Heart and renal drugs

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Author:
mfawcett
ID:
183792
Filename:
Heart and renal drugs
Updated:
2012-11-17 13:14:03
Tags:
moda heart cardiovascular renal kidney pharmacology
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Description:
Drugs from Henderson's first lectures
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  1. Forskolin
    Activates adenylyl cyclase and raises intracellular cAMP
  2. Quinidine
    • Class 1A antidysrhythmic: Blocks voltage gated Na channels
    • Increases AP duration
    • Intermediate rate of association/dissociation
  3. Procainamide
    • Class 1A antidysrhythmic: Blocks voltage gated Na channels
    • Increases AP duration
    • Intermediate rate of association/dissociation
  4. Class 1A antidysrhythmics (2)
    classification
    • Blocks voltage gated Na channels
    • Increases AP duration
    • Intermediate rate of association/dissociation
    • Quinidine and Procainamine
  5. Lidocaine
    • Class 1B antidysrhythmic: Blocks voltage gated Na channels
    • Decreases AP duration
    • Fast rate of association/dissociation
  6. Class 1B antidysthymic
    • Blocks voltage gated Na channels
    • Decreases AP duration
    • Fast rate of association/dissociation
    • Lidocaine
  7. Flecainide
    • Class 1C antidysrhythmic: Blocks voltage gated Na channel
    • Same AP duration
    • Slow rate of association/dissociation
  8. Class 1C antidysrhythmic
    • Blocks voltage gated Na channels
    • Same AP duration
    • Slow rate of association/dissociation
    • Flecainide
  9. Propanolol
    • Class II antidysrhytmic: Sympathetic antagonist (beta blocker)
    • Will also releive hypertension, but damp down sympathetic activity that occurs during a heart attack
    • Acute IV: decrease CO -> compensatory increase in TPR. this goes away after a while, causing a long term decrease in BP
  10. Atenolol
    • Class II antidysrhythmic: Sympathetic antagonist (beta blocker)
    • Will also releive hypertension, but damp down sympathetic activity that occurs during a heart attack
  11. Class II antidysrhythmics (2)
    • Propanolol and Atenolol
    • Beta blockers
  12. Amiodarone
    • Class III antidysrhythmic: Prolongs AP and refractory period
    • Under different conditions can block both inward (Na) and outward (K) currents
    • For ventricular dysrhythmias and re-entry that doesn't respond to class I
  13. Class III antidysrhythmic
    • Amiodarone
    • Prolongs AP and refractory period
    • Under different conditions can block both inward (Na) and outward (K) currents
    • For ventricular dysrhythmias and re-entry that doesn't respond to class I
  14. Verapamil
    • Class IV antidysrhythmic: Ca channel blocker
    • Acts primarily on nodal tissue (as AP highly dependent on L and T type Ca channels
    • Slow conduction rate, prolong refractory period
    • Can compromise excitation-contraction coupling
  15. Diltiazem
    • Class IV antidysrhythmic: Ca channel blocker
    • Acts primarily on nodal tissue (as AP highly dependent on L and T type Ca channels
    • Slow conduction rate, prolong refractory period
    • Can compromise excitation-contraction coupling
  16. Class IV antidysrhythmics (2)
    • Verapamil and Diltiazem
    • Ca channel blocker
    • Acts primarily on nodal tissue (as AP highly dependent on L and T type Ca channels
    • Slow conduction rate, prolong refractory period
    • Can compromise excitation-contraction coupling
  17. Digoxin
    • Cardiac glycoside
    • Inhibits Na/K ATPase -> reduces activity of NCX -> Increased intracellular calcium -> Increased contractile force of heart
    • Used in heart failure/dysrhythmias
  18. Digitoxin
    • Cardiac glycoside
    • Inhibits Na/K ATPase -> reduces activity of NCX
    • -> Increased intracellular calcium -> Increased contractile force
    • of heart
    • Used in heart failure/dysrhythmias
  19. Ouabain
    • Cardiac glycoside
    • Inhibits Na/K ATPase -> reduces activity of NCX
    • -> Increased intracellular calcium -> Increased contractile force
    • of heart
    • Too powerful to be used clinically; used experimentally
  20. 3 cardiac glycosides
    mechanism
    • Digoxin
    • Digitoxin
    • Ouabain
    • Inhibits Na/K ATPase -> reduces activity of NCX -> Increased intracellular calcium -> Increased contractile force of heart
  21. Dobutamine
    used for?
    disadvantages?
    • Beta-1 agonist
    • Produces positive inotropic effect
    • Used IV for shock/to improve CO after open heart surgery/in heart failure in the absence of hypertension
    • BUT increases cardiac O2 demand and HR -> may precipitate or reveal dysrhythmias
    • May precipitate/potentiate hypertension
  22. Bisoprolol
    • Beta blocker
    • Reduces damage due to chronic adrenergic stimulation eg downregulation and desensitisation of recepors, apoptosis
    • Potential danger of over-inhibition
    • Used for cardiac failure and hypertension
    • Decreases plasma renin, increases plasma NA -> CNS side effects inc insomnia, depression
  23. Carvediol
    • Beta blocker
    • Reduces damage due to chronic adrenergic stimulation eg downregulation and desensitisation of recepors, apoptosis
    • Potential danger of over-inhibition
  24. Milrinone
    • Phosphodiesterase type III inhibitor (cGMP inhibited)
    • Inodilator to increase cAMP and mimic beta stimulation
    • Used for heart failure
    • Can lead to dysrhythmias
    • Also vasodilation -> reduced after load on heart (therapeutically beneficial)
  25. Dypiridamole
    • Phosphodiesterase type V inhibitor (cGMP specific)
    • Inodilator to increase cAMP (cGMP?) and mimic beta stimulation
    • Used for heart failure
    • Can lead to dysrhythmias
    • Also vasodilation -> reduced after load on heart (therapeutically beneficial)
  26. Sildenafil
    • Phosphodiesterase type V inhibitor (cGMP specific)
    • AKA Viagra
    • Inodilator to increase cAMP (cGMP?) and mimic beta stimulation
    • Used for erectile dysfunction (could also be used for heart failure)
  27. Methyxamines
    • Caffeine and Theophylline
    • Non-selective phosphodiesterase inhibitors
    • Adenosine A1 and A2 antagonists
    • Cause release of Ca from intracellular stores
    • Positive inotropic and chronotropic effects -> can predispose dysrhythmias
  28. Caffeine
    • Non-selective phosphodiesterase inhibitor
    • Adenosine A1 antagonist
    • Cause release of Ca from intracellular stores
    • Positive inotropic and chronotropic effects -> can predispose dysrhythmias
  29. Theophylline
    • Non-selective phosphodiesterase inhibitor
    • Adenosine A2 antagonist
    • Cause release of Ca from intracellular stotres
    • Positive inotropic and chronotropic effects -> can predispose dysrhythmias
  30. Pimobendan
    • Calcium sensitiser - increases Ca binding efficiency to troponin
    • Peripheral vasodilation by inhibiting Phosphodiesterase type III
    • Inodilator used in canine dilated cardiomyopathy/mitral valve regurgitation
  31. Livosimendan
    • Calcium sensitiser - increases Ca binding efficiency to troponin
    • Peripheral vasodilation by inhibiting Phosphodiesterase type III
  32. Bosentan
    • Non-specific endothelin antagonist
    • (ETA and ETB both cause vascular smooth muscle contraction)
    • Used for pulmonary arterial hypertension
  33. Streptokinase
    • Clot lysis
    • Causes generation of plamin by binding to plasminogen activator
    • -> degradation of fibrin and clotting factors II, V, VII
    • 47kDa protein formed by haemolytic streptococci
  34. Anistreplase
    • Clot lysis
    • Comination of plasminogen (substrate) and anisoylated streptokinase
    • Anisoyl group is removed in the blood to activate it (half life ~2 hours)
    • Long lasting -> 4-6 hours
  35. Alteplase
    • Clot lysis
    • Recombinant human tissue plasminogen activator
    • Localised action: greater activity on plasminogen bound to fibrin in clots
    • Single chain
  36. Duteplase
    • Clot lysis
    • Recombinant human tissue plasminogen activator
    • Localised action: greater activity on plasminogen bound to fibrin in clots
    • Double chain
  37. Aspirin
    NSAID, used with clot lysing agents to prevent further thrombosis
  38. Clopidogrel
    • Anti-clot
    • Inhibits platelet aggregation by inhibiting ADP binding to platelets
  39. Eptifibatide
    • Anti-clotting agent
    • Inhibits glycoprotein IIb/IIIa receptor, needed for fibrinogen bridging between platelets and between platelets and foreign surfaces
    • Cyclic heptapeptide
  40. Tirofiban
    • Anti-clotting agent
    • Inhibits glycoprotein IIb/IIIa receptor, needed for fibrinogen bridging between platelets and between platelets and foreign surfaces
    • Non-peptide
    • Can be used for prevention of myocardial infarction in patients with unstable angina/those who have recently suffered certain types of myocardial infarction
  41. Abciximab
    2 mechanisms
    • Anti-clotting agent
    • Monoclonal antibody against glycoprotein IIb/IIIa receptor (needed for fibrinogen bridging between platelets and between platelets and foreign surfaces)
    • Also binds to vitronectin receptors on endothelial cells, vascular smooth muscle cells and platelets (involved in cell adhesion and homeostasis)
    • Used with coronary angioplasty for coronary artery thrombosis
  42. Heparin
    mech
    use
    • Anticoagulant
    • Activates antithrombin III via a conformational change
    • -> Inactivation of thrombin and proteases inc factor Xa
    • Produced by basophils and mast cells
    • Used for unstable angina, after MI, DVT, to prevent clots during and after surgery
    • Has to be given via injection
  43. Warfarin
    • Anticoagulant
    • Inhibits synthesis of clotting factors II, VII, IX, X and regulatory protein factors protein C, protein S, protein Z
    • Prophylactic to protect against thrombosis (eg with increased tendency/history/prosthetic heart valves)
    • Given orally
    • Interacts with food/drink/other drugs
    • Also used as a rodenticide
  44. Dabigatran
    • Anticoagulant
    • Thrombin inhibitor
    • Reduces risk of atrial fibrillation/stroke by 40% compared with warfarin
  45. Aminocaproic acid
    Competitvely inhibits plasminogen activation to prevent sever bleeding
  46. Tranexamic acid
    • Competitvely inhibits plasminogen activation to prevent sever bleeding
    • Analogue of aminocaproic acid
  47. Furosemide
    • Loop diuretic
    • Blocks NKCC in Thick AL
    • Also venodilation -> reduced atrial filling pressure
    • Potentiates action at nephron by increasing renal blood flow without a change in GFR (reducing the fraction of the blood flow filtered at the glomerulus)
  48. Bumetanide
    • Loop diuretic
    • Blocks NKCC in Thick AL
  49. Probenecid
    • Competes for uric acid carrier in proximal tubule
    • -> Inhibits uric acid reabsorption
    • Used to treat gout (depositon of sodium urate crystals in synovial joints)
  50. Hydrochlorothiazide
    • Thiazide diuretic
    • Block Na/Cl cotransport in early distal tubule/cortical segment of Thick AL
    • Some carbonic anhydrase inhibition
    • Thiazide diureticBlock Na/Cl cotransport in early distal tubule/cortical segment of Thick AL
  51. Bendroflumethiazide
    • Thiazide diuretic
    • Block Na/Cl cotransport in early distal tubule/cortical segment of Thick AL
    • Some carbonic anhydrase inhibition
    • Vasodilatory effects: initially relieve hypertension through diuretic effects, then through direct effects on blood vessels
  52. Diazoxide
    • Vasodilator, non-diuretic thiazide
    • Opens K sensitive ATP channels
    • Used in hypertensive emergencies
  53. Amiloride
    • Potassium sparing diuretic
    • Blocks apical Na channels in late distal tubule
  54. Triamterene
    • Potassium sparing diuretic
    • Blocks apical Na channels in late distal tubule
  55. Spironolactone
    • Potassium sparing diuretic
    • Aldosterone antagonist in late distal tubule
    • Reduced upregulation of Na channels and Na/K ATPase
  56. Canrenone
    • Metabolite of spironolactone - responsible for some of its effects?
    • (K sparing diuretic via aldosterone antagonist)
  57. Potassium canrenoate
    K sparing diuretic
  58. Acetazolamide
    • Carbonic anhydride inhibitor
    • Not potent enough for appreciable diuresis - would need >99% of channels blocked
    • Used for glacoma: supresses HCO3- secretion, inhibiting aqueous humour production
    • Can be used for altitude sickness due to changes in blood acid/base balance that increase the respiratory drive
  59. Mannitol
    • Polysaccharide osmotic diuretic
    • Reduces intracranial and intraocular pressure - useful in cerebral oedema due to head injuries
  60. Captopril
    ACE inhibitor, for hypertension and heart failure
  61. Enalapril
    • ACE inhibitor, for hypertension and heart failure
    • Needs to be converted to enalaprilat in liver
  62. Enalaprilat
    • ACE inhibitor, for hypertension and heart failure
    • Converted from enalapril in liver
  63. Saralasin
    • Angiotensin II partial agonist
    • Peptide - not suitable for oral administration
  64. Losartan
    • Angiotensin II antagonist
    • Non-peptide
    • an ARB: angiotensin receptor blocker, acting on AT1 receptors
  65. Aliskiren
    Renin inhibitor
  66. Atenolol
    • Beta 1 blocker
    • Hypertension
  67. Doxazosin
    • alpha-1 antagonist
    • used for hypertension: dilates resistance and capacitance vessels
    • Lack of tachycardia (lack of block of alpha-1 receptors?)
    • In CNS, decrease SNS by modulating baroceptor reflex mechanisms
  68. Prazosin
    • alpha-1 antagonist
    • used for hypertension, but more usually a veterinary sedative
    • reflex fall in BP on first dose -> fainting
  69. Phentolamine
    • non selective alpha-antagonist
    • used for hypertension
    • vasodilatation, reflex tachycardia
    • increased SNS activity -> increased renin release
  70. Nifedipine
    • L type Ca channel antagonist
    • Reduce hypertension - cardiovascular and mild diuretic effect
    • Usually combined with a beta blocker to combat reflex tachycardia
    • May inhibit Angiotensin II induced aldosterone release
    • May antagonise baroceptor responses - unimportant long term
  71. Minoxidil
    • K+ channel opener (ATP sensitive channels)
    • Used for hypertension (and severe refractory forms)
    • Causes hyperpolarisation and relaxation of vascular smooth muscle
    • Used with a beta blocker (to stop reflex tachycardia) and a diuretic (to increase blood volume)
  72. Nicorandil
    • K+ channel opener (ATP sensitive channels)
    • Used for hypertension, sometimes angina
    • Causes hyperpolarisation and relaxation of vascular smooth muscle
  73. Clonidine
    • Decreases BP when injected into ventrolateral medulla
    • Works on either alpha-2 receptors, or imidazoline I2 receptors
    • Antihypertensive
  74. Moxonidine
    • Centrally acting antihypertensive
    • Imidazoline - acts on I-1 receptors in ventrolateral medulla
    • Fewer side effects than alpha-2 agonists
  75. Guanfacine
    • alpha-2 agonist (more specific than clonidine)
    • lower antihypertensive efficacy - alpha-2 receptors less important than I-1?
  76. Guanethidine
    • Sympatholytic antihypertensive
    • Acts on synthesis and processing of transmitter
    • Can cause postural hypertension
  77. Reserpine
    • Sympatholytic antihypertensive
    • Acts on synthesis and processing of transmitter
    • Can cause severe depression
  78. Hexamethonium
    • Antihypertensive ganglion blocker
    • IV, rapid onset
    • Blocks all ganglionic transmission - has been superceded
  79. Trimetaphan
    • Antihypertensive ganglion blocker
    • IV, rapid onset
    • Blocks all ganglionic transmission - has been superceded
  80. Sodium Nitroprusside
    • Antihypertensive
    • Metabolised  -> NO
    • In solution, hydrolyses -> cyanide
    • Used IV in hypertensive emergencies
  81. Hydralazine
    • Antihypertensive
    • Arteriolar vasodilator
    • Mechanism unknown
    • Cheap - used quite a lot in 3rd world

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