Y3 FORMULARY
ACEi
Examples RAMIPRIL, LISINOPRIL, PERINDOPRIL
MOA - Block ACE – prevents Ang I Ang II so vasodilation of efferent arteriole ↓
PVR lowers BP
- Dilates efferent glomerular arteriole ↓ intraglomerular pressure and slows
progression of CKD
- Reduced aldosterone more Na and water excretion reduced venous return
lowers BP
- Activated by phase 1 metabolism in the liver
Indication 1. HTN: 1st or 2nd line - reduce risk of stroke, MI and death from CV disease
2. Chronic heart failure – 1st line for all grades
3. Ischaemic heart disease – ↓ risk of subsequent CV events
4. Diabetic nephropathy and CKD – ↓ proteinuria and progression of nephropathy
SE - Hypotension
- Persistent dry cough - due to ↑ bradykinin
- Hyperkalaemia - lower aldosterone means potassium retention
- Angioedema, Tongue swelling
- Can worsen renal failure if renal artery stenosis
Contraindicati - Patients with renal artery stenosis or AKI, pregnant and breastfeeding
ons women
Interactions - Potassium-elevating drugs and Potassium-sparring diuretics
- NSAIDS - increases risk of renal failure, reduce anti-hypertensive effects
Elimination - Metabolised in liver, excreted by kidneys – Ramipril is also excreted in stool
ARB
Examples LOSARTAN
MOA - Block Ang II on AT1 receptor vasodilation of efferent arteriole ↓ PVR lowers
BP
- Dilates efferent glomerular arteriole ↓ intraglomerular pressure and slows
progression of CKD
- Reduced aldosterone more Na and water excretion reduced venous return
lowers BP
Indication 1. HTN: 1st or 2nd line - reduce risk of stroke, MI and death from CV disease
2. Chronic heart failure – 1st line for all grades
3. Ischaemic heart disease – ↓ risk of subsequent CV events
4. Diabetic nephropathy and CKD – ↓ proteinuria and progression of nephropathy
SE Hypotension
Kidney failure if renal artery stenosis
Hyperkalaemia
Contraindicati Patients with renal artery stenosis or AKI, pregnant and breastfeeding women
ons
Interactions - Potassium-elevating drugs and Potassium-sparring diuretics
- NSAIDS - increases risk of renal failure
Elimination - Highly bound to plasma proteins, excreted by kidneys
Nitrates
Examples ISOSORBIDE MONONITRATE, GTN
MOA - Nitrates NO ↑ cGMP and decreased Ca 2+ in vascular smooth muscle so
muscles relax
- This causes venous vasodilatation which ↓ cardiac preload and L ventricular
filling
- Overall ↓ cardiac work and myocardial oxygen demand relieving angina and
cardiac failure
- Can also relieve coronary vasospasms and dilate collateral vessels – improving
coronary perfusion
Indication 1. Acute angina and chest pain assoc w/ ACS - Short-acting (GTN)
, 2. Prophylaxis of angina – Long-acting (Isosorbide mononitrate) if B or CCB not
tolerated
3. Pulmonary odema – IV nitrates in combination with oxygen and furosemide
SE - Flushing, headaches, light-headedness, hypotension
- Sustained use can lead to tolerance
Contraindicati - Severe aortic stenosis
ons - Haemodynamic instability e.g. hypotension
Interactions Phosphodiesterase inhibitors - these enhance and prolong hypotensive effect of
nitrates
Caution Patient’s taking antihypertensive medication as it may precipitate hypotension
Elimination Metabolised in liver, excreted in urine and 1% in faeces
Beta Blockers (beta-1-adrenorecptors)
Examples ATENOLOL, BISOPROLOL
MOA - ↓ force of contraction and speed of conduction of heart via the b-1 receptor on
pacemaker cells
- This relieves myocardial ischaemia by reducing cardiac work and oxygen
demand
- They slow ventricular rate in AF by prolonging refractory period of AVN
- They ↓ BP by ↓ renin secretion from kidney since this is mediated by 1-
receptors
Indication 1. Ischaemic heart disease - 1st line to improve symptoms assoc w/angina and
ACS
2. Chronic heart failure – 1st line to improve prognosis
3. AF – 1st line to reduce ventricular rate and to maintain sinus rhythm in
paroxysmal AF
4. Supraventricular tachycardiac (SVT) – 1st line in pt’s with no circulatory
compromise
5. HTN – if others (A,C or D) not tolerated
SE - Fatigue, cold extremities, headache, GI disturbance
- Sleep disturbance
- Bradycardia, bronchospasms
- Abrupt withdrawal rebound tachycardia
Contraindicati - Asthma – can cause bronchospasm
ons - Haemodynamic instability and heart block
Interactions - Non-dihydropyridines - both are -vely inotropic and chronotropic cause HF,
bradycardia, asystole
Caution - COPD – use bB that is b1-selective (bisoprolol) rather than nonselective
(propranolol)
- HF – start at low-dose dose and ↑ slowly as they may impair cardiac function
- Hepatic failure – dosage reduction
- Worsen symptoms of patients with peripheral vasucular disease
Elimination Metabolised in liver and excreted by kidneys, but atenolol remains unchanged in
urine and stool
CCB
Examples AMLODIPINE , NIFEDIPINE, DILTIAZEM, VERAPAMIL
MOA - ↓ entry of Ca2+ into vascular and cardiac cells relaxation and vasodilation in
arterial smooth muscle
- CCBs ↓ myocardial contractility – supress cardiac conduction across AVN – slows
ventricular rate
- ↓ cardiac rate, contractility and afterload ↓ myocardial oxygen demand
prevents angina
Dihydropyridines: amlodipine, nifedipine – selective for vasculature
Non-Dihydropyridines: verapamil, diltiazem– selective for heart (NB: diltiazem has
some effects on vessels)
Indication 1. HTN – 1st or 2nd line – amlodipine – ↓ risk of stroke, MI, death from CV disease
, 2. Stable angina – control symptoms
3. Supraventricular arrythmias (AVT, AF, atrial flutter) – Diltiazem and Verapamil
SE Amlodipine and nifedipine: ankle swelling, flushing, headache, palpitations,
constipation
Verapamil: constipation, bradycardia, heart block, HF
Diltiazem can cause any of these effects
Contraindicati - pt’s with AVN conduction delay - may provoke complete heart block
ons - Unstable angina – avoid amlodipine/nifedipine – causes ↑ contractility and HR
↑ oxygen demand
- Severe aortic stenosis - avoid amlodipine/nifedipine – can provoke collapse
Interactions - bB and non-dihydropyridines
Caution Use non-dihydropyridines with caution in pt’s with poor left ventricular function
Elimination Metabolised rapidly and almost completely by liver
Potassium sparring diuretics
Examples SPIRONOLACTONE, AMILORIDE
MOA - Acts on DCT inhibits reabsorption of Na+ by ENaC excretion of Na+ and
water, retention of K+
↓ excretion of K+ and H+ reduced blood pressure and increased serum
potassium levels
Indication 1. Hypokalaemia – as part of combination therapy with other diuretics
SE When used with other diuretics: dizziness, hypotension, urinary symptoms
Hypokalaemia, hypokalaemia or hyponatraemia may also occur
Contraindicati - Severe renal impairment and hyperkalaemia
ons - Hypokalaemia – effect of potassium may be unpredictable
- States of volume depletion
Interactions - Potassium-elevating drugs (e.g. supplements and aldosterone antagonist) –
risk of hyperkalaemia
Caution Renal clearance of drugs e.g. digoxin and lithium may be altered – requiring dose
adjustment
Elimination Metabolised in liver and excreted by kidneys
Thiazide diuretics
Examples BENDROFLUMETHIAZIDE
MOA - Inhibit the Na+/Cl- co-transporter in DCT prevents reabsorption of Na and water
- This caused an initial fall in extracellular fluid volume ↓ BP
Indication 1. HTN – alternative if CCB unsuitable (e.g. odema) or add-on if BP not controlled
by CCBs + ACEi or ARB
SE - Hyponatraemia
- Hypokalaemia – due to increased urinary K losses may cause cardiac
arrythmias
- Hyperglycaemia, hyperlipaemia, hypercholesterolaemia
- May cause impotence in men
Contraindicati - pt’s with hypokalaemia and hyponatremia
ons - Gout – since they reduce uric acid excretion
Interactions - NSAIDs – reduced effectiveness of thiazides
Caution Loop diuretics – need electrolyte monitoring
Elimination Metabolised in liver and excreted by kidneys
Loop diuretics
Examples FUROSEMIDE
MOA - Inhibit the Na+/K+/2Cl- co-transporter in ascending loop → water also inhibited
lowers BP
- They also cause venous vasodilatation – in HF, this ↓ preload and improved
contractility
Indication 1. Acute pulmonary odema – relief of breathlessness in conjugation with oxygen
and nitrates
2. Chronic HF – symptom relief of fluid overload
3. Other oedematous states – e.g. liver failure, renal disease
