Minaxolone

Minaxolone is a sedative and anesthetic drug that was developed in the 1970s. It is a steroid derivative, specifically a neuroactive steroid, which acts as a positive allosteric modulator of the GABAA receptor. Minaxolone was developed as a safer alternative to the barbiturate anesthetics which were in common use at the time, but was withdrawn from use after it was found to cause jaundice in some patients.

Pharmacology

Minaxolone acts as a positive allosteric modulator of the GABAA receptor, enhancing the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at this receptor. This results in sedative and anesthetic effects. As a neuroactive steroid, minaxolone has a different mechanism of action from most other anesthetics, which typically act by blocking sodium channels.

History

Minaxolone was developed in the 1970s as a safer alternative to the barbiturate anesthetics which were in common use at the time. However, it was withdrawn from use after it was found to cause jaundice in some patients.

Side effects

The most serious side effect of minaxolone is jaundice, which led to its withdrawal from use. Other side effects may include drowsiness, confusion, and loss of coordination.

See also

• List of neuroactive steroids
• List of GABAA receptor positive allosteric modulators

Minaxolone Resources
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