普瑞巴林
Pregabalin
(S)-3-(Aminomethyl)-5-methylhexanoic acid
別名: Lyrica · CI-1008 · PD-144723 · Alzain · Axalid · pregabalina · prégabaline · pregabalinum
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
經審核的 v13 劑量證據
結構化劑量計算證據Orthostatic tremor (extra-label)
須由已驗證獸醫確認
- q8-12h
NA
必須一併考量的臨床脈絡 (3)
- ■ This medicine may be given with or without food. If your animal vomits or acts sick after getting it on an empty stomach, try giving the medicine with food or a small treat to see if this helps. If vomiting continues, contact your veterinarian.
- ■ When it is used for seizure control, do not suddenly stop giving this medicine.
- Store capsules and oral solution at room temperature (25°C [77°F]); excursions permitted between 15°C to 30°C (59°F-86°F).
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。
概覽
普瑞巴林 (Pregabalin) 是一種 GABA 的結構類似物,與加巴噴丁 (Gabapentin) 相似,在獸醫學中主要用作抗癲癇藥和神經病理性疼痛鎮痛藥。
- 主要用途:作為難治性或複雜部分性癲癇發作的輔助治療,以及慢性/神經病理性疼痛的管理。
- 臨床要點:其效力被認為是加巴噴丁的 3-10 倍,因此可以使用較低的劑量體積,這對小型病患非常有利。
- 安全性:通常耐受性良好,最常見的劑量依賴性副作用為鎮靜和共濟失調。目前關於其在犬貓中的安全性和有效性資訊有限但正在增加。
作用機轉
Pregabalin is a structural analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). Despite its structure, it does not bind directly to GABA receptors.
- Binds with high affinity to the alpha-2-delta (α2δ) subunit of voltage-gated calcium channels (CaV) in the central nervous system.
- Binding → Decreased calcium influx at nerve terminals → Inhibition of the release of excitatory neurotransmitters (e.g., glutamate, substance P, norepinephrine).
- This reduction in excitatory neurotransmission produces its analgesic, anticonvulsant, and anxiolytic effects.
安全性與警告
禁忌症
- Hypersensitivity to pregabalin
- Pregnant animals (toxicity demonstrated in experimental studies)
- Abrupt discontinuation
不良反應
- Sedation
- Ataxia
- Somnolence
- Dizziness
- Difficulty with concentration/attention/memory
- Blurred vision
- Dry mouth
- Peripheral edema
- Constipation
- Weight gain
- Syncope
- Congestive heart failure
- Renal failure (reversible)
- Rhabdomyolysis
- Hypersensitivity reactions (angioedema, rash, blisters, wheezing)
- Decreased platelet production
- Increased creatine kinase
- Mild increases in hepatic enzyme activities (with prolonged therapy)
注意事項
Use with caution in patients with renal insufficiency; dosage adjustment should be considered (in humans, adjusted based on creatinine clearance). Use with caution in patients with heart failure. Abrupt discontinuation may lead to increased seizure frequency, diarrhea, headache, insomnia, or nausea. Weigh potential risks versus benefits in pregnant or nursing animals (FDA Category C in humans; very high dosages have caused skeletal malformations in rats and rabbits).
藥物交互作用
In humans, coadministration may increase risks of edema and hives.
May cause additive CNS depression.
In humans, cited as possibly reducing anticonvulsant effectiveness, though substantive evidence is weak.
監測
- Efficacy (seizure frequency, pain scores)
- Adverse effects (sedation, ataxia)
- Seizure frequency and severity
- Renal function (BUN, creatinine, USG)
- Hepatic enzyme activities (during prolonged therapy)
藥物動力學
半衰期
吸收
In humans, oral bioavailability is about 90%. Presence of food can delay the rate, but not the amount absorbed; can be administered regardless of feeding status.
分佈
Not bound to plasma proteins. Apparent volume of distribution is about 500 mL/kg.
代謝
Hepatic metabolism is negligible and it does not appear to affect hepatic enzymes.
排除
Almost exclusively cleared unchanged by renal routes. Renal clearance of 67-81 mL/minute in young, healthy human subjects.
過量
There is limited experience with overdoses of pregabalin in veterinary medicine. One human ingested 8 grams without significant effect. There is no specific antidote for overdose. Standard decontamination protocols can be employed if indicated. Contact an animal poison center for more information.
可用產品
劑型
- Capsules
- 75 mg capsule
- 100 mg capsule
- 150 mg capsule
- 200 mg capsule
- 225 mg capsule
- 300 mg capsule
- 20 mg/ml oral solution
人用標示
- Pregabalin Oral Capsules: 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, & 300 mg; Lyrica® (Pfizer); (Rx; C-V controlled substance)
- Pregabalin Oral Solution: 20 mg/mL; Lyrica® (Pfizer); (Rx; C-V controlled substance)
- Alzain capsules (various strengths)
- Axalid capsules (various strengths)
- Lyrica capsules (25 mg to 300 mg)
- Lyrica 20 mg/ml oral solution
各地核准狀態
POM CD SCHEDULE 3
POM CD SCHEDULE 3
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store capsules and oral solution at room temperature, 25°C (77°F); excursions permitted between 15-30°C (59-86°F). Use the oral solution within the first 45 days after opening the bottle.
飼主須知
- 預期反應:動物最常見的副作用是嗜睡(鎮靜)和有時走路不穩(共濟失調)。如果這些症狀嚴重或持續存在,請聯繫您的獸醫師。
- 重要警告:
請勿突然停藥! 未經獸醫師同意,突然停止使用普瑞巴林可能會導致副作用增加,並可能引發癲癇患畜的嚴重發作。請務必在獸醫師的指導下逐漸減量。
- 過敏反應:雖然罕見,但如果您發現皮疹、蕁麻疹、臉部腫脹、喘息或虛脫,請立即聯繫您的獸醫師。
- 給藥方式:可與食物一起或空腹給予。如果使用口服液,請在開瓶後 45 天丟棄未用完的部分。
VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠商最新仿單。
