コデイン
**コデイン**はフェナントレン誘導体のオピオイド作動薬であり、獣医学では主に**鎮咳薬**(咳止め)および軽度の**鎮痛薬**として使用されます。止瀉薬として使用されることもあります。 * **鎮痛**:軽度から中等度の疼痛に使用され、NSAIDsが無効または禁忌の場合によく用いられます。 * **鎮咳**:非生産性の咳(気管虚脱、慢性気管支炎など)の抑制に非常に有効です。 * **止瀉**:消化管の運動を低下させます。 > **臨床上のポイント**:人医療では広く使用されていますが、犬での使用には議論があります。犬は経口コデインの吸収が非常に悪く、活性代謝物(モルヒネ)に変換するための強力な酵素経路を欠いています。そのため、犬における鎮痛効果は非常にばらつきがあり、一般的にブプレノルフィンやメタドンなどの他のオピオイドに劣ると考えられています。
作用機序: Codeine acts as a weak agonist at **mu (μ) opioid receptors**. * **Analgesia**: Binds to **μ-receptors** in the central nervous system → inhibits the release of excitatory neurotransmitters (such as Substance P) in ascending pain pathways → alters the perception of and response to pain. * **Antitussive**: Causes direct depression of the **medullary cough center** in the brainstem. * **Antidiarrheal**: Binds to **enteric μ-receptors** → decreases gastrointestinal motility and increases sphincter tone. * **Metabolism Note**: In humans, codeine is a prodrug metabolized by the enzyme **CYP2D6** → **morphine**. Dogs lack significant CYP2D6-equivalent activity, relying mostly on codeine-6-glucuronide for any analgesic effect, which explains its limited efficacy in this species.
動物種別の用量
- Analgesic (mild to moderate acute pain) · 0.5-2 mg/kg PO titrated to effect q6-12h · PO · q6-12h · May use for chronic pain at lowest effective dose. Do NOT use combination products containing acetaminophen.
- Analgesic · 0.5-2 mg/kg PO q6-8h · PO · q6-8h · Do NOT use combination products containing acetaminophen.
- Analgesic · 0.5 mg/kg PO q6h · PO · q6h · Do NOT use combination products containing acetaminophen.
- Antitussive / Analgesia · 0.5 - 2 mg/kg · PO · q6h-q8h · As directed · Rarely used. MUST ensure the product does NOT contain paracetamol.
- Analgesic · 1 mL in 10-20 mL of drinking water · PO · Continuous · Using acetaminophen and codeine elixir. Add dextrose to enhance palatability.
- Antitussive · 1-2 mg/kg PO q6-12h · PO · q6-12h
- Antitussive · 0.1-0.3 mg/kg PO q8-12h up to 1-2 mg/kg PO q6-12h · PO · q6-12h · Whatever the starting point, the dose may need to be increased to achieve a satisfactory effect.
- Analgesic (mild to moderate acute pain) · 0.5-2 mg/kg PO titrated to effect q6-12h · PO · q6-12h · May use for chronic pain at lowest effective dose.
- Analgesic (in combination with acetaminophen) · 1-2 mg/kg (of the codeine) PO q6-8h · PO · q6-8h · Using a 60 mg codeine and 300 mg acetaminophen fixed-dose tablet. Do not use in cats.
投与経路
禁忌
- Hypersensitivity to narcotic analgesics
- Patients receiving monoamine oxidase inhibitors (MAOIs) like amitraz or selegiline
- Diarrhea caused by toxic ingestion (until toxin is eliminated)
- Repeated use in severe inflammatory bowel disease
- Scorpion stings (Centruroides sculpturatus and C. gertschi) as it may potentiate venom
- Combination products containing acetaminophen are STRICTLY CONTRAINDICATED in cats
- Hypersensitivity to opioids
- Severe respiratory depression or asthma
- Cats (especially if using combination products containing paracetamol)
有害事象
- Sedation (most common)
- Constipation
- Anorexia
- Vomiting
- Ileus
- Biliary and pancreatic duct spasms
- Respiratory depression (at high doses)
- Cats: CNS stimulation, hyperexcitability, tremors, seizures
- Sedation
- Nausea
薬物相互作用
- Anticholinergic drugs · May increase the chances of constipation developing
- Antidepressants (TCAs/MAOIs) · May potentiate CNS depressant effects
- CNS Depressants (anesthetics, antihistamines, phenothiazines, barbiturates, tranquilizers) · May cause increased CNS or respiratory depression
- Quinidine · May inhibit the transformation of codeine to morphine in the liver, decreasing its efficacy
- CNS Depressants (e.g., phenobarbital, diazepam) · Additive CNS and respiratory depression · moderate
- SSRIs / MAOIs · Increased risk of serotonin syndrome · major
- CNS Depressants (e.g., sedatives, anesthetics, antihistamines) · Additive CNS and respiratory depression · major
- Monoamine Oxidase Inhibitors (MAOIs) · May cause severe, unpredictable reactions (serotonin syndrome or severe respiratory depression) · major
モニタリング
- Efficacy (pain relief, reduction in coughing, or resolution of diarrhea)
- Adverse effects (sedation, respiratory rate, GI signs)
- Respiratory rate and depth
- Level of sedation
- Pain score or coughing frequency
- Bowel movements (monitor for constipation)
過量投与
Opiate overdosage may produce profound **respiratory and/or CNS depression**. Other effects can include cardiovascular collapse, hypothermia, and skeletal muscle hypotonia. * **Decontamination**: Oral ingestions should be removed using standard gut removal protocols. Inducing vomiting should be attempted with caution due to rapid changes in CNS status. * **Antidote**: **Naloxone** is the agent of choice for treating respiratory depression. In massive overdoses, naloxone doses may need to be repeated, as its effects may diminish before subtoxic levels of codeine are attained. * **Supportive Care**: Mechanical respiratory support should be considered in cases of severe respiratory depression. Contact an animal poison control center for further guidance.
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。