替硝唑
Tinidazole
1-[2-(ethylsulfonyl)ethyl]-2-methyl-5-nitroimidazole
別名: Tindamax · Estovyn-T · Fasigyn · Tiniba · Tiniameb · CP-12574 · tinidazolum
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
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Stomatitis, anaerobic infections | 15-25 mg/kg PO q12h | PO | q12h | 7 days | 🌎 NA |
| Giardiasis | 44 mg/kg PO q24h | PO | q24h | 6 days | 🌎 NA |
- Giardiasis: Potentially useful for trichomoniasis, amebiasis, and balantidiasis.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Stomatitis, anaerobic infections | 15 mg/kg PO q24h | PO | q24h | 7 days | 🌎 NA |
| Tritrichomonas foetus (experimental) | 30 mg/kg PO once daily | PO | q24h | 14 days | 🌎 NA |
- Tritrichomonas foetus (experimental): Decreased fecal shedding but failed to eradicate infection in 2 of 4 cats.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible anaerobic infections | 10-15 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
替硝唑 (Tinidazole) 是一種第二代 5-硝基咪唑類 (5-nitroimidazole) 抗菌與抗原蟲藥物，其結構與藥理作用與甲硝唑 (metronidazole) 相似。
主要臨床重點包括：
- 半衰期較長：與甲硝唑相比，替硝唑的作用時間更長，因此給藥頻率較低（例如貓可每日一次，而甲硝唑需每日兩次）。
- 抗厭氧菌效力：對絕對厭氧菌具有極佳的抗菌活性，特別是犬牙齦中常見的Porphyromonas spp.，使其在嚴重的牙科與口腔感染中非常有用。
- 抗原蟲活性：可作為治療梨形鞭毛蟲 (Giardia)、溶組織內阿米巴 (Entamoeba histolytica)、滴蟲 (Trichomonas) 及小袋纖毛蟲 (Balantidium) 感染的替代療法。
- 胎兒三毛滴蟲 (Tritrichomonas foetus)：雖然羅硝唑 (ronidazole) 通常是治療貓 T. foetus 的首選藥物，但替硝唑也曾被研究作為替代方案，儘管在某些情況下它可能僅能抑制排蟲而無法完全根除。
臨床提示：由於該藥物具有極度苦味，強烈建議將其配製成膠囊或添加重口味調味劑的懸浮液，特別是對於容易因苦味而過度流涎或拒藥的貓咪患者。
作用機轉
Tinidazole is a prodrug that requires activation within susceptible organisms.
- Uptake: The drug diffuses into the target anaerobic bacteria or protozoa.
- Reduction: Inside the cell, the nitro group of tinidazole is reduced by electron-transport proteins (such as ferredoxin or nitroreductase enzymes) specific to anaerobic metabolism.
- DNA Disruption: This reduction → generates highly reactive, unidentified polar nitro radical anions → these radicals bind to and disrupt DNA and nucleic acid synthesis → leading to strand breakage and rapid cell death.
This mechanism makes it rapidly bactericidal, trichomonacidal, and amebicidal.
安全性與警告
禁忌症
- Hypersensitivity to tinidazole or other 5-nitroimidazoles (e.g., metronidazole, ronidazole)
- Food-producing animals (prohibited use)
不良反應
- Vomiting
- Inappetence
- Diarrhea
- Neurotoxicity (ataxia, nystagmus, seizures)
- Hypersalivation (due to bitter taste)
注意事項
Use with caution in patients with hepatic dysfunction, as the drug is metabolized by the liver.
Use with extreme caution in animals susceptible to seizures or with pre-existing neurological disease, as 5-nitroimidazoles can cross the blood-brain barrier and cause neurotoxicity.
Black Box Warning (Human Label): Carcinogenicity has been seen in mice and rats treated chronically with metronidazole. Avoid unnecessary use and reserve for indicated conditions.
Reproductive/Nursing: Decreased fertility noted in male rats. Crosses the placenta (mutagenic potential; avoid in first trimester; FDA Category C). Distributed into maternal milk; use milk replacer if treating a nursing dam.
藥物交互作用
May induce a disulfiram-like reaction (nausea, vomiting, cramps).
May decrease the metabolism of tinidazole and increase the likelihood of dose-related side effects.
May decrease the metabolism of tinidazole and increase the likelihood of dose-related side effects.
Tinidazole may increase the serum levels of cyclosporine.
Tinidazole may increase the serum levels of tacrolimus.
Tinidazole may increase the serum levels of fluorouracil and increase the risk of toxicity.
Tinidazole may increase lithium serum levels and increase the risk for lithium toxicity.
May antagonize the therapeutic effects of metronidazole (and presumably tinidazole).
May increase the metabolism of tinidazole thereby decreasing blood levels.
May increase the metabolism of tinidazole thereby decreasing blood levels.
May increase the metabolism of tinidazole thereby decreasing blood levels.
May prolong the prothrombin time (PT). Avoid concurrent use if possible; otherwise, intensify monitoring.
監測
- Clinical efficacy in treating the infection
- Gastrointestinal tolerance
- Neurological signs (ataxia, nystagmus, seizures)
藥物動力學
半衰期
吸收
Practically completely absorbed after oral administration in dogs, cats, and horses.
分佈
Apparent volume of distribution (Vd) is 0.66 L/kg in dogs and horses, and 0.54 L/kg in cats.
代謝
Metabolized by the liver.
排除
Dogs clear the drug about twice as fast as cats.
過量
Very limited information is available. In rodent studies, the oral LD50 was >3.6 g/kg (mice) and >2 g/kg (rats).
Treatment of acute overdoses is symptomatic and supportive.
- Decontamination: Gastric lavage or induction of emesis may be helpful if performed shortly after ingestion and the patient is neurologically appropriate.
- Clearance: Hemodialysis can remove approximately 43% of the drug in the body (based on human data) in a 6-hour session.
可用產品
劑型
- Tablets (scored)
人用標示
- Tinidazole Tablets (scored): 250 mg & 500 mg (Tindamax®, generic)
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
Store tinidazole tablets at controlled room temperature (20-25°C) protected from light.
飼主須知
- 給藥方式：請將此藥物與食物一起餵食，以減少腸胃不適。
- 味道警告：此藥物非常苦。除非獸醫師指示，否則請勿壓碎或剝半藥片，因為苦味可能會導致您的寵物過度流口水或拒絕進食。
- 避免酒精：在服用此藥物期間，請確保您的寵物不會接觸到任何含有酒精的產品。
- 何時聯繫獸醫：如果腸胃道症狀（嘔吐、食慾不振、腹瀉）嚴重或持續存在，請聯繫您的獸醫師。
- 緊急症狀：如果您的寵物出現行為改變、眼球快速來回轉動（眼球震顫）、抽搐/癲癇，或行走/爬樓梯困難（共濟失調），請立即聯繫獸醫師。這些可能是藥物中毒的跡象。
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