Pharmacology Flashcards
Ramipril - class and mechanism
- ACEi = enalapril, lisinopril, captopril
- Competitive inhibitor
- Inhibits synthesis of AG2 which is a vasoconstrictor
- Therefore = vascular smooth muscle relaxation and vasodilation
ACEi - dose
- initially 1.25 - 2.5mg once daily for HTN
- Can be increased to 10mg a day
ACEi SE and contraindications
- SE = persistent dry cough, hyperkalaemia, renal failure
- CI = caution if on diuretics or renal impairment, pregnancy
ACEI monitoring
- renal function and electrolytes before starting and during treatment
BB - examples and mechanism
- 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
BB dose
- Angina = 5mg OD up to 10
- HF = 1.25 and increase
BB SE + contraindications + monitoring
- SE = dizziness, fatigue, impotence
- CI = COPD, asthma, DM, heart block
- Probably not in preg and BF
- Monitor lung function in COPD
CCB examples and mechanism
- 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
CCB dose
- Initially 5mg OD and increase to 10mg
CCB SE and contraindications
- CI = cardiogenic shock, aortic stenosis, unstable angina
- SE = abdo pain, dizzy
ARB examples and mechanism
- Candesartan, losartan, valsartan
- Competitive antagonist
- Selective inhibition of potent vasoconstrictor peptide angiotensin 2
- Vascular smooth muscle and vasodilation
ARB dose
Candesartan = start 4mg, maintenance 8-32mg
Losartan = 50mg OD
ARB SE and CI
- Hypotension
- CI = aortic of mitral stenosis
- No in pregnancy or BF
- Monitor renal function
Aspirin mechanism of action
- Targets cyclooxygenase enzymes
- Irreversible inhibitor
- Impairs synthesis of thromboxane A2 and prostacyclin within platelets
- Therefore reduces platelet aggregation
Aspirin dose
75mg for secondary prevention
Aspirin SE and CI
- CI = peptic ulcer, bleeding disorders, under 16s, haemophilia, asthma
- SE = GI irritation, ulceration and bleeding, bronchospasm
Clopidogrel mechanism of action
- ADP receptor pathway inhibitors
- Irreversible inhibitor of ADP receptor
- Inhibits binding of ADP to platelet receptor –> inhibits platelet aggregation
Clopidogrel dose
75mg for prevention
ACS = 300-600mg loading dose
Clopidogrel SE and CI
- CI = active bleeding, caution in hepatic and renal impairment
- Avoid in pregnancy
- SE = GI discomfort
Statin mechanism of action
- 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
Statins dose
10mg OD and can increase to 80
Statins monitoring, SE and CI
- CI = caution if myositis/rhabdomyolysis or liver disease
- No in pregnancy
- SE = arthralgia, GI
- Monitoring = lipid profiles, LFTs, CK
LMWH examples and mechanism of action
- Enoxaparin, dalteparin, tinzaparin
- Inhibit factor Xa which is needed to convert prothrombin to thrombin, therefore coagulation inhibited
- DOAC = anticoagulant
LMWH dose
- VTE pregnancy = 40-100mg 2X
- DVT prophylaxis = 20mg - 40mg
- DVT/PE tx = 1.5mg/kg every 24hrs
LMWH SE and CI
- CI = endocarditis, trauma, renal impairement, haemorrhagic disorders
- SE = haemorrhage, thrombocytopenia
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