药理毒理
他扎罗汀乳膏/凝胶为皮肤外用的维生素A酸类的前体药，具有调节表皮细胞分化和增殖以及减少炎症等作用。在动物和人体中通过快速的脱酯作用而被转化为他扎罗汀酸，该活性产物可相对选择性地与维A酸受体的β和γ亚型结合，但其治疗银屑病和寻常痤疮的确切机理尚不清楚。本品对家兔皮肤有局部刺激作用，但无全身毒性作用。致突变试验和致癌试验结果均为阴性。文献报道，生殖毒性试验显示家兔和大鼠外用和口服本品时，致畸试验呈阳性。大鼠口服他扎罗汀后可影响其生育力。他扎罗汀是一种能引起致畸作用的物质，人体用药达到什么水平能产生致畸作用尚不清楚。

药代动力学
据文献报道，外用他扎罗汀，其结构中的酯被水解生成活性代谢物他扎罗汀酸，在血浆中几乎不能检测出原药。他扎罗汀酸与血浆蛋白高度结合（＞99%）。他扎罗汀和他扎罗汀酸最终代谢为砜、亚砜以及其它极性化合物，所有这些代谢物均通过尿和粪便排泄。
无论健康人、银屑病、寻常痤疮患者外用他扎罗汀时，他扎罗汀酸的半衰期相似，均为18小时。对9名银屑病患者14天的多剂研究中，每天给药一次，将0.1%他扎罗汀乳膏涂于未包合的皮肤上（占体表面积5～35%；平均值±偏差为14±11%），最后一次给药后8小时，测得他扎罗汀酸的Cmax为2.31±2.78ng/ml，其中5位给药剂量为2mg/cm2的患者在第15天时，测得AUC0～24hr为31.2±35.2ng?hr/ml。0.05%或0.1%他扎罗汀乳膏治疗银屑病的临床试验中，139名患者有3名可检测出血浆中他扎罗汀浓度，最高的为0.09ng/ml，139名患者中有78名可检测到他扎罗汀酸。其中有3名使用0.1%乳膏的患者，其血浆中他扎罗汀酸浓度大于1ng/ml，最高为2.4ng/ml。
但由于血样随时间的变化，药物所涂皮损范围不同及用药剂量差别，准确的最大血浆浓度尚不清楚。
中重度寻常痤疮患者外用0.1%他扎罗汀乳膏，每天一次，其中8位用于面部，10位用于体表（占体表面积15%），均为女性患者，治疗29天。在第15天时两个剂量组的他扎罗汀酸Cmax和AUC值达峰值。皮损占体表15%面积的痤疮患者，其Cmax和AUC高于面部痤疮患者10倍。该研究中，第15天时，测得最大Cmax为1.91ng/ml。面部痤疮组第15天测得的他扎罗汀酸Cmax和AUC0-24h分别为0.10±0.06ng/ml和1.54±1.01ng?hr/ml；另一组（皮损占体表15%的痤疮患者）的Cmax和AUC0-24h分别为1.20±0.41ng/ml和17.01±6.15ng?hr/ml。面部痤疮试验组中，他扎罗汀酸的药代动力学均在第8天达到稳态，而躯体部位患者痤疮（占体表15%）的患者在第15天时达到稳态。
在一项Ⅲ期临床试验中，0.1%他扎罗汀乳膏用于治疗面部寻常痤疮，48位患者入组（男性26位，女性22位），每天用药一次，治疗12周。他扎罗汀酸的血浆浓度在第4和第8周时分别为0.078±0.073ng/ml（N=47）和0.052±0.037ng/ml（N=42）。个体血浆浓度最高为0.41ng/ml，为女性患者，发生于治疗第4周，他扎罗汀酸的浓度大小与年龄、体重无关。

适应症
适用于外用治疗寻常性斑块型银屑病及寻常痤疮。

用法用量
银屑病：外用，每晚临睡前半小时将适量本品涂于患处。用药前，先清洗患处；待皮肤干爽后，将药物均匀涂布于皮损上，形成一层薄膜；涂药后应轻轻揉擦，以促进药物吸收；之后再用肥皂将手洗净。
痤疮：清洁面部，待皮肤干爽后，取适量（2mg/cm2）他扎罗汀乳膏/凝胶涂于患处，形成一层薄膜，每天一次，每晚用药。

不良反应
银屑病：外用后，主要不良反应为瘙痒、红斑和灼热，少数患者（10%以下）有皮肤刺痛、干燥和水肿，有的出现皮炎、湿疹和银屑病恶化。
寻常痤疮：用药后主要的不良反应有脱屑、皮肤干燥、红斑、灼热，少数患者（1～5%）出现瘙痒、皮肤刺激、疼痛和刺痛。

禁忌
1、孕妇、哺乳期妇女及近期有生育愿望的妇女禁用。
2、对本品或其他维甲酸类药物过敏者禁用。

注意事项
1、育龄妇女在开始他扎罗汀乳膏/凝胶治疗前2周内，必须进行血清或尿液妊娠试验，确认为妊娠试验阴性后，在下次正常月经周期的第2天或第3天开始治疗。在治疗前，治疗期间和停止治疗后一段时间内，必须使用有效的避孕方法。治疗期间，如发生妊娠，应立即与医生联系，共同讨论对胎儿的危险性及是否继续妊娠等。
2、避免药物与眼睛、口腔和粘膜接触，并尽量避免药物与正常皮肤接触。如果与眼接触，应用水彻底冲洗。
3、如出现瘙痒等皮肤刺激作用，尽量不要搔抓，可涂少量润肤剂；严重时，医生应建议患者停用本品或隔天使用一次。
4、他扎罗汀乳膏不宜用于急性湿疹类皮肤病。
5、治疗期间，要避免在阳光下过多暴露。
6、本品不能口服。

孕妇及哺乳期妇女用药
本品有致畸性，禁用于孕妇。动物试验证明，在乳汁中能检测出放射活性分泌物，故本品禁用于哺乳期妇女。

儿童用药
对18岁以下的银屑病患者及12岁以下的痤疮患者使用本品的疗效和安全性资料尚未建立。

老年用药
老年患者与年轻患者用药的安全性和有效性没有差别，治疗寻常痤疮的临床试验中，他扎罗汀乳膏/凝胶尚未用于年龄大于65岁患者。

药物相互作用
1、患者在同时服用具有光敏性药物时（例如四环素、氟喹诺酮、酚噻嗪、磺胺），应小心使用，因为该类药物增加光敏性。
2、应避免同时使用能使皮肤变干燥的药物和化妆品。

药物过量
过量使用本品不会加快皮损好转，还会产生皮肤发红、脱皮及其他不适。

【原产地英文商品名】TAZORAC 0.05% CREAM 60g/piece
【原产地英文药品名】TAZAROTENE
【中文参考商品译名】
注：以产品不同规格和不同的价格，购买时请以电话咨询为准！
·TAZORAC 0.05%乳膏 30克/支
·TAZORAC 0.05%乳膏 60克/支
·TAZORAC 0.1%乳膏 30克/支
·TAZORAC 0.1%乳膏 30克/支
【中文参考商品译名】TAZORAC 0.05%乳膏 60克/支
【中文参考药品译名】他扎罗汀
【生产厂家中文参考译名】ALLERGAN
【生产厂家英文名】ALLERGAN

Tazorac
Generic Name: tazarotene topical (ta ZAR oh teen)
Brand Names: Avage, Tazorac

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What is Tazorac (tazarotene topical)?
Tazarotene is a compound similar to vitamin A. It helps the skin to renew itself more quickly and may improve the appearance and texture of skin.

The Tazorac brand of tazarotene topical gel and cream are used to treat plaque psoriasis (psoriasis with scaly patches) and to treat facial acne. The Avage brand of tazarotene cream is used to reduce the appearance of fine wrinkles on the face, mottled light and dark skin patches on the face, and benign facial lentigines (noncancerous freckles).

Tazarotene topical may also be used for purposes other than those listed in this medication guide.

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What is the most important information I should know about Tazorac (tazarotene topical)?
Do not use tazarotene topical if you are pregnant or if you could become pregnant. Tazarotene topical is in the FDA pregnancy category X. This means that tazarotene topical is known to cause birth defects in an unborn baby. You must take a pregnancy test and have negative results within two weeks before starting treatment with tazarotene topical and treatment should be started during a menstrual period. Brith control must be used during treatment. If you become pregnant, stop using birth control, or miss your menstrual period, immediately stop using tazarotene topical and notify your doctor. Avoid exposure to sunlight or artificial UV rays (e.g., sunlamps). Use a sunscreen (minimum SPF 15) and wear protective clothing during the day when being treated with tazarotene topical. Do not use tazarotene topical on skin that is sunburned, windburned, dry, chapped, or irritated. Also avoid using this medication in wounds or on areas of eczema. Wait until these conditions have fully healed before using tazarotene topical.

Avoid as much as possible other topical products with a strong drying effect, products with high concentrations of alcohol, astringents, spices, peel of lime, medicated soaps or shampoos, permanent wave solutions, electrolysis, chemical hair removers or waxes, or other products that might dry or irritate the skin unless instructed otherwise by your doctor.

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What should I discuss with my healthcare provider before using Tazorac (tazarotene topical)?
Do not use tazarotene topical without first talking to your doctor if you
are especially sensitive to sunlight;
spend a considerable amount of time in the sun;
have eczema, sunburn, or another skin condition;
are taking vitamin A;
lentigo maligna (a type of skin cancer);
are using other prescription or over-the-counter medicines on your skin; or
are taking any other prescription or over-the-counter medicines, including vitamins and herbal supplements.

You may not be able to use tazarotene topical, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.

Do not use tazarotene topical if you are pregnant or if you could become pregnant. Tazarotene topical is in the FDA pregnancy category X. This means that tazarotene topical is known to cause birth defects in an unborn baby. You must take a pregnancy test and have negative results within two weeks before starting treatment with tazarotene topical and treatment should be started during a menstrual period. Brith control must be used during treatment. If you become pregnant, stop using birth control, or miss your menstrual period, immediately stop using tazarotene topical and notify your doctor. It is not known whether tazarotene topical passes into breast milk. Do not use tazarotene topical without first talking to your doctor if you are breast-feeding a baby.

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How should I use Tazorac (tazarotene topical)?
Use tazarotene topical exactly as directed by your doctor. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you.

Wash your hands before and after applying this medication (unless affected areas are on the hands).

Tazarotene topical is usually applied once daily at bedtime. Follow your doctor's instructions.

Cleanse the skin with a gentle cleanser and allow it to dry completely (20 to 30 minutes). If a bath or shower is taken prior to application of tazarotene topical, the skin should be dry before applying the gel or cream. Apply a thin film of tazarotene topical to the affected skin. Avoid applying the medication to unaffected areas. If medication accidentally gets on areas that do not need treatment, wash it off.

If a cream or lotion is used to soften or lubricate the skin, it can be applied either before or after application of tazarotene topical. Allow the first cream or lotion applied to be absorbed into the skin and dry completely before application of the second product.

Do not apply tazarotene topical to the eyes, ears, nostrils, mouth, angles of the nose, mucous membranes, open sores, or irritated skin. If you get medication in any of these areas, rinse it off with water. Do not use tazarotene topical on skin that is sunburned, windburned, dry, chapped, or irritated. Also avoid using this medication in wounds or on areas of eczema. Wait until these conditions have fully healed before using tazarotene topical. Do not cover treated areas with dressings or bandages. Do not apply tazarotene topical more often than is directed. Using too much of this medication may cause marked skin redness, peeling, or discomfort and will not lead to more rapid or better results.

Application of this medication may cause a passing feeling of burning or stinging. If irritation is excessive, stop using tazarotene topical and contact your doctor.

Your skin may be more sensitive to weather extremes such as cold and wind during treatment with tazarotene topical. Protect your skin with clothing and use a moisturizing cream or lotion as needed.

Apply a sunscreen, SPF 15 or greater, to the skin daily.

Do not use tazarotene topical beyond the date printed on the bottom seal of the tube. Store tazarotene topical at room temperature away from moisture and heat.

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What happens if I miss a dose?
If you forget or miss a dose, do not try to make it up. Return to your normal application schedule as soon as you can. Do not apply a double dose of tazarotene topical.

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What happens if I overdose?
An overdose of this medication is unlikely to occur. If you do suspect an overdose, or if tazarotene topical has been ingested, call an emergency room or poison control center for advice.

Symptoms of excessive topical use of tazarotene topical include marked redness, peeling or discomfort.

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What should I avoid while using Tazorac (tazarotene topical)?
Avoid exposure to sunlight or artificial UV rays (e.g., sunlamps). Use a sunscreen (minimum SPF 15) and wear protective clothing during the day when being treated with tazarotene topical.
Your skin may be more sensitive to weather extremes such as cold and wind during treatment with tazarotene topical. Protect your skin with clothing and use a moisturizing cream or lotion as needed.

Do not use tazarotene topical on skin that is sunburned, windburned, dry, chapped, or irritated. Also avoid using this medication in wounds or on areas of eczema. Wait until these conditions have fully healed before using tazarotene topical.

Avoid as much as possible other topical products with a strong drying effect, products with high concentrations of alcohol, astringents, spices, peel of lime, medicated soaps or shampoos, permanent wave solutions, electrolysis, chemical hair removers or waxes, or other products that might dry or irritate the skin unless instructed otherwise by your doctor.

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Tazorac (tazarotene topical) side effects
Serious side effects are not likely to occur. Stop using tazarotene topical and seek emergency medical attention if you experience an allergic reaction (shortness of breath; closing of the throat; swelling of the lips, face, or tongue; or hives).

You may experience some skin burning, warmth, stinging, tingling, itching, redness, swelling, dryness, peeling, or irritation while using tazarotene topical. If these side effects are excessive, talk to your doctor. You may need a lower dose or less frequent applications of tazarotene topical.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.

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What other drugs will affect Tazorac (tazarotene topical)?
Do not use tazarotene topical without first talking to your doctor if you are taking any of the following medicines:
a thiazide diuretic such as hydrochlorothiazide (HCTZ, HydroDiuril, Esidrix, Microzide, Oretic), chlorothiazide (Diuril), chlorthalidone (Hygroton, Thalitone), indapamide (Lozol), metolazone (Mykrox, Zaroxolyn), and others;
a tetracycline antibiotic such as tetracycline (Sumycin, Panmycin, Robitet, others), minocycline (Dynacin, Minocin, Vectrin), doxycycline (Doryx, Monodox, Vibramycin, Vibra-Tabs), demeclocycline (Declomycin), and others;
a fluoroquinolone antibiotic such as lomefloxacin (Maxaquin), sparfloxacin (Zagam), ciprofloxacin (Cipro), ofloxacin (Floxin), and others;
a sulfonamide antibiotic such as sulfamethoxazole (Gantanol), sulfisoxazole (Gantrisin), sulfamethoxazole-trimethoprim (Bactrim, Septra, Cotrim), and others; or
a phenothiazine such as chlorpromazine (Thorazine), prochlorperazine (Compazine), fluphenazine (Permitil, Prolixin), promethazine (Phenergan, Promethegan), perphenazine (Trilafon), and others.

The medications listed above may increase the sensitivity of the skin to UV rays from sunlight or artificial light (e.g., sunlamps). Generally, tazarotene topical should not be used during treatment with any of the medicines listed above.

Avoid as much as possible other topical products with a strong drying effect, products with high concentrations of alcohol, astringents, spices, peel of lime, medicated soaps or shampoos, permanent wave solutions, electrolysis, chemical hair removers or waxes, or other products that might dry or irritate the skin unless instructed otherwise by your doctor.

Drugs other than those listed here may also interact with tazarotene topical. Talk to your doctor and pharmacist before taking or using any prescription or over-the-counter medicines, including vitamins and herbal products.

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Where can I get more information?
Your pharmacist has additional information about tazarotene topical written for health professionals that you may read.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.