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Flashcards in 1-3 Henderson Deck (46)
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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

2
Q

Verapamil

A

L-type Ca channel blocker
Phenylalkylamine
Binding site at S6 and part of S5-6 loop
Class 4 antidysrhythmic agent

3
Q

Diltiazem

A

Ca channel blocker
Benzothiazepines
Block from outside
Modulate DHP binding

4
Q

Propanolol

A

Non-specific B-antagonist

Blocks the effect of catecholamines

5
Q

Quinidine

A

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

6
Q

Procainamide

A

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

7
Q

Lidocaine (Class)

A

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

8
Q

Flecainide

A

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

9
Q

Propanolol/Atenolol

A

Antidysrhythmic agent
Class2
Sympathetic antagonists (B blockers)

10
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
11
Q

Oubain

A

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

12
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)

13
Q

Inodilators

A
Phosphodiesterase inhibitors 
Raise intracellular cAMP
Mimic B stimulation
Can lead to dysrhythmias
Vasodilation in smooth muscle, decreases afterload on heart
14
Q

Milrinone

A
Inodilator
Phosphodiesterase type 3 inhibitor
Raise intracellular cAMP 
cGMP inhibited 
Dysrhythmias - short term treatment of severe heart failure
15
Q

Sildenafil

A

Inodilator
Phosphodiesterase type 5 inhibitor
Raise intracellular cAMP
cGMP specific

16
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

17
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

18
Q

Levosimendan

A

Inositol/Ca sensitizer

Licensed for human use in heart failure in the UK

19
Q

Bosentan

A

Non specific Endothelin 1 antagonist

Treat pulmonary arterial hypertension

20
Q

Streptokinase

A

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

21
Q

Anistreplase

A

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

22
Q

Alteplase

A

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

23
Q

Aspirin

A

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

24
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

25
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

26
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

27
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

28
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

29
Q

Dabigatran

A

Thrombin inhibitor

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

30
Q

Aminocaproic acid

A

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

31
Q

Tranexamic acid

A

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

32
Q

Renin

A

Production of angiotensin2

33
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

34
Q

Bumetanide

A

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

35
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

36
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

37
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

38
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

39
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

40
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

41
Q

Captopril

A

ACE inhibitor - antagonism of renin-angiotensin system

Antihypertensive

42
Q

Enalapril

A

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

43
Q

Saralasin

A

Angiotensin 2 partial agonist

Peptide - not suitable for oral administration

44
Q

Losartan

A

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

45
Q

Amiodarone

A

Class 3 antidysrhythmic agent

Prolong action potential and refractory period

46
Q

Reserpine

A

Antihypertensive drug
a2-adrenoceptor agonist
Dope racehorses