Medetomidine Hydrochloride
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Product Description
Medetomidine hydrochloride, the stable and water-soluble hydrochloride salt form of medetomidine, is a highly potent selective α₂-adrenergic receptor agonist widely utilized in veterinary medicine as a sedative, analgesic, and muscle relaxant. By inhibiting norepinephrine release in the central nervous system, it produces dose-dependent sedation, profound muscle relaxation, and effective pain relief, making it a cornerstone agent for procedural restraint and minor surgical interventions in species such as dogs and cats. Although it induces notable cardiopulmonary effects—including reduced heart rate, cardiac output, and tear production, alongside transient diuresis and minimal impact on electroretinographic responses—its overall clinical profile supports safe use when appropriate supportive measures, such as ocular lubrication or fluid monitoring, are applied.
Synthesis and Production
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CAS Number: 86347-14-0 (free base), 86347-15-1 (hydrochloride)
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Synthesis Methods: Medetomidine is synthesized by attaching an imidazole ring to a 2,3-dimethylphenyl group. The hydrochloride salt form is produced by reacting the free base with hydrochloric acid to enhance stability and solubility for injection.
Uses and Applications
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Veterinary Medicine:
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Sedative and Analgesic: Used primarily as a sedative and analgesic in animals, often combined with ketamine or butorphanol.
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Pre-Anesthetic: Used before general anesthesia to reduce the dose of other anesthetic agents required.
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Chemical Restraint: Used for the safe handling and immobilization of exotic animals, wildlife, and zoo species.
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Reversible Effects: The effects of medetomidine can be rapidly reversed using an alpha-2 antagonist such as atipamezole.
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Human Medicine:
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Dexmedetomidine: The active S-enantiomer of medetomidine, used for sedation of mechanically ventilated patients in ICUs and procedural sedation.
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Research:
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Pharmacological Research: Studied for its effects on α₂-adrenoceptor pathways.
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Properties and Characteristics
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Physical Properties:
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Appearance: White to off-white crystalline powder
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Solubility: Freely soluble in water and alcohol
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Melting Point: Approximately 173–176 °C (decomposes)
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Chemical Properties:
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pKa: ~7.1 (imidazole nitrogen)
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LogP (base): ~2.8
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Pharmacology:
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Class: α₂-Adrenoceptor agonist (racemic mixture; active enantiomer is dexmedetomidine)
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Mechanism: High selectivity for α₂ vs α₁ receptors (~1620:1), causes sedation, analgesia, muscle relaxation, and anxiolysis by inhibiting the release of norepinephrine.
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Effects: Reduces sympathetic tone, leading to bradycardia and hypotension (initial hypertension possible).
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Safety and Handling
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Toxicity: High potency, risk of overdose in non-target species.
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Human Exposure: Can cause profound sedation, bradycardia, and respiratory depression.
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Storage: Store at 15–30°C, protected from light.
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Disposal: Follow local regulations for pharmaceutical waste.
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Handling: Wear proper personal protective equipment (PPE) to avoid accidental absorption or inhalation.
Related Compounds
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Dexmedetomidine: Active S-enantiomer used in human medicine.
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Atipamezole: Specific reversal agent for medetomidine.
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Xylazine: Less selective α₂ agonist used in veterinary medicine.
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Clonidine: α₂ agonist used in human medicine as an antihypertensive.
Regulatory and Safety Information
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Controlled Substance: Medetomidine is a controlled substance in many jurisdictions due to its potential for abuse and risk of human sedation.
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Contraindications: Use with caution in animals with pre-existing heart, liver, or kidney disease.
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Human Hazard: Harmful if absorbed through the skin or inhaled. Accidental injection in humans can be life-threatening.