Drug Interaction:
Drug Interactions- summary
CYP3A4 agents eg calcium blockers, cisapride, cyclosporine, ketoconazole +
Zileuton
use caution and careful monitoring when these agents are coadministered with zileuton
Zileuton + Pimozide -
Zileuton may inhibit pimozide metabolism whic may increase the risk of life-threatening
cardiac arrhthmias
Zileuton + propranolol -
Coadministration results in elevated propranolol concentration. Avoid coadministration.
Adjust dose of propranolol as needed
Zileuton + Terfenadine-
coadmin results in terfenadine concentration. Coadministration not recommended
Zileuton + theophyline-
coadmin results in increased theophylline concentration. Reduce dose of theophylline by
50% amd monitor theophylline comcentration
Zileuton + Warfarin-
coadmin results in clincaaly significant increase in prothrombin concentration.
Adjust warfarin dose.
Indication:
Asthma
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Zileuton Respiratory Abbott Laboratories 09-12-2010
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
Zileuton Uncaoted Bilayered 30-09-2010
Extended release Tablet 600mg
For the Prophylaxis and Chronic Treatment of Asthma in adults
Adverse Reaction:
Adverse reactions-
Nausea 4%
Pharyngolaryngeal pain 4%
Siniusitis 6%
Contra-Indications:
Acute liver disease or persistent transaminase elevations
Special precautions-
Acute asthma attacks- Zileton is not indicated for reversal of bronchospasm in acute asthma attacks. Therapy can be continued during acute exacerbations of asthma
Hepatic effects- if clinical signs of liver dysfunction (eg. fatigue, flu like symptoms, jaundice,lethargy, nausea, pruritus, upper quadrant pain ) develop or transaminase levels of 5 or more X the ULN occur, discontinue zileuton and follow levels until they return to normal.
Pregnancy- zileuton should be used during pregnancy only if the potential benefit benefit
justifies the potential risk to fetus
Lactation- decide to discontinue breast feeding or the drug depending upon the importance
of the drug to the mother.
Children- safety and efficacy for use in children below 12 years of age have not been established
Elderly- older patients appear to be at risk of ALT elevations
Monitoring- it is recommended that hepatic tansaminase be evaluated at initiation of treatment,
and during therapy with zileton .
Monitor serum ALT before treatment begins , once a month for the first 3 months,
every 2 o 3 times for the reminder of the year and periodically thereafter for patients
receiving long term therapy.
Dosages/ Overdosage Etc:
Indication-
Asthma
Dosage-
Two extended release tablets twice daily within 1 hour of morning and evening meals, for
a total daily dose of 2400mg
Zileuton extended release tablets should not be chewed
If the dose is missed the next dose should be taken at the scheduled time and not double
the dose.
Patient Information:
1. Inform patients that zileuton used for chronic asthma treatment, should be taken regularly
2. Inform patients that zileuton is not bronchodilator and should not be used to treat episodes of asthma
3. Advice patients if the dose is missed the next dose should be taken at the scheduled time and not double the dose.
4. Advice patients that zileuton extended release should be taken within 1 hour of morning and evening meals
5.Advice patients not to cut or chew sustained release formulation
6.Advice patients to seek medical attention if short acting bronchodilators are needed
more often than usual or if more than the maximum number of short acting inhaltions
prescribed for 24 hours are needed during treatment
7. Inform patients the most serious side effect of zileuton is elevation of liver enzymes tests
and that while taking zileuton they must return to their health care provider for liver enzyme test montoring on a regular basis.
8. Inform patients they must inform their Doctor if they experience signs andsymptoms of
liver dysfunction ( eg fatigue, lethargy, jaundice, nausea, pruritus, right upper quadrant pain)
Interaction with Food:
It is recommended that zileuton extended release be adminstered with food.
Pregnancy and lactation:
Pregnancy-
Zileuton should be used during pregnancy only if the potential benefit benefit
justifies the potential risk to fetus
Lactation-
Decide to discontinue breast feeding or the drug depending upon the importance
of the drug to the mother.
Children-
Safety and efficacy for use in children below 12 years of age have not been established
Elderly-
Older patients appear to be at risk of ALT elevations
Manufacturer Details