Pharmacology - Cardiovascular drugs

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Cardiovascular Drugs
Kuma N
Creado por Kuma N
Kuma N
Creado por Kuma N hace más de 6 años
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Platelet Physiology - Antiplatelets: prevent platelets from clumping together to form clots Endothelial damage stimulates intrinsic pathy way Exposed collagen enables platelets to bind to VWF Changing shape of platelet and causing the release of chemical mediators: ADP, Thromboxane, Thrombin
How do platelets adhere together? ADP binds to receptor P2Y12 on platelet causing the activation of glycoprotein 2a/2b Allowing cross-link via fibrinogen to an adjacent platelet
MOA
ASPIRIN
Indication Secondary Prevention of Cardiovascular disease (75ng) UA, NSTEMI, STEMI (300mg) AF (following an ischaemic stroke) Other: TIA, Acute Ischaemic Stroke, Acute Migraine Pyrexia, Pain, Pre-eclampsia
Contraindication Allergic disease, Anaemia, Asthma, Previous peptic ulceration Pregnancy (third trimester) - the risk of haemorrhage
Side effects Dyspepsia, Haemorrhage
CLOPIDOGREL
Indication Those who present with aspirin hypersensitivity can take it for TIA| Acute Ischemic Stroke| Peripheral Arterial Disease ACS (+aspirin) Acute MI with NSTEMI (+aspirin) Acute MI with STEMI (+aspirin)
Contraindication Active bleeding
Side effects Diarrhoea, haemorrhage
Coagulation Physiology - Anticoagulant: slow the process of making clots
General MOA Block production of proteins (cofactors) made in the liver that causes blood to clot Cofactors e.g. Thrombin & Fibrin Vitamin K controls the production of these cofactors Therefore a therapeutic target is a disruption of: Vitamin K and these cofactors
Warfarin MOA
Heparin MOA
Thrombolytics
B - BLOCKERS ...
B-Blocker Classification
Mechanism of Action Blocks Beta adrenoceptors Antagonising the sympathetic nervous system
Blocking B1 receptors Negatively inotropic (rate) & chronotropic (contraction)
Blocking B2 receptors Induces Peripheral Vasoconstriction & Bronchoconstriction
Uses Angina| Hypertension| Antidysrhythmic| Post MI| Heart failure
Contraindicated Severe Asthma/COPD| Heart block
Side effects Lethargy, Erectile Dysfunction, Headache
Hypertension Mode of action in hypertension not properly understood, but they: Reduce CO| Alter Baroceptor reflect sensitivity| Block peripheral adrenoceptors
Angina Reduce cardiac work Evidence that withdrawal may cause exacerbation of angina
MI Reduce the recurrence rate of MI
Arrhythmias Esmolol hydrochloride: Cardioselective BBlocker - IV for short term management of supraventricular arrhythmias, sinus tachycardia or hypertension. Sotalol hydrochloride: Non-cardioselective BBlocker - Suppresses ventricular ectopic beats & non-sustained ventricular tachycardia
Heart Failure B-Blocker - block sympathetic activity. Bisoprolol fumarate & carvedilol reduced mortality in stable heart failure
Thyrotoxicosis Used in peri-operative preparation for thyroidectomy Propranolol hydrochloride - can reverse clinical symptoms of thyrotoxicosis within 4 days.
Propanolol NON-CARDIOSELECTIVE Use: Hypertension, thyrotoxic crisis, phaeochromocytoma (+ alpha-blocker)
Contraindicated Contraindicated: Asthma, bronchospasms, obstructive airways disease cardiogenic shock, hypotension
Atenolol Uses: Hypertension, Angina, Arrhythmias,
Contraindicated General side effect: Asthma, cardiogenic shock, marked bradycardia, However: This is cardioselective - so side effects will be minimal
ACE INHIBITORS
Classification
Side effects Alopecia, angina pectoris, angioedema, hyperkalaemia
Contraindication hypersensitivity to ACE inhibitors Pregnancy Breastfeeding eGFR < 60mL/min
Monitoring Requirements BEFORE STARTING ACE - or INCREASING DOSAGE Monitor Renal function & Electrolytes should be checked Renal dysfunction may present as renal artery stenosis or reduce eGFR
Diuretics
Loop Diuretics (Used in Pulmonary oedema due to LVF & Patients with Chronic Heart Failure) Inhibit the Na/2Cl/K cotransporter SEs, dehydration, hypo Na+, K+, Ca2+
Thiazides Used in Hypertension (& in Heart failure to relieve oedema):
Potassium-sparing Diuretics Aldosterone antagonist: Block Aldosterone antagonists Amiloride: Blocks Epithelial Na channels in DCT
Vasodilators Image on MOA
Indication for use Heart failure, IHD, Hypertension
Examples Nitrates: Dilate veins and large arteries Reducing preload Hydrazine: (used with nitrate) Dilates resistant vessels, Reducing afterload Alpha-blocker: see next revision card
Alpha-blocker: Prazosin Prazosin: Dilates arteries and veins
Calcium Antagonist Reduce cell entry of calcium via voltage gated calcium channels in smooth muscle Result: increased coronary and peripheral vasodilation & reduce heart muscle O2 consumption
Classification
Dihydropyridine (peripheral vasodilators) Nifedipine Amlodipine
Dihydropyridine (Slow conduction at AV & SA Node) Verapamil Diltiazem (can also be used to treat hypertension, angina & dysrhythmias) Dilate coronary arteries and can cause reflex tachycardia, therefore often use with B blockers
Contraindication for non-dihydropyridine Never prescribe with B Blockers Risk of: Severe Bradycardia, +/- LVF
Side effects of CCBlockers Flushes, Headaches, Ankle oedema (diuretic unresponsive), Reduced LVF
Digoxin Blocks Na/K+ pump Slowing pulse in fast AF
Risk of digoxin toxicity esp in the elderly Often divided into acute or chronic toxicity. In both of these toxicities, cardiac effects are of the greatest concern Visible on an ECG
Management of toxicity Stop Digoxin, correct electrolyte imbalances: K+, Mg, Ca, Treat arrhythmias IV Digifab (antibody)
Sodium Channel blocker Class I antiarrhythmics PROCAINAMIDE & LIDOCAINE - terminate VT Note QT interval may be prolonged
Amiodarone Class III antiarrhythmic Prolonges Cardiac Action Potential - reducing potential tachyarrhythmias USED IN: Supra & Ventricular Tachycardia & Cardiac Arrest.
Ivabradine BLOCKS 'funny current'/ pacemaker potential 1) slowing pulse rate (without significant drop in bp) USED IN: Angina, Heart Failure,
Statins MOA: Inhibit HMG-COA Reductase, causing synthesis of cholesterol in the liver Increasing LDL receptor expression on hepatocytes leading to reduced circulating LDL cholesterol
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