Afloqualone

Afloqualone

Afloqualone is a quinaldine derivative and a more potent analogue of the muscle relaxant methaqualone. It acts as a sedative and muscle relaxant due to its agonist activity at the GABAa receptor, a class of receptors on which the major inhibitory neurotransmitter in the human central nervous system, gamma-aminobutyric acid (GABA), also acts. Afloqualone was developed in the 1980s in Japan as a treatment for muscle stiffness and spasm, particularly in conditions such as spinal cord injury and cerebrovascular accidents. It is known under the brand name Arofuto.

Pharmacology

Afloqualone binds to a specific site on the GABAa receptor, enhancing the effect of GABA by increasing the frequency of chloride channel opening within the receptor complex. This action leads to hyperpolarization of the neuron, making it less likely to fire action potentials and thus has an overall inhibitory effect on neurotransmission. This mechanism is similar to that of other sedative-hypnotic drugs like benzodiazepines, although the binding site and exact effect on the receptor may vary.

Clinical Use

Afloqualone is indicated for the treatment of conditions associated with muscle tension and spasm. It has been particularly useful in patients with spinal cord injuries or diseases affecting the central nervous system that lead to spasticity. Its muscle relaxant properties help in alleviating the discomfort and pain associated with these conditions. However, its use is generally limited to short-term treatment due to the risk of dependency and tolerance with long-term use.

Side Effects

The side effects of afloqualone can include dizziness, nausea, headache, and fatigue, which are common to many central nervous system depressants. More serious side effects may include dependency, withdrawal symptoms upon cessation, and the potential for overdose, particularly when combined with other central nervous system depressants like alcohol or benzodiazepines.

Legal Status

The legal status of afloqualone varies by country, with it being strictly controlled in some jurisdictions due to its potential for abuse and addiction. In countries where it is available, it is usually a prescription-only medication.

Conclusion

Afloqualone is a potent muscle relaxant and sedative drug that has found use in the treatment of conditions associated with muscle spasm and stiffness. While effective, its use must be carefully managed to avoid the risk of side effects, dependency, and abuse.