103 Drugs Flashcards
Heparin
Increases antithrombin III activity
Irreversibly inactivates factors IIa and Xa
Safe in pregnancy
Two types: unfractionated and low molecular weight
Anti-platelet agents
Block platelet activation
Good for treating arterial disease
- aspirin
- prasugrel
Anti-coagulants
Block production or activity of clotting factors
Used to treat venous disease
- warfarin
- heparins
Fibrinolytics
Primarily used to dissolve fibrin in arterial disease
Used to treat: MI, thromboembolic strokes, DVT, pulmonary embolism
- tissue plasminogen activator
- streptokinase
- urokinase
Aspirin
Blocks formation of thromboxane A2 in platelets
Lengthens bleeding time
Prophylaxis for MI
ADP receptor inhibitors
Prasugrel
Clopidogrel
Streptokinase
Protein secreted by streptococci
Binds to and activates human plasminogen
Inexpensive thrombolysis medication
Warfarin
Vitamin K antagonist
Prevents gamma carboxylation of factors II, VII, IX, X
Prolongs the extrinsic pathway
Monitored by the INR
Interactions with other drugs due to cytochrome P450
Side effects: teratogenic, haemorrhage risk, minor bleeding, skin necrosis, alopecia
Unfractionated heparin
Monitored by APTT
Safe in renal failure
Can be partially reversed with protamine sulphate
Thrombocytopenia and VTE rare complication resulting in heparin induced thrombocytopenia
Low molecular weight heparin
Not usually monitored
- tinzaparin
- enoxaparin
- dalteparin
Novel oral anti-coagulants
Alternative to warfarin
Two classes
- dabigatran: direct thrombin inhibitor
- rivaroxaban: direct factor Xa inhibitor
Dabigatran
Direct thrombin inhibitor
Indications
- VTE prophylaxis
- used for treatments of DVTs and PEs
- stroke prevention in atrial fibrillation
(argatroban- direct thrombin inhibitor given IV, safe in renal failure)
Rivaroxaban
Direct factor Xa inhibitor
Indications
- VTE prophylaxis
- used for treatment of DVTs and PEs
- stroke prevention
Apixaban is alternative drug
Types of anti-platelet drugs
Aspirin- cyclo-oxygenase inhibitor
Clopidogrel- ADP receptor blocker
Dipyridamole- inhibits phosphodiesterase
Prostacyclin- stimulates adenylate cyclase
Glycoprotein IIb/IIIa inhibiters
Glycoprotein IIb/IIIa inhibitors
Abciximab- monoclonal antibody
Eptifibatide- snake venom derivative
Tirofiban- blocks platelet aggregation
Thiazide and thiazide-like diuretics
Blocks reabsorption at the distal convoluted tube
- indapamide, nedrofluamethiazide
Side effects
- hypokalaemia
- increase in urate
- increase in glucose
- increase in blood lipids
Loop diuretics
Inhibits Na+ re-absorption from the proximal tube, K+ loss from distal tubule
Can lead to electrolyte abnormalities, hypovolaemia and diminished renal perfusion
- furosemide, bumetadine
K+ sparing diuretics
Inhibits aldosterone receptors in cortical collecting ducts
Promotes Na+ excretion and K+ re-absorption
Side effects: gynaecomastia, electrolyte and renal function abnormalities
- spironolactone, eplerenone
Statins
Drugs used to treat hypercholesterolaemia
Block endogenous cholesterol synthesis
Block HMG-CoA reductase
- simvastatin
Simvastatin
Natural statin
Prescribed for CAD prophylaxis
Especially in men over 50
ACEi
Block production of angiotensin
- vasodilation, BP lowering, reduce cardiac work
Side effects: cough, hypotension, renal impairment
- enalapril, ramipril, perindopril
ARNI
Angiotensin receptor inhibitor
- sacubitril, valsartan
Acts in activated RAAS
Blocks production of angiotensin
Promotes natriuresis
Side effects: hypotension, renal impairment
Beta blockers
Counteract active sympathetic system
- carvedilol, bisoprolol, metoprolol
Blocks noradrenaline/ adrenaline on adrenergic beta receptors
Slows HR, recudes BP
Side effects: bronchospasms , claudication, fatigue, vasoconstriction, hypoglycaemia
SA node blockade
Ivabradine
Blocks If channel with SA node
Slows HR, no BP effect
Side effects: visual aura, bradycardia, dizziness
Digoxin
Action
- increases myocardial contractility
- slows conduction at AV node
- excreted by kidneys
Ca2+ channel antagonists
Decrease frequency and force contraction
- phenylaklylamines, benzothiazepines
Increase dilation in arterioles
- dihydropyradines
Decrease cardiac workload
Side effects
- flushing and headaches
- peripheral oedema
Indapamide
Thiazide like diuretic
Hyperpolarises smooth muscle cells
Causes relaxation/ dilation of arteriole
Decrease in total peripheral resistance
Non selective beta blockers
B1 and B2
Propanolol
Selective beta blocker
B1 antagonist
Bisoprolol
Atropine
Blocker of muscarinic receptor
Dilates pupils, increases heart rate and reduces salivation and other secretions
Amlodipine
Ca2+ channel blocker acts preferentially on vasculature
Used as anti-hypertensive
Dihydropyridine
Non-DHP Ca2+ channel blockers
Verapamil
Diltiazem
Verapamil
Not a DHP
Blocks Ca2+
Used as antiarrhythmic
Blocks heart channels more than vessel channels
- affects nodal cells
- slows nodal rate
- protects ventricles from rapid atrial rhythms
Diltiazem
Not a DHP
Blocks Ca2+ channels
Used as antianginal and antiarrhythmic
Blocks heart and vessel channels
- slows nodal rate
- vasodilates coronary arteries
- prevents angina by reducing workload while increasing perfusion
Digoxin
Positive ionotropic agent
- increases stroke volume
- increases contractility
Works by inhibiting Na/K pump on membrane leads to increase Ca2+ in cytosol
Also stimulates vagus so slows heart rate and increases AV delay
Exetimibe
Potent and selective inhibitor of absorption of cholesterol in small bowel
Reduces flux of cholesterol esters in VLDL
Bile acid sequestrants
Bind bile acids in intestine, interrupt enterohepatic circulation of bile
Increased conversion of cholesterol to bile acids in liver
Increases LDLR activity, decreases LDLC
Limited by constipation and flatulence
