아티파메졸

알파-2 아드레날린 수용체 길항제

아티파메졸은 고도로 선택적이고 강력한 **알파-2 아드레날린 수용체 길항제**로, 수의학에서 주로 메데토미딘 및 덱스메데토미딘과 같은 알파-2 작용제의 역전제로 사용됩니다. 자일라진, 아미트라즈, 클로니딘과 같은 다른 알파-2 작용제를 역전시키기 위해 허가 외(off-label)로 사용될 수도 있습니다. **임상 요점:** * 아티파메졸은 알파-2:알파-1 선택성 비율이 8526:1로, 요힘빈이나 톨라졸린과 같은 구형 역전제보다 특이성이 훨씬 높습니다. 이러한 높은 특이성 덕분에 심혈관계 부작용이 적고 빠르고 깔끔한 각성을 유도합니다. * 진정 효과뿐만 아니라 **진통 효과도** 빠르게 역전시키므로 투여 전 환자의 통증을 평가해야 하며, 통증을 유발하는 시술을 받은 경우 대체 진통제(예: 마약성 진통제, NSAIDs)를 제공해야 합니다. * 아티파메졸의 반감기는 비교적 짧습니다(개에서 2-3시간). 지속 시간이 긴 알파-2 작용제(예: 아미트라즈)의 독성을 치료할 때, 원인 물질의 작용 시간이 역전제보다 길어 재진정을 유발할 수 있으므로 반복 투여가 필요할 수 있습니다.

작용 기전: Atipamezole competitively binds to central and peripheral **$\alpha_2$-adrenergic receptors**, displacing alpha-2 agonists. By blocking these receptors, it inhibits the negative feedback loop on presynaptic neurons $\rightarrow$ increases the release of **norepinephrine** into the synaptic cleft $\rightarrow$ leads to rapid arousal, reversal of sedation, increased heart rate, increased blood pressure, and loss of analgesia. It also antagonizes the diuretic action of alpha-2 agonists like xylazine.

동물 종별 용량

Goats

For reversal of alpha2-adrenergic agonists in caprine species · 0.02-0.1 mg/kg IV to effect · IV · Once
Small ruminants · 0.1-0.2 mg/kg slow IV or IM · IV/IM · Once · As a rule of thumb, if induction included ketamine or Telazol do not reverse alpha2 sooner than 30 and ideally 60 minutes after induction. This will allow enough of the ketamine or tiletamine to be metabolized.

Sheep

For reversal of alpha2-adrenergic agonists in ovine species · 0.02-0.1 mg/kg IV to effect · IV · Once
Small ruminants · 0.1-0.2 mg/kg slow IV or IM · IV/IM · Once · As a rule of thumb, if induction included ketamine or Telazol do not reverse alpha2 sooner than 30 and ideally 60 minutes after induction. This will allow enough of the ketamine or tiletamine to be metabolized.

Dogs

For reversal of medetomidine · Give IM an equal volume of Antisedan® and Domitor® is administered (mL per mL). The actual concentration of Antisedan® will be 5X that of Domitor®, as Antisedan® is 5 mg/mL versus Domitor®'s 1 mg/mL. · IM · Once
For reversal of medetomidine · As above, but may give IV as well as IM. If it has been at least 45 minutes since medetomidine was given, may give atipamezole at half the volume of medetomidine if administered IV. If after 10-15 minutes an IM dose of atipamezole has not seemed to reverse the effects of medetomidine, an additional dose of atipamezole at 1/2 the volume of the medetomidine dose may be given. · IV/IM · Once, may repeat
For reversal of dexmedetomidine · 0.2 mg/kg IM or IV · IM/IV · Once

투여 경로

IMIVSCIP

금기

Reptiles (Intravenous administration is contraindicated due to profound hypotension)

이상반응

Vomiting
Diarrhea
Hypersalivation
Tremors
Brief excitation or apprehensiveness
Aggression upon rapid waking
Profound hypotension (if given IV in reptiles)
Loss of analgesia

약물 상호작용

Alpha-1 adrenergic blockers (e.g., prazosin) · Atipamezole can partially block alpha-1 receptors and reduce the effects of prazosin.
Alpha-2 adrenergic agonists (e.g., detomidine, clonidine, brimonidine, xylazine, amitraz) · Atipamezole can reduce the effects (toxic or therapeutic) of these agents.
Medetomidine · Reverses sedative, analgesic, and cardiovascular effects (intended therapeutic interaction) · minor
Dexmedetomidine · Reverses sedative, analgesic, and cardiovascular effects (intended therapeutic interaction) · minor
Ketamine · If atipamezole is given less than 30 minutes after a medetomidine/ketamine combination in cats, it can cause severe CNS excitation during recovery. · major
Other alpha-2 antagonists · Additive antagonistic effects · moderate
Hypotensive agents · May exacerbate transient hypotension · minor

모니터링

Level of sedation and analgesia
Heart rate
Body temperature

과용량

Dogs receiving up to 10X the listed dosage apparently tolerated the drug without major effects. **Clinical signs of overdose:** * Panting * Excitement * Trembling * Vomiting * Soft or liquid feces * Vasodilatation of sclera * Muscle injury at the IM injection site Specific overdose therapy should generally not be necessary as effects are typically transient.

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