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Cardiology > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

3 beta adrenoreceptor agonists are?

A

dobutamine, adrenaline and noradrenaline (catecholamines)

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2
Q

All beta adrenoreceptor agonists will…

A

Produce an increase in force, rate and oxygen consumption but a decrease in cardiac efficiency.

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3
Q

Clinical uses of adrenaline?

A

IV injection in cardiac arrest

IM injection in anaphylaxis

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4
Q

Clinical use of dobutamine?

A

Acute but potentially reversible heart failure

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5
Q

Examples of beta blockers?

A
  • Beta 1 and 2= propranolol

* Beta 1 only= atenolol, bisoprolol, metoprolol

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6
Q

Atropine is a non-selective blocker of….

A

All acetyl choline muscarinic receptors

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7
Q

Effect of atropine? It is used in?

A

Increase in HR in normal subjects (at all but low doses)

First line in management of severe, or symptomatic bradycardia, particularly following myocardial infarction

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8
Q

Why must you give at least 300mg of atropine?

A

In low doses it makes bradycardia even worse

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9
Q

What does digoxin do?

A

Increases heart contractility

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10
Q

How does digoxin work?

A

It blocks the sodium potassium pump which results in increased calcium induced calcium release resulting in shortening of action potential and refractory period so force of contraction is increased.

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11
Q

Why and what are the side effects of digoxin?

A
  • Cardiac effects- propensity to cause arrhythmias and excessive depression of AV node conduction
  • Major 4- nausea, vomiting, diarrhoea and disturbances of colour vision

DUE TO NON-SELECTIVE BINDING TO Na/K ATPase

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12
Q

2 classes of drugs used to relax vascular smooth muscle?

A

Organic nitrates

Calcium channel blockers

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13
Q

Two examples of organic nitrate drugs and when are they used?

A

Glyceryltrinitrate (GTN) and isosorbide mononitrate (ISMN)

In all types of Angina

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14
Q

Describe GTN spray

A
  • Short acting only 30 mins.
  • It undergoes extensive first-pass metabolism (almost completely inactivated by the liver)
  • It is administered sublingually as a tablet or as a spray for rapid effect before exertion in stable angina or IV in conjunction with aspirin (in unstable angina)
  • More sustained effect if delivered by transdermal patch.
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15
Q

Describe ISMN

A
  • Longer-acting (t½ = 4 hours) – resistant to first-pass metabolism
  • Administered orally for prophylaxis and a more sustained effect (usually in the morning and at lunch)
  • Not used to relieve attacks only prevent.
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16
Q

Adverse effects of the organic nitrates?

A
  • Headaches may occur initially – due to arteriolar dilatation
  • Hypotension and fainting
  • Reflex tachycardia – prevented by co-administration of a β-blocker (which also improves stable and unstable angina by lowering myocardial oxygen requirement)
  • Formation of methaemoglobin (oxidation product of haemoglobin which does not carry oxygen) – rarely occurs.
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17
Q

Why is ISMN given in the morning and at lunch?

A

Allows a nitrate low period over night and in the evening meaning patients are less likely to develop a tolerance to it

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18
Q

What do calcium channel blockers do?

A

Calcium blockers physically block, or prevent the opening, of L-type channels in excitable tissues in response to depolarization and hence limit increased [Ca2+]i

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19
Q

Three main types of calcium channel blockers?

A
  • Verapamil- relatively selective for cardiac L-type channels- decrease in cardiac force- block the pore.
  • Amlodipine (dihydropyridine) compound- relatively selective for smooth muscle L-type channels)- act allosterically to prevent channel opening.
  • Dilitiazem- (intermediate selectivity)
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20
Q

What calcium blockers are used in hypertension and why?

A 
The dihydropyridines (amlodipine)
They have selectivity for smooth muscle L-type channels are preferred minimising the negative effects on the heart.
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21
Q

When are calcium channel blockers used in angina?

A

Prophylactic treatment, often used in combination with GTN particularly if beta-blockers are contraindicated

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22
Q

What does aliskerin do?

A

Inhibit the action of renin

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23
Q

What do ACE inhibitors do and example of one and adverse side effect?

A

Block conversion of angiotension 1 to angiotension 2. They also increase amount of bradykinin in the blood. Lisinopril. Dry cough.

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24
Q

What do Angiotension 1 receptor blockers do and when are they useful? (ARBs)

A

block the agonist action of angiotensin II at AT1 receptors in a competitive manner. Are useful as in patients who find the dry cough produced by ACEIs intolerable

25
Q

Clinical uses of ACE inhibitors and ARBs?

A

Hypertension, cardiac failure and following MI

26
Q

What are beta adrenoreceptor antagonists (beta blockers) no longer first line for? When are they used?

A

Hypertension

Used in treatment of heart failure in combination with other drugs to suppress adverse effects associated with elevated activity of the sympathetic nervous system and RAAS

27
Q

How do potassium channel openers work?

A

Cause hyperpolarization which switches off L-type Ca2+ channels . Act potently and primarily upon arterial smooth muscle resulting in relaxation of the smooth muscle.

28
Q

Examples of potassium channel openers?

A

Minoxidil and Nicorandil

29
Q

Examples and mechanisms of alpha 1 adrenoreceptor antagonists?

A

Cause vasodilatation by blocking vascular alpha 1-adrenoceptors. Reduced sympathetic transmission results in decreased MABP. The most frequently used compounds are prazosin and doxazosin – both are competitive antagonists.

30
Q

Anti cholesterol drugs?

A

Statins
Fibrates
PCSK 9 Inhibitors (used in familial hypercholesterolemia )

31
Q

Anti- hypertensive drugs?

A

1) Diuretics e.g. bendrofluazide and furosemide.
2) Beta blocker
3) Calcium channel blockers- dihydropyridines (amlodipine) and rate limiting calcium antagonists e.g. verapamil, dilitiazem.
4) Alpha blockers
5) ACE Inhibitors
6) Mineralcorticoid Antagonists

32
Q

Coronary artery disease common drugs?

A

1) Nitrates
2) Nicorandil- K ATP channel activator- lots of side effects- ulcers in GI tract and mouth, headache.
3) Ivabradine- If channel modulator in the sinus node (only works in someone in sinus rhythm). Altered visual disturbance
4) Ranolazine- Late sodium channel modulator, decrease calcium load on the heart, effective in refractory angina.

33
Q

Antiplatelet/thrombotic agents?

A

Aspirin, clopidogrel, plasugrel, ticagrelor

34
Q

Anticoagulant drugs?

A

Heparin, fondaparinux Warfarin, Rivaroxaban, Dabigatran, Edoxaban (oral)

35
Q

Heart failure drugs?

A
  • ACE Inhibitors
  • ARBs
  • Beta-blockers
  • Mineralocorticoid antagonists (Spironolactone, eplerenone)
  • Neprilysin inhibitors (salcubitril valsartan)
  • Diuretics
  • Digoxin
36
Q

Lipids e.g. ______1______ are insoluble in ___2____ and are transported in the plasma by _____3_____

A

1) triglycerides and cholesterylesters
2) water
3) lipoproteins that have a hydrophilic shell of phospholipids and free cholesterol

37
Q

The surface layer of lipoproteins is stabilised by…. these also act as…..

A

apoproteins which also act as ligands for cell surface receptors

38
Q

The four major types of lipoprotein are…

A

HDL, LDL, VLDL and chylomicrons

39
Q

Clearance of LDL particles is dependent upon? This is mainly expressed by the?

A

LDL receptor expressed by the liver

40
Q

Released cholesterol in the liver causes….

A

a decrease in LDL receptor expression

41
Q

How do statins work?

A

These inhibit HMG coA reductase which blocks synthesis of cholesterol in the liver leading to increased expression of LDL receptors which increases the clearance of cholesterol from the plasma.

42
Q

Adverse effects of statins? When are these effects more likely to occur?

A

Myositis (inflammation of muscles)
Very rarely rhabdomyolysis (death of muscle fibres).
Incidence is increased if the statin is combined with a fibrate.

43
Q

How do fibrates work?

A

Act as ligands for the nuclear transcription receptor PPARalpha to enhance the transcription of several genes including that encoding LPL. They cause a marked fall in plasma triglycerides.

44
Q

Fibrates are first line treatment for?

A

Those with very triglyceride levels.

45
Q

Adverse effects of fibrates?

A

More likely to happen if combined with statins is the myositis and rhabdomyolysis by also more risks of GI symptoms, pruritus and rash occurring.

46
Q

Examples of three bile acid binding resins?

A

Colestyramine, colestipol and colserelam

47
Q

How do bile acid binding resins work?

A

Cause the secretion of bile salts resulting in more cholesterol being converted to bile salts by interrupting enterohepatic recycling.

48
Q

Adverse effects of bile acid binding resins?

A

Can cause GI irritation

49
Q

How does ezetimibe work and when is it contraindicated?

A

Inhibits the transport protein in enterocytes of the duodenum reducing absorption of cholesterol. Contraindicated in breast feeding females.

50
Q

An arterial thrombus is __1___ and treated with ___2____

A venous thrombus is ___3___ and treated with __4____

A

1 white
2 anti-platelets
3 red
4 anticoagulants

51
Q

5 important anticoagulant drugs

A 
Rivaroxiban
Heparin
Fondaparinux
Dabigataran
Warfarin
52
Q

What does rivaroxiban directly inhibit?

A

Factor Xa

53
Q

Heparin inactivates both factor ____ and ____ via _____

A

Xa and lla

via anti-thrombin lll

54
Q

Fondaparinux and LMWHs only inactivate factor _____ via ______

A

Xa via anti-thrombin lll

55
Q

Warfarin works by blocking

A

Vitamin K reductase

56
Q

Dabigataran directly inhibits factor ____

A

lla

57
Q

Overdose of warfarin can be treated with

A

administration of vitamin K1 (as phytomenadione), or concentrate of plasma clotting factors (IV)

58
Q

What makes digoxin toxicity more likely/risky?

A

If patient is already on a lot of drugs ie someone in heart failure

59
Q

What drug can be used to treat VT?

A

Amiodarone

Cardiology (19 decks)

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