阿达帕林

阿达帕林
臨床資料
商品名（英语：Drug nomenclature）Differin, Teva, Pimpal, Gallet, Adelene, Adeferin
AHFS/Drugs.comMonograph
MedlinePlusa604001
核准狀況
懷孕分級
  • 澳: D
给药途径外用
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度透皮吸收率很低
排泄途徑胆汁
识别信息
  • 6-[3-(1-adamantyl)-4-methoxy-phenyl] naphthalene-2-carboxylic acid
CAS号106685-40-9  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.149.379 編輯維基數據鏈接
化学信息
化学式C28H28O3
摩尔质量412.53 g·mol−1
3D模型（JSmol（英语：JSmol））
  • O=C(O)c2ccc1cc(ccc1c2)c3cc(c(OC)cc3)C46CC5CC(CC(C4)C5)C6
  • InChI=1S/C28H28O3/c1-31-26-7-6-23(21-2-3-22-12-24(27(29)30)5-4-20(22)11-21)13-25(26)28-14-17-8-18(15-28)10-19(9-17)16-28/h2-7,11-13,17-19H,8-10,14-16H2,1H3,(H,29,30) checkY
  • Key:LZCDAPDGXCYOEH-UHFFFAOYSA-N checkY

阿达帕林（Adapalene）是第三代维A酸类外用药物，主要用于治疗轻中度痤疮，也被用来治疗毛囊角化症（非适应症型用药）和其他皮肤症状。[1]

历史

中国大陆销售的阿达帕林凝胶，商品名“达芙文”

阿达帕林1995年由法国高德美公司（英语：Galderma）研制，商品名为Differin（中国大陆译作达芙文，香港译作痘膚零，台灣译作痘膚潤）。

作用机理

阿达帕林通过抑制毛囊上皮细胞的分化与增殖而减少微小粉刺形成，使表皮下的粉刺停止生長。阿达帕林可抑制多核白细胞的化学趋化反应，通过抑制花生四烯酸经脂氧化反应转化为炎症介质来抑制多核白细胞的代谢。阿达帕林同维甲酸一样与特异的维甲酸核受体结合，但不同的是阿达帕林不与和蛋白结合的细胞质受体相结合。

通过抑制角质形成细胞分化与增殖来产生抗痤疮作用。除了去角质作用外，其还具有抗炎作用。

药理学

药物相互作用

阿达帕林表现出可增强克林霉素在局部的作用，但副作用也一样增大。[2]在使用克林霉素前3至5分钟使用阿达帕林凝胶可提高克林霉素的皮肤渗透率。相对单独使用克林霉素而言，合用可增强治疗的整体效果。[3]

与维A酸不同的是，阿达帕林已在同时使用过氧化苯甲酰时表现出更好的化学结构稳定性。[4]

药代动力学

阿达帕林的透皮吸收率很低。一项研究表明6个每日使用一次的患者，连续5天使用10g/1000 cm²，其血浆中药物浓度无法检出或低于0.35 ng/mL。[5]在体内主要分布于肝、脾、肾上腺和卵巢。主要通过氧-脱甲基、羟基化和结合反应代谢。主要通过胆汁排泄。

毒理学

阿达帕林在小鼠和大鼠中口服半数致死量大于10 ml/kg，长期使用会出现与维A酸类似的副作用。口服试验，雌性大鼠卵细胞性腺瘤与甲状腺癌发生率及雄性大鼠肾上腺髓质良性与恶性嗜铬细胞瘤发生率与使用量呈正线性相关。

参考文献

  1. ^ Rolewski S. Clinical review: topical retinoids. Dermatol Nurs. 2003, 15 (5): 447–50, 459–65 [2014-09-17]. PMID 14619325. （原始内容存档于2019-07-27）. 
  2. ^ Wolf JE, Kaplan D, Kraus SJ; et al. Efficacy and tolerability of combined topical treatment of acne vulgaris with adapalene and clindamycin: a multicenter, randomized, investigator-blinded study. J Am Acad Dermatol. 2003, 49 (3 Suppl): S211–7. PMID 12963897. doi:10.1067/S0190-9622(03)01152-6. 
  3. ^ Jain GK, Ahmed FJ. Adapalene pretreatment increases follicular penetration of clindamycin: in vitro and in vivo studies. Indian J Dermatol Venereol Leprol. 2007, 73 (5): 326–9. PMID 17921613. doi:10.4103/0378-6323.34010. 
  4. ^ Martin B, Meunier C, Montels D, Watts O. Chemical stability of adapalene and tretinoin when combined with benzoyl peroxide in presence and in absence of visible light and ultraviolet radiation. Br J Dermatol. October 1998,. 139 Suppl 52: 8–11. PMID 9990414. doi:10.1046/j.1365-2133.1998.1390s2008.x. 
  5. ^ DIFFERIN® (adapalene) Cream, 0.1% Label (PDF). FDA. May 25, 2000 [4 Oct 2011]. （原始内容存档 (PDF)于2017-02-16）. 

Read other articles:

The Suppliants (Aeschylus)

Play by Aeschylus For the play of the same name by Euripides, see The Suppliants (Euripides). The SuppliantsLa Danaide by Auguste RodinWritten byAeschylusChorusThe DanaïdesCharactersDanausPelasgusHerald of AegyptusAttendantsGenreTragedySettingshore of Argos The Suppliants (Ancient Greek: Ἱκέτιδες, Hiketides; Latin: Supplices), also called The Suppliant Maidens, The Suppliant Women, or Supplices [1] is a play by Aeschylus. It was probably first performed only a few years prev...

 

 

Allegorical interpretations of Genesis

Readings of the biblical Book of Genesis that treat elements of the narrative as symbols or types This article possibly contains original research. Please improve it by verifying the claims made and adding inline citations. Statements consisting only of original research should be removed. (February 2010) (Learn how and when to remove this template message) Part of a series onCreationism History Types Young Earth Time dilation creationism Old Earth day-age gap progressive Neo-creationism Bibl...

 

 

2023 New Jersey Senate election

State Senate elections of the U.S. state of New Jersey 2023 New Jersey State Senate election ← 2021 November 7, 2023 2027 → All 40 seats in the New Jersey Senate21 seats needed for a majority   Majority party Minority party   Leader Nicholas Scutari Anthony M. Bucco Party Democratic Republican Leader since January 11, 2022 July 1, 2023[1] Leader's seat 22nd (Linden) 25th (Boonton Twp.) Last election 24 seats 16 seats Seats before 25 ...

Nom Wah Tea Parlor

Restaurant in New York, NYNom Wah Tea ParlorRestaurant informationEstablished1920Owner(s)Wilson TangFood typeDim sumStreet address13 Doyers StCityNew YorkStateNYPostal/ZIP Code10013Coordinates40°42′52″N 73°59′53″W / 40.71449°N 73.99819°W / 40.71449; -73.99819Websitehttps://nomwah.com/ Nom Wah Tea Parlor (Chinese: 南華茶室; Cantonese Yale: Nàahm Wàh Chàhsāt; lit. 'South China Tea House'), opened in 1920, is the oldest continuously run...

 

 

Michigan Women's Hall of Fame

Betty Ford, première dame des États-Unis et du Michigan, intronisée au Temple de la renommée des femmes. Le Michigan Women's Hall of Fame (MWHOF) est un temple de la renommée qui rend hommage à des femmes remarquables, des personnalités historiques et contemporaines, qui ont un lien avec l'État américain du Michigan. Le temple de la renommée a été fondé en 1983 par Gladys Beckwith et est parrainé par la Michigan Women's Studies Association[1]. La génèse de l'Association et du ...

 

 

Anthony de Jasay

Hungarian economist, philosopher (1925–2019) Anthony de JasayBorn(1925-10-15)15 October 1925Aba, HungaryDied23 January 2019(2019-01-23) (aged 93)FranceNationalityHungarianEducationNuffield CollegeOccupation(s)Economist PhilosopherWebsitewww.dejasay.org Anthony de Jasay (15 October 1925 – 23 January 2019) was a Hungarian writer, economist, and right-libertarian philosopher.[1] He studied in Székesfehérvár and Budapest, and obtained a degree in agriculture. He then worked as...

Margaret Murray

Margaret MurrayMurray pada tahun 1928LahirMargaret Alice Murray13 Juli 1863Calcutta, Anglo-IndiaMeninggal13 November 1963(1963-11-13) (umur 100)Welwyn, Hertfordshire, InggrisKebangsaanInggrisAlmamaterUniversity College LondonPekerjaanEgiptolog, arkeolog, antropolog, folklorisTempat kerjaUniversity College London (1898–1935)Orang tuaJames Murray, Margaret Murray Margaret Alice Murray (13 Juli 1863 - 13 November 1963) adalah seorang egiptolog (pakar kebudayaan mesir) berkebangsaan Anglo...

 

 

List of Batman comics

Printed depictions of the DC superhero Batman #1 (spring 1940), art by Bob Kane and Jerry Robinson Batman has been featured in many ongoing series, annuals, miniseries, maxiseries, one-shots, graphic novels, trade paperbacks and intercompany crossovers published by DC Comics. These titles have been handled or coordinated through a single editorial section at DC Comics. This list also generally includes titles that have spun off of the core Batman titles to feature related characters and prese...

 

 

Mantecada

Spongy pastry originating in Spain MantecadasTypeSweet breadPlace of originSpainMain ingredientsFlour, eggs, butter, sugar  Media: Mantecadas Commercial mantecadas, one showing the open cajilla Mantecadas are spongy pastries originating in Spain. Perhaps the best known mantecadas are from Northwestern Spain, being a traditional product of the city of Astorga, province of León, as well as the nearby Maragateria comarca. They taste very much like pound cake. Other Spanish regions also...

Vologases IV

King of Kings of the Parthian Empire from 147 to 191 Vologases IV𐭅𐭋𐭂𐭔King of KingsVologases IV's portrait on the obverse of a tetradrachm, showing him wearing a beard and a tiara on his headKing of the Parthian EmpireReign147–191PredecessorVologases IIISuccessorOsroes II (rival king)Vologases V (successor)Died191IssuePacorusVologases VDynastyArsacid dynastyFatherMithridates VReligionZoroastrianism Vologases IV (Parthian: 𐭅𐭋𐭂𐭔 Walagash) was King of Kings of the Parthi...

 

 

Luiz Carlos de Almeida Peixoto

Questa voce sull'argomento cestisti brasiliani è solo un abbozzo. Contribuisci a migliorarla secondo le convenzioni di Wikipedia. Segui i suggerimenti del progetto di riferimento. Peixotinho Nazionalità  Brasile Pallacanestro CarrieraSquadre di club  BotafogoNazionale 1966-1974 BrasilePalmarès  Campionati sudamericani Argento Argentina 1966 Argento Uruguay 1969 Il simbolo → indica un trasferimento in prestito.   Modifica dati su Wikidata · Manuale Luiz Car...

 

 

دائرة لوطا

هذه المقالة تحتاج للمزيد من الوصلات للمقالات الأخرى للمساعدة في ترابط مقالات الموسوعة. فضلًا ساعد في تحسين هذه المقالة بإضافة وصلات إلى المقالات المتعلقة بها الموجودة في النص الحالي. (نوفمبر 2023) هذه المقالة بحاجة لصندوق معلومات. فضلًا ساعد في تحسين هذه المقالة بإضافة صندو�...

إبراهيم الدنبلي الخوئي

  هذه المقالة عن الشيخ إبراهيم الدنبلي الخوئي. لالأمير إبراهيم الدنبلي، طالع إبراهيم الدنبلي.   لمعانٍ أخرى، طالع الخوئي (توضيح). إبراهيم الدنبلي الخوئي معلومات شخصية الميلاد 1240 هـ[1] أو 1247 هـ.[2][3][4]خوي،  الدولة القاجارية.[1][2][4] الوفا...

 

 

Francisco Macías Nguema

1st President of Equatorial Guinea (1968–79) You can help expand this article with text translated from the corresponding article in Spanish. (July 2018) Click [show] for important translation instructions. Machine translation, like DeepL or Google Translate, is a useful starting point for translations, but translators must revise errors as necessary and confirm that the translation is accurate, rather than simply copy-pasting machine-translated text into the English Wikipedia. Conside...

 

 

العمالة الأجنبية في السعودية

بدأت العمالة الأجنبية في المملكة العربية السعودية والتي يقدر عددها بنحو 9 ملايين شخص اعتباراً من أبريل 2013،[1] بالتوافد إلى البلاد بعد فترة قصيرة من اكتشاف النفط في أواخر الثلاثينيات. كان الوافدون في البداية متألفين من الكوادر الفنية والمهنية والإدارية من العرب والغرب�...

Mohammed Wardi

Sudanese popular musician Mohammed Wardiمحمد عثمان حسن ورديBackground informationBirth nameMohammed Osman Hassan Salih WardiBorn(1932-07-19)19 July 1932[1]OriginSawarda, Wadi Halfa, Sudan[1]Died18 February 2012(2012-02-18) (aged 79)[2]Khartoum[2]GenresMusic of Sudan, Nobiin, Arabic musicOccupation(s)singer-songwriter, teacherInstrument(s)Singing, oud, tanbur, multiple instrumentsYears active1957–2012Musical artist Mohammed Osman Hassan Sa...

 

 

Laplacian matrix

Matrix representation of a graph In the mathematical field of graph theory, the Laplacian matrix, also called the graph Laplacian, admittance matrix, Kirchhoff matrix or discrete Laplacian, is a matrix representation of a graph. Named after Pierre-Simon Laplace, the graph Laplacian matrix can be viewed as a matrix form of the negative discrete Laplace operator on a graph approximating the negative continuous Laplacian obtained by the finite difference method. The Laplacian matrix relates to ...

 

 

جبال طوروس

جبال طوروس   الموقع تركيا  إحداثيات 36°59′47″N 33°00′07″E / 36.9964°N 33.0019°E / 36.9964; 33.0019   الارتفاع 3756 متر  الطول 600 كيلومتر  تعديل مصدري - تعديل   خريطة تضاريس جبال طوروس تبين موقعها في جنوب شرق الأناضول.جبال طوروس هي سلسلة جبلية تقع جنوب شرق منطقة شرق الأنا�...

نهائي كأس العالم 1986

نهائي كأس العالم لكرة القدم 1986الحدثكأس العالم لكرة القدم 1986 الأرجنتين ألمانيا الغربية 3 2 التاريخ29 June 1986الملعبملعب أزتيكا، مكسيكو سيتيرجل المباراةالمعلومات غير متوفرةالحكمروموالدو أربي فيلهو (اتحاد البرازيل لكرة القدم)الحضور114,600الطقسالمعلومات غير متوفرة → 1982 1990 ← أستض...

 

 

Jaken, Pati

JakenKecamatanNegara IndonesiaProvinsiJawa TengahKabupatenPatiPemerintahan • CamatAhmada Mangkunegara, S.STPPopulasi • Total45,209 jiwa (2.006) jiwaKode Kemendagri33.18.06 Kode BPS3318060 Luas58,52 km²Desa/kelurahan21 desa Jaken (bahasa Jawa: ꦗꦏꦼꦤ꧀) adalah sebuah kecamatan di Kabupaten Pati, Jawa Tengah, Indonesia. Kecamatan Jaken terletak di ujung timur dan tenggara dari Kabupaten Pati yang berbatasan langsung dengan wilayah Kabupaten Rembang. Dahu...