グリコピロレート
Glycopyrrolate
Glycopyrronium bromide
別名: Robinul-V · Robinul Forte · glycopyrronium bromide · AHR-504 · Acpan · AmTech · Gastrodyn · Glycostigmin
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
監査済み v13 用量エビデンス
確認済み・計算対象外のエビデンス確認済み・計算対象外のエビデンス (1)
エビデンス表示のみ（自動計算対象外）
Premedication (extra-label)
Premedication (extra-label): 0.01 – 0.02 mg/kg IM, SC, or IV
必ず考慮する臨床コンテキスト (1)
- Glycopyrrolate tablets should be stored in tight containers and both the injection and tablets should be stored at room temperature (15°C -30°C [59°F-86°F]).
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
グリコピロレートは合成第四級アンモニウム抗ムスカリン薬であり、主に麻酔前投薬、徐脈の治療、および唾液分泌過多の軽減に使用されます。アトロピンとは異なり、血液脳関門を通過しにくいため、中枢神経系の副作用が少なくなっています。
作用機序
Glycopyrrolate acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors (M1, M2, M3).
Acetylcholine → Blocked at Muscarinic Receptors → Decreased parasympathetic tone.
This blockade leads to:
- Heart: Vagolytic effect → Increased heart rate (tachycardia).
- Secretions: Antisialagogue effect → Profound reduction in salivary, tracheobronchial, and pharyngeal secretions.
- GI/Urinary: Decreased smooth muscle motility and tone.
- Eye: Mydriasis (pupil dilation) and cycloplegia.
安全性・警告
禁忌
- Narrow angle glaucoma
- Tachycardias
- Gastrointestinal ileus
- Urinary obstruction
- Hypersensitivity to the drug
- Pregnancy (per some manufacturer labels)
有害事象
- Dry secretions (xerostomia)
- Initial bradycardia followed by tachycardia
- Decreased gastrointestinal motility (risk of ileus)
- Decreased urinary tract motility
- Mydriasis and cycloplegia
注意事項
Use with extreme caution in patients with known or suspected GI infections, as decreased GI motility can prolong retention of toxins or causative agents. Use with extreme caution in patients with autonomic neuropathy.
Use cautiously in patients with hepatic or renal disease, geriatric or pediatric patients, hyperthyroidism, hypertension, congestive heart failure (CHF), tachyarrhythmias, prostatic hypertrophy, or esophageal reflux. Can produce sinus tachycardia and predispose hypotensive patients to cardiac arrhythmias (including ventricular fibrillation).
医薬品相互作用
May enhance the activity or toxicity of glycopyrrolate.
May enhance anticholinergic activity or toxicity.
May enhance anticholinergic activity or toxicity.
May enhance anticholinergic activity or toxicity.
May enhance anticholinergic activity or toxicity.
May aggravate signs seen with amitraz toxicity, leading to hypertension and further inhibition of peristalsis.
May decrease PO absorption; give oral glycopyrrolate at least 1 hour prior to oral antacids.
May increase intraocular pressure when used concurrently.
May increase serum digoxin levels; use regular digoxin tablets or oral liquid.
Increased gastric pH may decrease GI absorption; administer 2 hours after ketoconazole.
Glycopyrrolate may antagonize the prokinetic actions of metoclopramide.
監視
- Heart rate and rhythm
- Respiratory rate and effort
- Gastrointestinal motility (auscultation for bowel sounds)
- Salivary and respiratory secretions
薬物動態
吸収
Not completely absorbed after oral administration. In dogs, IV onset of action is generally within 1 minute. After IM or SC administration, peak effects occur approximately 30-45 minutes post-injection.
分布
Completely ionized quaternary ammonium compound; poor lipid solubility. Does not readily penetrate into the CNS or eye. Crosses the placenta only marginally.
代謝
Only a small amount is metabolized.
消失
Eliminated rapidly from the serum after IV administration (virtually no drug remains 30 minutes to 3 hours after dosing). Majority is eliminated unchanged in the feces and urine.
過剰投与
In dogs, the LD50 is reported to be 25 mg/kg IV. In cats, the LD50 after IM injection is 283 mg/kg. Because of its quaternary structure, minimal CNS effects would be expected after an overdose compared to atropine. Overdose may present with severe anticholinergic signs (extreme tachycardia, mydriasis, dry mucous membranes, ileus). Treatment is generally supportive.
製品
製剤
- Injection
- Tablets
動物用医薬品
- Glycopyrrolate for Injection: 0.2 mg/mL in 20 mL vials; Robinul-V (Pfizer), generic
ヒト用医薬品
- Glycopyrrolate Tablets: 1 mg & 2 mg; Robinul & Robinul Forte (Horizon); generic
- Glycopyrrolate Injection: 0.2 mg/mL in 1 mL, 2 mL, 5 mL, & 20 mL vials; Robinul (Robins); 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
Tablets should be stored in tight containers. Both injection and tablets should be stored at room temperature (15-30°C). Stable under ordinary conditions of light and temperature. Most stable in solution at an acidic pH; undergoes ester hydrolysis at pH above 6.
飼主向け情報
注射剤は、適切な心電図モニターが利用できる環境で専門スタッフによって投与されるのが最適です。ペットが自宅で錠剤を服用している場合は、口の渇きが一般的な副作用であるため、いつでも自由に水が飲めるようにしてください。便秘や排尿困難の兆候が見られた場合は、獣医師に連絡してください。
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