英文药名：Oxsoralen Lotion (Methoxsalen USP, 1%)

中文药名：甲氧沙林乳液1％

生产厂家：VALEANT
给药说明
Oxsoralen Lotion作为一种外用剂用于白癜风结合控制剂量的紫外线A（320-400纳米）或阳光。
【药品名称】
通用名称：甲氧沙林溶液
英文名称：Methoxsalen Solution
【成份】
甲氧沙林溶液主要成份为甲氧沙林，化学名称为：8-甲氧基—呋喃香豆素。
【性状】甲氧沙林溶液为微黄色或淡黄色的澄明液体。
【适应症】
用于银屑病及白癜风等。
【规格】
1%
【用法用量】
外用
1. 1％甲氧沙林溶液用于白癜风，患处涂擦1～2小时后，用长波紫外线照射患处。照射时光距为10～30cm，照射30分钟左右。每日1次。一般一个疗程为1个月。治愈后，每周或隔周照射1次以巩固疗效。如未治愈应继续治疗。如两个疗程结束，皮损仍无明显消退，可停止治疗。
治愈后如有复发，重复治疗仍然有效。
2．全身性或弥散性患者除用药方法同上外，需在医生指导下用黑光机照射治疗。
3．局限性白癜风或初起的白癜风患者患处涂擦药液后，应照射紫外线。
【不良反应】
配合长波紫外线照射后常见的不良反应是红斑，常在照射24～28小时出现；皮肤色素沉着，瘙痒。若照射剂量过大或时间过长，照射部位皮肤上可出现红肿、水疱、疼痛、脱屑，如有红肿、水疱等可暂时停用，待恢复后再用。
【禁忌】
1. 12岁以下儿童、年老体弱者禁用。
2．孕妇及哺乳期妇女禁用。
3．严重肝病患者禁用。
4．白内障或其他晶体疾病患者禁用。
5. 有光敏性疾病患者如：红斑狼疮、皮肌炎、卟啉症、多形性日光疹、着色性干皮病等患者禁用。
6. 对甲氧沙林溶液过敏者禁用。
【注意事项】
1．有皮肤癌病史、有日光敏感家族史、新近接受放射线或细胞毒治疗及有胃肠道疾病者应慎用。
2. 照射紫外线时及照射后8小时内应戴墨镜，并用黑布覆盖正常皮肤。
3．治疗期间不得服用含有呋喃香豆素的食物，如酸橙、无花果、香菜、芥、胡萝卜、芹菜等。
4．治疗期间应戒酒，不宜吃过于腥辣食物。
5．治疗银屑病，需8～10次治疗后出现较明显疗效。治疗白癜风则疗效出现更慢。
【孕妇及哺乳期妇女用药】
孕妇及哺乳期妇女禁用。
【儿童用药】
12岁以下儿童禁用。
【老年用药】
年老体弱患者禁用。
【贮藏】
密闭，遮光，在阴凉（不超过20℃）处保存。
【包装规格】
1 fl. oz.(29.57 mL)

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SPL UNCLASSIFIED SECTION
Rx Only
CAUTION
METHOXSALEN LOTION IS A POTENT TOPICAL DRUG. READ ENTIRE BROCHURE BEFORE PRESCRIBING OR USING THIS MEDICATION.
WARNING
METHOXSALEN LOTION IS A POTENT DRUG CAPABLE OF PRODUCING SEVERE BURNS IF IMPROPERLY USED. IT SHOULD BE APPLIED ONLY BY A PHYSICIAN UNDER CONTROLLED CONDITIONS FOR LIGHT EXPOSURE AND SUBSEQUENT LIGHT SHIELDING. THIS PREPARATION SHOULD NEVER BE DISPENSED TO A PATIENT.
I. DESCRIPTION
Oxsoralen Lotion is a clear, colorless to straw colored liquid with an odor of acetone. Each ml. of Oxsoralen Lotion contains 10 mg. methoxsalen in an inert vehicle containing alcohol (71% v/v), propylene glycol, acetone, and purified water.
Methoxsalen occurs as white to pale yellow crystals and can be obtained naturally from seeds of Ammi majus and roots of Heracleum Candicans or through synthesis. Methoxsalen is practically insoluble in water, sparingly soluble in ether, soluble in ether, soluble in acetone and acetic acid, freely soluble in chloroform. The chemical name of methoxsalen is 9-methoxy-7H-furo (3, 2g) (1)-benzopyran-7-one; its empirical formula is C12H804 andthe molecular weight is 216.19. The structural formula is:

II. CLINICAL PHARMACOLOGY
The exact mechanism of action of methoxsalen with the epidermal melanocytes and keratinocytes is not known. Psoralens given orally are preferentially taken up by epidermal cells (Artuc et al, 1979)1. The best known biochemical reaction of methoxsalen is with DNA. Methoxsalen, upon photoactivation, conjugates and forms covalent bonds with DNA which leads to the formation of both monofunctional (addition to a single strand of DNA) and bifunctional adducts (crosslinking of psoralen to both strands of DNA) (Dall'Acqua et al, 1971)2. Reactions with proteins have also been described (Yoshikawa et al, 1979)3.
Methoxsalen acts as a photosensitizer. Topical application of this drug and subsequent exposure to UVA, whether artificial or sunlight, can cause cell injury. If sufficient cell injury occurs in the skin an inflammatory reaction will result. The most obvious manifestation of this reaction is delayed erythema which may not begin for several hours and may not peak for 2 to 3 days or longer. It is crucial to realize that the length of time the skin remains sensitized or when the maximum erythema will occur is quite variable from person to person. The erythematous reaction is followed over several days or weeks by repair which is manifested by increased melanization of the epidermis and thickening of the stratum corneum. The exact mechanics are unknown but it has been suggested that melanocytes in the hair follicles are stimulated to move up the follicle and to repopulate the epidermis. (Ortonne, et al, 1979)4 
III. INDICATIONS AND USAGE
As a topical repigmenting agent in vitiligo in conjunction with controlled doses of ultraviolet A (320-400 nm) or sunlight.
IV. CONTRAINDICATIONS
A. Patients exhibiting idiosyncratic reactions to psoralen compounds or a history of sensitivity reactions to them.
B. Patients exhibiting melanoma or with a history of melanoma.
C. Patients exhibiting invasive skin carcinoma generally.
D. Patients with photosensitivity diseases such as porphyria, acute lupus erythematosus, xeroderma pigmentosum, etc.
E. Children under 12 since clinical studies to determine the efficacy and safety of treatment in this age group have not been done. 
V. WARNINGS
SKIN BURNS
Serious skin burns from either UVA or sunlight (even through window glass) can result if recommended exposure schedule is exceeded and/or protective covering or sunscreens are not used. The blistering of the skin sometimes encountered after UV exposure generally heals without complication or scarring. (Farrington Daniels, Jr., M.D., personal communication). Suitable covering of the area of application or a topical sunblock should follow the therapeutic UVA exposure.
CARCINOGENICITY
Animal Studies. Topical methoxsalen has been reported to be a potent photocarcinogen in certain strains of mice. (Pathak et al 1959) 5.
Human Studies. None of our clinical investigators reported skin cancer as a complication of topical treatment for vitiligo. However, it is recommended that caution be exercised when the patient is fair-skinned, has a history of prior coal tar UV treatment, or has had ionizing radiation or taken arsenical compounds. Such patients who subsequently have oral psoralen – UVA treatment (PUVA) are at increased risk for developing skin cancer.
CONCOMITANT THERAPY
Special care should be exercised in treating patients who are receiving concomitant therapy (either topically or systemically) with known photosensitizing agents such as anthralin, coal tar or coal tar derivatives, griseofulvin, phenothiazines, nalidixic acid, halogenated salicylanilides (bacteriostatic soaps), sulfonamides, tetracyclines, thiazides and certain organic staining dyes such as methylene blue, toluidine blue, rose bengal, and methyl orange. 
VI. PRECAUTIONS
A. This product should be applied only in small well-defined lesions and preferably on lesions which can be protected by clothing or a sunscreen from subsequent exposure to radiant UVA. If this product is used to treat vitiligo of face or hands, be very emphatic when instructing patient to keep the treated areas protected from light by use of protective clothing or sunscreening agents. The area of application may be highly photosensitive for several days and may result in severe burn injury if exposed to additional UV or sunlight.
B. CARCINOGENESISSee Warning Section.
C. Pregnancy Category CAnimal reproduction studies have not been conducted with topical methoxsalen. It is also not known whether methoxsalen can cause fetal harm when used topically on a pregnant woman or affect reproductive capacity. It is not known to what degree, if any, topical methoxsalen is absorbed systemically. Topical methoxsalen should be used in women only when clearly indicated.
D. Nursing MothersIt is not known whether topical methoxsalen is absorbed or excreted in human milk. Caution is advised when topical methoxsalen is used in a nursing mother.
E. Pediatric UsageSafety and effectiveness in children below the age of 12 years have not been established.
VII. ADVERSE REACTIONS
Systemic adverse reactions have not been reported. The most common adverse reaction is severe burns of the treated area from overexposure to UVA, including sunlight. TREATMENT MUST BE INDIVIDUALIZED. Minor blistering of the skin is not a contraindication to further treatment and generally heals without incident. Treatment would be the standard for burn therapy. Since 1953, many studies have demonstrated the safety and effectiveness of topical methoxsalen and UVA for the treatment of vitiligo when used as directed. (Lerner, A.B., et al, 1953)6 (Fitzpatrick, T.B., et al, 1966)7 (Fulton, James F. et al, 1969)8
VIII. OVERDOSAGE
This does not apply to topical usage. In the unlikely event that the lotion is ingested, standard procedures for poisoning should be followed, including gastric lavage. Protection from UVA or daylight for hours or days would also be necessary. The patient should be kept in a darkened room.
IX. ADMINISTRATION
OXSORALEN Lotion is applied to a well-defined area of vitiligo by the physician and the area is then exposed to a suitable source of UVA. Initial exposure time should be conservative and not exceed that which is predicted to be one-half the minimal erythema dose. Treatment intervals should be regulated by the erythema response; generally once a week is recommended or less often depending on results. The hands and fingers of the person applying the medication should be protected by gloves or finger cots to avoid photosensitization and possible burns.
Pigmentation may begin after a few weeks but significant repigmentation may require 6 to 9 months of treatment. Periodic re-treatment may be necessary to retain all of the new pigment. Idiopathic vitiligo is reversible but not equally reversible in every patient. Treatment must be individualized. Repigmentation will vary in completeness, time of onset, and duration. Repigmentation occurs more rapidly in fleshy areas such as face, abdomen, and buttocks and less rapidly over less fleshy areas such as the dorsum of the hands or feet.
X. HOW SUPPLIED
Oxsoralen Lotion containing 1% methoxsalen (8-methoxypsoralen) packaged in 1 ounce (29.57 ml) amber glass bottles (NDC 0187-0402-31). Store at 25°C (77°F); excursion permitted to 15°C-30°C (59°F-86°F).