Komiskey: Anti-asthmatics, Antihistamine, and COPD Flashcards
Synthesis of histamine occurs primarily in which two cell types?
mast cells and basophils
Histamine receptor H1 is found on smooth muscle, endothelium, and CNS tissue. Its activation results in?
vasodilatation, bronchoconstriction, smooth muscle activation, and separation of endothelial cells
Which histamine receptor regulates the release of other neurotransmitters?
H3
Stimulation of which cranial nerve causes bronchoconstriction and leads to cough?
Vagus
What type of receptor is H1?
G-protein coupled, linked to intercellular Gq, which activates phospholipase C
6 common first generation anti-histamines?
Diphenhydramine (Benadryl®) Chlorpheniramine (Chlor-Trimeton®) Brompheniramine (Dimetane®) Hydroxyzine (Atarax®) Cyproheptadine (Periactin®) Promethazine (Phenergan®)
Second generation anti-histamines? (unlikely to cause drowsiness)
Fexofenadine (Allegra®) (14h) Cetirizine (Zyrtec®) (8h) (kids metabolize faster) Levocetirizine (Xyzal®) Loratadine (Claritin®) (up to 28h) Desloratadine (Clarinex®)
LEVOcetirizine:
This drug is the active enantiomer of cetirizine and is believed to be more effective and have fewer adverse side effects.
Also it is not metabolized and is likely to be safer than other drugs due to a lack of possible drug interactions (Tillement).
It does not cross the BBB and does not cause significant drowsiness
Intranasal anti-histamines?
Azelastine, Olopatadine (better SE)
Antagonists of H1 receptor?
Mepyramine, triprolidine, cetirizine
Agonist of H1?
Histaprodifen
Antihistamines are_______ ________ _________, meaning that they shift the equilibrium of the receptor configuration to the inactive state and thus block histamine effects.
competitive inverse agonists
What could be a later development of asthma? What cell type will show up?
COPD, neutrophils
What is the early phase reaction of asthma?
bronchoconstriction
What is the late phase reaction of asthma?
inflammation, mucus hypersecretion, hyperresponsiveness
List “relievers” of asthma
SABAs:
Salbutamol
Fenoterol
Anti-Cholinergics:
Ipratropium Bromide
Tiotropium
List “controllers” of asthma
LABAs (bronchodilation lasts >12h; good for EIB prevention):
Formoterol (***onset in 5-10m)
Salmeterol (onset in 30-40m)
ICSs (used more as prophylaxis): Ciclesonide (**a PROdrug) Flunisolide (MDI, BID) Beclomethasone (MDI, BID) Triamcinolone (MDI, BID) Memotasone (MDI, BID) Budesonide (breath-activated powder delivery) Fluticasone (breath-activated powder delivery)
Oral CS (when ICS no longer work):
Prednisone
Prednilosone
(IV CS: Methylpredisolone, for untreatable asthma)
Leukotriene receptor agonist:
Monteluksat