部分中文富马酸依美斯汀处方资料（仅供参考）

英文名：EMEDASTINE DIFUMARATE

商品名：EMADINE OPH SOL 0.05%

中文名：富马酸依美斯汀滴眼液

制造商：美国诺华制药

适应症 

用于暂时缓解过敏性结膜炎的体征和症状。 

用法用量

推荐剂量为患眼每次1滴,每日2次,如需要可增加到每日4次。 

不良反应

在持续42天的临床对照试验中,最常见的不良反应是头疼（11％）。小于5％的患者出现下列并发症：异梦、乏力、怪味、视物模糊、眼部灼热或刺痛、角膜浸润、角膜着染、皮炎、不适、眼干、异物感、充血、角膜炎、瘙痒、鼻炎、鼻窦炎和流泪。有些表现与疾病本身的症状相似。 

禁 忌

对富马酸依美斯汀和埃美丁TM中任何成分过敏者禁用。 

注意事项

警告：

埃美丁TM只用于眼部滴用,不能用于注射或口服。 患者须知：为防止污染药瓶口和药液,不要使药瓶口接触眼睑和眼周部位。不用时应将药瓶口拧紧。如果药液变色,请勿再使用。 配戴隐形眼镜的患者,如果眼部充血,用埃美丁TM治疗期间建议其不要配戴隐形眼镜,因为埃美丁TM中的防腐剂苯扎氯铵可被软隐形眼镜吸收。戴用软隐形眼镜而且眼部不充血的患者,在滴药至少10分钟后才能重新戴用隐形眼镜。不能应用埃美丁TM治疗由隐形眼镜引起的眼部刺激症状。

请仔细阅读说明书并遵医嘱使用。 

儿童用药

尚未确定3岁以下儿童使用本品的安全性和有效性。 

老年患者用药：尚不明确。 

孕妇及哺乳期妇女用药 

妊娠：

妊娠类别B：在大鼠和兔子对富马酸依美斯汀进行了致畸及围产期和围产后的研究。在人眼最大用药量的15,000倍水平,富马酸依美斯汀没有显示出致畸作用,对围产期和围产后的新生儿发育也没有作用。但使用人眼最大用药量的70,000倍时,富马酸依美斯汀增加了大鼠体表、内脏和骨骼畸形的发生率。在孕妇中还没有进行恰当的、严格对照的试验。由于动物研究的结果并不总是能预计人的反应,因此只有明确需要时才能给孕妇使用本品。 哺乳期妇女：给大鼠口服依美斯汀后,在乳汁中发现药品。目前尚不清楚眼部滴用后,是否有足够量的全身吸收,而能在乳汁中发现一定量的依美斯汀。不管怎样,当给哺乳期妇女应用依美斯汀时,应特别谨慎。 

药物相互作用

如与其他药物同时使用可能会发生药物相互作用，详情其咨询医师或药师。 

药物过量

有报道每天口服本品15ml相当于7.5mg,可引起嗜睡和不适。对用药过量的病例,可采取对症和支持疗法。

包装

EMADINE OPH SOL 0.05% 5ML  EMEDASTINE DIFUMARATE    NOVARTIS PHARMACEUTICALS    00065-0325-05 

完整资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=98a010d5-4905-4abf-a9d2-c85a07daa23b

EMADINE® Eye Drops

SCHEDULING STATUS:

S2

PROPRIETARY NAME

(and dosage form):

EMADINE® Eye Drops

COMPOSITION

EMADINE® Eye Drops contains emedastine difumarate equivalent to 0.5 mg emedastine base per mL in a sterile ophthalmic solution preserved with benzalkonium chloride 0.01% (m/v). 

PHARMACOLOGICAL CLASSIFICATION

A.15.4 Ophthalmic preparations, other.

PHARMACOLOGICAL ACTION 

Emedastine is a potent, selective and topically effective histamine H1-antagonist. In vitro examinations of emedastine's affinity for histamine receptors (H1, H2 and H3) demonstrate 10,000-fold selectivity for the H1 histamine receptor; Kis = 1.3 nM, 49.064 nM and 12.430 nM, respectively. In vivo topical ocular administration of emedastine produces concentration-dependant inhibition of histamine-stimulated vascular permeability. Emedastine exhibits no significant effects on adrenergic, dopaminergic or serotonergic receptors.

Emedastine is absorbed systemically, as are other topically administered drugs. In a study involving 10 normal volunteers dosed bilaterally twice daily for 15 days with EMADINE 0.05% eye drops solution, plasma concentrations of the parent compound were generally below the quantitation limit of the assay (0.3 ng/mL). Samples in which emedastine was quantifiable ranged from 0.30 to 0.49 ng/mL.

The human oral bioavailability of emedastine is approximately 50% and maximum plasma concentrations were achieved within 1-2 hours after dosing.

Emedastine is principally metabolised by the liver. The elimination half-life of topical emedastine is 10 hours. Approximately 44% of an oral dose is recovered in the urine over 24 hours, with only 3.6% of the dose excreted as parent drug. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. The 5’-oxo analogues of 5- and 6-hydroxyemedastine and the N-oxide are also formed as minor metabolites.

INDICATIONS

EMADINE Eye Drops is indicated for the relief of the signs and symptoms of seasonal allergic conjunctivitis. 

EMADINE has not been studied in clinical trials for more than six weeks.

CONTRA-INDICATIONS

Hypersensitivity to any component of this product.

Safety in pregnancy and lactation has not been demonstrated.

WARNINGS

As the possibility of adverse effects on the corneal permeability and the danger of disruption of the corneal epithelium with prolonged or repeated usage of benzalkonium chloride preserved preparations cannot be excluded, regular ophthalmological examination is required. Caution should be exercised in the use of benzalkonium chloride preserved topical medication over an extended period in patients with extensive ocular surface disease.

DOSAGE AND DIRECTIONS FOR USE

Instil one drop of EMADINE Eye Drops to the affected eye(s) twice daily.

Elderly and Paediatric use: 

Safety and effectiveness have been established in paediatric patients between the ages of 4 and 16. 

 EMADINE Eye Drops has not been studied in elderly patients and therefore its use is not recommended in patients over the age of 65 years.

Hepatic and renal impairment use: 

EMADINE Eye Drops has not been studied in these patients and therefore its use is not recommended in this population.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS 

Undesirable effects: The most common ocular adverse reaction reported with EMADINE Eye Drops was discomfort (transient burning and stinging).

Ocular adverse reactions reported commonly included dry eye, ocular hyperaemia, ocular pruritis, blurred vision, corneal staining, tearing, lid oedema, infiltrate, foreign body sensation, conjunctivitis, keratitis, hordoleum, lid margin crusting, eye fatigue, decreased visual acuity, sticky sensation, ocular discharge, conjunctival oedema, accidental injury, photophobia and ocular irritation. 

Occasional nonocular adverse events were headache and rhinitis, cold syndrome, pain and back pain.

Special precautions for use

Do not instil EMADINE Eye Drops while wearing contact lenses, but wait 10 minutes after instillation before reinserting lenses.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT

A topical overdose may be flushed from the eye with warm tap water. Treatment should be supportive and symptomatic. In case of accidental ingestion of the content of a bottle of EMADINE, the potential of emedastine to increase the QT interval should be borne in mind and appropriate monitoring and management should be implemented.

IDENTIFICATION

Clear, colourless to pale yellow solution.

PRESENTATION

Opaque low density polyethylene DROP-TAINER™ bottles with a 5 mL fill, fitted with a natural dispensing tip as plug and white, linerless screw-on cap. 

STORAGE INSTRUCTIONS

Store below 25°C.

DO NOT USE MORE THAN 30 DAYS AFTER OPENING. 

KEEP OUT OF REACH OF CHILDREN.