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ブプレノルフィン

Buprenorphine

Buprenorphine hydrochloride

オピオイド部分アゴニストIVIMSCBuccal (Oral Transmucosal)EpiduralSublingual犬猫小型哺乳類フェレット馬

別名: Buprenex · Subutex · Suboxone · Butrans · Temgesic · Simbadol · Zorbium · Bupaq · Buprecare · Buprenodale · Buprevet · Vetergesic · Buprenorphine HCl · buprenorphini hydrochloridum · CL-112302 · NIH-8805 · UM-952 · Buprenorphinum

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

監査済み v13 用量エビデンス

構造化された用量計算エビデンス

Analgesia during gastrointestinal stasis

0.01–0.05 mg/kgSCIMIV

認証済み獣医師の確認が必要

  • q8–12h
必ず考慮する臨床コンテキスト (1)
  • Exclude emergent diagnoses (obstruction, enterotoxemia)
規制薬認証済み獣医師の確認が必要textbookプロトコル 2021監査 dose-audit-v13

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。

診察中ですか？VetSheet の AI が薬剤・用量・投与期間を構造化された診察記録に直接記入します。VetSheet の仕組みを見る

概要

ブプレノルフィンは、獣医療において広く使用されている​オピオイド部分アゴニスト​です。主に小動物の軽度から中等度の急性疼痛の管理に利用され、アルファ2アゴニストや解離性麻酔薬と組み合わせた短時間の不動化「カクテル」に組み込まれることがよくあります。

  • ​臨床上のポイント​: ブプレノルフィンは標準用量で「天井効果（シーリングエフェクト）」を示します。つまり、一定の用量を超えて増量しても追加の鎮痛効果は得られず、理論的には鎮痛効果が低下する可能性があります。
  • ​猫における利点​: 猫の口腔内pHは比較的アルカリ性であるため、ブプレノルフィンは高い脂溶性を示し、優れた​口腔粘膜（OTM）/ 頬粘膜吸収​を可能にします。猫では、頬粘膜投与のバイオアベイラビリティは筋肉内注射とほぼ同等であり、家庭での術後疼痛管理において非常に実用的な経路となります。
  • ​持続時間​: 純粋なミューアゴニスト（フェンタニルやメタドンなど）と比較して効果発現までの時間は長いですが、鎮痛効果の持続時間は著しく長くなります（通常6〜8時間、最大12時間）。
  • ​規制​: 本剤は規制薬物に指定されています。

作用機序

Buprenorphine exerts its analgesic effects by acting as a partial agonist at the mu (μ) opioid receptor and an antagonist at the kappa (κ) opioid receptor in the central nervous system.

  • High Affinity, Slow Dissociation: It binds to the μ-receptor with an affinity approximately 30 times greater than morphine. This tight binding → prolonged duration of action.
  • Receptor Competition: Because of its high affinity, it can displace pure μ-agonists from the receptor, potentially antagonizing their analgesic effects while reversing their sedative and respiratory depressant effects.
  • Naloxone Resistance: Its slow dissociation from the receptor makes it notoriously difficult to fully reverse with standard doses of the opioid antagonist naloxone; high doses of naloxone or the use of doxapram may be required in cases of severe respiratory depression.

安全性・警告

禁忌

  • Known hypersensitivity to buprenorphine

有害事象

  • Respiratory depression (rare but significant)
  • Sedation
  • Urine retention or difficulty voiding (particularly with high IV or epidural doses)
  • Excitement (horses)
  • Diminished gut sounds (horses)
  • Vomiting (rare in cats)

注意事項

Use with caution in patients with hypothyroidism, severe renal insufficiency, adrenocortical insufficiency (Addison's), and in geriatric or severely debilitated patients. Use cautiously in patients with compromised cardiopulmonary function due to the rare risk of respiratory depression. Extreme caution is required in patients with head trauma, increased CSF pressure, or CNS dysfunction (e.g., coma). Patients with severe hepatic dysfunction may eliminate the drug more slowly. May increase bile duct pressure; use cautiously in biliary tract disease.

医薬品相互作用

Local Anesthetics (mepivacaine, bupivacaine)

May be potentiated by concomitant use of buprenorphine

Anticonvulsants (phenobarbital, phenytoin)

May decrease plasma buprenorphine levels

Benzodiazepines

Case reports of humans developing respiratory/cardiovascular/CNS depression; use with caution

CNS Depressants (anesthetics, antihistamines, phenothiazines, barbiturates, alcohol)

May cause increased CNS or respiratory depression when used with buprenorphine

Erythromycin

Can increase plasma buprenorphine levels

Fentanyl (and other pure opiate agonists)

Buprenorphine may potentially antagonize some analgesic effects, but may also reverse some sedative and respiratory depressant effects

Halothane

Potentially can increase buprenorphine effects

Azole Antifungals (ketoconazole, itraconazole, fluconazole)

Can increase plasma buprenorphine levels

Monoamine Oxidase Inhibitors (selegiline, amitraz)

Possible additive effects or increased CNS depression

Naloxone

May reduce analgesia associated with high dose buprenorphine

Pancuronium

If used with buprenorphine may cause increased conjunctival changes

Rifampin

Potentially decrease plasma buprenorphine concentrations

MethadoneModerate

May antagonize the effects of full opioid agonists, though clinical relevance is debated. If analgesia is inadequate after buprenorphine, a full mu agonist may be administered without delay.

FentanylModerate

May antagonize the effects of full opioid agonists.

Anaesthetic agentsModerate

Reduces the doses of other drugs required for induction and maintenance of anaesthesia.

監視

  • Analgesic efficacy
  • Respiratory status
  • Cardiac status

薬物動態

半減期

猫6-7 hours馬6 hours

吸収

Rapidly absorbed following IM injection (40-90% in humans). Sublingual bioavailability is ~55% in humans. Oral doses undergo a high first-pass effect in the GI mucosa and liver. In cats, oral transmucosal (buccal) absorption is comparable to IM or IV administration. In dogs, oral transmucosal absorption is about 50%. Subcutaneous administration may be less bioavailable.

分布

Highly bound (96%) to plasma proteins (not albumin). Concentrates in the liver, but also found in the brain, GI tract, and placenta. Crosses the placenta and is found in maternal milk at concentrations equal to or greater than plasma. Volume of distribution in cats is approximately 8 L/kg.

代謝

Metabolized in the liver by N-dealkylation and glucuronidation.

消失

Metabolites are eliminated by biliary excretion into the feces (≈70%) and urinary excretion (≈27%). Clearance in cats is about 20 mL/kg/min.

過剰投与

Buprenorphine has a very high index of safety (ratio of lethal dose to effective dose is at least 1000:1 in rodents). Life-threatening acute overdoses are rare in veterinary medicine, but clinical signs are common.

  • ​Clinical Signs (Dogs)​: Vocalization, ataxia, hypersalivation, hypothermia, and lethargy.
  • Treatment: Supportive care. In cases of acute overdose causing severe respiratory or cardiac effects, naloxone and doxapram are suggested.

Note: Due to buprenorphine's extremely high affinity for the mu-receptor, standard doses of naloxone may be ineffective; very high doses of naloxone may be required to reverse respiratory depression.

製品

製剤

  • Sublingual tablets
  • Transdermal patch
  • Sublingual film/tablet with naloxone
  • Compounded sustained-release injection

動物用医薬品

  • Compounded sustained-release injectable (SC) product (zoopharm.net)

ヒト用医薬品

  • Buprenorphine HCl for Injection: 0.324 mg/mL (equivalent to 0.3 mg/mL buprenorphine) (Buprenex)
  • Buprenorphine HCl Sublingual Tablets: 2 mg & 8 mg (Subutex)
  • Buprenorphine HCl Transdermal System (Butrans)
  • Buprenorphine HCl Combinations (Sublingual Tablets): 2 mg buprenorphine/0.5 mg naloxone; 8 mg buprenorphine/2 mg naloxone (Suboxone)

規制ステータス

European Union✓ 承認済み処方箋医薬品 · Schedule 3 equivalentEMA
🐕 Dogs🐈 Cats

POM-V CD

United Kingdom✓ 承認済み処方箋医薬品 · Schedule 3VMD
🐕 Dogs🐈 Cats

POM-V CD SCHEDULE 3

規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

Store at room temperature (15-30° C). Avoid temperatures above 40° C or below freezing. Store away from bright light. Autoclaving may considerably decrease drug potency. Stable between a pH of 3.5-5.

飼主向け情報

ブプレノルフィンは強力な鎮痛薬であり、猫や小型犬のために自宅用に処方されることがよくあります。

  • ​投与のコツ​: 経口投与を指示された場合、​喉の奥に直接注入しないでください​。シリンジの先端を口の横（頬の内側や舌の下）に入れて液体を投与します。薬は歯茎から直接吸収されます。飲み込んでしまうと、効果を発揮する前に肝臓で大部分が破壊されてしまいます。
  • ​準備​: 自宅で正確に投与するために、あらかじめシリンジに1回分の用量を測り分けておくことを強くお勧めします。
  • ​予想される反応​: ペットは少し眠たそうにすることがあります。まれに、少し落ち着きがなくなったり、鳴いたりすることがあります。
  • ​安全性​: 指示通りに使用すれば非常に安全な薬ですが、規制薬物です。子供や他のペットの手の届かない場所に厳重に保管してください。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。