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1. Acamprosate, N-acetyl homotaurine, Campral
Acamprosate works by antagonizing glutamatergic N-methyl-D-aspartate receptors and agonizing gamma-aminobutyric acid (GABA) type α receptors. Certain serious side effects include diarrhea, allergic reactions, irregular heartbeats, and low or high blood pressure, while less serious side effects include headaches, insomnia, and impotence. Drugs.com.
2. Carisoprodol, SOMA, Carisoma, Sanoma
Carisoprodol is a centrally acting skeletal muscle relaxant that works by blocking pain sensations between the nerves and the brain. Effects include analgesia, anxiolysis, muscle relaxation (and relief from hypertonia), sedation, and somnolence. The usual dose of 350 mg is unlikely to engender prominent side effects other than somnolence, and mild to significant euphoria or dysphoria, but the euphoria is generally short lived. The intensity of the side effects of carisoprodol tends to lessen as therapy continues. Drugs.com.
3. Etaqualone, Aolan, Athinazone, Ethinazone
Etaqualone is an analogue of methaqualone. It has sedative, hypnotic, muscle relaxant, and central nervous system depressant properties, and was used for the treatment of insomnia. Drugs.com.
4. Kava Kava
Kava is a plant whose roots are used to produce a drink with sedative and anesthetic properties. Kava is sedating and is primarily consumed to relax without disrupting mental clarity. Research has suggested that kavalactones potentiate GABA-α activity, but do not alter levels of dopamine and serotonin in the CNS. It is thought modulate GABA activity by altering the lipid membrane structure and sodium channel function. There are serious safety concerns. Many cases of liver damage and even some deaths have been traced to kava use. It is used in many over-the-counter preparations and should be avoided. Drugs.com.
5. Methaqualone, Quaalude
Methaqualone is a sedative-hypnotic drug that is similar in effect to barbiturates, a general central nervous system depressant that increases the activity of the GABA receptors in the brain and nervous system. When GABA activity is increased, blood pressure drops and breathing and pulse rates slow, leading to a state of deep relaxation. Methaqualone’s effects generally last four to eight hours. Regular users build up a physical tolerance, requiring larger doses for the same effect. Overdose can lead to nervous system shut down, coma, and death. Effects can include euphoria, drowsiness, reduced heart rate, reduced respiration, increased sexual arousal (aphrodisia), and paresthesias (numbness of the fingers and toes). Larger doses can bring about respiratory depression, slurred speech, headache, and photophobia (excessive sensitivity to light). Drugs.com.
6. Methocarbamol, Robaxin, Robaxacet, Tylenol Body Pain Night, Robax Platinum, Robaxisal
Methocarbamol is a central muscle relaxant used to treat skeletal muscle spasms. Methocarbamol produces its clinical effects through agonism of the GABA receptor. Activation of the GABA receptor increases the amount of chloride ions that pass through the chloride channel of cells, resulting in a depressant effect by reducing the cells action potential (like dimming a light, the cell continues to function but at a lower capacity). Most GABAergics require GABA as a co-factor in order to activate the chloride channel. However, methocarbamol can activate the chloride channel in the absence of GABA; this ability is called direct agonism (as opposed to allosteric agonism) and is relatively rare among GABAergic drugs, being shared only by other carbamate derivatives and a handful of other substances. Drugs.com.
7. Muscimol, agarin, pantherine
Muscimol is the major psychoactive alkaloid present in many mushrooms of the Amanita genus. Muscimol binds to the same site on the GABA-α receptor complex as GABA itself, as opposed to other GABAergic drugs such as barbiturates and benzodiazepines which bind to separate regulatory sites. Muscimol alters neuronal activity in multiple regions including the cerebral cortex, hippocampus, and cerebellum. Muscimol is also a partial agonist at the GABA-α-rho receptor, and so its range of effects results from a combined action at both targets. In patients with Huntington's disease and chronic schizophrenia, oral doses of muscimol have been found to cause a rise of both prolactin and growth hormone. Many of muscimol's effects are consistent with its pharmacology as a GABA-α receptor agonist, presenting many depressant or sedative-hypnotic effects. Muscimol can cause dissociative hallucinations. Drugs.com.
8. Progabide, Gabrene
Progabide is an analog and prodrug of gamma-aminobutyric acid used in the treatment of epilepsy. It has agonistic activity at the GABA-α, GABA-β, and GABA-ρ receptors. Progabide has been investigated for many diseases besides epilepsy, including Parkinson's disease, schizophrenia, clinical depression, anxiety disorder, and spasticity with various levels of success. Wikipedia.
9. Propofol, Diprivan
Propofol is a short-acting, intravenously administered hypnotic/amnestic agent. Propofol has been proposed to have several mechanisms of action both through potentiation of GABA-α receptor activity, thereby slowing the channel-closing time, and also acting as a sodium channel blocker. Recent research has also suggested that the endocannabinoid system may contribute significantly to Propofol's anesthetic action and to its unique properties. Patients show great variability in their response to Propofol, at times showing profound sedation with small doses. A more serious but rare side effect is dystonia. Mild myoclonic movements are common, as with other intravenous hypnotic agents. This is for professional use only. Since it is used as an anesthetic agent for procedures and surgeries, it is important that the anesthesiologist is aware of the other GABA-ergic drugs you take. Drugs.com.
1. Hattan E, Angle MR, Chalk C. Unexpected benefit of propofol in stiff person syndrome. Neurology 2007;70:1641.
10. Scullcap
Scutellaria barbata, and Sculletaria laterifolia, also known as skullcap, helmetflower, hoodwort, and mad-dog weed, are a species of flowering plant in the mint family, Lamiaceae. It has been tested in clinical trials for the treatment of metastatic breast cancer. Extracts induced apoptosis in prostate cancer cells in laboratory studies. The plant is used as an herbal remedy for inflammation and traumatic injury. It may inhibit pituitary and chorionic gonadotropins, as well as prolactin. It is used in many over-the-counter preparations and should be avoided. Drugs.com.
11. Valerian
Valeriana officinalis has a calming effect, likely by indirectly promoting GABAergic activity. Crude extract of the root is often sold in the form of capsules. Valerian root has sedative and anxiolytic effects. It can also be classified as a drug, since its consumption produces a sedative or medicinal effect, while it is not exclusively a type of food. The amino acid valine is named after this plant. The mechanism of action of valerian in general, and as a mild sedative in particular, has not been fully elucidated, but it is generally believed that some of the GABA-analogs particularly valerenic acids as components of the essential oil along with other semi-volatile sesquiterpenoids appear to have some affinity for the GABA-α receptor. It is used in over-the-counter preparations and should be avoided. Drugs.com.
12. Valproate, Depakote/, Depakote ER, Depakene, Depakene Crono, Depacon, Depakine, Valparin, Stavzor.
Valproate’s mechanism of action includes enhanced neurotransmission of GABA by inhibiting GABA transaminase, which breaks down GABA. Valproic acid was first synthesized in 1882 by B.S. Burton as an analogue of valeric acid, found naturally in valerian. As an anticonvulsant, valproic acid is used to control absence seizures, tonic-clonic seizures (grand mal), complex partial seizures, juvenile myoclonic epilepsy, and the seizures associated with Lennox-Gastaut syndrome. It is also used in treatment of myoclonus. In some countries, parenteral preparations of valproate are used also as second-line treatment of status epilepticus as an alternative to phenytoin. Valproate is one of the most common drugs used to treat post-traumatic epilepsy. It is more recently being used to treat neuropathic pain, as a second-line agent, particularly lancinating pain from A delta fibers. Its anticonvulsant effect has been attributed to the blockade of voltage-dependent sodium channels and increased brain levels of gamma-aminobutyric acid (GABA). The GABAergic effect is also believed to contribute towards the anti-manic properties of valproate. Drugs.com.
1. Spehlmann R, Norcross K, Rasmus SC, et al.: Improvement of stiff-man syndrome with sodium valproate. Neurology 1981, 31:1162–1163. Link to article.
GABA-α AGONISTS