药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(2018112800124414.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分中文阿利维A酸凝胶剂处方资料(仅供参考)
分类名称
一级分类:抗肿瘤药物 二级分类:其他抗肿瘤药物 三级分类:
药品英文名: Alitretinoin
药品别名: Panretin、Panrexin
药物剂型: 局部凝胶剂:1%。
药理作用
本品可结合并激活细胞内的视黄酸受体(RAR)(如RARα,RARβ,RARγ)和视黄醛X受体(RXR)(如RXRα,RXRβ,RXRγ),从而增强基因转录。本品治疗与卡波济肉瘤有关损害的实际作用机制尚未完全阐明;不过,本品似乎可以影响基因表达,从而抑制细胞增殖,诱导细胞分化,激发健康细胞和癌细胞的凋亡。体外证实,本品可抑制卡波济肉瘤细胞生长。
药动学
局部应用本品后,未从血浆中检出本品及其代谢物的明显浓度。体外证实本品通过P450CYP2C9,3A4,1A1和1A2代谢。
适应证
局部治疗与卡波济肉瘤有关的皮肤损害。
禁忌证
对本品过敏者、哺乳者禁用。
注意事项
1.有过敏性皮炎史者慎用。
2.18以下岁儿童的安全性和有效性尚未确定。
3.本品凝胶不可接触眼、鼻孔、口唇、阴道、阴茎头、直肠和肛门。
不良反应
1.常见皮疹、瘙痒、剥脱性皮炎、皮肤病(表皮脱落、表皮裂开、结痂、排出液体、焦痂和渗出)。
2.有胚胎毒并致畸。
3.有光敏反应(包括日光或人工日光灯管)。
4.可能发生严重的局部皮肤反应(如严重的红斑、水肿和起疱)。
用法用量
1.局部使用本品0.1%凝胶的患者在应用之前沐浴或淋浴之后,须等候20min。局部用药后应使之干燥3~5min后才能穿衣。用药后至少3h内不能沐浴或淋浴
仅在局部病损区使用充分的凝胶,每天2次。根据耐受情况,用药次数可逐渐增加到3~4次。如用药范围已产生毒性,直至刺激感消除后才可恢复用药。3.患者感到用药有益处,就可持续给药。有些患者在超过14周治疗后才见到效应。在临床研究中有用到175周的。
药物相应作用
1.动物试验证实,本品与二乙甲苯酰胺(diethyl-toluamide)合用,可增加后者的毒性。
2.在接受抗病毒药(包括蛋白酶抑制剂在内的抗逆转病毒药)、大环内酯类抗生素或唑类抗真菌药的患者中使用本品凝胶剂,并未发现相互作用。
专家点评
本品主要用于与卡波济肉瘤有关的皮肤损害,且能长期局部使用,使用疗效尚未确定,如患者感到使用有好处,且能耐受,可持续使用,有临床报道使用本品175周仍未见明显局部刺激反应。
Category name
Class I: Antitumor Drugs Secondary Category: Other Antitumor Drugs Category 3:
English name of the drug: Alitretinoin
Drug Alias: Panretin, Panrexin
Pharmaceutical dosage form: Topical gel: 1%.
Pharmacological action
This product binds and activates intracellular retinoic acid receptors (RAR) (such as RARα, RARβ, RARγ) and retinal X receptors (RXR) (such as RXRα, RXRβ, RXRγ) to enhance gene transcription. The actual mechanism of action of this product in the treatment of damage associated with Kaposi's sarcoma has not been fully elucidated; however, this product seems to affect gene expression, thereby inhibiting cell proliferation, inducing cell differentiation, and inducing apoptosis in healthy cells and cancer cells. It was confirmed in vitro that this product can inhibit the growth of Kaposi's sarcoma cells.
Pharmacokinetics
After topical application of this product, the apparent concentration of this product and its metabolites was not detected from plasma. This product was confirmed to be metabolized by P450CYP2C9, 3A4, 1A1 and 1A2 in vitro.
Indications
Topical treatment of skin damage associated with Kaposi's sarcoma.
Contraindications
It is forbidden to those who are allergic to this product and breastfeeding.
Notes
1. Have a history of allergic dermatitis with caution.
The safety and efficacy of children under the age of 2.18 have not been determined.
3. This product gel should not touch the eyes, nostrils, lips, vagina, penile head, rectum and anus.
Adverse reactions
1. Common rash, itching, exfoliative dermatitis, skin disease (epidermal exfoliation, epidermal fissure, crusting, discharge of fluid, eschar and exudation).
2. Embryo poisoning and teratogenicity.
3. Photosensitive reactions (including daylight or artificial fluorescent tubes).
4. Severe local skin reactions (such as severe erythema, edema, and blistering) may occur.
Usage and Usage
1. Patients who use 0.1% gel on topical products should wait 20 minutes after bathing or showering before application. After topical application, it should be dried for 3 to 5 minutes before being put on. Do not bathe or shower for at least 3 hours after taking the medicine
Use sufficient gel only in the localized lesion area twice a day. According to the tolerance, the number of medications can be gradually increased to 3 to 4 times. If the scope of the medication has been toxic, the medication can be resumed until the irritation is removed. 3. The patient feels that the medication is beneficial and can be administered continuously. Some patients see the effect after more than 14 weeks of treatment. It is useful for 175 weeks in clinical research.
The corresponding effect of drugs
1. Animal tests have confirmed that this product can be combined with diethyl-toluamide to increase the toxicity of the latter.
2. In the patients who received antiviral drugs (antiretroviral drugs including protease inhibitors), macrolide antibiotics or azole antifungals, the gel was not found in each other. effect.
Expert Review
This product is mainly used for skin damage related to Kaposi's sarcoma, and can be used locally for a long time. The efficacy of the drug has not been determined. If the patient feels that it is beneficial to use, it can be tolerated and can be used continuously. No significant local irritation was observed for 175 weeks.
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(2018112800124414.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- |