설파살라진

항균제 / 항염증제 / 면역억제제 (설파제/살리실산염)

설파살라진은 아조 결합을 통해 설파제 항생제(**설파피리딘**)와 살리실산염 항염증제(**메살라민** 또는 **5-ASA**)를 결합한 독특한 국소 작용 전구약물입니다. - **주요 용도**: 개와 고양이의 **특발성 염증성 장질환(IBD)**, 특히 **형질세포-림프구성 결장염**(대장성 설사) 치료의 핵심 약물입니다. 개의 혈관염 보조 치료제로도 사용됩니다. - **제한점**: 활성화를 위해 결장 세균이 필요하므로 소장 질환에는 효과가 없습니다. - **임상 요점**: 결장염에 매우 효과적이지만, 개에서 **건성 각결막염(KCS)** 또는 "안구건조증"을 유발할 위험이 있어 수의학적 사용 시 주의 깊은 모니터링이 필요합니다. 조기에 발견하지 못하면 비가역적일 수 있습니다. 고양이는 살리실산염에 본질적으로 민감하므로 투여 시 각별한 주의가 필요합니다.

작용 기전: 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).

동물 종별 용량

Cats

Inflammatory large bowel disease · 10-20 mg/kg PO once daily. · PO · q24h · Unspecified · Use cautiously in cats because of their sensitivity to salicylates.
Inflammatory large bowel disease · 10-20 mg/kg PO q24 hours (once daily) tapered to the lowest effective dose · PO · q24h · Unspecified
Inflammatory large bowel disease · 10-20 mg/kg PO q8-12h (maximum of 10 days) · PO · q8-12h · Maximum 10 days
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
All uses (Management of colitis) · 10-20 mg/kg · PO · q8-12h

Ferrets

General · 10-20 mg/kg PO 2-3 times a day · PO · q8-12h · Unspecified
General · 25 mg (total dose) PO twice daily · PO · q12h · Unspecified

Dogs

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
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 · May consider an initial dose of 12.5 mg/kg, q8h. After signs resolve, reduce dosage by 25% at 2 week intervals.

투여 경로

금기

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

이상반응

Keratoconjunctivitis sicca (KCS) in dogs
Anorexia
Vomiting
Cholestatic jaundice
Hemolytic anemia
Leukopenia
Decreased sperm counts
Allergic dermatitis
Keratoconjunctivitis sicca (KCS)

약물 상호작용

Chlorpropamide · Hypoglycemic effects could be potentiated
Digoxin · Sulfasalazine may reduce absorption of digoxin · moderate
Ferrous sulfate (or other iron salts) · May decrease the blood levels of sulfasalazine if administered concurrently
Folic acid · Oral absorption of folic acid may be inhibited
Warfarin · Potentially sulfasalazine could potentiate warfarin
Folate · Measurement of serum folate concentration may be affected · minor
Thyroxine · May cause a reduction in serum thyroxine concentrations · minor

모니터링

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)

과용량

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.

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