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02. Cardiovascular > L17. Drugs Influencing the CVS > Flashcards

L17. Drugs Influencing the CVS Flashcards

1
Q

What is the clinical definition of hypertension?

A

Blood pressure > 140/90 mmHg

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2
Q

Hypertension is a risk factor for…

A 
Stroke
MI, Ischaemic heart disease, chronic heart failure
Aortic aneurysm, retinal haemorrhage
Renal Failure
Death
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3
Q

What are the risk factors for developing hypertension?

A

A multifactorial disease:

Smoking, diet, weight, stress, family Hx

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4
Q

What is the aim for hypertension therapies?

A

Reduce the blood pressure below 140/85
Or below 130/80 for diabetic for obese patients
Mainly achieved by reducing the risk factors

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5
Q 
For Homeostatic control of blood pressure:
Regulated variable is \_\_\_\_
Sensors \_\_\_\_
Controlled variables \_\_\_\_\_\_
Effectors \_\_\_\_\_ 
Effector Signals \_\_\_\_\_\_\_
A

Regulated variable is __Blood Pressure__
Sensors __Baroreceptors and Osmoreceptors__
Controlled variables __HR and SV (CO) and TPR____
Effectors __Blood vessels, Heart and Kidney___
Effector Signals __Neuronal and Hormonal__

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6
Q

Which system (Para or symp) takes precedence in controlling BP?

A

Sympathetic is the major regulator for changing blood pressure (parasympathetic is for rest situations)

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7
Q

What receptors to noradrenaline and adrenaline act on to control blood pressure?

A

alpha 1 adrenoreceptors in the blood vessels

beta 1 adrenoreceptors in the heart and in the kidneys

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8
Q

What are the main results of adrenaline acting on these receptors in blood y
pressure regulation?

A

Vasoconstriction
Increased HR
Increased Contractility
Increased Blood Volume

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9
Q

Describe the Renin-Angiotensin System

A

Noradrenaline binding to B1 receptors in the kidney
Stimulates secretion of renin by the kidney
Converts angiotensinogen into angiotensin I
ACE converts angiotensin I into angiotensin II
Angiotensin II

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10
Q

What are the main actions of Angiontensin II?

A 
Acts on AT1 receptors: Vasoconstriction of blood vessels
Acts on AT1 receptors: Release of aldosterone leading to salt and water retention
Cell growth (hypertrophy of the heart) 
Positive feedback to sympathetic nervous system (increase noradrenaline)
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11
Q

Why would we use Angiotensin Converting Enzyme Inhibitors (ACE inhibitors) in hypertension?

A

They prevent the conversion of AngI to AngII: reducing vascular tone, reducing aldosterone production (reduces water retention, reduces SV) and reduces cardiac hypertrophy

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12
Q

What is another mechanism of ACE inhibitors (involving bradykinin)?

A

ACE works like Kininase II: breaks down bradykinin

ACE inhibitors prevent bradykinin breakdown allowing it to have longer potent vasodilatory effects

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13
Q

What are the adverse effects of ACE inhibitors?

A 
Dose Dependent:
First dose hypotension
dry cough
loss of taste
hyperkalaemia (often given in combination with diuretics)
Acute renal failure
Itching, rash, angio-oedema
Foetal malformations
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14
Q

What are some contraindicators of ACE inhibitors?

A

Pregnancy
Bilateral renal stenosis
Angio-neurotic oedema

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15
Q

What are some examples of ACE inhibitors?

A 
The -PRILS
Captopril
Perindopril
Enalapril
Ramipril
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16
Q

What are the antiotensin receptor antagonists?

A

The SARTANS
Losartan
Candesartan

17
Q

What happens with you block the AT receptors?

A 
AT1 and AT2
Reduce vasoconstriction
Reduce aldosterone formation
Reduce cardiac hypertrophy
Reduce sympathetic activity (inhibits the positive feedback)
18
Q

What is the major difference between AT antagonists and ACE inhibitors (that it thought to make them safer)?

A

AT antagonists do not have an effect on bradykinin

19
Q

What are the adverse effects of AT antagonists?

A

Hyperkalaemia
Headache
Dizziness

20
Q

What are the contraindications for AT antagonists?

A

Contraindicators are the same for the ACE inhibitors:
Pregnancy
Bilateral renal stenosis
Angio-neurotic oedema

21
Q

What are the b1 adrenoreceptor antagonists?

A 
The -OLOLS
Propanolol
Timolol (nonselective)
atenolol
metoprolol (b1 selective)
pindolol (partial agonist for b1 and b2)
22
Q

What is the aim of using B1 adrenoreceptor antagonists in hypertension?

A

Reduce the Cardiac Output and reduce renin release (decreases blood volume) by preventing sympathetic innervation

23
Q

How to the B blockers vary within the class? [3]

A
  1. Vary with selectivity (for receptors)
  2. With intrinsic sympathomimetic activity (eg. partial agonist activity)
  3. Vary with lipid solubility (eg. ability to cross the blood brain barrier)
24
Q

What are the adverse effects of b adrenergic receptor antagonists?

A

Cold extremities: occurs acutely when CO is dropped by the drug, a reflex alpha 1 constriction occurs
Fatigue: puts a limit on the sympathetic nervous system to increase HR and blood vessel supply
Dreams and insomnia (CNS lipid solubility)
Bronchoconstriction (B2 adrenoreceptor blockage)

25
Q

What are some contraindications for b1 adrenergic receptor antagonists?

A

Asthma
Diabetes
AV conduction block
Must take care with heart failure and metabolic syndrome

26
Q

What are the Calcium Channel Blockers?

A

Vermpamil
Diltiazem

Dihydropyridines: felodipine and nifeipine

27
Q

What is the mechanism of action of the Calcium channel blockers in hypertension?

A

Inhibit voltage gated L-type Calcium channels in the myocardium and the vasculature.
= reduced cardiac and vascular contractility
= Reduced vascular resistance

28
Q

What are the 2 types of calcium channel blockers?

A
  1. reduce cardiac and vascular contractility

2. Reduce vascular resistance

29
Q

What are the adverse effects of calcium channel blockers?

A

Oedema, flushing, headache
Bradycardia (for reduced cardiac contractility)
Reflex tachycardia (for reduced vascular resistance)

30
Q

What is the mechanism of action of thiazide diuretics in terms of hypertension?

A

Inhibit NaCl co-transporter in the distal convoluted tubule of the kidneys leading to decreased reabsorption: increases the Na and water excretion form the kidney
Also has a loss of K from the collecting duct
= lowers blood volume

31
Q

What is an example of a thiazide diuretic used in hypertension?

A

Hydrochlorothiazide

32
Q

What is an adverse effect of the thiazide diauretics?

A

Hypokalaemia: Loss of K leading to gout, hyperglycaemia and allergic reactions

33
Q

What are some other drugs used in hypertension (when the main ones don’t work)?

A

Alpha 1 adrenoreceptor antagonists
Vasodilators
alpha 2 antagonists (CNS)
New renin inhibtors

34
Q

What are the main drugs used to combat hypertension?

A 
ABCD
Angiotensin System Inhibitors
B-adrenoreceptor antagonists
Calcium channel blockers
Diuretics
35
Q

Why do we have so many anti-hypertensive drugs?

A

Because it is a multifactorial disease with both neural and hormonal control
Multiple target organs, signals and proteins

Often use a combination of drugs

02. Cardiovascular (43 decks)

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