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MODA drugs > 3 - Cardiovascular and renal pharmacology > Flashcards

3 - Cardiovascular and renal pharmacology Flashcards

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1
Q

Lidocaine

A

Local anaesthetic acting on VGNa channels
Stabilise inactivated state and make it harder to reactivate
Acts on intracellular surface
Shows use dependence

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2
Q

Nifedipine

A

Dihydropyridine
2 binding sites
- S6 segment and association loop of domain 4
- Close to phenylalkylamine binding site

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3
Q

Verapamil

A

Phenylalkylamine

Binding site at S6 and part of S5-6 loop

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4
Q

Diltiazem

A

Benzothiazepines
Block from outside
Modulate DHP binding

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5
Q

Propanolol

A

Non-specific B-antagonist

Blocks the effect of catecholamines

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6
Q

Atenolol

A

B1-antagonist
Blocks the effect of catecholamines
Coupled to Gs GProtein, so coupled to a rise in cAMP

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7
Q

Quinidine

A

Anti-dysrhythmic drug
Class 1A
Block VGNa channels
Increased AP duration, intermediate rate of association/dissociation

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8
Q

Procainamide

A

Anti-dysrhythmic drug
Class 1A
Block VGNa channels
Increased AP duration, intermediate rate of association/dissociation

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9
Q

Lidocaine (Class)

A

Anti-dysrhythmic drug
Class 1B
Block VGNa channels
Decreased AP duration, fast rate of association/dissociation

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10
Q

Flecainide

A

Anti-dysrhythmic drug
Class 1C
Block VGNa channels
No effect on AP duration, slow rate of association/dissociation

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11
Q

Propanolol/Atenolol

A

Antidysrhythmic agent
Class2
Sympathetic antagonists (B blockers)

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12
Q

Digoxin / Digitoxin

A 
Cardiac glycosides
Antidysrhythmic
Alleviate oedema
Inhibit NaKATPase pump
Increase intracellular Na, reduce driving force for Ca exit, Ca builds up in cell
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13
Q

Oubain

A

Cardiac glycosides
Inhibit NaKATPase pump
Used experimentally - too powerful to be used clinically

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14
Q

Dobutamine

A

B1 selective analogue of dopamine
Intravenous
+ve ionotropic effect greater than chronotropic
Shock, increase CO after heart surgery, heart failure with no hypertension
However - increase oxygen demand, increase heart rate and blood pressure

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15
Q

Bisoprolol / Carvedilol

A

3rd generation B1 antagonist
Used in stable heart failure
Limit damaging effects of chronic stimulation by catecholamines and improve cardiac function
(reverse desensitization and downregulation of B adrenoceptors)

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16
Q

Inodilators

A 
Phosphodiesterase inhibitors
Raise intracellular cAMP
Mimic B stimulation
Can lead to dysrhythmias
Vasodilation in smooth muscle, decreases afterload on heart
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17
Q

Milrinone

A 
Inodilator
Phosphodiesterase type 3 inhibitor
Raide intracellular cAMP
cGMP inhibited
Dysrhythmias - short term treatment of severe heart failure
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18
Q

Dipyridamole

A

Inodilator
Phosphodiesterase type 5 inhibitor
Raise intracellular cAMP
cGMP specific

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19
Q

Sildenafil

A

Inodilator
Phosphodiesterase type 5 inhibitor
Raise intracellular cAMP
cGMP specific

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20
Q

Caffeine

A

Methylxanthine (caffeine/theophylline)
Non selective phosphodiesterase inhibitors
Also adenosine A1 A2 antagonists –> release of Ca from intracellular stores
Positive ionotropic and chronotropic effects

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21
Q

Pimobendan

A 
Inodilator
Calcium sensitizer
Increase cardiac Ca binding efficiency to troponin without more energy requirement
Peripheral vasodilation (PDE3 inhibitor)
-canine dilated cardiomyopathy
-canine mitral valve regurgitation
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22
Q

Levosimendan

A

Inositol/Ca sensitizer

Licensed for human use in heart failure in the UK

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23
Q

Bosentan

A

Non specific Endothelin 1 antagonist

Treat pulmonary arterial hypertension

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24
Q

Streptokinase

A

Clot lysis
Binds plasminogen activator and generates plasmin
Degradation of fibrin in clots and breakdown of clotting factors 2, 5, 7

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25
Anistreplase
Combination of plasminogen and anisoylated streptokinase Inactive until anisoyl group removed in blood More prolonged activity
26
Alteplase
Recombinant human tissue plasminogen activator Single chain Greater activity on plasminogen bound to fibrin in clots - localising action
27
Duteplase
Recombinant human tissue plasminogen activator Double chain Greater activity on plasminogen bound to fibrin in clots - localising action
28
Aspirin
Alongside clot lysis therapies Prevent further thrombosis Can cause GI bleeding by influencing gastric acid secretion
29
Clopidogrel
With aspirin, alongside clot lysis therapies Inhibits platelet aggregation by inhibiting ADP binding to receptor on platelets Improves morbidity and mortality in heart disease patients
30
Eptifibatide
Inhibitor of glycoprotein 2b/3a receptor (receptor needed for fibrinogen bridging between platelets) Cyclic heptapeptide inhibitor Prevention of myocardial infarction in patients with unstable angina
31
Tirofiban
Inhibitor of glycoprotein 2b/3a receptor (receptor needed for fibrinogen bridging between platelets) Non-peptide inhibitor Prevention of myocardial infarction in patients with unstable angina
32
Abciximab
Monoclonal antibody against glycoprotein 2b/3a receptor (prevents fibrinogen bridging between platelets) Also binds vitronectin receptor on platelets, endothelial cells and vascular smooth muscle cells - for coronary artery thrombosis
33
Heparin
Natural anticoagulant produced by basophils and mast cells Binds to enzyme inhibitor anti-thrombin 3 (AT3) exposing active site Activated AT3 inactivates thrombin and factor Xa Used for unstable angina, treat deep vein thrombosis and as a prophylactic drug to prevent clots
34
Warfarin
Inhibits clotting, given orally Inhibits synthesis of clotting factors 2, 7, 9 and 10 and regulatory factors protein C, S and Z Prevent clotting on prosthetic heart valves Interacts with many other chemicals Rodenticide
35
Dabigatran
Thrombin inhibitor | In patients with atrial fibrillation and one additional risk factor for stroke.
36
Aminocaproic acid
Similar to lysine, competitively inhibits plasminogen activation Inhibits severe bleeding caused by excessive clot lysis
37
Tranexamic acid
aminocaproic acid analogue Similar to lysine, competitively inhibits plasminogen activation Inhibits severe bleeding caused by excessive clot lysis
38
Renin
Production of angiotensin2
39
Furosemide
Loop diuretic 'High ceiling' - high rate of diuresis Sulphonamide Blocks NaK2Cl co transport in apical membrane thick ascending limb Weak inhibition of carbonic anhydrase Venodilation, reduce atrial filling pressure Increase renal blood flow without a change in GFR Ca Mg and K loss Metabolic alkalosis Uric acid excretion decreased --> gout
40
Bumetanide
Loop diuretic 'High ceiling' - high rate of diuresis Sulphonamide
41
Eptifibatide
Inhibitor of glycoprotein 2b/3a receptor (receptor needed for fibrinogen bridging between platelets) Cyclic heptapeptide inhibitor Prevention of myocardial infarction in patients with unstable angina
42
Tirofiban
Inhibitor of glycoprotein 2b/3a receptor (receptor needed for fibrinogen bridging between platelets) Non-peptide inhibitor Prevention of myocardial infarction in patients with unstable angina
43
Abciximab
Monoclonal antibody against glycoprotein 2b/3a receptor (prevents fibrinogen bridging between platelets) Also binds vitronectin receptor on platelets, endothelial cells and vascular smooth muscle cells - for coronary artery thrombosis
44
Heparin
Natural anticoagulant produced by basophils and mast cells Binds to enzyme inhibitor anti-thrombin 3 (AT3) exposing active site Activated AT3 inactivates thrombin and factor Xa Used for unstable angina, treat deep vein thrombosis and as a prophylactic drug to prevent clots
45
Warfarin
Inhibits clotting, given orally Inhibits synthesis of clotting factors 2, 7, 9 and 10 and regulatory factors protein C, S and Z Prevent clotting on prosthetic heart valves Interacts with many other chemicals Rodenticide
46
Dabigatran
Thrombin inhibitor | In patients with atrial fibrillation and one additional risk factor for stroke.
47
Aminocaproic acid
Similar to lysine, competitively inhibits plasminogen activation Inhibits severe bleeding caused by excessive clot lysis
48
Tranexamic acid
aminocaproic acid analogue Similar to lysine, competitively inhibits plasminogen activation Inhibits severe bleeding caused by excessive clot lysis
49
Renin
Production of angiotensin2
50
Furosemide
Loop diuretic 'High ceiling' - high rate of diuresis Sulphonamide
51
Bumetanide
Loop diuretic 'High ceiling' - high rate of diuresis Sulphonamide
52
Hydrochlorothiazide
Thiazide diuretic Some inhibition of carbonic anhydrase Cortical segment of thick ascending limb Distal tubule - block NaCl co transport Vasodilator effects by diuretic action and directly acting on vessels Metabolic alkalosis Hypokalaemia - cant use with cardiac glycosides, as potentiate action Increase Mg excretion but not Ca Uric acid excretion decreased --> gout
53
Bendroflumethiazide
Thiazide diuretic Some inhibition of carbonic anhydrase Cortical segment of thick ascending limb Distal tubule - block NaCl co transport Vasodilator effects by diuretic action and directly acting on vessels Metabolic alkalosis Hypokalaemia - cant use with cardiac glycosides, as potentiate action Increase Mg excretion but not Ca Uric acid excretion decreased --> gout
54
Amiloride
Potassium sparing diuretic Prevent Na reabsorption by blocking apical Na channels K is not drawn into lumen as no gradient created Weak diuretic effect
55
Triamterene
Potassium sparing diuretic Prevent Na reabsorption by blocking apical Na channels K is not drawn into lumen as no gradient created Weak diuretic effect
56
Spironolactone
Potassium sparing diuretic Antagonist to the action of aldosterone Aldosterone binds steroid receptor and translocates to nucleus, where synthesis of Na channels and NaKATPase Spironolactone metabolised to Canreone Potassium Canreonate acts as K sparing diuretic Compete for steroid receptor binding site Only effective when distal tubule cells under effect of aldosterone
57
Acetazolamide
Carbonic anhydrase inhibitor Inhibit NaHCO3 reabsorption in proximal and distal tubules NaHCO3 reabsorption is driven by the NaKATPase pump CAinhibitors decrease the availability of H, K loss is increased Therapeutic use in glaucoma Suppress HCO3 secretion, which forms aqueous humour in eye Excessive loss leads to metabolic acidosis
58
Mannitol
Osmotic diuretic Filtered at glomerulus but not reabsorbed Retain their osmotic equivalent of water so increase urine volume Used when urine flow reduced because low GFR causes excessive reabsorption of salt and water Maintain urine flow Rapidly reduces intracranial and intraocular pressure - does not cross BBB
59
Captopril
ACE inhibitor - antagonism of renin-angiotensin system | Antihypertensive
60
Enalapril
ACE inhibitor - antagonism of renin-angiotensin system Antihypertensive Converted in liver to active metabolite - enalaprilat
61
Saralasin
Angiotensin 2 partial agonist | Peptide - not suitable for oral administration
62
Losartan
Angiotensin 2 antagonist Angiotensin receptor blocker (ARB) Act on AT1 receptor
63
Verapamil (Class)
Class 4 antidysrhythmic agent | Ca channel blocker - reduce Ca entry
64
Amiodarone
Class 3 antidysrhythmic agent | Prolong action potential and refractory period
65
Isobutylmethylxanthine (IBMX) ?
Methylxanthine Non selective phosphodiesterase inhibitors Also adenosine A1 A2 antagonists --> release of Ca from intracellular stores Positive ionotropic and chronotropic effects
66
Reserpine
Antihypertensive drug a2-adrenoceptor agonist Dope racehorses

MODA drugs (5 decks)

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