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Biomedical Pharmacology > Lecture 12 - Cardiovascular Pharmacology > Flashcards

Lecture 12 - Cardiovascular Pharmacology Flashcards

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1
Q

What is hypertension?

A

Elevated blood pressure

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2
Q

What is the blood pressure of a healthy person?

A

120/80

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3
Q

Why does blood pressure increase with age?

A

Lifestyle effects
Natural aging process
Hardening of arteries (less distensible)

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4
Q

What is blood pressure controlled by?

A

Integrated system P

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5
Q

What are the primary contributors of blood pressure?

A

Cardiac output
Stroke volume
Heart rate
Total peripheral resistance

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6
Q

What can each of the factors that contribute to blood pressure be manipulated by?

A

Drug therapy

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7
Q

What happens when blood pressure goes down?

A

The sympathetic vasomotor centre activity increases in the brain due to activation of baroreceptors

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8
Q

What elevates blood pressure?

A

Cardiac stimulation
Activation of sympathetic nervous system
Venous constriction
Increasing venous rerun
Increase preload and force of contractility

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9
Q

How does cardiac stimulation increase cardiac output?

A

In terms of heart rate and force of contraction

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10
Q

What happens when blood pressure decreases?

A

Cause renin release

Due to reduced blood flow through juxtaglonerular apparatus

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11
Q

What are the effects of Angiotensin II?

A 
Venous constriction (elevate venous return)
Arterial constriction 
Knock on effect of aldosterone
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12
Q

What are the processes that bring BP down?

A

Arterial constriction
Increase in sympathetic vasomotor centre activity
Renin release
Venous constriction

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13
Q

What is the vasomotor centre?

A

Influences sympathetic outflow
Alpha 2 adrenoceptor agonist
Presynaptic modulation of neurotransmitter release

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14
Q

What does the sympathetic nerve terminal release?

A

Noradrenaline

Influences postsynaptic receptors

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15
Q

Where are alpha 2 adrenoceptor located?

A

Sympathetic nerve terminal

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16
Q

What happens when alpha 2 adrenoceptor is stimulated?

A

Negative effect mediated via influence on ca2+ channel opening
Decreases continued release of noradrenaline

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17
Q

What is Beta receptor antagonist (blockers)?

A

Direct effect on the heart (Beta 1 receptors)

Reduce contractility of the heart (reduce cardiac output - reduce BP)

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18
Q

What is vascular smooth muscle?

A

Vasodilators
Ca2+ channel antagonist
Angina and treatment of hypertension
Some diuretics - some vasodilatory effect

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19
Q

What is AT1 receptors?

A

Block synthesis of Angiotensin II or blocking the receptors itself

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20
Q

What is the effect of ACE inhibitors?

A

Influence adrenal cortex

Reduce effect of Angiotensin II

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21
Q

In the kidney, what does diuretics have an effect in?

A

Reducing overall circulating blood volume

Reduce blood pressure

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22
Q

What is the therapeutic approaches to treatment of hypertension?

A 
Vasomotor centre 
Sympathetic nerve terminals
Beta-adrenoceptors on heart 
Sympathetic Ganglia 
Angiotensin receptors on vessels 
Alpha-adrenoceptors on vessels
Vascular smooth muscle 
Adrenal cortex 
Kidney tubules 
Juxtaglomerular cells that release renin
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23
Q

Vasomotor centre

A

Alpha 2- Adrenoceptor agonists

Imidazoline receptor agonist

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24
Q

Sympathetic nerve terminals

A

Adrenergic neuron Antagonist

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25
Beta-adrenoceptors on heart
B-adrenoceptor Antagonist
26
Sympathetic Ganglia
Ganglion blockers
27
Angiotensin receptors on vessels
ACE inhibitors | AT1 receptor antagonist
28
Alpha- Adrenoceptor on vessels
Alpha 1 Antagonist
29
Vascular smooth muscle
``` Diuretics Vasodilators Nitrovasodilafors Calcium channel Antagonist Potassium channel openerds ```
30
Adrenal cortex
ACE Inhibitors of Angiotensin II formation | AT1 receptor antagonist
31
Kidney tubules
Diuretics | ACE inhibitors
32
Juxtaglomerular cells that release renin
B-Adrenoceptor Antagonist
33
B-adrenoceptor Antagonist
Pindolol Atenolol Propranolol
34
What is B-adrenoceptor Antagonist most important actions
B1 receptor blockade Decreased heart rate and cardiac output Reduced renin secretion
35
What is adrenoceptor Antagonist aided by?
Vasodilation of blood vessels supplying skeletal muscle
36
What happens when Beta receptors are stimulated?
Vascular muscle relaxation
37
What does some of Beta adrenoceptor agonist have?
Partial antagonist and partial agonist activity
38
What is pindolol?
Used for hypertension | Beta 1 Antagonist and Beta 2 partial agonist
39
What are some examples of alpha-adrenoceptor Antagonist?
Prazosin Doxazosin Phenoxybenzamine
40
What is alpha-adrenoceptor Antagonist?
Involves the reduction of arteriolar resistance By reducing sympathetic input Mediated by alpha 1 receptors
41
What is the result of stimulating alpha 1 receptors?
Contract smooth muscle
42
What is the result of blocking alpha 1 receptors?
Relaxation | Dilation of venous capacitance vessels
43
What happens at rest of alpha-adrenoceptor antagonist?
Ongoing sympathetic tone | Governing the overall diameter of blood vessels
44
What is the problem of alpha-adrenoceptor Antagonist?
Induce a reflex tachycardia Marked with non-selective compounds Can increase HDL
45
What is prazosin?
Short acting
46
What is doxazosin?
Long acting
47
What are the side effects related to the relaxtory effect upon smooth muscle (alpha-adrenoceptor Antagonist)
Postural hypotension (venous pooling) Legarthy (drowsy and dull) Palpitations
48
What are ACE inhibitors?
Reduce circulatory level of Angiotensin II | Block conversion from Angiotensin
49
What are examples of ACE inhibitors?
Captopril | Enalapril
50
What are the therapeutic effect of ACE inhibitors?
Hypotensive effect without reflex tachycardia (through relaxation of smooth muscle) Reduced aldosterone release Reversal of left ventricular hypertrophy Prevention of vascular changes by inhibition of cellular growth Reduced degradation of vasodilator kin in
51
What does Kinin have and is responsible for?
Vasodilatory effect | Responsible for inhibiting cough
52
What is Angiotensin receptor antagonist?
Block what Angiotensin II does at relevant receptor | AT1 receptor seen in vascular smooth muscles
53
What are examples for Angiotensin receptor antagonist?
Losartan | Valsartan
54
What are the side effects of Angiotensin receptor antagonist?
Headache | Legarthy
55
What is ACE inhibitor
Enalapril
56
What is Angiotensin inhibitor?
Valsartan
57
What are examples of directly acting vasodilators?
Calcium channel antagonist | Potassium channel activators
58
What does minoxidil lead to?
Hair growth
59
What are side effects of directly acting vasodilators?
``` Flushing and headache Reflex tachycardia Palpitations Salt and water retention Hirsutism (abnormal growth of hair on a woman’s face and body) ```
60
What is Hydralazine?
Produces relaxation
61
What are the side effects of Hydralazine?
Side effects include reflex sympathetic activation and SLE like syndrome
62
When is borderline hypertension more likely to be treated?
If patient has renal impairment Ischaemic heart disease Diabetes Previous stroke
63
Young: treatment of hypertension
B-adrenoceptor antagonist/ACE inhibitors
64
Elderly: treatment of hypertension
Ca2+ channel antagonist | Diuretics
65
What is an example of centrally active hypertensive ?
Methyldopa
66
What are the approaches to treating hypertension?
Step 1: one/two drug in the young beta-blocker or ACE inhibitor Step 2: getting no response, look at combining Step 3: if there is still no response, combine 2-3 compounds Step 4: look g at putting in another drug
67
What is the best approach to treating hypertension?
Single pill combining many different active compounds
68
What is Atherosclerosis?
Plaque formation Plaque rupture Thrombus formation Death and disability caused by heart attack
69
How is Atherosclerosis formed?
Cholesterol ridge core
70
Where is cholesterol embedded in?
Plaque because of removal from circulation
71
Where does plaque protrude as it grows?
Lumen of the blood vessels Reduces diameter of the blood vessel Reducing BF to one region
72
What happens when cap is eroded and exposed to the core?
Aggregation and activation of platelets which adhere to the Atherosclerosis plaque
73
Why is platelet aggregation a problem?
Blood clotting mechanism get involved
74
Why is cholesterol important?
Constituent of cell membrane | Precursor of many important steroids (bile salt, steroid hormones)
75
Where is cholesterol mainly synthesised?
Liver | HMG-CoA reductase
76
Where are LDL taken up by?
Liver (receptor mediated l) | Taken up into peripheral tissues (non-receptor mediated)
77
Why are HDL classified as good cholesterol?
Promote transport from peripheral tissues to liver Promote storage of LDL Removal from circulation
78
What are two pathways by which cholesterol accumulates in the liver?
Exogenous pathway | Endogenous pathway
79
Where does cholesterol come from?
Diet (direct circulation through portal system) | Or with fatty acids in diet combined with glycerol and cholesterol which are absorbed into bloodstream
80
What does chylomicrons contain?
Both cholesterol and triglycerides
81
What are chylomicrons?
Lipoprotein lipase which acts upon triglycerides breaking them down into free fatty acids which can be absorbed into peripheral tissue
82
How is cholesterol moved out of the liver?
In the form of very low LDL
83
Why is the endogenous pathway favoured?
Majority of cholesterol is synthesised from acetyl cOA
84
What is Dyslipidaemia?
Condition where lipid processing is disrupted Inherited disorder - altered synthesis of cholesterol familial hypercholesterolmia Diseases affecting lipid metabolism
85
What does Frederickson classification define?
Six groups based on which lipoprotein is elevated
86
What groups are most at risk of atheroma?
Groups IIa and IIb
87
What groups are triglyceride elevated in?
Type IIb but not in type 2a
88
When are Statins prescribed?
When there is an incidence of increased LDL cholesterol
89
What are examples of statin?
Simvastatin Lovostatin Pravastatin Atorvastatin
90
What does station reduce?
LDL cholesterol | Risk of death from cardiovascular events
91
Who should statins be considered for?
All patients at risk of any cardiovascular disease
92
When are Fibrates used?
Where there is an issue with cholesterol and triglycerides
93
What does fibrates have an influence upon?
Certain nuclear receptors
94
What is example of nuclear receptor?
PPARa These nuclear receptors will translocate to the nucleus when a relevant agonist binds to them Alteration in transcription of genetic material
95
What are examples of Fibrates?
Bezafibrate Gemfibrozil Ciprofibrate
96
What does Bezafibrate have significant effect upon?
Genes that code for lipases that can break down Chylomicrons

Biomedical Pharmacology (19 decks)

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