セルトラリン
Sertraline
Sertraline hydrochloride
別名: Zoloft · Altruline · Anilar · Aremis · Atenix · Besitran · Bicromil · Gladem · Insertec · Irradial · Lustral · Novativ · Sealdin · Serad · Sercerin · Serlain · Serta · Tatig · Tolrest · Tresleen · Sertraline HCl · CP-51974-01 · Sertralinum
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Treatment of compulsive disorders | 2-4 mg/kg PO once daily or divided twice daily | PO | q24h or q12h | — | 🌎 NA |
| Behavioral diagnoses | 1-2 mg/kg PO q24h (once daily) | PO | q24h | allow 6-8 weeks for initial trial | 🌎 NA |
| Behavioral diagnoses | 1-3 mg/kg PO once daily | PO | q24h | 3-6 months | 🌎 NA |
| Treatment of behavioral diagnoses | 0.25-0.5 mg/kg PO q24h (once a day) | PO | q24h | Minimum 4-6 months | 🌎 NA |
| Compulsive disorder, anxiety | 1-4 mg/kg PO q24h (once daily) | PO | q24h | — | 🌎 NA |
| Behavioral diagnoses | 0.5-4 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Generalized anxiety disorder | 0.5-4 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Anxiety-related behaviours (including compulsive type behaviour such as acral lick) | 1-3 mg/kg | PO | q24h | Long-term | 🌍 EU |
- Behavioral diagnoses: Plan is to use the drug for a limited time during which behavioral modification is employed. Wean off over 2-4 weeks by halving the dose weekly.
- Treatment of behavioral diagnoses: Treat for 3-5 weeks minimum to assess effects; treat until 'well' (minimum another 1-2 months), then treat another 1-2 months minimum. Wean off over 3-5 weeks or longer.
- Anxiety-related behaviours (including compulsive type behaviour such as acral lick): Higher doses are described in the literature.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Treatment of compulsive disorders | 0.5 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Urine marking (spraying), aggression, anxiety-including anxiogenic house soiling, phobias, fears | 0.5-1 mg/kg PO q24h (once daily) | PO | q24h | — | 🌎 NA |
| Treatment of behavioral diagnoses | 1 mg/kg PO q24h (once a day) | PO | q24h | Minimum 4-6 months | 🌎 NA |
| Treatment of fear, affective or dominance aggression | 0.5-1 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Generalized anxiety disorder | 0.5-1.5 mg/kg PO q24h | PO | q24h | — | 🌎 NA |
| Treatment of compulsive disorder, anxiety | 0.5-1 mg/kg PO q24h (once daily) | PO | q24h | — | 🌎 NA |
| Behavioral diagnoses | 0.25-1.3 mg/kg PO q24h | PO | q24h | — | 🌎 NA |
| Increase inhibitory control (e.g., play-related aggressive behaviour) | 0.5-1.5 mg/kg | PO | q24h | Long-term | 🌍 EU |
- Treatment of behavioral diagnoses: Treat for 3-5 weeks minimum to assess effects; treat until 'well' (minimum another 1-2 months), then treat another 1-2 months minimum. Wean off over 3-5 weeks or longer.
- Increase inhibitory control (e.g., play-related aggressive behaviour): Suggested use, but there are no good empirical studies published to support this.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
セルトラリンは広く使用されているヒト用抗うつ薬であり、獣医療においては犬や猫の様々な行動関連疾患の管理に適応外使用（オフラベル使用）されています。
主な臨床応用：
- 犬： 攻撃行動、全般性不安、および強迫性障害（例：肢端舐性皮膚炎、尾追い行動）。
- 猫： 尿マーキング（スプレー行動）、情動性または優位性攻撃行動、不安による不適切な排泄、恐怖症、および強迫性障害。
臨床上のポイント：
他のSSRIと同様に、セルトラリンが十分な臨床効果を発揮するまでには長期間（通常4〜8週間）の治療が必要です。この遅れは、神経受容体のダウンレギュレーションに時間を要するためです。ジェネリック医薬品が利用可能であるため比較的安価であり、長期的な行動管理において魅力的な選択肢となります。
作用機序
Sertraline is a highly selective inhibitor of the presynaptic reuptake of serotonin (5-hydroxytryptamine or 5-HT) in the central nervous system.
- Mechanism: Blocks the serotonin transporter (SERT) → prevents the reuptake of serotonin into the presynaptic neuron → increases the concentration of serotonin in the synaptic cleft → prolongs stimulation of postsynaptic 5-HT receptors.
- Receptor Specificity: Sertraline has minimal to no effect on the reuptake of dopamine or norepinephrine, and lacks significant affinity for adrenergic, cholinergic, or histaminergic receptors, which minimizes the side effects typically seen with tricyclic antidepressants (TCAs).
- Delayed Onset: The initial increase in synaptic serotonin stimulates presynaptic 5-HT1A autoreceptors, which temporarily decreases serotonin release. Over several weeks, these autoreceptors down-regulate, allowing for enhanced serotonin release and the onset of full therapeutic effects.
安全性・警告
禁忌
- Known hypersensitivity to sertraline or other SSRIs
- Concurrent use of Monoamine Oxidase Inhibitors (MAOIs) such as selegiline or amitraz
- Concurrent use of cisapride
- History of seizures or epilepsy
- Concurrent use of MAOIs (e.g., selegiline)
有害事象
- Anorexia (common in dogs, usually transient)
- Lethargy or sedation
- Gastrointestinal effects (vomiting, diarrhea)
- Anxiety or irritability
- Insomnia or hyperactivity
- Panting (dogs)
- Changes in elimination patterns (cats)
- Paradoxical aggressive behavior in previously non-aggressive animals
- Decreased appetite
- Trembling
- Restlessness
- Gastrointestinal disturbance
- Paradoxical increase in anxiety
- Potential increase in aggression
注意事項
Hepatic Impairment: Use with caution in patients with severe hepatic disease; dosages may need to be decreased or the dosing interval increased due to extensive hepatic metabolism. Geriatric Patients: Use with caution; dose adjustments may be necessary. Pregnancy: FDA Category C in humans. Animal studies (rats/rabbits) showed delayed ossification and decreased pup survival. Use only if benefits outweigh risks. Weaning: Avoid abrupt discontinuation; taper the dose gradually over several weeks to prevent withdrawal signs.
医薬品相互作用
Increased risk for serotonin syndrome
May increase sertraline levels
May decrease or reverse the effects of SSRIs
Sertraline may decrease diazepam clearance
Increased risk for serotonin syndrome
High risk for serotonin syndrome; use contraindicated. A 5-week washout period is required after discontinuing sertraline before starting an MAOI, and a 2-week washout if discontinuing an MAOI before starting sertraline.
Serotonin syndrome-like adverse effects possible
SSRIs can inhibit the metabolism of tramadol to active metabolites, decreasing efficacy and increasing the risk of toxicity (serotonin syndrome, seizures)
Sertraline may increase TCA blood levels and increase the risk for serotonin syndrome
Sertraline may increase the risk for bleeding
High risk of fatal serotonin syndrome. Do not use sertraline within 2 weeks of an MAOI, and do not use an MAOI within 6 weeks of stopping sertraline.
Sertraline antagonizes the effects of anticonvulsants and lowers the seizure threshold.
May lower the seizure threshold when used concurrently.
Increased risk of bleeding in the case of tissue trauma.
Increased risk of bleeding.
Increased risk of serotonin syndrome.
Increased risk of serotonin syndrome. Use only in exceptional cases with careful monitoring.
監視
- Efficacy (resolution or improvement of behavioral signs)
- Adverse effects, particularly changes in appetite and body weight
- Baseline liver function tests (consider re-testing as needed)
- Baseline ECG (consider re-testing as needed)
- Behavioral response (efficacy and paradoxical aggression/anxiety)
- Signs of serotonin syndrome (tremors, hyperthermia, agitation)
- Seizure activity
薬物動態
半減期
吸収
In humans, peak levels occur 30-45 minutes after oral dosing.
分布
In dogs, the volume of distribution is 25 L/kg. It is highly protein-bound (97% in dogs, 98% in humans).
代謝
Undergoes high first-pass metabolism in the liver. Primarily metabolized to N-desmethylsertraline, which is an active metabolite.
消失
In dogs, clearance is greater than 35 mL/min/kg, and bile is the major route of excretion.
過剰投与
Toxicity Profile: Most exposures in dogs below 20 mg/kg are not considered serious. However, massive overdoses can be life-threatening.
Clinical Signs of Overdose:
- Mild to Moderate: Vomiting, diarrhea, hypersalivation (especially in cats), lethargy, tachycardia, somnolence, and vocalization.
- Severe (Serotonin Syndrome): Muscle tremors, rigidity, agitation, hyperthermia, vocalization, hypertension or hypotension, tachycardia, seizures, coma, and potentially death.
Management: Handle aggressively with supportive and symptomatic treatment. Contact an animal poison control center (e.g., ASPCA APCC) for specific guidance.
製品
製剤
- Tablets
- Oral Solution Concentrate
- 50 mg oral tablet
- 100 mg oral tablet
ヒト用医薬品
- Sertraline HCl Tablets: 25 mg, 50 mg & 100 mg (as base); Zoloft® (Pfizer); generic
- Sertraline HCl Oral Solution Concentrate: 20 mg/mL in 60 mL; Zoloft® (Pfizer); generic
- Lustral 50 mg tablets
- Lustral 100 mg tablets
規制ステータス
Prescription Only Medicine (POM). Used under the cascade as no veterinary formulation is currently authorized.
Prescription Only Medicine (POM). Used under the cascade.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Store commercially available tablets and oral solution at controlled room temperature (25°C; 77°F); excursions permitted to 15-30°C (59-86°F). The oral solution must be diluted only in water, orange juice, ginger ale, lemonade, or lemon/lime soda, and used immediately after dilution.
飼主向け情報
期待される効果：
- 忍耐が鍵です： この薬はすぐには効果が現れません。ペットの行動に顕著な改善が見られるまでには、通常4〜8週間の毎日の継続的な投薬が必要です。
- 継続の重要性： 薬の効果を正確に判断するためには、数ヶ月間薬を使用し続ける必要があります。
重要なガイドライン：
- 急に服用を中止しないでください： 獣医師の指示がない限り、絶対に突然投薬を中止しないでください。離脱症状を引き起こす可能性があります。薬を中止する必要がある場合、獣医師が徐々に減量するスケジュールを指示します。
- 食欲の変化： 投薬開始時に食欲が低下することはよくあります（特に犬）。これは通常一時的なものです。手から直接食べさせたり、食事をより美味しく工夫したりしてみてください。ペットが全く食べなくなった場合は、獣医師に連絡してください。
- 行動の観察： この薬は脳内の化学物質に変化をもたらすため、不安の増強、落ち着きのなさ、予期せぬ攻撃性などの異常な行動がないか観察してください。重大な異常が見られた場合は、すぐに獣医師に報告してください。
- 液剤について： 経口液剤を使用する場合は、ペットに与える前に希釈する必要があります。水、オレンジジュース、ジンジャーエール、レモネード、またはレモン/ライムソーダとのみ混ぜ合わせ、混ぜた後はすぐに与えてください。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。