation

Biliary Spasm

Headache on Withdrawal

374
Q

Describe important pharmacodynamic/pharmacokinetic features of Codeine

A

Metabolised to morphine which is responsible for analgesic effects

Predominantly metabolised by the liver

Active metabolites are excreted in the urine so can accumulate in renal failure

10% of population resistant to codeine’s analgesic properties as they lack the demethylating enzyme that converts it to morphine

375
Q

Describe important pieces of patient information that should be given with Codeine

A

Can be taken with paracetamol for greater analgesic effect

Constipation is a likely side effect

376
Q

State the class of drug to which Morphine belongs

A

Opiate

377
Q

Describe the MOA of Morphine

A

Opioid receptor agonist; acts on mu, kappa and delta on presynaptic neurones

This gives numerous effects that increase nociceptive thresholds throughout the central and peripheral nervous system

378
Q

State indications for Morphine

A

Acute Severe Pain (incl. in setting of MI)

Acute Pulmonary Oedema

Chronic Pain

379
Q

State side effects of Morphine

A

Nausea

Vomiting

Abdominal Pain

Constipation

Respiratory Depression

Sedation

380
Q

Describe important pharmacodynamic/pharmacokinetic features of Morphine

A

Predominantly metabolised by the liver

Metabolites are active and can accumulate in renal failure

Accumulation can result in respiratory and central nervous system depression

381
Q

Describe important pieces of patient information that should be given with Morphine

A

Often given with an anti-emetic to reduce nausea/vomiting

382
Q

State the class of drug to which Oxycodone belongs

A

Opiate

383
Q

Describe the MOA of Oxycodone

A

Opioid receptor agonist; acts on mu, kappa and delta on presynaptic neurones

This gives numerous effects that increase nociceptive thresholds throughout the central and peripheral nervous system

384
Q

State indications for Oxycodone

A

Moderate to Severe Pain Relief in Cancer Patients

Post-Operative Pain

Severe Pain

385
Q

State side effects of Oxycodone

A

Nausea

Vomiting

Abdominal Pain

Constipation

386
Q

Describe important pharmacodynamic/pharmacokinetic features of Oxycodone

A

Available as long and short-acting preparations

Predominantly metabolised by the liver

Often administered via slow IV/SubCut infusion

387
Q

Describe important pieces of patient information that should be given with Oxycodone

A

Nausea and constipation are common side effects

388
Q

Give two examples of Non-Selective NSAIDs

A

Ibuprofen

Diclofenac

389
Q

Describe the MOA of Non-Selective NSAIDs

A

Non-selective inhibition of COX 1 and 2 enzymes, thereby decreasing the key inflammatory mediator prostaglandin from being synthesised

Thereby reduces pain, inflammation and swelling

390
Q

State indications for Non-Selective NSAIDs

A

Mild to Moderate Pain Relief

Rheumatic Disorders (e.g. RA or OA)

Fever (Anti-Pyretic Effect)

391
Q

State side effects of Non-Selective NSAIDs

A

Gastric and Duodenal Ulceration (risk increases with duration of therapy and dosage)

Nausea

Diarrhoea

Small increased risk of thrombotic events when used short-term, particularly diclofenac and high dose ibuprofen

Renal Impairment

Hyperkalaemia

Avoid in pregnancy, particularly the 3rd trimester (risk of closure of foetal ductus arteriosus in utero and pulmonary hypertension in newborn)

392
Q

Describe important pharmacodynamic/pharmacokinetic features of Non-Selective NSAIDs

A

Pain relief starts soon after the first dose, full analgesic effects can take up to one week and anti-inflammatory effects can take up to three weeks

Avoid in patients with renal impairment – use lowest dose, for shortest time if unavoidable

Caution should be used in the elderly – risk of gastrointenstinal bleeds.

393
Q

Describe important pieces of patient information that should be given with Non-Selective NSAIDs

A

Risk of stomach bleeds if on long-term use

Take with food or milk, to reduce abdominal discomfort and to reduce the risk of bleeding

Take only when required

In elderly patients a proton pump inhibitor is usually given alongside NSAID drugs

394
Q

Give an example of a Selective NSAID

A

Celecoxib

395
Q

Describe the MOA of Celecoxib

A

Selective inhibitor of COX-2, decreasing key inflammatory mediator prostaglandin from being synthesised

Thereby reduces pain, inflammation and swelling

(The gastrointestinal side effects are mediated via COX-1 inhibition)

396
Q

State indications for Celecoxib

A

Pain and Inflammation in: OA, RA, Ankylosing Spondylitis

397
Q

State side effects of Celecoxib

A

Gastric and Duodenal Ulceration (risk increases with duration of therapy and dosage)

Nausea

Diarrhoea

Renal Impairment

Hyperkalaemia

398
Q

Describe important pharmacodynamic/pharmacokinetic features of Celecoxib

A

Less incidence of serious gastrointestnal bleeds/ulceration compared to non-selective NSAIDs

Presumed higher risk of cardiovascular events, compared to non-selective NSAIDs

Avoid in patients with renal impairment – use lowest dose, for shortest time if unavoidable

Caution should be used in the elderly – risk of GI bleeds

Avoid in pregnancy particularly 3rd trimester (risk of closure of fetal ductus arteriosus in utero and pulmonary hypertension in newborn)

399
Q

Describe important pieces of patient information that should be given with Celecoxib

A

Risk of stomach bleeds if on long-term use

Take with food or milk to reduce abdominal discomfort and to reduce the risk of bleeding

Take only when required

400
Q

Describe the MOA of Paracetamol

A

A weak cyclooxygenase enzyme (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

401
Q

State indications for Paracetamol

A

Mild to Moderate Pain Relief

Fever

402
Q

State side effects of Paracetamol

A

Rash/Blood Disorders (Rare)

403
Q

Describe important pharmacodynamic/pharmacokinetic features of Paracetamol

A

Overdose must be avoided – severe liver damage can occur and can be fatal

Careful dosing in younger patients and patients with low body weight (reduce dose to 500mg 4-6 hourly, QID in patients <50kg)

404
Q

Describe important pieces of patient information that should be given with Paracetamol

A

Take only the prescribed amount and be wary of other over-the-counter medications that may contain paracetamol

405
Q

State the class of drug to which Allopurinol belongs

A

Xanthine Oxidase Inhibitors

406
Q

Describe the MOA of Allopurinol

A

Reduces synthesis of uric acid by competitively inhibiting xanthine oxidase

Reduces serum uric acid level

407
Q

State indications for Allopurinol

A

Prophylaxis of Gout

Prophylaxis of Calcium Oxalate Renal Stones

Hyperuricaemia Associated with Cancer Chemotherapy

408
Q

State side effects of Allopurinol

A

Rash

Hypersensitivity

GI Disturbance

Neutropenia (Rare)

409
Q

Describe important pharmacodynamic/pharmacokinetic features of Allopurinol

A

Not used to treat acute attack of gout, can exacerbate the inflammation, so should not be started during acute episodes

Cytochrome P450 enzyme inhibitor

Azathioprine metabolism affected

410
Q

Describe important pieces of patient information that should be given with Allopurinol

A

Rash and abdominal disturbances are relatively common

Rash should be reported to a doctor

Keep taking allopurinol, even when there is no sign of gout

In order to prevent an exacerbation of gout, an NSAID or cochicine is often prescribed for the first 3 months of therapy

Phase 3 (14 decks)

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