50+ Drugs Flashcards

1
Q

What are the indications for the use of aspirin?

A

Secondary prevention of thrombotic events

Pain relief

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2
Q

What is the mechanism of action of aspirin?

A

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

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3
Q

What are the side effects of aspirin?

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

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

A

True

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5
Q

What drug might be prescribed alongside aspirin?

A

Proton pump inhibitor

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6
Q

To which class of drugs does aspirin belong?

A

Anti platelet

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7
Q

What are the side effects of clopidogrel?

A

Bleeding
Abdominal pain
Diarrhoea

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8
Q

When should clopidogrel be avoided?

A

Liver failure

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9
Q

What are the side effects of tissue plasminogen activators?

A

Bleeding

Allergic reaction /angiooedema

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10
Q

Which tissue plasminogen activator is given as a single bolus?

A

Tenecteplase

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11
Q

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

A

Alteplase

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12
Q

Which anticoagulant is used in haemodialysis?

A

Heparin

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13
Q

What are the side effects of heparins?

A

Bleeding
Heparin induced thrombocytopenia
Osteoporosis

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14
Q

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

A

Heparins require therapeutic drug monitoring

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15
Q

How is therapeutic drug monitoring of unfractionated heparin conducted?

A

APTT

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16
Q

How can the anticoagulant effect of heparin be reversed?

A

Protamine

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17
Q

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

A

True

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18
Q

What are the side effects of warfarin?

A

Bleeding
Warfarin necrosis
Osteoporosis

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19
Q

How is therapeutic drug monitoring of warfarin conducted?

A

INR

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20
Q

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

A

Aspirin

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21
Q

What are the side effects of dabigatran?

A

Bleeding

Dyspepsia

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22
Q

What are the side effects of rivaroxaban and apixaban?

A

Bleeding

Nausea

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23
Q

What are the indications of rivaroxaban?

A

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

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24
Q

What enzyme system metabolises rivaroxaban and apixaban but not dabigatran?

A

CYP450

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25
What are the indications of apixaban?
Prophylaxis of VTE following hip/knee replacement surgery | Thromboprophylaxis in non-valvular AF
26
Give examples of cardio selective beta blockers?
Bisoprolol | Atenolol
27
What is the mechanism of action of cardio selective beta blockers?
Cardioselective beta 1 adrenoreceptor antagonists. Inhibit sympathetic stimulation of the heart and renal vasculature, Blockade of the SA node reduces heart rate, blockade of receptors in the myocardium depress cardiac contractility and blockage of beta-1 adrenoreceptors in renal tissues inhibits the release of renin
28
What are the indications for bisoprolol/atenolol?
Hypertension Angina Rate control in AF Bisoprolol is used as part of supportive therapy for mild/moderate heart failure
29
What are the side effects of cardiac selective beta blockers?
``` Bradycardia Hypotension Bronchospasm Fatigue Cold extremities Sleep disturbances Loss of hypoglycaemic awareness ```
30
In what patients should cardiac selective and non-cardioselective beta blockers be avoided?
Asthma / COPD due to risk of bronchospasm | History of frequent hypoglycaemia
31
Why should beta blockers and rate-limiting calcium channel blockers not be combined in anti-hypertensive therapy?
Risk of heart block
32
Give examples of rate-limiting calcium channel blockers?
Verapamil | Diltiazem
33
Give examples of non-cardioselective beta blockers?
Propranolol | Carvedilol
34
What is the mechanism of action of propranolol?
Non-cardioselective beta one adrenoreceptor antagonist
35
What is the mechanism of action of carvedilol?
Non-selective beta one, beta two and alpha one adrenergic receptor antagonist
36
What are the indications for the use of non-cardioselective beta blockers?
``` Hypertension Angina Anxiety Migraine prophylaxis Post MI prophylaxis Carvedilol may be sued as part of supportive therapy for mild/moderate heart failure ```
37
What are the side effects of non-cardioselective beta blockers?
``` Bradycardia Hypotension Bronchospasm Fatigue Cold extremities Sleep disturbances Loss of hypoglycaemic awareness ```
38
In what patients should non-cardioselective beta blockers be cautioned?
Diabetics due to risk of deranged carbohydrate metabolism
39
Why should propranolol be avoided in liver impairment?
It is lipid soluble and is predominantly cleared by the liver
40
Give examples of ACE inhibitors?
Ramipril Enalapril Lisinopril Perindopril
41
What are the indications for ACE inhibitors?
Hypertension Heart failure Nephropathy Prevention of cardiovascular events in high risk patients
42
What are the side effects of ACE inhibitors?
``` Dry cough Hypotension Hyperkalaemia Renal impairment Angiooedema ```
43
Why is a blood test requires at 1-2 weeks after starting ACE inhibitors?
To check electrolyte balance
44
In which patients are adverse drug reactions with ACE inhibitors most common?
``` High dose diuretic therapy Hypovolaemia Hyponatraemia Hypotension Unstable heart failure Renovascular disease ```
45
Give examples of nitrates
Isosorbide mononitrate | glyceryl trinitrate
46
Describe the mechanism of action of nitrates?
Converted to nitric oxide which is a potent vasodilator. These are cardioselective and act predominantly on coronary blood vessels, enhancing flow of blood to ischaemic areas of the myocardium. Additionally, nitrates reduce myocardial oxygen consumption by reducing cardiac preload and after load
47
What are the indications for the use of nitrates?
Angina | Severe hypertension
48
What are the side effects of nitrates?
Headache Postural hypotension Tachycardia
49
Tolerance to nitrates develops with long term use. How can this be avoided?
Patients should have a daily nitrate free period
50
How is isosorbide mononitrate administered?
Orally
51
How is glyceryl trinitrate administered?
Sublingual spray/tablet | IV
52
Give examples of rate limiting calcium channel blockers.
Verapamil | Dilitiazem
53
What is the mechanism of action of rate limiting calcium channel blockers
Prevents cellular entry of calcium by blocking l-type calcium channels. Myocardial and smooth muscle contractility is depressed and cardiac contractility is reduced, These dilate coronary blood vessels to reduce afterload. Antidysrythmic actions due to prolonged AV node conduction to depress the heart rate
54
What are the indications for rate limiting calcium channel blockers?
Supraventricular arrythmias Treatment of angina Hypertension
55
What are the side effects of verapamil?
``` Constipation Flushing Headache Dizziness Hypotension ```
56
What are the side effects of diltiazem?
``` GI disturbances Bradycardia Peripheral oedema Dizziness Headache Hypotension ```
57
When are rate limiting calcium channel blockers contraindicated and avoided?
Contraindicated - heart failure, left ventricular dysfunction Avoid - bradycardia, hypotension
58
Give examples of non rate-limiting calcium channel blockers?
Amlodipine Nifedipine Felodipine
59
Describe the mechanism of action of non rate-limiting calcium channel blockers?
Prevents cellular entry of calcium by blocking l-type calcium channels Myocardial and smooth muscle contractility is depressed. Dilate coronary blood vessels and reduce after load. Do not lower heart rate
60
What are the indications for the use of non-rate limiting calcium channel blockers?
Hypertension | Treatment of angina
61
What are the side effects of non-rate limiting calcium channel blockers?
``` Ankle oedema Abdominal pain / nausea Palpitations Flushing Headache Dizziness ```
62
When should non rate limiting calcium channel blockers be avoided?
Cardiogenic shock Unstable angina significant aortic stenosis
63
What makes ankle swelling with calcium channel blockers worse?
Hot weather
64
Give examples of HMG CoA reductase inhibitors?
Simvastatin Atorvastatin Pravastatin
65
Describe the mechanism of action of statins?
Completely inhibits HMG CoA reductase - the rate limiting enzyme in the mevalonate pathway of cholesterol synthesis. Increases LDL receptor expression on the surface of hepatocytes. Increases hepatic uptake of cholesterol, reducing plasma cholesterol levels, Reduces development of atherosclerotic plaques
66
What are the indications of HMG CoA reductase inhibitors?
Familial hypercholesterolaemia | prevention of cardiovascular events in high risk patients
67
What are the side effects of HMG CoA reductase inhibitors?
Myalgia Myopathy and rhabdomyolysis GI disturbances Liver abnormalities - deranged LFTs
68
What side effects of HMG CoA reductase inhibitors are dose related?
Myalgia | Rhabdomyolysis
69
Give an example of a cardiac glycoside?
Digoxin
70
Describe the mechanism of action of digoxin?
Increases vagal parasympathetic activity and inhibits the NA/K pump causing intracellular build up of sodium. In an effort to remove NA, Ca is brought into the cell by the action of Na/Ca exchangers. The build-up of Ca is responsible for the increased force of contraction of the heart and reduced rate of conduction through the AV node
71
What are the indications for cardiac glycosides (digoxin)?
Heart failure | Rate control in AF
72
What are the side effects of digoxin?
Nausea Vomiting Diarrhoea Confusion
73
What can be used to treat life threatening digoxin overdose?
Digoxin specific antibody
74
What are the major determinants for safe digoxin dosage?
Renal function Age Heart Disease
75
Digoxin has a narrow therapeutic index. T/F?
True
76
Give an example of an anti-arrhythmic drug?
Amiodarone
77
Describe the mechanism of action of amiodarone?
Amiodarone blocks cardiac potassium channels, prolonging depolarisation of the cardiac action potential. It restores regular sinus rhythm and slows AV node conduction
78
What are the indications of amiodarone?
Supraventricular / ventricular arrhythmias
79
What are the side effects of amiodarone?
``` Photosensitivity skin reactions Hypersensitivity reactions Hyper/hypothyroidism Pulmonary fibrosis corneal deposits neurological disturbances GI disturbances / hepatitis ```
80
How long can it take to achieve steady state amuodarone plasma concentrations?
Weeks to months
81
What monitoring blood tests are required during amiodarone treatment?
TFTs before treatment, every six months and if symptomatic | LFTs
82
Give examples of penicillins?
Flucloxacillin Amoxicillin Benzylpenicillin Penicillin V
83
Describe the mechanism of action of penicillins?
Attaches to penicillin-binding proteins on forming bacterial cell walls which inhibits the transpeptidase enzyme which cross-links the bacterial cell wall. Failure to cross-link causes bacterial cell autolysis.
84
What are the indications for flucloxacillin?
Soft tissue infection Staphylococcal endocarditis Otitis externa
85
What are the indications of amoxicillin?
Non-severe community acquired pneumonia
86
What are the side effects of penicillins?
Diarrhoea Vomiting Liver Function Impairment Hypersensitivity reactions
87
What is amoxicillin often combined with to prevent resistance?
Clavulinic acid - a beta lactase inhibitor
88
Give examples of cephalosporins?
Ceftriaxone | Cephalexin
89
What is the mechanism of action of cephalosporins?
Attaches to penicillin binding proteins on forming bacterial cell walls, inhibits transpeptidase enzyme which cross links the bacterial cell wall. Failure to cross link induces bacterial cell autolysis
90
Cephalosporins are less susceptible to beta lactamases than penicillins. T/F?
True
91
What are the indications for cephalosporins?
Serious infection - sepsis, pneumonia, meningitis
92
What are the side effects of cephalosporins?
Hypersensitivity reactions Antibiotic associated c.difficile Liver function impairment
93
How are cephalosporins secreted?
Renal excretion
94
Give an example of a glycopeptide?
Vancomycin
95
Describe the mechanism of action of vancomycin?
Bactericidal, inhibiting cell wall synthesis in gram positive bacteria
96
What are the indications for vancomycin?
Severe gram positive infections MRSA infection Severe c.difficile infection
97
What are the side effects of vancomycin?
``` Fever Rash Local phlebitis at site of infection Nephrotoxicity Ptottoxicity Blood disorders - neutriopenia Anaphylactoid reaction - red man syndrome - if infusion rate is too fast ```
98
Vancomycin requires therapeutic drug monitoring. T/F?
True
99
How can vancomycin be administered?
Continuous intravenous infusion or a pulsed infusion regimen
100
Describe the mechanism of action of gentamicin
Binds to the 30s ribosomal subunit to inhibit protein synthesis and induce prolonged post-antibiotic bacteriostatic effect, There is additional bactericidal action on the cell wall in high doses
101
What are the indications for gentamicin?
Gram negative infections (biliary tract infection, pyelonephritis, hospital acquired pneumonia Severe gram positive infections (soft tissue infections and endocarditis)
102
What are the side effects of gentamicin?
Nephrotoxicity | Ototoxicity
103
What are the indications for the use of quinolones?
``` Gram negative bacterial infection Respiratory tract infection Upper UTI Peritoneal infection Gonorrhoea Prostatitis ```
104
What are the side effects of quinolones?
GI toxicity QT prolongation C.difficile infection Tendonitis
105
What are the indications for macrolides?
Atypical organisms causing pneumonia / severe community acquired pneumonia Mild/moderate skin and soft tissue infection otitis media Lyme disease helicobacter pylori eradication therapy severe campylobacter infection
106
What are the indications for the use of trimethoprim?
First line for uncomplicated UTI Acute or chronic bronchitis Pneumocystis pneumnia
107
What is the mechanism of action of acyclovir?
A guanosine derivative, converted to triphosphate by infected cells, it then inhibits DNA polymerase, terminating the nucleotide chain and inhibiting viral DNA replication
108
What are the indications of acyclovir?
Herpes simples infection | Varicella zoster infection
109
To what class of drug does acyclovir belong?
Anti viral
110
What are the side effects of aciclovir?
Nausea Vomiting Local inflammation at infusion site if given IV
111
How can acyclovir be administered?
Oral IV Topical
112
Acyclovir penetrates well into the CSF. T/F?
True
113
Describe the mechanism of action of short and long acting beta adrenergic bronchodilators?
Relaxes bronchial smooth muscle, inducing bronchodilator. Inhibits pro-inflammatory cytokine release from mast cells and TNF-alpha release from monocytes to reduce airway inflammation. Stimulates cilia action which increases mucous clearance
114
What are the indications of short and long acting beta 2 adrenoreceptor agonists?
Asthma | COPD
115
What are the side effects of short and long acting beta 2 adrenoreceptor agonists?
Tremor Tachycardia/cardiac dysryhtmia Headache Sleep disturbances
116
Long acting beta 2 adrenoreceptor agonists can be used in rapidly deteriorating asthma. T/F?
False - they have too slow an onset for this so short acting beta 2 agonists should be used instead
117
Give examples of anti-muscarinic bronchodilators?
Tiotropuim | Ipratropium bromide
118
Describe the mechanism of action of anti muscarinic bronchodilators?
Muscarinic receptor M3 antagonists produce bronchodilators effects. It reduces mucous secretion and may increase bronchial mucous clearance by stimulating cilia
119
What are the indications for anti-muscarinic bronchodilators?
Asthma COPD Rhinitis
120
What are the side effects of anti-muscarinic bronchodilators?
Dry mouth Cough Constipation
121
Why should nebuliser ipratropium bromide always be administered via a mouth piece?
To minimise the risk of acute angle closure glaucoma
122
Give an example of an inhaled corticosteroid?
Beclomethasone
123
Describe the mechanism of action of inhaled corticosteroids?
Anti-inflammatory effect on airways Decrease formation of pro-inflammatory cytokines Up-regulates beta 2 adrenoreceptors in airways
124
What are the indications for inhaled corticosteroids?
COPD | Asthma
125
What are the side effects of inhaled corticosteroids?
oral candidiasis adrenal suppression osteoporosis
126
All patients on inhaled corticosteroids need to carry a steroid user card. T/F?
False - only those on high dose ICS
127
Give examples of antihistamines?
Chlorpheniramine Desloratidine Fexofenadine Hydroxyzine
128
Describe the mechanism of action of antihistamines?
H1 receptor antagonist | Inhibits histamine mediated contraction and vasodilation of the bronchial smooth muscle
129
What are the indications for antihistamines?
Anaphylaxis Hay fever Urticaria Sedation
130
What are the side effects of antihistamines?
Drowsiness | Tinnitus
131
How do antihistamines cause sedation?
Central nervous system H1 antagonism
132
What are the implications of the sedative effects on antihistamines for patients?
Can't drive or operate heavy machinery
133
Describe the mechanism of action of levodopa?
Pro-drug which crosses the BBB and is converted to dopamine. This increases stratal dopaminergic neurotransmission
134
What is the indication for the use of levodopa?
Parkinson's disease
135
What are the side effects of levodopa?
``` Dyskinesia Compulsive disorders Hallucinations Nausea GI upset ```
136
What is co-administered with levodopa to reduce the side effects?
Dopamine decarboxylase inhibitor or COMT inhibitor
137
Give examples of dopamine agonists?
``` Apomorphine Pramipexole Bromocriptine Pergolide Rotigotine ```
138
Describe the mechanism of action fo dopamine agonists?
Stimulate post synaptic dopamine receptors Apomorphine is non selective for D1 and D2 Prampipexole is selective for D3 receptor
139
What is the indication for the use of dopamine agonists?
Parkinson's disease
140
What are the side effects of apomorphine?
Pain at site of injection, nausea, vomiting
141
What are the side effects of pramipexole?
Hallucinations Nausea Drowsiness Involuntary movement
142
How is apomorphine administered?
Parenterally
143
Give an example of a catechol-o-methyl transferaseinhibitor?
Entacapone
144
What is the mechanism of action of entacapone?
Prevents peripheral breakdown of levodopa by inhibiting COMT, therefore more levodopa reaches the brain
145
What is the indication for entacapone?
Parkinson's disease in conjunction with L-DOPA and dopamine decaroxylase inhibitor
146
What are the side effects of entacapone?
``` Dyskinesia Nausea Abdominal pain Vomiting Dry mouth Dizziness ```
147
Describe the mechanism of action of carbamazepine?
Voltage gated sodium channel blocker on the pre-synaptic membrane Blocks the sodium influx reduces neuronal excitability and decreases the action potential
148
What are the indications for the use of carbamezepine?
Epilepsy Trigeminal neuralgia Neuropathic pain
149
What are the side effects of carbamazepine?
``` Dizzziness Dry mouth Ataxia Fatugue Headache Dipolopia Blurred vision Hyponatraemia Stevens Johnsons syndrome ```
150
What food can significantly increase serum levels of carbamazepine?
Grapefruit
151
Give examples of voltage gated sodium channel antagonists used as anti-epileptics?
Carbamezepine | Lamotrigrine
152
Give examples of voltage gated potassium channel agonists used as anti-epileptics?
Retigabine
153
Give an example of a SV2A vesicle antagonist used as an anti-epileptic drug?
Levetiracetam
154
Give examples of voltage gated calcium channel antagonists used as anti-epileptics?
Pregabalin | Gabapentin
155
Give examples of GABA metabolism inhibitors used as anti-epileptic drugs?
Valproate | Vigabatrin
156
Give examples of GABA transporter antagonists used as anti-epileptic drugs?
Tiagabine
157
Give examples of GABA receptor agonists used as anti-epileptic drugs?
Benzzodiazepines
158
Describe the mechanism of action of sodium valproate?
Weak sodium ion channel blocker Inhibitor of GABA degrading enzymes Increased GABA stops action potentials
159
What are the indications of sodium valproate?
Epilepsy Bipolar disorder Depression
160
What are the side effects of sodium valproate?
``` Nausea Diarrhoea Gastric irritation Weight gain Hyponatraemia Behavioural disturbances Confusion Stevens Johnson syndrome ```
161
What blood test must be conducted before and during the initial 6 months of sodium valproate therapy?
LFTs
162
Describe the mechanism of action of phenytoin?
Acts as a voltage gated sodium channel blocker on the pre-synaptic neuronal membrane Limits action potential transmission to limit spread of seizure activity
163
What are the indications for phenytoin?
Epilepsy | Trigeminal neuralgia
164
What are the side effects of phenytoin?
``` Insomnia Headache Rash Constipation Vomiting Gingival hyperplasia Liver damage Steven Johnson syndrome Thrombocytopenia ```
165
Phenytoin has a narrow therapeutic index. T/F?
True
166
What information is important for patients on phenytoin to know?
Avoid alcohol Take with food to reduce irritaition Do not take calcium, aluminium, magnesium or iron supplements within 2 hours of ingestion
167
Describe the mechanism of action of lamotrigine?
Varied mechanism of action Inhibits voltage gated sodium channels and/or calcium channels Acts on pre-synaptic neuronal membrane Reduces action potential and excitatory signals
168
What are the indications for lamotrigine?
Epilepsy | Depressive episodes associated with bipolar disorder
169
What are the side effects of lamotrigrine?
``` Nausea Vomiting Diarrhoea Tremor Insomnia Blurred vision Aggression Skin reactions- Steven Johnson syndrome and toxic epidermal necrolysis ```
170
What will cause the half-life of lamotrigine to double?
Chronic renal impairment
171
What is the mechanism of action of levetiracetam?
SV2A is a synaptic vesicle protein required for neurotransmitter release which is blocked by levetiracetam to induce an anti-epileptic effect
172
What is the indication for levetiracetam?
Epilepsy
173
What are the side effects of levetiracetam?
``` Headache Fatigue Anxiety Irritability Drowsiness Constipation ```
174
Cytochrome p450 is not involved in the metabolism of levetiracetam. T/F?
True
175
Give examples of selective serotonin reuptake inhibitors?
``` Citalopram Fluoxetine Paroxetine Escotalopram Sertraline ```
176
Describe the mechanism of action of SSRIs?
Inhibitition of reuptake of serotonin at the serotonin reuptake pump of the synaptic cleft in the CNS. Increases serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors
177
What are the indications of SSRIs?
Depression Obsessive compulsive disorder Bulimia
178
What are the side effects of SSRIs?
``` Dry mouth Nausea Insomnia Anxiety Decreased libido Seizures Dyskinesia ```
179
Why do SSRIs have fewer side effects than tricyclic antidepressants?
They bind with less affinity to histamine, acetylcholine and norepinephrine receptors
180
Give examples of tricyclic antidepressants?
Amitriptyline Imipramine Doxepin
181
Describe the mechanism of action of tricyclic antidepressants?
Block the reuptake of monoamines by binding to the monoamine pump at the pre-synaptic cleft which reduces the rupture or norepinephrine and/or serotonin
182
What are the indications of tricyclic antidepressants?
Depression Panic disorders Neuropathic pain
183
What are the side effects of tricyclic antidepressants?
``` Sedation Postural hypotension Tachycardia Urinary retention Dry mouth Blurred vision Diplopia ```
184
What can occur with overdose of tricyclic antidepressants?
Seizures | Cardiac arrhythmias
185
Give examples of first generation antipsychotics?
Haloperidol | Chlorpromazine
186
Give examples of atypical anti-psychotics?
Olanzapine | Clozapine
187
Describe the mechanism of action of anti-psychotics?
Block dopamine receptors, Action on mesolimic and nigrostriatal parts of the brain. Also have anti-histaminergic and anti-cholinergic effects. Reduce positive symptoms of schizophrenia
188
What are the indications of anti-psychotics?
``` Schizzophrenia Mania Delusions/hallucinations Bahvioural problems Haloperidol is an anti-emetic ```
189
What are the side effects of anti-psychotics?
``` Sedation Postural hypotension Tachycardia Urinary retention Dry mouth Blurry vision ```
190
Give examples of benzodiazepines?
Diazepam Lorazepam Midazolam
191
Describe the mechanism of action 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 bran
192
What are the indications for benzodiazepines?
Anxiety Epilepsy Muscle spasm Alcohol withdrawal
193
What are the side effects of benzodiazepines?
Sedation Ataxia Altered mental status Insomnia
194
How can diazepam be administered?
Oral Rectal Parenteral
195
How can lorazepam by administered?
Oral | Parenteral
196
Which benzodiazepine is used most often in patients with liver failure?
Lorazepam as it accumulates less with long term use
197
Give an example of a short acting benzodiazepine?
Midazolam
198
Give examples of glucocorticoids which can be given orally?
Prednisolone Hydrocortisone Dexamethasone
199
Give examples of glucocorticoids which can be given topically?
Hydrocortisone Betamethasone Clobetasone
200
Give examples of glucocorticoids which can be given parenterally?
Methylprednisolone Hydrocortisone Triamcinolone
201
Describe the mechanism of action of glucocorticoids?
Bind to glucocorticoid receptors causing up regulation of a variety of anti-inflammatory mediators and down regulation of pro-inflammatory mediators. Also increase gluconeogenesis and some glucocorticoids have mineralocorticoid activity
202
What are the indications for these of glucocorticoids?
Replacement therapy in adrenal insufficiency Post transplant immunosupression Treatment of exacerbations of inflammatory conditions(e.g. eczema, RA, IBD) Acute asthma
203
What are the side effects of glucocorticoids?
``` Sleep disturbance Modd disturbance Hyperglycaemia Immunodeficiency Easy bruising Moon faces Increased abdominal fat Glaucoma Striae Hypertension Gastric irritation ```
204
What information is it important for patients on glucocorticoids to know?
Avoid alcohol and caffeine Take with food to avoid gastric irritation Don't stop suddenly Always inform doctors that they are on steroids and carry a steroid card Double dose when ill
205
Give an example of a corticosteroid which has predominant glucocorticoid activity and low mineralocorticoid activity?
Prednisolone, gbetamethasone, dexamethasone
206
Give examples of corticosteroids which show much glucocorticoid and mineralocorticoid activity?
Hydrocortisone | Fludrocortisone
207
Give examples of anti-TNF agents?
Etanercept Infliximab Adalimumab
208
Describe the mechanism of action of anti-TNF agents?
Anti TNF-alpha and beta. Blocks its interactions with TNF cell receptors TNF alpha and beta produced from macrophages and T cells Stimulates cytokines IL1/8/6. Reduces inflammation
209
What is the indication for anti-TNF agents?
RA Psoriatic arthritis Ankylosing spondylitis Juvenile arthritis
210
What are the side effects of anti-TNF agents?
Injection site reactions Flu-Like symptoms(fever, headache, runny nose) Immune deficiency
211
Give examples of immunosupressants
Methotrexate Azathioprine Mercaptopurine
212
Describe the mechanism of action of azathioprine?
Blocks purine synthesis mainly in lymphocytes
213
Describe the mechanism of action of methotrexate?
Stops the action of the enzyme dihydrofolate needed for the production. of DNA
214
What are the indications for. the use of immunosuppressants?
Post transplantation immunosuppression inflammatory bowel disease renal vasculitis paediatric leukaemia (methotrexate)
215
What are the side effects of immunosuppressants?
``` Bone marrow suppression Risk of infection Nephrotoxicity Hepatotoxicity Seizures GI upset Mucosal ulceration Alopecia ```
216
Immunosuppressants cross the blood brain barrier. T/F?
False
217
Which patients are more prone to azathioprine and mercaptopurine related marrow suppression?
Patients with low levels of thiopurine and methyltransferase
218
Give examples of PPIs
Omeprazole Lansoprazole Pantoprazole
219
Describe the mechanism of action of PPIs?
Bind to H/K ATPase pump on gastric parietal cells | Reduces HCl production and hence reduces gastric acidity
220
What are the indications for the use of PPIs?
``` Peptic ulcers GORD H.pylori infection prophylaxis in patients on long term NSAIDs Zollinger Ellison syndrome ```
221
What are the side effects of PPIs?
``` Nausea Vomiting Insomnia Vertigo Headaches ```
222
Which PPI is an. inhibitor of CYP450?
Omeprazole
223
What information is it important for patients on PPIs to know?
Avoid alcohol | take 30-60 mins before food
224
Give examples of. H2 receptor antagonists?
Ranitidine Cimetidine Famotidine Nizatifine
225
Describe the mechanism of action of H2 receptor antagonists?
Histamine binds to H2 receptors on. gastric parietal cells stimulating gastric acid secretion H2 antagonists inhibit this by reduced cAMP and hence reducing the activity of H/K ATPase
226
What are the indications for the use of H2 receptor antagonists?
Peptic ulcer GORD Zollinger Ellison. syndrome
227
What are the side effects of H2 receptor antagonists?
``` Headache Dizziness Diarrhoea Reduced B12 absorption Gynaecomastia ```
228
Which H2 receptor antagonist. is. an inhibitor of CYP450?
Cimetidine
229
Give examples of laxatives
Lactulose | Senaa
230
Describe the mechanism of action of lactulose?
Reduces water reabsorption in the. intestine - pulls water into the bowel to promote distension and movement
231
Describe the mechanism of action of Senna?
Stimulant/irritant agent
232
What are the indications for. the use of laxatives?
Constipation pregnancy prophylaxis in opiate analgesic use
233
What are the side effects of laxatives?
Dehydration salt loss abdominal cramps fatigue
234
Why is Senna recommended for short term use only?
Risk organ failure with long term use or abuse
235
What are. the four broad types of laxatives?
Bulk producing. agents (lactulose) Stool softeners Simulant or irritant (senna) Hydrating agents (milk of magnesia)
236
Give an example of an anti-emetic?
Cyclizine
237
Describe the mechanism of action of cyclizine?
histamine. H1 receptor antagonist, acts on. vomiting centre. in. the medullary region. Also has mild anticholinergic and antimuscarinic effects
238
What are the indications for the use of anti-emetics?
Nausea and vomiting Motion sickness Vertigo and dizziness Prophylaxis alongside chemotherapy and opiate. analgesic use
239
What are the side effects of anti-emetics?
Headache Sedation Diarrhoea
240
What are the five broad types of anti-emetic?
``` Anticholinergics Antihistamine Serotonin antagonist Phenothiazine Motility stimulants ```
241
Give an example of an anticholinergic antiemetic?
Hyoscine. hydrobromide
242
Give an example of a serotonin antagonist antiemetic?
Ondansetron
243
Give an example of a phenothiazine antiemetic?
Prochlorperazine
244
Give an example of a motility stimulant antiemetic?
Metoclorpramide
245
Describe the mechanism of action of metclopramide?
Dopamine D2 receptor antagonist, raises activity in the chemoreceptor. trigger zone and increases gastric emptying and intestinal transit. Reduces oesophageal reflux
246
What are the indications for the use of metclopramide?
Nausea Vomiting To increase gastric emptying
247
What are the side effects of metclopramide?
``` Dystonia Confusion Dizziness Diarrhoea Parkinsonism with long term use ```
248
How can metclopramide be administered?
Oral | Parenterally
249
Describe the mechanism of action of prochlorperazine?
Anti-psychotic drug which is used as an anti-emetic. Dopamine D2 receptor antagonist causes increases dopamine turnover
250
What. are the indications for the. use of prochlorperazine?
Nausea Vomiting Adjunct in some psychotic disorders
251
What are the side effects of prochlorperazine?
Dry mouth Tachycardia restlessness drowsiness
252
Give examples of thiazide diuretics?
Bendroflumethazide Indapamide Chlortalidone
253
Describe the. mechanism of action of thiazide diuretics?
Inhibit sodium/chloride transporters at the distal convulsed tubule and collecting duct Increases sodium, chloride and water excretion
254
What are the indications of thiazide diuretics?
Hypertension | Oedema of cardiac/renal/hepatic/iatrogenic origin
255
What are the side effects of thiazide diuretics?
``` Hypokalaemia Hypomagnesaemia Hyponatraemia Hypercalcaeia Hyperuricaemia Reduced glucose tolerance Hypersensitivity reactions ```
256
What drug reduces. the efficacy of thiazide diuretics?
NSAIDs
257
Give examples of loop diuretics?
Furosemide Bumetanide Torasemide
258
Describe the mechanism of action of loop diuretics?
Na/Cl/K symporter antagonists | Act on the thick ascending loop of Henley to increase the secretion of sodium, potassium, chloride and water
259
What are the indications of loop diuretics?
``` Hypertension Hyperkalaemia Heart failure Cirrhosis of the liver Nephrotic syndrome ```
260
What are the side effects of loop diuretics?
Hypokalaemia, hypovolaemia, hyperuricaemia Metabolic acidosis Abdominal pain Ototoxicity
261
Give an example of a long acting insulin
Glargine
262
Describe the mechanism of action of insulin
Insulin increases cellular uptake of glucose. It stimulates glycogenesis, encourages DNA synthesis and promotes release of growth hormone.
263
Give an example of a short acting insulin
Novorapid
264
Give an example of a fast-acting intermediate-acting mix insulin
Humalog mix
265
What are the indications for insulin?
T1DM T2DM Hyperkalaemia (in conjunction with dextrose)
266
What are the side effects of insulin?
Hypoglycaemia - sweats, shakes, tachycardia, headache, weakness, fatigue Oedema Injection site reactions
267
What type of insulin can be given IV?
Short acting e.g. act rapid
268
Describe the time to reach circulation, peak and duration of action of rapid acting insulin?
Reaches circulation within 15 mins after injection peaks 30 to 90 mins later lasts for up to 5 hours
269
Describe the time to reach circulation, peak and duration of action of short acting insulin?
Reaches circulation 30 mins after injection peaks 2-4 hours later lasts for up 4-8 hours
270
Describe the time to reach circulation, peak and duration of action of intermediate acting insulin?
Reaches circulation 2-6 hours after injection peaks 4-14 hours later lasts for up 20 hours
271
Describe the time to reach circulation, peak and duration of action of long acting insulin?
Reaches circulation 6-14 hours after injection minimal peak lasts for up 24 hours
272
Give examples of sulphonylureas
Gliclazide | Glimepiride
273
Describe the mechanism of action of sulphonylureas?
Stimulates beta cells in the pancreas to produce more insulin. Increases cellular glucose uptake and glycogenesis and reduces gluconeogenesis
274
What is the duration of action of Gliclazide?
~12 hours
275
What is the indication for the use of sulphonylureas?
T2DM
276
What are the side effects of sulphonylureas?
``` Hypoglycaemia Rashes Nausea Vomiting Stomach pain Indigestion Weight gain ```
277
Give an example of a long acting sulphonylurea?
Glimepiride
278
Give and example of a biguanide?
Metformin
279
Describe the mechanism of action of biguanides
Increase the activity of AMP-dependent protein kinase (AMPL) which inhibits gluconeogenesis and reduces insulin resistance
280
What are the indications for the use of metformin?
T2DM | Metabolic and reproductive abnormalities associated with PCOS
281
What are the side effects of metformin?
``` Diarrhoea Nausea Vomiting Taste disturbances Lack of appetite Risk of lactic acidosis with illness and renal failure ```
282
When should metformin not be used?
Pregnancy | Renal failure
283
Give examples of GLP1 agonists
Exanatide | Liraglutide
284
Describe the mechanism of action of GLP1 agonists
GLP-1 is a hormone which is release after meals to increase insulin secretion. GLP1 agonists act on GLP1 receptors to increase insulin secretion, decrease glucagon secretion and reduce hunger
285
What are the indications for the use of GLP1 agonists?
T2DM (in association with excess weight)
286
What are the side effects of GLP1 agonists?
Hypoglycaemia Nausea Vomiting Diarrhoea
287
How is GLP1 administered?
Bi-daily injections
288
What is the mechanism of action of levothyroxine?
Thyroxine increases. the metabolic rate of all tissues in the body, Levothyroxine is a synthetically prepared T4 which is converted to T3 in the liver and kidney. It maintains brain function, food metabolism and body temperature
289
What are the indications for the use of levothyroxine?
Hypothyroidism | Chronic lymphocytic thyroiditis
290
What are the side effects of levothyroxine?
``` Chest pain Coma Diarrhoea Tachycardia Itching Muscle cramps ```
291
How long after starting levothyroxine should TFTs be checked?
6 weeks
292
Give examples of anti-thyroid drugs?
Carbimazole | Propylthiouracil
293
Describe the mechanism of action of anti-thyroid drugs
Reduces activity of peroxidase enzyme required for the production of thyroid hormones and may also reduce peripheral conversion fo T4 to. T3
294
What are the indications for the use of anti-thyroid drugs?
Hyperthyroidism Thyrotoxicosis Preparing patients for thyroid surgery
295
What. are the side effects of anti-thyroid drugs?
Rash Sore throat Agranulocytosis
296
Carbimazole is a prodrug. T/F?
True
297
Why can carbimazole not be used in pregnancy?
It can cross the placenta
298
What drug is usually co-prescribed with anti-thyroid agents?
Beta blockers
299
Give examples of bisphosphonates?
Aledronate | Ibandronate
300
Describe the mechanism of action of bisphosphonates
Inhibits osteoclast bone resorption | No effect on bone formation
301
What are the indications for bisphosphonates?
Post menopausal osteoporosis Reduces risk of vertebral and hip fractures Paget's disease of bone
302
What are the side effects of bisphosphonates?
``` Abdominal pain Dyspepsia Acid regurgitation Dysphagia Headache ```
303
Give examples of the oral contraceptive pill
Microgynon (combined) | Cerazette (progesterone only)
304
Describe the mechanism of action of the oral contraceptive pill
Acts on female reproductive tract, the mammary glands, hypothalamus and. pituitary gland. Reduces the production of gonadotropin releasing hormone Blunts LH surge. that stimulates ovulation
305
Describe the indications for the oral contraceptive pill
Contraception Menopausal and postmenopausal. disorders Polycystic ovarian syndrome
306
Describe the side effects of the oral contraceptive pill
Mood swings Headache Breast tenderness Increased risk of breast and ovarian cancer Increased risk of venous thromboembolic disease
307
What drugs can worsen the efficacy of the oral contraceptive pill?
Antibiotics | Some enzyme inducers
308
What information is it important for the patient to know when on the oral contraceptive pill?
Important to take the tablet at the same time everyday | Use alternative forms of contraception when taking concurrent antibiotics or enzyme inducers
309
Describe the mechanism of action of codeine, oxycodone and morphine?
Acts on mu, kappa and delta on presynaptic neutrons, this gives numerous effects that increase nociceptive thresholds throughout the central and peripheral nervous system
310
What are the indications for the use fo codeine?
Mild to moderate pain Persistent dry cough Diarrhoea
311
What. are the side effects of codeine?
``` Nausea Vomiting Constipation Biliary spasm Headache on withdrawal ```
312
Why are some people resistant to codeine's analgesic properties?
10% of the population lack the demthylating enzyme which converts codeine to morphine
313
Codeine can be taken with paracetamol. T/F?
True
314
What are the indications for the use of morphine?
Acute severe pain - MI Acute pulmonary oedema Chronic pain
315
What are the side effects of morphine?
``` Nausea Vomiting Abdominal pain Constipation Respiratory depression Sedation ```
316
What can happen with accumulation of morphine?
Respiratory and CNS. depression
317
What drug is morphine often co-administered with?
Anti-emetic
318
What are the indications for the use. of oxycodone?
Moderate to severe pain relief in cancer patients Postoperative pain Severe pain
319
What are the side effects of oxycodone?
Nausea Vomiting Abdominal pain Constipation
320
Give examples of non-selective NSAIDs?
Ibuprofen | Diclofenac
321
Describe the mechanism of action of non-selective NSAIDs
Non-selective inhibits of COX (1+2) enzymes, decreasing key inflammatory mediator prostaglandins from being synthesised which reduces pain, inflammation and swelling
322
Describe the indications of non-selective NSAIDs
Mild to moderate. pain relief Rheumatic disorders - RA, OA Fever
323
What. are the side effects of non-selective NSAIDs?
``` Gastric and duodenal. ulceration Nausea Diarrhoea Increased risk of thrombotic events Renal impairment Hyperkalaemia ```
324
Why should NSAIDs be avoided in pregnancy?
Risk of closure of foetal. ductus arterioles in utero and pulmonary hypertension in the newborn
325
In elderly patients what drug is usually co-prescribed with. non-selective NSAIDs?
PPIs
326
Give an example of a selective NSAID
Celecoxib
327
Describe the mechanism of action of selective NSAIDs
Selective inhibitor of COX2, decreasing key inflammatory mediator prostaglandins from being synthesised. This reduces pain, inflammation and swelling
328
GI side effects of NSAIDs are mediate by COX2. T/F?
False - they are mediated by COX1
329
What are the indications fo the use of selective NSAIDs?
Pain and inflammation in OA, RA, ankylosing spondylitis
330
What are the side effects of selective NSAIDs?
``` Gastric and duodenal ulceration Nausea Diarrhoea Renal impairment Hyperkalaemia ```
331
There is a higher risk of. cardiovascular events with selective compared to non-selective NSAIDs. T/F?
True
332
Describe the mechanism of action of paracetamol?
Weak COX inhibitor with selectivity for brain COX. It therefore lacks peripheral anti-inflammatory actions but is useful in increasing the threshold for nociceptive activation by inhibiting prostaglandin synthesis and its effects centrally
333
What are the indications for the use of paracetamol?
Mild to moderate pain relief | Fever
334
What are the side effects of paracetamol?
Rash | Blood disorders
335
Give an example of a xanthine oxidase inhibitor?
Allopurinol
336
Describe the mechanism of action fo allopurinol?
Reduces synthesis of uric acid by competitively inhibiting xanthine oxidase, this reduces serum uric acid level
337
Describe the indications for the use of xanthine oxidase inhibitors
Prophylaxis of. gout Prophylaxis of calcium oxalate renal stone Hyperuricaemia associated with cancer chemotherapy
338
What are the side effects of xanthine oxidase inhibitors?
Rash Hypersensitivity GI disturbance Neutropenia
339
Why should xanthine oxidase inhibitors not be used to treat acute attacks of gout?
They can exacerbate the inflammation