シサプリド
シサプリドは強力な消化管運動機能改善剤であり、獣医療では主に**猫の巨大結腸症**、**胃うっ滞**、**逆流性食道炎**の管理に使用されます。 > **臨床上のポイント:** ヒトにおいて重篤な不整脈(QT延長)を引き起こすリスクがあるため、シサプリドはヒト用市場から自主回収されました。現在、獣医療の患者向けには**調剤薬局(コンパウンディング・ファーマシー)**を通じてのみ入手可能です。ヒトにおける心臓へのリスクにもかかわらず、犬や猫では一般的に非常に良好な忍容性を示します。 食道から結腸に至るまでの運動を刺激するのに非常に効果的であり、猫の慢性便秘治療の基礎となる薬剤です。
作用機序: Cisapride acts primarily as a **serotonin 5-HT4 receptor agonist** in the gastrointestinal tract. * **5-HT4 activation** → stimulates the release of **acetylcholine** at the myenteric plexus. * This increases lower esophageal sphincter pressure, enhances esophageal peristalsis, and accelerates gastric emptying and colonic motility. * Unlike metoclopramide, it has minimal dopamine receptor blockade (no extrapyramidal effects) and does not stimulate gastric acid secretion. * Acetylcholinesterase activity is not inhibited.
動物種別の用量
- For chronic constipation (e.g., megacolon) · 2.5 mg (for cats up to 10 pounds) or 5 mg (for cats 11 pounds or heavier) three times daily, 30 minutes before food. Cats weighing greater than 16 pounds may require 7.5 mg. · PO · q8h · In combination with a stool softener and a bulk agent.
- For chronic constipation (e.g., megacolon) · 1.25-2.5 mg per cat two to three times a day · PO · q8-12h · Cats with hepatic insufficiency should be treated with half the usual dose; probably most effective when given 15 minutes before a meal.
- For chronic constipation (e.g., megacolon) · 2.5-5 mg per cat PO q8-12h · PO · q8-12h
- For chronic constipation (e.g., megacolon) · 5 mg per cat (total dose) PO q8-12h · PO · q8-12h
- For gastric stasis · 0.1 mg/kg PO two to three times daily; cats tolerate 2.5 mg doses without problems · PO · q8-12h
- To reduce the risk for esophageal stricture formation in cases of esophagitis · 0.5-0.75 mg/kg PO three times daily. · PO · q8h
- As a promotility agent (Foals with periparturient asphyxia) · 10 mg (total dose) PO q6-8h. · PO · q6-8h · Adequate time for healing of damaged bowel before using prokinetic agents is essential.
- Promotility (Mice, Rats, Gerbils, Hamsters, Guinea pigs, Chinchillas) · 0.1-0.5 mg/kg PO q12h · PO · q12h
用量は獣医療従事者向けの臨床リファレンスです。必ず最新の添付文書と個々の患者で確認してください。
投与経路
禁忌
- Gastrointestinal perforation
- Gastrointestinal obstruction
- Gastrointestinal hemorrhage
- Hypersensitivity to cisapride
有害事象
- Vomiting
- Diarrhea
- Abdominal discomfort
- Prolonged QT intervals or cardiac arrhythmias (very rare in veterinary patients)
薬物相互作用
- Anticholinergic agents · May diminish the prokinetic effects of cisapride.
- Benzodiazepines · Cisapride may enhance the sedative effects of benzodiazepines.
- Warfarin · Cisapride may enhance anticoagulant effects; additional monitoring and dosage adjustments may be required.
- Oral drugs with a narrow therapeutic index · Cisapride decreases GI transit times, potentially altering the absorption of other oral drugs. Serum levels may need closer monitoring.
- CYP3A4 Inhibitors (Amiodarone, Ketoconazole, Itraconazole, Fluconazole, Chloramphenicol, Cimetidine, Fluvoxamine, Grapefruit juice, Macrolides except azithromycin) · Inhibit cisapride metabolism, leading to increased cisapride levels and an increased risk for cisapride cardiotoxicity.
- QT-prolonging drugs (Amiodarone, Clarithromycin, Moxifloxacin, Procainamide, Quinidine, Sotalol, Tricyclic Antidepressants) · May increase the risk of QT interval prolongation and fatal arrhythmias when used concurrently with cisapride.
モニタリング
- Efficacy (resolution of GI stasis, constipation, regurgitation)
- Adverse effects profile (GI upset, signs of arrhythmias)
過量投与
LD50 doses in various lab animals range from 160 - 4000 mg/kg. The reported oral lethal dose in dogs is 640 mg/kg. **Clinical Signs:** Most common adverse effects seen in dogs and cats are diarrhea, lethargy, ataxia, hypersalivation, muscle fasciculations, agitation, abnormal behavior, hyperthermia, and possibly seizures (dogs). **Treatment:** Significant overdoses should be handled using standard gut emptying protocols when appropriate. Supportive therapy should be initiated when required. **Activated charcoal** is effective in binding unabsorbed cisapride.
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。