GIAZO （巴柳氮二钠），SALIX公司生产，规格1.1G，剂型为片剂。该药品以前FDA批准剂型为胶囊。
GIAZO Rx
Pharmacological Class:
Aminosalicylate.
Active Ingredient(s):
Balsalazide disodium (prodrug of mesalamine) 1.1g; tabs; contains sodium 126mg/tab.
Company
Salix Pharmaceuticals, Inc
Indication(s):
Treatment of mildly-to-moderately active ulcerative colitis in male patients.
Limitations of use: effectiveness in treatment of female patients was not demonstrated. Safety and effectiveness of therapy beyond 8 weeks have not been established.
Pharmacology:
Balsalazide is a prodrug of mesalamine (5-aminosalicylic acid, 5-ASA). The mechanism of action of 5-ASA is unknown, but appears to be local to the colonic mucosa rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, ie, prostanoids, and through the lipoxygenase pathways, ie, leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that 5-ASA diminishes inflammation by blocking production ofarachidonic acid metabolites in the colon.
Clinical Trials:
A double-blind, placebo-controlled, multicenter trial was conducted in 250 adult patients (49% male) with mildly-to-moderately active ulcerative colitis. Disease activity was assessed using a modified Mayo Disease Activity Index (MMDAI), which was a sum of four subscores (bowel frequency, rectal bleeding, endoscopic appearance, and physician’s global assessment), each ranging from 0–3, with higher scores indicating worse disease. The median baseline MMDAI score was 8 and the median baseline rectal bleeding subscore was 2. Patients were randomized 2:1 to receive 8 weeks of treatment with either Giazo 3.3g twice daily or placebo.
The primary efficacy endpoint was the proportion of patients that achieved clinical improvement and improvement in the rectal bleeding subscale of the MMDAI at the end of 8 weeks of treatment. Clinical improvement was defined as having both a ≥3 point improvement from baseline in the MMDAI score and a ≥1 point improvement from baseline in the rectal bleeding subscore. Two key secondary efficacy endpoints were the proportion of patients with clinical remission and mucosal healing at the end of 8 weeks of treatment.
After 8 weeks of treatment, the proportion of patients who met the definition of clinical improvement was greater for the Giazo-treated group compared to the placebo group. These differences were statistically significant in the overall population (55% with Giazo vs. 40% for placebo, P=0.0237); however, these effects were entirely driven by the results in the male subpopulation (57% with Giazo vs. 20% for placebo). After adjusting for multiplicity, statistically significant differences were also seen in the male patients for clinical remission (35% with Giazo vs. 13% for placebo) and for mucosal healing (52% with Giazo vs. 20% for placebo). Effectiveness of Giazo was not demonstrated in the female subpopulation in the clinical trial.
Legal Classification:
Rx
Adults:
≥18yrs: 3 tabs twice daily; max 8 weeks.
Children:
<18yrs: not established.
Warnings/Precautions:
Monitor for worsening symptoms of ulcerative colitis. Discontinue if acute intolerance syndrome is suspected. Known or history of renal impairment. Monitor renal function prior to initating and periodically during therapy. Hepatic impairment; consider monitoring LFTs during therapy. Elderly. Pregnancy (Cat. B). Nursing mothers.
Adverse Reaction(s)
In male patients: anemia, diarrhea, pharyngolaryngeal pain, UTI.
How Supplied:
Tabs—180

LAST UPDATED:
6/14/2013