GABA Agonists Drug Class

The GABA agonists are a wide family of drugs employed for an even wider family of conditions. There are two main types of GABA receptor – GABA A and GABA B – and this distinction determines the activity of the drug. For example, the drug baclofen is an agonist at GABA B receptors, and is therefore used in conditions such as muscle spasticity and alcoholism. Many drugs act as agonists at GABA A receptors, such as benzodiazepines, non-benzodiazepines, and anaesthetics. Though the use of GABA A agonists is not limited to these classes, these three groups typify what is classically considered a GABA A drug. GABA A agonists are associated with properties such as sedation, muscle relaxation, anticonvulsant activity, and anxiolytic effects. GABA is an important inhibitory neurotransmitter in the brain and agonists augment this inhibitory effect. As a result, conditions such as epilepsy – which involves over-activity in the brain – can be curbed through administration with a GABA A agonist. As a consequence, their side-effects are also associated with drowsiness, dizziness, and concentration difficulties. However, these drugs have proven to be an enduring class not least because of how effective they are against a wide range of ailments.

GABA Agonists Drugs

Below you will find a list of drugs that fall under the class of GABA Agonists.

GABA Agonists Uses

The use of the GABA A agonist will depend on which specific class of drugs are involved.

If the GABA A agonists are, for example, benzodiazepines, they will be used in the treatment of conditions such as anxiety, depression, alcoholism, seizures, insomnia, and panic attacks. Their use is by no means limited to these conditions but these are the general parameters by which these drugs are typically prescribed.

If, however, the GABA A agonists are drugs such as etomidate or propofol, they will be employed as general anaesthetics. Both of these drugs are actively used in general anaesthesia to this day, with etomidate used for the induction of anaesthesia, and propofol used for both the induction and maintenance of anaesthesia throughout the operation.

The Z-Drugs are also examples of GABA A agonists. This family of drugs includes Zolpidem, Zaleplon, and Zopiclone. All three of these drugs are used in the short-term treatment of insomnia.

GABA Agonists Side Effects

Side-effects from all GABA A drugs are relatively consistent. Patients can expect to experience:

  • drowsiness
  • concentration and memory difficulties
  • dizziness
  • reduction in libido

One of the main problems with the benzodiazepine class in particular are their preponderance to toleration and dependence. This means that more of the drug will be required to deliver the necessary therapeutic effect, though this is at the risk of the patient becoming dependent on the drug in question. Z-drugs suffer from the same side-effects, though these drugs are only usually prescribed on a short-term basis; in order to establish the underlying cause of the inability to sleep effectively.

GABA Agonists Interactions

Given that GABA A agonists have the property of muscle relaxation, these drugs should be avoided in patients with respiratory difficulties. If GABA A agonists are prescribed for the treatment of either anxiety or depression, aggressive or suicidal behaviour may result. This is a serious warning and patients should be closely monitored as a result.

GABA A agonists should be avoided wherever possible in those who are pregnant. The side-effect risks are exacerbated in elderly patients, who eliminate these drugs at a slower rate than younger patients. GABA A agonists interact with alcohol, opiate drugs, and other GABA A drugs to increase the risk of respiratory depression, lethargy, and rebound insomnia.