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Ch75 Dermatological Pharmacology
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== Miscellaneous Agents == === Capsaicin (辣椒素) === Capsaicin is an alkaloid derived from plants of the Solanaceae family (i.e., hot chili peppers). Capsaicin interacts with the transient receptor potential vanilloid type 1 (TRPV1) receptor on C-fiber sensory neurons. TRPV1 is a ligand-gated nonselective cation channel of the TRP family, modulated by a variety of noxious stimuli. Chronic exposure to capsaicin first stimulates and then desensitizes this channel to capsaicin and diverse other noxious stimuli. Capsaicin also causes local depletion of substance P, an endogenous neuropeptide involved in sensory perception and pain transmission. Capsaicin (cream, lotion, gel, roll-on, and transdermal patch) is FDA-approved for the temporary relief of minor aches and pains associated with backache, strains, and arthritis. It is also approved in patch form by prescription for postherpetic neuralgia and is used for off-label treatment of painful diabetic neuropathy and some forms of pruritus. <b style=color:#f80>辣椒碱 (Capsaicin) </b>是一种来源于茄科植物(即辣椒)的生物碱。辣椒碱可与 C 纤维感觉神经元上的 TRPV1 受体相互作用。TRPV1 (Transient Receptor Potential Vanilloid, 瞬时受体电位香草素) 是 TRP 家族的配体门控非选择性阳离子通道,受各种有害刺激的调节。缓慢接触辣椒碱最初会刺激该通道,但很快该通道会对辣椒碱和其他各种有害刺激脱敏。辣椒碱还会导致 P 物质的局部耗竭,P 物质是一种参与感觉知觉和疼痛传递的内源性神经肽。辣椒碱(乳膏、化妆水、凝胶、滚珠和透皮贴剂)已获得 FDA 批准,用于<b style=color:#0b0>暂时缓解</b>与<b style=color:#f80>背痛</b>、<b style=color:#f80>拉伤</b>和<b style=color:#f80>关节炎</b>相关的轻微疼痛。它还被批准为<b style=color:#f80>贴剂</b>形式用于治疗<b style=color:#f80>带状疱疹后神经痛</b>,并用于<b style=color:#0b0>疼痛性</b><b style=color:#f80>糖尿病神经病变</b>和某些形式的瘙痒症的超适应症治疗。 <b style=color:#0cf>【注】</b>辣椒素可与辣椒碱互换使用。化学名:(反)-N-[(4-羟基-3-甲氧基苯基)-甲基]-8-甲基-6-壬烯基酰胺。分子式:C18H27NO3,极微溶于水 (30'C 60min 0.01mg/ml),部分溶于乙醇 (25'C 60min 0.14mg/ml),溶解度均随温度升高而增大,溶解度顺序: 正丁醇 > 石油醚 > 乙酸丁酯、甲醇、乙醇、乙醚 > 乙酸乙酯 > 正己烷 > 水 辣椒碱在醇类溶剂、醚类溶剂和脂类溶剂中的溶解度均随溶剂碳链长度增加而增大,原因是随溶剂碳链长度增加,溶剂的极性逐渐降低,与弱极性辣椒碱的极性更加接近,根据相似相溶原理,辣椒碱的溶解度相应增加 。 药用乳膏辣椒碱含量为 10g:2.5mg,约 0.025%, 万分之2.5。其主要作用于 C 型感觉神经元(负责传导皮肤痛觉和瘙痒)的轴突,<b style=color:#0b0>耗竭 P 物质</b>(一种参与感觉知觉和疼痛传递的神经递质),<b style=color:#0b0>阻断痛觉传回中枢</b>。黄豆粒大小药效约 4 小时左右,药效过,痛觉会恢复,需再次涂抹黄豆粒大小。。。 [[文件:Capsaicin.jpg]] <br> === Bentoquatam (季铵盐) === 季铵盐(双(氢化牛脂烷基)二甲基季铵膨润土盐)是季铵盐-18(由牛脂脂肪酸制成的季铵盐)和膨润土的混合物。这种有机粘土混合物被批准用于 OTC 作局部屏蔽药,以防止对毒藤、橡树或漆树的<b style=color:#f80>漆酚树脂过敏</b>性接触性皮炎。如有暴露于漆酚的潜在风险可提前 15 分钟以上用 5% 的外用乳液涂抹,并每 4 小时重抹一次。 Bentoquatam (quaternium-18 bentonite) is a mixture of quaternium-18 (quaternary ammonium chloride salts made from the fatty acids of tallow) and bentonite clay. This organoclay mixture is approved for OTC use as a topical barrier to prevent allergic contact dermatitis to the urushiol resin of poison ivy, oak, or sumac. The 5% topical lotion must be applied prophylactically at least 15 min prior to potential risk for exposure to urushiol and reapplied every 4 h. <br> === Coal tar (煤焦油) === 煤焦油是煤的蒸馏产物,是 10,000 多种化合物的混合物。它在皮肤病学中主要用于治疗<b style=color:#f80>炎症性皮肤病</b>,例如<b style=color:#0b0>牛皮癣、脂溢性皮炎和特应性皮炎</b>或其他形式的<b>湿疹性皮炎</b>。<b style=color:#e00>作用机制尚不清楚</b>,尽管已知它会抑制 DNA 合成。煤焦油具有抗炎、抗菌和止痒活性。此外,它在 UVA 和 330 至 550 nm 波长之间的可见光谱中具有光敏作用。多种配方和产品可在市场上或通过复合获得,包括含有粗煤焦油、煤焦油提取物或煤焦油溶液的配方和产品(Sandhu 和 Schwartz,2011 年)。煤焦油溶液,也称为 Liquor carbonis detergens,是煤焦油的醇提取物,用聚山梨酯 80 乳化,以产生更美观的产品。煤焦油可与 UVB 光疗(例如 Goeckerman 方案)、局部水杨酸或局部皮质类固醇联合使用。煤焦油产品通常因其难闻的气味、凌乱和可能弄脏衣服而被患者耐受。它还可引起毛囊炎或刺激性接触性皮炎。尽管煤焦油的职业暴露与恶性肿瘤(例如阴囊癌)有关,但接受局部煤焦油产品治疗的银屑病或特应性皮炎患者患癌症的风险并未增加(Menter 等人,2009a)。 Coal tar is a distillation product from coal, a mixture of over 10,000 compounds. It is used in dermatology primarily for the treatment of inflammatory skin conditions such as psoriasis, seborrheic dermatitis, and atopic dermatitis or other forms of eczematous dermatitis. The mechanism of action is unknown, although it is known to suppress DNA synthesis. Coal tar has anti-inflammatory, antimicrobial, and antipruritic activity. In addition, it has a photosensitizing effect within the UVA and visible light spectrum between wavelengths of 330 and 550 nm. Multiple formulations and products are available commercially or through compounding, including those containing crude coal tar, coal tar extracts, or coal tar solution (Sandhu and Schwartz, 2011). Coal tar solution, also known as liquor carbonis detergens, is an alcohol extract of coal tar emulsified with polysorbate 80 to yield a more cosmetically acceptable product. Coal tar may be used in combination with UVB phototherapy (e.g., Goeckerman regimen), topical salicylic acid, or topical corticosteroids. Coal tar products are often poorly tolerated by patients due to its unpleasant odor, messiness, and potential for staining of clothing. It can also cause folliculitis or irritant contact dermatitis. Although occupational exposures to coal tar have been associated with malignancies (e.g., scrotal cancer), patients with psoriasis or atopic dermatitis who are treated with topical coal tar products have not exhibited increased risk of cancer (Menter et al., 2009a). <br> === Anthralin (蒽林) === 蒽林(地蒽醇)是绿菊素的合成版本,来源于巴西阿拉罗巴树的树皮,用于治疗<b style=color:#0b0>牛皮癣和斑秃</b>;<b style=color:#e00>其作用机制尚不清楚</b>(Menter et al., 2009a)。蒽林的使用受到限制,因为它可能引起刺激性接触性皮炎,并可能弄脏皮肤、头发、指甲、织物和家居用品。 Anthralin (dithranol), a synthetic version of chrysarobin, is derived from the bark of the Brazilian araroba tree and is used in the treatment of psoriasis and alopecia areata; its mechanisms of action are unclear (Menter et al., 2009a). Use of anthralin has been limited by the potential to cause irritant contact dermatitis and to stain skin, hair, nails, fabrics, and household items. <br> === Brimonidine (溴莫尼定) === <b style=color:#f80>溴莫尼定 (0.33% 外用凝胶)</b> 是一种 α2 肾上腺素能激动剂,被批准用于每日一次治疗<b style=color:#0b0>酒渣鼻持续性红斑</b>。它会导致暂时性血管收缩,并且有<b style=color:#e00>反跳性红斑</b>的报道。 <b style=color:#f80>羟甲唑啉(1% 乳膏)</b> 是一种 α1 肾上腺素能激动剂,被批准用于成人<b style=color:#0b0>持续性酒渣鼻面部红斑</b>的每日一次治疗。亦可致暂时性血管收缩;患者<b style=color:#e00>反弹性红斑发生率不到 1% </b>。 Brimonidine (0.33% topical gel) is an α2 adrenergic agonist approved for once-daily treatment of persistent erythema of rosacea. It causes temporary vasoconstriction, and rebound erythema has been reported. Oxymetazoline (1% cream) is an α1 adrenergic agonist approved for once-daily treatment of persistent facial erythema of rosacea in adults. It also causes temporary vasoconstriction; rebound erythema occurs in less than 1% of patients. <br>
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