50 Drugs Flashcards
State the class of drugs to which Aspirin belongs
Anti-Platelet
Describe the MOA of Aspirin
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
State indications for Aspirin
Secondary prevention of thrombotic events Pain relief
State side effects of Aspirin
Bleeding Peptic Ulcer Disease Angiooedema Bronchospasm Reye’s Syndrome
Describe important pharmacokinetic features of Aspirin
Half life increases with very large doses (therefore pharmacokinetics may be non-linear in overdose)
State some important pieces of patient information that should be given alongside Aspirin
May be advisable to take PPI with long term aspirin Avoid OTC preparations containing aspirin Not to be take by children under 16
State the class of drugs to which Clopidogrel belongs
Anti-Platelet
Describe the MOA of Clopidogrel
Irreversibly blocks the ADP receptor on platelet cell membranes Therefore prevents formation of the GPIIb/IIIa complex, required for platelet aggregation Decreased thrombus formation
State indications for Clopidogrel
Secondary prevention of thrombotic events
State side effects of Clopidogrel
Abdominal Pain Diarrhoea Bleeding
Describe important pharmacokinetic/pharmacodynamic features of Clopidogrel
Should be avoided in patients with liver failure
State some important pieces of patient information that should be given alongside Clopidogrel
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
Give examples of Recombinant Tissue Plasminogen Activators
Tenecteplase Alteplase
Describe the MOA of Recombinant Tissue Plasminogen Activators
Catalyses conversion of plasminogen to plasmin to promote fibrin clot lysis
State indications for the use of Recombinant Tissue Plasminogen Activators
Acute Ischaemic Stroke (within 4.5 hours) Myocardial Infarction (within 12 hours) Massive Pulmonary Embolism
State side effects of Recombinant Tissue Plasminogen Activators
Bleeding Allergy Angiooedema
Describe important pharmacokinetic/pharmacodynamic features of Recombinant Tissue Plasminogen Activators
Alteplase is given as a bolus-infusion regimen Tenecteplase is given as a single bolus Interacts with other blood thinners (anticoagulants/antiplatelets)
State some important pieces of patient information that should be given alongside Recombinant Tissue Plasminogen Activators
Patient should be made aware of the risk benefit ratio which should include reference to bleeding complications
Describe the MOA of Unfractioned Heparin
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
State the indications for Unfractioned Heparin
Treatment and Prophylaxis of Thromboembolic Disease
Renal Dialysis (Haemodialysis)
Treatment of Acute Coronary Syndrome
State the side effects of Unfractioned Heparin
Bleeding
Heparin-Induced Thrombocytopaenia
Osteoporosis
State important pharmacokinetic/pharmacodynamic features of Unfractioned Heparin
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)
State some important pieces of patient information that should be given with Unfractioned Heparin
Risk of bleeding
Requires regular blood monitoring
Describe the MOA of LMW Heparin
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
State the indications for LMW Heparin
Treatment and Prophylaxis of Thromboembolic Disease
Renal Dialysis (Haemodialysis)
Treatment of Acute Coronary Syndrome
State the side effects of LMW Heparin
Bleeding
Heparin-Induced Thrombocytopaenia
Osteoporosis
Describe important pharmacokinetic/pharmacodynamic features of LMW Heparin
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
State some important pieces of patient information that should be given with LMW Heparin
Risk of Bleeding
Requires Injection
May need regular monitoring in prolonged therapy (FBC to check for thrombocytopaenia)
To which class of drugs does Warfarin belong?
Vitamin K Antagonists
Describe the MOA of Warfarin
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
State indications for Warfarin
Treatment of Venous Thromboembolism
Thromboprophylaxis in AF/Metallic Heart Valves/Cardiomyopathy
State side effects of Warfarin
Bleeding (risk increases with increasing INR)
Warfarin Necrosis
Osteoporosis
Describe important pharmacokinetic/pharmacodynamic features of Warfarin
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
State some important pieces of patient information that should be given with Warfarin
Need for compliance and attendance for monitoring
Care needed with alcohol
Must inform doctor before starting new drugs
Should avoid OTC preparations including aspirin
To which class of drugs does Dabigatran belong?
Direct Thrombin Inhibitors
Describe the MOA of Dabigatran
Direct thrombin inhibitor that prevents conversion of fibrinogen to fibrin
Thus prevents thrombus formation
State indications for Dabigatran
Prophylaxis of Venous Thromboembolism (especially post-operative)
Thromboprophylaxis in Non-Valvular AF
State side effects of Dabigatran
Bleeding
Dyspepsia
Describe important pharmacodynamic/pharmacokinetic features of Dabigatran
Rapid onset of action
No food and few drug interactions
Not metabolised by CYP450
No need for therapeutic monitoring
No available antidote
State some important pieces of patient information that should be given with Dabigatran
Risk of bleeding
To which class of drugs does Rivaroxaban belong?
Factor Xa Inhibitors
Describe the MOA of Rivaroxaban
Inhibits conversion of prothrombin to thrombin, thereby reducing thrombin concentrations in the blood
This inhibits formation of fibrin clots
State indications for Rivaroxaban
Prophylaxis of Venous Thromboembolism (especially post-operatively)
Thromboprophylaxis in Non-Valvular AF
Treatment fo Venous Thromboembolism
State side effects of Rivaroxaban
Nausea
Bleeding
Describe important pharmacodynamic/pharmacokinetic features of Rivaroxaban
Predictable drug interactions (metabolised by CYP450 and CYP3A4)
No need for therapeutic monitoring
Currently no available antidote
Describe important pieces of patient information that should be given with Rivaroxaban
Risk of bleeding
To which class of drugs does Apixaban belong?
Factor Xa Antagonists
Describe the MOA of Apixaban
Inhibits conversion of prothrombin to thrombin, thereby reducing concentration of thrombin in the blood
This inhibits formation of fibrin clots
State indications for Apixaban
Prophylaxis of Venous Thromboembolism Following Hip or Knee Replacement Surgery
Thromboprophylaxis in Non-Valvular AF
State side effects of Apixaban
Nausea
Bleeding
Describe important pharmacodynamic/pharmacokinetic features of Apixaban
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
Describe important pieces of patient information that should be given with Apixaban
Risk of bleeding
Give examples of drugs in the class of ‘Cardioselective Beta Blockers’
Atenolol
Bisoprolol
Describe the MOA of Cardioselective Beta Blockers
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
State indications for the use of Cardioselective Beta Blockers such as Atenolol and Bisoprolol
Hypertension
Angina
Rate Control in AF
(Bisoprolol may be used as supportive therapy in mild-moderate Heart Failure)
State side effects of Cardioselective Beta Blockers such as Atenolol and Bisoprolol
Bradycardia
Hypotension
Bronchospasm
Fatigue
Cold Extremities
Sleep Disturbance
Loss of Hypoglycaemic Awareness
Describe important pharmacodynamic/pharmacokinetic features of Cardioselective Beta Blockers such as Atenolol and Bisoprolol
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
Describe important pieces of patient information that should be given with Cardioselective Beta Blockers such as Atenolol and Bisoprolol
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
Give examples of Non-Cardioselective Beta Blockers
Propranolol
Carvedilol
Describe the MOA of Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol
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
State indications for Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol
Hypertension
Anxiety
Angina
Migraine Prophylaxis
Post-MI Prophylaxis
(Carvedilol may be used as supportive therapy for mild-moderate heart failure)
State side effects of Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol
Bradycardia
Hypotension
Bronchospasm
Fatigue
Cold Extremities
Sleep Disturbances
Loss of Hypoglycaemic Awareness
Describe important pharmacodynamic/pharmacokinetic features of Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol
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
Describe important pieces of patient information that should be given with Non-Cardioselective Beta Blockers such as Propranolol and Carvedilol
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
Give examples of ACE Inhibitors
Ramipril
Enalapril
Lisinopril
Perindopril
Describe the MOA of ACE Inhibitors
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
State indications of ACE Inhibitors
Hypertension
Heart Failure
Nephropathy
Prevention of CV Events in High Risk Patients
State side effects of ACE Inhibitors
Dry Cough
Hypotension
Hyperkalaemia
Renal Impairment
Angiodema
Describe important pharmacodynamic/pharmacokinetic features of ACE Inhibitors
Adverse drug reactions are higher in patients with:
High Dose Diuretics
Hypovolaemia
Hyponatraemia
Hypotension
Unstable Heart Failure
Renovascular Disease
Describe important pieces of information that should be given with ACE Inhibitors
Blood test require at 1-2 weeks to check electrolyte balance
Dry cough is a common (10%) side effect
Give examples of Nitrates
Isosorbide Mononitrate
Glyceryl Trinitrate (GTN)
Describe the MOA of Nitrates
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
State indications for Nitrates
Treatment of Angina
Severe HTN (IV GTN may be used)
State side effects of Nitrates
Headaches
Postural Hypotension
Dizziness
Tachycardia
Describe important pharmacodynamic/pharmacokinetic features of Nitrates
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
Describe important pieces of patient information that should be given with Nitrates
Headache is a common initial side effect but incidence decreases with long term use
GTN should be taken before activity that brings on angina
Give two examples of Rate Limiting Calcium Channel Blockers
Verapamil
Diltiazem
Describe the MOA of Rate Limiting Calcium Channel Blockers
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
State indications for Rate Limiting Calcium Channel Blockers
Supraventricular Arrhythmias
Angina
Hypertension
State side effects of Rate Limiting Calcium Channel Blockers
Verapamil - Constipation, Flushing, Headache, Dizziness, Hypotension
Diltiazem - GI Disturbances, Bradycardia, Peripheral Oedema, Dizziness, Headache, Hypotension
Describe important pharmacodynamic/pharmacokinetic features of Rate Limiting Calcium Channel Blockers
Contra-indicated in heart failure and LV dysfunction due to potent negative inotropy
Avoid in bradycardia and hypotension
Do not use with beta-blockers
Describe important pieces of patient information that should be given with Rate Limiting Calcium Channel Blockers
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
Give examples of Non-Rate Limiting Calcium Channel Blockers
Amlodipine
Nifedipine
Felodipine
Describe the MOA of Non-Rate Limiting Calcium Channel Blockers
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)
State indications for Non-Rate Limiting Calcium Channel Blockers
Hypertension
Angina
State side effects of Non-Rate Limiting Calcium Channel Blockers
Ankle Oedema
Nausea
Abdominal Pain
Palpitations
Headaches
Dizziness
Flushing
Describe important pharmacodynamic/pharmacokinetic features of Non-Rate Limiting Calcium Channel Blockers
Avoid in:
Cardiogenic Shock, Unstable Angina, Significant Aortic Stenosis
Describe important pieces of patient information that should be given with Non-Rate Limiting Calcium Channel Blockers
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
Give examples of HMG CoA-Reductase Inhibitors
Atorvastatin
Simvastatin
Pravastatin
Describe the MOA of HMG CoA-Reductase Inhibitors
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
State indications for HMG CoA-Reductase Inhibitors
Familial Hypercholesterolaemia
Prevention of CV Events in High-Risk Patients
State side effects of HMG CoA-Reductase Inhibitors
Myalgia
Myopathy and Rhabdomyolysis
GI Disturbances
LFT Derangement
Describe important pharmacodynamic/pharmacokinetic features of HMG CoA-Reductase Inhibitors
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
Describe important pieces of patient information that should be given with HMG CoA-Reductase Inhibitors
Report any unexplained muscle pains to their GP, who will check a creatine kinase blood level
Diarrhoea and abdominal pain may be present initially
To which class of drug does Digoxin belong?
Cardiac Glycosides
Describe the MOA of Digoxin
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
State indications for Digoxin
Heart Failure
Rate Control in AF
Describe side effects of Digoxin
Nausea
Vomiting
Diarrhoea
Confusion
Describe important pharmacodynamic/pharmacokinetic features of Digoxin
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
Describe important pieces of patient information that should be given with Digoxin
Risk of Toxicity
State the class of drug to which Amiodarone belongs
Anti-Arrhythmics
Describe the MOA of Amiodarone
Amiodarone blocks cardiac K+ channels, prolonging repolarization of the cardiac action potential to restore regular sinus rhythm
It also slows atrioventricular nodal conduction
State indications for Amiodarone
Supraventricular/Ventricular Arrhythmias
State side effects of Amiodarone
Photosensitivity Skin Reactions
Hypersensitivity Reactions
Hyper/Hypothyroidism
Pulmonary Fibrosis
Corneal Deposits
Neurological Disturbances
GI Disturbances/Hepatitis
Describe important pharmacodynamic/pharmacokinetic features of Amiodarone
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
Describe important pieces of patient information that should be given with Amiodarone
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)
Give examples of drugs in the Penicillins class
Flucloxacillin
Amoxicillin
Benzylpenicillin
Penicillin V
Describe the MOA of Penicillins
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
State indications for Penicillins
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
State side effects of Penicillins
Diarrhoea
Vomiting
Impaired Liver Function
Hypersensitivity Reaction
Describe important pharmacodynamic/pharmacokinetic features of Penicillins
Good Oral Absorption
Flucloxacillin: Beta-Lactamase Stable/Insensitive
Amoxicillin: Beta-Lactamase Susceptible (often combined with Claculinic Acid, a beta-lactamase inhibitor)
Describe important pieces of patient information that should be given with Penicillins
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.
Give two example of Cephalosporin antibiotics
Ceftriaxone
Cephalexin
Describe the MOA of Cephalosporins
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
State indications for Cephalosporins
Serious Infection: Septicaemia, Pneumonia, Meningitis
State side effects of Cephalosporins
Hypersensitivity Reactions
Antibiotics Associated C. Diff
Impaired Liver Function
Describe important pharmacodynamic/pharmacokinetic features of Cephalosporins
Renal Excretion
Longer Half-Life, Needs to be given once daily
Describe important pieces of patient information that should be given with Cephalosporins
Diarrhoea is a common side effect
Report any incidence of a rash after use – risk of hypersensitivity reactions
To which class of drug does Vancomycin belong?
Glycopeptide Antibiotic
Describe the MOA of Vancomycin
Bactericidal, inhibiting cell-wall synthesis in Gram +ve bacteria
State indications for Vancomycin
Severe Gram +ve Infections
MRSA
Severe C. Diff
State side effects of Vancomycin
Fever
Rash
Local Phlebitis at Injection Site
Nephrotoxicity
Ototoxicity
Blood Disorders, inc. Neutropenia
Anaphylactoid Reaction (Red Many Syndrome is Infusion Rate Too Fast)
Describe important pharmacodynamic/pharmacokinetic features of Vancomycin
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
Describe important pieces of patient information that should be given with Vancomycin
Risk of kidney damage
Patients should report any changes in hearing
Regular blood tests required for monitoring
State the class of drug to which Gentamicin belongs
Aminoglycosides
Describe the MOA of Gentamicin
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)
State indications for Gentamicin
Severe Gram -ve Infection (e.g. Biliary Tract Infection, Pyelonephritis, Hospital Acquired Pneumonia)
Some Gram +ve Infections (e.g. Soft Tissue Infection and Endocarditis)
State side effects of Gentamicin
Nephrotoxicity
Ototoxicity
Describe important pharmacodynamic/pharmacokinetic features of Gentamicin
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
Describe important pieces of patient information that should be given with Gentamicin
Ask patients to report any change to their hearing
Risk of kidney damage so monitoring of drug levels and renal function tests are required
State the class of drug to which Ciprofloxacin belongs
Quinolone
Describe the MOA of Ciprofloxacin
Interferes with bacterial DNA replication and repair
Broad spectrum bactericidal antibiotic, provides both Gram +ve and -ve cover
State indications for Ciprofloxacin
Gram -ve Bacterial Infection
Respiratory Tract Infection
Upper UTI
Peritoneal Infection
Gonorrhoea
Prostatitis
State side effects of Ciprofloxacin
GI Toxicity
QT Segment Prolongation
C. Diff Infection
Tendonitis
Describe important pieces of patient information that should be given with Ciprofloxacin
Risk of diarrhoea after use
Give two examples of Macrolide antibiotics
Clarithromycin
Erythromycin
Describe the MOA of Macrolide antibiotics
Binds to 50s ribosomal subunit
Inhibits bacterial protein synthesis
State indications for Macrolide antibiotics
Atypical Organisms Causing Pneumonia
Severe CAP
Severe Campylobacter Infection
Mild-Moderate Skin and Soft Tissue Infection
Otitis Media
Lyme Disease
H.Pylori Eradication Therapy
State side effects of Macrolide antibiotics
Diarrhoea
Vomiting
QT Segment Prolongation
Ototoxicity
Describe important pharmacodynamic/pharmacokinetic features of Macrolide antibiotics
Uses hepatic enzyme Cytochrome P450 pathway
Can interact with all drugs using this pathway, especially Simvastatin, Atorvastatin and Warfarin
Describe important pieces of patient information that should be given with Macrolide antibiotics
Risk of Diarrhoea
Senses of smell and taste may be disturbed during therapy
Tooth and tongue discolouration may occur during therapy
State the class of drug to which Trimethoprim belongs
Inhibitor of Folate Synthesis
Describe the MOA of Trimethoprim
Inhibits folate metabolism pathway and leads to impaired nucleotide synthesis
Therefore interferes with bacterial DNA replication
State indications for Trimethoprim
1st Line Antibiotic in Uncomplicated UTI
Acute/Chronic Bronchitis
Pneumocystis Pneumonia
Good Range of Gram +ve and -ve Cover
Some MRSA Cover
State side effects of Trimethoprim
Elevated Serum Creatinine
Hyperkalaemia
Depressed Haematopoiesis
Rash
GI Disturbance
Describe important pharmacodynamic/pharmacokinetic features of Trimethoprim
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
Describe important pieces of patient information that should be given with Trimethoprim
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
State the class of drug to which Aciclovir belongs
Anti-Virals
Describe the MOA of Aciclovir
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
State indications for Aciclovir
Herpes SImplex Infection
Varicella Zoster Infection
State side effects of Aciclovir
Nausea
Vomiting
Local Inflammation at Infusion Site (IV Only)
Describe important pharmacodynamic/pharmacokinetic features of Aciclovir
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
Describe important pieces of patient information that should be given Aciclovir
Multiple/repeat doses may be required in immunosuppressed patients
Type of infection or recurrent infections may prompt HIV infection
State the class of drug to which Salbutamol belongs
Beta-Adrenergic Bronchodilators
(Short-Acting)
Describe the MOA of Salbutamol
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
State indications for Salbutamol
Asthma
COPD
State side effects of Salbutamol
Tremor
Tachycardia
Cardiac Dysrhythmia
Headache
Sleep Disturbance
Describe important pharmacodynamic/pharmacokinetic features of Salbutamol
Only a small percentage of inhaled drug reaches target in the airways (a spacer may improve delivery)
Describe important pieces of patient information that should be given with Salbutamol
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
State the class of drug to which Salmeterol belongs
Beta-Adrenergic Bronchodilators
(Long-Acting)
Describe the MOA of Salmeterol
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
State indications for Salmeterol
Asthma
COPD
State side effects of Salmeterol
Tremor
Tachycardia
Cardiac Dysrhythmia
Headache
Sleep Disturbance
Describe important pharmacodynamic/pharmacokinetic features of features of Salmeterol
Not to be commenced in patients with rapidly deteriorating asthma due to slower onset of action than SABAs
Describe important pieces of patient information that should be given with Salmeterol
Report any deterioration in symptoms following initiation of LABA
Do not exceed stated dose
Seek medical advice when stated dose fails to control symptoms
Give two examples of Anti-Muscarinic Bronchodilators
Tiotropium
Ipratropium Bromide
Describe the MOA of Anti-Muscarinic Bronchodilators
Muscarinic receptor (M3) antagonists producing bronchodilatory effects
Reduces mucus secretion and may increase bronchial mucus clearance by stimulating cilia
State indications for Anti-Muscarinic Bronchodilators
Asthma
COPD
Rhinitis
State side effects of Anti-Muscarinic Bronchodilators
Dry Mouth
Cough
Constipation
Describe important pharmacodynamic/pharmacokinetic features of Anti-Muscarinic Bronchodilators
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
Describe important pieces of patient information that should be given with Anti-Muscarinic Bronchodilators
Good inhaler technique improves efficacy
Cough may arise
State the class of drug to which Beclomethasone belongs
Inhaled Corticosteroids
Describe the MOA of Beclomethasone
Anti-inflammatory effect on the airways
Decreases formation of pro-inflammatory cytokines
Up-regulates Beta-2 Adrenoceptor in airways
State indications for Beclomethasone
Asthma
COPD
State side effects of Beclomethasone
Oral Candidiasis (Thrush)
Adrenal Suppression
Osteoporosis
Describe important pharmacodynamic/pharmacokinetic features of Beclomethasone
Takes several weeks to months for full effect of therapy
Spacer devices can reduce risk of thrush and improve drug delivery
Describe important pieces of patient information that should be given with Beclomethasone
If on higher doses, should carry a steroid card
Increase dose during periods of illness
Give example of Anti-Histamine (H1 Receptor Antagonist) drugs
Chlorpheniramine
Desloratidine
Fexofenadine
Hydroxyzine
Describe the MOA of Anti-Histamines
H1 Receptor Antagonists
Inhibit histamine-mediated contraction and vasodilation of the bronchial smooth muscle
State indications for Anti-Histamines
Anaphylaxis
Hay Fever
Urticaria
Sedation
State side effects of Anti-Histamines
Drowsiness
Tinnitus
Describe important pharmacodynamic/pharmacokinetic features of Anti-Histamines
Renally excreted
Sedation arises from CNS H1 antagonism (second generation H1 antagonists do not cross BBB in therapeutic doses)
Describe important pieces of patient information that should be given with Anti-Histamines
Do not operate heavy machinery
Do not drive
Describe the MOA of Levodopa
Pro-drug (dopamine precursor)
Crosses the BBB and is converted to dopamine
Striatal dopaminergic neurotransmission is increased
State the indications for Levodopa
Parkinson’s Disease
State side effects of Levodopa
Dyskinesia
Compulsive Disorders
Hallucinations
Nausea
GI Upset
Describe important pharmacodynamic/pharmacokinetic features of Levodopa
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
Describe important pieces of patient information that should be given with Levodopa
Dyskinesia is common
Reduced efficacy over time
Avoid abrupt withdrawal
Give examples of Dopamine Agonists
Apomorphine
Pramipexole
Bromocriptine
Pergolide
Rotigotine
Describe the MOA of Dopamine Agonists
Stimulate post-synaptic dopamine receptors
Apomorphine: Non-Selective D1 and D2 Dopamine subfamily of receptors
Pramipexole: Selective D3 Receptor
State indications for Dopamine Agonists
Parkinson’s Disease
State side effects of Dopamine Agonists
Apomorphine: Pain at Injection Site, Nausea and Vomiting
Pramipexole: Hallucinations, Nausea, Drowsiness, Involuntary Movements
Describe important pharmacodynamic/pharmacokinetic features of Dopamine Agonists
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)
Describe important pieces of patient information that should be given with Dopamine Agonists
Apomorphine can only be injected
Dopamine Agonists are weaker than L-Dopa so treatment may need to be modified in time
State the class of drug to which Entacapone belongs
Catechol-o-methyl Transferase (COMT) Inhibitor
Describe the MOA of Entacapone
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
State indications for Entacapone
Parkinson’s Disease
In conjuncion with L-Dopa and Dopamine Decarboxylase Inhibitors
State side effects of Entacapone
Dyskinesia
Nausea
Abdominal Pain
Vomiting
Dry Mouth
Dizziness
Describe important pharmacodynamic/pharmacokinetic features of Entacapone
Rapidly absorbed
L-Dopa dose may need to be reduced by 10-30% when given with Entacapone
Describe important pieces of patient information that should be given with Entacapone
Urine may turn brown, this is normal
Could become lightheaded/dizzy while doing daily activities
Avoid abrupt withdrawal
State the class of drug to which Carbamazepine belongs
Anti-Epileptic
Describe the MOA of Carbamazepine
Voltage-gated Na+ channel blocker on the pre-synaptic membrane
Blocks the Na+ influx, reduces neuronal excitability and decreases the action potential
State indications for Carbamazepine
Epilepsy
Trigeminal Neuralgia
Neuropathic Pain
State side effects of Carbamazepine
Dizziness
Dry Mouth
Ataxia
Fatigue
Headache
Diplopia
Blurred Vision
Hyponatraemia
Stevens-Johnson Syndrome (Rare)
Describe important pharmacodynamic/pharmacokinetic features of Carbamazepine
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
Describe important pieces of patient information that should be given with Carbamazepine
Avoid alcohol
Avoid grapefruit
State the class of drug to which Sodium Valproate belongs
Anti-Epileptic
Describe the MOA of Sodium Valproate
Weak sodium ion channel blocker
Inhibitor of GABA degrading enzymes
Increased GABA stops action potential
State indications for Sodium Valproate
Epilepsy
Bipolar Disorder
Depression
State side effects of Sodium Valproate
Nausea
Diarrhoea
Gastric Irritation
Weight Gain
Hyponatraemia
Behavioural Disturbance
Confusion
Stevens-Johnson Syndrome (Rare)
Describe important pharmacodynamic/pharmacokinetic features of Sodium Valproate
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
Describe important pieces of patient information that should be given with Sodium Valproate
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
State the class of drug to which Phenytoin belongs
Anti-Epileptics
Describe the MOA of Phenytoin
Acts as a voltage-gated Na+ channel blocker on the pre-synaptic neuronal membrane
Limits action potential transmission
Hence limits spread of seizure activity
State indications for Phenytoin
Epilepsy (incl. Status Epilepticus)
Trigeminal Neuralgia
State side effects of Phenytoin
Insomnia
Headache
Rash
Constipation
Vomiting
Gingival Hyperplasia
Liver Damage
Stevens-Johnson Syndrome
Leucopenia
Thrombocytopenia
Describe important pharmacodynamic/pharmacokinetic features of Phenytoin
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
Describe important pieces of patient information that should be given with Phenytoin
Avoid alcohol
Do not take calcium, aluminium, magnesium or iron supplements within 2 hours of ingestion
Take with food to reduce irritation
State the class of drug to which Lamotrigine belongs
Anti-Epileptic
Describe the MOA of Lamotrigine
Varied MOA
Inhibits voltage-gated Na+ channels and/or Ca2+ channels
Acts on pre-synaptic neuronal membrane
Reduces action potential and excitatory signals
State indications for Lamotrigine
Epilepsy (Focal and Generalised Seizures)
Depressive Disorders associated with Bipolar Disorder
State side effects of Lamotrigine
Nausea
Vomiting
Diarrhoea
Tremor
Insomnia
Blurred Vision
Aggression
Skin Reactions (incl. Stevens-Johnson Syndrome and Toxic Epidermal Necrolysis)
Describe important pharmacodynamic/pharmacokinetic features of Lamotrigine
Half-life doubles in chronic renal impairment so dose adjustment is required
Describe important pieces of patient information that should be given with Lamotrigine
Take without regard to meals
Seeks medical advice if any rash or signs/symptoms of hypersensitivity
State the class of drug to which Levetiracetam
Anti-Epileptic
Describe the MOA of Levetiracetam
SV2A is a synaptic vesicle protein required for neurotransmitter release
Levetiracetam blocks this and reduces neurotransmitter release
Induces an anti-epileptic effect
State indications for Levetiracetam
Epilepsy
State side effects of Levetiracetam
Headache
Fatigue
Anxiety
Irritability
Drowsiness
Constipation
Describe important pharmacodynamic/pharmacokinetic features of Levetiracetam
Rapidly and almost completely absorbed after oral administration (99%)
Food does not affect bioavailability
Cytochrome P450 is not involved in its metabolism
Describe important pieces of patient information that should be given with Levetiracetam
May affect ability to drive or operate machinery
Not recommended during pregnancy or breast feeding
Give examples of Selective Serotonin Reuptake Inhibitors (SSRIs)
Citalopram
Fluoxetine
Paroxetine
Escitalopram
Sertraline
Describe the MOA of SSRIs
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
State indications for SSRIs
Depression
Bulimia
Obsessive Compulsive Disorder
State side effects of SSRIs
Dry Mouth
Nausea
Insomnia
Anxiety
Decreased Libido
Seizures
Dyskinesia
Describe important pharmacodynamic/pharmacokinetic features of SSRIs
SSRIs bind with less affinity to histamine, acetylcholine and noradrenaline receptors than TCAs leading to fewer side effects
Less dangerous in overdose than TCAs
Describe important pieces of patient information that should be given with SSRIs
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)
Give examples of Tricyclic Antidepressants (TCAs)
Amitriptyline
Imipramine
Doxepin
Describe the MOA of TCAs
Stops the reuptake of monoamines
Binds to monoamine pump at pre-synaptic cleft
The reduced reuptake of noradrenaline and/or serotonin combats depression
State indications for TCAs
Depression
Panic Disorders
Neuropathic Pain
State side effects of TCAs
Sedation (anti-histaminergic effects)
Postural Hypotension, Tachycardia (anti-adrenergic effects)
Urinary Retention, Dry Mouth, Blurred Vision, Diplopia (anti-cholinergic effects)
Describe important pharmacodynamic/pharmacokinetic features of TCAs
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
Describe important pieces of patient information that should be given with TCAs
Reduction in depressive symptoms may take several weeks to appear
TCA overdose can be serious and cause seizures and cardiac arrythmias
Give examples of Anti-Psychotic drugs
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
Describe the MOA of Anti-Psychotics
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
State indications for Anti-Psychotics
Schizophrenia
Mania
Delusions
Hallucinations
Behavioural Problems
Anti-Emetic (Haloperidol)
State side effects of Anti-Psychotics
Sedation (anti-histaminergic effect)
Postural Hypotension, Tachycardia (anti-adrenergic effect)
Urinary Retention, Dry Mouth, Blurry Vision (anti-cholinergic effect)
Describe important pharmacodynamic/pharmacokinetic features of Anti-Psychotics
Has effects on numerous receptor symptoms within the CNS
Describe important pieces of patient information that should be given with Anti-Psychotics
Symptoms may not always disappear while on medication
Dosage may have to be increased if no improvement is made after a few weeks
Give examples of Benzodiazepines
Diazepam
Lorazepam
Midazolam
Describe the MOA of Benzodiazepines
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
State indications for Benzodiazepines
Anxiety
Epilepsy
Muscle Spasm
Alcohol Withdrawal
State side effects of Benzodiazepines
Sedation
Ataxia
Altered Mental State
Insomnia
Describe important pharmacodynamic/pharmacokinetic features of Benzodiazepines
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
Describe important pieces of patient information that should be given with Benzodiazepines
Monitor breathing and report if severe breathlessness or palpitations
Only prescribed for short terms due to risk of addiction
Give examples (three each) of oral, topical and parenteral glucocorticoids
Oral - Prednisolone, Hydrocortisone, Dexamethasone
Topical - Hydrocortisone, Betamethasone, Clobetasone
Parenteral - Methylprednisolone, Hydrocortisone, Triamcinolone
Describe the MOA of glucocorticoids
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
State indications for glucocorticoids
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
State side effects of glucocorticoids
Sleep Disturbance
Mood Disturbance/Psychosis
Hyperglycaemia
Immunodeficiency
Easy Bruising
Moon-Faced
Increased Abdominal Fat
Glaucoma
Striae
Hypertension
Gastric Irritation
Describe important pharmacodynamic/pharmacokinetic features of glucocorticoids
Variety of different preparations are available
Drugs have differing degrees of glucocorticoid and mineralocorticoid activity
Describe important pieces of patient information that should be given with glucocorticoids
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
State the relative glucocorticoid/mineralocorticoid activity of Prednisolone, Betamethasone, Hydrocortisone, Dexamethasone and Fludrocortisone
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
Give three examples of Anti-TNF Agents
Etanercept (Receptor Fusion Protein)
Infliximab (Monoclonal Antibody)
Adalimumab (Monoclonal Antibody)
Describe the MOA of Anti-TNF Agents
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
State indications for Anti-TNF Agents
Rheumatoid Arthritis
Psoriatic Arthritis
Ankylosing Spondylitis
Juvenile Arthritis
State side effects of Anti-TNF Agents
Injection Site Reactions
Flu-Like Symptoms (Fever, Headache, Runny Nose)
Immune Deficiency (Particular risk of Legionella and Listeria and reactivation of TB)
Describe important pharmacodynamic/pharmacokinetic features of Anti-TNF Agents
Given parenterally by subcutaneous injection
Describe important pieces of patient information that should be given with Anti-TNF Agents
Maintain good hygiene and report symptoms of infection early
Give examples of Immunosuppressant drugs
Methotrexate
Azathioprine
Mercaptopurine
Describe the MOA of immunosuppressants
Disrupt DNA synthesis
Azathioprine: Blocks purine synthesis mainly in lymphocytes
Methotrexate: Stops the action of the enzyme dihydrofolate needed for production of DNA
State indications for immunosuppressant drugs
Post Transplantation Immunosuppression
Inflammatory Bowel Disease
Renal Vasculitis
Paediatric Leukaemia (Methotrexate)
State side effects of immunosuppressant drugs
Bone Marrow Suppression (Leucopenia)
Risk of Infection
Nephrotoxicity
Hepatotoxicity
Seizures
GI Upset
Mucosal Ulceration
Alopecia
Describe important pharmacodynamic/pharmacokinetic features of immunosuppressant drugs
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
Describe important pieces of patient information that should be given with immunosuppressant drugs
Limit caffeine intake
Take without regard to meals
Give examples of Proton Pump Inhibitors
Omeprazole
Lansoprazole
Pantoprazole
Describe the MOA of PPIs
Bind to H/K ATPase pump on gastric parietal cells
Reduces HCl production and hence reduces gastric acidity
State indications for PPIs
Peptic Ulcers
Gastro-Oesophageal Reflux Disease
H. Pylori Infection
Prophylaxis in Patiens Receiving Long Term NSAIDs
State side effects of PPIs
Nausea
Vomiting
Insomnia
Vertigo
Headaches
Describe important pharmacodynamic/pharmacokinetic features of PPIs
Omeprazole is an inhibitor of cytochrome P450 enzymes
Describe important pieces of patient information that should be given with PPIs
Avoid alcohol
Take 30-60 minutes before food
Give examples of H2 receptor antagonists
Ranitidine
Cimetidine
Famotidine
Nizatidine
Describe the MOA of H2 receptor antagonists
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
State indications for H2 receptor antagonists
Peptic Ulcer
Gastro-Oesophagal Reflux Disease
Zollinger-Ellison Syndrome
State side effects of H2 receptor antagonists
Headache
Dizziness
Diarrhoea
Reduced B12 Absorption
Gynaecomastia
Describe important pharmacodynamic/pharmacokinetic features of H2 receptor antagonists
Cimetidine is an inhibitor of cytochrome P450 enzymes
Describe important pieces of patient information that should be given with H2 receptor antagonists
Avoid a high protein diet
Take without regard to meals
Give examples of Laxatives
Lactulose
Senna
Describe the MOA of Laxatives
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
State indications for Laxatives
Constipation
Pregnancy
Prophylaxis in Opiate Analgesic Use
State side effects of Laxatives
Dehydration
Salt Loss
Abdominal Cramps
Fatigue
Describe important pharmacodynamic/pharmacokinetic features of Laxatives
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
Describe important pieces of patient information that should be given with Laxatives
Take liberally without regard to meals
To which class of drug does Cyclizine belong?
Anti-Emetic
Describe the MOA of Cyclizine
H1 Histamine Receptor Antagonist
Acts on vomiting centre in the medullary region
Mild anti-cholinergic and anti-muscarinic effects
State indications for Cyclizine
Nausea and Vomiting
Motion Sickness
Vertigo and Dizziness
Prophylaxis alongisde chemotherapy and opiate analgesic use
State side effects of Cyclizine
Headache
Sedation
Diarrhoea
Describe important pharmacodynamic/pharmacokinetic features of Cyclizine
Can also be a central nervous system depressant
Describe important pieces of patient information that should be given with Cyclizine
Avoid alcohol
Food may reduce irritation
Take without regard to meals
To which class of drug does Metoclopramide belong?
Anti-Emetic
Describe the MOA of Metoclopramide
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
State indications for Metoclopramide
Nausea
Vomiting
To increase gastric emptying
State side effects of Metoclopramide
Dystonia (due to dopamine antagonism)
Confusion
Dizziness
Diarrhoea
Parkinsonism with long-term use
Describe important pharmacodynamic/pharmacokinetic features of Metoclopramide
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
Describe important pieces of patient information that should be given with Metoclopramide
Avoid alcohol
Take 30 minutes before food
To which class of drug does Prochlorperazine belong?
Anti-Emetic
Describe the MOA of Prochlorperazine
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)
State indications for Prochlorperazine
Nausea
Vomiting
Adjunct in some psychotic disorders
State side effects of Prochlorperazine
Dry mouth
Tachycardia
Restlessness
Drowsiness
Describe important pharmacodynamic/pharmacokinetic features of Prochlorperazine
Anti-cholinergic and alpha-adrenergic receptors antagonism occurs leading to sedation, muscle relaxation and hypotension
The dose differs substantially when given parenterally
Describe important pieces of patient information that should be given with Prochlorperazine
Avoid alcohol and caffeine
Take with food and a full glass of water
Give examples of Thiazide Diuretics
Bendroflumethiazide
Indapamide
Chlortalidone
Describe the MOA of Thiazide Diuretics
Inhibit Na/Cl transporter at the distal convoluted tubule and collecting duct
Increases Na/Cl and water excretion
State indications for Thiazide Diuretics
Hypertension
Oedema of Cardiac/Renal/Hepatic/Iatrogenic Origin
State side effects of Thiazide Diuretics
Hypokalaemia
Hypomagnesaemia
Hyponatraemia
Hypercalcaemia
Hyperuricaemia
Reduced Glucose Tolerance
Hypersensitivity Reactions - Rashes, Pneumonitis
Describe important pharmacodynamic/pharmacokinetic features of Thiazide Diuretics
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
Describe important pieces of patient information that should be given with Thiazide Diuretics
Urinary frequency usually not affected
Report if sudden rash
Make aware of risk of electrolyte imbalance
Give examples of Loop Diuretics
Furosemide
Bumetanide
Torasemide
Describe the MOA of Loop Diuretics
Na/Cl/K Symporter Antagonists
Act on the thick ascending loop of henle
Increase secretion of Na/K/Cl and water
State indications for Loop Diuretics
Hypertension
Hyperkalaemia
Heart Failure
Cirrhosis of the Liver (Fluid Retention)
Nephrotic Syndrome
State side effects of Loop Diuretics
Hypokalaemia
hypovolaemia
Hyperuricaemia
Metabolic Acidosis
Abdominal Pain
Ototoxicity
Describe important pharmacodynamic/pharmacokinetic features of Loop Diuretics
60% absorbed in patients with normal renal function
Renal and hepatic excretion - increased half-life for patients with renal or hepatic disease
Describe important pieces of patient information that should be given with Loop Diuretics
Avoid alcohol excess
Urinary frequency increases
Describe the different insulin preparations available
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
Describe the MOA of Insulin
Increases cellular uptake of glucose
Stimulates glycogenesis, encourages DNA synthesis and promotes release of growth hormone
State indications for Insulin
Type 1 Diabetes Mellitus
Type 2 Diabetes Mellitus
Hyperkalemia (in conjunction with Dextrose)
State side effects of Insulin
Hypoglycaemia
Sweats, Shakes, Tachycardia, Headache, Weakness, Fatigue (typically signs of hypoglycaemia)
Oedema
Injection Site Reactions
Describe important pharmacodynamic/pharmacokinetic features of Insulin
Patients are given varying types of insulin combinations based on their activities and preferences
Given subcutaneously and short-acting (actrapid) can be given IV
Describe important pieces of patient information that should be given with Insulin
Only in the form of an injection
Compliance is very important
Never skip a meal when on insulin
Give two examples of Sulphonylureas
Gliclazide
Glimepiride
Describe the MOA of Sulphonylureas
Stimulates beta cells of the pancreas to produce more insulin
Increase cellular glucose uptake and glycogenesis while reducing gluconeogenesis
State indications for Sulphonylureas
Type 2 Diabetes Mellitus
State side effects of Sulphonylureas
Hypoglycaemia
Rashes
Nausea
Vomiting
Stomach Pain
Indigestion
Weight Gain
Describe important pharmacodynamic/pharmacokinetic features of Sulphonylureas
Renally excreted so accumulates in renal failure
Gliclazide is short-acting (12 hours)
Glimepiride is long-acting
Describe important pieces of patient information that should be given with Sulphonylureas
Compliance is important
Maintain constant diet
Avoid alcohol
To which class of drug does Metformin belong?
Biguanides
Describe the MOA of Metformin
Increases the activity of AMP-Dependent Protein Kinase (AMPK)
This inhibits gluconeogenesis and reduces insulin resistance
State indications for Metformin
Type 2 Diabetes Mellitus
Metabolic/Reproductive Abnormalities Associated with Polycystic Ovarian Syndrome
State side effects of Metformin
Diarrhoea
Nausea
Vomiting
Taste Disturbance
Lack of Appetite
Risk of LActic Acidosis in Patients with Renal Failure
Describe important pharmacodynamic/pharmacokinetic features of Metformin
Not recommended in pregnancy
Not recommended in renal failure if eGFR<30
Absorption reduces when taken with food
Describe important pieces of patient information that should be given with Metformin
Take them at the same time everyday
Avoid alcohol
Does not increase weight
Give examples of GLP-1 Agonists
Exanatide
Liraglutide
(Glucagon Like Peptide)
Describe the MOA of GLP-1 Agonists
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
State indications for GLP-1 Agonists
Type 2 Diabetes Mellitus + Excess Weight
State side effects of GLP-1 Agonists
Hypoglycaemia
Nausea
Vomiting
Diarrhoea
Describe important pharmacodynamic/pharmacokinetic features of GLP-1 Agonists
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
Describe important pieces of patient information that should be given with GLP-1 Agonists
Only given as injections
Twice a day
To which class of drug does Levothyroxine belong?
Synthetic Thyroid Hormone
Describe the MOA of Levothyroxine
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
State indications for Levothyroxine
Hypothyroidism
Chronic Lymphocytic Thyroiditis
State side effects of Levothyroxine
Chest Pain
Coma
Diarrhoea
Tachycardia
Itching
Muscle Cramps
(If dosing is correct, side effects are unusual)
Describe important pharmacodynamic/pharmacokinetic features of Levothyroxine
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
Describe important pieces of patient information that should be given with Levothyroxine
Take 30-60 minutes before breakfast
Give examples of Anti-Thyroid Thionamides
Carbimazole
Propylthiouracil
Describe the MOA of Anti-Thyroid Thionamides
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
State indications for Anti-Thyroid Thionamides
Hyperthyroidism
Thyrotoxicosis
Preparing Patients for Thyroid Surgery
State side effects of Anti-Thyroid Thionamides
Rash
Agranulocytosis
Sore Throat
Describe important pharmacodynamic/pharmacokinetic features of Anti-Thyroid Thionamides
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
Describe important pieces of patient information that should be given with Anti-Thyroid Thionamides
Compliance is important
Regular blood checks will be needed to monitor treatment response and renal and hepatic function and full blood counts
Give examples of Bisphosphonates
Alendronate (Alendronic Acid)
Ibandronate
Risedronate
Zalendronate (Zalendronic Acid)
Describe the MOA of Bisphosphonates
Inhibits osteoclast bone resorption
No effect on bone formation
Little effect on bone density but large effect on fracture risk
State indications for Bisphosphonates
Osteoporosis
Paget’s Disease of the Bone
State side effects of Bisphosphonates
Abdominal Pain
Dyspepsia
Acid Regurgitation
Dysphagia
Headache
Avascular Necrosis of the Jaw (Rare but important)
Atypical Femoral Fracture (Rare but important)
Describe important pharmacodynamic/pharmacokinetic features of Bisphosphonates
Bioavailability reduces with breakfast (with coffee or orange juice)
Describe important pieces of patient information that should be given with Bisphosphonates
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
Give examples of the Oral Contraceptive Pill (OCP)
Microgynon (Combined)
Cerazette (Progestogen Only)
Describe the MOA of the OCP
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
State indications for the OCP
Contraception
Menopausal and Postmenopausal Disorders
Polycyctsic Ovarian Syndrome
State side effects of the OCP
Mood Swings
Headache
Breast Tenderness
Increased Risk of Breast and Ovarian Cancer
Increased Risk of Venous Thromboembolic Disease
Describe important pharmacodynamic/pharmacokinetic features of the OCP
Antibiotics and some enzyme inducers (e.g. St John’s Wort) can reduce efficacy
Describe important pieces of patient information that should be given with the OCP
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
State the class of drug to which Codeine belongs
Opiate
Describe the MOA of Codeine
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
State indications for Codeine
Mild to Moderate Pain
Persistent Dry Cough
Diarrhoea
State side effects of Codeine
Nausea
Vomiting
Constipation
Biliary Spasm
Headache on Withdrawal
Describe important pharmacodynamic/pharmacokinetic features of Codeine
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
Describe important pieces of patient information that should be given with Codeine
Can be taken with paracetamol for greater analgesic effect
Constipation is a likely side effect
State the class of drug to which Morphine belongs
Opiate
Describe the MOA of Morphine
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
State indications for Morphine
Acute Severe Pain (incl. in setting of MI)
Acute Pulmonary Oedema
Chronic Pain
State side effects of Morphine
Nausea
Vomiting
Abdominal Pain
Constipation
Respiratory Depression
Sedation
Describe important pharmacodynamic/pharmacokinetic features of Morphine
Predominantly metabolised by the liver
Metabolites are active and can accumulate in renal failure
Accumulation can result in respiratory and central nervous system depression
Describe important pieces of patient information that should be given with Morphine
Often given with an anti-emetic to reduce nausea/vomiting
State the class of drug to which Oxycodone belongs
Opiate
Describe the MOA of Oxycodone
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
State indications for Oxycodone
Moderate to Severe Pain Relief in Cancer Patients
Post-Operative Pain
Severe Pain
State side effects of Oxycodone
Nausea
Vomiting
Abdominal Pain
Constipation
Describe important pharmacodynamic/pharmacokinetic features of Oxycodone
Available as long and short-acting preparations
Predominantly metabolised by the liver
Often administered via slow IV/SubCut infusion
Describe important pieces of patient information that should be given with Oxycodone
Nausea and constipation are common side effects
Give two examples of Non-Selective NSAIDs
Ibuprofen
Diclofenac
Describe the MOA of Non-Selective NSAIDs
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
State indications for Non-Selective NSAIDs
Mild to Moderate Pain Relief
Rheumatic Disorders (e.g. RA or OA)
Fever (Anti-Pyretic Effect)
State side effects of Non-Selective NSAIDs
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)
Describe important pharmacodynamic/pharmacokinetic features of Non-Selective NSAIDs
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.
Describe important pieces of patient information that should be given with Non-Selective NSAIDs
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
Give an example of a Selective NSAID
Celecoxib
Describe the MOA of Celecoxib
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)
State indications for Celecoxib
Pain and Inflammation in: OA, RA, Ankylosing Spondylitis
State side effects of Celecoxib
Gastric and Duodenal Ulceration (risk increases with duration of therapy and dosage)
Nausea
Diarrhoea
Renal Impairment
Hyperkalaemia
Describe important pharmacodynamic/pharmacokinetic features of Celecoxib
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)
Describe important pieces of patient information that should be given with Celecoxib
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
Describe the MOA of Paracetamol
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
State indications for Paracetamol
Mild to Moderate Pain Relief
Fever
State side effects of Paracetamol
Rash/Blood Disorders (Rare)
Describe important pharmacodynamic/pharmacokinetic features of Paracetamol
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)
Describe important pieces of patient information that should be given with Paracetamol
Take only the prescribed amount and be wary of other over-the-counter medications that may contain paracetamol
State the class of drug to which Allopurinol belongs
Xanthine Oxidase Inhibitors
Describe the MOA of Allopurinol
Reduces synthesis of uric acid by competitively inhibiting xanthine oxidase
Reduces serum uric acid level
State indications for Allopurinol
Prophylaxis of Gout
Prophylaxis of Calcium Oxalate Renal Stones
Hyperuricaemia Associated with Cancer Chemotherapy
State side effects of Allopurinol
Rash
Hypersensitivity
GI Disturbance
Neutropenia (Rare)
Describe important pharmacodynamic/pharmacokinetic features of Allopurinol
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
Describe important pieces of patient information that should be given with Allopurinol
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
