馬羅皮坦
Maropitant
(2S,3S)-2-benzhydryl-N-(5-tert-butyl-2methoxybenzyl) quinuclidin-3-amine citrate
別名: Cerenia · Prevomax · Vetemex · CJ-11,972 · Maropitant citrate
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| 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.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| 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.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
馬羅皮坦（Cerenia®）是一種強效的神經激肽-1 (NK-1) 受體拮抗劑，廣泛用於預防和治療犬貓的急性嘔吐及暈車。除了止吐作用外，它還具有內臟鎮痛的特性，並能降低全身麻醉劑（如七氟醚）的需求量。
作用機制
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.
安全性與警告
禁忌症
- 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
不良反應
- 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.
藥物相互作用
Use with caution; maropitant is highly protein-bound (99.5%) and could theoretically compete for binding sites, though clinical significance is undetermined.
Maropitant has an affinity for calcium-channels; concurrent use should be avoided.
Maropitant is highly bound to plasma proteins and may compete with other highly bound drugs, potentially altering free drug concentrations.
監測
- 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
藥物動力學
半衰期
吸收
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).
分佈
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.
排除
Eliminated primarily by the liver. Urinary recovery of maropitant and its major metabolite is minimal (<1%).
過量
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.
可用產品
劑型
- Oral tablets
- 10 mg/ml injectable solution
- 16 mg oral tablet
- 24 mg oral tablet
- 160 mg oral tablet
獸醫用
- 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
各地核准狀態
POM-V classification
POM-V classification
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Injectable solution: Store at controlled room temperature 20-25°C (68-77°F). Must be used within 28 days of first vial puncture. Tablets: Packaged in foil to protect from moisture uptake; keep in blister packs until use. Halved tablets show no loss of potency for 48 hours.
飼主須知
- 給藥技巧：請勿將藥錠緊緊包裹或埋在食物/零食中，這可能會延遲藥錠的溶解與吸收。
- 飲食建議：避免在給藥前讓寵物長時間空腹。
- 預防暈車：在給予暈車藥前一小時，餵食少量餐點或零食，可減少給藥後引發的行前嘔吐。
- 注射部位：皮下注射可能會引起短暫的疼痛或腫脹。
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