Pharmacology Flashcards

1
Q

Medication for acne

A

Tetracyclines

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2
Q

Acute coronary syndrome

A

ACE inhibitors
Aspirin
Beta blockers
Clopidogrel
Fibrinolytic drugs
Heparins and fondaparinux
Nitrates
Strong opioids
Statins

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3
Q

Addison’s disease

A

Systemic corticosteroids (glucocorticoids)

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4
Q

Adrenal insufficiency

A

Systemic corticosteroids (glucocorticoids)

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5
Q

Psychomotor agitation

A

Phenothiazines antiemetics
First-generation (typical) antipsychotics
Second-generation (atypical) antipsychotics

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6
Q

Alcohol withdrawal

A

Benzodiazepines

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7
Q

Allergy

A

Antihistamines (H1-receptor antagonists)
Systemic corticosteroids (glucocorticoids)

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8
Q

Anaemia

A

Iron
Vitamins

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9
Q

Medications for anaphylaxis

A

Adrenaline (epinephrine)
Antihistamines (H1-receptor antagonists)
Systemic corticosteroids (glucocorticoids)

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10
Q

Angina

A

Beta blockers
Calcium channel blockers
Nicorandil
Nitrates

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11
Q

Anxiety

A

SSRI antidepressants
Venlafaxine and mirtazepine antidepressants
Benzodiazepines
Gabapentin and pregabalin

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12
Q

Ascites

A

Aldosterone antagonists
Loop diuretics
Colloids (plasma substitutes)

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13
Q

Asthma

A

Antimuscarinic bronchodilators
Beta 2 agonists
Compound (beta 2 agonist-corticosteroid) inhalers
Inhaled corticosteroids (glucocorticoids)

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14
Q

AF and atrial flutter

A

Amiodarone
Aspirin
Beta blockers
Calcium channel blockers
Clopidogrel
Digoxin
Warfarin

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15
Q

Autoimmune disease

A

Aminosalicylates
Systemic corticosteroids (glucocorticoids)
Methotrexate

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16
Q

Benign prostatic hyperplasia

A

Alpha blockers
5 alpha-reductase inhibitors

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17
Q

Bipolar disorder

A

First-generation (typical) antipsychotics
Second-generation (atypical) antipsychotics
Carbamazepine
Valproate

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18
Q

Bone metastases

A

Bisphosphonates

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19
Q

Drugs for bowel preparation

A

Osmotic laxatives

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20
Q

Bradycardia

A

Antimuscarinics

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21
Q

Breathlessness

A

Loop diuretics
Strong opioids

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22
Q

Carbon monoxide poisoning

A

Oxygen

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23
Q

Medications for cardiac arrest

A

Adrenaline (epinephrine)
Amiodarone

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24
Q

Chemotherapy

A

Allopurinol
Systemic corticosteroids (glucocorticoids)
Methotrexate
Serotonin 5-HT3-receptor antagonists antiemetics

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25
Childhood immunisations
Vaccines
26
Chronic kidney disease
Angiotensin receptor blockers ACE inhibitors Calcium and vitamin D
27
Chronic obstructive pulmonary disease
Antimuscarinic bronchodilators Beta 2 agonists Compound (beta 2 agonist-corticosteroid) inhalers Inhaled corticosteroids (glucocorticoids)
28
Things to prescribe for circulatory compromise
Colloids (plasma substitutes) Compound sodium lactate (Hartmann's solution) Sodium chloride
29
Clostridium difficile colitis
Metronidazole Vancomycin
30
Constipation
Bulk-forming laxatives Osmotic laxatives Stimulant laxatives
31
Contrast nephropathy
Acetylcysteine (N-acetylcysteine)
32
Hormonal contraception
Oestrogens and progestogens
33
Deep vein thrombosis
Heparins and fondaparinux Warfarin
34
Dental infection
Metronidazole
35
Depression
SSRI antidepressants Tricyclics antidepressants Venlafaxine and mirtazepine
36
Diabetes mellitus
Insulin Metformin Sulphonylureas Thiazolidinediones
37
Diabetic ketoacidosis
Insulin
38
Diabetic nephropathy
Angiotensin receptor blockers ACE inhibitors
39
Drugs for diarrhoea
Antimotility drugs Bulk-forming laxatives
40
Dry eyes
Ocular lubricants (artificial tears)
41
Dry skin
Emollients
42
Dyspepsia
Alginates and antacids H2 receptor antagonists Proton pump inhibitors
43
Eczema
Topical corticosteroids (glucocorticoids) Emollients
44
Endocarditis
Aminoglycosides Penicillins Penicillinase-resistant penicillin Vancomycin
45
Absence seizures
Valproate
46
Focal seizures
Carbamazepine Gabapentin and pregabalin Phenytoin Valproate
47
Generalised epilepsy
Phenytoin Valproate
48
Medications for status epilepticus
Benzodiazepines Phenytoin
49
Erectile dysfunction
Phosphodiesterase (type 5) inhibitors
50
Faecal impaction
Bulk-forming laxatives Osmotic laxatives Stimulant laxatives
51
Fever
Aspirin Paracetamol
52
6 fluid and electrolyte therapy
Colloids (plasma substitutes) Compound sodium lactate (Hartmann's solution) Glucose (dextrose) IV potassium Oral potassium Sodium chloride
53
Medications for gastro-oesophageal reflux disease
Alginates and antacids H2 receptor antagonists Proton pump inhibitors
54
Generalised anxiety disorder
Venlafaxine and mirtazepine antidepressants Gabapentin and pregabalin
55
Open-angle glaucoma
Prostaglandin analogue eye drops
56
Gout
Allopurinol Non-steroidal anti-inflammatory drugs
57
Hay fever (seasonal allergic rhinitis)
Antihistamines (H1-receptor antagonists)
58
Heart failure
Aldosterone antagonists Angiotensin receptor blockers ACE inhibitors Beta blockers Digoxin Loop diuretics
59
Heart valve replacement
Warfarin
60
Helicobacter pylori eradication
Macrolide Broad-spectrum penicillins Proton pump inhibitors
61
Hepatic encephalopathy
Osmotic laxatives
62
Hormonal replacement therapy
Oestrogens and progestogens
63
Hyperaldosteronism
Aldosterone antagonists
64
Hypercalcaemia of malignancy
Bisphosphonates
65
Hyperglyaemic hyperosmolar syndrome
Insulin
66
Medications for hyperkalaemia
Beta 2 agonists Calcium and vitamin D Glucose (dextrose) Insulin
67
Hyperlipidaemia
Statins
68
Medications for hypertension
Alpha blockers Angiotensin receptor blockers ACE inhibitors Beta blockers Calcium channel blockers Thiazide and thiazide-like diuretics
69
Hyperuricaemia
Allopurinol
70
Hypocalcaemia
Calcium and vitamin D
71
Hypoglycaemia
Glucose (dextrose)
72
Hypokalaemia
Potassium-sparing diuretics IV potassium Oral potassium
73
Hypopituitarism
Systemic corticosteroids (glucocorticoids) Thyroid hormones
74
Hypothyroidism
Thyroid hormones
75
Hypoxaemia
Oxygen
76
Urinary incontinence
Antimuscarinics
77
Complicated infection
Cephalosporins and carbapenems Antipseudomonal penicillins
78
Fungal infection
Antifungal drugs
79
Protozoal infection
Metronidazole
80
Inflammation
Corticosteroids (glucocorticoids) (systemic/inhaled/topical) NSAIDs
81
Insomnia
Benzodiazepines Z-drugs
82
Irritable bowel syndrome
Antimuscarinics
83
Ischaemic heart disease
Angiotensin receptor blockers ACE inhibitors Aspirin Beta blockers Clopidogrel Fibrinolytic drugs Statins
84
Keratoconjunctivitis sicca
Ocular lubricants (artificial tears)
85
Korsakoff's psychosis
Vitamins
86
Leg cramps
Quinine
87
Local anaesthesia
Adrenaline (epinephrine) Lidocaine
88
Lyme disease
Tetracyclines
89
Malaria
Quinine
90
Meningitis
Cephalosporins and carbapenems Penicillins
91
Migraine
Gabapentin and pregabalin
92
Mucosal bleeding
Adrenaline (epinephrine)
93
Myocardial perfusion scan
Dipyridamole
94
Nausea and vomiting
Antiemetics - Dopamine D2-receptor antagonists - Histamine H1-receptor antagonists - Phenothiazines - Serotonin 5-HT3-receptor antagonists First-generation (typical) antipsychotics
95
Prevention of neural tube defects
Vitamins
96
Obsessive compulsive disorder
SSRI antidepressants
97
Ocular hypertension
Prostaglandin analogue eye drops
98
Drugs for oedema
Loop diuretics
99
Opioid toxicity
Naloxone
100
Osteomyelitis
Penicillinase-resistant penicillins Vancomycin
101
Osteoporosis
Bisphosphonates Calcium and vitamin D
102
Overdose
Acetylcysteine (N-acetylcysteine) Activated charcoal
103
Paget's disease
Bisphosphonates
104
Pain
Aspirin NSAIDs Compound preparations opioids Strong opioids Weak opioids Paracetamol
105
Neuropathic pain
Tricyclics and related drugs antidepressants Gabapentin and pregabalin
106
Panic disorders
SSRI antidepressants
107
Paracentesis
Colloids (plasma substitutes)
108
Secondary Parkinsonism
Dopaminergic drugs for Parkinson's disease
109
Parkinson's disease
Dopaminergic drugs for Parkinson's disease
110
Peptic ulcer disease
H2-receptor antagonists Proton pump inhibitors
111
Peripheral arterial disease
Aspirin Clopidogrel
112
Pneumonia
Cephalosporins and carbapenems Macrolides Metronidazole Penicillins Antipseudomonal penicillins Broad-spectrum penicillins Quinolones Tetracyclines
113
Pneumocystis pneumonia
Trimethoprim (as co-trimoxazole)
114
Pneumothorax
Oxygen
115
Poisoning
Acetylcysteine (N-acetylcysteine) Activated charcoal Benzodiazepines Naloxone Oxygen Vitamins
116
Pruritis
Antihistamines (H1-receptor antagonists)
117
Psoriasis
Emollients Methotrexate
118
Pulmonary embolus
Fibrinolytic drugs Heparins and fondaparinux Warfarin
119
Pulmonary hypertension
Phosphodiesterase (type 5) inhibitors
120
Pulmonary oedema
Loop diuretics Nitrates Strong opioids
121
Pyelonephritis
Aminoglycosides
122
Reconstitution and dilution of drugs
Glucose (dextrose) Sodium chloride
123
Respiratory secretions
Acetylcysteine (N-acetylcysteine) Cardiovascular and GI uses antimuscarinics
124
Rheumatoid arthritis
Aminosalicylates Methotrexate
125
Schizophrenia
First-generation (typical) antipsychotics Second-generation (atypical) antipsychotics
126
Sedation
Benzodiazepines
127
Sepsis
Aminoglycosides Cephalosporins and carbapenems Penicillins Antipseudomonal penicillins Vancomycin
128
Intra-abdominal sepsis
Aminoglycosides Metronidazole Antipseudomonal penicillins Broad-spectrum penicillins
129
Septic arthritis
Penicillinase-resistant penicillins
130
Shock
Colloids (plasma substitutes) Compound sodium lactate (Hartmann's solution) Sodium chloride
131
Skin and soft tissue infection
Macrolides Penicillins Antipseudomonal penicillins Penicillinase-resistant penicillins
132
Sjogren's syndrome
Ocular lubricants (artificial tears)
133
Smoking cessation
Nicotine replacement and related drugs
134
Stroke
Aspirin Clopidogrel Dipyridamole Fibrinolytic drugs
135
Subacute combined degeneration of the cord
Vitamins
136
Supraventricular tachycardia
Adenosine Amiodarone Beta blockers Calcium channel blockers
137
Tetanus
Penicillins
138
Thiamine deficiency
Vitamins
139
Tonsilitis
Penicillins
140
Trigeminal neuralgia
Carbamazepine
141
Tumour lysis syndrome
Allopurinol
142
Ulcerative colitis
Aminosalicylates
143
Urinary catheterisation
Lidocaine
144
UTI
Cephalosporins and carbapenems Nitrofurantoin Antipseudomonal penicillins Broad-spectrum penicillins Quinolones Trimethoprim
145
Urticaria
Antihistamines (H1-receptor antagonists)
146
Vaccinations
Vaccines
147
Prophylaxis of venous thromboembolism
Heparins and fondaparinux
148
Treatment of venous thromboembolism
Fibrinolytic drugs Heparins and fondaparinux Warfarin
149
Ventricular fibrillation
Adrenaline (epinephrine) Amiodarone Lidocaine
150
Ventricular tachycardia
Adrenaline (epinephrine) Amiodarone Lidocaine
151
Vitamin D deficiency
Calcium and vitamin D
152
Vitamin K deficiency bleeding
Vitamins
153
Reversal of warfarin
Vitamins
154
Wernicke's encephalopathy
Vitamins
155
Acetylcysteine (N-acetylcysteine)
Antidote for paracetamol poisoning To prevent renal injury due to radiographic contrast material (contrast nephropathy) To reduce viscosity of respiratory secretions (acting as a mucolytic)
156
How does acetylcysteine work as an antidote to paracetamol poisoning?
Paracetamol is metabolised by conjugation with glucuronic acid and sulfate and a small amount is converted to NAPQI (hepatotoxic). This is detoxified by conjugation with glutathione, which is overwhelmed in paracetamol poisoning. Acetylcysteine replenishes the body's supply of glutathione.
157
Activated charcoal
Reduce absorption of certain poisons (including some drugs in overdose) from the gut Increase the elimination of certain poisons
158
Adenosine
Supraventricular tachycardia
159
What are contraindications for adenosine?
Hypotension Coronary ischaemia Decompensated heart failure Asthma COPD
160
Which drug prolongs and potentiates the effect of adenosine?
Dipyridamole
161
Adrenaline (epinephrine)
Cardiac arrest Anaphylaxis Local vasoconstriction, e.g. during endoscopy to control mucosal bleeding or mixed with local anaesthetic drugs to prolong local anaesthesia
162
How does adrenaline work?
Potent agonist of the alpha 1, alpha 2, beta 1 and beta 2 adrenoceptors, and so has many sympathetic effects. * Vasoconstriction of vessels supplying skin, mucosa and abdominal viscera (mainly alpha 1) * Increases in heart rate, force of contraction and myocardial excitability (beta 1) * Vasodilatation of vessels supplying the heart and muscles (beta 2) * Bronchodilatation (beta 2) * Suppression of inflammatory mediator release from mast cells (beta 2)
163
Which drug can cause widespread vasoconstriction when being treated with adrenaline?
Beta blocker Alpha 1 mediated vasoconstricting effect is not opposed by beta 2 mediated vasodilatation
164
What is the presciption of adrenaline in cardiac arrest and anaphylaxis?
Cardiac arrest: 1mg IV after the third shock (or ASAP if not shockable) and repeated every 3-5 minutes thereafter Anaphylaxis: 500ug IM, repeated after 5 minutes if necessary
165
Aldosterone antagonists
Ascites and oedema due to liver cirrhosis (spironolactone) Chronic heart failure Primary hyperaldosteronism
166
How do aldosterone antagonists work?
Inhibit the effect of aldosterone by competitively binding to the aldosterone receptor. This increases sodium and water excretion and potassium retention.
167
Important adverse effects of aldosterone antagonists
Hyperkalaemia, which can lead to muscle weakness, arrhythmias and cardiac arrest Spironolactone causes gynaecomastia
168
What are contraindications of aldosterone antagonists?
Severe renal impairment Hyperkalaemia Addison's disease (who are aldosterone deficient)
169
Alginates and antacids
Gastro-oesophageal reflux disease Dyspepsia
170
How do alginates and antacids work?
Alginates increase the viscosity of the stomach contents, which reduces the reflux of stomach acid into the oesophagus Antacids buffer stomach acids
171
How can alginates and antacids interact with other drugs?
Divalent cations in compound alginates can bind to other drugs, reducing their absorption. Antacids can reduce serum concentrations of other drugs, so the doses should be taken at different times, e.g. ACE inhibitors, some antibiotics, bisphosphonates, digoxin, levothyroxine and proton pump inhibitors. They can also increase the excretion of aspirin and lithium.
172
When should alginates and antacids be taken?
Following meals, before bedtime and/or when symptoms occur
173
Allopurinol
Prevent acute attacks of gout Prevent uric acid and calcium oxalate renal stones Prevent hyperuricaemia and tumour lysis syndrome associated with chemotherapy
174
How does allopurinol work?
Xanthine oxidase inhibitor Xanthine oxidase metabolises xanthine (produced from purines) to uric acid. Inhibition of xanthine oxidase lowers plasma uric acid concentrations and reduces precipitation of uric acid in the joints or kidneys.
175
What are contraindications to allopurinol?
Acute attacks of gout Recurrent skin rash Signs of more severe hypersensitivity
176
Alpha blockers
Benign prostatic hyperplasia Resistant hypertension
177
Alpha blockers
Most drugs in this class are selective for the alpha 1-adrenoceptor, which is found mainly in smooth muscle, including in blood vessels and the urinary tract (the bladder neck and prostate in particular). Blockage induces relaxation, and so vasodilatation and a fall in BP and reduced resistance to bladder outflow.
178
What are some important adverse effects of alpha blockers?
Postural hypotension Dizziness Syncope
179
When should alpha blockers be taken?
At bedtime (to reduce BP lowering effect)
180
Aminoglycosides
Severe infections, particularly those caused by Gram-negative aerobes (including Pseudomonas aeruginosa) * Severe sepsis, including where the source is unidentified * Pyelonephritis and complicated UTI * Biliary and other intra-abdominal sepsis * Endocarditis
181
How do aminoglycosides work?
Bind irreversibly to bacterial ribosomes (30S subunit) and inhibit protein synthesis. They are bactericidal (kill bacteria). Their spectrum of action includes Gram-negative aerobic bacteria, staphylococci and mycobacteria.
182
Why do aminoglycosides only work on certain bacteria?
Enter bacterial cells via an oxygen-dependent transport system. Streptococci and anaerobic bacteria don't have this transport system, so have innate aminoglycoside resistance. Other bacteria acquire resistance through reduced cell membrane permeability to aminoglycosides or acquisition of enzymes that modify aminoglycosides to prevent them from reaching the ribosomes. As penicillins weaken bacterial cell walls, they may enhance aminoglycoside activity by increasing bacterial uptake.
183
What are the most important adverse effects of aminoglycosides?
Nephrotoxicity and ototoxicity They accumulate in renal tubular epithelial cells and cochlear and vestibular hair cells where they trigger apoptosis andcell death. Nephrotoxicity presents as reduced urine output and rising serum creatinine and urea. Ototoxicity may present with hearing loss, tinnitus (cochlear damage) and/or vertigo (vestibular damage).
184
Which groups of people are most susceptible to renal, cochlear and vestibular damage from aminoglycosides? Those with which condition should not take aminoglycosides unless absolutely necessary?
Neonates, elderly and those with renal impairment Myasthenia gravis
185
Aminosalicylates
Ulcerative colitis (mesalazine) Rheumatoid arthritis (sulfasalazine)
186
How do aminosalicylates work?
Release 5-aminosalicylic acid (5-ASA), which has anti-inflammatory and immunosuppressive effects
187
What are adverse effects of aminosalicylates?
GI upset and headache Serious blood abnormalities (e.g. leucopenia, thrombocytopenia) Renal impairment Sulfasalazine can cause decrrease in number of sperm
188
What is a contraindication to aminosalicylates?
Aspirin hypersensitivity (aspirin is a salicylate, too)
189
2 aldosterone antagonists
Spironolactone Epleronone
190
2 alginates and antacids
Gaviscon Peptac
191
3 alpha blockers
Doxazosin Tamsulosin Alfuzosin
192
2 aminoglycosides
Gentamicin Amikacin
193
2 aminosalicylates
Mesalazine Sulfasalazine
194
How can mesalazine be given to someone with ulcerative colitis?
Enema or suppository Oral
195
Amiodarone
Tachyarrhythmias, including AF, atrial flutter, supraventricular tachycardia, ventricular tachycardia and refractory ventricular fibrillation
196
How does amiodarone work?
Many effects on myocardial cells, including blockade of sodium, calcium and potassium channels, and antagonism of alpha- and beta-adrenergic receptors. This reduces spontaneous depolarisation, slows conduction velocity and increases resistace to depolarisation, including in the AV node. By interfering with the AV node conduction, amiodarone reduces the ventricular rate in AF and atrial flutter. It may also increase the chance of conversion to, and maintenanec of, sinus rhythm.
197
What are some adverse effects of taking amiodarone chronically?
Pneumonitis Bradycardia and AV block Hepatitis Photosensitivity and grey discolouration Thyroid abnormalities
198
In patients with which conditions should amiodarone be avoided?
Severe hypotension Heart block Active thyroid disease
199
For which drugs should the dose be halved if amiodarone is started?
Digoxin Diltiazem Verapamil
200
When is amiodarone used in cardiac arrest?
For VF or pulseless VT immediately after the 3rd shock, 300mg IV followed by 20mL of 0.9% sodium chloride or 5% glucose as a flush
201
Angiotensin-converting enzyme inhibitors
Hypertension Chronic heart failure Ischaemic heart disease Diabetic nephropathy and chronic kidney disease with proteinuria
202
How do ACE inhibitors work?
Block the action of ACE, to prevent the conversion of angiotensin 1 to angiotensin 2. Angiotensin 2 is a vasoconstrictor and stimulates aldosterone secretion. Blocking its action reduces peripheral vascular resistance, which lowers BP. It particularly dilates the efferent glomerular arteriole, which reduces intraglomerular pressure and slows the progression of CKD. Reducing the aldosterone level promotes water and sodium excretion, which helps to reduce venous return, which is beneficial in heart failure.
203
What are common adverse effects of ACE inhibitors and ARBs?
Hypotension Persistent dry cough (*!ACE inhibitors only!* increased levels of bradykinin) Hyperkalaemia (lower aldosterone level promotes K+ retention) Renal failure
204
What are contraindications to ACE inhibitors?
Renal artery stenosis or AKI Pregnancy or breastfeeding
205
3 ACE inhibitors
Ramipril Lisinopril Perindopril
206
Angiotensin receptor blockers
When ACE inhibitors are not tolerated due to cough (same indications): * Hypertension * Chronic heart failure * Ischaemic heart disease * Diabetic nephropathy and chronic kidney disease with proteinuria
207
How do ARBs work?
Block the action of angiotensin 2 on the AT1 receptor. Angiotensin 2 is a vasoconstrictor and stimulates aldosterone secretion. Blocking its action reduces peripheral vascular resistance, which lowers BP. It particularly dilates the efferent glomerular arteriole, which reduces intraglomerular pressure and slows the progression of CKD. Reducing aldosterone level promotes water and sodium excretion, which helps to reduce venous return, which is beneficial in heart failure.
208
3 ARBs
Losartan Candesartan Irbesartan
209
Selective serotonin reuptake inhibitors
Moderate-to-severe depression and mild depression if psychological treatments fail Panic disorder Obsessive compulsive disorder
210
How do SSRIs work?
Inhibit neuronal reuptake of serotonin (5-HT) from the synaptic cleft, increasing its availability for neurotransmission
211
Adverse effects of SSRIs
GI upset, appetite and weight disturbance Hypersensitivity reactions, including skin rash Hyponatraemia (confusion and reduced consciousness) Suicidal thoughts and behaviour Lower the seizure threshold, prolong the QT interval and can predispose to arrhythmias Increase risk of bleeding Serotonin syndrome - autonomic hyperactivity, altered mental state and neuromuscular excitation
212
People with which conditions should SSRIs be prescribed with caution?
Epilepsy Peptic ulcer disease
213
4 SSRIs
Citalopram Fluoxetine Sertraline Escitalopram
214
What does a patient starting on antidepressants need to be told?
Symptoms should improve over a few weeks, particularly sleep and appetite Carry on with drug treatment for at least 6 months after they feel better to stop the depression from coming back Don't stop treatment suddenly, as it may cause tummy upset, flu-like symptoms and sleeplessness; instead reduce the dose slowly over 4 weeks
215
Tricyclics and related drugs
Moderate-to-severe depression (where SSRIs are ineffective) Neuropathic pain (not licensed)
216
How do tricyclic antidepressants work?
Inhibit neuronal reuptake of serotonin (5-HT) and noradrenaline from the synaptic cleft, increasing their availability for neurotransmission. Also has extensive adverse effects due to blocking a wide array of receptors, including muscarinic, histamine (H1), alpha-adrenergic and dopamine (D2) receptors.
217
Adverse effects of tricylic antidepressants
Antimuscarinic: dry mouth, constipation, urinary retention and blurred vision H1 and alpha 1 receptors: sedation and hypotension Arrhythmias and ECG changes (prolongation of QT and QRS durations) Convulsions, hallucinations and mania Dopamine receptors: breast changes and sexual dysfunction, and rarely extrapyramidal symptoms (tremor and dyskinesia)
218
Which groups of people are particularly at risk of adverse effects from tricylic antidepressants?
**Elderly** **Cardiovascular** **disease** **Epilepsy** Constipation Prostatic hypertrophy Raised intraocular pressure
219
2 tricyclic antidepressants
Amitriptyline Lofepramine
220
Venlafaxine and mirtazapine
Major depression where SSRIs are ineffective Generalised anxiety disorder (venlafaxine)
221
How does venlafaxine work?
Serotonin and noradrenaline reuptake inhibitor (SNRI), which interferes with uptake of these neurotransmitters from the synaptic cleft. Increase availability of monoamines for neurotransmission. Weak antagonist of muscarinic and histamine (H1) receptors.
222
How does mirtazapine work?
Antagonist of inhibitory pre-synaptic alpha 2-adrenoceptors. Increase availability of monoamines for neurotransmission. Potent antagonist of histamine (H1) but not muscarinic receptors.
223
Adverse effects of venlafaxine and mirtazapine
GI upset (dry mouth, nausea, change in weight, diarrhoea or constipation) CNS effects (headache, abnormal dreams, insomnia, confusion, convulsions) Hyponatraemia Serotonin syndrome Suicidal thoughts and behaviour
224
When should mirtazapine be taken?
At night (sedative)
225
Dopamine D2-receptor antagonists
Prophylaxis and treatment of nausea and vomiting, particulary in the context of reduced gut motility
226
How do dopamine D2-receptor antagonists work?
Dopamine, acting via D2 receptors, is: * The main receptor in the chemoreceptor trigger zone, which is responsible for sensing emetogenic substances in the blood (e.g. drugs) * An important neurotransmitter in the gut, where it promotes relaxation of the stomach and lower oesophageal sphincter and inhibits gastroduodenal coordination. Blocking D2 receptors has a prokinetic effect, promoting gastric emptying (e.g. opioids, diabetic gastroparesis)
227
What are some adverse effects of dopamine D2-receptor antagonists?
Diarrhoea Extrapyramidal symptoms (metoclopramide) - acute dystonic reaction, e.g. oculogyric crisis
228
What are contraindications to dopamine D2-receptor antagonists?
GI obstruction GI perforation Antipsychotics (metoclopramide) Dopaminergic agents for Parkinson's disease (metoclopramide)
229
2 dopamine D2-receptor antagonists
Metoclopramide Domperidone
230
Histamine H1-receptor antagonists
Prophylaxis and treatment of nausea and vomiting, particularly in the context of motion sickness or vertigo
231
How do histamine H1-receptor antagonists work?
Histamine (H1) and acetylcholine (muscarinic) receptors predominate in the vomiting centre and in its communication with the vestibular system.
232
Contraindications to histamine H1-receptor antagonists
Hepatic encephalopathy Prostatic hypertrophy
233
3 histamine H1-receptor antagonists
Cyclizine Cinnarizine Promethazine
234
Phenothiazines
Prophylaxis and treatment of nausea and vomiting in a wide range of conditions, particularly when due to vertigo Psychotic disorders, e.g. schizophrenia
235
How does phenothiazine work?
Blockade of various receptors, including dopamine (D2) receptors in the chemoreceptor trigger zone and gut and, to a lesser extent, histamine (H1) and acetylcholine (muscarinic) receptors in the vomiting centre and vestibular system
236
Adverse effects of phenothiazines
Drowsiness Postural hypotension Extrapyramidal syndromes (D2 receptor blockade) - acute dystonic reaction (e.g. oculogyric crisis), tardive dyskinesia QT interval prolongation
237
What are contraindications to phenothiazines?
Severe liver disease Prostatic hypertrophy
238
2 phenothiazines
Prochlorperazine Chlorpromazine
239
Serotonin 5-HT3-receptor antagonists
Prophylaxis and treatment of nausea and vomiting, particularly in the context of general anaesthesia and chemotherapy
240
How do serotonin 5-HT3-receptor antagonists work?
High density of 5-HT3 receptors in chemoreceptor trigger zone Serotonin is the key neurotransmitter released by the gut in response to emetogenic stimuli. Acting on 5-HT3 receptors, it stimulates the vagus nerve, which activates the vomiting centre via the solitary tract nucleus.
241
2 serotonin 5-HT3-receptor antagonists
Ondansetron Granisetron
242
Antifungal drugs
Treatment of local fungal infections, including of the oropharynx, vagina or skin Systemic treatment of invasive or disseminated fungal infections
243
How do antifungal drugs work?
Polyene antifungals (nystatin) bind to ergosterol in fungal cell membranes, creating a polar pore which allows intracellular ions to leak out of the cell, which kills or slows the growth of the fungi. Imidazole (clotrimazole) and triazole (fluconazole) antifungals inhibit ergosterol synthesis, impairing cell membrane synthesis, cell growth and replication.
244
Adverse effects to fluconazole
GI upset (nausea, vomiting, diarrhoea, abdominal pain) Headache Hepatitis Hypersensitivity (skin rash, cutaneous reactions, anaphylaxis) Severe hepatic toxicity Prolonged QT interval (arrhythmias)
245
Contraindications to fluconazole
Pregnancy
246
Antihistamines (H1-receptor antagonists)
Allergies, particularly hay fever Aid relief of itchiness (pruritis) and hives (urticaria) due, for example, to insect bites, infections (chickenpox) and drug allergies Adjunctive treatment in anaphylaxis, after administratno of adrenaline and other life-saving measures
247
3 antifungals
Nystatin Clotrimazole Fluconazole
248
How do H1-receptor antagonists work?
Histamine is released from storage granules in mast cells as a result of antigen binding to IgE on the cell surfaces. Mainly via H1 receptors, histamine induces features of immediate type 1 hypersensitivity: increased capillary permeability casing oedema formation, vasodilatation causing erythema and itch due to sensory nerve stimulation. When histamine is released in the nasopharynx, as in hay fever, it causes nasal irritation, sneezing, rhinorrhoea, congestion, conjunctivitis and tich. In the skin, it cause urticaria. Widespread histamine release, as in anaphylaxis, produces generalised vasodilatation and vascular leakage, with consequent hypotension. Antihistamine blocks the H1 receptor.
249
H1-receptor antagonists
Cetirizine Loratadine Fexofenadine Chlorphenamine
250
Antimotility drugs
Diarrhoea, usually in the context of irritable bowel syndrome or viral gastroenteritis
251
How do opioids work as antimotility drugs?
Agonist of opioid u-receptors in the GI tract, which increases non-propulsive contractions of the gut smooth muscle, but reduces propulsive (peristaltic) contractions. As a result, transit of bowel contents is slowed and anal sphincter tone is increased. Slower gut transit allows more time for water absorption, which hardens the stool.
252
Contraindications of loperamide
Acute ulcerative colitis (inhibition of peristalsis increases risk of megacolon and perforation) Clostridium difficile colitis Acute bloody diarrhoea
253
Antimotility drugs
Loperamide Codeine phosphate
254
Antimuscarinic bronchodilators
Chronic obstructive pulmonary disease Asthma
255
How do antimuscarinic bronchodilators work?
Bind to muscarinic receptor, where they act as a competitive inhibitor of acetylcholine. Blocking the receptor reduces smooth muscle tone (including in the respiratoy tract) and reduces secretions from glands in the respiratory and GI tract.
256
Which condition do antimuscarinics need to be used with caution?
Angle-closure glaucoma Arrhythmias
257
3 antimuscarinic bronchodilators
Ipratropium Tiotropium Glycopyrronium
258
Antimuscarinics for CV and GI uses
Severe or symptomatic bradycardia (atropine) Irritiable bowel syndrome (hyoscine butylbromide) Reducing copious respiratory secretions (hyoscine butylbromide)
259
How do antimuscarinics work CV and GI?
Bind to muscarinic receptors, where they act as competitive inhibitor of acetylcholine. Blocking the receptor results in increased heart rate and conduction, reduced smooth muscle tone and peristaltic contraction (including in the gut and urinary tract) and reduce secretions from glands in the respiratory tract and gut.
260
Adverse effects of antimuscarinics
Tachycardia Dry mouth Constipation Urinary retention in those with BPH Blurred vision
261
Antimuscarinic for GI and CV symptoms
Atropine Hyoscine butylbromide Glycopyrronium
262
Antimuscarinics for GU use
Reduce urinary frequency, urgency and urinary incontinence in overactive bladder
263
How do antimuscarinics work GU?
Bind to muscarinic receptors, where they act as competitive inhibitor of acetylcholine. Contraction of the smooth muscle of the bladder is under parasympathetic control. Blocking muscarinic receptors promotes bladder relaxation, increasing bladder capacity. Relatively selective for the M3 receptor.
264
Contraindication to antimuscarinics GU
UTI
265
3 antimuscarinics GU
Oxybutynin Tolterodine Solifenacin
266
First-generation (typical) antipsychotics
Urgent treatment of severe psychomotor agitation that is causing dangerous or violent behaviour, or to calm patient to permit assessment Schizophrenia Bipolar disorder, particularly in acute episodes of mania or hypomania Nause and vomiting, particularly in palliative care setting
267
How do typical antipsychotics (FGA) work?
Block the post-synaptic dopamine D2 receptors. D2 blockade of the mesolimbic/mesocortical pathway between the midbrain and limbic system/frontal cortex. D2 receptors also found in chemoreceptor trigger zone, where blockade accounts for their use in nausea and vomiting.
268
Adverse effects of antipsychotics
Extrapyramidal effects (D2 blockade in nigrostriatal pathway) - acute dystonic reactions (involuntary parkinsonian movements or muscle spasms), akathisia (state of internal restlessness) and neuroleptic malinancy syndrome (rigidity, confusion, autonomic dysregulation, pyrexia), tardive dyskinesia Drowsiness Hypotension QT prolongation (arrhythmias) Erectile dysfunction Hyperprolactinaemia (tuberohypophyseal D1 blockade) - menstrual disturbance, galactorrhoea, breast pain
269
3 first generation (typical) antipsychotics
Haloperidol Chlorpromazine Prochlorperazine
270
Ways of administering typical antipsychotics
Orally (tablet and liquid) Slow-release IM ('depot') injection Rapid-acting IM injection (haloperidol) IV (haloperidol)
271
Who do you need to be careful with when prescribing antipsychotics?
Elderly Dementia Parkinson's disease
272
Second-generation (atypical) antipsychotics
Urgent treatment of severe psychomotor agitation that is causing dangerous or violent behaviour, or to calm patient to permit assessment Schizophrenia, particularly when extrapyramidal SEs have complicated the use of typical antipsychotics or negative symptoms are prominent Bipolar disorder, particularly in acute episodes of mania or hypomania
273
Why can second-generation (atypical) antipsychotics be considered better than typical?
Improved efficacy in 'treatment-resistant' schizophrenia and against negative symptoms (higher affinity for other receptors, particularly 5-HT2A receptors) Lower risk of extrapyramidal symptoms (looser binding to the D2 receptors)
274
What is a common problem with second-generation (atypical) antipsychotics?
Metabolic disturbance - weight gain, DM, lipid changes
275
What are 2 rare adverse effects of clozapine?
Agranulocytosis (severe deficiency of neutrophils) Myocarditis
276
Who must not be given clozapine?
Severe heart disease History of neutropenia
277
4 second-generation (atypical) antipsychotics
Quetiapine Olanzapine Risperidone Clozapine
278
Aspirin
Acute coronary syndrome and acute ischaemic stroke Long-term secondary prevention of thrombotic arterial events in those with cardiovascular, cerebrovascular and peripheral arterial disease Reduce the risk of intracardiac thrombus and embolic stroke in AF where warfarin and novel oral anticoagulants are contraindicated Mild-to-moderate pain and fever
279
How does aspirin work?
Irreversibly inhibits cyclooxygenase (COX) to reduce production of the pro-aggregatory factor thromboxane from arachidonic acid, reducing platelet aggregation and the risk of arterial occlusion
280
Adverse effects of aspirin
GI irritation GI ulceration and haemorrhage Hypersensitivity reactions (bronchospasm)
281
Who should not be given aspirin?
Children under 16 (Reye's syndrome) Aspirin hypersensitivity Third trimester of pregnancy (premature closure of ductus arteriosus)
282
How does the dose of aspirin change when given for acute coronary syndrome vs acute ischaemic stroke vs long-term prevention of thrombosis?
ACS: once-only loading dose of 300mg followed by a regular dose of 75mg daily Acute ischaemic stroke: aspirin 300mg daily for 2 weeks before switching to 75mg daily Prevention of thrombosis: low-dose aspirin 75mg daily
283
When taking low-dose aspirin, what additional medication should be considered in those at risk of GI complications?
Proton pump inhibitor, e.g. omeprazole 20mg daily
284
When should aspirin be taen?
After food
285
Benzodiazepines
Seizures and status epilepticus Alcohol withdrawal reactions Sedation for interventional procedures Short-term treatment of severe, disabling or distressing anxiety or insomnia
286
How do benzodiazepines work?
Facilitate and enhance binding of GABA to GABAA receptor. Depressant effect on synaptic transmission, resulting in reduced anxiety, sleepiness, sedation and anticonxulsive effects.
287
Who should avoid benzodiazepines?
Respiratory impairment Neuromuscular disease, e.g. myasthenia gravis Liver failure (hepatic encephalopathy)
288
5 benzodiazepines
Diazepam Temazepam Lorazepam Chlordiazepoxide Midazolam
289
Which benzodiazepine is recommended for seizures and why?
Lorazepam (initial dose 4mg IV) or diazepam (10mg IV or rectally) Long-acting
290
Beta2-agonists
Asthma: short-acting to relieve breathlessness and long-acting as step 3 treatment for chronic asthma COPD: short-acting to relieve breathlessness and long-acting as an option for second-line therapy Hyperkalaemia (nebulised)
291
How do beta2-agonists work?
Beta2 receptors are found in smooth muscle of the bronchi, GI tract, uterus and blood vessels. Stimulation of this G protein-coupled receptor activates a signalling cascade that leads to smooth muscle relaxation. This improves airflow in constricted airways, reducing the symptoms of breathlessness. Also stimulate Na+/K+-ATPase pumps on cell surface membranes, causing a shift of K+ from extracellular to intracellular compartment.
292
2 short-acting beta2-agonists
Salbutamol Terbutaline
293
2 long-acting beta2-agonists
Salmeterol Formoterol
294
Adverse effects of beta2-agonists
Fight or flight * Tachycardia * Palpitations * Anxiety * Tremor Promote glycogenolysis > increased serum glucose Muscle cramps
295
Use of what can help improve airway deposition and treatment efficacy of inhaled medication?
Spacer with metered dose inhalers
296
Beta blockers
Ischaemic heart disease (angina and acute coronary syndrome) Chronic heart failure AF Supraventricular tachycardia Hypertension
297
How do beta blockers work?
Beta1-adrenoreceptors are located mainly in the heart and beta2-adrenoreceptors are found mainly in smooth muscle of blood vessels and the airways. Beta blockers reduce force of contraction and speed of conduction in the heart, relieving myocardial ischaemia by reducing cardiac work and oxygen demand and increasing myocardial perfusion. Slow the ventricular rate in AF by prolonging the refractory period of the AV node. Lower BP in a variety of ways, including reducing renin secretion from the kidney.
298
Adverse effects of beta blockers
Fatigue Cold extremities Headache GI disturbance, e.g. nausea Sleep disturbance and nightmares Impotence
299
Who should not have beta blockers?
Asthma Non-dihydropyridine calcium channel blockers, e.g. verapamil, diltiazem Haemodynamic instability Heart block
300
4 beta blockers
Bisoprolol Atenolol Propranolol Metoprolol
301
Bisphosphonates
Osteoporotic fragility fractures (alendronic acid) Severe hypercalcaemia of malignancy (pamidronate and zoledronic acid) Myeloma and breast cancer with bone metastases (pamidronate and zoledronic acid) Metabolically-active Paget's disease
302
How do bisphosphonates work?
Reduce bone turnover by inhibiting the action of osteoclasts, the cells responsible for bone resorption. As bone is resorbed, bisphosphonates accumulate in osteoclasts, where they inhibit activity and promote apoptosis, resulting in reduction in bone loss and improvement in bone mass.
303
Adverse effects of bisphosphonates
Oesophagitis (when taken orally) Hypophosphataemia Osteonecrosis of the jaw Atypical femoral fracture
304
Who cannot have bisphosphonates?
Severe renal impairment Hypocalcaemia Upper GI disorders (oral administration only)
305
3 bisphosphonates
Alendronic acid Disodium pamidronate Zoledronic acid
306
How should alendronic acid be taken
Swallowed whole At least 30 minutes before breakfast or other medications With plenty of water Remain upright for 30 minutes after taking (reduce oesophageal irritation)
307
Calcium and vitamin D
Osteoporosis (Ca + vit D) Chronic kidney disease (secondary hyperparathyroidism and renal osteodystrophy) (Ca + vit D) Severe hyperkalaemia to prevent life-threatening arrhythmias (Ca) Hypocalcaemia that is symptomatic (e.g. paraesthesia, tetany, seizures) or severe (Ca) Vitamin D deficiency, including for rickets and osteomalacia (vit D)
308
4 calcium and vit D
Calcium carbonate Calcium gluconate Colecalciferol Alfacalcidol
309
Calcium channel blockers
Hypertension (amlodipine, nifedipine) Stable angina Supraventricular arrhythmais (diltiazem, verapamil)
310
How do calcium channel blockers work?
Decrease Ca entry into vascular and cardiac cells, reducing intracellular calcium concentration. This causes relaxation and vasodilation in arterial smooth muscle, lowering arterial pressure. Reduce myocardial contractility. Suppress cardiac conduction, particularly across the AV node, slowing ventricular rate.
311
What are the 2 types of calcium channel blockers and how do they differ?
Dihydropyridines (amlodipine, nifedipine): relatively selective for vasculature Non-dihydropyridines: more cardioselective
312
Adverse effects of amlodipine and nifedipine
Ankle swelling Flushing Headache Palpitations
313
Adverse effects of verapamil
Constipation Bradycardia Heart block Cardiac failure
314
4 calcium channel blockers
Amlodipine Nifedipine Diltiazem Verapamil
315
Carbamazepine
Epilepsy, for focal seizures and primary generalised seizures Trigeminal neuralgia Bipolar disorder, as an option for prophylaxis in those resistant or intolerant of other medication
316
Adverse effects of carbamazepine
GI upset (nausea and vomiting) Neurological effects (dizziness and ataxia) Oedema Hyponatraemia Hypersensitvity (mild maculopapular skin rash) Antiepileptic hypersensitivity syndrome (severe skin reactions, fever, lymphadenopathy, systemic involvement and 10% mortality)
317
Who should not have carbamazepine?
Antiepileptic hypersensitivity syndrome Pregnancy
318
Cephalosporins and carbapenems
Urinary and respiratory tract infections (oral cephalosporins) Treatment of infections that are very severe or complicated, or caused by antibiotic-resistant organisms (IV cephalosporins and carbapenems)
319
How do cephalosporins and carbapenems work?
Beta-lactam ring. During bacterial cell growth, they inhibit enzymes responsible for cross-linking peptidoglycans in bacterial cell walls, which weakens cell walls, preventing them from maintaining an osmotic gradient, resulting in bacterial cell swelling, lysis and death.
320
Which antibiotic is more resistant to beta-lactamases and why?
Cephalosporins and carbapenems due to fusion of the beta-lactam ring with a dihydrothiazine ring (cephalosporins) or hydroxyethyl side chain (carbapenems)
321
Adverse effects of cephalosporins and carbapenems
GI upset (nausea and diarrhoea) Antibiotic-associated colitis Hypersensitivity CNS toxicity (seizures)
322
2 cephalosporins
Cefalexin Cefotaxime
323
2 carbapenems
Meropenem Ertapenem
324
How can cephalosporins be administered vs carbapenems?
Cephalosporins: orally (tablets, capsules, suspension), injection (IV, bolus injection, infusion), IM Carbapenems: IV injection or infusion
325
Clopidogrel
Generally prescribed with aspirin * Acute coronary syndrome * Prevent occlusion of coronary artery stents * Long-term secondary prevention of thrombotic arterial events in those with cardiovascular, cerebrovascular and peripheral arterial disease * Reduce the risk of intracardiac thrombus and embolic stroke in AF where warfarin and novel oral anticoagulants are contraindicated
326
How does clopidogrel work?
Prevents platelet aggregation and reduces the risk of arterial occlusion by binding irreversibly to adenosine diphosphate (ADP) receptors (P2Y12 subtype) on the surface of platelets
327
Adverse effects of clopidogrel
Bleeding GI upset (dyspepsia, abdominal pain, diarrhoea) Thrombocytopenia
328
Who shouldn't be prescribed clopidogrel?
Active bleeding 7 days before elective surgery and other procedures
329
Compound (beta2-agonist-corticosteroid) inhalers
Asthma: control of symptoms and prevention of exacerbations COPD: control of symptoms and prevention of exacerbations
330
How do compound inhalers work?
Inhaled corticosteroid suppresses airway inflammation Long-acting beta2-agonist (LABA) stimulates bronchodilation
331
2 compound inhalers
Seretide Symbicort
332
What advice can be given to patients taking compound inhalers to avoid sore mouth and hoarse voice?
Rinse mouth and gargle after taking inhaler
333
Systemic corticosteroids (glucocorticoids)
Allergic or inflammatory disorders, e.g. anaphylaxis and asthma Suppression of autoimmune disease, e.g. inflammatory bowel disease and inflammatory arthritis Treatment of some cancers as part of chemotherapy or to reduce tumour-associated swelling Hormone replacement in adrenal insufficiency or hypopituitarism
334
How do systemic corticosteroids work?
Mainly glucocorticoid effects. Bind to cytosolic glucocorticoid receptors, which then translocate to the nucleus and bind to glucocorticoid-response elements, which regulate gene suppression. Upregulate anti-inflammatory genes and downregulate pro-inflammatory genes (cytokines, tumour necrosis factor alpha). Direct actions on inflammatory cells: suppression of circulating monocytes and eosinophils. Metabolic effects: increase gluconeogenesis from increased circulating amino and fatty acids, released by catabolism of muscle and fat. Mineralocorticoid effects: Na+ and water retention and L+ excretion in the renal tubule.
335
Adverse effects of systemic corticosteroids
Infection DM Osteoporosis Proximal muscle weakness Skin thinning with easy bruising Gastritis Mood and behavioural changes: insomnia, confusion, psychosis and suicidal ideas Addisonian crisis (If withdrawn suddenly) Mineralocorticoid actions: HTN, hypokalaemia and oedema
336
3 systemic corticosteroids
Prednisolone Hydrocortisone Dexamethasone
337
Inhaled corticosteroids (glucocorticoids)
Asthma COPD
338
How do inhaled corticosteroids work for asthma and COPD?
Pass through the plasma membrane and interact with receptors in the cytopmas. Activated receptor passes into the nucleus to modify the transciption of a large number of genes. Pro-inflammatory interleukins, cytokines and chemokines are downregulated, while anti-inflammatory proteins are upregulated. In the airways, this reduces mucosal inflammation, widens the airways and reduces mucus secretion.
339
Adverse effects of inhaled corticosteroids
Oral candidiasis Hoarse voice
340
3 inhaled corticosteroids
Beclometasone Budesonide Fluticasone
341
Topical corticosteroids (glucocorticoids)
Inflammatory skin conditions, e.g. eczema
342
2 topical corticosteroids
Hydrocortisone Betamethasone
343
Digoxin
AF and atrial flutter Severe heart failure
344
How does digoxin work?
Negatively chronotropic (reduces heart rate) and positively inotropic (increases force of contraction). Indirect pathway increases vagal (parasympathetic) tone, reducing conduction at the AV node, preventing some impulses from being transmitted to the ventricles, thereby reducing the ventricular rate. Direct effect on myocytes through inhibition of Na+/K+-ATPase pumps, causing Na+ to accumulate in the cell. As cellular extrusion of Ca requires low intracellular Na concentrations, elevation of intracellular Na causes Ca to accumulate in the cell, increasin contractile force.
345
Adverse effects of digoxin
Bradycardia GI disturbance Rash Dizziness Visual disturbance (blurred or yellow vision)
346
What are contraindications to digoxin?
Second-degree heart blok and intermittent complete heart block Ventricular arrhythmias
347
Dipyridamole
Cerebrovascular disease (TIA or ischaemic stroke), for secondary prevention of stroke Induce tachycardia during a myocardial perfusion scan in the diagnosis of ischaemic heart disease
348
How does dipyridamole work?
Antiplatelet and vasodilatory effects. Inrease in intra-platelet cyclic adenosine monophosphate (cAMP) that inhibits platelet aggregation, reducing the risk of artieral occlusion. Blocks cellular uptake of adenosine, prolonging its effect on blood vessels to produce vasodilation.
349
Loop diuretics
Relief of breathlessness in acute pulmonary oedema Symptomatic treatment of fluid overload in chronic heart failure Symptomatic treatment of fluid overload in other oedematous states, e.g. due to renal disease or liver failure
350
How do loop diuretics work?
Act principally on the ascending limb of the loop of Henle, where they inhibit the Na/K/2Cl co-transporter, which is responsible for transporting Na, K and Cl ions from the tubular lumen into the epithelial cell, and so water then follows by osmosis. Inhibiting this has a potent diuretic effect. Direct effect on blood vessels, causing dilatation of capacitance veins.
351
Adverse effects of loop diuretics
Dehydration Hypotension Low electrolyte state
352
What are contraindications to loop diuretics?
Hypovolaemia Dehydration
353
2 loop diuretics
Furosemide Bumetanide
354
Potassium-sparing diuretics
Hypokalaemia arising from loop- or thiazide-diuretic therapy
355
How do potassium-sparing diuretics work?
Weak diuretics. Counteract potassium loss and enhance diuresis when combined with another diuretic. Acts on distal convoluted tubules in the kidney. Inhibits the reabsorption of Na and therefore water by epithelial sodium channels, leading to sodium and water excretion and retention of potassium.
356
Who should not take potassium-sparing diuretics?
Severe renal impairment Hyperkalaemia K supplements Aldosterone antagonists
357
1 potassium-sparing diuretic
Amiloride
358
Thiazide and thiazide-like diuretics
Hypertension
359
How do thiazide diuretics work?
Inhibit the Na/Cl co-transporter in the distal convoluted tubule of the nephron. This prevents reabsorption of sodium and its osmotically associated water. The resulting diuresis causes an initial fall in extracellular fluid volume. Vasodilatation.
360
Adverse effects of thiazide diuretics
Hyponatraemia Hypokalaemia (arrhythmias)
361
3 thiazide (and thiazide-like) diuretics
Bendroflumethiazide Indapamide Chlortalidone
362
Dopaminergic drugs
Early Parkinson's disease Later Parkinson's disease Secondary parkinsonism
363
How do dopaminergic drugs work?
Precursor of dopamine that can enter the brain via a membrane transporter
364
Adverse effects of dopaminergic drugs
Nausea Drowsiness Confusion Hallucinations Hypotension Dyskinesia (excessive and involuntary movement)
365
3 dopaminergic drugs
Levodopa Ropinirole Pramipexol
366
What is important about the administration of Parkinson's medications?
Taken at the right time, to produce the best symptom control
367
Emollients
Topical treatment for all dry or scaling skin disorders
368
How do emollients work?
Replace water content in dry skin. Contain oils or paraffin-based products that help to soften the skin and can reduce water loss by protecting against evaporation from the skin surface.
369
2 emollients
Aqueous cream Liquid paraffin
370
Fibrinolytic drugs
Acute ischaemic stroke (alteplase) Acute STEMI (alteplase, streptokinase) Massive PE with haemodynamc instability
371
How do fibrinolytic drugs work?
Catalyse the conversion of plasminogen to plasma, which acts to dissolve fibrinous clots and re-canalise occluded vessels. This allows reperfusion of affected tissue, preventing or limiting tissue infarction and cell death.
372
Adverse effects of fibrinolytic drugs
Nause and vomiting Bruising Hypotension Serious bleeding Allergic reaction Cardiogenic shock Cardiac arrest Cerebral oedema (brain infarction) Arrhythmia (heart infarction)
373
What are contraindications to fibrinolytic drugs?
Bleeding: recent haemorrhage, recent trauma or surgery Bleeding disorders Severe hypertension Peptic ulcers Previous streptokinase treatment
374
2 fibrinolytic drugs
Alteplase Streptokinase
375
Gabapentin and pregabalin
Focal epilepsies Neuropathic pain (pregabalin) Migraine prophylaxis (gabapentin) Generalised anxiety disorder (pregabalin)
376
How does gabapentin and pregabalin work?
Binds with voltage-sensitive Ca channels, where it prevents the inflow of Ca and inhibits neurotransmitter release. This interferes with synaptic transmission and reduces neuronal excitability.
377
H2-receptor antagonists
Peptic ulcer disease GORD and dyspepsia
378
How do H2-receptor antagonists work?
Reduce gastric acid secretion. Histamine is released by local pararine cells and binds to H2-receptors on the gastric parietal cell. Via a second-messenger system, this activates the proton pump. Blocking the H2-receptors therefore reduces acid secretion.
379
1 H2-receptor antagonist
Ranitidine
380
Heparins and fondaparinux
Venous thromboembolism: DVT and PE Acute coronary syndrome
381
How do heparins and fondaparinux work?
Thrombin and factor Xa are key components of the final common coagulation pathway that leads to formation of a fibrin clot. By inhibiting their function, they prevent the formation and propagation of blood clots. Unfractionated heparin activates antithrombin, which inactivates clotting factor Xa and thrombin. LMWH preferentially inhibit factor Xa. Fondaparinux inhibits factor Xa only.
382
In which patients should anticoagulants be used cautiously?
Clotting disorders Severe uncontrolled hypertension Recent surgery or trauma Invasive procedures (lumbar puncture, spinal anaesthesia)
383
3 heparins
Enoxaparin Dalteparin Unfractionated heparin
384
Insulin
Type 1 and 2 DM Diabetic emergencies (DKA, hyperglycaemia hyperosmolar syndrome) (IV) Perioperative glycaemic control in selected DM patients Hyperkalaemia
385