Adrenaline Flashcards
Role of Adrenaline as a drug
Agonist
- Hormone
- Neurotransmitter (fight/flight)
- Affect heart rate, blood vessel diameter, air passage diameter
Role of Noradrenaline as a drug
Neurotransmitter which affects heart rate
Alpha-adrenoceptor agonist
Biosynthesis of Adrenaline
Alpha receptor agonist
Phenylepherine
Beta receptor agonist
Isoetharine (non-selective)
Alpha + beta receptor agonist
Adrenaline
Role of Beta2 receptor
Relaxes bronchi
Stimulates insulin release
Inhibits histamine release from mast cells
Isoetharine: SABA or LABA
SABA
How is isoetharine converted to its inactive form
Taken up by tissues + methylated by COMT
Replace Meta-OH with -CH2OH = more resistant to metabolism
Difference between Isoprenaline and Salbutamol
Fenoterol: SABA or LABA?
SABA
Also stimulates Beta1 when used well above recommended dose
(Withdrawn from market due to mortality)
Structure-activity relationships of each part of the structure
Which salbutamol is the active form?
R is the active form
(S blocks metabolism of R)
What structure in salbutamol produces selectivity for Beta2 receptors?
t-butyl group
Describe the synthesis of salbutamol
Mechanism of Fries re-arrangement
Mechanism of reduction in Salbutamol Synthesis
Difference between Salmeterol to Salbutamol
LABA - slow onset in the prevention/management
Bulky N-substituent
Selective for Beta2 - receptors
More lipophilic
Acts 2x longer than salbutamol
Describe the mechanism of bromination/halogenation via keto-enol tautomerism
