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Cardiology > Lecture 9 - Cardiovascular Pharmacology 2 > Flashcards

Lecture 9 - Cardiovascular Pharmacology 2 Flashcards

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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
Non-selective alpha - adrenergic receptors?
Short term management of pheochromocytoma - catecholamine secreting tumour - severe hypertension reflec tachycardia
26
Example of Non-selective alpha - adrenergic receptors
Phenoxybenzamine
27
Beta blocker to treat?
angina
28
What do beta blockers do?
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
What are the effects?
Decreased BP in hypertensives and reduced cardiac output, long term due to fall in peripheral vascular resistance
30
What are the classification of Beta blockers
``` 5 GROUPS Non-selective Beta anatagonists Non selective beta and alpha 1 antagonists beta 1 -selective antagonists beta 2 - selective antagonists partial agonists ```
31
non-selective beta antagonists
bind equally to beta 1 and beta 2 eg propanolol and timolol used in treatment of hypertension and angina 1st generation
32
Non selective beta and alpha 1 antagonists
Eg. Carvedilol used for treatment of Heart failure and labetalol in hypertension mainly in pregnancy and sever hypertension 3rd generation
33
Beta 1 selective antagonists
Cardioselective - atenolol metoprolol and bisoprolol - selectivity is dose related treatment for hypertension and angina
34
Higher dosages of what type of drug can cause Beta 2 receptor blockage
Beta 1 selective antagonists
35
Beta 2 selective antagonists
not clinically relevant as they will block receptors that help relaxation.
36
Partial agonists
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
Which class of beta blockers have reduced effect on carbohydrate metabolism
Partial agonists | pindolol and acebutalol
38
Cardiovascular use of beta blockers?
ischaemic heart disease (post mi and angina) , hypertension, heart failure, cardiac dysrhythmias
39
What is angina pectoris
Clinical manifestation of coronary heart disease
40
What happens in angina
Chest pain occurs when coronary blood flow is insufficient to supply O2 requirements of myocardium
41
What is stable angina
Plaque narrowed coronary artery. usually exercise induced
42
Unstable angina
Blocked coronary artery
43
Beta adrenergic receptor anatagonists and stable angina
decrease in heart rate prolongation of diastole -longer time for LV to perfuse Decrease in BP (reduced renin release and peripheral symp activity)
44
What is variant angina
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
Unstable angina
Patients at risk of MI Undergo PCI Long term treatment with aspirin, Beta blocker and ACE inhibitor
46
Normal blood pressure
120-135/70-85 mmhg
47
hypertension definition
BP more than 140/90
48
Target treatment for BP to becomeʔ
less than 140/90 for normal person | Diabetic - 130/80
49
What causes long term change in peripheral resistance in using beta blockers
inhibition of renin secretion bloackge of presynaptic beta receptors central effect from lipophilic beta receptors eg propanolol
50
Why does heart failure occur
insufficient cardiac output to adequately perfuse the tissues despite normal filling of the heart.
51
Symptoms of heart failure
fatigue, oedema, breathlessness and reduced exercise tolerance
52
Causes of heart failure
valvular disease, cardiomyopathy, and ChD
53
how to treat heart failure
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
important benefical effects of beta blockers
reduction in cardiac remodelling
55
3 licensed beta blockers for treatment of heart failure
Bisoprolol - beta 1 selective antagonist Carvedilol - non-selective beta blockers with alpha 1 blocking action nebivolol - b1 selective and nitric oxide activity
56
how do Class 2 antiarrhyhthmic agents (Beta blockers) actʔ
Act by inhibiting sympathetic input to the pacing regions of the heart (SA and AV nodes; β1-adrenergic receptors).
57
When are class 2 antiarrhythmic agents used (beta blockers) ʔ
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
What are the adverse effects of beta blockersʔ
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
Adverse effects of Beta blockers occurs whenʔ
As a consequence of blocking both beta 1 and beta 2 adrenergic receptors
60
What do calcium channel blockers act onʔ
smooth muscle and myocardium
61
What does the l-type calcium channel determineʔ
Vascular tone and cardiac contractility
62
3 classes of calcium channel blockers
Dihydropyridines - amlodipine , nifedipine - very little effect on cardiac tissue Benzothiazipines - diltiazem Phenylalkylamines - verapamil

Cardiology (12 decks)

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