Pharmacology Flashcards

1
Q

Ramipril - class and mechanism

A
  • ACEi = enalapril, lisinopril, captopril
  • Competitive inhibitor
  • Inhibits synthesis of AG2 which is a vasoconstrictor
  • Therefore = vascular smooth muscle relaxation and vasodilation
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2
Q

ACEi - dose

A
  • initially 1.25 - 2.5mg once daily for HTN
  • Can be increased to 10mg a day
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3
Q

ACEi SE and contraindications

A
  • SE = persistent dry cough, hyperkalaemia, renal failure
  • CI = caution if on diuretics or renal impairment, pregnancy
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4
Q

ACEI monitoring

A
  • renal function and electrolytes before starting and during treatment
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5
Q

BB - examples and mechanism

A
  • Bisoprolol, atenolol, metoprolol
  • target beta adrenoreceptors in heart, peripheral vasculature, bronchi
  • Competitive antagonist
  • Inhibits binding of normal ligand noradrenaline released from sympathetic adrenergic neurons –> inhibits activation of adenylyl cyclase enzymes –> reduced CAMP
    –> reduced intracellular Ca
  • Reduced contractility, reduced heart rate
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6
Q

BB dose

A
  • Angina = 5mg OD up to 10
  • HF = 1.25 and increase
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7
Q

BB SE + contraindications + monitoring

A
  • SE = dizziness, fatigue, impotence
  • CI = COPD, asthma, DM, heart block
  • Probably not in preg and BF
  • Monitor lung function in COPD
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8
Q

CCB examples and mechanism

A
  • amlodipine, felodipine, lercanidipine, nidefipine
  • Antagonist
  • Inhibits influx of ca into vascular smooth muscle cells through L type Ca channels
  • Therefore decreased arterial smooth muscle contractility –> vasodilation
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9
Q

CCB dose

A
  • Initially 5mg OD and increase to 10mg
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10
Q

CCB SE and contraindications

A
  • CI = cardiogenic shock, aortic stenosis, unstable angina
  • SE = abdo pain, dizzy
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11
Q

ARB examples and mechanism

A
  • Candesartan, losartan, valsartan
  • Competitive antagonist
  • Selective inhibition of potent vasoconstrictor peptide angiotensin 2
  • Vascular smooth muscle and vasodilation
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12
Q

ARB dose

A

Candesartan = start 4mg, maintenance 8-32mg
Losartan = 50mg OD

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13
Q

ARB SE and CI

A
  • Hypotension
  • CI = aortic of mitral stenosis
  • No in pregnancy or BF
  • Monitor renal function
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14
Q

Aspirin mechanism of action

A
  • Targets cyclooxygenase enzymes
  • Irreversible inhibitor
  • Impairs synthesis of thromboxane A2 and prostacyclin within platelets
  • Therefore reduces platelet aggregation
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15
Q

Aspirin dose

A

75mg for secondary prevention

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16
Q

Aspirin SE and CI

A
  • CI = peptic ulcer, bleeding disorders, under 16s, haemophilia, asthma
  • SE = GI irritation, ulceration and bleeding, bronchospasm
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17
Q

Clopidogrel mechanism of action

A
  • ADP receptor pathway inhibitors
  • Irreversible inhibitor of ADP receptor
  • Inhibits binding of ADP to platelet receptor –> inhibits platelet aggregation
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18
Q

Clopidogrel dose

A

75mg for prevention
ACS = 300-600mg loading dose

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19
Q

Clopidogrel SE and CI

A
  • CI = active bleeding, caution in hepatic and renal impairment
  • Avoid in pregnancy
  • SE = GI discomfort
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20
Q

Statin mechanism of action

A
  • HMG co-enzyme A reductase inhibitors
  • Competitive inhibitor
  • inhibition if HMG co-enzyme A reductase reduces hepatic cholesterol synthesis through mevalonate pathway
  • Upregulation of LDL receptor and increased hepatic removal of LDL from circulation
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21
Q

Statins dose

A

10mg OD and can increase to 80

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22
Q

Statins monitoring, SE and CI

A
  • CI = caution if myositis/rhabdomyolysis or liver disease
  • No in pregnancy
  • SE = arthralgia, GI
  • Monitoring = lipid profiles, LFTs, CK
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23
Q

LMWH examples and mechanism of action

A
  • Enoxaparin, dalteparin, tinzaparin
  • Inhibit factor Xa which is needed to convert prothrombin to thrombin, therefore coagulation inhibited
  • DOAC = anticoagulant
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24
Q

LMWH dose

A
  • VTE pregnancy = 40-100mg 2X
  • DVT prophylaxis = 20mg - 40mg
  • DVT/PE tx = 1.5mg/kg every 24hrs
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25
LMWH SE and CI
- CI = endocarditis, trauma, renal impairement, haemorrhagic disorders - SE = haemorrhage, thrombocytopenia
26
What can happen when restarthing levothyroxine after a cessation?
- CO suddenly increases - Angina, palpitations, SOB, HF - So should be reinitiated at a low dose and gradually increased
27
NSAID examples and mechanism
- ibuprofen, naproxen, diclofenac - Target cox-2 enzymes and cox-1 isoform also affected - Inhibit cix-mediated conversion of arachidonic acid to prostaglandins and thromboxanes = vasodilation, oedema, pain
28
NSAID dose
- Ibuprofen = 300-400mg 3-4 times a day - Naproxen = 0.5-1g daily in rheumatic
29
NSAID SE and CI
- Gastric irritation, ulceration and bleeding - Compromised renal blood flow - Caution in asthma
30
Paracetamol mechanism of action
inhibits synthesis of prostaglandins from arachidonic acid = cox3 enzyme - peripherally blocks generation of pain impulses, reduced central pain signalling
31
paracetamol dose
0.5-1g every 4-6 hours, max 4g daily
32
PPI examples and mechanism of action
- lansoprazole, pantoprazole, omeprazole - target H K ATPase pump at the secretory surface of gastric parietal cells - Irreversible inhibitor = inhibits final transport of hydrogen ions into gastric lumen
33
PPI dose
- 20-40mg
34
PPI SE and CI
- GI disturbance - rebound acid hypersecretion - if red flags rule out GI malignancy before prescribing
35
Antiplatelet examples and mechanism of action
- Clopidogrel, prasugrel - inhibits binding of adp to platelet receptor therefore prevents platelet aggregation
36
Antiplatelet dose
- secomdary prevention 75mg - loading dose for MI 300mg
37
Antiplatelet SE and CI
- GI disturbance - not in pregnancy - caution in hepatic and renal impairment
38
Loop diuretics examples and mechanism of action
- furosemide, bumetanide - competitive inhibitor at the chloride binding site of the symporter - prevents transport of sodium from the lumen of loop of henle = diuresis
39
Loop diuretic dose
- 20-40mg for oedema - 80mg for resistant htn
40
Loop diuretic se and ci
- postural hypotension, electrolyte disturbances = hypok - caution in hypovolaemia - avoid in anuria, hypona/k
41
K sparing diuretics and mechanism of action
- spironalacton and epleronone - competitive antagonist targets intracellular aldosterone receptors in renal tubules
42
K sparing dose
- HF = 25-50mg - ascites = 50BD - 200BD
43
K sparing SE and CI
- GI upset, hyperk - avoid in addisons
44
Thiazide diuretic SE and CI
- hypokalaemia - hyponatraemia - hypercalcaemia and glycaemia - gout - avoid in addisons
45
thiazide diuretics examples and MoA
- bendroflumethiazide, indapamide - inhibitor, targets Na Cl symporter in DCT, inhibits NaCl reabsorption therefore reduce BV and rpessure
46
thiazide diuretic dose
- Bendro = 5-10mg for oedema, 2.5 for HTN
47
aminosalicylates examples and MoA
- mesalazine, sulfasalazine - inhibits prostaglandin production = reduces colonic inflammation
48
SE and dose for mesalazine
- GI upset - 1.2 - 4.8g until remission then 2.4g
49
SSRI exmaples and MoA
- fluoxetine, sertraline, citalopram - prevents re-uptake of serotonin from cleft = prolonged serotonin = prolonged neuronal activity
50
SSRI SE and CI
- GI upset - anorexia - Bleeding - NMS - CI = epilepsy, DM, pregnancy, mania
51
Sertraline dose
- 50mg OD then increase in 50mg to max 200
52
TCA examples and MoA
- amitryptilline, nortryptilline - increased presence of serotonin and noradrenaline in cleft
53
amitriptyline dose
- 75mg daily starting dose - 150-200mg
54
amitryptilline SE and CI
- antimuscarinic, weight gain, abdo pain - cardiotoxic in overdose - CI = hepatic, elderly, suicude risk, epilepsy
55
dopamine antagonist anti-emetics
- domperidone - mecoclopramide 10mg up to 3Xd - prokinetic effect on GI tract - extrapyramidal sx
56
antihistamine anti-emetics
- cyclizine 50mg up to 3xd - antimuscarinic
57
5 hydroxytryptamine anti-emetics
ondansetron = for emetogenic chemotherapy = 8mg 1hr prior - consitpation, flushing
58
benzodiazepines examples and MoA
- diazepam, lorazepam - hyperpolarization = further excitation
59
SE and Ci diazepam dose
- amnesia, ataxia, confusion - psychomotor impairement - rep depression - 2mg increased to 15-30mg if needed
60
salbutamol MoA
- bronchial smooth muscle relaxation and bronchodilation
61
salbuamol SE and CI
- fin tremor, headaches, cramps - hypokalaemia
62
salbutamol doses
- ingaler = 100-200mcg 4xd - nebs = 2.5 - 5mg 4xd - powder 200-400mcg 4xd
63
alendronic acid moa, dose, se
- bisphosphonate - prevents further reduction in bone mass - 10mg daily - SE = gi, oesophagitis, necrosis jaw - empty stomach, 30mins pre breakgast
64
corticosteroids moa
- upregulation of gene transcription
65