オキシブチニン
オキシブチニンは泌尿生殖器の平滑筋弛緩薬および抗コリン薬です。獣医学においては、主に犬の**排尿筋過反射**(過活動膀胱または切迫性尿失禁)や、猫白血病ウイルス(FeLV)に関連する排尿筋不安定症の猫に対する補助療法として使用されます。 主な臨床的ポイント: * 膀胱容量を増加させ、抑制されない収縮を減少させる尿路鎮痙薬として作用します。 * 直接的な平滑筋弛緩作用と抗コリン作用の両方を持ちます。 * **臨床上の注意点:** 抗コリン作用があるため、副交感神経の緊張低下により悪化する状態(緑内障、消化管うっ滞、頻脈性不整脈など)の患者には極めて慎重に使用する必要があります。
作用機序: Oxybutynin exerts its effects via a dual mechanism of action on the lower urinary tract: 1. **Antimuscarinic (atropine-like) effect:** It competitively antagonizes acetylcholine at postganglionic muscarinic receptors. It has a high affinity for **M1, M2, and M3 receptors**, with M3 being the primary receptor mediating bladder detrusor contraction. 2. **Direct spasmolytic (papaverine-like) effect:** It directly relaxes smooth muscle independent of its anticholinergic activity. These combined actions → relaxation of the bladder detrusor muscle → **increased maximum bladder capacity** → **decreased frequency and amplitude of uninhibited detrusor contractions** → delayed initial desire to void.
動物種別の用量
- To decrease bladder contractility (detrusor hyperreflexia) · 0.5-1 mg (total dose) · PO · q8-12h · Juvenile animals may require a prolonged dosing interval.
- To decrease bladder contractility (detrusor hyperreflexia) · 0.5-1.25 mg per cat · PO · q8-12h
- Detrusor hyperreflexia · 0.5-1.25 mg per cat · PO · q8-12h
- To decrease bladder contractility (detrusor hyperreflexia) · 0.2 mg/kg · PO · q8-12h · Most dogs are dosed at 1.25-3.75 mg (total dose) q12h. Juvenile animals may require a prolonged dosing interval.
- To decrease bladder contractility (detrusor hyperreflexia) · 1.25-5 mg (total dose) · PO · q8-12h
- To decrease bladder contractility (detrusor hyperreflexia) · 2-5 mg (total dose) · PO · q8-12h
- Detrusor hyperreflexia (refractory incontinence) · 0.2 mg/kg · PO · q8-12h
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
- Obstructive GI tract disease
- Intestinal atony or paralytic ileus
- Angle closure glaucoma
- Hiatal hernia
- Cardiac disease (especially mitral stenosis, arrhythmias, tachycardia, CHF)
- Myasthenia gravis
- Hyperthyroidism
- Prostatic hypertrophy
- Severe ulcerative colitis
- Urinary retention or other obstructive uropathies
- Obstructive GI disease
- Ileus
- Gastrooesophageal reflux
- Glaucoma
- Cardiac disease
- Obstructive urinary disease
有害事象
- Diarrhea
- Constipation
- Urinary retention
- Hypersalivation
- Sedation
- Dry mouth (xerostomia)
- Dry eyes (keratoconjunctivitis sicca)
- Tachycardia
- Anorexia
- Vomiting
- Weakness
- Mydriasis (pupil dilation)
- Diarrhoea
- Dry mouth
- Dry eyes
- Skin reactions
- Palpitations
薬物相互作用
- Anticholinergic agents (e.g., atropine, propantheline, tricyclic antidepressants, antihistamines) · May intensify oxybutynin's anticholinergic adverse effects.
- Azole antifungals (e.g., ketoconazole) · May inhibit metabolism and increase oxybutynin systemic levels.
- CNS depressants · May exacerbate the sedating effects of oxybutynin. · moderate
- Macrolide antibiotics (e.g., erythromycin, clarithromycin) · May inhibit metabolism and increase oxybutynin systemic levels.
- Anticholinergic agents · Additive anticholinergic side effects (e.g., severe constipation, urinary retention, tachycardia) · major
- Azole antifungals · Potential CYP inhibition leading to increased oxybutynin plasma concentrations · moderate
- Macrolide antibiotics · Potential CYP inhibition leading to increased oxybutynin plasma concentrations · moderate
モニタリング
- Clinical efficacy (reduction in urinary incontinence or frequency)
- Adverse effects (signs of anticholinergic toxicity such as dry mouth, tachycardia, constipation, or urinary retention)
- Urinary output and frequency
- Heart rate
- Bowel movements (monitor for constipation)
- Signs of excessive sedation
過量投与
Overdosage can lead to severe anticholinergic toxicity. * **CNS effects:** Restlessness, excitement, seizures. * **Cardiovascular effects:** Hypertension or hypotension, tachycardia, circulatory failure. * **Other signs:** Fever, nausea, vomiting. * **Massive overdose:** May lead to paralysis, coma, respiratory failure, and death. **Treatment:** Consists of general techniques to limit GI absorption (e.g., emesis, activated charcoal) and supportive care. Intravenous **physostigmine** may be useful to reverse severe anticholinergic signs.
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。