1.2 Leukotriene receptors

Bolinger

what is a leukotriene

potent lipid mediator of inflammation and allergic reactions

leukotriene receptor antagonists work by inhibiting…

cysteinyl leukotriene receptors

mast cells release ____ leukotrienes in allergy

cysteinyl

leukotriene receptor antagonists are used for patients with which diseases

allergic rhinitis and asthma

symptoms of allergic rhinitis

runny nose (clear rhinorrhea)

sneezing

congestion

post nasal drip

itchy nose, eyes, throat, and ears

symptoms of rhinitis

disturbed sleep

fatigue

poor work or school performance

loss of smell or tatse

montelukast is approved for the treatment of perennial allergic rhinitis in children aged _____

6 months and up

montelukast is approved for the treatment of ____ allergic rhinitis in children aged 6 months +

perennial

montelukast is approved for the treatment of ____ allergic rhinitis in children aged 2 yrs +

seasonal

montelukast is approved for the treatment of seasonal allergic rhinitis in children aged _____

2 years+

True or false:

montelukast is 1st line for allergic rhinitis

false

leukotriene receptor antagonists are less effective than…

peripherally selective antihistamines, and intranasal steroids

combination of leukotriene antagonists with antihistamines leads to…

additive effects (more effective than when used seprately)

montelukast can be used as monotherapy for…

children with mild persistent asthma and coexisting allergic rhinitis

what is the only anti-leukotriene agent approved for management of allergic rhinitis?

montelukast

montelukast is selective for which receptor?

CysLT1

montelukast is selective for CysLT1 receptor which will prevent which leukotrienes from activating said receptor?

D3 and E4

D3 and E4 leukotrienes are excreted by…

various cells (mast included)

which leukotrienes may cause asthma and allergic rhinitis

D3 and E4

dosage forms of montelukast

oral tablet

chewable table

granule formulation

True or false:

leukotriene receptor antagonists are well-tolerated and are rarely associated with behavioral changes

true

oral bioavailability is typically targets a MW’s of…

500 or less

Montelukast is a member of _____, a monocarboxylic acid and an aliphatic sulfide.

quinolines

montelukast absorption

quickly absorbed following administration by the oral route

oral bioavailability of montelukast

64%

montelukast and food

can take without regard to meals

steady state volume of distribution for montelukast

8-11 L

mean half life of montelukast

2.7-5.5 hrs