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利福平

Rifampin

Rifampicin (semi-synthetic zwitterion derivative of rifamycin B)

抗菌藥物 (利福黴素類)POIV

別名: Rifadin · Rimactane · Ba-41166/E · L-5103 · NSC-113926 · rifaldazine · rifampicinum · rifamycin AMP · Rifampin

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

WHO 極重要抗生素請謹慎使用,避免不必要的處方
10-20 mg/kg PO q8-12hPO· q8-12h
🐕

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。

各物種劑量

🌎 NA — North America🌍 EU — Europe

適應症劑量途徑頻次療程地區
Combination therapy of atypical Mycobacteria infections; treatment of resistant Staph endocarditis10-20 mg/kg PO q8-12hPOq8-12h🌎 NA
Alternate treatment for scarred pyogranulomatous pyoderma5-10 mg/kg PO q24hPOq24h4-8 weeks🌎 NA
Actinomycosis10-20 mg/kg PO q12hPOq12h🌎 NA
Susceptible infections (e.g., mycobacteriosis, resistant staphylococcal pyoderma, ehrlichiosis)10-15 mg/kgPOq24hDuration depends on the specific infection being treated🌍 EU
  • Combination therapy of atypical Mycobacteria infections; treatment of resistant Staph endocarditis: In combination with amoxicillin/clavulanate or trimethoprim/sulfa
  • Alternate treatment for scarred pyogranulomatous pyoderma: Must be used with another antibiotic to reduce risk for resistance development (e.g., cephalexin or a potentiated sulfonamide). Monitor CBC, liver screens, and UA every 2 to 3 weeks.
  • Susceptible infections (e.g., mycobacteriosis, resistant staphylococcal pyoderma, ehrlichiosis): Must be used in combination with other antimicrobial drugs to prevent the emergence of resistant organisms.

適應症劑量途徑頻次療程地區
Susceptible infections (e.g., mycobacteriosis, Rhodococcus equi, chlamydiosis, bartonellosis)10-15 mg/kgPOq24hDuration depends on the specific infection being treated🌍 EU
  • Susceptible infections (e.g., mycobacteriosis, Rhodococcus equi, chlamydiosis, bartonellosis): Must be used in combination with other antimicrobial drugs to prevent the emergence of resistant organisms.

適應症劑量途徑頻次療程地區
Treatment of mycobacteriosis45 mg/kg PO once dailyPOq24h🌎 NA
  • Treatment of mycobacteriosis: In combination with ethambutol (30 mg/kg PO once daily) and one of the following: clofazimine (6 mg/kg PO once daily) or isoniazid (30 mg/kg PO once daily).

適應症劑量途徑頻次療程地區
Treatment of Rhodococcus equi (C. equi) infections in foals5 mg/kg PO two times dailyPOq12h🌎 NA
Treatment of Rhodococcus equi (C. equi) infections in foals5 mg/kg PO two times daily or 10 mg/kg PO once dailyPOq12h or q24h4-9 weeks🌎 NA
Treatment of proliferative enteropathy caused by Lawsonia intracellularis in foals10 mg/kg PO once dailyPOq24hminimum of 21 days🌎 NA
  • Treatment of Rhodococcus equi (C. equi) infections in foals: With erythromycin 15-25 mg/kg, PO q12-24h. Clarithromycin may be superior due to erythromycin side effects.
  • Treatment of Rhodococcus equi (C. equi) infections in foals: With erythromycin 25 mg/kg, PO q6-8h.
  • Treatment of proliferative enteropathy caused by Lawsonia intracellularis in foals: In combination with erythromycin estolate (25 mg/kg PO q6-8h)

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概覽

利福平是一種高脂溶性、半合成的抗菌藥物,屬於利福黴素類。在獸醫學中,它是治療深層細胞內感染的基石療法,特別是馬駒的​馬紅球菌 (Rhodococcus equi)​ 感染。

由於其具有穿透乾酪樣物質、骨骼、膿瘍和巨噬細胞的卓越能力,對抗細胞內病原體(如分枝桿菌、金黃色葡萄球菌和胞內勞森菌)非常有效。在高濃度下,它也具有一定的抗真菌和抗病毒活性。

​臨床要點:​ 利福平​絕對不能​作為單一療法使用。細菌可透過單一步驟突變迅速產生抗藥性。它總是與其他抗菌藥物(例如馬用的紅黴素或克拉黴素,或狗用的頭孢菌素/磺胺類藥物)合併開立。

作用機制

Rifampin can be bactericidal or bacteriostatic depending on the concentration and the susceptibility of the target organism.

  • ​Target:​ It binds strongly to the beta subunit of bacterial DNA-dependent RNA polymerase.
  • ​Pathway:​ Binding inhibits the enzyme → suppresses the initiation of chain formation for RNA synthesis → halts bacterial protein production → cell death.
  • ​Selectivity:​ Rifampin is highly selective for bacterial enzymes and does not inhibit mammalian RNA polymerase, providing a wide margin of safety for the host.

安全性與警告

禁忌症

  • Hypersensitivity to rifampin or other rifamycins
  • Use with extreme caution in patients with preexisting hepatic dysfunction
  • Pregnancy (teratogenic at high doses)
  • Pre-existing liver disease or hepatic dysfunction

不良反應

  • Red-orange discoloration of bodily fluids (urine, tears, sweat, saliva)
  • Gastrointestinal distress (anorexia, vomiting, diarrhea)
  • Elevated liver enzymes and potential hepatotoxicity
  • Rashes and erythema (noted in cats and humans)
  • In horses (especially with macrolides): mild diarrhea to severe enterocolitis, hyperthermia, and acute respiratory distress
  • Intravenous use in horses (rare): CNS depression, sweating, hemolysis, anorexia
  • Elevated serum hepatic enzymes
  • Clinical hepatitis
  • Orange-red discoloration of urine, saliva, tears, and feces
  • Gastrointestinal upset (anorexia, vomiting, diarrhea)

注意事項

Use with caution in patients with preexisting hepatic dysfunction; dosage reduction may be necessary. Never use as a monotherapy due to the rapid development of bacterial resistance. Rifampin is a potent inducer of hepatic microsomal enzymes, which can significantly alter the metabolism of concurrently administered drugs. It is excreted in maternal milk; use with caution in nursing veterinary patients. May cause false-positive BSP (bromosulfophthalein) test results and interfere with microbiologic assays of serum folate and vitamin B12.

藥物相互作用

Fluoroquinolones

In vitro antagonism has been reported; concurrent use should be avoided.

BarbituratesMajor

Decreased serum levels and shortened half-life due to hepatic microsomal enzyme induction by rifampin.

Benzodiazepines (e.g., diazepam)

Decreased serum levels and shortened half-life due to hepatic enzyme induction.

Chloramphenicol

Decreased serum levels and shortened half-life due to hepatic enzyme induction.

Corticosteroids

Decreased serum levels and shortened half-life due to hepatic enzyme induction.

Dapsone

Decreased serum levels and shortened half-life due to hepatic enzyme induction.

Ketoconazole

Decreased serum levels and shortened half-life due to hepatic enzyme induction.

Propranolol

Decreased serum levels and shortened half-life due to hepatic enzyme induction.

Quinidine

Decreased serum levels and shortened half-life due to hepatic enzyme induction.

Warfarin

Decreased serum levels and shortened half-life due to hepatic enzyme induction.

TheophyllineMajor

Increased rate of metabolism of theophylline due to hepatic enzyme induction.

ItraconazoleMajor

Increased rate of metabolism of itraconazole due to hepatic enzyme induction, leading to subtherapeutic antifungal levels.

監測

  • Clinical efficacy and resolution of infection
  • Liver function tests (especially with long-term therapy)
  • Chest radiographs and plasma fibrinogen levels (prognostic indicators for C. equi infections in foals after 1 week of therapy)
  • Baseline and periodic serum hepatic enzyme levels (ALT, AST, ALP, Bilirubin)
  • Clinical signs of hepatitis (icterus, anorexia, vomiting, lethargy)

藥物動力學

半衰期

Unknown8 hours6-8 hours

吸收

Relatively well absorbed from the GI tract. Oral bioavailability is about 40-70% in horses and 37% in adult sheep. Concurrent food administration may delay and slightly reduce peak plasma levels.

分佈

Very lipophilic. Readily penetrates most body tissues (including bone and prostate), cells, and fluids (including CSF). Uniquely penetrates abscesses and caseous material. 70-90% bound to serum proteins. Distributes into milk and crosses the placenta. Volume of distribution is ~0.9 L/kg in horses and 1.3 L/kg in sheep.

代謝

Metabolized in the liver to a deacetylated form that retains antibacterial activity. Rifampin induces hepatic microsomal enzymes, meaning elimination rates may increase over time with repeated dosing (auto-induction).

排除

Both the active metabolite and unchanged drug are excreted primarily in the bile, but up to 30% may be excreted in the urine. The parent drug undergoes substantial enterohepatic recirculation, but the metabolite does not.

過量

Clinical signs of oral rifampin overdose are generally extensions of its adverse effects, including gastrointestinal distress, orange-red coloring of fluids, and skin erythema (noted particularly in cats).

Massive overdoses carry a significant risk of hepatotoxicity. Dogs may exhibit central nervous system depression.

​Treatment:​

  • Empty the gut following standard decontamination protocols for massive oral overdosage.
  • Monitor liver enzymes closely.
  • Initiate supportive treatment as necessary.

可用產品

劑型

  • Oral capsules
  • Lyophilized powder for injection
  • 150 mg capsule
  • 300 mg capsule
  • 20 mg/ml syrup

人用標示

  • Rifampin Oral Capsules: 150 mg & 300 mg (Rifadin®, Rimactane®, generic)
  • Rifampin Lyophilized Powder for Injection Solution: 600 mg (Rifadin®, generic)
  • Rifadin 150 mg capsules
  • Rifadin 300 mg capsules
  • Rifadin 20 mg/ml syrup
  • Rimactane capsules

各地核准狀態

European Union✗ 未核准處方藥EMA

Human authorized products used under the prescribing cascade. Rifamycins are critically important antimicrobials.

United Kingdom✗ 未核准處方藥VMD

POM (Prescription Only Medicine). Used under the cascade.

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Rifampin capsules should be stored in tight, light-resistant containers, preferably at room temperature (15-30°C).

飼主須知

  • ​無害的變色:​ 此藥物可能會使您寵物的尿液、眼淚、汗水和唾液變成紅橘色。這是完全正常且無害的,但請注意它可能會永久染到布料、地毯或淺色毛髮上。
  • ​給藥方式:​ 為了獲得最佳吸收效果,請在空腹時給予此藥物。如果引起腸胃不適,可以與少量零食一起餵食。
  • ​合併治療:​ 利福平幾乎總是與另一種抗生素一起開立。務必完全按照指示給予兩種藥物並完成整個療程。切勿提早停藥,因為細菌會很快對利福平產生抗藥性。
  • ​注意事項:​ 如果您發現寵物有嚴重腹瀉、食慾不振、極度嗜睡或眼睛/牙齦發黃(黃疸),請聯絡您的獸醫師,因為這些可能是肝臟壓力的徵兆。

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