英文药名：Xifaxan(Rifaximin Tablets)

中文药名：利福昔明片

生产厂家：SALIX PHARMS
药品介绍
利福昔明(Rifaximin)为利福霉素的衍生物，通过与细菌DNA-依赖RNA聚合酶的β-亚单位不可逆的结合而抑制细菌RNA的合成，最终抑制细菌蛋白质的合成。是第一个非氨基糖苷类肠道用抗生素。临床主要用于对利福昔明敏感的病原菌引起的肠道感染。
2010年3月25日，美国食品药品管理局（FDA）宣布批准利福昔明（Xifaxan）用于降低肝性脑病（HE）的复发风险。此前Xifaxan曾作为治疗旅行者腹泻药物获批。此次利福昔明作为罕见病药获优先审评的资格并批准此新适应症。
一项安慰剂随机对照临床试验评估了Xifaxan治疗HE的有效性，该临床试验的受试者由美国、加拿大和俄罗斯的成年患者组成。参加试验的肝病患者为无HE症状或有轻度HE症状者，与使用安慰剂治疗的患者相比，使用Xifaxan治疗的患者更少出现肝性脑病。
Xifaxan在严重肝病患者中的疗效尚未得以确认。在试验过程中，由于大部分患者同时服用了半乳糖甙果糖（一种合成糖，有助于阻止肠道的氨吸收进入血液），因此，无法评估Xifaxan作为单独治疗HE的确切疗效。
Xifaxan的常见不良反应主要为上下肢肿胀（外周性水肿）、恶心、嗳气和头痛。

XIFAXANTA 200 mg Film-coated Tablets
1. Name of the medicinal product
▼ Xifaxanta 200 mg film-coated tablets
2. Qualitative and quantitative composition
One film-coated tablet contains:
Rifaximin 200 mg
Excipients:
For a full list of excipients, see section 6.1.
3. Pharmaceutical form
Film-coated tablet
Pink circular biconvex film-coated tablets, with “AW” printed on both sides.
4. Clinical particulars
4.1 Therapeutic indications
Xifaxanta 200mg film-coated tablets are indicated for the treatment of travellers' diarrhoea that is not associated with any of:
Fever
Bloody diarrhoea
Eight or more unformed stools in the previous 24 h
Occult blood or leucocytes in the stool.
Xifaxanta 200mg film-coated tablets may shorten the duration of diarrhoea when this is associated with non-invasive strains of E.coli (see sections 4.4 and 5.1).
4.2 Posology and method of administration
Posology
200 mg every 8 hours for three days (total 9 doses).
Rifaximin must not be used for more than 3 days even if symptoms continue and a second course of treatment must not be taken (see section 4.4).
Rifaximin can be administered with or without food.
Paediatric population
The safety and efficacy of Xifaxanta 200 mg film-coated tablets in children (aged less than 18 years) have not been established.
A dosage adjustment for patients with hepatic or renal insufficiency is not necessary.
Method of administration
Orally with a glass of water.
4.3 Contraindications
Hypersensitivity to the active substance, to any rifamycin (e.g. rifampicin or rifabutin) or to any of the excipients.
4.4 Special warnings and precautions for use
Clinical data have shown that Rifaximin is not effective in the treatment of travellers' diarrhoea caused by invasive enteric pathogens such as Campylobacter, Salmonella and Shighella, which typically produce dysentery-like diarrhoea characterised by fever, blood in the stool and high stool frequency.
If symptoms worsen treatment with Rifaximin should be interrupted.
If symptoms have not resolved after 3 days of treatment, or recur shortly afterwards, a second course of Rifaximin should not be administered.
Clostridium difficile associated diarrhoea (CDAD) has been reported with use of nearly all antibacterial agents, including Rifaximin. The potential association of Rifaximin treatment with CDAD and pseudomembranous colitis (PMC) cannot be ruled out.
Paediatric population
Xifaxanta 200 mg film-coated tablets are not recommended for use in children (<18 years old).
4.5 Interaction with other medicinal products and other forms of interaction
There is no experience regarding administration of rifaximin to subjects who are taking another rifamycin antibacterial agent to treat a systemic bacterial infection. Due to the lack of data and the potential for severe disruption of gut flora with unknown consequences rifaximin should not be administered concomitantly with other rifamycins.
Due to the negligible gastrointestinal absorption of orally administered Rifaximin (less than 1%), the systemic drug interaction potential is low.
In vitro data show that Rifaximin is a weak inducer of the CYP3A4 isoenzyme of the P450 cytochrome. Drug-drug interaction studies investigating the clinical interaction between Rifaximin and drugs metabolised by the human cytochrome P450 isoenzymes demonstrated that Rifaximin did not significantly affect the pharmacokinetics of midazolam or an oral contraceptive containing ethinyl estradiol and norgestimate. Therefore, clinical interactions with drugs metabolised by these isoenzymes are not expected.
The potential for drug-drug interactions to occur at the level of gut transporter systems has not been evaluated and cannot be ruled out.
No drug interaction studies investigating the concomitant intake of Rifaximin and other drugs that might be used during an episode of travellers' diarrhoea (e.g. loperamide, charcoal) are available. Patients should take Rifaximin at least 2 hours after the administration of charcoal.
4.6 Fertility, pregnancy and lactation
For Rifaximin no clinical data on exposed pregnancies are available.
Animal studies have shown reproductive toxicity (see 5.3).
Rifaximin is not recommended during pregnancy and in women of childbearing potential not using contraception (see Section 5.3).
It is not known whether rifaximin is excreted in human milk. A decision should be taken whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
4.7 Effects on ability to drive and use machines
No studies on the effects on the ability to drive and use machines have been performed.
In clinical controlled trials dizziness has been reported but rifaximin has negligible influence on the ability to drive and use machines.
4.8 Undesirable effects
In clinical studies in subjects who received Rifaximin for treatment of travellers' diarrhoea Adverse Reactions considered as being at least possibly related to Rifaximin have been categorised by organ system and frequency.

MedDRA System Organ Class (ver. 12.1)	Common (≥1/100 to <1/10)	Uncommon (≥ 1/1.000 to < 1/100)
Infections and infestations		Candidiasis, Herpes simplex, Nasopharyngitis, Pharyngitis, Upper respiratory tract infection
Blood and lymphatic system disorder		Lymphocytosis, Monocytosis, Neutropenia
Metabolism and nutrition disorders		Decreased appetite, Dehydration
Psychiatric Disorders		Abnormal dreams, Depressed mood, Insomnia, Nervousness
Nervous system disorders	Dizziness, Headache	Hypoesthesia, Migraine, Paraesthesia, Sinus headache, Somnolence
Eye disorders		Diplopia
Ear and labyrinth disorders		Ear pain, Vertigo
Cardiac disorders		Palpitations
Vascular disorders		Blood pressure increased Hot flush
Respiratory, thoracic, and mediastinal disorders		Cough, Dry throat, Dyspnoea, Nasal congestion, Oropharyngeal pain, Rhinorrhea
Gastrointestinal disorders	Abdominal pain, Constipation, Defecation urgency, Diarrhoea, Flatulence, bloating and distension, Nausea and vomiting symptoms, Rectal tenesmus	Abdominal pain upper, Dry lips, Dyspepsia, Gastrointestinal motility disorder, Faeces hard, Haematochezia, Mucous stools, Taste disorders
Hepatobiliary disorders		Aspartate aminotransferase increased
Skin and subcutaneous tissue disorders		Rashes, eruptions and exanthemas NEC Sunburn
Musculoskeletal and connective tissue disorders		Back pain, Muscle spasms, Muscular weakness, Myalgia Neck pain
Renal and urinary disorders		Blood in urine present Glycosuria, Pollakiuria, Polyuria Proteinuria
Reproductive system and breast disorders		Polymenorrhoea
General disorders and administration site conditions	Pyrexia	Asthenic conditions, Chills, Cold sweat, Hyperhidrosis, Influenza like illness, Oedema peripheral, Pain and discomfort NEC

Post-marketing experienceDuring post-approval use of Rifaximin further undesirable effects have been reported.
The frequency of these reactions is not known (cannot be estimated from the available data).

MedDRA System Organ Class (ver. 12.1)	Frequency not known
Infections and infestations	Clostridial infections
Blood and lymphatic system disorder	Thrombocytopenia
Immune system disorders	Anaphylactic responses, Angioedemas, Hypersensitivity
Vascular disorders	Presyncope
Hepatobiliary disorders	Liver function tests abnormalities
Skin and subcutaneous tissue disorders	Dermatitis Eczema Erythemas Pruritus NEC Urticarias
Investigations	International normalised ratio abnormalities

4.9 Overdose
No case of overdose has been reported.
In clinical trials with patients suffering from travellers' diarrhoea doses of up to 1800 mg/day have been tolerated without any severe clinical signs.
In case of overdose gastric emptying and administration of appropriate supportive treatment are recommended.
5. Pharmacological properties
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: intestinal anti-infective agents, antibiotics. ATC code: A07AA11
Mode of action
Rifaximin is an antibacterial agent of the rifamycin class that binds irreversibly to the beta sub-unit of the bacterial enzyme DNA-dependent RNA polymerase and consequently inhibits bacterial RNA synthesis.
Mechanism of resistance
The main mechanism of acquiring resistance to rifaximin appears to involve: a mutation in the rpoB gene encoding the bacterial RNA polymerase.
Susceptibility
Rifaximin is a non-absorbed antibacterial agent.In vitro susceptibility testing cannot be used to reliably establish susceptibility or resistance of bacteria to Rifaximin. There are currently insufficient data available to support the setting of a clinical breakpoint for susceptibility testing.
5.2 Pharmacokinetic properties
Absorption
Pharmacokinetic studies in rats, dogs and humans demonstrated that after oral administration Rifaximin in the polymorph α form is virtually not absorbed (less than 1%). Following the administration of therapeutic doses of Rifaximin in healthy volunteers and patients with damaged intestinal mucosa (Inflammatory Bowel Disease), plasma levels are negligible (less than 10 ng/ml). Systemic absorption of Rifaximin is increased but not by a clinically relevant extent by administration within 30 minutes of a high-fat breakfast.
Elimination
The urinary recovery of Rifaximin does not exceed 0.4% of the administered dose.
Special Populations
No clinical data are available on the use of Rifaximin in patients with impaired renal function.
In patients with hepatic encephalopathy mean peak plasma concentrations of 13.5 ng/mL Rifaximin were detected after administration of 800 mg Rifaximin three times daily for 7 days. Less than 0.1% of the administered dose was recovered after 7 days. Because of the limited systemic absorption of Rifaximin, no specific dosing adjustments are recommended for patients with hepatic insufficiency.
5.3 Preclinical safety data
Preclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity and genotoxicity Morphological alterations have been observed in the foetuses of Rifaximin orally administered rats and rabbits.
6. Pharmaceutical particulars
6.1 List of excipients
Tablet core:
Sodium starch glycolate type A
glycerol distearate
colloidal anhydrous silica
talc
microcrystalline cellulose
Tablet coating:
hypromellose,
titanium dioxide
disodium edetate
propylene glycol
red iron oxide E172.
6.2 Incompatibilities
Not applicable.
6.3 Shelf life
Original packing: 3 years.
6.4 Special precautions for storage
This medicinal product does not require any special storage conditions.
6.5 Nature and contents of container
PVC/PE/PVDC -Aluminium blister pack containing 9 tablets.
6.6 Special precautions for disposal and other handling
No special requirements.
7. Marketing authorisation holder
Norgine Pharmaceuticals Limited
Moorhall Road
Harefield
Uxbridge
UB9 6NS
8. Marketing authorisation number(s)
PL 20011/0021
9. Date of first authorisation/renewal of the authorisation
02/12/2010 / 01/12/2015
10. Date of revision of the text
01/06/2011

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注：以下产品不同规格和不同价格，购买以咨询为准！
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产地国家: 美国
原产地英文商品名:
XIFAXAN UNIT DOSE PACK 550mg/tab 60tabs/bottle
原产地英文药品名:
RIFAXIMIN
中文参考商品译名:
XIFAXAN单位剂量包装 550毫克/片 60片/瓶
中文参考药品译名:
利福昔明
中文参考化合物名称:
4-脱氧-4-甲基砒啶[1，2-1，2]咪唑井[5，4-环]利福霉素SV
生产厂家中文参考译名:
SALIX PHARMS
生产厂家英文名:
SALIX PHARMS
----------------------------------------------
产地国家: 美国
原产地英文商品名:
XIFAXAN UNIT DOSE PACK 200mg/tab 100tabs/bottle
原产地英文药品名:
RIFAXIMIN
中文参考商品译名:
XIFAXAN单位剂量包装 200毫克/片 100片/瓶
中文参考药品译名:
利福昔明
中文参考化合物名称:
4-脱氧-4-甲基砒啶[1，2-1，2]咪唑井[5，4-环]利福霉素SV
生产厂家中文参考译名:
SALIX PHARMS
生产厂家英文名:
SALIX PHARMS
----------------------------------------------
产地国家: 美国
原产地英文商品名:
XIFAXAN 550mg/tab 60tabs/bottle
原产地英文药品名:
RIFAXIMIN
中文参考商品译名:
XIFAXAN 550毫克/片 60片/瓶
中文参考药品译名:
利福昔明
中文参考化合物名称:
4-脱氧-4-甲基砒啶[1，2-1，2]咪唑井[5，4-环]利福霉素SV
生产厂家中文参考译名:
SALIX PHARMS
生产厂家英文名:
SALIX PHARMS
----------------------------------------------
产地国家: 美国
原产地英文商品名:
XIFAXAN 200mg/tab 30tabs/bottle
原产地英文药品名:
RIFAXIMIN
中文参考商品译名:
XIFAXAN 200毫克/片 30片/瓶
中文参考药品译名:
利福昔明
中文参考化合物名称:
4-脱氧-4-甲基砒啶[1，2-1，2]咪唑井[5，4-环]利福霉素SV
生产厂家中文参考译名:
SALIX PHARMS
生产厂家英文名:
SALIX PHARMS
----------------------------------------------
产地国家: 美国
原产地英文商品名:
XIFAXAN 200mg/tab 100tabs/bottle
原产地英文药品名:
RIFAXIMIN
中文参考商品译名:
XIFAXAN 200毫克/片 100片/瓶
中文参考药品译名:
利福昔明
中文参考化合物名称:
4-脱氧-4-甲基砒啶[1，2-1，2]咪唑井[5，4-环]利福霉素SV
生产厂家中文参考译名:
SALIX PHARMS
生产厂家英文名:
SALIX PHARMS