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Pharamacology > Cardiovascular > Flashcards

Cardiovascular Flashcards

1
Q

What are organic nitrates used to treat? How do they work?

A

Treat angina

Mimic NO-> vasodilation by activating guanylyl cyclase ->cGMP->reduces intracellular Ca2+

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2
Q

Effect of dilating venous capacitance vessels

A

Peripheral poling of blood -> reduced venous return -> reduced preload -> reduced myocardial O2 demand

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3
Q

Effect of dilating arterial resistance vessels

A

Reduced resistance to L ventricular emptying (afterload) so lowers blood pressure -> decreased cardiac work

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4
Q

Effect of dilating coronary arteries

A

Blood supply to ischaemic areas of myocardium and relieves coronary vasospasm

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5
Q

2 examples of organic nitrate and details

A 
GTN = Glyceryl Trinitrate (sublingually, 100% 1st pass metabolism, 1/2 life 2 mins)
Isosorbide Mononitrate (orally, longer 1/2 life)
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6
Q

Sinus node inhibitors treat what? How?

A

Treat angina by lowering heart rate -> less stress on myocardium
Inhibits If channels in cardiac pacemaker cells to reduce diastolic depolarisation of SA node

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7
Q

Example of sinus node inhibitor?

A

Ivabradine

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8
Q

What is Ivabradine?

A

A sinus node inhibitor used to treat angina by slowing dow heart rate

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9
Q

What is GTN?

A

Glyceryl Trinitrate is an organic nitrate used to treat angina by causing vasodilation

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10
Q

What is Isosorbide Mononitrate?

A

An organic nitrate used to treat angina by causing vasodilation

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11
Q

What do B-adrenoreceptor antagonists treat and how?

A

Treat angina and hypertension by slowing heart rate.
Block NA at B-receptors, blocking Ca2+ entering cell and blocking adenylyl cyclase forming cAMP (so less Ca2+ in SR-> cardiac contractility force and velocity decreased)
Also treat hypertension through secretion of renin from JGA

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12
Q

Side effects of B-adrenoreceptor antagonists

A

Tiredness, bradycardia, bronchospasm (B2 effects), congestive heart failure, cold hands (B1), nightmares and impotence (CNS effects)

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13
Q

3 examples of B-adrenoreceptor antagonists that are selective for B1

A

Metoprolol, Atenolol, Bisoprolol

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14
Q

What is Metoprolol?

A

B1-adrenoreceptor antagonist

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15
Q

What is propranolol?

A

B-adrenoreceptor antagonist (not selective for B1)

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16
Q

Name 6 B-blockers

A

Propranolol, Metoprolol, Atenolol, Bisoprolol, Labetalol, Carvedilol

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17
Q

How do calcium channel blockers work? What do they treat?

A

Treat angina and high bp
Blocks Ca2+ channels in membrane (discourages release from SR too) so no excitation/contraction coupling ->relaxation &dilation

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18
Q

Side effects of calcium channel blockers?

A

Vasodilator effects-headache
Reduced contractility- heart failure and peripheral oedema
Gut disturbance

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19
Q

Name the two classes of calcium channel blockers

A

Dihydropyridines and Non dihydropyridines

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20
Q

Name 4 calcium channel blockers of 2 classes

A

Dihydropyridines- Amlodipine, Nifedipine

Non-dihydropyridines- Diltiazem, Veapamil

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21
Q

What is Nifedipine?

A

A calcium channel blocker used to treat angina or high blood pressure

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22
Q

What do potassium channel openers treat and how?

A

Angina by causing hyperpolarisation of smooth muscle cells so Ca2+ channels resist opening
Also generates NO for venous dilation

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23
Q

Name a potassium channel opener and the type of channel it works on

A

Nicorandil- ATP-sensitive K+ channel

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24
Q

What is Nicorandil?

A

A K+ channel opener used to treat angina

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25
Q

Name 5 things that activate platelets

A

vWF, collagen, thrombin, ADP and thromboxane (TXA2)

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26
Q

Name 3 things that inhibit platelet aggregation

A

NO, ADPase, Prostacyclin (PGI2)

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27
Q

What are platelets?

A

Non nucleated fragments of megakaryocytes in bone marrow

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28
Q

What drug works by irreversibly inhibiting COX-1? How does this cause the effect?

A

Low dose aspirin (75mg/day), acetylation of COX-1 means reduced thomboxane (TXA2) synthesis so reduced platelet aggregation

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29
Q

What is low dose aspirin used for?

A

Frontline anti-platelet drug, used to prevent MI in patients with previous MI/angina

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30
Q

For thrombolysis after MI what drugs are used?

A

Medium dose aspirin (150-300mg) + Clopidogrel

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31
Q

What is Clopidogrel?

A

An anti platelet drug-
Non competitive antagonist, irreversibly blocks platelet ADP receptors (P2Y12) and reduced expression of gpIIb/gpIIIa and production of TXA2

32
Q

Problems with Clopidogrel?

A

Inter-individual variability (14% poor converters from prodrug by P450)
Side effects- GI bleeds and severe neutropenia

33
Q

Glycoprotein IIb/IIIa antagonists work by-

A

Blocking the GP IIb/IIIa receptors for fibrinogen, fibrin, collagen and vWF so disabling binding of platelets to subendothelium and thrombus formation

34
Q

Give 2 examples of GPIIb/IIIa antagonists and how they are administered

A

Abciximab- IV

Tirofiban- IV

35
Q

What is Tirofiban and when is it used?

A

Non peptide anti platelet drug (antagonist of gpIIb/IIIa)

Used in angioplasty procedures (eg stents) with Heparin and Aspirin

36
Q

Name 2 other anti platelet drugs

A

Dipyridamole

Epoprostenol

37
Q

How does Dipyridamole work?

A

Inhibits platelet phophodiesterase, increases cAMP, reduces aggregation and promotes vasodilation

38
Q

How does Epoprostenol work?

A

By mimicking anti-aggregatory effects of prostacyclin (PGI2) and increases cAMP to reduce platelet adhesion

39
Q

Name 3 thrombolytic drugs and how they work

A

Activate plasminogen to plasmin to degrade fibrin
Streptokinase (from streptococcus),
Anistreplase (acylated strep-plasmingogen complex), Urokinase (from human urine)

40
Q

Name 3 rt-PA drugs and why they are better than others

A

Alteplase, Reteplase, Tenecteplase

Recombinant tissue plasminogen activators so no allergies

41
Q

In acute MI what are the 4 stages of treatment?

A

Reduce anginal pain, initiate reperfusion, protect myocardium and secondary prevention

42
Q

What drugs are used to reduce anginal pain in acute MI?

A

Oxygen, GTN, Opiate and an anti-emetic (Metoclopramide)

Anti emetic= against vomiting and nausea

43
Q

What drugs are used to initiate reperfusion in acute MI?

A

Anti platelet (Clopidogrel, Aspirin)
Thrombolytic (rt-PA)
Primary angioplasty
Anticoagulant (Heparin)

44
Q

What drugs are used to protect the myocardium in acute MI?

A

ß-blocker and ACE inhibitor

45
Q

What does secondary prevention in acute MI involve?

A

Aspirin (low dose), lipid lowering drug (statin) and lifestyle changes

46
Q

Give 4 other approaches to deal with acute MI

A

Delivery of thrombolytic drugs with arterial catheter
PTCA (precutaneous transluminal coronary angioplasty)
Coronary stents
Artery/vein grafts to aorta

47
Q

Give 2 examples of ACE inhibitors

A

Captopril

Ramipril

48
Q

What is Captopril?

A

An ACE inhibitor used in heart failure and hypertension

49
Q

How do ACE inhibitors work?

A

By blocking conversion of AngI -> AngII
Inhibits breakdown of bradykinin- vasodilation, lowers bp & dry cough
Reduces preload, afterload and is antifibrotic

50
Q

Name 2 AT1 receptor antagonists

A

Losartan
Candesartan
(SARTAN)

51
Q

How do AT1 receptor antagonists work?

A

By inhibiting AngII actions

So antifibrotic, vasodilative (less NA release)

52
Q

Name 4 classes of anti-coagulant drugs

A

Warfarin, Heparins, Oligosaccharides, Direct thrombin inhibitors, Direct factor Xa inhibitors

53
Q

How does Warfarin work?

A

Inhibits decarboxylation of clotting factors by competing with Vit K (so clotting factors can’t be activated)

54
Q

What is the antidote for warfarin?

A

Vit K or plasma donation

55
Q

How is warfarin administered and what are its side effects?

A 
Administered orally (slow onset and offset)
Side effects= haemorrhage, crosses placenta, narrow therapeutic index and metabolised by P450
56
Q

What affects the metabolism of warfarin?

A

Alcohol& Cimetidine increase activity of warfarin
Phenobrabitone& Pheytoin decrease activity of warfarin
Antibiotics increase activity of warfarin (gut flora produce vit K which competes with warfarin)

57
Q

How do Heparins work?

A

By enhancing the activity of Anti-thrombin III 1000fold! which suppresses activity of thrombin and factor X
Heparin+ATIII+active clotting factor -> Inactive clotting factor+ATIII+Heparin

58
Q

Side effects of unfractionated Heparin and antidote

A

Haemorrhage (esp in elderly&heavy drinkers)
Osteoporosis (over several weeks)
Thrombocytopenia (not enough platelets in blood)

59
Q

Name 2 low MW heparins

A

Dalteparin and Enoxaparin

60
Q

Why are low MW better than unfractionated heparin?

A

Double the duration, 2xdaily SC injection, predictible effects and less risk of osteoporosis and thrombocytopenia

61
Q

How do Oligosaccharides work?

A

Anticoagulant,
Pentasaccharide unit binds to ATIII
Longer 1/2 life, parenteral

62
Q

Name an oligosaccharide and its purpose

A

Fondparinux, anti coagulant

63
Q

What is Fondparinux?

A

An oligosaccharide anti coagulant

64
Q

Name 2 direct thrombin inhibitors

A

Lepirudin

Dabigatran

65
Q

How do thrombin inhibitors work? How do you administer them?

A

Rapidly inhibit thrombin (so no fibrin activation) independently of ATIII
Lepirudin- parenteral as protein from leeches
Dabigatran- orally

66
Q

What is Lepirudin?

A

An anti coagulant

Direct thrombin inhibitor

67
Q

Name a direct factor Xa inhibitor

A

Rivaroxaban (XABAN)

68
Q

How do direct factor Xa inhibs work and how are they administered?

A

Inhibit activated factor X so prevent conversion of prothrombin->thrombin
Orally administered

69
Q

What is the main use for direct thrombin inhibitors?

A

For DVT prophylaxis

70
Q

What drugs are used in hypertension (in order of prescription)

A 
ACE inhibitors (or AngII receptor blocker) 
Calcium channel blockers
Diuretic (thiazide-like)
71
Q

What is the problem with dihydropyridine CCBs?

A

Reflex tachycardia when reduces peripheral resistance. Can cause peripheral oedema as only dilated arterial side so nowhere for fluid to go.

72
Q

Explain how non-dihydropyridines work

A

Block calcium channels with a negative chronotropic effect (slow SA firing) and negative inotropic effect (reduced contractility)

73
Q

Name 4 other types of anti-hypertensive drugs

A

Alpha-antagonists, K+ channel openers, nitrovasodilators and centrally acting SNS.

74
Q

What drug might be used to treat hypertension in pregnancy?

A

Alpha-antagonists eg Methyldopa.

Treats pre-eclampsia

75
Q

What are the centrally acting anti-hypertensives?

A

Imidazoline receptor agonists (eg Moxonidine)

Decreased SNS activity

76
Q

What factors need to be considered when treating hypertensive patients

A

White coat syndrome, age, ethnicity, pregnancy stage

Pharamacology (16 decks)

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