ペントサンポリ硫酸ナトリウム
**ペントサンポリ硫酸ナトリウム (PPS)** は、ブナのヘミセルロースから誘導された半合成のヘパリン様高分子炭水化物誘導体です。獣医学においては、主に**変形性関節症疾患修飾薬 (DMOAD)** として、また下部尿路疾患の補助療法として利用されています。 主な臨床応用： * **変形性関節症 (OA)：** 犬、猫、馬において、関節機能の改善、炎症の軽減、軟骨の健康促進に使用されます。 * **特発性猫下部尿路疾患 (FLUTD) / 間質性膀胱炎：** 膀胱尿路上皮の保護的なグリコサミノグリカン (GAG) 層の修復を助けるために適応外使用されますが、短期的な急性増悪に対する臨床的有効性は十分に実証されていません。 *臨床のポイント：* 構造的にはヘパリンに似ていますが、抗凝固作用は著しく弱いです（ヘパリンの約1/15）。しかし、出血性疾患のある患者や手術を受ける患者には依然として注意が必要です。
作用機序: Pentosan polysulfate sodium exhibits multiple pharmacological effects depending on the target tissue: * **Osteoarthritis (Disease-Modifying Effects):** * **Inhibits catabolic enzymes:** Downregulates **matrix metalloproteinases (MMPs)** and **aggrecanases** that degrade articular cartilage. * **Stimulates matrix synthesis:** Promotes the synthesis of **hyaluronic acid** by synovial fibroblasts and preserves proteoglycan content within the cartilage matrix. * **Improves microcirculation:** Its mild anticoagulant, fibrinolytic, and hypolipidemic properties help mobilize thrombi and lipid deposits in subchondral blood vessels, thereby increasing synovial blood flow and nutrition to the joint. * **Interstitial Cystitis / FLUTD:** * **Urothelial Protection:** Excreted partially unchanged in the urine, PPS adheres to the mucosal membranes of the bladder wall. It acts as a synthetic **glycosaminoglycan (GAG) buffer**, preventing irritating urinary solutes and toxins from reaching and damaging the underlying transitional epithelial cells. * **Analgesia:** Provides mild local analgesic and anti-inflammatory effects within the bladder wall.
動物種別の用量
- Persistent or recurrent FLUTD · 2-16 mg/kg PO q12h · PO · q12h · Recent studies have not shown any statistical benefit.
- Persistent or recurrent FLUTD · 8 mg/kg PO q12h · PO · q12h · Recent studies have not shown any statistical benefit.
- Osteoarthritis · 3 mg/kg IM on four occasions with an interval of 7 days between injections. · IM · q7d · 4 doses
- Osteoarthritis · Inject mixture back into joint · Intra-articular · Once · Prepare site as for surgery. Avoid iodine based skin preps; use neutral soapless cleanser. Withdraw ~1 mL synovial fluid, mix with pentosan in syringe, inject back. Firmly bandage and confine for 3-4 hours. Rest horse for 2 weeks, follow with 2 weeks graded walking.
- Osteoarthritis (High loading dose for treatment of OA signs of pain, lameness and stiffness) · 20 mg/kg PO twice weekly for 5 weeks · PO · twice weekly · 5 weeks · Always give on an empty stomach.
- Osteoarthritis (Medium Loading dose for management of OA after joint surgery) · 10 mg/kg PO once weekly for 12 weeks · PO · once weekly · 12 weeks · Always give on an empty stomach.
- Osteoarthritis (Maintenance dose) · 10 mg/kg once weekly for 4 weeks as needed · PO · once weekly · 4 weeks · Always give on an empty stomach.
- Osteoarthritis · 3 mg/kg IM or SC on four occasions with an interval of 5-7 days between injections · IM/SC · q5-7d · 4 doses
投与経路
禁忌
- Known hypersensitivity to pentosan polysulfate sodium
- Patients with active bleeding disorders
- Use with caution prior to surgery
有害事象
- Vomiting
- Anorexia
- Lethargy
- Mild depression
- Bleeding or prolonged coagulation times (dose-dependent increase in PTT in horses)
- Transient increases in liver enzymes (reported in humans)
薬物相互作用
- NSAIDs (e.g., carprofen, meloxicam) · May increase the risk of bleeding due to concurrent effects on coagulation and platelet function; use cautiously.
- Aspirin · Increased risk of bleeding due to combined anticoagulant and antiplatelet effects.
- Heparin · Additive anticoagulant effects; increased risk of hemorrhage.
モニタリング
- Clinical efficacy (improvement in lameness/mobility for OA, or reduction in urinary signs for FLUTD)
- Signs of bleeding or bruising
- Intra-articular bleeding (when administered directly into joints)
過量投与
Information regarding overdoses is limited. * **Potential Signs:** Overdoses could potentially cause bleeding, thrombocytopenia, gastrointestinal distress, and liver function abnormalities. * **Treatment:** Treatment recommendations are basically supportive in nature. If an acute oral overdose occurs, consider standard protocols for drug removal from the gut (e.g., emesis, activated charcoal) if performed promptly.
VetSheet の薬剤リファレンスは、獣医療従事者向けの臨床意思決定支援を目的としており、専門的判断やメーカーの最新添付文書に代わるものではありません。