ジフェノキシレートおよびアトロピン
**ジフェノキシレート**は、メペリジンに構造が類似した合成フェニルピペリジン誘導体のオピオイド作動薬です。獣医療では主に犬の**止瀉薬**および**鎮咳薬**(咳止め)として使用されます。 主な薬理学的特徴: * **運動性の調節**:消化管の通過時間を遅らせることで水分の吸収を促し、下痢を軽減します。 * **乱用防止**:市販の製剤には、治療量以下の**硫酸アトロピン**が含まれています。通常量ではアトロピンの臨床的影響はありませんが、過剰摂取すると不快な抗コリン作用(口渇、頻脈など)が生じるため、乱用防止に役立ちます。 * **規制薬物**:オピオイドの性質を持つため、**第V種向精神薬**に分類されます。 > **臨床上のポイント**:猫への使用は、逆説的な興奮行動を引き起こすリスクがあるため、非常に議論の余地があります。体重10kg未満の小型犬では、強力な錠剤による偶発的な過剰投与を防ぎ、正確な用量調整を可能にするため、液剤の使用が強く推奨されます。
作用機序: Diphenoxylate exerts its effects primarily through interaction with opioid receptors in the gastrointestinal tract and central nervous system: * **GI Motility**: Binds to **μ-opioid receptors** in the enteric nervous system (myenteric plexus) → decreases the release of acetylcholine and prostaglandins → inhibits excessive GI propulsion and increases segmental (non-propulsive) contractions → **prolongs intestinal transit time**. * **Secretion Reduction**: Decreases intestinal secretion induced by cholera toxin, prostaglandin E2, and non-cAMP/cGMP mediated diarrheas. Enhances mucosal fluid and electrolyte absorption. * **Antitussive Effect**: Acts directly on the **medullary cough center** in the brain → depresses the cough reflex. * **Atropine Component**: Acts as a competitive antagonist at **muscarinic acetylcholine receptors**, though its dose in this combination is too low to exert significant systemic anticholinergic effects unless overdosed.
動物種別の用量
- As an antidiarrheal · 0.08-0.1 mg/kg PO q12h · PO · q12h · Use in cats is controversial.
- As an antidiarrheal · 0.1-0.2 mg/kg PO q12h · PO · q12h
- As an antidiarrheal · 0.05 mg/kg PO three times a day · PO · TID · Maximum 5 days · Probably should not be given longer than 5 days and are potentially contraindicated when diarrhea is suspected to be caused by enteric infections
- As an antidiarrheal · 0.05-0.2 mg/kg PO q8-12h · PO · q8-12h
- As an antidiarrheal · 0.05-0.1 mg/kg PO three to four times a day. · PO · TID to QID
- As an antitussive · Approximately 0.25 mg/kg PO q8-12h · PO · q8-12h
- As an antitussive · 0.2-0.5 mg/kg PO q12h · PO · q12h · Until clinical signs subside · May be used for extended periods. Constipation is an occasional problem, but stool softeners can alleviate.
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
- Known hypersensitivity to narcotic analgesics
- Patients receiving monoamine oxidase inhibitors (MAOIs)
- Diarrhea caused by toxic ingestion (until the toxin is eliminated from the GI tract)
- Intestinal obstruction
- Bacterial-induced acute diarrhea (may enhance bacterial proliferation)
有害事象
- Constipation
- Bloat
- Sedation
- Paralytic ileus (potential)
- Toxic megacolon (potential)
- Pancreatitis (potential)
- CNS depression or excitation
- Excitatory behavior (especially in cats)
薬物相互作用
- CNS Depressant Drugs (anesthetics, antihistamines, phenothiazines, barbiturates, tranquilizers, alcohol) · May cause increased CNS or respiratory depression when used concurrently.
- Monoamine Oxidase Inhibitors (MAOIs) (e.g., amitraz, selegiline) · Contraindicated. Do not use opiate antidiarrheals for at least 14 days after receiving MAOIs due to risk of severe adverse reactions.
モニタリング
- Clinical efficacy (resolution of diarrhea or cough)
- Fluid and electrolyte status (especially in severe diarrhea)
- CNS effects (sedation or excitation), particularly if using high dosages
- Bowel movements (monitor for constipation)
- Plasma amylase and lipase (may be artificially increased for up to 24 hours post-administration)
過量投与
Acute overdosage can result in severe **CNS, cardiovascular, gastrointestinal, or respiratory toxicity**. * **Delayed Absorption**: Because opiates significantly reduce GI motility, absorption of the drug from the GI tract may be delayed and prolonged, meaning toxicity can worsen over time. * **Opiate Toxicity**: Signs include profound sedation, respiratory depression, and pinpoint pupils. **Naloxone** may be necessary to reverse the opiate effects. * **Atropine Toxicity**: Massive overdoses may induce atropine toxicity (dry mouth, tachycardia, hyperthermia, dilated pupils, agitation).
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。