プロパンテリン臭化物
Propantheline Bromide
Propantheline bromide
別名: Pro-Banthine · bromuro de propantelina · propanthelini bromidum · Bropantil · Corrigast · Ercorax Rollon · Ercoril · Ercotina · Pantheline · Probamide
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Detrusor hyperreflexia, urge incontinence | 0.2 mg/kg PO q6-8h; increase dose if necessary to the lowest dose that will control clinical signs | PO | q6-8h | — | 🌎 NA |
| Detrusor hyperreflexia, urge incontinence | 7.5-30 mg (total dose) PO once a day to q8h | PO | q24h to q8h | — | 🌎 NA |
| Detrusor hyperreflexia, urge incontinence | 7.5-15 mg (total dose) PO q12h; occasionally dosages of 30 mg q8h are required | PO | q12h | — | 🌎 NA |
| Sinus bradycardia, incomplete AV block, etc. | 0.25-0.5 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Sinus bradycardia, incomplete AV block, etc. | 7.5-30 mg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Colitis, irritable bowel syndrome, etc. | 0.25 mg/kg PO three times a day | PO | TID | Do not use longer than 48-72 hours (48 hours for acute colitis) | 🌎 NA |
| Colitis, irritable bowel syndrome, etc. | 0.5 mg/kg two to three times daily | PO | BID-TID | — | 🌎 NA |
| As an antiemetic/antidiarrheal | 0.25 mg/kg PO q8h | PO | q8h | — | 🌎 NA |
- Sinus bradycardia, incomplete AV block, etc.: Usually well tolerated, but improvement is usually partial and often temporary.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Detrusor hyperreflexia, urge incontinence | 0.25-0.5 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Detrusor hyperreflexia, urge incontinence | 5-7.5 mg (total dose) PO once a day to once every 3 days | PO | q24h to q72h | — | 🌎 NA |
| Detrusor hyperreflexia, urge incontinence | 5-7.5 mg (total dose) PO q8h; 7.5 mg PO q72h | PO | q8h or q72h | — | 🌎 NA |
| Sinus bradycardia, incomplete AV block, etc. | 0.8-1.6 mg/kg three times daily | PO | TID | — | 🌎 NA |
| Sinus bradycardia, incomplete AV block, etc. | 7.5 mg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Chronic colitis | 0.5 mg/kg two to three times daily | PO | BID-TID | — | 🌎 NA |
| As an antiemetic/antidiarrheal | 0.25 mg/kg PO q8h | PO | q8h | — | 🌎 NA |
- Detrusor hyperreflexia, urge incontinence: Empirical dosage. Further studies required to substantiate beneficial effect.
- Sinus bradycardia, incomplete AV block, etc.: Although generally ineffective, a trial may be attempted.
- Sinus bradycardia, incomplete AV block, etc.: Usually well tolerated, but improvement is usually partial and often temporary.
馬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| To reduce rectal contractions during oocyte collection | 0.04 mg/kg IV | IV | Once | — | 🌎 NA |
| To inhibit peristalsis for 2 hours during rectal surgery | 30 mg IV | IV | Once | — | 🌎 NA |
- To reduce rectal contractions during oocyte collection: Must be freshly prepared and filtered through a 0.22 micron-filter from oral tablets.
- To inhibit peristalsis for 2 hours during rectal surgery: Must be freshly prepared and filtered through a 0.22 micron-filter from oral tablets.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
プロパンテリン臭化物は、合成の第四級アンモニウム抗ムスカリン(抗コリン)薬です。獣医学では主にその鎮痙作用および分泌抑制作用のために使用されます。
主な臨床用途:
- 小動物: 下痢、排尿筋過反射(切迫性尿失禁)、および抗コリン薬に反応する徐脈の治療。
- 馬: 結腸の蠕動運動を抑え、直腸を弛緩させるために静脈内投与され、直腸検査や手術をより安全に行うために用いられます。
臨床のポイント: プロパンテリンは第四級アンモニウム化合物であるため、常にイオン化しており水溶性が高いです。この構造的特徴により、血液脳関門(BBB)を通過したり眼に浸透したりしにくくなっています。その結果、アトロピンのような第三級アミンと比較して、中枢神経系(CNS)や眼への副作用を大幅に抑えつつ、末梢の抗コリン作用(消化管の弛緩や心拍数の増加など)をもたらします。
作用機序
Propantheline acts as a competitive antagonist at muscarinic acetylcholine receptors (primarily M1, M2, and M3 subtypes) located on smooth muscle, cardiac muscle, and exocrine glands.
- Gastrointestinal Tract: Blockade of M3 receptors → decreased smooth muscle tone and peristalsis (antispasmodic effect) + reduced gastric acid secretion.
- Urinary Tract: Blockade of M3 receptors on the detrusor muscle → relaxation of the bladder wall → increased bladder capacity and reduced urge incontinence.
- Cardiovascular System: Blockade of M2 receptors on the sinoatrial (SA) node → vagolytic effect → increased heart rate.
- Exocrine Glands: Blockade of muscarinic receptors → decreased salivation and respiratory secretions.
安全性・警告
禁忌
- Hypersensitivity to anticholinergics
- Tachycardias secondary to thyrotoxicosis or cardiac insufficiency
- Myocardial ischemia
- Unstable cardiac status during acute hemorrhage
- Gastrointestinal obstructive disease
- Paralytic ileus
- Severe ulcerative colitis
- Obstructive uropathy
- Myasthenia gravis (unless used to reverse adverse muscarinic effects secondary to therapy)
有害事象
- Dry mouth (xerostomia)
- Dry eyes (keratoconjunctivitis sicca)
- Urinary hesitancy or retention
- Tachycardia
- Constipation
- Vomiting (especially in cats)
- Hypersalivation (especially in cats)
- Ileus (at high doses, potentially leading to bacterial overgrowth)
注意事項
Extreme Caution:
- GI Infections: Can decrease GI motility and prolong retention of causative agents or toxins, worsening clinical signs.
- Autonomic Neuropathy: Use with extreme caution.
Caution:
- Hepatic or renal disease
- Hyperthyroidism
- Hypertension
- Congestive Heart Failure (CHF)
- Tachyarrhythmias
- Prostatic hypertrophy
- Esophageal reflux
- Geriatric or pediatric patients
- Nursing patients (unknown if excreted in milk, but anticholinergics can reduce milk production and cause toxicity in neonates)
医薬品相互作用
May enhance the anticholinergic activity of propantheline.
May enhance the activity of propantheline.
Propantheline may decrease the absorption of cimetidine.
Long-term concurrent use may increase intraocular pressure.
May enhance the activity of propantheline.
May potentiate the adverse effects of propantheline.
Propantheline may enhance the actions of nitrofurantoin.
May enhance the anticholinergic activity of propantheline.
Propantheline may enhance their actions.
Propantheline delays absorption but increases peak serum levels of ranitidine; relative bioavailability of ranitidine may increase by 23%.
Propantheline may enhance their actions.
監視
- Clinical efficacy (resolution of diarrhea, incontinence, or bradycardia)
- Heart rate and rhythm (if indicated)
- Adverse effects (dry mouth, constipation, urinary retention)
薬物動態
吸収
Incompletely absorbed after oral administration due to complete ionization. Food decreases the amount absorbed. Variably absorbed in dogs; dosages require individual titration.
分布
Poorly lipid soluble; does not extensively penetrate into the CNS or eye.
代謝
Believed to be prevalently metabolized in the GI tract and/or liver.
消失
Less than 5% of an oral dose is excreted unchanged in the urine.
過剰投与
Toxicity Profile: Because of its quaternary structure, minimal CNS effects are expected following an overdose compared to tertiary amines like atropine.
Treatment:
- Decontamination: If recent oral ingestion, empty gut contents and administer activated charcoal and saline cathartics.
- Supportive Care: Treat clinical signs symptomatically. Fluid therapy and standard treatments for shock may be instituted. Do not use phenothiazines as they may exacerbate anticholinergic effects.
- Antidote (Physostigmine): Controversial. Reserve for extreme agitation/risk of injury, or severe/life-threatening supraventricular and sinus tachycardias.
- Human pediatric dose (reasonable for small animals): 0.02 mg/kg slow IV; may repeat q10 minutes until reversal of toxic effects.
- Note: Physostigmine adverse effects (bronchoconstriction, bradycardia, seizures) may be treated with small doses of IV atropine.
製品
製剤
- Tablets (Human-labeled): 7.5 mg, 15 mg
- Injectable: No commercial veterinary product available; must be freshly compounded/filtered from oral tablets for equine IV use
ヒト用医薬品
- Propantheline Bromide Tablets: 7.5 mg & 15 mg (Pro-Banthine®; generic)
規制ステータス
規制データなし: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Propantheline bromide tablets should be stored at room temperature in tight containers.
飼主向け情報
重要: プロパンテリンは、下痢、尿失禁、または徐脈の治療に使用されます。平滑肌を弛緩させ、腺の分泌を減少させる働きがあります。
- 口の渇き: ペットの口が渇くことがあります。10〜15分おきにペットの舌に少量の水を含ませることで和らげることができます。
- 症状の悪化に注意: 長引く嘔吐や下痢は深刻な状態を招く可能性があります。症状が改善しない、または悪化する場合は、すぐに獣医師に連絡してください。
- その他の副作用: 便秘、排尿困難、または心拍数の異常な増加に注意してください。猫の場合、この薬を服用した後に時々よだれを垂らしたり嘔吐したりすることがあります。
- 投薬について: 処方された通りに正確に投与してください。獣医師に相談せずに急に投薬を中止しないでください。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。
