FULYZAQ (crofelemer) tablet, coated
[Salix Pharmaceuticals, Inc.]
 美国FDA于2012年12月31日批准了Fulyzaq (crofelemer)，用于缓解HIV/AIDS患者因服用抗逆转录病毒药物引起的腹泻症状，为治疗HIV感染的辅助用药。在Napo制药公司的许可下，Fulyzaq由alix Pharmaceuticals公司负责销售。
很多HIV/AIDS患者都存在腹泻症状，这也是患者停止或切换抗反转录病毒疗法的普遍原因。Fulyzaq旨在用于治疗HIV/AIDS患者非病毒、细菌和寄生物感染造成的腹泻。患者每天服用两次Fulyzaq控制水性腹泻，舒缓胃肠道中电解质和水分泌。
Fulyzaq从龙血巴豆红色汁液中提取，是FDA批准的第二个植物处方药。植物药通常是一种或多种植物物质经多级纯化得到的复合物。2006年，FDA批准了第一个植物处方药Veregen (sinecatechins)，治疗外生殖器和肛周尖锐湿疣。
Julie Beitz博士介绍到“迄今为止FDA未批准过治疗HIV相关腹泻的药物，Fulyzaq对有此复杂情况的HIV/AIDS患者有帮助。”
向其它类型的药物一样，植物药的安全性和有效性也需通过临床试验来评估。此外，植物药的生产厂家必须确保对原材料严格控制，执行种植和采摘规范，以及复杂混合物的分析检测。
Fulyzaq的安全性和有效性由374个HIV-阳性患者入组的临床实验来评估，这些患者都接受抗反转录病毒治疗，且曾有1个月或更长时间的腹泻病史。每次水泻次数的中位数未2.5次/天。由感染或胃肠道疾病引起的腹泻患者排除在本试验之外。患者被随机指定服用Fulyzaq或安慰剂，一天2次。
临床试验旨在测定临床应答，确定每周有2次或更少水泻症状的患者人数。结果显示，服用Fulyzaq的患者中有17.6％有临床应答，而安慰剂组为8％。在一些患者中，能观察到长达20个周的持续抗腹泻效果。
在开始Fulyzaq治疗前，医师应该进行适当的测试，已确保腹泻不是因感染或胃肠道疾病引起的。临床试验中服用Fulyzaq的患者报告的副作用通常包括上呼吸道感染，支气管炎，咳嗽，肠胃气胀和肝酶胆红素水平增高。
HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use FULYZAQ safely and effectively. See full prescribing information for FULYZAQ.
FULYZAQ (crofelemer) delayed-release tablets for oral use
Initial U.S. Approval: 2012
 
INDICATIONS AND USAGE
FULYZAQ is an anti-diarrheal indicated for the symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy.(1)
DOSAGE AND ADMINISTRATION
One 125 mg delayed-release tablet taken orally twice a day, with or without food.(2)

DOSAGE FORMS AND STRENGTHS
Delayed-Release Tablets: 125 mg (3)

CONTRAINDICATIONS
None (4)
WARNINGS AND PRECAUTIONS
Rule out infectious etiologies of diarrhea before starting crofelemer. If infectious etiologies are not considered, there is a risk that patients with infectious etiologies will not receive the appropriate therapy and their disease may worsen. (5.1)

ADVERSE REACTIONS
Most common adverse reactions (incidence ≥ 3%) are upper respiratory tract infection, bronchitis, cough, flatulence and increased bilirubin. (6)

To report SUSPECTED ADVERSE REACTIONS, contact Salix Pharmaceuticals at 1-800-508-0024 or www.Salix.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
USE IN SPECIFIC POPULATIONS
• Pregnancy: Based on animal data, may cause fetal harm. (8.1)
• Pediatric Use: Safety and effectiveness of FULYZAQ has not been established in patients less than 18 years of age. (8.4)
See 17 for PATIENT COUNSELING INFORMATION.
Revised: 02/2013

Back to Highlights and Tabs
FULL PRESCRIBING INFORMATION: CONTENTS*
1 INDICATIONS AND USAGE
2 DOSAGE AND ADMINISTRATION
3 DOSAGE FORMS AND STRENGTHS
4 CONTRAINDICATIONS
5 WARNINGS AND PRECAUTIONS
6 ADVERSE REACTIONS
7 DRUG INTERACTIONS
8 USE IN SPECIFIC POPULATIONS
8.1 Pregnancy
8.3 Nursing Mothers
8.4 Pediatric Use
8.5 Geriatric Use
8.6 CD4 Count and HIV Viral Load
10 OVERDOSAGE
11 DESCRIPTION
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
12.2 Pharmacodynamics
12.3 Pharmacokinetics
13 NONCLINICAL TOXICOLOGY
13.1 Carcinogenesis and Mutagenesis and Impairment of Fertility
14 CLINICAL STUDIES
16 HOW SUPPLIED
17 PATIENT COUNSEL