www.thetinman.org Copyright © All rights reserved.
GABA-transaminase inhibitors bind to enzymes and decreases their activity. Blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance.
w Phenelzine, Nardil, Nardelzine
w Vigabatrin, Sabril
w Lemon balm (Melissa officinalis).
GABA analogues mimic the activity of GABA and typically have relaxing, anti-anxiety, and anti-convulsive effects. Many of the substances are known to cause
anterograde amnesia and retrograde amnesia.
w Gabapentin,Neurontin, Gabarone
w Gabapentin enacarbil, Regnit, Horizant
w Hopantenic acid, homopantothenic acid, Pantogam
w Pregabalin, Lyrica
GABA supplements. Medical literature is pretty clear that there is little chance that GABA taken orally will penetrate the blood-brain barrier. However, there is evidence that GABA administered through an IV or intramuscular injection will penetrate the blood-brain barrier. This is not currently used as a treatment but is used for research.
Muscle relaxers have not proven to help as much with spasms or stiffness, but are prescribed.
w Dantrolene, Dantrium, Dantamacrin, Dantolen
w Carbamazepine, Tegretol, Equetro
w Cyclobenzaprine, Flexeril, Flexmid, Amrix
w Metaxalone, Skelaxin
w Methocarbamol, Robaxin
w Tizanidine, Zanaflex, Sirdalud
Corticosteroids are sometimes used in combination with GABAergic drugs to treat spasms and autoimmune disease.
w Hydrocortisone, hydrocortisone acetate
w Cortisone acetate
w Tixocortal pivalate, Pivalone
w Prednisone Continue Reading
Anti-seizure medications are used to treat co-morbid epilepsy and seizure disorders.
w Levetiracetam, Keppra.
w Stiripentol, Diacomet
w Oxcarbazepine, Trileptal
w Eslicarbazepine acetate, Aptiom, Zebinix, Exalief
w Depecon, Valproate
w Ethotoin, Pegnanone
w Phenytoin, Dilantin, Phenytek, et al.
w Fosphenytoin, Prodilantin, Cerebyx
w Zaleplon, Sonata, Starnoc, Andante
w Zopiclone, Zimovane, Imovane, Lunesta
Opiate analgesics treat pain, but are not advised for long-term treatment.
w Demerol, meperidine, Pethidine
w Fentanyl, Actiq, Durogesic, et al.
w Hydrocodone, Norco, Vicodin, Lortab
w Morphine (numerous brand names)
w Nucynta, tapentadol, Palexia, TAPAL
w Oxycodone, Oxecta, OxyCONTIN, et al.
w Propoxyphene, Darvon, Darvocet et al.
w Tramadol, Ultram, Tramol
UNDERSTANDING GABA-ERGIC DRUGS
In simplistic terms, GABA is the major inhibitory neurotransmitter in the central nervous system. Glutamate is the major excitatory neurotransmitter. They act as the gas pedal and brakes along the neural network. Glutamate hastens the messages. GABA slows them down. GAD65 is necessary for the creation of GABA from glutamate. If antibodies kill off GAD65, it results in reduced production of GABA. The nervous system brakes fail and the neurotransmission speeds up (or does not slow down when required). In the spinal cord, a reduced level of GABA can lead to hyperexcitable motor neurons, rigidity, and spasms of both agonist and antagonist muscles. GAD65 antibodies have not proven to be the causative factor of SPS, but it is clear that the spasms and stiffness respond to treatment with GABA-ergic medications.
There are three receptors for gamma-aminobutyric acid (GABA). GABA-α and GABA-ρ receptors are ion channels that signal chloride and diminish further action potentials (quieting the neural noise). GABA-α and GABA-ρ receptors produce sedative and hypnotic effects as well as producing anti-convulsion properties. The GABA-β receptor belongs to the class of G-Protein coupled receptors that inhibit adenylate cyclase, therefore leading to decreased cyclic adenosine monophosphate (cAMP). GABA-β receptors also produce sedative effects and lead to changes in gene transcription.
Each type of GABA receptor can be activated by agonists, inactivated by antagonists, or supported by analogues.
GABA antagonists should be avoided. They reduce the amount of circulating GABA and would work against the GABA-enhancing drugs.
GABA-α antagonists include: bicuculline, cicutoxin,
flumazenil, furosemide, gabazine, oenanthotoxin, picrotoxin,
GABA-β antagonists include phaclofen and saclofen.
GABA-α agonists activate GABA-α receptors.
w Acamprosate, N-acetyl homotaurine, Campral
w Carisoprodol, Soma, Carisoma, Sanoma
w Etaqualone, Aolan, Athinazone, Ethinazone
w Kava kava
w Methaqualone, Quaalude
w Methocarbamol, Robaxin, Robaxacet et al.
w Muscimol, Agarin, Pantherine
w Progabide, Gabrene
w Propofol, Diprivan
w Valproate, Depakote, Depakene, et al.
GABA Positive Allosteric Modulators are not true GABA-α agonists, but bind to the GABA receptors. They cannot induce a response from the neuron without an actual agonist being present.
Alcohol (Ethanol) falls under this category and can substantially compound the effects of GABAergic drugs. They should not be taken together.
w Allobarbital, allobarbitone, Cibalgine, Dial-Ciba
w Amobarbital sodium, sodium Amytal
w Barbital, barbitone, Verona, Medinal
w Bromazepam, Lectopam, Lexotan, et al.
w Clonazepam, Klonopin, Rivotril, et al.
w Tranxene, chlorazepate, Novo-Clopate
w Chlordiazepoxidel, Librium, et al.
w Diazepam, Valium
w Flurazepam, Dalmane, Dalmadorm
w Lorazepam, Ativan, Orfidal
w Midazolam, Versed, Dormicum, Hypnovel
w Nitrazepam, Alodorm, Arem, Insoma, etc.
w Oxazepam, Serax, Alepam, Medopam, etc.
w Alprazolam, Xanax
GABA-β agonists stimulate GABA-β receptors.
w Baclofen, Kemstrol, Lioresal et al.
w GHB (γ-Hydroxybutyric acid)
w GHV (γ-Hydroxybutyric acid)
GABA-ρ agonists stimulate GABA-ρ receptors.
w GABOB (y-Amino-beta-hydroxybutyric acid)
w Progabide, Gabrene
GABA reuptake inhibitors block the action of the GABA acid transporters (GATs). This in turn leads to increased extracellular concentrations of GABA and therefore an increase in GABAergic neurotransmission.
w Hyperforin (found in St. John’s wort)
w Tiagabine, Gabitril
Warning: Never experiment with medications on your own. Take them only on the advice and under the supervision of medical professionals.