药品名称
【通用名】他扎罗汀乳膏/凝胶
【成份】本品主要成份是他扎罗汀
化学名称: 6-[（3，4-二氢-4，4-二甲基-2H-1-苯并噻喃-6-基）乙炔基]-3-吡啶羧酸乙酯
分子式：C21H21NO2S
分子量：351.46
【性状】本品为乳剂型基质的白色乳膏。

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 0.1% GEL 100g/piece
【原产地英文药品名】TAZAROTENE
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·TAZORAC 0.05%凝胶 100克/支
·TAZORAC 0.05%凝胶 30克/支
·TAZORAC 0.1%凝胶 30克/支
·TAZORAC 0.1%凝胶 100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(TAZAROTENE)

Tazorac Information

Tazarotene is the generic name for Tazorac, a product that can be purchased under two main forms: Cream or Gel. This topical medication is a retinoid prodrug that contains benzyl alcohol (as a main preservative), sodium thiosulfate, purified water, sorbitan monooleate, carbomer 1342, carbomer 934P, edetate disodium, sodium hydroxide, mineral oil, and so on.

Tazorac Indications

In most cases, Tazorac is prescribed to patients who are suffering from acne vulgaris, as it is an effective remedy for mild or moderate facial acne. Studies have shown that the use of this product can also provide numerous beneficial results for patients who are suffering from psoriasis. In case you are interested in starting a therapy course with Tazorac, you should discuss with your PD the benefits and risks that are associated with this treatment.

Tazorac Warnings

The use of the Tazorac gel or cream is highly contraindicated in the case of pregnant females or in that of women who are planning to become pregnant any time soon, as such a therapy is a potential hazard to the development of the baby. Moreover, your personal physician will probably insist upon your employing an effective birth control method during your treatment with this drug (in the case of female individuals). All patients who are considering using this medical remedy should make sure that they are not allergic to any of the components of Tazorac. You can learn all about this product’s ingredients from your local pharmacist.

Tazorac Intake Guidelines

This type of medication has been approved and designed for external use. However, one must not apply Tazorac on irritated or eczematous skin areas, as this can lead to the worsening of such conditions (severe skin dryness and irritation). You must avoid applying this product on wet skin (if you have washed your hands or taken a shower, make sure that you thoroughly dry the needed skin area before applying Tazorac). If your physician has instructed you to also employ certain emollients during your therapy with this drug, make sure that you apply them at least 60 minutes before using Tazorac.

Tazorac Dosage

In the early stages of one’s therapy course with Tazorac, he or she will probably be advised to use the 0.05% Cream or Gel. If this form of therapy is well tolerated, the physician may later on prescribe the patient a more powerful form of medication (the 0.1% Cream or Gel). The product must be applied on the needed skin area(s) once per day, if possible, in the evening. You must use a sufficient amount of Tazorac as to cover the affected skin with a thin film of medication. If you are not satisfied with the results of your treatment with this medication, you should discuss with your PD the possibility of increasing your daily dose of medication, of using a more powerful form of Tazorac or of starting to use a different topical remedy. You must not change your medication or your dosing routine without your doctor’s consent.

Tazorac Overdose

Applying excessive amounts of Tazorac (Gel or Cream) can lead to the developing of several symptoms, especially peeling, skin redness or discomfort. This condition is not a life-threatening one, but you should alert your PD and discuss with him or her the clinical implications of Tazorac over-dosage. Oral ingestion of this medication is considered a medical emergency. If you have accidentally swallowed a certain amount of your medication, you should go to the nearest medical center, where you will be kept under close monitoring and you will receive all needed supportive medical assistance.

Tazorac Missed Dose

Missed doses of Tazorac can and will diminish the effectiveness of your therapy course. This is why we strongly recommend you to discuss this aspect with your PD and determine the best way in which you can correct such undesirable situations. Do not deviate from your physician’s instructions.

Tazorac Side Effects

Of all the patients who are being treated with Tazorac, 10 to 30% of them experienced some adverse manifestations. Here is a list of the most common side effects associated with the use of the Tazarotene Cream: desquamation, burning sensation, erythema, skin dryness, etc. While using Tazorac Gel, several patients accused the development of pruritus, erythema, stinging and burning. In case you experience these or other unusual symptoms during your therapy with this topical remedy, you should alert your PD. He or she will make any needed adjustments to your current dosing routine. Such symptoms normally fade away in time, as your organism adjusts to the ingredients of this drug. If they are unusually bothersome, you may have to discontinue using Tazorac.

Tazorac Drug Reactions

One’s therapy with Tazorac should be closely monitored by a health care professional if the patient is also following a treatment course with any photo-sensitizers, as the use of Tazarotene will probably enhance the adverse reactions of such remedies. The most common classes of drugs that fit into this pharmaceutical category are: sulfonamides, phenothiazines, tetracyclines, thiazides, and fluoroquinolones. If such a therapeutic combination of drugs cannot be avoided, it is imperative that the patient takes into consideration the needed precautions. Your PD will tell you more about the importance of using effective sunscreens (creams or gels with SPF at least 15) and of wearing protective clothing. Furthermore, one should not apply any products that have a strong drying effect on the skin area that is being treated with this prodrug.