W6 Drugs for the Respiratory System ll

Question 1

What are examples of Tropane Alkaloids? (derived from the tropane skeleton)

Answer 1

Cocaine
Hyoscyamine and Scopolamin
Calystegine A

Question 2

What are the features of SAMAs?

Answer 2

Short-Acting Muscarinic Antagonists
* Ipratropium Bromide
* Bronchodilator
* Onset around 30 mins
* Effects last 3-5 hours
* Quaternary nitrogen compound
* Does not discriminate between
muscarinic receptor subtypes

Question 3

LAMA + SAMA
Wht are the key differences and how would they impact activity?

Answer 3

*Addition of methylene groups= Increase, lipophilicity
* Addition of ring system= Increase size, rigidity, hydrophobicity (pockets)
* Addition of carboxylic acid= Inc hydrophilicity, H-bonding, Salt formation

Question 4

Competitive vs non-competitive antagonism:
which is dependent on relative conc Of the agonsit and antagonist?

Answer 4

Competitive antagonism as non-competitive acts at a different site

Question 5

What are the features of LAMAs?
examples?

Answer 5

Tiotropium, Glycopyrronium
* A few common drugs
* Bronchodilator (blocks bronchoconstriction)
* Onset varies – can be rapid
* Effects last 12-24 hours (depending on
drug)
* Also quaternary nitrogen compounds
* Greater selectivity for M₃ receptor

Question 6

Examples of corticosteroids?

Answer 6

• Beclometasone, budesonide, ciclesonide,nfluticasone, mometasone, prednisolone
• Anti-inflammatory effects
• Multiple mechanisms of action (inhibit
  PGE₂ and PGI₂, inhibit leukotrienes, up-
  regulate β₂ receptors) – Dr Heal

Cortisone– Cortisol
Prednisone– Prednisolone
Active forms bind to GR and MR

Question 7

Examples of mucolytic agents?

Answer 7

N-acetylcysteine
Erdosteine
Carbocysteine