マロピタント

Maropitant

(2S,3S)-2-benzhydryl-N-(5-tert-butyl-2methoxybenzyl) quinuclidin-3-amine citrate

ニューロキニン-1（NK1）受容体拮抗薬 / 制吐薬SCPOIV犬猫

別名: Cerenia · Prevomax · Vetemex · CJ-11,972 · Maropitant citrate

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

1 mg/kgSC· q24h· up to 5 consecutive days

体重— 🐕

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
Prevention of acute vomiting	1 mg/kg	SC	q24h	up to 5 consecutive days	🌎 NA
Prevention of acute vomiting	2 mg/kg	PO	q24h	up to 5 consecutive days	🌎 NA
Treatment of acute vomiting	1 mg/kg	SC	q24h	up to 5 consecutive days	🌎 NA
Prevention of vomiting due to motion sickness	8 mg/kg (minimum dose)	PO	q24h	up to 2 consecutive days	🌎 NA
Treatment and prevention of vomiting (including chemotherapy)	Dose not specified in text	PO/SC/IV	Not specified (duration of activity is 24 hours)	Up to 5 days	🌍 EU
Motion sickness	Dose not specified in text	PO/SC/IV	Not specified	Up to 2 days	🌍 EU

Prevention of acute vomiting: Given at least one hour prior to anticipated emetogenic event
Prevention of acute vomiting: Given at least two hours prior to anticipated emetogenic event
Treatment of acute vomiting: If a longer duration of therapy is needed, a 48 hour washout period is recommended due to accumulation of the drug.
Prevention of vomiting due to motion sickness: Given at least two hours prior to travel. If a longer duration of therapy is needed, a 72 hour washout period is recommended.
Treatment and prevention of vomiting (including chemotherapy): Repeat treatment at a lower dose may be adequate in some individuals. If longer periods of treatment are required, a 72-hour interval is recommended between courses.
Motion sickness: Not all preparations are specifically licensed for this purpose.

猫

適応	用量	経路	頻度	期間	地域
As an antiemetic	1 mg/kg	SC or PO	Unknown	—	🌎 NA
As an antiemetic	0.5-1 mg/kg	SC	once daily	up to 5 days	🌎 NA
Treatment of vomiting	Dose not specified in text	SC/IV	Not specified	Not specified	🌍 EU

As an antiemetic: Based on pharmacokinetic study
Treatment of vomiting: Treatment by injection is recommended for frequent vomiting. Very high doses may cause haemolysis.

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。

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概要

マロピタント（Cerenia®）は、犬および猫の急性嘔吐や乗り物酔いの予防・治療に広く使用される強力なニューロキニン-1（NK-1）受容体拮抗薬です。制吐作用に加えて、内臓鎮痛効果もあり、セボフルランなどの全身麻酔薬の必要量を減少させることが知られています。

作用機序

Maropitant exerts its effects by acting as a potent and selective antagonist at the neurokinin-1 (NK-1) receptors in the central nervous system (specifically the emetic center and chemoreceptor trigger zone).

Substance P Inhibition: It competitively binds to NK-1 receptors, blocking the binding of Substance P, a key neuropeptide/neurotransmitter involved in the emetic pathway.
Dual Action: Because Substance P is the final common pathway for vomiting, maropitant effectively suppresses emesis triggered by both central and peripheral stimuli.
Pain Modulation: Substance P is also heavily involved in nociception; blocking its receptors in the visceral pathways provides significant visceral pain relief.

安全性・警告

禁忌

Puppies less than 11 weeks old (due to risk of bone marrow hypoplasia)
Suspected gastrointestinal obstruction
Suspected gastrointestinal perforation
Use for longer than 48 hours without a definitive diagnosis

有害事象

Pre-travel vomiting (especially at higher motion sickness doses)
Hypersalivation
Pain or swelling at the subcutaneous injection site
Diarrhea
Anorexia
Localized injection site reactions (cats)
Transient pain reaction during injection (very common, especially in cats)
Haemolysis (at very high doses in cats)

注意事項

Use with caution in dogs with hepatic dysfunction as maropitant is hepatically metabolized. Use with caution in puppies less than 11 weeks old due to a higher frequency and severity of bone marrow hypoplasia. The safe use of maropitant has not been evaluated in breeding, pregnant, or lactating dogs; use only following a benefit/risk assessment.

医薬品相互作用

Highly protein-bound medications

Use with caution; maropitant is highly protein-bound (99.5%) and could theoretically compete for binding sites, though clinical significance is undetermined.

Calcium-channel antagonistsMajor

Maropitant has an affinity for calcium-channels; concurrent use should be avoided.

Highly protein-bound drugsModerate

Maropitant is highly bound to plasma proteins and may compete with other highly bound drugs, potentially altering free drug concentrations.

監視

Clinical efficacy (decreased episodes of vomiting)
Adverse effects (e.g., injection site pain, hypersalivation)
Resolution of vomiting
Liver function (in patients with pre-existing hepatic disease)
Signs of gastrointestinal obstruction or perforation

薬物動態

半減期

猫Approximately 15 hours犬8.84 hours (SC); 4.03 hours (PO)

吸収

Rapidly absorbed after PO & SC administration. Bioavailability in dogs: 24% (2 mg/kg PO), 37% (8 mg/kg PO), and 91% (1 mg/kg SC). Feeding status does not affect bioavailability. In cats, bioavailability is ~50% (PO) and 100+% (SC).

分布

Plasma protein binding is very high (99.5%).

代謝

Hepatic metabolism involves two cytochrome P450 enzymes: CYP2D15 (low capacity, high affinity) and CYP3A12 (high capacity, low affinity). The major pharmacologically active metabolite is CJ-18,518.

消失

Eliminated primarily by the liver. Urinary recovery of maropitant and its major metabolite is minimal (<1%).

過剰投与

Maropitant has a wide margin of safety.

Dogs: Tolerance has been confirmed at doses up to 3 times the recommended oral dose (8 mg/kg) for 3 times longer than the maximum duration.
High-Dose Toxicity (20 mg/kg/day in dogs): Can cause emesis, significant body weight loss (8-15%), ECG changes (slight increases in P-R interval, P wave duration, and QRS amplitude), slightly lower serum albumin, and increased adrenal weights.
Rodent Studies: Doses up to 30-100 mg/kg PO caused decreased activity, irregular/labored respiration, ataxia, and tremors.

製品

製剤

Oral tablets
10 mg/ml injectable solution
16 mg oral tablet
24 mg oral tablet
160 mg oral tablet

動物用医薬品

Maropitant Citrate Injectable Solution: 10 mg/mL in 20 mL multidose vials (Cerenia®)
Maropitant Citrate Oral Tablets: 16 mg, 24 mg, 60 mg, and 160 mg in blister packs (Cerenia®)
Cerenia 10 mg/ml solution for injection
Cerenia 16 mg, 24 mg, 60 mg, 160 mg tablets
Prevomax 10 mg/ml solution for injection
Vetemex 10 mg/ml solution for injection

規制ステータス

European Union✓ 承認済み処方箋医薬品EMA

🐕 Dogs🐈 Cats

POM-V classification

United Kingdom✓ 承認済み処方箋医薬品VMD