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 部分中文Daren处方资料（仅供参考）
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依美斯汀Emedastine 
中文别名：依美斯汀、依美司汀酯、依米司汀

英文别名：Daren、Emedastine Difumarate、Remicut   

药品类别：抗组织胺药

药理药动
    本品是一新型强效抗过敏药物。选择性和竞争性拮抗 H1受体活性。已经证实，它在体外各种标本具有强力的浓度依赖性的抑制组织胺和白细胞三烯(LTC4)的释放。

药动学
    在第Ⅰ期试验，5名健康志愿者饭后单次口服本品片剂0.5、1、2、和4mg，另试验单次空腹口服2mg，和以2mg每天2次连服14天。单次剂量口服后，血浆峰值分别为0.736、1.30、2.76和4.10ng/ml，达峰时间在1.14～1.83小时；半衰期分别为2.76、2.96、3.16和4.12小时；AUC分别为3.52、7.31、17.2和29.8ng/L·h。进食与禁食相比，餐后给药，血浆峰值和达峰时间明显较高，而AUC明显较低。多次重复给药在3天后达稳定状态。
    另一项第Ⅰ期研究，以缓释胶囊。2mg和8mg单次给药及多次给药(2mg/每天2次连服14天)。单次2mg和8mg给药峰值浓度分别为1.26和4.96ng/ml，达峰时间分别为3.05和5.38小时；半衰期为6.98和8.67小时；AUC与片剂相似15.7ng／ml·h。多次口服，在5天后达稳定状态，与口服片剂峰值和谷值相比两组差别甚微。

适应症：适用于过敏性鼻炎和荨麻疹。

用法用量：成人通常剂量1～2mg，每天2次，早饭后和睡前口服。

制剂与规格：缓释胶囊每粒 1mg和2mg两种。

不良反应：可有倦睡、不适、头痛、麻木、头晕、头重、耳鸣。口干、恶心或呕吐、厌食、胃部不适和胃痛也有报告。可能偶尔发生皮疹，如果发生这些症状应停药。总胆红素、GOT、GPT、碱磷酶、LDH和γ-GTP也可能升高，发现这些情况应小心监护病人包括停药，如果发生异常应采取对症处置。也有报告尿蛋白、尿潜血及血尿。

禁忌症：服用本品应劝告病人避免执行可能发生危险的任务，包括开车、操纵机器等。
肝功能障碍患者应慎用。老年病人推荐以 1mg开始给药。本品对妊娠的安全性尚未确定。因此对妊娠和可能妊娠的妇女用药必须判断治疗的益处大于潜在危险性方可应用。本品动物试验已发现进入乳汁。因此必需治疗时应劝告授乳妇女停止授乳。对儿童的安全性也未确定。

U.S. Brand Names
Emadine®

Index Terms
Emedastine Difumarate

Pharmacologic Category
Histamine H1 Antagonist
Histamine H1 Antagonist, Second Generation

Pharmacologic Category Synonyms
Antihistamine
Antihistamine, H1 Selective
H1 Antagonist
H1 Blocker
Second Generation H1 Antagonist

Use: Labeled Indications
Treatment of allergic conjunctivitis

Pregnancy Risk Factor
B

Lactation
Excretion in breast milk unknown/use caution

Contraindications
Hypersensitivity to emedastine or any component of the formulation

Warnings/Precautions
Concerns related to adverse effects:
• Bacterial keratitis: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis.

Special populations:
• Contact lens wearers: Contains benzalkonium chloride which may be absorbed by contact lenses; remove contact lenses prior to use and wait 15 minutes before reinserting.
• Pediatrics: Safety and efficacy have not been established in children <3 years of age.

Other warnings/precautions:
• Appropriate use: For topical ophthalmic use only.

Adverse Reactions
>10%: Central nervous system: Headache (11%)
1% to 10%:
Cardiovascular: Hyperemia
Central nervous system: Abnormal dreams
Dermatologic: Dermatitis, keratitis, pruritus
Gastrointestinal: Taste (unpleasant)
Neuromuscular & skeletal: Weakness
Ocular: Blurred vision, corneal infiltrates, corneal staining, dry eyes, transient burning or stinging
Respiratory: Rhinitis, sinusitis
Miscellaneous: Tearing

Drug Interactions
There are no known significant interactions.

Storage
Store at 4°C to 30°C (39°F to 86°F). Solution should not be used if it becomes discolored.

Mechanism of Action
Selective histamine H1-receptor antagonist for topical ophthalmic use

Pharmacodynamics/Kinetics
Absorption: Ocular: Minimal
Half-life elimination: Oral: Plasma: 3-4 hours

Dosage
Ophthalmic: Children ?3 years and Adults: Instill 1 drop in affected eye up to 4 times/day

Administration: Other
Emadine® is for topical ophthalmic use only, not for injection. Soft contact lenses should not be worn during treatment if eyes are red; if there is no redness, wait 10 minutes following emedastine instillation before inserting contact lenses. Do not allow dropper tip to touch eyelids or surrounding area of the eye.

Dental Health: Effects on Dental Treatment
No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions

Mental Health: Effects on Mental Status
May cause drowsiness or abnormal dreams

Mental Health: Effects on Psychiatric Treatment
None reported

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于2010年5月14日更新