부프레노르핀

오피오이드 부분 작용제

부프레노르핀은 수의학에서 널리 사용되는 **오피오이드 부분 작용제**입니다. 주로 소동물의 경도 및 중등도 급성 통증 관리에 사용되며, 알파-2 작용제 및 해리성 마취제와 함께 단기 보정용 '칵테일' 요법에 자주 포함됩니다. * **임상적 특징**: 부프레노르핀은 표준 용량에서 "천장 효과(ceiling effect)"를 나타냅니다. 즉, 특정 지점 이상으로 용량을 늘려도 추가적인 진통 효과를 얻지 못할 수 있으며 이론적으로 진통 효능이 감소할 수 있습니다. * **고양이에서의 장점**: 고양이의 구강 pH는 비교적 알칼리성이어서 부프레노르핀이 높은 지용성을 띠게 되며, 이는 우수한 **구강 점막(OTM) / 볼 점막 흡수**를 가능하게 합니다. 고양이에서 볼 점막 투여는 근육 주사와 거의 동일한 생체이용률을 가지므로 가정 내 수술 후 통증 관리에 매우 실용적인 투여 경로입니다. * **지속 시간**: 순수 뮤-작용제(펜타닐 또는 메타돈 등)에 비해 작용 발현 시간은 길지만, 진통 지속 시간은 훨씬 깁니다(일반적으로 6~8시간, 최대 12시간). * **규제**: 이 약물은 마약류(향정신성의약품)로 분류됩니다.

작용 기전: Buprenorphine exerts its analgesic effects by acting as a **partial agonist at the mu (μ) opioid receptor** and an **antagonist at the kappa (κ) opioid receptor** in the central nervous system. * **High Affinity, Slow Dissociation**: It binds to the μ-receptor with an affinity approximately 30 times greater than morphine. This tight binding → prolonged duration of action. * **Receptor Competition**: Because of its high affinity, it can displace pure μ-agonists from the receptor, potentially antagonizing their analgesic effects while reversing their sedative and respiratory depressant effects. * **Naloxone Resistance**: Its slow dissociation from the receptor makes it notoriously difficult to fully reverse with standard doses of the opioid antagonist **naloxone**; high doses of naloxone or the use of doxapram may be required in cases of severe respiratory depression.

동물 종별 용량

Dogs

Analgesia · 0.005-0.02 mg/kg IM, IV or SC q6-12h · IM, IV, SC · q6-12h
Analgesia · 2-4 micrograms/kg/hour · IV · continuous infusion
Analgesia · 0.005-0.03 mg/kg IV, IM, SC, epidural · IV, IM, SC, epidural
Analgesia · 0.006-0.02 mg/kg IV, IM, SQ · IV, IM, SQ · 6-12 hours · Relatively effective analgesic, but may be difficult to reverse with naloxone if untoward effects are seen.
Analgesia · 0.02 mg/kg · IV, IM, SC · q6h · SC route is listed in historical dosing but text notes it is not recommended due to potentially lower efficacy compared to IM/IV.

Ferrets

Analgesia · 0.01-0.05 mg/kg SC or IM 2-3 times daily · SC, IM · 2-3 times daily

Cats

Analgesia · 0.01-0.03 mg/kg IM, IV, Buccal · IM, IV, Buccal · up to 6 hours · Buccal use is well accepted by cats.
Analgesia · 0.01-0.03 mg/kg PO transmucosally (squirted directly into the mouth) q8h · PO transmucosal · q8h
Analgesia · 0.01-0.03 mg/kg IM, IV, SC q6-8h; 0.01-0.03 mg/kg PO q6-12h · IM, IV, SC, PO · q6-12h
Analgesia · 1-3 micrograms/kg/hour · IV · continuous infusion

투여 경로

IVIMSCBuccal (Oral Transmucosal)EpiduralSublingual

금기

Known hypersensitivity to buprenorphine

이상반응

Respiratory depression (rare but significant)
Sedation
Urine retention or difficulty voiding (particularly with high IV or epidural doses)
Excitement (horses)
Diminished gut sounds (horses)
Vomiting (rare in cats)

약물 상호작용

Local Anesthetics (mepivacaine, bupivacaine) · May be potentiated by concomitant use of buprenorphine
Anticonvulsants (phenobarbital, phenytoin) · May decrease plasma buprenorphine levels
Benzodiazepines · Case reports of humans developing respiratory/cardiovascular/CNS depression; use with caution
CNS Depressants (anesthetics, antihistamines, phenothiazines, barbiturates, alcohol) · May cause increased CNS or respiratory depression when used with buprenorphine
Erythromycin · Can increase plasma buprenorphine levels
Fentanyl (and other pure opiate agonists) · Buprenorphine may potentially antagonize some analgesic effects, but may also reverse some sedative and respiratory depressant effects
Halothane · Potentially can increase buprenorphine effects
Azole Antifungals (ketoconazole, itraconazole, fluconazole) · Can increase plasma buprenorphine levels
Monoamine Oxidase Inhibitors (selegiline, amitraz) · Possible additive effects or increased CNS depression
Naloxone · May reduce analgesia associated with high dose buprenorphine
Pancuronium · If used with buprenorphine may cause increased conjunctival changes
Rifampin · Potentially decrease plasma buprenorphine concentrations

모니터링

Analgesic efficacy
Respiratory status
Cardiac status

과용량

Buprenorphine has a very high index of safety (ratio of lethal dose to effective dose is at least 1000:1 in rodents). Life-threatening acute overdoses are rare in veterinary medicine, but clinical signs are common. * **Clinical Signs (Dogs)**: Vocalization, ataxia, hypersalivation, hypothermia, and lethargy. * **Treatment**: Supportive care. In cases of acute overdose causing severe respiratory or cardiac effects, **naloxone** and **doxapram** are suggested. > **Note**: Due to buprenorphine's extremely high affinity for the mu-receptor, standard doses of naloxone may be ineffective; very high doses of naloxone may be required to reverse respiratory depression.

VetSheet 약물 레퍼런스는 면허 수의 전문가를 위한 임상 의사결정 보조 도구이며, 전문적 판단이나 제조사의 최신 라벨을 대신하지 않습니다.