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MODA drugs > 3 - Cardiovascular and renal pharmacology > Flashcards

3 - Cardiovascular and renal pharmacology Flashcards

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
Q

Anistreplase

A

Combination of plasminogen and anisoylated streptokinase
Inactive until anisoyl group removed in blood
More prolonged activity

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26
Q

Alteplase

A

Recombinant human tissue plasminogen activator
Single chain
Greater activity on plasminogen bound to fibrin in clots - localising action

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27
Q

Duteplase

A

Recombinant human tissue plasminogen activator
Double chain
Greater activity on plasminogen bound to fibrin in clots - localising action

28
Q

Aspirin

A

Alongside clot lysis therapies
Prevent further thrombosis
Can cause GI bleeding by influencing gastric acid secretion

29
Q

Clopidogrel

A

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
Q

Eptifibatide

A

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
Q

Tirofiban

A

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
Q

Abciximab

A

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
Q

Heparin

A

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
Q

Warfarin

A

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
Q

Dabigatran

A

Thrombin inhibitor

In patients with atrial fibrillation and one additional risk factor for stroke.

36
Q

Aminocaproic acid

A

Similar to lysine, competitively inhibits plasminogen activation
Inhibits severe bleeding caused by excessive clot lysis

37
Q

Tranexamic acid

A

aminocaproic acid analogue
Similar to lysine, competitively inhibits plasminogen activation
Inhibits severe bleeding caused by excessive clot lysis

38
Q

Renin

A

Production of angiotensin2

39
Q

Furosemide

A

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
Q

Bumetanide

A

Loop diuretic
‘High ceiling’ - high rate of diuresis
Sulphonamide

41
Q

Eptifibatide

A

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
Q

Tirofiban

A

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
Q

Abciximab

A

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
Q

Heparin

A

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
Q

Warfarin

A

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
Q

Dabigatran

A

Thrombin inhibitor

In patients with atrial fibrillation and one additional risk factor for stroke.

47
Q

Aminocaproic acid

A

Similar to lysine, competitively inhibits plasminogen activation
Inhibits severe bleeding caused by excessive clot lysis

48
Q

Tranexamic acid

A

aminocaproic acid analogue
Similar to lysine, competitively inhibits plasminogen activation
Inhibits severe bleeding caused by excessive clot lysis

49
Q

Renin

A

Production of angiotensin2

50
Q

Furosemide

A

Loop diuretic
‘High ceiling’ - high rate of diuresis
Sulphonamide

51
Q

Bumetanide

A

Loop diuretic
‘High ceiling’ - high rate of diuresis
Sulphonamide

52
Q

Hydrochlorothiazide

A

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
Q

Bendroflumethiazide

A

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
Q

Amiloride

A

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
Q

Triamterene

A

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
Q

Spironolactone

A

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
Q

Acetazolamide

A

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
Q

Mannitol

A

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
Q

Captopril

A

ACE inhibitor - antagonism of renin-angiotensin system

Antihypertensive

60
Q

Enalapril

A

ACE inhibitor - antagonism of renin-angiotensin system
Antihypertensive
Converted in liver to active metabolite - enalaprilat

61
Q

Saralasin

A

Angiotensin 2 partial agonist

Peptide - not suitable for oral administration

62
Q

Losartan

A

Angiotensin 2 antagonist
Angiotensin receptor blocker (ARB)
Act on AT1 receptor

63
Q

Verapamil (Class)

A

Class 4 antidysrhythmic agent

Ca channel blocker - reduce Ca entry

64
Q

Amiodarone

A

Class 3 antidysrhythmic agent

Prolong action potential and refractory period

65
Q

Isobutylmethylxanthine (IBMX) ?

A

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

66
Q

Reserpine

A

Antihypertensive drug
a2-adrenoceptor agonist
Dope racehorses

MODA drugs (5 decks)

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