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Part 3 – PM3B COPY T > (PM3B) Adrenergic Therapeutics > Flashcards

(PM3B) Adrenergic Therapeutics Flashcards

1
Q

What are the stages in catecholamine synthesis?

A

(1) Tyrosine converted to DOPA via tyrosine hydroxyls
(2) DOPA converted to dopamine via DOPA decarboxylase
(3) Dopamine converted to noradrenaline via dopamine ß-hydroxylase
(4) Noradrenaline converted to adrenaline via phenylethanolamine N-methyltransferase

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2
Q

What molecule provides negative feedback in catecholamine synthesis?

A

Noradrenaline

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3
Q

Where is noradrenaline released?

A

ALL post-ganglionic sympathetic fibres

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4
Q

Where is adrenaline released?

A

Adrenal gland

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5
Q

On which molecule does noradrenaline provide negative feedback on, in catecholamine synthesis?

A

Tyrosine hydroxylase

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6
Q

Where does noradrenaline bind?

A

Either alpha/beta adrenoceptors

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7
Q

What are the adrenoceptor subtypes?

A

(1) alpha-1
(2) alpha-2
(3) beta-1
(4) beta-2
(5) beta-3

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8
Q

What subtypes of alpha-1 adrenoceptor are there?

A

(1) alpha-1A
(2) alpha-1B
(3) alpha-1D

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9
Q

What subtypes of alpha-2 adrenoceptor are there?

A

(1) alpha-2A/D
(2) alpha-1B
(3) alpha-1C

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10
Q

Where are alpha-1 adrenoceptors located?

A

Smooth muscle

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11
Q

Where are alpha-2 adrenoceptors located?

A

(1) Smooth muscle

(2) Nerve terminals

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12
Q

Where are beta-1 adrenoceptors located?

A

Heart

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13
Q

Where are beta-2 adrenoceptors located?

A

(1) Smooth muscle
(2) Heart
(3) Skeletal muscle
(4) Nerve terminals

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14
Q

Where are beta-3 adrenoceptors located?

A

(1) Skeletal muscle

(2) Fat

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15
Q

What is the function of alpha-1 adrenoceptors?

A

(1) Vasoconstriction
(2) Contraction – relax GIT
(3) Glycogenolysis

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16
Q

What is the function of alpha-2 adrenoceptors?

A

(1) Contraction

(2) Inhibition of neurotransmitter release

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17
Q

What is the function of beta-1 adrenoceptors?

A

Increase cardiac rate + force

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18
Q

What is the function of beta-2 adrenoceptors?

A

(1) Vasodilation

(2) Bronchodilation

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19
Q

What is the function of beta-3 adrenoceptors?

A

(1) Thermogenesis

(2) Lipolysis

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20
Q

Which G protein does the alpha-1 adrenoceptor act on?

A

G-alpha-q

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21
Q

Which G protein does the alpha-2 adrenoceptor act on?

A

G-alpha-i/o

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22
Q

Which G protein does the beta-1 adrenoceptor act on?

A

G-alpha-s

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23
Q

Which G protein does the beta-2 adrenoceptor act on?

A

G-alpha-s

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24
Q

Which G protein does the beta-3 adrenoceptor act on?

A

G-alpha-s

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25
What is the response of alpha-1 adrenoceptor binding?
Increased IP3
26
What is the response of alpha-2 adrenoceptor binding?
Decreased cAMP
27
What is the response of beta-1 adrenoceptor binding?
Increased cAMP
28
What is the response of beta-2 adrenoceptor binding?
Increased cAMP
29
What is the response of beta-3 adrenoceptor binding?
Increased cAMP
30
For which adrenoceptor subtype does noradrenaline have the greatest potency?
alpha-1
31
For which adrenoceptor subtype does noradrenaline have the poorest potency?
beta-2 beta-3
32
What are some selective agonists of alpha-1 adrenoceptors?
(1) Phenylephrine | (2) Methoxamine
33
What are some selective agonists of alpha-2 adrenoceptors?
(1) Clonidine | (2) Brimonidine
34
What are some selective agonists of beta-1 adrenoceptors?
(1) Dobutamine | (2) Xamoterol
35
What are some selective agonists of beta-2 adrenoceptors?
(1) Salbutamol (2) Terbutaline (3) Ritodrine
36
What are some selective agonists of beta-3 adrenoceptors?
Mirabegron
37
What are some selective agonists of alpha-1 adrenoceptors?
(1) Doxacin | (2) Terazosin
38
What are some selective agonists of alpha-2 adrenoceptors?
(1) Yohimbine | (2) Idazoxan
39
What are some selective agonists of beta-1 adrenoceptors?
(1) Atenolol (2) Metoprolol (3) Bexatolol
40
What are some selective agonists of beta-2 adrenoceptors?
Butoxamine
41
What are some selective agonists of beta-3 adrenoceptors?
None/ unknown
42
Where is tyrosine hydroxylase found?
ONLY in noradrenergic neurones
43
What are the stages of adrenergic transmission?
(1) Tyrosine converted to noradrenaline (2) Noradrenaline packaged into vesicles (3) Noradrenaline vesicles move into synaptic cleft via exocytosis (4) Noradrenaline binds to postsynaptic cell receptors/ uptake 1 transport system/ uptake 2 transport system/ alpha-2 adrenoceptor on presynaptic membrane
44
What is given in event of cardiac arrest? Why?
Adrenaline 1 in 10000 dilution IV Causes vasoconstriction via alpha-1 and beta adrenoceptor stimulation
45
What is given in event of cardiogenic shock?
ß1-selective adrenoceptor agonist Dobutamine Increased cardiac output
46
What is given to treat asthma?
ß2-selective agonists e. g. salbutamol/ terbutaline (short-acting) e. g. salmeterol/ formoterol (long-acting)
47
What is given to treat an overactive bladder (incontinence), with specific regard to adrenergic transmission?
ß3-selective agonist Mirabegron Only when anti-muscarinic drugs are ineffective/ contraindicated
48
What effects does the adrenaline in an EpiPen have on the adrenergic receptors during anaphylaxis?
(1) Bronchodilation via ß2 adrenoceptor | (2) Increased BP via alpha-1 adrenoceptor
49
What is the treatment of glaucoma using adrenoceptor agonists?
Adrenaline/ brimonidine/ apraclonidine - selective alpha2-agonists - used to reduce intraocular pressure - used when ß-blockers are inappropriate
50
What is local anaesthesia using adrenoceptor agonists?
Adrenaline - prolongs LA action - e.g. lidocaine in dental procedures - e.g. bupivacaine in spinal anaesthesia
51
What is the use of adrenoceptor agonists in labour?
ß2-selective agonists e.g. ritodrine/ salbutamol Smooth muscle relaxant Inhibit sympathetic-induced contraction of uterus Prevention of premature labour from 24-33 weeks
52
How long can ß2-selective agonists prolong premature labour for?
Maximum 48 hours
53
Which ß2-selective agonists can prolong premature labour for?
(1) Ritodrine | (2) Salbutamol
54
How many weeks gestation is considered premature?
24-33 weeks
55
What are the effects of alpha-adrenoceptor antagonists on blood pressure?
Doxazosin/ terazosin Cause vasodilation Decrease arterial BP Not first line Treatment of hypertension
56
What are the effects of alpha-adrenoceptor antagonists on benign prostatic hyperplasia?
alpha-1A adrenoceptor selective antagonists - e.g. alfuzosin/ indoramin/ tamsulosin Relaxes smooth muscle in bladder + prostate Treats enlargement of prostate + improves urinary retention
57
What are the cardiovascular effects of beta-adrenoceptor antagonists?
Non-selective = propranolol/ timolol ß1-selective = metoprolol/ atenolol Important drugs in the treatment of: - angina - MI - dysrhythmia - heart failure - hypertension
58
What are the effects of beta-adrenoceptor antagonists on glaucoma?
Topical ß-blocker Betaxolol – ß1-selective Act to reduce production of aqueous humour - reduce intraocular pressure can also use carteolol/ timolol eye drops
59
What are the effects of beta-adrenoceptor antagonists on migraines?
Propranolol/ metaprolol Migraine prophylaxis
60
What are some side-effects of beta-adrenoceptor antagonists?
(1) Cardiac depression/ bradycardia (2) Fatigue + tiredness (3) Cold extremities – reduced blood flow
61
Can cardioselective beta-adrenoceptor antagonists be taken in a patient with asthma or COPD?
No Contraindicated
62
What are some contraindications for beta-adrenoceptor antagonists?
(1) Cardioselective beta-blockers in patients with asthma or COPD (2) Eye drops used for glaucoma for patients with cardiovascular disease (3) Patients prone to hypoglycaemia - ß2-receptors control glucose release from the liver (4) Liver disease
63
Give an example of an adrenoceptor partial agonist.
Clonidine
64
What is clonidine?
alpha-2 partial agonist Used in treatment of hypertension
65
What is the mechanism of action of clonidine?
(1) Activation of alpha-2 adrenoceptor (2) Causes negative feedback on noradrenaline release in presynaptic membrane (3) Down-regulation of noradrenaline reduce alpha-1-mediated vasoconstriction
66
What is the mechanism of action of alpha-2 partial agonists?
(1) Activation of alpha-2 adrenoceptor (2) Causes negative feedback on noradrenaline release in presynaptic membrane (3) Down-regulation of noradrenaline reduce alpha-1-mediated vasoconstriction
67
Give two examples of indirect sympathomimetics that are used therapeutically as nasal decongestants.
(1) Ephedrine | (2) Pseudoephedrine
68
What is the mechanism of action of ephedrine?
(1) Acts as substrate for uptake transport system in presynaptic membrane (2) Leads to noradrenaline release (3) Causes vasoconstriction (4) Reduces nasal blood flow + oedema (congestion)
69
What is the mechanism of action of pseudoephedrine?
(1) Acts as substrate for uptake transport system in presynaptic membrane (2) Leads to noradrenaline release (3) Causes vasoconstriction (4) Reduces nasal blood flow + oedema (congestion)
70
What is the mechanism of action of indirect sympathomimetics?
(1) Acts as substrate for uptake transport system in presynaptic membrane (2) Leads to noradrenaline release (3) Causes vasoconstriction (4) Reduces nasal blood flow + oedema (congestion)
71
Other than ephedrine and pseudoephedrine, name substrates of uptake transport system 1 in the presynaptic membrane.
(1) Tyramine | (2) Amphetamine
72
When are substrates of uptake transport system 1 used therapeutically?
(1) Narcolepsy (2) ADHD (3) Appetite suppression
73
What other actions do substrates of uptake transport system 1 have therapeutically?
Pyschoactive agents e.g. cocaine/ tricyclic antidepressants Treatment of depression
74
What are the enzymes responsible for catecholamine metabolism (breakdown)?
(1) Monoamine oxidase (MAO) - MAO-A - MAO-B - found in mitochondria in sympathetic nerve terminals/ liver/ intestinal epithelium (2) Catechol-O-methyl-transferase (COMT)
75
What is the significance of COMT and MAO?
Enzymes Responsible for catecholamine metabolism (breakdown)
76
What is an MAOI?
Monoamine oxidase inhibitor
77
What are some therapeutic uses of MAOIs?
(1) Anti-depressant - e.g. phenelzine - if SSRIs/ TCAs are ineffective (2) Parkinson's disease - MAO-B selective - prevention of dopamine breakdown - slows disease progression - e.g. selegiline/ rasagiline

Part 3 – PM3B COPY T (33 decks)

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