Heart and Lung pharmacology Flashcards
What 4 drugs are used for treatment of a NSTEMI?
What do they work on?
Anti platelet (for a thrombus)
LMWH (for a thrombus)
Statin (for cholesterol plaques)
Beta blocker/nitrates (anti-ischaemic)
Give 2 examples of anti-platelets
Clopidogrel
Aspirin
Give 3 non-pharmacological treatments of a STEMI
Give 2 pharmacological treatments
- PCI (primary percutaneous coronary intervention)
- Thrombolysis
- Angioplasty (place a stent through the radial artery or/and suck clots out)
Aggressive anti thrombotic and anti platelet
3 treatments for heart block
Atropine: Stimulates AVN (not in cardiac transplant)
Isoprenaline: B1 agonist like adrenaline
Pacemaker
How do you treat digoxin toxicity?
What disease process is this relevant to?
Digoxin specific antibody fragments
Heart block
How do you treat beta blocker/calcium toxicity?
What disease process is this relevant to?
Glucagon
Heart block
Pharmacological treatments for atrial fibrillation (3)
Examples
Ventricular rate control (B blockers, digoxin, verapamil)
Antithrombotics (warfarin or NOAC - not aspirin)
Anticoagulation in those who benefit (risky peeps)
Give 3 examples of class 1 anti-arrhythmic drugs What class of drugs are they? What phase do they work on?
a. Disopyramine
b. Lidocaine
c. Flecadinine
Na channel blocker
Works on phase 0
What effect does Disopyramide have on the heart’s electrical activity?
What is its clinical use?
Increases AP duration
SVT/VT
What effect does Lidocaine have on the heart’s electrical activity?
What is its clinical use?
Decreases AP duration
VT
What effect does Flecadinine have on the heart’s electrical activity?
What is its clinical use?
No effect on AP duration
SVT/VT
Give 2 examples of class 2 anti-arrhythmic drugs What class of drugs are they? What phase do they work on?
Atenolol, Sotalol
Beta blockers
Works on phase 4
Explain the MOA of beta blockers
Block SAN and block sympathetic activation to reduce ventricular contractility and slow heart rate
Also improves myocardial oxygen demand:supply ratio
Negative chronotropic and inotropic
What is the clinical use of beta blockers? (5 e.g.)
SVT
Arrhythmia’s, hypertension, stable heart failure, ischaemic heart disease, reduce mortality after MI
7 side effects of beta blockers
Bronchospasm, Can worsen heart failure, Cold extremities, Fatigue, Impotence, Nightmares, Wheeze
5 contraindications of beta blockers
Asthma (B2), AV block, Carconogenic shock, Hypotension, PVD, Untreated phaeochromocytoma
Give 2 examples of class 3 anti-arrhythmic drugs
What class of drugs are they? What phase do they work on? What do they do to the electrical activity of the heart? 2 clinical uses
Amiodarone, Sotalol
Potassium channel blocker
Works on phase 3
Increased AP duration and refractory period
SVT/VT
7 side effects of Amiodarone
Abnormal cardiac rhythm Blue-grey skin discolouration Corneal microdeposits Hypo/hyper thyroidism (contains iodine) Lung fibrosis Photosensivity reactions
Pharmacokinetics of amiodarone
- How long does it take to work?
- Vd and t1/2
Takes a week to work
High Vd and half life (lipid soluble)
When is Lidocaine used?
When amiodarone is contraindicated/ineffective
Give 4 examples of class 4 anti-arrhythmic drugs What class of drugs are they? What phase do they work on?
Verapamil, Diltiazem, Amlodipine, Nifedipine
Calcium channel blocker
Works on phase 2
Explain the mechanism of action of calcium channel blockers
Reduces ventricle contraction, dilates vessels and reduces myocardial oxygen demand
Block AVN and SAN
What is the clinical use of calcium channel blockers?
SVT
Hypertension, Angina, Arrhythmia
8 side effects of calcium channel blockers
ankle oedema, increased appetite, drowsy, flushed, gastro-oesophageal reflux, reduced blood pressure, reduced heart rate, lightheaded
4 contraindications of calcium channel blockers
Carcinogenic shock, Moderate/severe heart failure, Pregnancy, Severe bradycardia
What are the 4 anti-arrhythmic drugs not included in the V-W classification?
Adenosine
Digoxin
Magenium
Atropine
What is the MOA of Adenosine?
- What effect does it have on electrical action?
- What is its clinical use?
Potassium channel activation
Slows AVN and pacemaker conduction
SVT
Explain the MOA of digoxin
What is its effect on the electrical activity of the heart?
Blocks the Na/K pump to reduce Na into mysoctes
This increases N/Ca pump to increase Na in and Ca out of myocytes
Reduce heart contractility (positive inotropic effect)
Also blocks the AVN
3 clinical uses of digoxin
AF, Atrial flutter and end stage congestive heart failure
What is the MOA of Magnesium?
- What is its clinical use?
Calcium channel blocker
VF and digoxin toxicity
What is the MOA of Atropine?
- What effect does it have on electrical action?
- What is its clinical use?
Antimuscarinic
Increases SAN and AVN conduction
Bradycardia
Pharmacokinetics of digoxin
- Therapeutic index
- Loading dose
- Vd and t1/2
Small therapeutic index but needs a high loading dose
Has a large vD and half life
6 side effects of digoxin
2 cautions
- Arrhythmia
- Alter electrolytes (caution)
- CNS (confusion, nightmares, agitation)
- GI effects
- Renal toxicity (not metabolised) (caution with CKD)
- Yellow and blurred vision
3 drugs which digoxin interacts with
Amoidarone and Verapamil (increase digoxin levels)
Diuretics (reduce Na and Mg)
What are the 4 drugs used to treat hypertension?
ACEi
Beta blockers
Ca antagonists
Diuretics
What are the 2 classes of calcium antagonists?
Dihydropyridines
Non-hydropyridines
2 examples of dihydropyridines
What is their MOA?
What drug do you combine them with?
Amlodipine and Nifedipine
Vasodilation and smooth muscle contraction
Use with a beta blocker
2 examples of non-hydropyridines
What is their MOA?
What are they also useful to treat
Verapamil and Diltiazem
Slow heart rate
(Angina)
4 side effects of dihydropyridines
Ankle oedema, flushing, tachycardia, worse angina
What is the MOA of Monoxiail?
What drugs do you combine it with?
Opens potassium channels causing vasodilation
Reduces peripheral resistance causing increased CO and fluid retention
MUST use with a diuretic/beta blocker
What is the MOA of alpha blockers?
What are they used to treat?
Example
Block A1 receptors > sympathetic vasoconstriction
Treats hypotension
e.g. Doxazoin
What is the MOA of clonidine/methylDOPA?
What is it used to treat?
2 side effects
Stimulate A1 receptors > reduced sympathetic outflow
Treats hypertension
Sedation and dry mouth
What are the 5 drugs which can be used in the treatment of pulmonary oedema?
Diamorphine Oxygen Diuretic IV nitrate Dobutamine
Why do you give diamorphine?
Reduces anxiety and vasodilates
Why do you need to keep increasing the dose of IV nitrate?
Patients become pharmacologically tolerant very quickly
Why is dobutamine given?
When is it given?
Inotropic support
Only if the patient is in shock as can > arrhythmias
What are the 2 potassium sparing diuretics?
How do they work?
Amiloride: Blocks Na/K exchanger (old)
Spironolactone: Mineralocorticoid receptor antagonist blocking aldosterone
3 examples of thiazide diuretics
What is their MOA?
2 ‘problems’
Bendrofluazine, Metolazone, Chlorthialidone
Blocks Na/Cl transporter in DCT
Metabolically upsetting to ions and low ceiling (reduced dose = same effect)
3 examples of loop diuretics
What is their MOA?
2 ‘problems’
Furosemide, Bumetanide, Torasemide
Block Na/K/Cl cotransporter in ascending LoH
Metabolically upsetting to ions and high ceiling (increased dose = increased effect)
What are the 5 classes of drugs used in chronic heart failure treatment?
- Diuretics
- ACE inhibitors
- Mineralocorticoid receptor antagonists
- ARB blockers
- Beta blockers
Positive and negative for diuretics
Improve symptoms but not prognosis
Define euvolemic
Fluid balance
Which ACEi is used in chronic heart failure?
Enalapril
Explain ACE escape
ACE is not the only enzyme which converts ANG 1 > ANG 2
7 effects of ANG
Aldosterone, Efferent arteriole constriction, Myocardial hypertrophy, Na retention, Thirst, Vasoconstrict, Vessel hypertrophy,
3 effects of ACEi
Vasodilate, Na excretion, Increase kinins
6 side effects of ACEi
Angio-oedema, Cough, Hypotension, Increased K and creatinine, Rash, Reduced Hb, Renal artery stenosis
Which clinical trial showed ACEi benefit?
Consensus
What do you need to monitor when using ACEi?
Potassium
What is the MOA of mineralocorticoid receptor antagonists?
Why are they needed?
Block aldosterone
Not fully supresssed by ACEi due to ACE escape
Give 2 examples of mineralocorticoid receptor antagonists
Which is selective/non-selective?
2 side effects?
Spironolactone: non-selective (inreased K and testosrerone)
Eplerenone: selective
Give 3 examples of ARB Blockers
What is their MOA?
Losartan, Valsartan, Candesartan
Angiotension receptor blocker
Explain the advantages (2) and disadvantages (3) of ARB blockers
Advantages:
- Overcome ACE escape
- No cough
Disadvantages:
- Same effects on renal function
- No effect on mortality (but decreases hospital admissions)
- ACE breaks down kinins so blocking ACE increases kinins > vasodilation (good for heart failure) - ARB’s miss this
What is ISA and why is it bad for heart failure?
Intrinsic symathomimetic activity
Stimulates sympathetic activity before blocking
Give 5 examples of beta blockers without ISA
Which are selective and which are non-selective?
Atenolol, Bisprolol, Metoprolol (selective)
Timolol, Pronanolol (non-selective)
Give 2 examples of alpha blocking beta antagonists
Carvedilol
Lavetolol
What is the MOA of Ivabradine
Who is the drug prescribed in?
Blocks the SAN pacemarker current to reduce blood pressure
Used in patients with a heart rate above 70bpm despite a maximum dose of beta blockers
What is the MOA of Sacubitril and Valsartan?
Sacubitril is an NEP inhibitor (breaks down naturietic peptides to increase sodium and water levels)
Vlasartan is an angiotensin receptor blocker
What is the MOA of Candozatril?
Is it still used?
Blocked NEP but NEP also breaks own ANG2 so levels increased
Early drug - didn’t work
What is the MOA of Omapatrilat?
Is it still used?
Blocks ACEi and NEP but increases kinins
Early drug
What does digoxin do to the starling curve?
Moves it up and to the left
What effect does digoxin have on the carotid sinus?
Sympathetic and vagotonic
- reduces heart rate
- reduces AVN conduction
What 4 drugs should you avoid when treating chronic heart failure?
Ca antagnists
Positive inotrops e.g. digoxin (unless end stage)
Anti-arrhythmic’s
Variable evidence on statins and aspirin
Give 3 examples of new heart failure drugs
AVP antagonists
Calcium sensitisers
Nesiritide
What drugs are used to treat cancers with an ALK or ROS1 mutation?
What is the suffix for the drug?
Translocation inhibitors
e.g. nib
What drugs are used to treat cancers with a PD1/PDL1 antigen on the Tcell/tumour?
What is the suffix for the drug?
Monoclonal antibodies
e.g. mab
2 examples of antibiotics used to treat mycoplasma pneumoniae infection
Macrolide and Tetracycline
2 examples of antibiotics used to treat legionella pneumophilia infection
Macrolide and Quinolone
What antibiotics do you usually use to treat HAP?
Macrolide
What is the MOA of Rifampicin?
Inhibits RNA synthesis
What is the MOA of Isoiazid?
Inhibits cell wall synthesis
What is the MOA of Pyrazinamide?
Disrupts plasma membrane and energy metabolism
What is the MOA of Ethambutole?
Inhibits cell wall synthesis
What is the TB treatment schedule?
All (+/-) E for 2 months
Then R and I for 4 months
What drug is given as a supplement when starting on TB medication?
Pyridoxine
What are the new drugs given towards asthma
Monoclonal antibodies against IL5 to switch off eosinophils
e.g. ‘-zumab’
Give 2 drugs used for the management of IPF
Anti fibrotic medication e.g. Pirfenidone
Tyrosine kinase inhibitors e.g. Nintedanib
What drug can be used to reduce breathlesness?
Opiates
What is the MOA of beta agonists?
Reverse bronchoconstriction
What is the MOA of steroids in the lungs?
Increase B2 receptor synthesis to suppress cytokines
What is the MOA of montelukast?
Is it more or less effective than steroids?
Leukotrine receptor antagonist
Blocks bronchoconstriction
Less effective than steroids
Give 2 examples of LABA
Formeterol
Salmeterol
What is the MOA of theophylline?
What other disease can it be used to treat?
Bronchodilator and immune modulator
Treatment of heart block in MI, transplant, spinal injury
Give 3 drugs used to treat COPD
What is their MOA?
Salbutamol and Ipatropium (short acting bronchodilators)
Tiotropium (long acting bronchodilator