ヒヨスチアミン
**ヒヨスチアミン**はベラドンナアルカロイドであり、ラセミ体アトロピンの高活性な左旋性異性体です。活性エナンチオマーであるため、中枢および末梢の抗コリン作用においてアトロピンよりも著しく強力です。 獣医学での使用は比較的限られていますが、他の抗コリン薬(グリコピロレートやアトロピンなど)の有用な代替薬として機能します。主に以下の目的で使用されます: * **消化管運動亢進:** 痙攣を軽減することにより、過敏性腸症候群(IBS)などの状態を管理します。 * **心血管サポート:** 症候性徐脈または洞不全症候群の治療。 * **周術期の使用:** 流涎過多、尿道痙攣、気道分泌物の減少に役立つ可能性がありますが、動物における臨床データは乏しいです。 > **臨床のポイント:** ヒヨスチアミンはグリコピロレートのような4級抗コリン薬よりも血液脳関門を容易に通過するため、逆説的興奮や鎮静などの中枢神経系(CNS)の副作用について患者を注意深く監視する必要があります。
作用機序: Hyoscyamine acts as a competitive, reversible antagonist of acetylcholine at **muscarinic receptors** (M1-M5) located on smooth muscle, cardiac muscle, and glandular cells. * **Gastrointestinal/Urinary:** Blocks parasympathetic stimulation → relaxes smooth muscle → decreases GI and urinary tract motility and spasms. * **Secretions:** Inhibits glandular muscarinic receptors → dose-dependent reduction in salivary, bronchial, pharyngeal, and gastric secretions. * **Cardiovascular:** Blocks vagal (parasympathetic) tone at the sinoatrial (SA) node → increases heart rate. * **Ocular:** Paralyzes the pupillary sphincter muscle → causes mydriasis (pupil dilation).
動物種別の用量
- Irritable bowel syndrome · 0.003-0.006 mg/kg PO two to three times a day · PO · q8-12h · Assumed to be for immediate release oral dosage forms.
- Long-term management of symptomatic patients with sinus node disease · 0.003-0.006 mg/kg PO q8h · PO · q8h · Long-term · Assumed to be for immediate release oral dosage forms.
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
- Hypersensitivity to hyoscyamine or other belladonna alkaloids
- Glaucoma (narrow or wide angle)
- Intestinal obstruction or intestinal atony
- Toxic megacolon
- Severe ulcerative colitis
- Obstructive uropathy
- Acute hemorrhage with cardiovascular instability
有害事象
- Mydriasis (pupil dilation)
- Xerostomia (dry mouth)
- Constipation
- Urinary retention
- Xerophthalmia (dry eyes)
- Tachycardia
- CNS effects (somnolence, delirium, or paradoxical excitement at higher doses)
薬物相互作用
- Antacids (magnesium, aluminum, calcium salts) · May interfere with the gastrointestinal absorption of hyoscyamine.
- Other Anticholinergics (e.g., atropine, glycopyrrolate) · Additive anticholinergic actions and increased risk of adverse effects.
- First-Generation Antihistamines (e.g., diphenhydramine) · Additive anticholinergic actions and increased risk of adverse effects.
- Prokinetic Agents (e.g., cisapride, metoclopramide) · Hyoscyamine may antagonize and counteract their gastrointestinal prokinetic effects.
モニタリング
- Clinical efficacy (resolution of GI spasms or improvement in heart rate)
- Heart rate and rhythm
- Bowel elimination (monitor for constipation/ileus)
- Urinary elimination (monitor for urinary retention)
過量投与
Significant overdosage can be life-threatening; contacting an animal poison control center is strongly advised. The LD50 in rats is 375 mg/kg. **Clinical Signs of Toxicity:** * Intensified anticholinergic effects: severe tachycardia, mydriasis, urinary retention, and absent gut sounds (ileus). * CNS signs: behavioral changes, severe depression, delirium, or seizures. **Treatment:** * **Decontamination:** Protocols to decrease oral absorption (e.g., emesis, activated charcoal) should be considered if the overdose was recent and the patient is asymptomatic. * **Antidote:** Severe anticholinergic effects can be treated with **physostigmine** or **neostigmine**, but this should *only* be done under the strict guidance of a poison control center due to the risk of cholinergic crisis. * **Supportive Care:** Delirium or excitement can be managed with small doses of short-acting barbiturates or benzodiazepines. Hyoscyamine can be removed by hemodialysis.
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。