클로라제페이트
Clorazepate
Clorazepate dipotassium
다른 이름: Tranxene-SD · Gen-Xene · Tranxene T-tab · Abbott-35616 · AH-3232 · 4306-CB · clorazepic acid · dipotassium clorazepate · dikalii clorazepas
VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
동물 종별 용량
🌎 NA — North America🌍 EU — Europe
개
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| Adjunctive medication in the treatment of seizures (in combination with phenobarbital) | 1-2 mg/kg PO q12h, but may need to divide q12h dose and give q8h to minimize adverse effects and maintain therapeutic levels | PO | q8-12h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures (in combination with phenobarbital) | 0.5-1 mg/kg PO q8h | PO | q8h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures | 1-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures | 2-4 mg/kg PO twice daily, some dogs may require three times daily | PO | q8-12h | — | 🌎 NA |
| Third-line agent for seizures | 1-2 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Management of cluster seizures | 0.5-2 mg/kg two to three times daily | PO | q8-12h | 48-96 hours | 🌎 NA |
| Adjunctive therapy for fears and phobias | 11.25-22.5 mg per dog PO once to twice daily | PO | q12-24h | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 22.5 mg for large dogs, 11.25 mg for medium dogs and 5.6 mg for small dogs PO | PO | prn | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 0.55-2.2 mg/kg PO as needed up to q8h | PO | up to q8h | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 0.2-1 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
- Adjunctive medication in the treatment of seizures (in combination with phenobarbital): No advantage gained with using sustained release products. May affect phenobarb levels; monitor 2 and 4 weeks later.
- Management of cluster seizures: Give immediately after first seizure and stop after 48-96 hours. Used only during seizure activity, not as maintenance.
- Adjunctive therapy for fears and phobias: Recommends the sustained-delivery product (Tranxene-SD).
- Adjunctive therapy for fears and phobias: Using sustained delivery product. Adjust dosage according to dog's response.
- Adjunctive therapy for fears and phobias: Titrate to clinical sedation; dose may vary for individual dogs.
고양이
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| Anxiolytic or for compulsive behaviors | 0.2-0.5 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Alternative drug to phenobarbital for seizures | 3.75-7.5 mg (total dose per cat) PO once to twice daily | PO | q12-24h | — | 🌎 NA |
- Alternative drug to phenobarbital for seizures: Similar precautions are necessary as described for diazepam use in cats (risk of hepatic necrosis).
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
개요
클로라제페이트는 벤조디아제핀계 약물로, 수의학에서는 주로 보조 항경련제 및 불안이나 공포와 관련된 행동 장애 치료에 사용됩니다.
- 임상 요점: 이 약물은 전구약물(prodrug)로, 흡수되기 전에 위산 환경에서 빠르게 활성 대사체인 노르디아제팜(Nordiazepam)으로 변환되어야 합니다。
- 개에서는 난치성 발작을 치료하기 위해 페노바르비탈과 함께 자주 사용됩니다. 항경련 효과에 대한 내성이 발생할 수 있으나, 클로나제팜보다는 내성 발생 속도가 느린 것으로 보고됩니다.
- 고양이에서는 항불안제로 사용되거나 발작 관리를 위해 페노바르비탈의 대체제로 사용되기도 하지만, 경구용 벤조디아제핀이 고양이에서 특이체질성 간독성을 유발할 위험이 있으므로 주의가 필요합니다.
작용 기전
Benzodiazepines exert their effects by enhancing the inhibitory activity of gamma-aminobutyric acid (GABA) in the central nervous system.
- Mechanism: They bind to specific allosteric sites on the GABA-A receptor complex → increases the frequency of chloride channel opening → cellular hyperpolarization → decreased neuronal excitability.
- This depression of subcortical CNS levels (primarily limbic, thalamic, and hypothalamic) produces the characteristic anxiolytic, sedative, skeletal muscle relaxant, and anticonvulsant effects.
- Other postulated mechanisms include antagonism of serotonin and diminished release or turnover of acetylcholine in the CNS.
안전성·주의사항
금기사항
- Hypersensitivity to benzodiazepines
- Significant liver disease/dysfunction
- Acute narrow angle glaucoma
- Fear-induced aggression (relative contraindication; may disinhibit bite inhibition)
부작용
- Sedation (most common)
- Ataxia
- Physical dependence (with chronic use)
- Acute hepatic necrosis (idiosyncratic in cats)
- Paradoxical excitation or disinhibition of aggression
주의
Use with extreme caution in aggressive animals, particularly those with fear-induced aggression, as benzodiazepines can disinhibit anxiety-based bite inhibition and provoke attacks. Benzodiazepines may exacerbate myasthenia gravis. Safe use during pregnancy is not established (FDA Category D in humans; teratogenic effects noted in lab animals). The active metabolite, nordiazepam, is distributed into milk and may affect nursing neonates. Abrupt withdrawal after chronic use can precipitate severe rebound seizures.
약물 상호작용
May increase serum levels of benzodiazepines by inhibiting their metabolism.
May decrease the metabolism of benzodiazepines, leading to prolonged effects.
Additive CNS depression; may cause profound sedation or respiratory depression.
May decrease the metabolism of benzodiazepines.
Complex interaction: Clorazepate may initially increase phenobarbital serum levels. Over time, clorazepate levels may decrease, leading to decreased phenobarbital levels. Requires close monitoring.
May decrease clorazepate concentrations.
May induce hepatic microsomal enzymes and decrease the pharmacologic effects of benzodiazepines.
모니터링
- Clinical efficacy (seizure frequency or behavioral improvement)
- Adverse effects (sedation, ataxia)
- Liver enzymes (especially critical in cats due to risk of acute hepatic necrosis)
- Phenobarbital serum levels (if used concurrently, monitor at 2 and 4 weeks after adding clorazepate)
약동학
흡수
In dogs, peak serum levels generally occur within 1-2 hours.
분포
Volume of distribution is about 1.8 L/kg after multiple dosing in dogs. Nordiazepam is distributed into milk.
대사
Clorazepate is a prodrug that is rapidly decarboxylated in the acidic environment of the stomach to nordiazepam (active) and other metabolites.
배설
Eliminated primarily via hepatic metabolism and subsequent renal excretion of metabolites.
과다투여
When used alone, clorazepate overdoses are generally limited to significant CNS depression (confusion, coma, decreased reflexes, profound sedation).
- Treatment: Consists of standard protocols for removing and/or binding the drug in the gut (e.g., emesis if asymptomatic and recent, activated charcoal) and supportive systemic measures.
- The use of analeptic agents (CNS stimulants such as caffeine, amphetamines) is generally not recommended.
- Flumazenil (a specific benzodiazepine reversal agent) may be considered for very serious, life-threatening overdoses.
제품
제형
- Capsules
- Sustained-release tablets
인용의약품
- Clorazepate Dipotassium Tablets: 3.75 mg, 7.5 mg, & 15 mg (Tranxene T-tab; generic)
규제 현황
규제 데이터 없음: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
보관·안정성
Clorazepate dipotassium is unstable in the presence of water. Keep the desiccant packets in the original container of the capsules and tablets. Consider adding a desiccant packet to the prescription vial when dispensing large quantities.
보호자 정보
중요 경고: 갑자기 약물 투여를 중단하지 마십시오. 갑작스러운 중단은 생명을 위협하는 심각한 금단성 발작을 유발할 수 있습니다. 약물을 중단해야 할 경우 반드시 수의사와 상담하여 점진적인 감량 계획을 세우십시오.
- 규칙적인 투여가 핵심: 항경련 치료 실패의 주요 원인은 약물 투여를 건너뛰는 것입니다. 매일 일정한 시간에 약을 투여하십시오.
- 고양이 보호자 안내: 고양이가 식욕 부진, 구토, 또는 눈의 흰자위나 잇몸이 노랗게 변하는 증상(황달)을 보이면 심각한 간 반응을 의미할 수 있으므로 즉시 수의사에게 연락하십시오.
- 부작용: 특히 약물 복용 초기에는 반려동물이 졸려 하거나, 비틀거리거나, 움직임이 둔해질 수 있습니다. 이러한 증상은 몸이 약에 적응함에 따라 대개 호전됩니다.
- 보관 방법: 이 약물은 수분에 노출되면 빠르게 분해되므로, 방습제(건조제)가 포함된 원래의 용기에 보관하십시오.
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