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A. General Pharmacology > 1. Adrenergics & Antiadrenergics > Flashcards

1. Adrenergics & Antiadrenergics Flashcards

1
Q

What is the pre-cursor to norepinephrine

A

Dopamine

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2
Q

Rate-limiting enzyme for the biosynthesis of catecholamines

A

Tyrosine hydroxylase

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3
Q

Role of alpha 1 and alpha 2 adrenoceptors

A
  1. Vasoconstriction in visceral organs, mucous membranes and small blood vessels
  2. Shutting down GI and visceral functions
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4
Q

Role of beta 1 and beta 2 adrenoceptors

A
  1. Vasodilation of blood vessels supplying skeletal muscles
  2. Stimulation of the heart (mainly beta 1)
  3. Bronchodilation in the lungs (mainly beta 2)
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5
Q

Role of beta 3 adrenoceptors

A
  1. Lipolysis
  2. Thermogenesis
  3. Relax bladder
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6
Q

Types of direct adrenergic agents

A 
alpha 1: phenylephrine 
alpha 2: brimonidine 
non-selective alpha: oxymetazoline 
beta 1: dobutamine 
beta 2: salbutamol, terbutaline
beta 3: mirabegron 
non-selective beta: isoprenaline 
alpha 1 & beta 1: dopamine 
beta 3: mirabegron 
both alpha and beta: noradrenaline (more selective at alpha) & adrenaline (more selective at beta)
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7
Q

Uses for noradrenaline

A

severe hypotension

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8
Q

Uses for adrenaline

A
  1. anaphylactic shock
  2. cardiac resuscitation
  3. with local anaesthetics
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9
Q

Uses for dopamine

A
  1. cardiac resuscitation

2. severe hypotension

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10
Q

Major adverse effects of noradrenaline, adrenaline and dopamine

A
  1. hypertension
  2. tachycardia
  3. reflex bradycardia
  4. ventricular arrhythmias
  5. necrosis due to vasoconstriction at site of injection
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11
Q

Uses for oxymetazoline

A

nasal decongestant

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12
Q

Major adverse effect of oxymetazoline

A

rebound congestion

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13
Q

Uses for phenylephrine

A
  1. hypotension

2. nasal decongestant

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14
Q

Major adverse effect of phenylephrine

A
  1. hypertension

2. reflex bradycardia

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15
Q

Uses for brimonidine

A

open-angle glaucoma (topical to eye)

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16
Q

Major adverse effect of brimonidine

A
  1. hypotension (compare with systemic clonidine)
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17
Q

Uses for isoprenaline

A
  1. asthma

2. cardiac resuscitation

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18
Q

Major adverse effects of isoprenaline

A
  1. arrhythmias

2. tachycardias

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19
Q

Uses for dobutamine

A

congestive heart failure

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20
Q

Major advise effect of dobutamine

A

tachycardia

21
Q

Uses for salbutamol/terbutaline

A
  1. asthma

2. premature labour

22
Q

Major adverse effects of salbutamol/terbutaline

A
  1. arrhythmias
  2. tachycardia
  3. vasodilation
23
Q

Uses for mirabegron

A

overactive bladder

24
Q

Major adverse effects of mirabegron

A
  1. arrhythmias

2. tachycardias

25
Q

Types of indirect adrenergic agents

A
  1. Inhibition of enzymatic breakdown of catecholamines: moclobemide
  2. Block of uptake 1: tricyclic antidepressants
  3. Displacement of endogenous noradrenaline: ephedrine and pseudoephedrine
26
Q

MOA & uses of moclobemide

A
  1. MAO A inhibitor increases the biological availability of catecholamines
  2. Used as antidepressant
27
Q

MOA & uses of tricyclic antidepressants

A
  1. Increases synaptic availability of NA but not adrenaline
  2. Mood enhancing effects in the CNS
  3. Used as antidepressant
28
Q

MOA & uses of ephedrine and pseudoephedrine

A
  1. Taken up into the adrenergic terminals and compete with NA for vesicular compartment
  2. Ephedrine and pseudoephedrine are also competitive substrates for MAO
  3. Used as nasal decongestant

*ephedrine has additional alpha and beta-adrenoceptor agonist activity

29
Q

Types of direct antiadrenergic agents

A

alpha 1: prazosin
non-selective alpha: phenoxybenzamine
beta 1: atenolol, betaxolol
non-selective beta: propranolol, sotalol, timolol

30
Q

MOA & uses of phenoxybenzamine

A
  1. Irreversible and non-selective alpha-adrenoceptor antagonist
  2. Management of pheochromocytoma
31
Q

Major adverse effects of phenoxybenzamine

A
  1. postural hypotension
  2. reflex tachycardia
  3. nasal congestion
  4. inhibition of ejaculation
  5. drowsiness
32
Q

MOA & uses of prazosin

A
  1. alpha1-adrenoceptor antagonist
  2. block vasoconstriction (esp. visceral blood flow)
  3. used to treat chronic hypertension and urinary symptoms of BPH
33
Q

Adverse effects of prazosin

A
  1. nasal congestion
  2. abnormal ejaculation
  3. drowsiness
  4. tachycardia (less common)
34
Q

MOA and uses of propranolol

A
  1. beta-adrenoceptor antagonist
  2. used to treat hypertension, angina, arrhythmias, excessive catecholamine action in hyperthyroidism
  3. additional antihypertensive action due to block of renin by beta1 antagonism
35
Q

MOA & uses of sotalol

A
  1. beta-adrenoceptor antagonist
  2. beta-blocker (class II antiarrhythmic)
  3. prolongation of cardiac action potential duration (class III antiarrhythmic)
  4. additional antihypertensive action due to block of renin by beta1 antagonism
36
Q

Major adverse effects of propranolol and sotalol

A
  1. Bronchoconstriction: contraindicated in asthma
  2. Heart failure
  3. Propranolol has direct membrane effects (local anaesthetic-like actions) hence not used as topical application to the eye
37
Q

MOA & uses of timolol

A
  1. beta-adrenoceptor antagonist
  2. used to treat glaucoma (reduces intraocular pressure by decreasing aqueous secretion from the ciliary epithelium)
  3. no local anaesthetic action therefore better for topical application to the eye as it does not block protective reflexes
38
Q

Major adverse effects of timolol

A

topical application to eye limits systemic adverse effects

39
Q

MOA & uses of atenolol

A
  1. beta1-adrenoceptor anatagonist

2. used to treat hypertension, angina, MI

40
Q

Atenolol is contraindicated for use in?

A

Topical application to the eye as it has direct membrane effects at high concentration (local anaesthetic-like actions)

41
Q

MOA & uses of betaxolol

A
  1. beta1-adrenoceptor antagonist
  2. used for treatment of glaucoma
  3. no local anaesthetic action
42
Q

Major adverse effects of betaxolol

A

topical application to eye limits systemic adverse effects

43
Q

Is there a need to exercise caution when using beta1-adrenoceptor antagonists in asthmatics?

A

YES! Although relatively selective for beta1-adrenoceptors, still have some level of beta2-adrenoceptor antagonism

44
Q

Beta-blockers have to be used with caution in what medical condition

A

Diabetes! They can mask symptoms of hypoglycaemia (e.g. tremor, heart pounding)

45
Q

Types of indirect antiadrenergic agents

A
  1. Agonists at presynaptic autoreceptors: dexmedetomidine, clonidine
  2. Decreasing noradrenaline synthesis: Methyldopa
46
Q

MOA & uses of dexmedetomidine

A
  1. act as a presynaptic alpha2-adrenoceptor agonist which are autoreceptors involved in feedback inhibition of NA release, hence decreasing NA release
  2. decrease in NA reduces visceral vasoconstriction and in CNS causes sedation and hypotension
  3. used as a sedative
47
Q

Adverse effects of dexmedetomidine

A
  1. hypotension

2. dry mouth

48
Q

MOA & uses of methyldopa

A
  1. inhibits tyrosine hydroxylase, the rate limiting enzyme in adrenaline and noradrenaline synthesis
  2. results in the formation of false neurotransmitter methylnoradrenaline
  3. presynaptic alpha2-adrenoceptor agonist
  4. used in the treatment of hypertension
49
Q

Adverse effects of methyldopa

A
  1. Haemolytic anemia

2. Hepatotoxicity

A. General Pharmacology (7 decks)

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