プロメタジン
プロメタジンはフェノチアジン系誘導体であり、獣医療では主に制吐薬および抗ヒスタミン薬として利用されます。 * **主な用途**: 犬や猫の悪心・嘔吐の管理に時折使用され、アトピー性皮膚炎の犬の掻痒症に対しても試験的に使用されています(ただし後者の有効性は一般的に低いです)。 * **薬理学的特徴**: アセプロマジンのようなトランキライザーと構造的に類似していますが、プロメタジンは強力な抗ヒスタミン作用に加え、制吐作用、抗コリン作用、鎮静作用、および軽度の局所麻酔作用を持つことが特徴です。 > **臨床のポイント**: 鎮静や錐体外路系の副作用のリスクがあるため、マロピタントやオンダンセトロンなどの新しい制吐薬、あるいはジフェンヒドラミンなどの標準的な抗ヒスタミン薬と比較して、現代の獣医療で処方されることは比較的まれです。
作用機序: Promethazine exerts its effects through competitive antagonism at multiple receptor sites centrally and peripherally: * **H1-Receptor Antagonism**: Competitively blocks histamine at H1 receptors → reduces allergic responses and pruritus. * **D2-Dopaminergic Antagonism**: Blocks dopamine receptors in the Chemoreceptor Trigger Zone (CRTZ) of the medulla → provides central **antiemetic** effects. * **Muscarinic Antagonism**: Blocks acetylcholine at muscarinic receptors → contributes to antiemetic efficacy and causes anticholinergic side effects (e.g., dry mouth). * **Alpha-1 Adrenergic Antagonism**: Blocks peripheral alpha-1 receptors → can lead to vasodilation and subsequent hypotension.
動物種別の用量
- As an antiemetic · 2 mg/kg PO or IM once daily · PO/IM · q24h
- As an antihistamine · 0.2-0.4 mg/kg PO three to four times a day · PO · q6-8h
- As an antihistamine · 1-2 mg/kg PO q12h · PO · q12h
- As an antiemetic · 2 mg/kg PO or IM once daily · PO/IM · q24h
- As an antihistamine · 0.2-0.4 mg/kg PO three to four times a day · PO · q6-8h
- As an antihistamine · 1-2 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
- Hypovolemia or shock (due to hypotensive effects)
- Tetanus or strychnine intoxication (due to extrapyramidal effects)
- Human label black box warning: Contraindicated in children < 2 years old (fatal respiratory depression)
- Known hypersensitivity to phenothiazines
- Severe central nervous system depression
- Comatose patients
- Use with caution in patients with seizure disorders
- Use with caution in patients with severe hepatic or cardiovascular disease
有害事象
- Sedation or lethargy
- Anticholinergic effects (dry mouth, urinary retention, decreased GI motility)
- Hypotension (especially with rapid IV administration or in hypovolemic patients)
- Extrapyramidal signs (tremors, rigidity, torticollis) - rare but possible
- Sedation / Lethargy
- Dry mucous membranes (anticholinergic effect)
- Tachycardia
- Hypotension
- Paradoxical excitation (especially in cats)
- Gastrointestinal disturbances
薬物相互作用
- Antacids · May cause reduced GI absorption of oral phenothiazines.
- Antidiarrheal mixtures (e.g., Kaolin/pectin, bismuth subsalicylate) · May cause reduced GI absorption of oral phenothiazines.
- Atropine & other anticholinergics · May have additive anticholinergic effects when used with promethazine.
- CNS Depressant Agents (barbiturates, narcotics, anesthetics) · May cause additive CNS depression if used with phenothiazines.
- Epinephrine · Phenothiazines block alpha-adrenergic receptors; concomitant epinephrine can lead to unopposed beta-activity causing vasodilation and increased cardiac rate (epinephrine reversal). · major
- Metoclopramide · Phenothiazines may potentiate the extrapyramidal effects of metoclopramide.
- Monoamine Oxidase Inhibitors (MAOIs) · May potentiate extrapyramidal effects.
- Opiates · May enhance the hypotensive effects of phenothiazines; dosages may need to be reduced.
- Organophosphate Agents · Phenothiazines should not be given within one month of worming with these agents as their toxic effects may be potentiated.
- CNS Depressants (e.g., opioids, barbiturates, anesthetics) · Additive central nervous system depression and sedation. · major
- Anticholinergic agents (e.g., atropine, glycopyrrolate) · Additive anticholinergic effects (tachycardia, dry mouth, ileus). · moderate
モニタリング
- Clinical efficacy (resolution of vomiting or pruritus)
- Degree of sedation
- Hydration status (if vomiting persists)
- Heart rate and rhythm
- Blood pressure (especially with IV use)
- Level of consciousness / CNS status
- Respiratory rate
過量投与
Overdose may result in profound sedation, severe hypotension, or acute extrapyramidal clinical signs (e.g., torticollis, tremors, excessive salivation, rigidity). * **Treatment**: Supportive care is primary. Acute extrapyramidal signs have been successfully treated with injectable **diphenhydramine** in humans. Hypotension should be treated with IV fluids; avoid epinephrine due to the risk of epinephrine reversal (use alpha-agonists like phenylephrine if pressors are required).
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。