Controlled medication - Leukotriene Modifiers

Question 1

Montelukast (Singulair®)
Dosage form

Answer 1

Tablets
granule packets

Question 2

Montelukast (Singulair®)
dosing

Answer 2

Dosing in 0-4-year-olds
- 4mg at bedtime
Dosing in 5-11-year-olds
- 5mg by mouth at bedtime
Adult dosing’- 10mg by mouth at bedtime

Question 3

Zafirlukast (Accolate®)
dosage form

Answer 3

Tablets

Question 4

Zafirlukast (Accolate®)
Dosing

Answer 4

Dosing in 5-11-year-olds
- 10mg by mouth BID
Adult dosing
- 20mg by mouth BID

Question 5

Zileuton (Zyflo CR®)
dosage form

Answer 5

IR tablets
ER tablets

Question 6

Zileuton (Zyflo CR®)
dosing

Answer 6

Adult dosing
- IR - 600mg 4 times daily
- ER - 1200mg by mouth BID

Question 7

Adverse effects

Answer 7

AE: neuropsychiatric events (agitation, anxiety, abnormal dreams, hallucinations, depression, suicidal thinking), Churg-Strauss syndrome (rare), increased hepatic transaminases (zafirlukast and zileuton)
* Less effective than low dose ICS and ICS/LABA in asthma
* Have not be adequately trialed in COPD * Montelukast
o Minor substrate of CYP2C8/9 and 3A4
o Not for acute relief of symptoms
o Boxed warning: neuropsychiatric events
* Zafirlukast
o Take at least 1 hour before or 2 hours after
meals
o Can increase INR
o Major substrate, minor inhibitor of CYP 2C9
* Zileuton
o Weak CYP1A2 inhibitor o Take with food