メペリジン
メペリジン(別名ペチジン)は、主に鎮痛に使用される合成**オピオイド作動薬**です。 **臨床上のポイント:** * 歴史的にはよく使用されていましたが、作用時間が非常に短く(犬や猫では1〜2時間未満)、特に静脈内投与時に**ヒスタミン遊離**や低血圧を引き起こす傾向が高いため、現代の獣医療での使用は大幅に減少しています。 * 他の多くのオピオイドとは異なり、メペリジンは**抗コリン作用(迷走神経遮断作用)および陰性変力作用**を有しており、純粋なμ作動薬で通常見られる徐脈ではなく、頻脈を引き起こす可能性があります。 * 効力はモルヒネの約1/3〜1/8ですが、等鎮痛用量では同程度の呼吸抑制を引き起こします。 * 本剤はスケジュールII(C-II)の規制薬物です。
作用機序: Meperidine acts primarily as an agonist at the **mu (μ) opioid receptors** in the central nervous system (CNS) and peripheral tissues. * **Receptor Binding:** Binds to G-protein coupled mu receptors → inhibits adenylate cyclase → decreases intracellular cAMP. * **Ion Channel Modulation:** Promotes opening of potassium channels (causing hyperpolarization) and inhibits voltage-gated calcium channels (decreasing neurotransmitter release). * **Analgesia:** Inhibits ascending nociceptive pathways and alters the perception of pain. * **Unique Mechanisms:** Exhibits **anticholinergic (vagolytic)** effects and can cause direct mast cell degranulation leading to **histamine release**.
動物種別の用量
- Perioperative pain · 3-5 mg/kg · IM, SC · 1-2 hours
- Analgesia · 2-5 mg/kg · IM, SC · short (30 minutes to an hour)
- Pre-medication · 3-4 mg/kg · IM · In healthy cats
- Post-op analgesia · 1-2 mg/kg · IM · In healthy cats
- General Note · Not recommended for cats
- Analgesia (mild to moderate pain) · 5-10 mg/kg · IM, SC · q1-2h · Depending on pain assessment · Frequent redosing is required.
- Restraining agent (preanesthetic) · 1-2 mg/kg · IM · 45-60 minutes before anesthesia · Used in combination with promazine (2 mg/kg IM) and atropine (0.07-0.09 mg/kg IM) in separate sites.
- Analgesia · 2 mg/kg · IM · q4h · as needed
- Analgesia · 5-10 mg/kg · SC, IM · q2-3h
- Analgesia · Up to 200 mg total dose · IM
投与経路
禁忌
- Hypersensitivity to narcotic analgesics
- Patients receiving monamine oxidase inhibitors (MAOIs)
- Diarrhea caused by a toxic ingestion (until toxin is eliminated)
- Envenomations from Centruroides scorpion species, Gila monsters, or Mexican beaded lizards
- Intravenous (IV) administration
- Animals at risk from histamine release (e.g., skin allergies, asthma, mast cell tumours)
有害事象
- Respiratory depression
- Histamine release
- Bronchoconstriction (dogs)
- CNS depression
- Nausea and vomiting
- Decreased intestinal peristalsis
- Mydriasis (dogs)
- Salivation (especially cats)
- Physical dependence (chronic use)
- Tachycardia with PVCs (horses)
- Profuse sweating (horses)
- Hyperpnea (horses)
- Severe hypotension (if given IV rapidly)
- Hypotension (especially if given IV)
- Tachycardia
- Bronchoconstriction
薬物相互作用
- CNS Depressants (anesthetics, antihistamines, phenothiazines, barbiturates, tranquilizers) · May cause increased CNS or respiratory depression when used with meperidine.
- Diuretics · Opiates may decrease efficacy in CHF patients.
- Isoniazid · Meperidine may enhance INH adverse effects.
- Monamine Oxidase Inhibitors (MAOIs) (e.g., amitraz, selegiline) · Contraindicated. Can cause severe opiate overdose signs; avoid meperidine for at least 14 days after receiving MAOIs.
- Skeletal Muscle Relaxants · Meperidine may enhance neuromuscular blockade.
- Tricyclic Antidepressants (clomipramine, amitriptyline) · Meperidine may exacerbate the effects of tricyclic antidepressants.
- Warfarin · Opiates may potentiate anticoagulant activity.
- CNS depressants (anaesthetics, antihistamines, barbiturates, phenothiazines, tranquillizers) · Increased CNS or respiratory depression · moderate
- Monoamine oxidase inhibitors (MAOIs) · Serious interaction resulting in coma, convulsions, and hyperpyrexia · major
モニタリング
- Respiratory rate and depth
- CNS level of depression or excitation
- Blood pressure (especially with IV use)
- Analgesic activity
- Pain score
- Heart rate
- Blood pressure
- Signs of histamine release (urticaria, bronchoconstriction)
過量投与
Overdosage may produce profound **respiratory and/or CNS depression**. Other effects can include cardiovascular collapse, hypothermia, and skeletal muscle hypotonia. * **Species Differences:** Some species (especially cats) may demonstrate CNS excitability (hyperreflexia, tremors) and seizures at doses >20 mg/kg. * **Treatment:** **Naloxone** is the agent of choice for respiratory depression. In massive overdoses, naloxone doses may need to be repeated, as its effects can diminish before subtoxic levels of meperidine are attained. Mechanical respiratory support should be considered. Pentobarbital has been suggested for CNS excitement/seizures in cats, but extreme caution is required as barbiturates and narcotics have additive respiratory depressant effects.
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。