Cardiovascular & Renal Pharmacology

Question 1

Acetazolamide

Answer 1

Carbonic anhydrase inhibitor - inhibits NaHCO3 reabsorption

Weak diuretics only used in glaucoma & to acclimatise to high altitudes

Question 2

Saralasin

Answer 2

Angiotensin II partial agonist but doesn’t match up to other antihypertensives because it’s a peptide

Question 3

Clopidogrel

Answer 3

Inhibits ADP-binding to its receptor on platelets inhibiting aggregation
Combined with low dose oral aspirin reduces mortality/morbidity in a range of heart diseases

Question 4

Amiloride, Triamterene

Answer 4

Potassium-sparing diuretics
Block apical Na channels
Diuresis weak but K-loss reduced

Question 5

Problems with loop/thiazide diuretics

Answer 5

Hypokalaemia and resulting metabolic alkalosis
Increased Mg loss (Ca loss increased with loop, decreased in thiazide)
Decreased uric acid excretion potentially leading to gout

Question 6

Tirofiban

Answer 6

Non-peptide inhibitor of alpha-IIb-beta-3-integrin (responsible for fibrinogen bridging between platelets)
Used to prevent MI in unstable angina or after certain types of MI

Question 7

Theophylline

Answer 7

Non-selective PDE inhibitor and adenosine receptor antagonist have positive ino/chronotropic effects

Question 8

Diltiazem

Answer 8

Benzothiazepine - blocks L-type calcium channels from the outside

Question 9

Spironolactone

Answer 9

Aldosterone receptor antagonist

Metabolised in liver to canrenone, salt: potassium canrenoate acts as a potassium-sparing diuretic

Question 10

Eptifibatide

Answer 10

Cyclic heptapeptide inhibitor of alpha-IIb-beta-3-integrin (responsible for fibrinogen bridging between platelets)

Question 11

Losartan

Answer 11

Non-peptide AT-1 receptor antagonist blocking angiotensin II function

Question 12

Nifedipine

Answer 12

Dihydropyridine - blocks L-type calcium channels

Binding modified by benzothiazepines

Question 13

Alteplase, duteplase

Answer 13

Single chain/double chain recombinant tissue plasminogen activators
Greater activity on plasminogen bound to fibrin localising its activity

Question 14

Class II antidysrhythmics

Answer 14

Beta-blockers: Propranolol, Atenolol

Question 15

Dobutamine

Answer 15

Beta-1-receptor agonist (inotropic>chronotropic) given IV in shock, to increase CO after open heart surgery and in heart failure without hypertension

Question 16

Class IV antidysrhythmics

Answer 16

Calcium channel blockers - verapamil

Question 17

Bisoprolol, carvedilol

Answer 17

Third-generation B-1-receptor antagonists limit effects of chronic SNS stimulation in congestive heart failure

Question 18

Abciximab

Answer 18

mAb against the receptor binding the vitronectin receptor

Used with coronary angioplasty for coronary artery thrombosis

Question 19

Furosemide, Bumetanide

Answer 19

Loop diuretics - very powerful
Effects reduced on repeated administration
Block NKCC in TAL, furosemide also a venodilator

Question 20

Anistreplase

Answer 20

Combined plasminogen and anisoylated streptokinase

Streptokinase inactive until anisoyl group is removed giving prolonged activity

Question 21

Class I antidysrhythmics

Answer 21

Block voltage-gated sodium channels:
1A: Quinidine, Procainamide
1B: Lidocaine
1C: Flecainide

Question 22

Aminocaproic acid, Tranexamic acid

Answer 22

Inhibit plasminogen activation to prevent excessive clot lysis
Chemically similar to lysine

Question 23

Verapamil

Answer 23

Phenylalkylamine - blocks L-type calcium channels from the outside

Question 24

Rivaroxaban

Answer 24

Inhibits factor Xa (first of its kind)

Prophylaxis after knee/hip surgery

Question 25

Digoxin, Digitoxin, Ouabain

Answer 25

Cardiac glycosides: block Na/K-ATPase

Question 26

Mannitol

Answer 26

Osmotic diuretic filtered but not reabsorbed at all | Useful in cerebral oedema (reduce ICP) and where urine flow reduced due to excessive reabsorption

Question 27

Streptokinase

Answer 27

Activates plasminogen

Question 28

Levosimendan (& pimobendan - vets)

Answer 28

New class of inodilators - calcium sensitisers Increase calcium sensitivity binding efficiency without increasing energy demand Inhibits PDE III giving its peripheral vasodilatory effects

Question 29

Class III antidysrhythmics

Answer 29

Prolong AP and therefore refractory period: Amiodarone

Question 30

Dabigatran

Answer 30

Inhibits thrombin | Used in atrial fibrillation with one other stroke risk factor & after knee/hip surgery

Question 31

Milrinone

Answer 31

Inodilator most often used in heart failure especially short-term in severe failure unresponsive to conventional therapy - inhibits PDE-III

Question 32

Hydrochlorothiazide, Bendroflumethiazide

Answer 32

Thiazide diuretics | Block Na/Cl co-transport in TAL/DT, in long term also have vasodilator effects

Question 33

Captopril, Enalapril

Answer 33

ACE inhibitors reducing pre/afterload (TPR) | Used in heart failure and hypertension

Question 34

Warfarin

Answer 34

Inhibits synthesis of clotting factors (II, VII, IX, X) & regulatory factor proteins (C, S & Z) Used prophylactically from recurrence or with prosthetic valves

Question 35

Heparin

Answer 35

Naturally occurring anticoagulant in mast cells/basophils Activates antithrombin III which inhibits thrombin & factor Xa Used prophylactically (during/after surgery) & in DVT Must be injected