サラゾスルファピリジン / スルファサラジン
Sulfasalazine
Salicylazosulfapyridine
別名: Azulfidine EN-tabs · salazosulfapyridine · salicylazosulfapyridine · sulfasalazinum · sulphasalazine · Aculfin · Azulfin · Colo-Pleon · Pleon RA · Pyralin · SAS · Salazopirina · Salazoprin · Salazopyrina · Salazopyrine · Salisulf Gastroprotetto · Salopyrine · Saridine · Sazo · Sulazine · Ulco
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Inflammatory large bowel disease | 20-40 mg/kg PO q8h for 3 weeks, followed by 20-40 mg/kg q12h for 3 weeks, and 10-20 mg/kg q12h for 3 weeks. | PO | q8h then q12h | 9 weeks | 🌎 NA |
| Inflammatory large bowel disease | 20-48.4 mg/kg (maximum total dose of one gram in refractory patients) PO q8h. | PO | q8h | Minimum 4 weeks | 🌎 NA |
| Chronic colitis | 20-50 mg/kg (up to a maximum of 1 gram) three times daily. | PO | q8h | Variable | 🌎 NA |
| Inflammatory large bowel disease | 10-25 mg/kg PO three times a day for 4-6 weeks. | PO | q8h | 4-6 weeks | 🌎 NA |
| Adjunctive treatment of vasculitis | 20-40 mg/kg PO q8h | PO | q8h | Unspecified | 🌎 NA |
| Adjunctive treatment of vasculitis | 25 mg/kg PO three times a day. | PO | q8h | Unspecified | 🌎 NA |
| All uses (Management of colitis) | 15-30 mg/kg | PO | q8-12h | — | 🌍 EU |
- Inflammatory large bowel disease: May consider an initial dose of 12.5 mg/kg, q8h. After signs resolve, reduce dosage by 25% at 2 week intervals.
- Chronic colitis: Initial dosage usually 20-30 mg/kg TID. Reduce dose at 2-4 week intervals if stool remains normal.
- Inflammatory large bowel disease: With resolution of clinical signs, reduce dose by 25 percent at 2 week intervals.
- All uses (Management of colitis): maximum 6 g/day
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Inflammatory large bowel disease | 10-20 mg/kg PO once daily. | PO | q24h | Unspecified | 🌎 NA |
| Inflammatory large bowel disease | 10-20 mg/kg PO q24 hours (once daily) tapered to the lowest effective dose | PO | q24h | Unspecified | 🌎 NA |
| Inflammatory large bowel disease | 10-20 mg/kg PO q8-12h (maximum of 10 days) | PO | q8-12h | Maximum 10 days | 🌎 NA |
| Inflammatory large bowel disease | 10-20 mg/kg PO q8-24h; up to a maximum of 10 days treatment | PO | q8-24h | Maximum 10 days | 🌎 NA |
| All uses (Management of colitis) | 10-20 mg/kg | PO | q8-12h | — | 🌍 EU |
- Inflammatory large bowel disease: Use cautiously in cats because of their sensitivity to salicylates.
フェレット
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| General | 10-20 mg/kg PO 2-3 times a day | PO | q8-12h | Unspecified | 🌎 NA |
| General | 25 mg (total dose) PO twice daily | PO | q12h | Unspecified | 🌎 NA |
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
スルファサラジンは、サルファ系抗菌薬（スルファピリジン）とサリチル酸系抗炎症薬（メサラジンまたは5-ASA）がアゾ結合したユニークな局所作用型プロドラッグです。
- 主な用途: 犬および猫の特発性炎症性腸疾患 (IBD)、特に形質細胞・リンパ球性大腸炎（大腸性下痢）の基本的な治療薬です。犬の血管炎の補助治療としても使用されます。
- 制限事項: 活性化に結腸の細菌を必要とするため、小腸の疾患には効果がありません。
- 臨床上のポイント: 大腸炎には非常に有効ですが、犬では乾性角結膜炎 (KCS)（ドライアイ）のリスクがあるため、獣医療での使用には慎重なモニタリングが必要です。早期に発見されない場合、不可逆的な損傷につながる可能性があります。猫はサリチル酸塩に対して本来敏感であるため、慎重な投与が必要です。
作用機序
Sulfasalazine acts as a targeted delivery vehicle to transport anti-inflammatory medication directly to the colon.
- Delivery: The intact drug passes mostly unabsorbed (only 10-33% absorbed) through the stomach and small intestine.
- Activation: In the colon, bacterial azoreductase enzymes cleave the diazo bond.
- Mechanism:
- 5-Aminosalicylic Acid (5-ASA / Mesalamine) → Acts locally on the colonic mucosa to inhibit cyclooxygenase (COX) and lipoxygenase (LOX) pathways → Decreases production of pro-inflammatory prostaglandins and leukotrienes. It also acts as a local free radical scavenger.
- Sulfapyridine → Provides local antibacterial effects, though it is rapidly absorbed systemically and is responsible for the majority of the drug's adverse effects (e.g., KCS, hepatotoxicity).
安全性・警告
禁忌
- Hypersensitivity to sulfasalazine, sulfonamides, or salicylates
- Intestinal or urinary obstructions
- Doberman pinschers (highly susceptible to sulfonamide-induced polysystemic immune complex disease)
- Dobermanns (appear to be highly sensitive to adverse effects associated with sulfapyridine)
- Patients with known hypersensitivity to sulfonamides or salicylates
有害事象
- Keratoconjunctivitis sicca (KCS) in dogs
- Anorexia
- Vomiting
- Cholestatic jaundice
- Hemolytic anemia
- Leukopenia
- Decreased sperm counts
- Allergic dermatitis
注意事項
Use with caution in animals with preexisting liver, renal, or hematologic diseases.
Feline Warning: Because cats have a deficient glucuronidation pathway, they are highly sensitive to salicylates. Use extreme caution and strict dosing when using this drug in cats.
Use with caution in nursing patients, as sulfonamides are excreted in milk and may cause kernicterus in newborns.
医薬品相互作用
Hypoglycemic effects could be potentiated
Sulfasalazine may reduce absorption of digoxin
May decrease the blood levels of sulfasalazine if administered concurrently
Oral absorption of folic acid may be inhibited
Potentially sulfasalazine could potentiate warfarin
Measurement of serum folate concentration may be affected
May cause a reduction in serum thyroxine concentrations
監視
- Clinical efficacy (resolution of diarrhea/colitis signs)
- Schirmer tear tests (STT) prior to therapy and on rechecks (especially in middle-aged to older dogs) to monitor for KCS
- Complete Blood Count (CBC) occasionally with chronic therapy
- Liver function tests occasionally with chronic therapy
- Schirmer tear test (STT) periodically
- Clinical signs of KCS (ocular discharge, blepharospasm)
- Liver enzymes (due to risk of cholestatic jaundice)
- Thyroid panel (if on long-term therapy)
薬物動態
吸収
Only about 10-33% of an orally administered dose is absorbed. The unabsorbed drug is cleaved in the colon. The sulfapyridine component is rapidly absorbed from the colon, but only a small percentage of the 5-ASA is absorbed.
分布
Sulfonamides are excreted in milk and can cross the placenta.
代謝
Unabsorbed and biliary excreted drug is cleaved into 5-ASA and sulfapyridine in the colon by bacterial flora. Absorbed sulfapyridine and 5-ASA are hepatically metabolized.
消失
Renally excreted. Some of the initially absorbed intact drug is excreted unchanged in the bile.
過剰投与
Massive overdoses could cause significant salicylate and/or sulfonamide toxicity.
- Treatment: Standard protocols for decontamination (empty stomach, cathartics, etc.) should be considered.
- Supportive Care: Urine alkalinization and forced diuresis may be beneficial in selected cases to enhance elimination.
製品
製剤
- Delayed-Release Tablets (enteric coated)
- 500 mg tablet
- 250 mg/5 ml oral suspension
ヒト用医薬品
- Sulfasalazine Tablets: 500 mg (Azulfidine, generic)
- Sulfasalazine Delayed-Release Tablets: 500 mg (enteric coated) (Azulfidine EN-tabs, generic)
- Salazopyrin 500 mg tablet
- Salazopyrin 250 mg/5 ml oral suspension
規制ステータス
Used under the cascade. POM (Prescription Only Medicine).
Used under the prescribing cascade. POM-V.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Tablets (plain or enteric-coated) should be stored at temperatures less than 40°C, preferably at room temperature (15-30°C) in well-closed containers. Oral suspension should be stored at room temperature; avoid freezing.
飼主向け情報
重要な警告: この薬は犬に「ドライアイ」（乾性角結膜炎）を引き起こす可能性があり、放置すると永久的な失明につながる恐れがあります。
- ペットの目を注意深く観察してください。目を細める、充血、ドロドロした黄色や緑色の目やに、または目が濁って乾燥しているように見える場合は、すぐに獣医師に連絡してください。
- 投与方法: 胃の不快感を軽減するため、食事と一緒に与えてください。腸溶錠を使用している場合は、砕いたり割ったりしないでください。
- 猫に関する注意: 猫はこの薬に対して非常に敏感です。獣医師の正確な投与指示に従い、処方された期間を超えて使用しないでください。
- 副作用: 食欲不振、嘔吐、または歯茎や目の黄色化（黄疸）に注意してください。
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