アルフェンタニル
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.
動物種別の用量
- As a premed · 5 micrograms/kg alfentanil with 0.3-0.6 mg of atropine · IV · 30 seconds before injecting propofol · Can reduce the dose of propofol needed to induce anesthesia to 2 mg/kg, but apnea may still occur.
- As a constant rate infusion for pain · Loading dose of 0.5-1 micrograms/kg, then a CRI of 0.5-1 micrograms/kg per minute. · IV · CRI
- As an analgesic supplement to anesthesia · 2-5 micrograms/kg · IV · q20 minutes
- For intra-operative analgesia in patients with intracranial disease · 0.2 micrograms/kg/minute · IV · CRI
- Intraoperative analgesia · 0.001-0.005 mg/kg · IV · single bolus · Administer slowly to avoid severe bradycardia
- Intraoperative analgesia · 0.001-0.0025 mg/kg/min · IV · continuous rate infusion · Best method of administration due to short duration of action
- Intraoperative analgesia · 0.001 mg/kg · IV · single bolus · Administer slowly to avoid severe bradycardia
- Intraoperative analgesia · 0.001 mg/kg/min · IV · continuous rate infusion · Best method of administration due to short duration of action
用量は獣医療従事者向けの臨床リファレンスです。必ず最新の添付文書と個々の患者で確認してください。
投与経路
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)
薬物相互作用
- CYP3A4 Inhibitors (erythromycin, cimetidine, ketoconazole, itraconazole, fluconazole, diltiazem) · May increase the half-life and decrease the clearance of alfentanil leading to prolonged effect and an increased risk of respiratory depression
- Beta-blockers · May produce bradycardia or hypotension if used concurrently with alfentanil
- Other anesthetic agents · May produce bradycardia or hypotension; respiratory or CNS depression may be exacerbated
- Inhaled anaesthetics · Reduces the dose requirements of concurrently administered anaesthetics by at least 50% · major
- Monoamine oxidase inhibitors (MAOIs) · Risk of serotonin toxicity · major
モニタリング
- Anesthetic and/or analgesic efficacy
- Cardiac rate and rhythm
- Respiratory rate and depth
- Pulse oximetry or other methods to measure blood oxygenation
過量投与
### 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.
VetSheet の薬剤リファレンスは、獣医療従事者向けの臨床意思決定支援を目的としており、専門的判断やメーカーの最新添付文書に代わるものではありません。