클로라제페이트

벤조디아제핀계 (항불안제, 진정수면제, 항경련제)

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.

동물 종별 용량

Cats

Anxiolytic or for compulsive behaviors · 0.2-0.5 mg/kg PO q12-24h · PO · q12-24h
Alternative drug to phenobarbital for seizures · 3.75-7.5 mg (total dose per cat) PO once to twice daily · PO · q12-24h · Similar precautions are necessary as described for diazepam use in cats (risk of hepatic necrosis).

Dogs

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
Adjunctive medication in the treatment of seizures (in combination with phenobarbital) · 0.5-1 mg/kg PO q8h · PO · q8h · No advantage gained with using sustained release products. May affect phenobarb levels; monitor 2 and 4 weeks later.
Adjunctive medication in the treatment of seizures · 1-2 mg/kg PO q12h · PO · q12h
Adjunctive medication in the treatment of seizures · 2-4 mg/kg PO twice daily, some dogs may require three times daily · PO · q8-12h
Third-line agent for seizures · 1-2 mg/kg PO q8-12h · PO · q8-12h
Management of cluster seizures · 0.5-2 mg/kg two to three times daily · PO · q8-12h · 48-96 hours · 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 · 11.25-22.5 mg per dog PO once to twice daily · PO · q12-24h · Recommends the sustained-delivery product (Tranxene-SD).

투여 경로

금기

Hypersensitivity to benzodiazepines
Significant liver disease/dysfunction
Acute narrow angle glaucoma
Fear-induced aggression (relative contraindication; may disinhibit bite inhibition)

이상반응

Sedation (most common)
Ataxia
Physical dependence (with chronic use)
Acute hepatic necrosis (idiosyncratic in cats)
Paradoxical excitation or disinhibition of aggression

약물 상호작용

Azole Antifungals (itraconazole, ketoconazole) · May increase serum levels of benzodiazepines by inhibiting their metabolism.
Cimetidine · May decrease the metabolism of benzodiazepines, leading to prolonged effects.
CNS Depressants (barbiturates, narcotics, anesthetics) · Additive CNS depression; may cause profound sedation or respiratory depression.
Erythromycin · May decrease the metabolism of benzodiazepines.
Phenobarbital · Complex interaction: Clorazepate may initially increase phenobarbital serum levels. Over time, clorazepate levels may decrease, leading to decreased phenobarbital levels. Requires close monitoring.
Phenytoin · May decrease clorazepate concentrations.
Rifampin · 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)

과용량

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.

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