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PODT- Treatment > 6. Clinical Pharmacology of Adrenoceptor Antagonists > Flashcards

6. Clinical Pharmacology of Adrenoceptor Antagonists Flashcards

1
Q

What is the effect of adrenoceptors on the rate of contraction and what is the primary receptor?

A

Increase

Beta 1

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2
Q

What is the effect of adrenoceptors on cardiac conductivity and what is the primary receptor?

A

Increase

Beta 1

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3
Q

What is the effect of adrenoceptors on the force of contraction and what is the primary receptor?

A

Increase

Beta 1

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4
Q

What is the effect of adrenoceptors on the arteries and what is the primary receptor?

A

Constriction

alpha 1

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5
Q

What is the effect of adrenoceptors on the skeletal muscleand what is the primary receptor?

A

dilation

beta 2

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6
Q

What is the effect of adrenoceptors on the veins and what is the primary receptor?

A

constriction

alpha 1

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7
Q

What is the effect of adrenoceptors on the aiways and what is the primary receptor?

A

relax

Beta 2

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8
Q

What is the effect of adrenoceptors on the kidney and what is the primary receptor?

A

increased renin secretion

Beta 1

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9
Q

What is the effect of adrenoceptors on the peripheral sympathetic nerves and what is the primary receptor?

A

Increased release beta 2

Decreased release alpha 2

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10
Q

What is the effect of adrenoceptors on the decreased sympathetic outflow and what is the primary receptor?

A

Alpha 2

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11
Q

What is an adrenoceptor antagonist?

A

Drugs which occupy adrenoceptors and prevent the action of adrenaline and noradrenaline

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12
Q

What are examples of adrenoceptor antagonists?

A 
Beta blockers (-lol)
Alpha1 blockers (-osin)
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13
Q

What are the pharmacodynamic properties of beta adrenoceptor anatgonists?

A

Selectivity
Partial agonist activity
Additional actions

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14
Q

What are the pharmacokinetic properties of beta adrenoceptor anatgonists?

A

Solubility in water vs lipid
Ability to enter CNS
Route of elimination

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15
Q

What does a partial agaonist do?

A

Counter sympathetic hyperactivity

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16
Q

Why are partial agonists useful?

A

Advantageous in situations where some cardiac stimulation beneficial

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17
Q

Why are partial agonists useful?

A

Advantageous in situations where some cardiac stimulation beneficial

18
Q

What is the molecular mechanism of action of beta 1 adrenoceptor antagonists?

A

Stimulation of beta 1 adrenoceptors by adrenaline leads to activation of adenyalte cyclase and elevation of cAMP resulting in >contraction of heart muscle

This process is inhibited by beta1 adrenoceptor antagonists

19
Q

What is the action of cardiovascular blockers?

A

Reduce the heart rate, cardiac conductivity and force of contraction
Decrease cardiac work and oxygen demand
reduce blood pressure

20
Q

Why do beta- blockers lower blood pressure?

A

Initial fall in cardiac output then delayed indirect fall in peripheral vascular resistance and lead to a blood pressure decrease

21
Q

What are the uses of beta blockers?

A 
Arhythmias 
angina pectoris 
post MI 
heart failure 
Migraine 
glaucoma 
physical effects of anxiety
22
Q

What is the use of beta blockers and hypertension?

A

Less widely used now just for hypertension in absence of other compelling indications

23
Q

What are the anti-arrythymic affects of beta-blockers?

A

Sympathtetic effects on automaticity and conductivity
-periods of abnormally fast heart beat arising in upper chambers of the heart

Management of atrial fibirilation
-chaotic electrical activity in atria resulting in irregularly irregular rhythm, pumonig of the heart is less sufficient

Useful for rate control : AV node to decrease the number of impulses that conduct into ventricles

24
Q

How are beta blockers used in angina pectoris?

A

Used in prophylaxis of stable angina

Blunt sympathetic response to excersize
Reduce myocardial oxygen demand by reducing heart rate and contracitilty
Prolonged diastole also imprves perfusion of sub-endocardial myocardium and oxygen supply

25
Q

What are the reasons for benefits post MI?

A

Decrease in cardiac work and oxygen demand
Attenuate ventricular remodelling
Decrease in incidence of supra ventricular tachycardias
Decrease in incidence of ventricular dysrrhythmias

26
Q

Why are beta beta blockers useful in heart failure?

A

Reduce mortaility in all grades of heart failure
Reduce morbidity
Improve symptoms, excersize tolerance, cardiac function

27
Q

What is the benefits of reduced heart rate?

A

Prolong diastole, improve chamber filling

Reduce ischaemia

28
Q

What are further additional uses of beta blockers?

A

Prophylaxis of migraine attack
Topically in glaucoma
Symptomatic relief in anxiety

29
Q

What are adverse effects of beta blockers?

A 
Bradycardia 
Heart block 
Central effects 
Beta 2 adrenoceptor antagonism
Adverse metabolic effects
30
Q

What is bradycardia?

A
  • lowered HR leading to reduced CO - hypotension- fainting/weak/dizzy
  • less marked with partial agonists
31
Q

What is meant by heart block?

A

impaired conduction of electrical impulse from atria to ventricles resulting in dropped beats

32
Q

What are adverse central effects of beta blockers?

A

fatigue
nightmares etc
less lipid soluble

33
Q

What is mean by beta 2 adrenoceptor antagonism?

A

Poor tissue perfusion in PVD IC
exacerbation of Raynauds
COld hands and feet
Bronchospasm in asthmatics

34
Q

What are adverse metabolic effects of beta-blockers?

A

Prolonged hypoglycaemia
Interfere with autonomic and metabolic repsonses to hypoglycaemia, worsening glycaemic control
Tendency to dyslipidaemia

35
Q

What are contra-indications of beta blocker use?

A 
Bradycardia and heart block
asthma 
Acute decompensated heart failure
Type 1 diabetes mellitus
Claudication
36
Q

What are some side effects of beta blockers?

A

Hypertension
Angina pectoris/ myocardial ischaemia
acute MI

37
Q

What is the explanation of the adverse side effects of beta blockers?

A

Rebound sympathetic stimulation of heart following prolonged beta receptor blockade

38
Q

What are other drugs which slow the heart/ depress cardiac function?

A

Rate-limiting calcium channel modulators

39
Q

What is the cardiovascular effects of alpha adrenoceptor antagonists?

A

Reduce peripheral vascular resistance
-antagonise postsynaptic adrenoceptors BUT
cause rebound increase in HR, cardiac output and oxygen demand

40
Q

What are the clinical uses of alpha adrenoceptor antagonists?

A

Management of resistant hypertension
Hypertension secondary to phaeochromocytoma
Relieve urinary retention in prostate hyperplasia

PODT- Treatment (12 decks)

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