Asthma drugs

Question 1

What mediates bronchoconstriction problems in asthma?

Answer 1

inflammatory processes and parasympathetic tone.

Question 2

What are the beta-2 agonists? How do they differ in use and toxicity?

Answer 2

albuterol: used short term in a rescue inhaler

salmeterol/fometerol: used as long-term asthma prophylaxis. toxicity: arrhythmia and tremor

Question 3

methylxanthines: mechanism and use

Answer 3

ex. theophylline. works by blocking phosphdiesterase, which is normally responsible for cAMP breakdown. this relaxes bronchial tone. Theophylline also blocks the effects of adenosine (which promotes bronchoconstriction)
use is limited because of narrow therapeutic range/toxicities (cardiotoxicity, neurotoxicity). (metabolized by P-450)

Question 4

ipatropium: mechanism and use

Answer 4

this is a muscarinic antagonist. it competitively blocks muscarinic receptors to prevent bronchoconstriction.
it is also used for COPD
tiotropium is also used for COPD

Question 5

What corticosteroids are used for asthma? How are they used, specifically?

Answer 5

fluticasone, beclomethasone.
these are inhaled steroids that are considered first-line treatment for chronic asthma.
they block the production of most cytokines by inactivating NF-kappaB. NF-kB is the transcription factor that induces the production of TNF-alpha and other inflammatory agents.

Question 6

montelukast mechanism and use

Answer 6

(also zafirulkast)

this is an inhibitor of the leukotriene receptors that. it is particularly useful for aspirin-induced asthma.

Question 7

ziluten mechanism and use

Answer 7

blocks the lipooxygenase pathway and reduces production of leukotrienes from arachidonic acid.

Question 8

omalizumab: mechanism and use

Answer 8

this is a monoclonal antibody against IgE. it binds unbound serum IgE and blocks binding to the FCe receptors. used in allergic asthma that is resistant to inhaled steroids and long-acting beta 2 agonists

Question 9

methacholine: mechanism and use

Answer 9

this is a muscarinic agonist that is used in bronchial provocation challenge to help in asthma diagnosis.

Question 10

bosetan: mechanism and use

Answer 10

this is used to treat pulmonary arterial hypertension. it is a competitive antagonist of the endothelin-1 receptors and decreases pulmonary vascular resistance.