テルミコシン
**テルミコシン**は、タイロシンから合成された半合成**マクロライド系抗生物質**であり、主に獣医学において、*Mannheimia haemolytica*、*Pasteurella multocida*、および*Histophilus somni*に関連する牛および羊の呼吸器疾患（BRD）の治療に使用されます。 * **主な特徴**: * 脂溶性が高く、組織への移行性に優れています。**肺組織**および肺胞マクロファージに能動的に濃縮され、呼吸器感染症に対する標的治療を提供します。 * 反芻動物には主に**皮下（SC）**注射で投与され、豚には飼料添加薬として投与されます。 > **重大な警告**: テルミコシンは多くの動物種において安全域が狭いです。ヒト、豚、馬、ラクダ科動物、および非ヒト霊長類に誤って注射した場合、重度の心血管毒性により**急速に死に至る**可能性があります。
作用機序: Tilmicosin exerts its bacteriostatic effect by penetrating the bacterial cell membrane and reversibly binding to the **50S ribosomal subunit**. * **Mechanism**: Binds to the **50S subunit** → blocks the exit tunnel for newly synthesized peptides → inhibits translocation of peptidyl-tRNA → **premature termination of bacterial protein synthesis**. * It exhibits time-dependent antibacterial activity and has a prolonged post-antibiotic effect (PAE), especially against respiratory pathogens. Its accumulation in macrophages allows it to be delivered directly to the site of infection via chemotaxis.
動物種別の用量
- Susceptible infections · 10 mg/kg SC (not more than 15 mL per injection site). · SC · Single dose · Subcutaneous injection under the skin in the neck, or if not accessible, behind the shoulders and over the ribs is suggested. Do not use in lambs less than 15 kg of body weight.
- Treatment of pneumonic pasteurellosis · 10 mg/kg SC every 72 hours · SC · q72h · Subcutaneous injection under the skin in the neck, or if not accessible, behind the shoulders and over the ribs is suggested.
- Susceptible infections · 10 mg/kg SC (not more than 15 mL per injection site) · SC · Single dose
- Susceptible infections (Rabbits) - Regimen 1 · 25 mg/kg SC once; repeat in 3 days if necessary. · SC · Once, repeat in 3 days PRN · Can cause weakness, pallor, tachypnea and sudden death. May cause acute death if given IV. SC injections can cause local swelling and necrosis.
- Susceptible infections (Rabbits) - Regimen 2 · 5 mg/kg SC on day 0, if no reaction, give 10 mg/kg SC on days 7 and 14. · SC · Days 0, 7, 14 · 14 days · Can cause weakness, pallor, tachypnea and sudden death. May cause acute death if given IV. SC injections can cause local swelling and necrosis.
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
- Intravenous (IV) administration (can be fatal)
- Use in automatically powered syringes
- Injection in swine, non-human primates, horses, and camelids
- Use in lactating ewes if milk is intended for human consumption
- Use in veal calves
- Use in female dairy cattle 20 months or older
有害事象
- Local tissue reaction and trim loss (if given IM)
- Edema at the site of subcutaneous injection
- Severe cardiovascular toxicity (fatalities) if given IV
- Fatalities in swine, non-human primates, and potentially horses if injected
- Severe reactions in camelids
薬物相互作用
- Epinephrine · Increased mortality associated with tilmicosin in swine.
- Other Macrolides / Lincosamides · Potential cross-resistance and competitive binding at the 50S ribosomal subunit (extrapolated from erythromycin).
モニタリング
- Clinical efficacy (resolution of respiratory signs)
- Injection site reactions
- Slaughter withdrawal times (28 days for cattle/sheep injection; 7 days for swine feed)
過量投与
The **cardiovascular system** is the primary target of acute toxicity, likely due to calcium channel blockade leading to negative inotropic effects, tachycardia, and fatal arrhythmias. * **Cattle**: Doses up to 50 mg/kg IM did not cause death, but SC doses of 150 mg/kg caused fatalities, as did IV doses of 5 mg/kg. * **Swine**: Doses as low as 10 mg/kg caused increased respiration, emesis, and seizures; 20 mg/kg IM caused death in most animals tested. * **Monkeys**: 10 mg/kg caused no signs of toxicity; 20 mg/kg caused vomiting; 30 mg/kg caused death. > **HUMAN EXPOSURE**: In cases of human injection, **contact a physician immediately**. Apply ice to the injection site. Emergency medical telephone numbers: 1-800-722-0987 or 1-317-276-2000.
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。