英文药名: Oxsoralen-ultra(methoxsalen capsules)

中文药名: 甲氧沙林胶囊(强)

生产厂家: ICN Pharmaceuticals

药品名称

通用名称：甲氧沙林
英文名：Methoxsalen
其它中文名：8-甲氧补骨脂素、8-甲氧基补骨脂素、甲氧补骨脂素、敏白灵
其它英文名：8-Methoxypsoralen、Meladinin、Methoxypsoralen、Methoxysoralen
规格

甲氧沙林硬胶囊10mg,甲氧沙林乳液 30ml.
药理作用　

药效学
本品为补骨脂素的衍生物，有光感活力。使引起表皮红斑、黑色素和细胞毒的确切机制尚不清楚，但能使黑色素形成细胞中的酪氨酸酶活力增加，亦可抑制 DNA合成、细胞分裂和表皮更替，有效的色素形成需要有机能的黑色素细胞存在。
药动学
口服约 95％从胃肠道吸收，有些患者效果差，推测与吸收不良有关。蛋白结合率高。可被320～400nm的长波紫外线A激活，最大作用波长为 365nm。Ｔ1/2硬胶囊为 1.1小时，软胶囊为 2小时。白癜风患者需 6个月或更长时间起效，银屑病需30余次(10周或更长时间)，皮肤对日光敏感性增加为l小时，皮肤晒黑数天内。光敏达峰时间硬胶囊为 3.9～4.25小时，软胶囊为1.5～2.1小时。平均最小红斑量(MED)软胶囊的要比硬胶囊每 1平方厘米的能量少。与 250ml牛奶进服时血药浓度峰值硬胶囊为l.5～6小时(平均 3小时)，软胶囊为 0.5～4小时(平均 1.8小时)。作用时间，增加皮肤对日光敏感约 8小时。本品在肝脏代谢，代谢物主要从肾脏排泄，8小时内排出 80～90％，24小时内95％，粪便排出 4～10％。
适应症　

本品需与长波紫外线 A(UVA)合用(两者合用方式称PUVA)治疗白癜风、银屑病、蕈样肉芽肿；PUVA亦用于治疗斑秃、异位性皮炎、湿疹、扁平苔藓，增加皮肤的日光耐受性。
用法用量

(1)治牛皮癣：
①加黑光照射法：方法同补骨脂素，1次服用量为 30—50mg。
②加紫外线照射法：饭后服20—50mg， 1小时后矿泉水全身浸浴 20—30分钟， 2小时后长波紫外线照射，照射量从最小红斑量开始逐渐增加。外用者于照射前，距正常皮肤 0.5cm处的皮损范围内涂本品的 0.5％配剂。按此法每日治疗 1次(星期日休息)，持续至皮损消失后逐渐减少治疗次数，直至每周或每月 1次，长期巩固治疗。据报道，按本法治疗 46例，治愈(皮损全部消失) 45例，显效 1例。平均治疗 9次见效， 60次痊愈。
(2)治白癜风： 0.1溶液(白癜风溶液)涂搽。
1．硬胶囊剂成人常用量：
①白癜风，在照射 UVA前 2— 4小时口服20mg，每周 2— 3次(至少相隔 48小时)，日光照射时，对淡肤色者首次不超过 15分钟，对中等度肤色者，不超过20分钟，对深肤色者不超过25分钟，根据出现红斑和压痛情况，以后每次治疗可增加5分钟，如采用人工光源照射时，首次照射时间不超过日光照射发生红斑时间的一半；
②银屑病或草样肉芽肿，在照射 UVA前24小时，按体重口服0.6mg/kg，每周 2— 3次(至少相隔 48小时)，暴光时间需按照采用特殊光源的说明根据皮肤类型和治疗效应而定，暴光次数可逐渐减少至维持治疗。

下面为参照体重的通常剂量表。

体重（kg） 剂量（mg）
<30 10
30－50 20
51－65 30
66－80 40
81－90 50
91－115 60
>115 70
12岁以上儿童剂量同成人常用量，12岁以下禁用。
2．软胶囊成人常用量：治疗银屑病，在照射 UVA前 1.5— 2小时按体重口服0.4mg/kg，每周 2— 3次，余同硬胶囊。
3．外用洗剂涂在白癜风损害上，等 1一 2分钟待干，再涂 1次，2— 2.5小时照光；随后以肥皂和水洗净，盖上遮光物。日光照射开始不超过 1分钟，以后逐渐增加。人工光源首次照射时间不超过暴晒日光产生红斑的一半时间，通常3— 5天或7天照射1次。
任何疑问,请遵医嘱!
禁用/慎用

下列情况应禁用：严重心血管病、白化病、夏令水疱病、传染源白斑、急性红斑狼疮、皮肌炎、多形性日光疹、卟啉病、着色性干皮病、白内障、肝功能损害。
下列情况应慎用：慢性感染、胃肠道疾病、皮肤癌病史、日光敏感家族史，新近接受过 X射线或细胞毒治疗、砷剂、煤焦油和 UVB治疗者。
给药说明　

对长期应用本品的患者，需定期随访抗核抗体试验、血象、肝肾功能、需注意有无白内障、黑色素瘤或皮肤癌的发生。
①口服可能需在 6— 8周起作用，不要随意增加药物剂量或 UVB照射。硬胶囊剂与食物或牛奶一起服(软胶囊剂与低脂肪饮食或低脂肪牛奶一起服)，以减少胃肠道刺激；
②治疗中不要将本品软胶囊与硬胶囊互换，因前者比后者具较大生物有效性和较早发生光敏；
③有些临床医师认为治疗银屑病经15次照射无效应时，需增加剂量，通常本品剂量不需增加；
④本品剂量根据体重计算，倘患者体重改变，不要改变剂量，如体重改变显著，可调整 UVA暴光时间；
⑤倘用作增加皮肤对日光的耐受性，治疗限制在 14天内；
⑥暴晒日光或紫外线时间需根据患者皮肤类型和耐受性而个体化，在高原和中午日光暴晒时间需缩短；
⑦对有红皮病型银屑病患者采取同日光过敏皮肤类型相同的治疗；
⑧采用PUVA治疗前24小时和治疗后 8小时，需保护皮肤勿晒阳光(包括透过玻璃窗或多云天气)，穿长袖衬衫、宽松长裤、阔边帽、戴手套和具有保护系数至少15遮光物质涂在不能以衣服遮盖的部位，口唇涂防光系数至少 15的唇膏；
⑨在面、腹、臀等部位，最快出现色素再生，四肢和手足较迟；
⑩倘皮肤出现烧灼或水泡，暂停治疗；倘发生肝功能受损，需减少本品剂量或停止治疗；对超剂量的治疗：在 2— 3小时内，导引呕吐，将患者移至暗室至少24小时，如发生意外的照射过度或曝晒日光，可将患者移至暗室至少24小时，如在 24小时内出现Ⅱ度烧伤(显著红斑而无水肿)，提示开始潜在的严重烧伤信号，因对 PUVA的红斑反应峰通常约发生在口服本品 48小时后，根据发生的范围和严重度进行烧伤的对症治疗。
外用比口服更能引起不易预料的光敏感效应，仅适于在小于 10平方立米的面积上涂用，照射日光或 UVA后将所涂药品去掉；照射日光或 UVA的时间亦需根据患者的皮肤类型和耐受性适当调节。外用时造成表皮中的本品浓度较口服时为高，故通常采用的 UVA剂量较口服时为低。在外用和 UVA照射治疗后，至少 12— 48小时避免日光照射。当色素比红斑形成早且很长时间时，皮肤可以对本品产生耐受性，色素沉着过度可减少以后的效应。稀释至 1：1000或 1：10000的浓度可避免严重反应。色素形成通常在治疗数周后开始，但显著色素再生需经6— 9个月，需周期性再治疗，以保持所有新生色素。
不良反应

①曾报道可发生白内障；
②动物实验发现本品能诱发 UVA的致癌作用，对人有增加鳞状细胞癌发生的危险性，特别是患者存在危险因子时如淡色皮肤，对日光敏感，皮肤癌病史，暴露于电离放射，过多在日光中曝晒，或以焦油和紫外线B(UVB)、砷或外用氮芥治疗过的患者；
③皮肤早老表现；
④中毒性肝炎；
⑤紫外线超剂量或超时间照射的症候为皮肤起水泡和脱屑、发红和疼痛、特别是足和小腿的肿胀；
⑥还可有皮肤瘙痒、恶心、头晕、头痛、精神抑郁、神经质和失眠。对骨髓造血系统有影响,可有白细胞减少.
药物相互作用

治疗期间不食用含有呋喃香豆素的食物(如酸橙、无花果、香菜、芥末、胡萝卜或芹菜)，以免发生附加的光毒性危险；与其他光敏性药物亦不得同时服用；与吩噻嗪类药物同用可加剧对脉络膜、视网膜和晶体的眼内光化学损伤。

包装规格：

甲氧沙林胶囊（强）|Oxsoralen-ultra (methoxsalen capsules)  10mg*100 胶囊/盒 

甲氧沙林胶囊|Ultramop (Methoxsalen Capsules)   10mg*100 胶囊/盒

甲氧沙林片|Oxsoralen (methoxsalen)    10mg*120 片/盒

甲氧沙林乳液|Oxsoralen(methoxsalen lotion) ：  30ml/瓶

甲氧沙林露1%|Ultramop (Methoxsalen Lotion)     25ml/瓶 

Oxsoralen (methoxsalen) is for the treatment of severe psoriasis. Certain skin problems present a unique set of challenges that can evoke a wide range of personal respo

nses. Among the many diseases are psoriasis, producing red and scaly patches; vitiligo, a disease in which skin color is lost; and mycosis fungoides, a type of lymphoma. Methoxsalen, the active ingredient in Oxsoralen-Ultra, belongs to the group of compounds called psoralens. It is used along with ultraviolet light (found in sunlight and some special lamps) in a treatment call PUVA (Psoralen plus UVA) to treat psoriasis and vitiligo. Methoxsalen is also used together with ultraviolet light in photopheresis, used to treat the white blood cells associated with mycosis fungoides.

PUVA is an acronym for Psoralen plus UVA light and is a special type of phototherapy that combines the use of the drug Oxsoralen Ultra (methoxsalen) with exposure of the skin to UVA (ultraviolet A) light. Oxsoralen Ultra (methoxsalen) capsules make the skin more sensitive to light.

Ultraviolet A light is composed of the longest wavelengths in the ultraviolet spectrum. However, UVA light does have the property of being able to react with light-activated chemicals in the skin, or so-called photosensitizing agents. Psoralens, such as those present in Oxsoralen Ultra (methoxsalen), are photosensitizing compounds that are activated by UVA light. If they are present in the skin at the time of exposure to UVA light, they greatly increase the effect of the light on the skin. This increased sensitivity is the key to the beneficial effect of PUVA therapy.

PUVA is an effective therapy for severe recalcitrant psoriasis. Another benefit of PUVA therapy is that it tends to induce long-term remissions in psoriasis.

Your doctor will prescribe the appropriate number of Oxsoralen-Ultra (Methoxsalen Capsules, USP, 10mg) capsules to take before a PUVA treatment. Be sure to always take the exact dosage prescribed. Swallow the capsules with low-fat food or milk 1.5 to 2 hours before your appointment.

The PUVA treatment should only take place in your doctor's office, where you will stand in a special lighted area or booth for a short period of time. (A hand-held light unit may be used for smaller body areas.) In the PUVA treatment area, you will be surrounded by light bulbs that deliver special UVA light. You will be unclothed or partially clothed (depending on the size of the area to be treated) and you must wear UVA protective goggles, which will be provided by your doctor. Male genitalia must be shielded unless the area is being treated for psoriasis. Other sensitive areas such as the face, lips and breasts may also require protection. Treatment time may last from a few seconds to over 10 minutes and may vary from one treatment to the next.

Psoriasis sufferers who have been treated unsuccessfully with conventional treatments are candidates for PUVA therapy. PUVA therapy involves the ingestion of Oxsoralen-Ultra (Methoxsalen Capsules, USP, 10mg) 1.5 to 2 hours prior to exposure to UVA light. The dose of Oxsoralen-Ultra capsules you take is held constant and is determined by your weight. The interval between taking Oxsoralen-Ultra capsules and being exposed to light is also held constant because peak levels of psoralen are usually reached in the skin between 1.5 to 2 hours after ingestion.

The variable in PUVA therapy is the dose of UVA light you are given. The initial dose is low and may be determined by your past history of sunburning and suntanning, or by testing your response to PUVA. The dose of UVA light is gradually increased in subsequent treatment as your tolerance to the treatment increases.

The dose of UVA light delivered during PUVA therapy is measured in joules per square centimeter (a measure of energy) and is translated into a given number of minutes of treatment. The output of the treatment units varies over time and different units emit different amounts of energy. Therefore, even if your dose of UVA light is constant, your treatment times may vary. Treatments will be required two to three times each week until your skin disease has cleared. Less frequent treatment is necessary to maintain a clear state. Most patients develop a tan or deepening of their normal skin pigmentation from PUVA therapy. The tanning may be uneven at first, with skin color lighter in areas affected by psoriasis. Some patients also develop freckles   particularly dark freckles   in areas affected by psoriasis. Burning from light treatment is a potential serious side effect of PUVA therapy. Regardless of how carefully light treatment is administered, some redness is likely to occur, especially at the beginning of therapy. If you experience any degree of redness or burning following treatment, be sure to alert your medical provider. The light dose may need to be lowered or you may need to skip a treatment. The most common side effects of PUVA therapy are:

Skin Burning. Serious burns from either UVA or sunlight (even through a window glass) can result if the recommended dosage of the drug and/or exposure schedules are exceeded.
Sunburn. Some redness is likely to occur in the skin at the beginning of PUVA therapy.
Pigmentation. Many patients observe pigmentation or tanning of their skin.
Nausea. Nausea may occur after taking the Oxsoralen-Ultra (Methoxsalen Capsules, USP, 10mg) capsules. This may be avoided or lessened by taking the medication with milk or grain-type foods such as crackers, toast or bagels, or by taking the drug just after a meal.
Itching. Itching commonly occurs as a result of light treatment. Numerous ointments are available to soothe mild itching. It is important to make your medical provider aware of any itching you have. With severe itching, it may be necessary to lower the light dose or skip a treatment. Call your medical provider before taking your capsules if itching is severe.
Dry skin. If PUVA therapy leads to dry skin, apply a moisturizing lotion while your skin is still damp after showering or bathing. If the moisturizer does not relieve your dry skin, ask your medical provider for other recommendations.
Friction blisters. Blisters are a fairly common occurrence, particularly on the hands and feet.
Ankle edema. A small number of patients develop swelling of the ankles as the first sign of phototoxicity.
Aggravation of skin disease. PUVA can sometimes aggravate and worsen the skin disease.
Increased hair growth. Hypertrichosis, or an increased growth of hair, particularly on the face, is an occasional side effect.

The total number of treatments depends on your diagnosis. In the beginning, treatments will be necessary two to three times per week. Eventually, the number decreases to a maintenance schedule or reaches a point at which you can stop completely if your skin remains clear. Your treatment must be spaced so that at least 48 hours elapse between sessions. The average course of treatment lasts approximately 12 weeks. PUVA therapy clears or dramatically improves psoriasis in over 84% of patients and can lead to extended remissions. Once your skin has cleared, you may continue PUVA therapy on a maintenance schedule of once a week, and then gradually decrease your treatments to one per month if your skin remains clear. If it is still clear after three to four months of maintenance therapy, you may discontinue PUVA therapy. If you experience a flare-up, therapy will be reinstated two to three times a week.

Long-term effects associated with PUVA therapy:

Skin cancer. Some people are at a higher risk than the normal population for developing skin cancer, including people who have had previous non-melanoma skin cancer, arsenic therapy or X-ray therapy to the skin, as well as individuals with extremely light complexions which always burn and never tan. In general, these patients are not considered for PUVA therapy unless strong extenuating circumstances exist in favor of it. For all other patients, there may be a minimally higher incidence of skin cancer. Because it is impossible to know exactly how much light a patient needs in order to produce a skin cancer, your skin should frequently be examined for abnormal growths throughout your PUVA therapy.
Cataracts. Animal studies show that cataracts may be produced as a result of excess PUVA therapy when no eye protection is used. If a patient undergoing PUVA therapy does not carefully protect his or her eyes by wearing appropriate protective sunglasses, there may be a risk of developing cataracts. To date, very few eye problems have been experienced with our patients since most are conscientious about following the simple instructions for eye protection during and following PUVA therapy. Pre-treatment eye exams and yearly followup exams are also required.

Shielding the eyes after Oxsoralen-Ultra capsule ingestion and for 24 hours thereafter during daylight hours is an absolute requirement. Make sure you wear special wraparound sunglasses that absorb ultraviolet light or block it entirely. These special sunglasses should be worn when you are outdoors, riding in a car or sitting near a window. Do not attempt to drive in dim light while wearing dark glasses. On non-treatment days, you should routinely wear either plastic wraparound or UVA-blocking sunglasses. Prescription sunglasses should be checked for their ability to block UVA light. This check may be performed at the phototherapy unit by your phototherapist. Do not allow your skin or lips to be exposed to sunlight for eight hours after treatment. In addition, do not expose your skin to either sunlight or sunlamps within 24 hours of treatment. It is advisable to wear protective clothing (i.e., hat, gloves, long sleeves) to cover as much of your body as possible, and to use a UVA-blocking sunscreen product with a sun protection factor (SPF) of at least 15. You must not sunbathe for 24 hours before and after PUVA therapy.