チレタミン / ゾラゼパム
Tiletamine / Zolazepam
Tiletamine hydrochloride / Zolazepam hydrochloride
別名: Telazol · CI-634 · CL-399 · CN-54521-2 · CI-716
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Diagnostic purposes | 6.6-9.9 mg/kg | IM | Once | — | 🌎 NA |
| Minor procedures of short duration | 9.9-13.2 mg/kg | IM | Once | — | 🌎 NA |
| General anesthesia/restraint | 3-10 mg/kg IM or SC or 2-5 mg/kg IV | IM/SC/IV | Once | — | 🌎 NA |
| Aggressive (difficult to handle) dogs requiring more sedation | 1-2 mg/kg | IM | Once | — | 🌎 NA |
- Diagnostic purposes: Supplemental doses should be less than initial dose. Max total dose 26.4 mg/kg. Use Atropine 0.04 mg/kg concurrently.
- Minor procedures of short duration: Supplemental doses should be less than initial dose. Max total dose 26.4 mg/kg. Use Atropine 0.04 mg/kg concurrently.
- General anesthesia/restraint: Based upon the combination of drugs.
- Aggressive (difficult to handle) dogs requiring more sedation: Only if insufficient sedation from opioid, higher dose medetomidine, and midazolam.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Procedures such as dentistry, abscess treatment, foreign body removal | 9.7-11.9 mg/kg | IM | Once | — | 🌎 NA |
| Procedures requiring mild to moderate analgesia (lacerations, castration) | 10.6-12.5 mg/kg | IM | Once | — | 🌎 NA |
| Ovariohysterectomy and onychectomy | 14.3-15.8 mg/kg | IM | Once | — | 🌎 NA |
| General anesthesia/restraint | 3-10 mg/kg IM or SC or 2-5 mg/kg IV | IM/SC/IV | Once | — | 🌎 NA |
- Procedures such as dentistry, abscess treatment, foreign body removal: Max total dose 72 mg/kg. Use Atropine 0.04 mg/kg concurrently.
- Procedures requiring mild to moderate analgesia (lacerations, castration): Max total dose 72 mg/kg. Use Atropine 0.04 mg/kg concurrently.
- Ovariohysterectomy and onychectomy: Max total dose 72 mg/kg. Use Atropine 0.04 mg/kg concurrently.
- General anesthesia/restraint: Based upon the combination of drugs.
小型哺乳類
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Chemical restraint (Gerbils) | 20 mg/kg IP (in combination with xylazine 10 mg/kg) | IP | Once | — | 🌎 NA |
| Chemical restraint (Mice) | 80-100 mg/kg | IM | Once | — | 🌎 NA |
| Chemical restraint (Rats) | 20-60 mg/kg | IM | Once | — | 🌎 NA |
| Chemical restraint (Hamsters/Gerbils) | 20-80 mg/kg | IM | Once | — | 🌎 NA |
| Chemical restraint (Guinea pig) | 10-80 mg/kg | IM | Once | — | 🌎 NA |
| Chemical restraint (Chinchillas) | 20-40 mg/kg | IM | Once | — | 🌎 NA |
| Immobilization/anesthesia (Hamsters) | 50-80 mg/kg | IP | Once | — | 🌎 NA |
| Chemical restraint (Gerbils) | 10-30 mg/kg | IP | Once | — | 🌎 NA |
| Immobilization (Mice) | 80 mg/kg | IP | Once | — | 🌎 NA |
| Light anesthesia (Rats) | 40 mg/kg | IP | Once | — | 🌎 NA |
| Immobilization (Guinea pigs) | 40-60 mg/kg | IM | Once | — | 🌎 NA |
| Prior to inhalation anesthesia (Small rodents) | 6-10 mg/kg | IM | Once | — | 🌎 NA |
- Prior to inhalation anesthesia (Small rodents): Advantages: better muscle relaxation, small volume, rapid induction. Disadvantages: increased secretions, variable recovery.
フェレット
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Sedative/analgesic | 22 mg/kg IM combined with glycopyrrolate (0.01 mg/kg IM) | IM | Once | — | 🌎 NA |
| Sedative/analgesic | 22 mg/kg | IM | Once | — | 🌎 NA |
| Sedative/analgesic | Telazol (1.5 mg/kg) plus xylazine (1.5 mg/kg) | IM | Once | — | 🌎 NA |
| Sedative/analgesic | Telazol (1.5 mg/kg) plus xylazine (1.5 mg/kg) plus butorphanol (0.2 mg/kg) | IM | Once | — | 🌎 NA |
| Sedative/analgesic | 22 mg/kg | IM | Once | — | 🌎 NA |
- Sedative/analgesic: Rapid onset, but slow and rough recovery (3-4 hours)
- Sedative/analgesic: Telazol alone
- Sedative/analgesic: May reverse xylazine with yohimbine (0.05 mg/kg IM)
- Sedative/analgesic: May reverse xylazine with yohimbine (0.05 mg/kg IM)
鳥
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Anesthesia/Restraint (Ratites) | 5 mg/kg | IM/IV | Once | — | 🌎 NA |
爬虫類
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Facilitate handling and anesthesia (Large Snakes) | 3 mg/kg | IM | Once | — | 🌎 NA |
| Facilitate handling and anesthesia (Crocodilians) | 4-8 mg/kg | IM | Once | — | 🌎 NA |
| General anesthesia | 3-10 mg/kg | IM | Once | — | 🌎 NA |
| Sedation for minor procedures | 4-10 mg/kg | IM | Once | — | 🌎 NA |
| Sedation/tranquillization or to facilitate intubation | 5 mg/kg | IM | Once | — | 🌎 NA |
- Facilitate handling and anesthesia (Large Snakes): Administer 30-45 minutes prior to handling. Sedation may persist for up to 48 hours.
- General anesthesia: Lizards/snakes generally lower end; chelonians may require high end. Monitor closely for apnea.
- Sedation for minor procedures: At higher doses (15-40 mg/kg), recovery may be greatly prolonged.
- Sedation/tranquillization or to facilitate intubation: Repeat if needed. Higher doses (6 mg/kg) associated with very long recovery times, especially in chelonians (72 hours).
馬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Anesthesia induction | Xylazine 1.1 mg/kg IV, 5 minutes prior to Telazol at 1.65-2.2 mg/kg IV | IV | Once | — | 🌎 NA |
- Anesthesia induction: ARCI UCGFS Class 2 Drug
牛
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Induction agent for cattle, llamas/alpacas | Xylazine at 0.05-0.1 mg/kg IV, IM, then Telazol at 2-4 mg/kg IV (IM) | IV/IM | Once | — | 🌎 NA |
| Restraint/Anesthesia (Llamas) | 4.7-6 mg/kg | IM | Once | — | 🌎 NA |
羊
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Induction agent | Xylazine at 0.05-0.1 mg/kg IV, IM, then Telazol at 2-4 mg/kg IV (IM) | IV/IM | Once | — | 🌎 NA |
- Induction agent: Caution: xylazine can cause severe hypoxemia and pulmonary edema in sheep.
ヤギ
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Induction agent | Xylazine at 0.05-0.1 mg/kg IV, IM, then Telazol at 2-4 mg/kg IV (IM) | IV/IM | Once | — | 🌎 NA |
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
チレタミン/ゾラゼパム（一般的な商品名：Telazol®）は、獣医療で広く使用されている注射用の麻酔・精神安定薬の配合剤です。2つの異なる薬理学的薬剤が1:1の割合で配合されています：
- チレタミン：ケタミンと化学的に関連する解離性麻酔薬で、深い鎮痛と健忘をもたらします。
- ゾラゼパム：ベンゾジアゼピン系のマイナートランキライザーであり、筋弛緩、抗不安作用を提供し、解離性麻酔薬単独で通常見られる筋肉の硬直や痙攣のリスクを打ち消します。
犬および猫の保定、小手術、麻酔用としてFDAに正式に承認されていますが、馬、反芻動物、豚、鳥類、爬虫類、エキゾチック/野生動物など、非常に多くの種で適応外使用として広く用いられています。
臨床のポイント： 2つの成分の作用時間は動物種によって異なります。犬ではチレタミンの作用がゾラゼパムより長く続くため、麻酔時間よりも鎮静時間が短くなります（覚醒が荒れる可能性があります）。猫ではゾラゼパムの作用がチレタミンより長く続くため、覚醒時に長時間の鎮静状態が得られます。
作用機序
The combination works synergistically through two distinct central nervous system pathways:
- Tiletamine acts as a non-competitive NMDA (N-methyl-D-aspartate) receptor antagonist. By blocking the excitatory neurotransmitter glutamate at the NMDA receptor → it prevents calcium influx into neurons → inducing a state of dissociative anesthesia characterized by catalepsy, profound somatic analgesia, and amnesia, while maintaining cranial nerve reflexes (e.g., palpebral, laryngeal).
- Zolazepam acts as a GABA-A receptor agonist. It binds to the benzodiazepine site on the GABA-A receptor complex → enhances the binding of the inhibitory neurotransmitter GABA → increases chloride ion influx → resulting in hyperpolarization of the neuron. This provides muscle relaxation, anxiolysis, and anticonvulsant effects, smoothing the induction and recovery phases of the dissociative anesthetic.
安全性・警告
禁忌
- Pancreatic disease
- Severe cardiac disease
- Severe pulmonary disease
- Rabbits (due to reports of renal toxicity/nephrosis)
- Large exotic cats, especially tigers (may cause seizures, permanent neurologic abnormalities, or death)
- Cesarean section (crosses placenta, causes fetal respiratory depression)
有害事象
- Respiratory depression and transient apnea
- Pain upon IM injection (especially in cats due to low pH)
- Athetoid movements (involuntary writhing/twitching)
- Tachycardia (especially in dogs)
- Emesis during emergence
- Excessive salivation and bronchial/tracheal secretions
- Vocalization and erratic/prolonged recovery
- Hypothermia
- Muscle rigidity or hypertonia
- Hypertension or hypotension
- Cyanosis, pulmonary edema, or cardiac arrest (rare/at high doses)
注意事項
Renal Dysfunction: Animals with renal disease may experience prolonged duration of anesthetic action or recovery times. Dosages may need reduction in geriatric or debilitated patients.
Hypothermia: May cause significant hypothermia. Susceptible animals (small body surface area, low ambient temperatures) must be monitored carefully and provided supplemental heat.
Reflexes Maintained: Like ketamine, Telazol does not abolish pinnal, palpebral, pedal, laryngeal, and pharyngeal reflexes. Use alone may not be adequate for surgery in these areas.
Ocular Protection: Cats' eyes remain open after administration. Protect from injury and apply an ophthalmic lubricant (e.g., Lacrilube) to prevent corneal drying.
Airway Management: Cats reportedly do not tolerate endotracheal tubes well with this agent alone.
Species Specific Warnings: Contraindicated in tigers and generally avoided in large exotic cats. Not recommended in rabbits due to nephrotoxicity.
医薬品相互作用
Dosage may need to be reduced when used concomitantly with Telazol.
Dosage may need to be reduced when used concomitantly with Telazol.
In cats, anesthesia is prolonged on average by 30 minutes. No apparent effect on recovery times in dogs.
Can cause increased respiratory and cardiac depression.
May cause enhanced or prolonged respiratory depression (extrapolated from ketamine).
May induce hypertension and tachycardia (extrapolated from ketamine).
May increase zolazepam (benzodiazepine) levels.
May increase zolazepam levels.
May increase zolazepam levels.
May increase zolazepam levels.
May increase hypnotic effects and risk of hypotension/respiratory depression.
May decrease peak levels and AUC of zolazepam.
May decrease peak levels and AUC of zolazepam.
監視
- Level of anesthesia and analgesia
- Respiratory function (rate, depth, pulse oximetry)
- Cardiovascular status (heart rate, rhythm, blood pressure)
- Body temperature (monitor for hypothermia)
- Eye moisture and corneal integrity (especially in cats)
薬物動態
半減期
吸収
Onset of action is variable but generally rapid. In cats, IM onset is 1-7 minutes. In dogs, IM onset averages 7.5 minutes.
分布
Crosses the placenta.
代謝
Hepatic metabolism. The duration of effect of the two components varies by species (zolazepam lasts longer in cats; tiletamine lasts longer in dogs).
消失
Less than 4% of the drugs are excreted unchanged in the urine in dogs.
過剰投与
The manufacturer claims a 2X margin of safety in dogs and a 4.5X margin of safety in cats.
- Clinical Signs: Excessive respiratory depression, prolonged anesthesia, potential cardiovascular collapse.
- Treatment: In massive overdoses, mechanically assisted ventilation should be performed if necessary. Treat other clinical signs symptomatically and supportively.
- Reversal/Stimulation: A preliminary study in dogs suggests that doxapram at 5.5 mg/kg will enhance respirations and arousal after Telazol administration.
Note: High doses of tiletamine have caused acute tubular necrosis in New Zealand white rabbits.
製品
製剤
- Injectable lyophilized powder for reconstitution: 50 mg/mL tiletamine + 50 mg/mL zolazepam (100 mg/mL combined)
動物用医薬品
- Telazol® (Pfizer): Tiletamine HCl (equivalent to 250 mg free base) and Zolazepam HCl (equivalent to 250 mg free base) as lyophilized powder in 5 mL vials. Reconstituted with 5 mL sterile water yields 50 mg/mL of each drug (100 mg/mL combined). (Rx, C-III)
規制ステータス
規制データなし: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
After reconstitution, solutions may be stored for 4 days at room temperature and 14 days if refrigerated. Do not use solutions that contain a precipitate or are discolored.
飼主向け情報
この薬は注射用の麻酔薬および精神安定薬であり、処置中のペットを安全に鎮静または麻酔するために、動物病院内で獣医療従事者によってのみ使用されます。
- 覚醒時： 薬の効果が切れるにつれて、ペットの覚醒に時間がかかったり、少し落ち着きがない状態（鳴く、ピクピク動く、ふらつくなど）になることがあります。これは正常な反応ですが、完全に回復するまでは静かで安全、かつ暖かい環境に置いてあげてください。
- 目のケア： この薬は鎮静中も目が開いたままになることがあるため、獣医師が保護用の眼軟膏を塗布します。処置後、目の周りに軟膏が残っていることがあります。
- 体温： 薬の影響で体温が下がることがあるため、回復中はペットを暖かく保つ必要があります。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。