Alfadolone

Alphadolone.svg

Alfadolone is a neuroactive steroid used in veterinary medicine as an anesthetic agent. It is commonly used in combination with alfaxalone to produce a neurosteroid anesthetic known as Althesin. Alfadolone is known for its rapid onset and short duration of action, making it suitable for procedures requiring quick recovery times.

Chemical Structure and Properties

Alfadolone is a synthetic steroid with a chemical structure similar to that of naturally occurring progesterone. It is classified as a neurosteroid due to its ability to modulate GABA_A receptors, which are responsible for its anesthetic properties.

Mechanism of Action

Alfadolone exerts its effects by enhancing the activity of the gamma-aminobutyric acid (GABA) neurotransmitter at the GABA_A receptor. This action increases the inhibitory effects of GABA, leading to sedation, anesthesia, and muscle relaxation.

Clinical Use

In veterinary practice, alfadolone is used primarily for the induction and maintenance of anesthesia in small animals. It is often administered intravenously and is valued for its rapid onset and short duration of action. The combination of alfadolone and alfaxalone in Althesin provides a balanced anesthetic effect with minimal cardiovascular and respiratory depression.

Side Effects and Precautions

While alfadolone is generally well-tolerated, it can cause side effects such as hypotension, respiratory depression, and allergic reactions. Careful monitoring of the animal's vital signs is essential during its use. It is contraindicated in animals with known hypersensitivity to steroids or those with severe liver disease.

Pharmacokinetics

Alfadolone is rapidly metabolized in the liver and excreted primarily in the urine. Its short half-life contributes to its quick recovery profile, making it an ideal choice for short surgical procedures.

History and Development

Alfadolone was developed in the 1970s as part of the search for safer and more effective anesthetic agents. Its combination with alfaxalone in Althesin represented a significant advancement in veterinary anesthesia, providing a reliable and controllable anesthetic option.

See Also

• Alfaxalone
• Neurosteroid
• GABA_A receptor
• Veterinary anesthesia