Cardiovascular Block Drugs

Drugs affecting haemostasis

Drug name Class Indications Mechanism Adverse effects/Contraindications

Heparin Anticoagulant - prevention and treatment - Anti-thrombin III allosteric modulator Risk of bleeding and hemorrhage,
(Reversed by of venous (increases activity) thrombocytopenia, osteoporosis
protamine) thromboembolism
- Prophylactic to prevent
thrombosis during surgery
- Dalteparin Anticoagulant, - Same as heparin - Anti-thrombin III allosteric modulator Risk of bleeding and hemorrhage,
- Enoxaparin Low molecular - can be administered (increases activity) thrombocytopenia (less than heparin),
weight heparin subcu. so safe to use at osteoporosis (less than heparin)
home
- Warfarin Anticoagulant - Prevention and treatment - Inhibits vitamin K reductases which - Bleeding/haemorrhage
(Reversed by Vit K or of DVT and PE inhibits synthesis of clotting factors II, - Crosses placenta
fresh frozen plasma) - Prevention for TE VII, IX, X
- oral administration
- Hirudin Anticoagulant - Prophylactic for - Thrombin inhibitor
thrombosis
- Rivaroxaban NOAC - Prophylactic for - Factor Xa inhibitor
(Reversed by thrombosis
Andexanat alfa) - oral administration
- Dabigatran NOAC - Prophylactic for - Thrombin inhibitor
(Reversed by thrombosis
Idarucizumab) - oral administration
- Aspirin Anti-platelet agent - Prevention of primary and - Irreversible non-selective inhibitor of - Increased risk of GI bleeding
secondary CV events COX - Contraindicated in those with bleeding
- oral administration disorder, or taking other anti-coagulants
- Abciximab Anti-platelet agent - Used in combination with - Inhibits all pathways of platelet
heparin or LMWH for high- aggregation via GPIIb/IIIa receptor
risk coronary surgery
- parenteral administration
- Clopidogrel Anti-platelet agent - Used in combination with - ADP receptor antagonist (P2Y12)
low dose aspirin for acute
coronary syndromes
- oral administration
- Streptokinase Thrombolytic - Treatment for acute - Activates plasminogen to plasmin - Once in a lifetime drug because it is antigenic
drugs thromboembolic disorders which degrades stable clots (body generates ab after 4 days)
- Parenteral administration
Alteplase Thrombolytic - Treatment for acute - Activates plasminogen to plasmin
drugs thromboembolic disorders which degrades stable clots
- Parenteral administration - More selective for fibrin bound
plasminogen (considered clot selective)
Drugs affecting cardiovascular structure and function
Enalapril ACEi Hypertension - 1st hypotension
- dry cough
- loss of taste
- hyperkaliemia
- itching & rash
- angio-oedema
- acute renal failure
- foetal malformations
Candesartan AT1 receptor Hypertension, use if
inhibitor adverse effects with ACEi
- Prazosin α 1 – receptor Hypertension Decrease vasoconstriction - 1st dose hypotension
- Terazosin antagonist - postural hypotension (elderly)
- Doxazosin - nasal congestion

an α )
it’s a sin to block being - headache

- Propranolol β1 & β2 Hypertension, heart failure, - Reduce CO - Contraindicated in asthma (risk of airway
receptor
(lol, you’re such a
- Timolol angina - Reduce renin release constriction) and atrioventricular block
antagonist
β)
- Atenolol Selective for β 1 Hypertension, heart failure, - Reduce CO - Contraindicated in asthma (risk of airway
- Metoprolol angina - Reduce renin release constriction) and atrioventricular block
Partial β 1 & β 2
receptor
- Pindolol Hypertension, heart failure - Reduce CO - Contraindicated in asthma (risk of airway

antagonist
- Reduce renin release constriction) and atrioventricular block

- Felodipine Vascular selective Hypertension, Angina - Inhibit calcium influx used for - Oedema
- Nifedipine L-type Ca2+ vasoconstriction - Flushing & headache
(Dipine your arteries in channel blocker - Increase cardiac contractility and rate - Reflex tachycardia
ketchup) - Contraindicated for patients with heart
 failure and tachyarrhythmia

- Verapamil Non-selective L- Hypertension, Angina - Relative effects on cardiac and - Oedema

- Diltiazem type Ca2+ channel vascular smooth muscle - Flushing & headache
blocker - Reflex tachycardia
- Contraindicated for patients with heart
failure and tachyarrhythmia
Thiazide Diuretic Hypertension - Increase Na+ and water excretion
- Decrease Na+ and Cl- reabsorption
Furosemide Diuretic Heart failure Inhibits Na-K-Cl cotransporter in loop
of Henle: first line oedema therapy,
blood volume reduction, limits water
retention
Spironolactone Diuretic Heart failure Reduces systemic aldosterone: first
line oedema therapy, blood volume
reduction, limits water retention
Digoxin Cardiac glycoside - Heart Failure - Inhibits Na+/K+-ATPase (Excitable tissues: GIT, Heart, Brain)
- Atrial fibrillation - Results in increased sarcoplasmic Ca2+ - Anorexia
- Nausea
- Diarrhoea
- Drowsiness
- Confusion
- Psychosis

β 1 receptor
- Fibrillations
Dobutamine - Heart failure short term - Increase cardiac work
partial agonist support - O2 demand
- Risk of dysrhythmias

- Fucks with β receptor signalling

- Receptor downregulation

cascade
Milrinone Phosphodiesterase - Heart failure short term - Increase cardiac work
inhibitor support - O2 demand
- Risk of dysrhythmias
Lidocaine Class I Na+ channel - Dysrhythmia - Slows phase 0 of ventricular action Dose dependent:
blocker potential - Lip and tongue numbness
- Light headedness
- Visual disturbance
- Muscular twitching
- Convulsions
 - Coma
- Respiratory arrest
- CV depression
Drugs affecting the ANS
Bethanecol Muscarinic - Urinary retention and GIT
receptor agonist paralysis
Pilocarpine Muscarinic - Glaucoma (elevated - Headache (vasodilation)
receptor agonist intraocular pressure)
Ipratropium/Tiotropium Muscarinic - COPD
receptor
antagonist
Atropine Muscarinic - Anti-spasmodic
receptor - Pre-anaesthesia
antagonist - Pupil dilation for eye
exam
- Acetylcholinesterase
inhibitor poisoning
- Reduce sweating
- Some forms of
bradycardia
Hyoscine Muscarinic - Motion sickness
receptor
antagonist
Acetylcholinesterase - Myasthenia gravis - Inhibits breakdown of acetylcholine
inhibitors - Glaucoma
- Alzheimer’s
Phenylephrine α1& α2 - Nasal decongestant
receptor - Raise blood pressure
agonist (reflex bradycardia)
Prazosin α1& α2 - Hypertension
receptor
antagonist
Clonidine α 2 receptor - Hypertension
agonist - Sedation
Dobutamine β 1 receptor - Heart failure
agonist
Salbutamol β 2 receptor - Asthma
agonist
Local Mediators
- Chlorpheniramine H1 receptor
- Promethazine antagonist
Drug Regulation of Serum Lipids

-Atorvastatin Statins -hypercholesterolaemia -Competitive inhibition of HMG-CoA -Mild GI symptoms

-Fluvastatin reductase -Headaches
-Pravastatin -Insomnia
-Simvastatin -Dizziness
- Drug-drug interactions with Cyt. P450
metabolism
-Cholestyramine Bile acid -hypercholesteremia - Inhibits resorption of bile acids - Abdominal discomfort
-Colestipol sequestrants -decreases cholesterol and thus - Bloating
requires LDL from circulation to - Constipation
replenish cholesterol - Flatulence

Ezetimibe NPC1L1 -hypercholesteremia - Inhibits cholesterol absorption into -Diarrhea

transporter enterocytes without affecting bile salt -Headache
inhibitor or ADEK absorption -Tiredness
-Allergic reactions
-Severe joint or stomach pain

Niacin -hypercholesteremia - Lowers secretion of VLDL from liver - flushing

-Lowers LDL & TAGs - hypotension
-Increases HDL - nausea/vomiting
-Lowers apo A
- Evolovumab PCSK9 inhibitors - Familial and sever - Facilitates recycling of LDL receptors - Injection site reactions
- Alirocumab uncontrolled in hepatocytes -Nasopharyngitis
hypercholesterolaemia - Upper respiratory tract infections
- Gemfibrozil Fibrates -Hypertriglyceridemia - Bind to nuclear receptors (PPARα ) - Elevation of aminotransferases
- Fenofibrate and alter gene expression -GI disturbances
- Increased LPL synthesis
- EPA Omega 3 FA - Decreases VLDL and therefore TAGs - aftertaste, fishy burps
- DHA - Diarrhea, abdominal discomfort
- Blood thinning
Drug Treatment of Ischaemic Heart Disease (IHD)
- Glyceryl trinitrate Nitrates - Angina - Increase NO production leading to - Postural hypotension from venous pooling
- Isosorbide dinitrate dephosphorylation of myosin LC - Headache & flushing from arterial dilation
(isosorbide-5- - Decrease preload - Reflex tachycardia
mononitrate is active
metabolite)
β1 & β2
(lol, you’re such a
- Propranolol Hypertension, Angina - Reduce CO - Asthma (risk of airway constriction)
receptor
β)
- Reduce renin release - Atrioventricular block
antagonist - Cold extremities
- Bradycardia worsening heart block in
patients with coronary disease
- Atenolol Selective for β 1 Hypertension, Angina - Reduce CO - Asthma (risk of airway constriction)
- Reduce renin release - Atrioventricular block
- Cold extremities
- Bradycardia worsening heart block in
patients with coronary disease
- Felodipine Vascular selective Hypertension, Angina - Inhibit calcium influx used for - Oedema
- Nifedipine L-type Ca2+ vasoconstriction - Flushing & headache
(Dipine your arteries in channel blocker - Increase cardiac contractility and rate - reflex tachycardia
ketchup) - NOT for heart failure
- Verapamil Non-selective L- Hypertension, Angina - Relative effects on cardiac and - NOT for heart failure (bradycardia)
- Diltiazem type Ca2+ channel vascular smooth muscle - Flushing, headache, oedema
blocker - Bradycardia
- AV block
Ivabradine Sinus node Na+ /K+ Angina - Decreases velocity of diastolic - Brightness in visual field and blurred vision
funny current depolarization (funny currents in eye)
inhibition - Bradycardia
- Conduction abnormalities