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Cardiology > Lecture 9 - Cardiovascular Pharmacology 2 > Flashcards

Lecture 9 - Cardiovascular Pharmacology 2 Flashcards

1
Q

What does the sympathetic nervous system do?

A

Activation during exercise, excitement, and emergencies,

flight or fight

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2
Q

Parasympathetic?

A

Rest and digest
concerned with conserving energy
Symp and parasymp - anatagonistic - in a state of balance

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3
Q

Difference between paraympathetic and sympathetic axons?

A

Symp - highly branched

Parasymp = few branches

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4
Q

What are the neurotransmitters released by preganglionic axons?

A

Acetylcholine for both

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5
Q

What are the neurotransmitters released by postganglionic axons?

A

Symp - noradrenaline (adrenergic)

Parasymp - acetylcholine

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6
Q

What role does the adrenal medulla play in the sympathetic division?

A

Secretes adrenaline
Acetylcholine released by preganglionic fibres act on nicotinic acetylchloline receptors, causing chromaffin storage - cell depolarisation - calicum influx - triggers exocytosis of chromaffin granules and release of adrenaline

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7
Q

What sympathetic responses are observed?

A 
dilation of pupil
dilation of bronchioles
increased heart rate
blood vessel constriction
gastrointestinal relax
bladder relax
uterus relax
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8
Q

Synthesis of noradreanalin in sympathetic neurons

A

Synthesised from l-tyrosine
intermediate - L dopa and dopamine - made in cytoplasm
actively transported to storage vesicles where converted to NA

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9
Q

How is adrenalin synthesised in the medulla?

A

NA Converted to Adrenaline by enzyme phenylethanolamine n-methyl transferase in adrenal medulla

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10
Q

What are the classes of adrenergic receptors?

A

alpha - 1 and 2

beta - 1,2,3

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11
Q

Stimulation of alpha 1 receptor produces what second messenger?

A

inositol triphosphate and diacylglycerol . Gg mediated

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12
Q

What happens on stimulation of alpha 2 receptors?

A

Inhibition of adenylate cyclase and decreasing cAMP formation. Gi mediated

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13
Q

What happens on stimulation of B receptors?

A

activate adenylate cyclase, increasing cyclic AMP formation. Gs mediated.

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14
Q

Result of stimulation of alpha 1 and 2 receptors on smooth muscle cells

A

1 - contraction

2- inhibit release of noradrenaline (negative feedback)

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15
Q

Stimulation of Beta 1

A

Increases heart conduction, velocity

On kidneys - causes renin release (+ve feedback)

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16
Q

Stimulation of Beta 2

A

Smooth muscle relaxation
tremor in skeletal muscle
increases glycogenolysis in liver and skeletal muscle
(positive feedback)

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17
Q

Stimulation of Beta 3

A

lipolysis in fat cells

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18
Q

What does cAMP do?

A

Promote Ca2+ influx in response to membrane depolarisation - release of NA and ATP

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19
Q

alpha 1 - adrenergic receptor

A

stimulates contraction

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20
Q

alpha 2

A

inhibits nor adrenaline release

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21
Q

Beta1/2

A

stimulates noradrenaline relase

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22
Q

B2

A

stimulates relaxation

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23
Q

What are alpha adrenergic receptor blockers?

A

used in treatment of hypertension

inhibit vasomotor tone - reduce vasoconstriction - decrease resistance

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24
Q

Examples of alpha adrenergic receptor blockers

A

Doxazosin/Prazosin

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25
Q

Non-selective alpha - adrenergic receptors?

A

Short term management of pheochromocytoma - catecholamine secreting tumour - severe hypertension
reflec tachycardia

26
Q

Example of Non-selective alpha - adrenergic receptors

A

Phenoxybenzamine

27
Q

Beta blocker to treat?

A

angina

28
Q

What do beta blockers do?

A

block the positive chronotropic (rate) and ionotropic (activation of receptor) actions of endogenous catecholamines at Beta 1 adrenergic receptors - results in decreased heart rate and myocardial activity.

29
Q

What are the effects?

A

Decreased BP in hypertensives and reduced cardiac output, long term due to fall in peripheral vascular resistance

30
Q

What are the classification of Beta blockers

A 
5 GROUPS
Non-selective Beta anatagonists
Non selective beta and alpha 1 antagonists 
beta 1 -selective antagonists
beta 2 - selective antagonists
partial agonists
31
Q

non-selective beta antagonists

A

bind equally to beta 1 and beta 2
eg propanolol and timolol
used in treatment of hypertension and angina
1st generation

32
Q

Non selective beta and alpha 1 antagonists

A

Eg. Carvedilol used for treatment of Heart failure and labetalol in hypertension mainly in pregnancy and sever hypertension
3rd generation

33
Q

Beta 1 selective antagonists

A

Cardioselective - atenolol metoprolol and bisoprolol - selectivity is dose related
treatment for hypertension and angina

34
Q

Higher dosages of what type of drug can cause Beta 2 receptor blockage

A

Beta 1 selective antagonists

35
Q

Beta 2 selective antagonists

A

not clinically relevant as they will block receptors that help relaxation.

36
Q

Partial agonists

A

pindolol beta 1 and beta 2 receptor and acebutalol (B1) individuals with excessive bradychardia with sustained beta blocker therapy and diabetics. treatment of hypertension and diabetes

37
Q

Which class of beta blockers have reduced effect on carbohydrate metabolism

A

Partial agonists

pindolol and acebutalol

38
Q

Cardiovascular use of beta blockers?

A

ischaemic heart disease (post mi and angina) , hypertension, heart failure, cardiac dysrhythmias

39
Q

What is angina pectoris

A

Clinical manifestation of coronary heart disease

40
Q

What happens in angina

A

Chest pain occurs when coronary blood flow is insufficient to supply O2 requirements of myocardium

41
Q

What is stable angina

A

Plaque narrowed coronary artery. usually exercise induced

42
Q

Unstable angina

A

Blocked coronary artery

43
Q

Beta adrenergic receptor anatagonists and stable angina

A

decrease in heart rate
prolongation of diastole
-longer time for LV to perfuse
Decrease in BP (reduced renin release and peripheral symp activity)

44
Q

What is variant angina

A

artery spasms when at rest
beta blockers not given due to unopposed alpha adrenergic constriction of catecholamines
used a calcium channel blocker instead causes periphal arteriolar dilation and afterload reduction

45
Q

Unstable angina

A

Patients at risk of MI
Undergo PCI
Long term treatment with aspirin, Beta blocker and ACE inhibitor

46
Q

Normal blood pressure

A

120-135/70-85 mmhg

47
Q

hypertension definition

A

BP more than 140/90

48
Q

Target treatment for BP to becomeʔ

A

less than 140/90 for normal person

Diabetic - 130/80

49
Q

What causes long term change in peripheral resistance in using beta blockers

A

inhibition of renin secretion
bloackge of presynaptic beta receptors
central effect from lipophilic beta receptors eg propanolol

50
Q

Why does heart failure occur

A

insufficient cardiac output to adequately perfuse the tissues despite normal filling of the heart.

51
Q

Symptoms of heart failure

A

fatigue, oedema, breathlessness and reduced exercise tolerance

52
Q

Causes of heart failure

A

valvular disease, cardiomyopathy, and ChD

53
Q

how to treat heart failure

A

initially stabilise condition using ACE inhibitor (or ArB) and a diuretic
introduce Beta blockers gradually
beneficial effect is additive of ACE inhibitor and angiotensin 2 antagonist

54
Q

important benefical effects of beta blockers

A

reduction in cardiac remodelling

55
Q

3 licensed beta blockers for treatment of heart failure

A

Bisoprolol - beta 1 selective antagonist
Carvedilol - non-selective beta blockers with alpha 1 blocking action
nebivolol - b1 selective and nitric oxide activity

56
Q

how do Class 2 antiarrhyhthmic agents (Beta blockers) actʔ

A

Act by inhibiting sympathetic input to the pacing regions of the heart (SA and AV nodes; β1-adrenergic receptors).

57
Q

When are class 2 antiarrhythmic agents used (beta blockers) ʔ

A

treatment of supraventricular and ventricular arrhythmias
prevent tacchycardia induced by stress or exercise
reduce mortality in 1st year following myocardial infarction (prevents ventricular dysrhythmias?)

58
Q

What are the adverse effects of beta blockersʔ

A

Bronchoconstriction - in asthma patients
Cardiac failure - patients with heart disease may depend on sympathetic drive
Bradycardia - in patients with defects in AV conduction
abrupt discontinuation of long term treatment
Diabetic - mask warning signs (palpitations and tremor) of impending hypogylcaemia
prolong hypocglycaemia
fatigue
cold extremities (block of b2)
CnS effects

59
Q

Adverse effects of Beta blockers occurs whenʔ

A

As a consequence of blocking both beta 1 and beta 2 adrenergic receptors

60
Q

What do calcium channel blockers act onʔ

A

smooth muscle and myocardium

61
Q

What does the l-type calcium channel determineʔ

A

Vascular tone and cardiac contractility

62
Q

3 classes of calcium channel blockers

A

Dihydropyridines - amlodipine , nifedipine - very little effect on cardiac tissue
Benzothiazipines - diltiazem
Phenylalkylamines - verapamil

Cardiology (12 decks)

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