Source: European Medicines Agency (EU) Revision Year: 2011 Publisher: Pfizer Limited, Sandwich, Kent, CT13 9NJ, United Kingdom
Treatment of patients with pulmonary arterial hypertension (PAH) classified as WHO functional class III, to improve exercise capacity. Efficacy has been shown in primary pulmonary hypertension and in pulmonary hypertension associated with connective tissue disease.
Treatment should only be initiated and monitored by a physician experienced in the treatment of PAH.
Thelin is to be taken orally as a dose of 100 mg once daily. It may be taken with or without food and without regard to the time of day.
In the case of clinical deterioration despite Thelin treatment for at least 12 weeks, alternative therapies should be considered. However, a number of patients who showed no response by week 12 of treatment with Thelin responded favourably by week 24, so an additional 12 weeks of treatment may be considered.
Higher doses did not confer additional benefit sufficient to offset the increased risk of adverse reactions, particularly liver injury (see section 4.4).
There is limited experience with abrupt discontinuation of sitaxentan sodium. No evidence for acute rebound has been observed.
Studies in patients with pre-existing liver impairment have not been conducted. Thelin is contraindicated in patients with elevated liver aminotransferases prior to initiation of treatment (>3 x Upper Limit of Normal (ULN)) or with elevated direct bilirubin >2 x ULN prior to initiation of treatment (see section 4.3).
No dose adjustment is required in patients with renal impairment.
Thelin is not recommended for use in children and adolescents below 18 years due to a lack of data on safety and efficacy.
No dosage adjustment is needed in patients over the age of 65 years.
The efficacy and safety of Thelin co-administration with other treatments for PAH (eg, epoprostenol, sildenafil, iloprost) has not been studied in controlled clinical trials. Therefore, caution is recommended in case of co-administration.
There is no specific experience with the management of Thelin overdose. In the event of overdose, symptomatic and supportive measures should be employed.
During clinical trials, Thelin was given as a daily oral dose of 1000 mg/day for 7 days to healthy volunteers. The most common adverse effects at this dose were headache, nausea, and vomiting.
In an open-label hypertension study, 10 patients received 480 mg twice daily (approximately a 10-fold increase in daily dose compared to the MRHD) for up to 2 weeks. Headaches (some severe), peripheral oedema, and anaemias were the most common adverse events reported in these patients, none of which were considered serious.
In an open-label PAH study, one fatal case of hepatic failure has been reported after chronic dosing of sitaxentan at 600 mg/day administered as 300 mg bid.
Shelf life: 24 months.
Store below 25°C.
PVC/ACLAR/paper-backed aluminium blisters containing 14 tablets.
Cartons contain 14, 28, 56, or 84 tablets.
High-density polyethylene (HDPE) bottles containing 28 tablets.
Not all pack sizes may be marketed.
No special requirements.
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