Mecloqualone

Mecloqualone is a quinazolinone class GABAergic and is an analogue of methaqualone that was first made in the 1960s and marketed mainly in France and some other European countries. It has sedative, hypnotic, and anxiolytic properties caused by its agonist activity at the β subtype of the GABAa receptor and was used for the treatment of insomnia.

Pharmacology

Mecloqualone is a central nervous system depressant that enhances the activity of the GABA neurotransmitter. It does this by binding to the GABAa receptor at the β1 subtype, which makes the receptor have a greater affinity for the GABA neurotransmitter. This increases the frequency of opening of the associated Chloride ion channel and hyperpolarizes the membrane of the neuron. This results in a decrease in neuronal excitability.

History

Mecloqualone was developed by a team at William S. Merrell Company in the 1960s. It was introduced to the French market by Theraplix under the brand name Méquinol in 1965. It was marketed as a safer alternative to barbiturate drugs, although it has largely been withdrawn from use due to problems with abuse and dependence. It is still occasionally prescribed on a very limited basis, particularly in patients with severe insomnia who have not responded to other treatments.

Side effects

Side effects of mecloqualone include dizziness, nausea, vomiting, confusion, and seizures. Long-term use can result in tolerance, dependence, and withdrawal symptoms on discontinuation.

Legal status

Mecloqualone is a controlled substance in many countries due to its potential for abuse. In the United States, it is a Schedule I drug under the Controlled Substances Act. In Canada, it is a Schedule III drug under the Controlled Drugs and Substances Act.

See also

• Methaqualone
• Afloqualone
• Etaqualone
• Mebroqualone
• Methylmethaqualone

Sedatives and Hypnotics

• Antihistamines
• Diphenhydramine
• Doxylamine
• Hydroxyzine

• Barbiturates
  • Amobarbital
  • Butabarbital
  • Phenobarbital
  • Secobarbital

• Benzodiazepines
  • Diazepam
  • Estazolam
  • Flurazepam
  • Quazepam
  • Temazepam
  • Triazolam

• Benzodiazepine Receptor Agonists
  • Eszopiclone
  • Zaleplon
  • Zolpidem

• Herbals
  • Chamomile (Matricaria recutita)
  • Hops (Humulus lupulus)
  • Lavender (Lavandula angustifolia)
  • Passionflower (Passiflora incarnata)
  • Valerian (Valeriana officinalis)

• Melatonin and its Analogues
  • Melatonin
  • Ramelteon
  • Tasimelteon

Miscellaneous Agents

• • Buspirone
  • Chloral hydrate
  • Doxepin
  • Meprobamate
  • Sodium Oxybate (Narcolepsy Agent)
  • Suvorexant

 

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