アルフェンタニル
Alfentanil
Alfentanil Hydrochloride
別名: Fanaxal · Fentalim · Limifen · Rapifen · alfentanyl · Alfentanilum
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 (extra-label) — Intraoperative analgesia in patients with intracranial disease
認証済み獣医師の確認が必要
NA
必ず考慮する臨床コンテキスト (3)
- NOTE: In obese patients, calculate doses based on lean body weight.
- Analgesia (extra-label):
- Alfentanil injection should be stored protected from light at controlled room temperature (20°C-25°C; 68°F-77°F).
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。
概要
アルフェンタニルは、フェンタニルに構造的に関連するフェニルピペリジン系の強力で短時間作用型の合成オピオイドです。
主な特徴は以下の通りです:
- 迅速な発現と短い作用時間: 脂溶性が高く、血液脳関門を急速に通過するため、短時間の処置や持続静注(CRI)に最適です。
- 麻酔補助薬: 主に強力な鎮痛を提供し、導入または維持麻酔薬(プロポフォール、イソフルランなど)の必要量を減らすために使用されます。
- 動物種特異性: 獣医療での経験はフェンタニルに比べて限られていますが、特に猫の麻酔時の補助療法として有用であるとされています。
- 規制状況: 乱用の可能性が高いため、スケジュールIIの規制薬物に指定されています。
作用機序
Alfentanil acts primarily as a potent and highly selective agonist at mu (μ) opioid receptors in the central nervous system.
- Mechanism: Binds to pre- and post-synaptic μ-receptors → inhibits adenylate cyclase → decreases intracellular cAMP → promotes opening of inward-rectifying potassium channels → hyperpolarization of the neuron.
- Neurotransmitter Inhibition: Concurrently inhibits voltage-gated calcium channels → decreases the release of excitatory nociceptive neurotransmitters (such as substance P and glutamate) → profound analgesia and sedation.
- Systemic Effects: Causes dose-dependent respiratory depression by decreasing the responsiveness of the brainstem respiratory centers to carbon dioxide.
安全性・警告
禁忌
- Patients hypersensitive to opioids
有害事象
- Dose-related respiratory depression
- Bradycardia
- CNS depression
- Dose-related skeletal muscle rigidity
- Asystole (rare)
- Hypercarbia (rare)
- Hypersensitivity reactions (rare)
注意事項
Critical Warning: Because of the drug's potency and potential for significant adverse effects, it should only be used in situations where patient vital signs can be continuously monitored.
- Dose Adjustments: Initial dosage reduction may be required in geriatric or debilitated patients, particularly those with diminished cardiopulmonary function or liver disease.
- Muscle Rigidity: Dose-related skeletal muscle rigidity is not uncommon; neuromuscular blockers are routinely used in conjunction.
- Laboratory Artifacts: May increase plasma levels of amylase or lipase secondary to increased biliary tract pressure. Values may be unreliable for 24 hours post-administration.
医薬品相互作用
May increase the half-life and decrease the clearance of alfentanil leading to prolonged effect and an increased risk of respiratory depression
May produce bradycardia or hypotension if used concurrently with alfentanil
May produce bradycardia or hypotension; respiratory or CNS depression may be exacerbated
Reduces the dose requirements of concurrently administered anaesthetics by at least 50%
Risk of serotonin toxicity
監視
- Anesthetic and/or analgesic efficacy
- Cardiac rate and rhythm
- Respiratory rate and depth
- Pulse oximetry or other methods to measure blood oxygenation
薬物動態
半減期
吸収
In humans, onset of anesthetic action occurs within 2 minutes after IV dosing, and within 5 minutes of IM injection. Peak effects occur approximately 15 minutes after IM injection.
分布
Steady state volume of distribution in dogs is about 0.56 L/kg. In humans, Vd is 0.4-1 L/kg. About 90% of the drug is bound to plasma proteins.
代謝
Primarily metabolized in the liver to inactive metabolites.
消失
Metabolites are excreted by the kidneys into the urine; only about 1% of the drug is excreted unchanged into the urine. Clearance in dogs is approximately 30 mL/kg/minute.
過剰投与
Signs of Toxicity
- Severe IV Overdose: Circulatory collapse, pulmonary edema, seizures, cardiac arrest, and death.
- Less Severe Overdose: CNS and respiratory depression, coma, hypotension, muscle flaccidity, and miosis.
Treatment
- Supportive Care: Provide cardiovascular and respiratory support (e.g., mechanical ventilation, IV fluids) as necessary.
- Antidote: Administration of an opiate antagonist such as naloxone. Although alfentanil has a relatively rapid half-life, multiple doses of naloxone may be necessary.
Measurement Precaution: Because of the drug's extreme potency, the use of a tuberculin syringe to measure dosages less than 1 mL, along with a dosage calculation and measurement double-check system, is strongly recommended.
製品
製剤
- Injection: 500 micrograms/mL
ヒト用医薬品
- Alfentanil HCl for injection: 500 micrograms (as base)/mL in 2, 5 mL, 10 mL, & 20 mL amps; preservative-free; Alfenta® (Akorn); generic (Abbott); (Rx, C-II)
規制ステータス
Controlled Drug
POM CD SCHEDULE 2
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Alfentanil injection should be stored protected from light at room temperature. Compatible with Normal Saline, D5 in Normal Saline, D5W, and Lactated Ringers in concentrations up to 80 micrograms/mL.
飼主向け情報
アルフェンタニルは、麻酔および重度の疼痛管理に厳密に使用される非常に強力なオピオイド薬です。
- 専門家専用: この薬は、高度な患者モニタリング(心電図や酸素モニターなど)が利用可能な臨床環境において、獣医療の専門家によってのみ投与されます。
- 安全性: 呼吸や心拍数を低下させる可能性があるため、処置中、ペットは常に厳密に監視されます。
- 麻酔後: 処置後、ペットはぼんやりしたり眠そうにしたりすることがありますが、これはオピオイド麻酔薬の正常な反応です。
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。
