Drugs for Respiratory System I Flashcards
1
Q
Class of drug in respiratory system
A
- Beta-1 agonist (SABA +LAMA )
- Leukotriene receptor antagonist
- Methylxanthines
- Muscarinic Agents (SAMA + LAMA)
- Corticosteroids
- Mucolytic Agents
2
Q
Pharmacophore
A
- Section of the drug structure that is responsible for its biological activity and binds to receptor
3
Q
Pharmacophore modelling
A
- Docking method screening a library of molecules to determine which theroretically could be active
4
Q
Short-Acting Beta-2 Agonists (SABA)
A
- Beta-2 receptors
- Causes smooth muscle relaxation and
dilation of the airways - Rapid onset
5
Q
Long-Acting Beta-2 Agonists (LABAs)
A
- Act directly on beta-2 receptors
- Causes smooth muscle relaxation and dilation of the airways
- Rapid onset is also possible
- Effects can last for up to 12 hours
Beta-2 Agonists (SABA + LABA)
6
Q
Why are molecules long acting
A
- Need to look at the rest of the molecule
- Hydrophobicity allow drug to remain near the receptor for longer
7
Q
Leukotriene Receptor Antagonists
A
- Cysteinyl leukotrienes cause bronchoconstriction, smooth muscle hypersensitivity, inflammation and mucus formation
- Reach maximal plasma concentration at 3hrs
- Half life up to 10hrs - bronchodialation and antinflammatory effect
8
Q
Hydrophobicity
A
- Tendancy of non-polar groups of a molecule to aggregate in order to minimise the unfavourable exposition to surrounding polar solvent
9
Q
Lipophilicity
A
- Measure of the affinity of molecule for a non-polar solvent in a biphasic system constituted by a polar and non-polar solvent
10
Q
Addition of methylene groups
A
- Increase size and lipophilicity
11
Q
Increase degree of saturation
A
- Increase flexible
12
Q
Addition of ring system
A
- Increase size, ridgidity and hydrophobicity
13
Q
Addition of halogen group
A
- Increase lipophilicity
- Reactivity and electrophilicity
14
Q
Addition of methyl groups
A
- Increase Lipophilicity, size (binding pockets)
15
Q
Addition of hydroxy groups
A
- Increase hydrophilicity
- H-bonding
