PHRM30003 Study Guide - Final Guide: Asthma, Azithromycin, Omalizumab
5 Jun 2018
School
Department
Course
Professor
Drug name
Drug class
Molecular target(s)
Mechanism
/Function
Contradiction
/
AE/
Notes
Asthma
Salbutamol
Terbutaline
SABA
= short acting beta agonist
Reliever
Beta2 AR
Rapid onset
Short duration
AE:
Beta1 – tachycardia
Beta2 – tremor
Formoterol
Salmeterol
LABA
= long acting beta agonist
Controller
Beta2 AR
S: slow onset
F: rapid onset
Both long duration
Formoterol: highly lipophilic long
residence time
Duration: dose-dependent
Administer with low dose due to
background tone of ADR
Co-administer with SABA for acute
suppression
Try to avoid over desensitisation of
receptors – tolerance
Co-administer with inhaled GCs for anti-
inflammatory
Indacaterol
Vilanterol
uLABA
Beta2 AR
Once daily
Improved version of LABA
Ipratropium
Tiotropium
Glycopyrolate
Umeclidinium
LAMA
= long acting muscarinic
agonist
Preventer
M3R
on Airway SM
Ipra: non-selective
Stimuli: histamine, tachykinins, bradykinin
Enhance by viral infection/epithelial damage
Prevent manifestation of reflex airway
obstruction
Much less effective than beta2 agonist
M2 and M3 are structurally similar
LAMA has connectivity selective to M3 than
M2
tiotropium has same affinity for all M
subtypes but a more rapid dissociation for
M2 hence relative kinetic M3 selectivity
Beclomethasone
Budesonide
Fluticasone
Inhale
GCs
(topical)
Preventer
Anti-inflammatory
Gene transcription
Su
ppress:
- Inducible enzymes of inflammation –
PLA2
- Inflammatory cytokine – TNF-alpha
- Adhesion molecule – ICAM1
Induce:
- Annexin-1
- Beta2 AR
Slow onset with max benefit
Start at effective dose – step down
Combine with LABA
Prednisolone
Systemic (oral) GCs
Gene transcription
For acute exacerbation
Strong AE
Dupilumab
mAb
IL
-
4 receptor alpha
Can block both IL
-
4 and IL
-
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