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| | Goodman & Gilman’s: The Pharmacological Basis of Therapeutics, 14th Edition | | Goodman & Gilman’s: The Pharmacological Basis of Therapeutics, 14th Edition |
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| − | == Ch61 Antifungal Agents ==
| + | [[Ch61 Antifungal Agents]] 抗真菌剂 |
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| − | 抗真菌剂 | + | |
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| − | Systemic Antifungal Agents: Drugs for Deeply Invasive Fungal Infections (全身性抗真菌药物：治疗深侵袭性真菌感染的药物)
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| − | * '''Amphotericin B''' (两性霉素 B)
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| − | * '''Flucytosine''' (氟胞嘧啶)
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| − | * '''Imidazoles and Triazoles''' (咪唑类和三唑类)
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| − | ** Ketoconazole (酮康唑)
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| − | ** Itraconazole (伊曲康唑)
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| − | ** Fluconazole (氟康唑)
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| − | ** Voriconazole (伏立康唑)
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| − | ** Posaconazole (泊沙康唑)
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| − | ** Isavuconazole (艾沙康唑)
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| − | * '''Echinocandins''' (棘白菌素)
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| − | ** Caspofungin (卡泊芬净)
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| − | ** Micafungin (米卡芬净)
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| − | ** Anidulafungin (阿尼杜拉芬净)
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| − | * '''Other Systemic Antifungal Agents''' (其他全身性抗真菌药)
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| − | ** Griseofulvin (灰黄霉素)
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| − | ** Terbinafine (特比萘芬)
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| − | * '''Agents Active Against Microsporidia and Pneumocystis''' (对小孢子虫和肺孢子虫有活性的药物)
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| − | ** Albendazole (阿苯达唑)
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| − | ** Fumagillin (烟曲霉素)
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| − | ** Pentamidine (喷他脒)
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| − | <br>
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| − | === 特比萘芬 (Terbinafine) ===
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| − | Terbinafine is a synthetic allylamine, structurally similar to the topical agent naftifine (see discussion that follows). It inhibits fungal squalene epoxidase and thereby reduces ergosterol biosynthesis.
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| − | 特比萘芬是一种合成烯丙胺，在结构上类似于外用剂萘替芬（见下面的讨论）。它抑制真菌角鲨烯环氧化酶，从而减少麦角甾醇的生物合成。
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| − | '''ADME''': Terbinafine is well absorbed, but bioavailability is about 40% due to first-pass metabolism in the liver. The drug accumulates in skin, nails, and fat. The initial t1/2 is about 12 h but extends to 200 to 400 h at steady state. Terbinafine is not recommended in patients with marked azotemia or hepatic failure. Rifampin decreases and cimetidine increases plasma terbinafine concentrations.
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| − | '''ADME'''：特比萘芬吸收良好，但由于肝脏中的首过代谢，生物利用度约为 40%。该药物在皮肤、指甲和脂肪中积累。初始 t1/2 约为 12 小时，但在稳态下延长至 200 至 400 小时。不推荐将特比萘芬用于明显氮质血症或肝功能衰竭的患者。利福平降低血浆特比萘芬浓度，西咪替丁增加血浆特比萘芬浓度。
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| − | '''Therapeutic Uses''': Terbinafine, given as one 250-mg tablet daily for adults, is somewhat more effective than itraconazole for nail onychomycosis. Duration of treatment varies with the site of infection but typically ranges between 6 and 12 weeks. The efficacy for the treatment of onychomycosis can be improved by the simultaneous use of amorolfine 5% nail lacquer (amorolfine is not approved for use in the U.S.). Terbinafine is also effective for the treatment of tinea capitis and has been used for the off-label treatment of ringworm elsewhere on the body.
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| − | '''治疗用途'''： 特比萘芬，成人每天一片 250 毫克片剂，比伊曲康唑对指甲甲真菌病更有效。治疗持续时间因感染部位而异，但通常在 6 至 12 周之间。同时使用 5% 阿莫罗芬指甲油可以提高治疗甲癣的疗效（阿莫罗芬在美国未获批使用）。特比萘芬对治疗头癣也有效，并已用于身体其他部位的癣的超说明书治疗。
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| − | '''Adverse Effects''': The drug is well tolerated, with a low incidence of GI distress, headache, or rash. Very rarely, fatal hepatotoxicity, severe neutropenia, Stevens-Johnson syndrome, or toxic epidermal necrolysis may occur. Systemic terbinafine therapy for onychomycosis should be postponed until after pregnancy is complete.
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| − | '''不良反应'''：该药物耐受性良好，胃肠道不适、头痛或皮疹的发生率较低。极少数情况下，可能会发生致命的肝毒性、严重的中性粒细胞减少、Stevens-Johnson 综合征或中毒性表皮坏死松解症。甲癣的全身性特比萘芬治疗应推迟到妊娠完成后。
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| − | <br>
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| − | Topical Antifungal Agents (外用抗真菌药)
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| − | * '''Topical Imidazoles and Triazoles''' (外用咪唑类和三唑类)
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| − | ** Clotrimazole (克霉唑)
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| − | ** Econazole (益康唑)
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| − | ** Efinaconazole (艾氟康唑)
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| − | ** Miconazole (咪康唑)
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| − | ** Luliconazole (卢立康唑)
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| − | ** Terconazole and Butoconazole (特康唑和布托康唑)
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| − | ** Tioconazole (噻康唑)
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| − | ** Oxiconazole, Sulconazole, and Sertaconazole (奥昔康唑、磺康唑和舍他康唑)
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| − | ** Ketoconazole (酮康唑)
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| − | * '''Structurally Diverse Antifungal Agents''' (结构多样的抗真菌剂)
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| − | ** Ciclopirox Olamine (环吡酮乙醇胺)
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| − | ** Haloprogin （盐丙蛋白）
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| − | ** Tolnaftate (托萘酯)
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| − | ** Naftifine (萘替芬)
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| − | ** Terbinafine (特比萘芬)
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| − | ** Butenafine (布特萘芬)
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| − | ** Tavaborole (他伐硼罗)
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| − | ** Nystatin (制霉菌素)
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| − | ** Undecylenic Acid (十一烯酸)
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| − | ** Benzoic and Salicylic Acids (苯甲酸和水杨酸)
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