Cardiovascular Pharmacology 💊 Flashcards by Jasmin bullock

What are examples of class 1 anti arrhythmic drugs?

Lidocaine, flecainide, propafenone

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What are examples of class 2 anti arrhythmic drugs?

Bisoprolol, metoprolol, propranolol

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What are examples of class 3 anti arrhythmic drugs?

Amiodarone, sotalol

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What are examples of class 4 anti arrhythmic drugs?

Verapamil, diltiazem

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What what kind of tissue will lidocaine have most of an effect?

Fast beating or ischaemic tissue

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When are class 1b agents used?

In ventricular tachycardia especially during ischaemia

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What is the effect of class 1b drugs on an ECG?

No difference to normal tissue. It fast beating or ischaemic tissue the QRS will be prolonged

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What are the side effects of class 1b anti arrhythmic drugs?

Dizziness, drowsiness, abdominal upset

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What is automaticity?

The ability to spontaneously depolarise and generate an action potential

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How do class 1C anti arrhythmics affect an ECG?

Increased PR, QRS and QT

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Why must IV amiodarone be administered through a central line and not a peripheral cannula?

Can cause thrombophlebitis if through peripheral cannula

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What is the action of class 1 anti arrhythmics?

Sodium channel blockers

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What is the action of class 2 anti arrhythmics?

Beta blockers- beta adrenergic antagonists

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What is the action of class 3 anti arrhythmics?

Potassium channel blockers

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What is the action of class 4 anti arrhythmics?

Calcium channel blockers

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How do class 1B drugs affect the fast cardiac action potential in cardiac myocytes?

Shorten refractory period and action potential duration

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What affect do beta blockers have on slow action potential in SA node?

Decreased slope of phase 4 depolarisation and prolonged depolarisation

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What effect of beta blockers can be seen on an ECG?

Increased PR interval

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What effect do class 3 drugs have on action potential in cardiac myocytes?

Slow repolarisation so prolong refractory period and action potential duration

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What affect do class 4 drugs have on the slow action potential in SA node?

Slow rise of action potential and prolong repolarisation- increasing refractory period and increasing PR interval

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Why are beta blockers used in atrial fibrillation?

They decrease heart rate and promote conversion to sinus rhythm

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Why would we use long term oral anti-coagulant therapy in a patient with atrial fibrillation?

This reduces the risk of stroke associated with AF

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Why would a class 2 or 4 drug be used in AV nodal re-entry (a type of SVT)?

These drugs slow conduction through the AV node

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Why is it that class 1 anti arrhythmics show greater effects on areas of damaged or fast beating cardiac tissue?

They bind more rapidly to open or inactivated Na+ channels so show greater effects in tissues that are frequently depolarising

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What is the drug of choice for ventricular arrhythmias, what are other alternatives?

Drug of choice is amiodarone however lidocaine and mexiletine can also be used in conjunction with amiodarone

Out of the two class 1B anti arrhythmics which is given orally and which IV?

Lidocaine- IV | Mexiletine- orally

What are the therapeutic uses of flecainide?

Used in AF in patients without structural heart disease and in refractory ventricular arrhythmias

What are common adverse effects with beta blockers?

Bradycardia, hypotension and fatigue

What drugs can prevent life-threatening arrhythmias occurring subsequent to myocardial infarction?

Beta-blockers

Which drugs can be used in AF to control rate?

Bisoprolol, verapamil, diltiazem

Which drugs can be used in AF for rhythm control?

Sotalol, flecainide with bisoprolol, amiodarone

Which IV drugs would you use for ventricular tachycardia?

IV metoprolol/ lidocaine or amiodarone

Which drug is best for Wolff Parkinson White syndrome?

Flecainide

What are the side effects fo ACEi?

Dry cough, hypo tension, hyperkalaemia, angioedema, exacerbation of renal disease

What are some DDIs of ACEi?

Caution with other hypotensives and drugs that increase potassium, also with NSAIDs

What are some side effects of angiotensin receptor blockers?

Hypotension, hyperkalaemia, exacerbation of renal disease

What is the difference between Phenylalkylamines and dihydropyridine Calcium channel blockers?

``` Phenylalkylamines are cardio selective and so are used class 4 anti-arrhythmics Dihydropyridines are used as hypotensives ```

What are some adverse drug reactions of calcium channel blockers (dihydropyridines)?

Hypotension, dizziness, palpitations, ankle swelling and flushing (many side effects are from vasodilation the drug causes)

What are contraindications for using. Calcium channel blocker to treat hypertension?

Aortic stenosis, unstable angina

What would the effect be on sim a statin if the patient would taking amlodipine simultaneously?

There would be increased effect of the statin as amlodipine is a CYP3A4 inhibitor preventing metabolism of the statin

What are some adverse drug reactions of class 4 anti-arrhythmic agents?

Heart block, bradycardia, cardiac failure, constipation

What are some ADRs of spironolactone?

Hyperkalaemia, gynaecomastia

What are some contraindications for spironolactone use?

Addison’s disease, hyperkalaemia, pregnancy

How do alpha blockers head reduce blood pressure?

They are antagonists selective to alpha 1 adrenoreceptors found in blood vessels that normally increase sympathetic tone. Therefore they help reduce sympathetic tone

What are some ADRs associated with alpha blockers?

Dizziness, syncope, headache, fatigue, postural hypotension

Why would you try to avoid giving alpha blockers along side dihydropyridines?

Both cause peripheral vasodilation so there is a risk of oedema

How do beta blockers help reduce blood pressure?

Reduce heart rate and contractility and also decrease sympathetic tone of blood vessels

What are some ADRs associated with beta blockers?

Bronchospasm, heart block, lethargy, impotence

What are some contraindications for beta blockers?

Asthma, AV node dysfunction, hepatic failure

Why would you avoid giving someone with gout a thiazide/thiazide-like diuretic?

They have an adverse drug reaction of hyperuricaemia

If a patient was over 55 or from a black-African/African-Caribbean ethnicity what would be your first line hypertension treatment?

Calcium channel blocker

If a patient was under 55 and not from a black-African/African-Caribbean ethnicity what would be your first line hypertension treatment?

ACEi or ARB

If a patient has hypertension with type 2 diabetes which drug is first line to treat the hypertension?

ACEi or ARB

What is an example of an alpha-adrenoreceptor blocker?

Doxazosin

Why are CCBs first line for younger and black African-Caribbean groups?

Much less likely to have increased renin

Why can spironolactone cause gynaecomastia?

Spironolactone reduces androgen activity causing an imbalance in oestrogen to androgen ratio

When should a beta or alpha blocker be considered over spironolactone to rest resistant hypertension?

When potassium levels are higher than 4.5mmol, due to risk of hyperkalaemia with spironolactone

Which of arterial and venous thrombi have higher platelet content?

Arterial

Which of anti-platelets and anticoagulants work better at preventing venous thrombi?

Anticoagulants | Antiplatelets work best for arterial thrombi

How does aspirin work as an anti platelet?

Inhibits COX-1 mediated production of thromboxane A2 which is a platelet aggregating agent

What are some ADRs of aspirin?

GI irritation, peptic ulcers, haemorrhage and hypersensitivity

What are contraindications to aspirin use?

Reye’s syndrome (dont give to under 16s), hypersensitivity and pregnancy (third trimester)

When can low dose aspirin be used?

AF, secondary prevention of stroke, TIa and acute coronary syndromes, post PCI, after MI

What are some examples of ADP receptor antagonists?

Clopidogrel, prasugrel and ticagrelor

Is clopidogrel a reversible or irreversible inhibitor?

Clopidogrel is an irreversible inhibitor

Which of ticagrelor and clopidogrel have a faster onset?

Ticagrelor has a more rapid onset of action than clopidogrel

How does dipyridamole act as an anti-platelet?

Phosphodiesterase inhibitor inhibiting GP2b/3a expression | Prevents adenosine re-uptake, increased plasma conc, inhibits platelet aggregation

What is an example of a glycoprotein 2b/3a inhibitor?

Abciximab

What are examples of two fibrinolytic agents?

Streptokinase and alteplase

Why can streptokinase only be used once?

The body develops antibodies to it

What drugs works to stop bleeding by inhibiting fibrinolysis?

Transexamic acid

Why should ACEi be offered to all patients post MI once haemodynamic ally stable?

Prevents left ventricular remodelling

Why is clopidogrel contraindicated in hepatic failure?

Metabolised in liver by CYPs to produce active metabolites

Which of the DOACs is a direct thrombin inhibitor?

Dabigatran

What agents can be used to reverse the defects of warfarin?

Vitamin K and prothrombin complex concentrate

Which clotting factors production are affected by warfarin as they require vitamin K as a cofactor for activation?

2, 7, 9, 10

What enzyme does warfarin inhibit?

Vitamin K epoxide reductase

What drugs can increase the effects of warfarin?

CYP2C9 inhibitors, cephalosporins, high protein binding drugs, drugs that decrease Vit K absorption

What are some drugs which increase warfarin metabolism and therefore decrease its effects?

Barbiturates, phenytoin, rifampicin, St Johns Wort

What would a higher INR indicate in regards to how anti coagulated the blood is?

High INR= more anti coagulated

What are some DOACs which are direct Xa inhibitors?

Apixaban, edoxaban, rivaroxaban

What are two examples of low molecular weight heparins?

Dalteparin, enoxaparin

What is fondaparinux?

Synthetic pentasaccharide (heparin)

How does heparin work as an anticoagulant?

Inhibits clotting factor Xa

What are some ADRs related to heparin from common to rare?

Bruising/bleeding Heparin induced thrombocytopenia Hyperkalaemia Osteoporosis (long term use)

What is the reversal agent of heparin?

Protamine sulphate

What is an example of a cholesterol absorption inhibitor?

Ezetimibe

Ezetimibe is an inhibitor of what transporter at the brush border?

NPC1L1

What drug class is alirocumab an example of?

PCSK9 inhibitors

How do PCSK9 inhibitors help to reduce plasma lipid levels?

Prevent LDL receptor degradation

What statin (+dose)do we use for primary and secondary prevention of CVD?

Primary: 20mg atorvastatin Secondary: 80mg atorvastatin

What enzyme do statins inhibit?

HMG-CoA reductase

How does simvastatin’s half life compare to atorvastatin’s?

Simvastatin has a short half life of around 2 hours | Atorvastatin has a longer half life of around 24 hours

What are ADRs associated with statins?

GI disruption, nausea, headache, myalgia | Very rarely- rhabdomyolysis

What drugs can affect statin effects?

Amiodarone, amlodipine, diltiazem, macrolides (these all increase plasma conc of the statin by inhibiting CYP3A4)

What is an example of a fibrate used in hyperlipidaemia?

Fenofibrate

How do vibrates help treat hyperlipidaemia?

Activation of PPAR-a gene which increases lipoprotein lipase production

What are some ADRs associated with fibrates?

Gall stones (cholelithiasis), GI upset are rarely myositis