프로판텔린 브로마이드

4급 암모늄 항무스카린제

**프로판텔린 브로마이드(Propantheline bromide)**는 합성 4급 암모늄 항무스카린(항콜린) 제제입니다. 수의학에서는 주로 진경 및 분비 억제 특성을 위해 사용됩니다. **주요 임상 용도:** * **소동물:** 설사, 배뇨근 반사 항진(절박성 요실금) 및 항콜린제 반응성 서맥의 관리. * **말:** 결장 연동 운동을 감소시키고 직장을 이완시키기 위해 정맥 투여하여 직장 검사 및 수술을 더 안전하게 수행할 수 있도록 돕습니다. **임상 요점:** 프로판텔린은 4급 암모늄 화합물이기 때문에 영구적으로 이온화되어 있으며 수용성이 높습니다. 이러한 구조적 특징으로 인해 혈액뇌장벽(BBB)을 쉽게 통과하거나 눈으로 침투하지 못합니다. 결과적으로 아트로핀과 같은 3급 아민에 비해 중추신경계(CNS) 또는 안구 부작용이 현저히 적으면서 말초 항콜린 효과(위장관 이완 및 심박수 증가 등)를 제공합니다.

작용 기전: **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.

동물 종별 용량

Cats

Detrusor hyperreflexia, urge incontinence · 0.25-0.5 mg/kg PO q12-24h · PO · q12-24h · Empirical dosage. Further studies required to substantiate beneficial effect.
Detrusor hyperreflexia, urge incontinence · 5-7.5 mg (total dose) PO once a day to once every 3 days · PO · q24h to q72h
Detrusor hyperreflexia, urge incontinence · 5-7.5 mg (total dose) PO q8h; 7.5 mg PO q72h · PO · q8h or q72h
Sinus bradycardia, incomplete AV block, etc. · 0.8-1.6 mg/kg three times daily · PO · TID · Although generally ineffective, a trial may be attempted.
Sinus bradycardia, incomplete AV block, etc. · 7.5 mg PO q8-12h · PO · q8-12h · Usually well tolerated, but improvement is usually partial and often temporary.
Chronic colitis · 0.5 mg/kg two to three times daily · PO · BID-TID
As an antiemetic/antidiarrheal · 0.25 mg/kg PO q8h · PO · q8h

Horses

To reduce rectal contractions during oocyte collection · 0.04 mg/kg IV · IV · Once · Must be freshly prepared and filtered through a 0.22 micron-filter from oral tablets.
To inhibit peristalsis for 2 hours during rectal surgery · 30 mg IV · IV · Once · Must be freshly prepared and filtered through a 0.22 micron-filter from oral tablets.

Dogs

투여 경로

POIV

금기

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)

이상반응

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)

약물 상호작용

Antihistamines · May enhance the anticholinergic activity of propantheline.
Benzodiazepines · May enhance the activity of propantheline.
Cimetidine · Propantheline may decrease the absorption of cimetidine.
Corticosteroids · Long-term concurrent use may increase intraocular pressure.
Meperidine · May enhance the activity of propantheline.
Nitrates · May potentiate the adverse effects of propantheline.
Nitrofurantoin · Propantheline may enhance the actions of nitrofurantoin.
Phenothiazines · May enhance the anticholinergic activity of propantheline.
Sympathomimetics · Propantheline may enhance their actions.
Ranitidine · Propantheline delays absorption but increases peak serum levels of ranitidine; relative bioavailability of ranitidine may increase by 23%.
Thiazide Diuretics · Propantheline may enhance their actions.

모니터링

Clinical efficacy (resolution of diarrhea, incontinence, or bradycardia)
Heart rate and rhythm (if indicated)
Adverse effects (dry mouth, constipation, urinary retention)

과용량

**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.

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