プロポフォール
プロポフォールは短時間作用型で高脂溶性の静脈内麻酔薬であり、獣医療において全身麻酔の導入および維持に広く使用されています。発現が早く、スムーズで迅速な回復が得られるため、外来での診断や小手術に特に有用です。 **主な臨床的特徴:** * **迅速な発現と回復:** 30〜60秒以内に麻酔を導入します。中枢神経系から他の組織への再分布により、回復は通常スムーズかつ迅速です。 * **臓器機能:** 軽度から中等度の心疾患、または肝疾患や腎疾患を持つ動物にも安全に使用できます。 * **適応外使用:** 難治性てんかん重積状態に対する持続静脈内投与(CRI)として頻繁に利用され、特にペントバルビタールが禁忌となる肝性脳症の症例で有用です。 * **猫に関する注意事項:** 猫は犬のような強力なグルクロン酸抱合経路を持たないため、連日の使用や長時間の輸注により、回復の遅延、ハインツ小体性貧血、倦怠感を引き起こしやすくなります。 > **臨床のポイント:** プロポフォールには**鎮痛作用がありません**。痛みを伴う処置には、適切な周術期鎮痛プロトコル(オピオイド、NSAIDs、局所麻酔ブロックなど)を併用する必要があります。
作用機序: While the monograph notes the mechanism is not well understood, **modern pharmacological consensus** indicates that propofol primarily acts as a positive allosteric modulator of inhibitory **GABA_A receptors** in the central nervous system. * **Mechanism:** Propofol binds to GABA_A receptors → increases the inward conductance of chloride ions → hyperpolarizes the postsynaptic neuronal membrane → profound CNS depression and hypnosis. * **Cardiovascular & Respiratory:** Causes dose-dependent direct myocardial depression, vasodilation (arterial hypotension), and significant respiratory depression (apnea is common with rapid boluses). * **Other Effects:** Decreases intraocular pressure (IOP), possesses antiemetic properties, and at sub-anesthetic doses, can act as an appetite stimulant in dogs.
動物種別の用量
- Induction of general anesthesia (no premedication) · 4.1-8 mg/kg · IV · titrated · Mean induction dose 7.4 mg/kg.
- Induction of general anesthesia (with premedication) · 2.7-8 mg/kg · IV · titrated · Dose sparing effect of 16-24%.
- Maintenance of general anesthesia (no premedication) · 0.8-5 mg/kg · IV · intermittent · Duration of anesthesia following each dose is approx 3-5 minutes.
- Single injection induction (with acepromazine +/- butorphanol) · 4-6 mg/kg · IV · single dose · Doses of 8-13 mg/kg IV allow intubation without topical anesthesia.
- Induction of anaesthesia (unpremedicated) · 8 mg/kg · IV · single dose · as needed · Administer slowly over 30-60 seconds. Titrate to effect.
- Induction of anaesthesia (premedicated) · 2-5 mg/kg · IV · single dose · as needed · Administer slowly over 30-60 seconds. Titrate to effect.
- Maintenance of anaesthesia · 0.1-0.4 mg/kg/min · IV · CRI · as needed · Likely to result in a prolonged recovery in cats. Dose depends on other agents given in combination. Do not use benzyl alcohol formulations for CRI.
- Anesthesia (Rabbits) · 5-14 mg/kg slow IV (20 mg/kg/minute) to effect · IV · titrated · Not recommended as the sole agent for maintenance.
- Anesthesia (Mice) · 26 mg/kg · IV · single dose
投与経路
禁忌
- Hypersensitivity to propofol or any component of the product
- Patients where general anesthesia or sedation is strictly contraindicated
- Use of benzyl alcohol-preserved formulations for maintenance of anaesthesia via continuous rate infusion (CRI)
有害事象
- Transient respiratory depression and apnea (especially with rapid IV administration)
- Arterial hypotension and bradycardia
- Cyanosis (secondary to apnea)
- Seizure-like clinical signs during induction (paddling, opisthotonus, myoclonic twitching)
- Histamine release and rare anaphylactoid reactions
- Cats (with repeated/prolonged use): Heinz body anemia, slowed recovery, anorexia, lethargy, diarrhea
- Apnoea (especially with rapid injection)
- Cyanosis
- Bradycardia
- Severe hypotension
- Muscle rigidity and tremors (dogs)
- Paradoxical muscle movements (dogs)
- Heinz body anaemia (cats, with repeated daily use)
- Pain on IV injection
薬物相互作用
- Inhalation Anesthetics (halothane, isoflurane) · Propofol serum concentrations may be increased; propofol induction may require higher initial inhalant concentrations due to rapid recovery.
- Local Anesthetics · Propofol dosage requirements for sedation or hypnosis may be reduced.
- Anticholinergics · Propofol-induced bradycardia may be exacerbated, particularly when opiate premedicants are used.
- Chloramphenicol · May decrease clearance of propofol and increase recovery times.
- Clonidine · When used as a premed, may reduce propofol dosage requirements.
- CNS Depressants (acepromazine, diazepam, etc.) · Increased sedative, anesthetic, and cardiorespiratory depression possible; propofol dose should generally be reduced by ~25%.
- Hepatic P-450 Inhibitors (cimetidine, ketoconazole) · May potentially increase recovery times associated with propofol (especially significant in cats).
- Fentanyl · Increased risk for bradycardia.
- Medetomidine · Hypoxemia may occur when propofol is used after medetomidine; dosage adjustments and adequate monitoring required.
- Metoclopramide · May reduce the propofol dose required for induction by 20-25%.
- Midazolam · Synergistic effects; midazolam plasma concentrations may be increased up to 20%.
モニタリング
- Level of anesthesia/CNS effects
- Respiratory rate, rhythm, and depth (monitor for apnea/cyanosis)
- Cardiovascular status (cardiac rate/rhythm, blood pressure, pulse oximetry)
- Respiratory rate, rhythm, and depth (capnography recommended)
- Heart rate and rhythm (ECG)
- Blood pressure
- Oxygen saturation (SpO2)
- Depth of anaesthesia
過量投与
Overdosages are likely to cause **significant respiratory depression** (apnea) and potentially severe **cardiovascular depression** (hypotension, bradycardia). **Treatment:** 1. Immediately discontinue propofol administration. 2. Establish an airway and provide **artificial ventilation with 100% oxygen**. 3. Administer symptomatic and supportive treatment for cardiovascular depression (e.g., intravenous fluid therapy, vasopressors, anticholinergics like atropine or glycopyrrolate).
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。