Dexmedetomidine
Dexmedetomidine is a potent, highly specific **alpha-2 adrenergic agonist** used primarily as a sedative, analgesic, and preanesthetic in veterinary medicine. It is the dextrorotatory enantiomer of medetomidine, making it approximately twice as potent as the racemic mixture. **Key Clinical Features:** * **Biphasic Cardiovascular Response:** Initial peripheral vasoconstriction leads to transient hypertension and a pronounced reflex bradycardia. This is followed by a central sympatholytic effect causing normotension or mild hypotension, while bradycardia persists. * **Analgesia:** Provides excellent visceral and somatic analgesia, often synergistic with opioids (e.g., "kitty magic" or "doggie magic" protocols). * **Reversibility:** Effects can be rapidly and completely reversed using the specific alpha-2 antagonist **atipamezole**. * **Dosing:** In dogs, dosing is uniquely based on **body surface area (BSA)** rather than strictly by weight, as smaller dogs require higher per-kg doses to achieve similar sedation levels.
กลไกการออกฤทธิ์: Dexmedetomidine acts as a highly selective agonist at **pre-synaptic alpha-2 adrenergic receptors** in the central and peripheral nervous systems. * **CNS Effects:** Activation of alpha-2 receptors in the locus coeruleus → decreased norepinephrine release → profound sedation, anxiolysis, and analgesia. * **Cardiovascular Effects:** Activation of peripheral post-synaptic alpha-2B receptors in vascular smooth muscle → intense vasoconstriction → increased systemic vascular resistance (SVR) → reflex bradycardia mediated by baroreceptors. Central alpha-2A activation subsequently decreases sympathetic outflow. * **Other Effects:** Decreases GI secretions, alters intestinal motility, induces diuresis (via inhibition of ADH), and causes mild muscle relaxation.
ขนาดยาตามชนิดสัตว์
- Sedation and analgesia · 40 micrograms/kg IM · IM · Single dose · Fasted for 12 hours prior. Apply eye lubricant. Peak effects at 30 minutes.
- Sedation and analgesia · 375 micrograms/m2 body surface area (BSA) IV; 500 micrograms/m2 BSA IM · IV/IM · Single dose · Microgram/kg dosage decreases as body weight increases. Fast for 12 hours prior. Peak effects at 30 minutes.
- Preanesthetic · 125-375 micrograms/m2 IM · IM · Single dose · Accurate dosing not possible < 2 kg.
- Premed prior to propofol or face mask induction (geriatric/renal/liver dysfunction) · 62.5 micrograms/m2 · IM/IV · Single dose · Combine with equal volumes of opioid and ketamine.
- Slightly heavier sedation for radiographic procedures (ASA II or III) · 125 micrograms/m2 · IM/IV · Single dose · Combine with equal volumes of opioid and ketamine.
- Minor surgery, Penn hip or OFA-types of radiographic procedures · 250 micrograms/m2 · IM/IV · Single dose · Combine with equal volumes of opioid and ketamine.
- Surgical plane of anesthesia for OHE, castration, or abdominal surgery · 375 micrograms/m2 · IM/IV · Single dose · Combine with equal volumes of opioid and ketamine. Lateral recumbency in 5-8 minutes.
- Immobilizing extremely fractious dogs and wolf-hybrid dogs · 500 micrograms/m2 · IM · Single dose · Combine with equal volumes of opioid and ketamine. Rarely required.
วิธีการให้ยา
ข้อห้ามใช้
- Cardiovascular disease
- Respiratory disorders
- Liver or kidney diseases
- Shock or severe debilitation
- Stress due to extreme heat, cold, or fatigue
- Puppies < 16 weeks (US label) or < 6 months (UK label)
- Kittens < 12 weeks (US label) or < 5 months (UK label)
- Hypersensitivity to the active substance
อาการไม่พึงประสงค์
- Bradycardia (profound)
- Occasional AV blocks
- Decreased respiration / Apnea
- Hypothermia
- Urination
- Vomiting
- Hyperglycemia
- Pain on injection (IM)
- Prolonged sedation
- Paradoxical excitation
- Hypersensitivity
- Pulmonary edema
- Death from circulatory failure (rare)
- Muscle tremors
- Transient hypertension
- Reduced tear production
อันตรกิริยาระหว่างยา
- Anesthetics, Opiates, Sedative/Hypnotics · Effects may be additive; dosage reduction of one or both agents may be required. General anesthetic requirements may be reduced between 30-60%.
- Atropine, Glycopyrrolate · Can significantly increase arterial blood pressure and heart rate; use together is not recommended in dogs due to increased cardiac workload.
- Epinephrine · Possesses alpha agonist effects; do not use to treat cardiac effects caused by dexmedetomidine.
- Yohimbine · May reverse the effects, but atipamezole is preferred for clinical use.
การติดตาม
- Level of sedation and analgesia
- Heart rate and rhythm
- Blood pressure
- Respiration rate and pulse oximetry
- Body temperature (monitor for hypothermia)
การได้รับยาเกินขนาด
Single doses of up to 5X (IV) and 10X (IM) were tolerated in dogs, but adverse effects (heart block, PVCs, tachycardia, profound sedation) can occur. > **Important:** Treatment of dexmedetomidine-induced bradycardia with anticholinergic agents (atropine or glycopyrrolate) is usually **not recommended** due to the risk of severe hypertension and arrhythmias. **Atipamezole** is the safest and most effective choice to reverse any dexmedetomidine-induced effects or overdose.
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