加巴噴丁
Gabapentin
1-(aminomethyl)cyclohexaneacetic acid
別名: Neurontin · Aclonium · Equipax · Gantin · Gabarone · Neurostil · Progresse · CI-945 · GOE-3450 · Gabapentinum
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 |
|---|---|---|---|---|---|
| Ancillary therapy of refractory seizures | 10-20 mg/kg | PO | q6-8h | — | 🌎 NA |
| Ancillary therapy of refractory seizures | 10-30 mg/kg | PO | q8-12h | — | 🌎 NA |
| Ancillary therapy of refractory seizures | 25-60 mg/kg/day divided q6-8h | PO | q6-8h | — | 🌎 NA |
| Ancillary therapy of refractory seizures | 10 mg/kg | PO | q8h | 3 months | 🌎 NA |
| Ancillary therapy of refractory seizures | 10-30 mg/kg | PO | q8h | — | 🌎 NA |
| Adjunctive treatment of chronic or cancer pain | 3 mg/kg | PO | once a day | — | 🌎 NA |
| Analgesic | 1.25-10 mg/kg | PO | q24h | — | 🌎 NA |
| Analgesic | 5-10 mg/kg | PO | 2-3 times a day | — | 🌎 NA |
| Analgesic | 2.5-10 mg/kg (up to 15 mg/kg) | PO | 1-3 times a day | — | 🌎 NA |
| Adjunctive seizure therapy / Chronic pain | 10-20 mg/kg | PO | q6-8h | — | 🌍 EU |
- Ancillary therapy of refractory seizures: Author notes gabapentin is the least effective of the newer antiepileptic drugs, particularly in dogs.
- Ancillary therapy of refractory seizures: Author initially uses 10 mg/kg PO q8h.
- Ancillary therapy of refractory seizures: For uncontrolled seizures when phenobarbital and potassium bromide levels were therapeutic, or sub-therapeutic but had unacceptable side effects.
- Analgesic: Most VIN consultants recommend this dose.
- Adjunctive seizure therapy / Chronic pain: starting dose; incremental dose increases are recommended
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Ancillary therapy of refractory seizures | 5-10 mg/kg | PO | q8-12h | — | 🌎 NA |
| Ancillary therapy of refractory seizures | 5 mg/kg | PO | three times daily | — | 🌎 NA |
| Ancillary therapy of refractory seizures | 10-30 mg/kg | PO | q8-12h | — | 🌎 NA |
| Analgesic | 1.25-10 mg/kg | PO | q24h | — | 🌎 NA |
| Adjunctive treatment of chronic or cancer pain | 3 mg/kg | PO | once a day | — | 🌎 NA |
| Adjunctive analgesia associated with neuropathic pain | 2.5-5 mg/kg | PO | q12h | — | 🌎 NA |
| Analgesic | 5-10 mg/kg | PO | 2-3 times a day | — | 🌎 NA |
| Analgesic | 50 mg (total dose) per cat | PO | 1-3 times a day | — | 🌎 NA |
| Adjunctive seizure therapy / Chronic pain | 5-10 mg/kg | PO | q8-12h | — | 🌍 EU |
- Adjunctive analgesia associated with neuropathic pain: Author starts at 5 mg/kg and increases (up to 10 mg/kg) if no effect seen in two hours. Wean off slowly. Reduce in renal insufficiency.
- Analgesic: Most VIN consultants recommend this dose.
- Adjunctive seizure therapy / Chronic pain: starting dose; incremental dose increases are recommended
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
加巴噴丁是γ-氨基丁酸（GABA）的結構類似物，在獸醫學中廣泛用於其神經病理性鎮痛和抗癲癇特性。
- 鎮痛作用：對慢性、適應不良和神經病理性疼痛（例如骨關節炎、椎間盤疾病、癌症疼痛）非常有效。通常作為多模式鎮痛方案的一部分。
- 癲癇管理：用作難治性或複雜部分性癲癇發作的輔助抗癲癇藥物（AED），但作為單一藥物的療效有限。
- 行為/抗焦慮：越來越多地在貓和狗中標示外使用，以減少就診或壓力事件前的恐懼、焦慮和壓力（FAS）。
作用機轉
Despite its name, gabapentin does not bind to GABA receptors, nor does it affect GABA synthesis or uptake.
- Binds selectively to the α2-δ (alpha-2-delta) subunit of voltage-gated calcium channels (CaV) in the central nervous system.
- Inhibition of Calcium Influx → Decreased presynaptic calcium currents.
- Reduced Neurotransmitter Release → Suppresses the release of excitatory neurotransmitters including glutamate, substance P, and norepinephrine in the dorsal horn of the spinal cord.
- This dampens neuronal excitability, effectively preventing allodynia (pain from non-noxious stimuli) and hyperalgesia (exaggerated pain response).
安全性與警告
禁忌症
- Hypersensitivity to gabapentin
- Use of xylitol-containing human oral solutions in dogs
- Oral solutions containing xylitol (highly toxic to dogs)
不良反應
- Ataxia
- Dizziness (humans)
- Somnolence
- Peripheral edema (humans)
- Withdrawal-precipitated seizures (if abruptly discontinued)
- Increased rate of pancreatic adenocarcinoma (noted in male rats)
- Mild sedation
- False-positive urinary protein tests (reported in humans)
- Hepatic toxicity (rare, reported in humans)
注意事項
WARNING: Commercially available human oral solutions (e.g., Neurontin) often contain xylitol (up to 300 mg/mL), which is highly toxic to dogs, causing severe hypoglycemia and hepatotoxicity. Avoid use in dogs.
- Renal Insufficiency: Eliminated primarily via the kidneys. Use with caution and consider dosage adjustments in patients with renal impairment. Dogs partially metabolize the drug (30-40%), so mild to moderate renal dysfunction may not require adjustment.
- Withdrawal: Abrupt discontinuation can lead to withdrawal-precipitated seizures. Taper the dose gradually when discontinuing, especially in epileptic patients.
- Laboratory Alterations: May cause false-positive urinary protein readings on Ames N-Multistix SG dipstick tests. Use a sulfosalicylic acid precipitation test instead.
藥物交互作用
Oral antacids given concurrently may decrease oral bioavailability of gabapentin by 20%; separate doses by at least 2 hours.
Co-administration may increase gabapentin AUC and efficacy/adverse effects. Gabapentin may reduce hydrocodone AUC, potentially reducing its effectiveness.
May increase gabapentin levels.
Reduced absorption of gabapentin from the GI tract. Administer gabapentin at least 2 hours after antacids.
Reduced renal clearance of gabapentin (not considered clinically important).
監測
- Clinical efficacy (reduction in pain scores or seizure frequency)
- Adverse effects (sedation, ataxia)
- Renal function (in patients with pre-existing disease)
- Clinical response (pain scores, seizure frequency)
- Renal and hepatic function in compromised patients
藥物動力學
半衰期
吸收
Dogs: Oral bioavailability ~80% at 50 mg/kg. Peak plasma levels at 2 hours. Cats: Bioavailability ~90% (high interpatient variation 50-120%). Peak levels at 100 minutes. Horses: Rapidly absorbed, peak levels within 2 hours.
分佈
Cats: Volume of distribution is relatively low (Vdss 0.65 L/kg). Humans: Minimally bound to plasma proteins; CSF levels are ~20% of plasma levels.
代謝
Dogs: Partially metabolized (30-40%) to N-methyl-gabapentin. Humans: Not significantly metabolized.
排除
Primarily via renal routes (excreted unchanged in urine in humans). Cats: Clearance ~3 mL/min/kg.
過量
In humans, massive overdoses (up to 49 grams) have been reported without fatality.
- Clinical Signs: Ataxia, lethargy, somnolence, vomiting, and diarrhea.
- Xylitol Toxicity Risk: The human oral solution contains 300 mg/mL of xylitol. Doses as low as 0.33 mL/kg of this solution can cause severe hypoglycemia or hepatotoxicity in dogs.
- Treatment: Primarily supportive. General decontamination (emesis, activated charcoal, cathartics) if caught early. The drug can be removed via hemodialysis. If xylitol toxicity is suspected secondary to the human liquid formulation, aggressive treatment for hypoglycemia and liver protection is required; contact an animal poison control center.
可用產品
劑型
- Capsules
- Tablets
- Compounded Oral Suspension
- 100 mg capsule
- 300 mg capsule
- 400 mg capsule
- 600 mg film-coated tablet
- 800 mg film-coated tablet
- 50 mg/ml oral solution
人用標示
- Gabapentin Oral Capsules & Tablets: 100 mg, 300 mg, 400 mg, 600 mg, 800 mg (Neurontin, generic)
- Gabapentin Oral Solution: 250 mg/5mL (50 mg/mL) (Neurontin) - Contains xylitol! Use with caution in dogs.
- Neurontin 100 mg, 300 mg, 400 mg capsules
- Neurontin 600 mg, 800 mg film-coated tablets
- Neurontin 50 mg/ml oral solution
各地核准狀態
POM CD Schedule 3
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Capsules and tablets: Store at room temperature (25°C / 77°F); excursions permitted to 15-30°C. Oral liquid: Store in the refrigerator at 2-8°C (36-46°F). Compounded suspensions are most stable at pH 5.5-6.5.
飼主須知
什麼是加巴噴丁？ 加巴噴丁是一種用於治療慢性神經痛的藥物，較少用於幫助控制癲癇發作。它也常被用來減少寵物在看獸醫等壓力事件前的恐懼和焦慮。
如何給藥
- 可與食物一起或空腹服用。
- 絕對不要將人類用的液體製劑（Neurontin）給您的狗服用（除非由獸醫藥局特別調配），因為它含有木糖醇（xylitol），這是一種對狗具有劇毒甚至致命的人工甜味劑。
需要注意什麼
- 最常見的副作用是嗜睡和走路不穩（共濟失調）。這些副作用通常很輕微，並且隨著您的寵物適應藥物後會有所改善。
- 如果您的寵物顯得過度昏睡或極度不協調，請聯繫您的獸醫。
重要提示
- 如果您的寵物因癲癇發作而服用加巴噴丁，請勿突然停藥，因為這可能會引發嚴重的戒斷性癲癇發作。在更改劑量之前，請務必諮詢您的獸醫。
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