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克立馬斯汀

Clemastine

Clemastine fumarate

抗組織胺藥 (H1受體拮抗劑)POIV狗貓

別名: Tavist Allergy · Dayhist-1 · Agasten · Aller-Eze · Antihist-1 · Clamist · Contac 12 Hour Allergy · Tavegil · Tavegyl · meclastine fumarate · mecloprodin fumarate · clemastini fumaras · HS-592 · Clemastine fumarate

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

0.05-0.1 mg/kg PO q12hPO· q12h
— 🐕

劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。

各物種劑量

🌎 NA — North America🌍 EU — Europe

狗

適應症劑量途徑頻次療程地區
Allergic conditions (Historical dosing - Efficacy doubtful)0.05-0.1 mg/kg PO q12hPOq12h—🌎 NA
  • Allergic conditions (Historical dosing - Efficacy doubtful): Oral bioavailability is <5%. An oral dose of 0.5 mg/kg only slightly inhibited wheal formation. Further dosing studies are needed before recommending therapeutic oral use.

貓

適應症劑量途徑頻次療程地區
Antihistamine0.68 mg per cat PO twice dailyPOq12h—🌎 NA
Antihistamine0.34-0.68 mg per cat PO q12hPOq12h—🌎 NA
Atopy0.15 mg/kg PO q 12 hrsPOq12h—🌎 NA
  • Atopy: Efficacy may be increased by combining with omega 3 fatty acids.

劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。

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概覽

克立馬斯汀是一種第一代乙醇胺類抗組織胺藥物，主要用於緩解過敏症狀。其特點為具有較強的抗膽鹼作用，但鎮靜副作用較一般第一代抗組織胺低。在狗與馬的口服生體可用率極低，因此口服給藥的臨床療效受到質疑。

作用機轉

Like other first-generation antihistamines, clemastine acts as a competitive antagonist (or inverse agonist) at H1-receptors.

  • ​Mechanism:​ Competes with histamine for H1-receptor sites on effector cells (smooth muscle, endothelium, CNS) → prevents histamine-induced bronchoconstriction, vasodilation, and increased capillary permeability.
  • ​Note:​ It does not block the release of histamine from mast cells or basophils, but rather antagonizes its downstream effects.
  • Exhibits significant ​anticholinergic (antimuscarinic)​ activity, which contributes to both its drying effects on mucous membranes and potential side effects.

安全性與警告

禁忌症

  • Known hypersensitivity to clemastine

不良反應

  • Sedation (dogs)
  • Paradoxical hyperactivity (dogs)
  • Anticholinergic effects: dry mucous membranes, tachycardia, urinary retention
  • Diarrhea (cats)
  • Fixed drug reaction (cats - rare)

注意事項

Use with caution in patients with prostatic hypertrophy, bladder neck obstruction, severe cardiac failure, angle-closure glaucoma, or pyeloduodenal obstruction. Antihistamines should be discontinued 3-7 days before intradermal skin testing to prevent false-negative wheal and flare responses. Use with caution in pregnant or nursing animals, especially with newborns, as the drug enters maternal milk.

藥物交互作用

CNS Depressant Medications (e.g., barbiturates, tranquilizers)

Additive CNS depression may occur.

Monoamine Oxidase Inhibitors (e.g., furazolidone, amitraz, selegiline)

May intensify the anticholinergic effects of clemastine.

CNS Depressants (e.g., phenobarbital, gabapentin, opioids)Moderate

Additive CNS depression and sedation

Anticholinergic drugsModerate

Additive anticholinergic effects (dry mouth, urinary retention)

監測

  • Clinical efficacy (reduction in pruritus, allergic signs)
  • Adverse effects (sedation, hyperactivity, anticholinergic signs)

藥物動力學

半衰期

馬5.4 hours (terminal)狗4 hours (IV)

吸收

Dogs: Very low oral bioavailability (3%). Horses: Poor oral bioavailability (3-4%). Humans: Variable bioavailability (20-70%).

分佈

Dogs: High volume of distribution (13.4 L/kg); 98% protein bound. Horses: Volume of distribution at steady-state is 3.8 L/kg. Distributes into milk.

代謝

Appears to be extensively metabolized (based on human data).

排除

Metabolites are eliminated in the urine. Clearance in dogs: 2.1 L/hr/kg. Clearance in horses: 0.79 L/hr/kg.

過量

There are no specific antidotes for clemastine overdose.

  • ​Management:​ Handle significant overdoses using standard gut-emptying protocols (emesis/gastric lavage) when appropriate, followed by supportive therapy.
  • ​Clinical Signs:​ Overdose signs are extensions of the drug's side effects, principally CNS depression (though CNS stimulation/seizures may occur), severe anticholinergic effects (severe drying of mucous membranes, tachycardia, urinary retention, hyperthermia), and possibly hypotension.
  • ​Specific Treatments:​ Physostigmine may be considered to treat serious CNS anticholinergic effects. Diazepam can be employed to treat seizures if necessary.

可用產品

劑型

  • Oral tablets
  • Oral syrup

人用標示

  • Clemastine Fumarate Oral Tablets: 1.34 mg (equivalent to 1 mg clemastine), 2.68 mg (equivalent to 2 mg clemastine)
  • Clemastine Oral Syrup: 0.67 mg/5 mL (equivalent to 0.5 mg clemastine)

各地核准狀態

European Union✓ 已核准EMA

Available as a human product used off-label in veterinary medicine.

United Kingdom✓ 已核准VMD

Classified as GSL (General Sales List) in the UK, meaning it can be sold without a prescription.

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Oral tablets and solution should be stored in tight, light-resistant containers at room temperature.

飼主須知

抗組織胺藥物可用於緩解過敏症狀，但無法治癒潛在的過敏疾病。可能會引起寵物嗜睡或異常興奮，也可能出現口乾。貓咪較常出現腹瀉的副作用。請務必遵照獸醫指示給藥。

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