甲氧苄啶/磺胺嘧啶 與 甲氧苄啶/磺胺甲噁唑
Sulfadiazine/Trimethoprim and Sulfamethoxazole/Trimethoprim
Trimethoprim/Sulfadiazine, Trimethoprim/Sulfamethoxazole
別名: Co-trimoxazole · Tribrissen · Bactrim · Septra · Tucoprim · Uniprim · Di-Biotic · Cotrim · Sulfatrim · Trivetrin · Borgal · SMX-TMP · trimethoprim-sulfamethoxazole · sulfadiazine-trimethoprim · TMP-SDZ · Co-trimazine
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
經審核的 v13 劑量證據
結構化劑量計算證據Coccidiosis
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必須同時考慮的臨床上下文 (3)
- NOTE: There is significant controversy regarding the frequency of administration of these drugs. See Pharmacokinetics for more information. Unless otherwise noted, doses are for combined sulfa-/trimethoprim. See Monitoring if treatment is expected to be longer than 7 days.
- Bacterial cystitis (extra-label): Potentiated sulfonamides (ie, sulfa-/ trimethoprim, sulfadimethoxine/ormetoprim) are first-tier drugs only if regional pathogen susceptibility patterns are known. 32
- Unless otherwise instructed by the manufacturer, sulfa-/trimethoprim products should be stored at room temperature of 20°C to 25°C (68°F-77°F) in tight containers and protected from freezing. Shake suspensions well before use.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
增效磺胺類藥物（常被稱為 TMS、SMZ-TMP 或 co-trimoxazole）是獸醫學中廣泛使用的廣效、殺菌性抗菌複合藥物。
關鍵臨床要點：
- 優異的組織穿透力： 具高脂溶性，能達到難以穿透的組織（如前列腺、血腦屏障 (CNS) 和眼睛）的治療濃度。
- 廣效性： 對許多革蘭氏陽性與陰性菌有效，包含許多抗甲氧苯青黴素葡萄球菌 (MRSA/MRSP) 菌株、諾卡氏菌，以及某些原蟲（弓形蟲、球蟲、肺囊蟲）。
- 受膿液去活化： 藥效會被化膿性碎屑和壞死組織（富含 PABA 和胸苷）顯著抑制。必須引流膿瘍才能發揮藥效。
- 品種敏感性： 杜賓犬對磺胺類藥物誘發的多系統免疫複合體疾病（過敏反應）具有已知的品種特異性易感性。
- 劑型： 雖然有獸醫核准的甲氧苄啶/磺胺嘧啶產品，但許多獸醫師也會以仿單標示外使用 (off-label use) 的方式，使用人類核准的甲氧苄啶/磺胺甲噁唑 (Bactrim®, Septra®)，且療效相似。
作用機制
Potentiated sulfas exhibit synergistic, bactericidal activity by sequentially blocking the bacterial folic acid synthesis pathway. Mammalian cells are largely unaffected because they utilize preformed dietary folate rather than synthesizing it.
- Sulfonamides (Bacteriostatic alone): Act as structural analogues of para-aminobenzoic acid (PABA). They competitively inhibit the bacterial enzyme dihydropteroate synthase → blocks the conversion of PABA to dihydrofolic acid (DFA).
- Trimethoprim (Bactericidal alone): Reversibly inhibits the bacterial enzyme dihydrofolate reductase → blocks the conversion of DFA to tetrahydrofolic acid (THFA).
- Synergy: The sequential blockade completely depletes THFA, an essential cofactor for bacterial DNA and RNA synthesis, leading to rapid bacterial cell death.
Pharmacologic Note: The optimal in vitro ratio for most susceptible bacteria is 1:20 (trimethoprim:sulfa), but synergistic activity occurs across a wide range (1:1 to 1:40). The serum concentration of the trimethoprim component is generally considered the primary driver of efficacy.
安全性與警告
禁忌症
- Hypersensitivity to sulfonamides, thiazides, or sulfonylurea agents
- Severe renal or hepatic impairment
- Doberman pinschers (highly susceptible to immune complex disease)
- Marked blood dyscrasias
- Animals intended for food (in the USA/certain jurisdictions)
不良反應
- Dogs: Keratoconjunctivitis sicca (KCS/dry eye - potentially irreversible)
- Dogs: Hypersensitivity reactions (Type 1 anaphylaxis or Type 3 serum sickness, polyarthritis, urticaria, facial swelling)
- Dogs: Acute neutrophilic hepatitis with icterus, idiosyncratic hepatic necrosis
- Dogs: Vomiting, anorexia, diarrhea
- Dogs: Hemolytic anemia, agranulocytosis
- Dogs: Hypothyroidism (with extended therapy)
- Dogs: Crystalluria, hematuria, polyuria, polydipsia
- Cats: Anorexia, crystalluria, hematuria, leukopenias, anemias
- Horses: Transient pruritus (after IV injection), diarrhea, hypersensitivity, hematologic effects
- Injection site reactions: Swelling, pain, tissue damage (IM, SC, or extravasation)
注意事項
Use with caution in patients with pre-existing hepatic or renal disease. Because of its potential for crystallization in the urine, avoid use in dogs known to have uroliths, at increased risk for developing uroliths, or those with highly concentrated (dehydrated) or acidic urine. Potentially teratogenic (cleft palate reported); weigh risk vs. benefit in pregnant animals. Use with caution in nursing animals as sulfonamides are excreted in milk and may cause kernicterus in neonates.
藥物相互作用
May cause toxic delirium (reported in humans)
May decrease the bioavailability of sulfonamides if administered concurrently
May increase the risk of nephrotoxicity
May increase digoxin levels
May increase risk for thrombocytopenia
May potentiate hypoglycemic effects
May displace from plasma proteins and increase risk for toxic effects; can also interfere with MTX assays
May increase half-life of phenytoin
May decrease efficacy of the antidepressant
May prolong INR/PT and increase bleeding risk
監測
- Clinical efficacy
- Adverse effects (GI, hypersensitivity)
- Complete blood counts (CBC) periodically with chronic therapy
- Schirmer Tear Test (STT) in dogs to monitor tear production (e.g., at 5 days, then every 2-3 weeks)
- Thyroid function tests (baseline and ongoing) for dogs on long-term treatment
藥物動力學
半衰期
吸收
Well absorbed after oral administration, with peak levels occurring about 1-4 hours after dosing. More slowly absorbed after subcutaneous administration. In ruminants >8 weeks old, trimethoprim is trapped in the ruminoreticulum after oral administration and undergoes degradation.
分佈
Well distributed in the body. Enters CSF at about 50% of serum levels when meninges are inflamed. Crosses the placenta and distributes into milk. Relatively well distributed into the prostate. Volume of distribution for trimethoprim: 1.49 L/kg (dogs), 0.59-1.51 L/kg (horses). Vd for sulfadiazine in dogs is 1.02 L/kg.
代謝
Metabolized by the liver. Sulfas are primarily acetylated and conjugated with glucuronic acid. Trimethoprim is metabolized to oxide and hydroxylated metabolites. Trimethoprim may be more extensively metabolized in the liver in adult ruminants.
排除
Renally excreted unchanged via glomerular filtration and tubular secretion, as well as hepatic metabolism. Trimethoprim is rapidly eliminated from serum but may persist longer in tissues.
過量
Manifestations of acute overdosage include GI distress (nausea, vomiting, diarrhea), CNS toxicity (depression, headache, confusion), facial swelling, bone marrow depression, and elevated serum aminotransferases.
Treatment:
- Oral Overdose: Empty the stomach following usual protocols and initiate symptomatic/supportive therapy.
- Fluid Therapy: Maintain hydration. Acidification of urine may increase renal elimination of trimethoprim but increases the risk of sulfonamide crystalluria (especially with sulfadiazine).
- Monitoring: Monitor complete blood counts and liver parameters.
- Bone Marrow Suppression: If severe and associated with chronic overdose, may be treated with folinic acid (leucovorin).
- Note: Peritoneal dialysis is not effective in removing TMP or sulfas from circulation.
可用產品
劑型
- Oral Paste
- Sterile Injection
- Oral Powder
- Oral Tablets
- Oral Suspension
獸醫用
- Trimethoprim/Sulfadiazine Oral Paste: 67 mg TMP / 333 mg SDZ per gram (Tribrissen 400 Oral Paste)
- Trimethoprim/Sulfadiazine Sterile Injection: 48% (Di-Biotic 48%, Tribrissen 48% Injection)
- Trimethoprim/Sulfadiazine Powder: 67 mg TMP / 333 mg SDZ per gram (Tucoprim, Uniprim)
- Trimethoprim/Sulfadoxine (Canada): Trivetrin, Borgal
人用標示
- Trimethoprim Tablets: 100 mg, 200 mg (Proloprim, Trimpex)
- Trimethoprim/Sulfamethoxazole (TMP-SMZ) Tablets: 80 mg TMP / 400 mg SMX (Bactrim, Septra)
- Trimethoprim/Sulfamethoxazole Double Strength (DS) Tablets: 160 mg TMP / 800 mg SMX (Bactrim DS, Septra DS)
- Trimethoprim/Sulfamethoxazole Oral Suspension: 8 mg TMP / 40 mg SMX per mL (Septra, Cotrim Pediatric, Sulfatrim)
- Trimethoprim/Sulfamethoxazole Injection: 16 mg TMP / 80 mg SMX per mL
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Unless otherwise instructed by the manufacturer, trimethoprim/sulfadiazine and co-trimoxazole products should be stored at room temperature (15-30°C) in tight containers.
飼主須知
寵物主人重要指引：
- 保持水分充足： 在服藥期間，請確保您的寵物隨時有充足的新鮮飲水。脫水可能導致藥物在腎臟或尿液中形成結晶。
- 注意眼睛狀況（犬隻）： 此藥物可能會減少淚液分泌，導致「乾眼症」（乾燥性角結膜炎）。如果您發現狗狗瞇眼、揉眼睛、眼睛發紅或出現濃稠的黃綠色眼屎，請立即聯繫您的獸醫師。
- 過敏反應： 杜賓犬和某些大型犬較容易發生過敏反應。如果您發現寵物臉部腫脹、起疹子、不明原因發燒、關節僵硬/跛行，或眼睛/牙齦發黃，請立即停藥並聯繫獸醫師。
- 給藥方式： 可與食物一起或空腹餵食。如果使用口服懸浮液，在抽取每次劑量前請充分搖勻。藥水不需要冷藏。
- 完成療程： 即使您的寵物看起來已經完全康復，也請務必按照獸醫師的指示完成整個處方療程，以預防抗藥性細菌的產生。
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