시프로헵타딘

항히스타민제 / 세로토닌 길항제

시프로헵타딘은 강력한 항세로토닌 특성을 지닌 1세대 항히스타민제입니다. 수의학에서는 항히스타민 효과보다는 주로 허가 외(off-label) 작용을 목적으로 사용됩니다. **주요 수의학적 용도:** * **식욕 촉진제:** 역사적으로 고양이의 1차 식욕 촉진제로 사용되었으나, 현대 임상에서는 주로 미르타자핀(mirtazapine)이나 카프로모렐린(capromorelin)으로 대체되었습니다. 하지만 다른 약물을 사용할 수 없거나 금기인 경우 여전히 유용한 대안입니다. * **세로토닌 증후군 해독제:** 개와 고양이의 세로토닌 독성(예: 사람의 SSRI/SNRI 항우울제 또는 5-HTP 영양제 오식) 치료에 있어 **표준(gold standard)** 보조 치료제입니다. * **마류 의학:** 말의 광원성 헤드 쉐이킹(photic head shaking) 관리 및 뇌하수체 중엽 기능 장애(PPID / 말 쿠싱병)의 2차 또는 보조 요법으로 사용됩니다(단, PPID에는 페르골리드가 훨씬 우수합니다). * **고양이 천식 및 소양증:** 고양이의 호산구성 기도 염증이나 알레르기성 피부 질환에 간혹 사용되지만, 임상적 효능은 제한적입니다. > **임상 팁:** 시프로헵타딘은 간에서 대사되고 신장으로 배설되므로, 만성 신장 질환(CKD)이 있는 고양이에서는 용량 조절이 권장됩니다.

작용 기전: Cyproheptadine exhibits a multi-receptor antagonism profile: * **Serotonin (5-HT) Antagonism:** Competitively binds to **5-HT2A receptors** in the hypothalamus → blocks serotonin-induced satiety → stimulates appetite. In serotonin syndrome, blocking these receptors reverses life-threatening neuromuscular and autonomic hyperactivity. * **Histamine (H1) Antagonism:** Competes with histamine for **H1-receptors** on effector cells → prevents histamine-mediated capillary permeability, smooth muscle spasm, and pruritus. It does *not* prevent histamine release. * **Anticholinergic Activity:** Weakly antagonizes **muscarinic receptors** → leads to common side effects like dry mouth and urinary retention. * **Calcium Channel Blockade:** Exhibits mild calcium channel blocking properties, which may contribute to its efficacy in equine photic head shaking.

동물 종별 용량

Cats

As an appetite stimulant · 2-4 mg per cat · PO · once or twice daily
As an appetite stimulant · 1-4 mg/cat, or 0.35-1 mg/kg · PO · once or twice a day
As an appetite stimulant · 2 mg per cat · PO · q12h
As an appetite stimulant · 0.35-1 mg/kg · PO · q12h · May be dosed less frequently if inappetence is mild.
As an appetite stimulant in cats with renal insufficiency · 1 mg per cat · PO · q12h
As an antihistamine/antipruritic · 2 mg per cat · PO · q12h
As an antihistamine/antipruritic · 2 mg per cat or 1.1 mg/kg · PO · q12h
For feline asthma · 2 mg · PO · q12h · Particularly when cats are maxed out on dosages of corticosteroids and terbutaline. Therapeutic response may not be seen for 4-7 days, but CNS depression can occur in 24 hours.
For adjunctive treatment of serotonin syndrome · 2-4 mg (total dose) · PO · q4-6h · until signs have resolved · In cases where PO dosing not possible (severe vomiting), may crush tablets and mix with saline and give rectally.
Management of allergic disease / Appetite stimulation / Aortic thromboembolism · 0.1-0.5 mg/kg · PO · q8-12h

Horses

투여 경로

PORectal (off-label for severe vomiting)

금기

Hypersensitivity to cyproheptadine
Prostatic hypertrophy
Bladder neck obstruction
Severe cardiac failure
Angle-closure glaucoma
Pyeloduodenal obstruction
Urinary retention (relative)
Angle-closure glaucoma (relative)
Pyloroduodenal obstruction (relative)

이상반응

Sedation / CNS depression
Paradoxical hyperexcitability or agitation (especially in cats)
Anticholinergic effects (dry mucous membranes, urinary retention, tachycardia)
Hemolytic anemia in cats (rare)
Polyphagia (in dogs at higher doses)
Mild depression, anorexia, or lethargy (in horses)
Mild sedation
Polyphagia
Weight gain
Reduced seizure threshold

약물 상호작용

CNS Depressants (barbiturates, tranquilizers, etc.) · Additive CNS depression
SSRIs (sertraline, fluoxetine, paroxetine, etc.) · Cyproheptadine may decrease the efficacy of the SSRI due to its serotonin antagonist properties

모니터링

Clinical efficacy (e.g., body weight if used for anorexia, resolution of neurologic signs if used for serotonin syndrome)
Adverse effects (sedation, anticholinergic signs)
Serum BUN/Creatinine in cats with long-term use
Appetite and weight gain
Resolution of allergic signs
Neurological status (seizure activity)

과용량

There are no specific antidotes available for cyproheptadine overdose. **Clinical Signs of Toxicity:** * Extensions of pharmacological effects: profound CNS depression (though paradoxical CNS stimulation/seizures may occur). * Severe anticholinergic effects: extreme drying of mucous membranes, tachycardia, urinary retention, hyperthermia. * Hypotension. **Management:** * **Decontamination:** Standard gut emptying protocols (emesis/activated charcoal) if caught early and patient is stable. * **Supportive Care:** IV fluids for hypotension, temperature regulation. * **Specific Interventions:** Physostigmine may be considered for life-threatening central anticholinergic effects. Diazepam should be employed to treat seizures if they occur. > *Note: Horses receiving 2x the recommended dose apparently showed no untoward effects.*

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