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Pharamacology > Cardiovascular > Flashcards

Cardiovascular Flashcards

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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
Name 5 things that activate platelets
vWF, collagen, thrombin, ADP and thromboxane (TXA2)
26
Name 3 things that inhibit platelet aggregation
NO, ADPase, Prostacyclin (PGI2)
27
What are platelets?
Non nucleated fragments of megakaryocytes in bone marrow
28
What drug works by irreversibly inhibiting COX-1? How does this cause the effect?
Low dose aspirin (75mg/day), acetylation of COX-1 means reduced thomboxane (TXA2) synthesis so reduced platelet aggregation
29
What is low dose aspirin used for?
Frontline anti-platelet drug, used to prevent MI in patients with previous MI/angina
30
For thrombolysis after MI what drugs are used?
Medium dose aspirin (150-300mg) + Clopidogrel
31
What is Clopidogrel?
An anti platelet drug- Non competitive antagonist, irreversibly blocks platelet ADP receptors (P2Y12) and reduced expression of gpIIb/gpIIIa and production of TXA2
32
Problems with Clopidogrel?
Inter-individual variability (14% poor converters from prodrug by P450) Side effects- GI bleeds and severe neutropenia
33
Glycoprotein IIb/IIIa antagonists work by-
Blocking the GP IIb/IIIa receptors for fibrinogen, fibrin, collagen and vWF so disabling binding of platelets to subendothelium and thrombus formation
34
Give 2 examples of GPIIb/IIIa antagonists and how they are administered
Abciximab- IV | Tirofiban- IV
35
What is Tirofiban and when is it used?
Non peptide anti platelet drug (antagonist of gpIIb/IIIa) | Used in angioplasty procedures (eg stents) with Heparin and Aspirin
36
Name 2 other anti platelet drugs
Dipyridamole | Epoprostenol
37
How does Dipyridamole work?
Inhibits platelet phophodiesterase, increases cAMP, reduces aggregation and promotes vasodilation
38
How does Epoprostenol work?
By mimicking anti-aggregatory effects of prostacyclin (PGI2) and increases cAMP to reduce platelet adhesion
39
Name 3 thrombolytic drugs and how they work
Activate plasminogen to plasmin to degrade fibrin Streptokinase (from streptococcus), Anistreplase (acylated strep-plasmingogen complex), Urokinase (from human urine)
40
Name 3 rt-PA drugs and why they are better than others
Alteplase, Reteplase, Tenecteplase | Recombinant tissue plasminogen activators so no allergies
41
In acute MI what are the 4 stages of treatment?
Reduce anginal pain, initiate reperfusion, protect myocardium and secondary prevention
42
What drugs are used to reduce anginal pain in acute MI?
Oxygen, GTN, Opiate and an anti-emetic (Metoclopramide) | Anti emetic= against vomiting and nausea
43
What drugs are used to initiate reperfusion in acute MI?
Anti platelet (Clopidogrel, Aspirin) Thrombolytic (rt-PA) Primary angioplasty Anticoagulant (Heparin)
44
What drugs are used to protect the myocardium in acute MI?
ß-blocker and ACE inhibitor
45
What does secondary prevention in acute MI involve?
Aspirin (low dose), lipid lowering drug (statin) and lifestyle changes
46
Give 4 other approaches to deal with acute MI
Delivery of thrombolytic drugs with arterial catheter PTCA (precutaneous transluminal coronary angioplasty) Coronary stents Artery/vein grafts to aorta
47
Give 2 examples of ACE inhibitors
Captopril | Ramipril
48
What is Captopril?
An ACE inhibitor used in heart failure and hypertension
49
How do ACE inhibitors work?
By blocking conversion of AngI -> AngII Inhibits breakdown of bradykinin- vasodilation, lowers bp & dry cough Reduces preload, afterload and is antifibrotic
50
Name 2 AT1 receptor antagonists
Losartan Candesartan (SARTAN)
51
How do AT1 receptor antagonists work?
By inhibiting AngII actions | So antifibrotic, vasodilative (less NA release)
52
Name 4 classes of anti-coagulant drugs
Warfarin, Heparins, Oligosaccharides, Direct thrombin inhibitors, Direct factor Xa inhibitors
53
How does Warfarin work?
Inhibits decarboxylation of clotting factors by competing with Vit K (so clotting factors can't be activated)
54
What is the antidote for warfarin?
Vit K or plasma donation
55
How is warfarin administered and what are its side effects?
``` Administered orally (slow onset and offset) Side effects= haemorrhage, crosses placenta, narrow therapeutic index and metabolised by P450 ```
56
What affects the metabolism of warfarin?
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
How do Heparins work?
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
Side effects of unfractionated Heparin and antidote
Haemorrhage (esp in elderly&heavy drinkers) Osteoporosis (over several weeks) Thrombocytopenia (not enough platelets in blood)
59
Name 2 low MW heparins
Dalteparin and Enoxaparin
60
Why are low MW better than unfractionated heparin?
Double the duration, 2xdaily SC injection, predictible effects and less risk of osteoporosis and thrombocytopenia
61
How do Oligosaccharides work?
Anticoagulant, Pentasaccharide unit binds to ATIII Longer 1/2 life, parenteral
62
Name an oligosaccharide and its purpose
Fondparinux, anti coagulant
63
What is Fondparinux?
An oligosaccharide anti coagulant
64
Name 2 direct thrombin inhibitors
Lepirudin | Dabigatran
65
How do thrombin inhibitors work? How do you administer them?
Rapidly inhibit thrombin (so no fibrin activation) independently of ATIII Lepirudin- parenteral as protein from leeches Dabigatran- orally
66
What is Lepirudin?
An anti coagulant | Direct thrombin inhibitor
67
Name a direct factor Xa inhibitor
Rivaroxaban (XABAN)
68
How do direct factor Xa inhibs work and how are they administered?
Inhibit activated factor X so prevent conversion of prothrombin->thrombin Orally administered
69
What is the main use for direct thrombin inhibitors?
For DVT prophylaxis
70
What drugs are used in hypertension (in order of prescription)
``` ACE inhibitors (or AngII receptor blocker) Calcium channel blockers Diuretic (thiazide-like) ```
71
What is the problem with dihydropyridine CCBs?
Reflex tachycardia when reduces peripheral resistance. Can cause peripheral oedema as only dilated arterial side so nowhere for fluid to go.
72
Explain how non-dihydropyridines work
Block calcium channels with a negative chronotropic effect (slow SA firing) and negative inotropic effect (reduced contractility)
73
Name 4 other types of anti-hypertensive drugs
Alpha-antagonists, K+ channel openers, nitrovasodilators and centrally acting SNS.
74
What drug might be used to treat hypertension in pregnancy?
Alpha-antagonists eg Methyldopa. | Treats pre-eclampsia
75
What are the centrally acting anti-hypertensives?
Imidazoline receptor agonists (eg Moxonidine) | Decreased SNS activity
76
What factors need to be considered when treating hypertensive patients
White coat syndrome, age, ethnicity, pregnancy stage

Pharamacology (16 decks)

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