部份中文盐酸奥洛他定处方资料（仅供参考）
药品名：奥洛他定滴眼液
商品名：Pataday,Patanol
英文名：Olapatidine Ophthalmic Solution(eye drops)
规格：滴眼剂0.2% X 2.5ml, 0.1% X 5ml
【主要成份】盐酸奥洛他定。
【性状】本药为无色至微黄色澄明液体。
药理毒理
奥洛他定是肥大细胞稳定剂及相对选择性组胺H1-受体拮抗剂。活体和体外实验中均能抑制I型速发型过敏反应。奥洛他定对α-肾上腺素能受体，多巴胺受体，毒蕈碱I型和II型受体及5-羟色胺受体没有作用。以500 mg/公斤/日和200 mg/公斤/日的剂量分别给小鼠和大鼠口服奥洛他定，未引起癌变。按每滴40uL算，这些剂量比最大的人眼推荐用量大78，125和31，250倍。在体外进行的细菌逆转突变试验，体外哺乳动物染色体畸变测试或小鼠微核试验等未观察到诱发突变的可能性。给雄和雌的大鼠口服最大人眼推荐用量的62，500倍剂量的奥洛他定后，生育指数稍有下降且受孕率下降 ；口服最大人眼推荐用量的7，800倍时未发现影响生育功能。
药代动力学
在人类局部滴眼后，只有极少量奥洛他定进入全身循环。在2次有关健康志愿者(共24人)的研究中，双眼滴用0.15%的奥洛他定滴眼液，每12小时1次，共用2周，血浆浓度普遍低于可检测值(<0.5 ng/mL)。仅在用药后2小时内有些血浆样本中可检测到奥洛他定，浓度为0.5-1.3 ng/mL。血浆半衰期约为3小时，主要由肾脏排出约60-70%的原药。在尿中发现2种代谢产物单一去甲和N－氧化物，浓度很低。
适应症
适用于治疗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1-2滴，每日2次，间隔6-8小时以上。任何疑问，请遵医嘱！
不良反应
已有报告，用药后头痛的发生率为7%。下列不良反应已有报告，发生率小于5% ：乏力，视力模糊，烧灼或刺痛感，感冒综合征，眼干，异物感，充血，过敏，角膜炎，眼睑水肿，恶心，咽炎，瘙痒，鼻炎，鼻窦炎及味觉倒错。相当一部分的不良反应和疾病本身的症状相似。
禁忌
对该产品中的任何成分过敏者禁用。
注意事项
只限眼局部滴用，不能注射。配戴角膜接触镜的患者，使用奥洛他定滴眼液时，请勿配戴角膜接触镜。本品开盖4周后应不再使用。
孕妇和哺乳期妇女用药
妊娠：
妊娠类别C：在大鼠和兔子中未发现奥洛他定有致畸胎作用。然而在器官发生期大鼠用600 mg/公斤/日，或最大人眼推荐用量的93，750倍时 ；兔子用400 mg/公斤/日，或最大人眼推荐用量的62，500倍时，胎儿成活率下降。在孕妇方面尚无适当的对照研究。因为动物研究并不总和人的反应一样，当该药对母亲的好处大于对胚胎或胎儿可能的危险时，孕妇可用此药。
哺乳期妇女：口服此药的哺乳期大鼠的奶中发现含有奥洛他定。还不知道眼局部滴用后是否会有足够量的全身吸收，以致在母乳中可测到药物。不管怎样，哺乳的母亲用奥洛他定滴眼液时应谨慎。
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。
包装规格
PATADAY OPTH SOL 0.2% 2.5ML  OLOPATADINE HCL  NOVARTIS PHARMACEUTICALS  00065-0272-25 
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e1eb5130-e59d-4590-8b04-7b1a6adae5bd
PATADAY(olopatadine hydrochloride ophthalmic solution) 0.2%
Generic Name: olopatadine hydrochloride
Dosage Form: ophthalmic solution
Indications and Usage for Pataday
Pataday™ solution is indicated for the treatment of ocular itching associated with allergic conjunctivitis.
Pataday Dosage and Administration
The recommended dose is one drop in each affected eye once a day.
Dosage Forms and Strengths
Ophthalmic solution 0.2%: each ml contains 2.22 mg of olopatadine hydrochloride.
Contraindications
None.
Warnings and Precautions
For topical ocular use only.
Not for injection or oral use.
Contamination of Tip and Solution
As with any eye drop, to prevent contaminating the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use.
Contact Lens Use
Patients should be advised not to wear a contact lens if their eye is red.
Pataday™ (olopatadine hydrochloride ophthalmic solution) 0.2% should not be used to treat contact lens related irritation.
The preservative in Pataday™ solution, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red, should be instructed to wait at least ten minutes after instilling Pataday™ (olopatadine hydrochloride ophthalmic solution) 0.2% before they insert their contact lenses.
Adverse Reactions
Symptoms similar to cold syndrome and pharyngitis were reported at an incidence of approximately 10%.
The following adverse experiences have been reported in 5% or less of patients:
Ocular: blurred vision, burning or stinging, conjunctivitis, dry eye, foreign body sensation, hyperemia, hypersensitivity, keratitis, lid edema, pain and ocular pruritus.
Non-ocular: asthenia, back pain, flu syndrome, headache, increased cough, infection, nausea, rhinitis, sinusitis and taste perversion.
Some of these events were similar to the underlying disease being studied.
USE IN SPECIFIC POPULATIONS
Pregnancy
Teratogenic effects: Pregnancy Category C
Olopatadine was found not to be teratogenic in rats and rabbits. However, rats treated at 600 mg/kg/day, or 150,000 times the MROHD and rabbits treated at 400 mg/kg/day, or approximately 100,000 times the MROHD, during organogenesis showed a decrease in live fetuses. In addition, rats treated with 600 mg/kg/day of olopatadine during organogenesis showed a decrease in fetal weight. Further, rats treated with 600 mg/kg/day of olopatadine during late gestation through the lactation period showed a decrease in neonatal survival and body weight. There are, however, no adequate and well- controlled studies in pregnant women. Because animal studies are not always predictive of human responses, this drug should be used in pregnant women only if the potential benefit to the mother justifies the potential risk to the embryo or fetus.
Nursing Mothers
Olopatadine has been identified in the milk of nursing rats following oral administration. It is not known whether topical ocular administration could result in sufficient systemic absorption to produce detectable quantities in the human breast milk. Nevertheless, caution should be exercised when Pataday™ (olopatadine hydrochloride ophthalmic solution) 0.2% is administered to a nursing mother.
Pediatric Use
Safety and effectiveness in pediatric patients below the age of 2 years have not been established.
Geriatric Use
No overall differences in safety and effectiveness have been observed between elderly and younger patients.
Pataday Description
Pataday™ (olopatadine hydrochloride ophthalmic solution) 0.2% is a sterile ophthalmic solution containing olopatadine for topical administration to the eyes. Olopatadine hydrochloride is a white, crystalline, water-soluble powder with a molecular weight of 373.88 and a molecular formula of C21H23NO3 • HCl.
The chemical structure is presented below:
Chemical Name: 11-[(Z)-3-(Dimethylamino) propylidene]-6-11-dihydrodibenz[b,e] oxepin-2-acetic acid, hydrochloride
Each mL of Pataday™ solution contains: Active: 2.22 mg olopatadine hydrochloride equivalent to 2 mg olopatadine. Inactives: povidone; dibasic sodium phosphate; sodium chloride; edetate disodium; benzalkonium chloride 0.01% (preservative); hydrochloric acid/sodium hydroxide (adjust pH); and purified water.
It has a pH of approximately 7 and an osmolality of approximately 300 mOsm/kg.
Pataday - Clinical Pharmacology
Mechanism of Action
Olopatadine is a mast cell stabilizer and a histamine H1 antagonist. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.
Pharmacokinetics
Systemic bioavailability data upon topical ocular administration of Pataday™ solution are not available. Following topical ocular administration of olopatadine 0.15% ophthalmic solution in man, olopatadine was shown to have a low systemic exposure. Two studies in normal volunteers (totaling 24 subjects) dosed bilaterally with olopatadine 0.15% ophthalmic solution once every 12 hours for 2 weeks demonstrated plasma concentrations to be generally below the quantitation limit of the assay (< 0.5 ng/mL). Samples in which olopatadine was quantifiable were typically found within 2 hours of dosing and ranged from 0.5 to 1.3 ng/mL. The elimination half-life in plasma following oral dosing was 8 to 12 hours, and elimination was predominantly through renal excretion. Approximately 60 - 70% of the dose was recovered in the urine as parent drug. Two metabolites, the mono-desmethyl and the N-oxide, were detected at low concentrations in the urine.
Nonclinical Toxicology
Carcinogenesis, Mutagenesis, Impairment of Fertility
Olopatadine administered orally was not carcinogenic in mice and rats in doses up to 500 mg/kg/day and 200 mg/kg/day, respectively. Based on a 40 μL drop size and a 50 kg person, these doses were approximately 150,000 and 50,000 times higher than the maximum recommended ocular human dose (MROHD). No mutagenic potential was observed when olopatadine was tested in an in vitro bacterial reverse mutation (Ames) test, an in vitro mammalian chromosome aberration assay or an in vivo mouse micronucleus test. Olopatadine administered to male and female rats at oral doses of approximately 100,000 times MROHD level resulted in a slight decrease in the fertility index and reduced implantation rate; no effects on reproductive function were observed at doses of approximately 15,000 times the MROHD level.
Clinical Studies
Results from clinical studies of up to 12 weeks duration demonstrate that Pataday™ solution when dosed once a day is effective in the treatment of ocular itching associated with allergic conjunctivitis.
How Supplied/Storage and Handling
Pataday™ (olopatadine hydrochloride ophthalmic solution) 0.2% is supplied in a white, oval, low density polyethylene DROP-TAINER® dispenser with a natural low density polyethylene dispensing plug and a white polypropylene cap. Tamper evidence is provided with a shrink band around the closure and neck area of the package.
2.5 mL fill in 4 mL bottle (NDC 0065-0272-25)
Storage
Store at 2°C to 25°C (36°F to 77°F)