英文药名: Uvadex(methoxsalen  TABLETS)

中文药名: 甲氧沙林片
药品介绍
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。

What is Generic Uvadex (Methoxsalen)?
Generic Uvadex (Methoxsalen) is a naturally occurring substance that is reactive to light. It works by enhancing the body's sensitivity to ultraviolet light A (UVA).Generic Uvadex (Methoxsalen) is used in combination with UVA light therapy to treat severe psoriasis.Generic Uvadex (Methoxsalen) may also be used for other purposes not listed in this medication guide.
What is the most important information I should know about Generic Uvadex (Methoxsalen)?
You should not use this medication if you are allergic to Generic Uvadex (Methoxsalen), or if you have a history of skin cancer or damage to the lenses of your eyes due to surgery, injury, or genetic condition.Before taking Generic Uvadex (Methoxsalen), tell your doctor if you have lupus, porphyria, heart disease, kidney or liver disease, a history of cataracts, a skin pigment disorder, if you are extremely sensitive to sunlight, or if you have recently gained or lost weight.
There are many other drugs that can interact with Generic Uvadex (Methoxsalen), including drugs applied to the skin. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.After taking Generic Uvadex (Methoxsalen) and receiving UVA treatment, you must protect your eyes and skin from natural sunlight (even sun shining through a window).
Wear wraparound UVA-absorbing sunglasses for at least 24 hours after your light treatment, even while you are indoors near a window.You may develop cataracts if you do not properly protect your eyes after you are treated with Generic Uvadex (Methoxsalen) and UVA treatment.Use a sunscreen with a minimum SPF of 15, and wear protective clothing including a hat and gloves for at least 8 hours after your light treatment.
Follow your doctor's instructions about applying topical psoriasis medications or any moisturizing lotions after your Generic Uvadex (Methoxsalen) and UVA treatment.
What should I discuss with my health care provider before taking Generic Uvadex (Methoxsalen)?
You should not use this medication if you are allergic to Generic Uvadex (Methoxsalen), or if you have:
* a history of skin cancer; or   
* damage to the lenses of your eyes due to surgery, injury, or genetic condition.
If you have certain conditions, you may need a dose adjustment or special tests to safely use this medication. Before using Generic Uvadex (Methoxsalen), tell your doctor if you have:
* heart disease;   
* kidney disease;   
* liver disease;   
* systemic lupus erythematosus;   
* porphyria (a genetic enzyme disorder that causes symptoms affecting the skin or nervous system);   
* a history of cataracts;   
* a skin pigment disorder;   
* if you are extremely sensitive to sunlight; or   
* if you have recently gained or lost weight.
FDA pregnancy category C. Generic Uvadex (Methoxsalen) may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether Generic Uvadex (Methoxsalen) passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.
How should I take Generic Uvadex (Methoxsalen)?
Take this medication exactly as prescribed by your doctor. Do not take Generic Uvadex (Methoxsalen) in larger amounts or for longer than recommended. Follow the directions on your prescription label. Taking too much Generic Uvadex (Methoxsalen) can cause your skin to be overly sensitive to light, and severe sunburn may result.Generic Uvadex (Methoxsalen) is usually taken 90 minutes to 2 hours before you are scheduled to receive UVA treatment. The timing of your medication may depend on whether you are taking the soft gelatin capsule or the hard gelatin capsule.
The Generic Uvadex (Methoxsalen) soft gelatin capsule is more easily absorbed in the body than the hard gelatin capsule. For this reason, you may be sensitive to UVA treatment more quickly after taking the soft gelatin capsule.Take this medication with low-fat food or milk if it upsets your stomach. After taking Generic Uvadex (Methoxsalen) and receiving UVA treatment, you must protect your eyes from natural sunlight (even sun shining through a window). Wear sunglasses for at least 24 hours after treatment. For utmost protection, wear a pair of wraparound UVA-absorbing sunglasses, even while you are indoors near a window.
You may develop cataracts if you do not properly protect your eyes after you are treated with Generic Uvadex (Methoxsalen) and UVA treatment.
Follow your doctor's instructions about applying topical psoriasis medications or any moisturizing lotions after your Generic Uvadex (Methoxsalen) and UVA treatment.
While taking Generic Uvadex (Methoxsalen), check your skin regularly for signs of skin cancer, such as a small growth or nodule, a scaly or crusted lesion, a brownish spot or speckles, or a change in the size, color, or feel of a mole. After receiving UVA treatments, you may need to check your skin for signs of cancer throughout the rest of your life.If you store Generic Uvadex (Methoxsalen) at home, keep it at room temperature away from moisture and heat.
What happens if I miss a dose?
Call your doctor for instructions if you miss your Generic Uvadex (Methoxsalen) dose or forget to take the medicine within 90 minutes to 2 hours before your scheduled UVA treatment.The timing of when you take Generic Uvadex (Methoxsalen) is critical in relation to UVA treatment. Therefore, you may need to reschedule your light therapy appointment if you have not taken Generic Uvadex (Methoxsalen) at the proper time beforehand.
What happens if I overdose?
Stay in a dark room and call your doctor at once if you think you have used too much of this medicine. You will be extremely sensitive to light after an overdose, and you may need to seek emergency medical attention.
Overdose symptoms may include nausea, dizziness, or fainting.
What should I avoid while taking Generic Uvadex (Methoxsalen)?
Generic Uvadex (Methoxsalen) will make your skin more sensitive to sunlight and sunburn may result. Even sunlight shining through a glass window can expose you to harmful UV rays. Avoid exposure to sunlight or artificial UV rays other than your scheduled light therapy treatments.
Before your UVA treatment: Do not expose your skin to sunlight for at least 24 hours before you take Generic Uvadex (Methoxsalen). Avoid applying sunscreen to areas of psoriasis that will be treated with UVA therapy.
After your UVA treatment: Do not expose your skin to sunlight for at least 8 hours after your UVA treatment. Wear protective clothing including a hat and gloves. Use a sunscreen with a minimum SPF of 15, and apply it to all uncovered skin areas exposed to light.
Side effects of Generic Uvadex (Methoxsalen):
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Generic Uvadex (Methoxsalen) is expected to produce skin redness that may not occur until several hours after your UVA treatment. This redness may last for 2 or 3 days. You may also have slight swelling. These are normal effects of the medication and UVA treatment.Call your doctor at once if you have a serious side effect such as:
* severe skin redness within 24 hours after UVA treatment;   
* severe itching, swelling, or skin discomfort;   
* blisters, pimples, or skin rash;   
* feeling like you might pass out; or   
* worsening of your psoriasis.
Less serious side effects may include:
* nausea, upset stomach;   
* headache, dizziness;   
* depressed mood;   
* sleep problems (insomnia);   
* feeling nervous;   
* leg pain; or   
* mild skin itching or tenderness.
This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect.
What other drugs will affect Generic Uvadex (Methoxsalen)?
Tell your doctor about all medications you use now or have used in the past (including those applied to the skin), especially:
* arsenic trioxide (Trisenox);   
* anthralin (Drithrocreme, Micanol);   
* a bacteriostatic soap;   
* coal tar (Betatar Gel, Denorex, Fototar, Ionil T, MG217, Neutrogena T/Gel or T/Derm, Tegrin Medicated Soap, and others);   
* griseofulvin (Fulvicin, Grisactin);   
* nalidixic acid (NegGram);   
* a staining dye such as methylene blue, toluene blue, rose bengal, or methyl orange;
* a sulfa drug (Bactrim, Gantanol, Septra, and others);   
* a diuretic (water pill) such as chlorothiazide (Diuril), hydrochlorothiazide (HCTZ, HydroDiuril, Hyzaar, Lopressor, Vasoretic, Zestoretic),       chlorthalidone (Hygroton, Thalitone), indapamide (Lozol), metolazone (Mykrox, Zaroxolyn), and others;
* an antibiotic such as ciprofloxacin (Cipro), ofloxacin (Floxin), norfloxacin (Noroxin), levofloxacin (Levaquin), lomefloxacin (Maxaquin), and others;   
* a tetracycline antibiotic such as demeclocycline (Declomycin), doxycycline (Adoxa, Doryx, Oracea, Vibramycin), minocycline (Dynacin, Minocin, Solodyn, Vectrin), or tetracycline (Brodspec, Panmycin, Sumycin, Tetracap); or   
* medicine to treat a psychiatric disorder, such as chlorpromazine (Thorazine), fluphenazine (Prolixin), mesoridazine (Serentil), perphenazine (Trilafon), prochlorperazine (Compazine), thioridazine (Mellaril), or trifluperazine (Stelazine).
This list is not complete and there may be other drugs that can interact with Generic Uvadex (Methoxsalen). Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.