GABAA receptor antagonists, inverse agonists or negative allosteric modulators
GABAA receptor antagonists are drugs that bind to
GABAA receptors but do not activate them and inhibit the action of GABA. Thus it blocks both the endogenous and exogenous actions of GABAA receptor agonists.[18][19]
Camphor injections for psychiatric treatment were inefficient and were replaced by
pentylenetetrazol. Seizures induced by chemicals like flurothyl were clinically effective as electric convulsions with lesser side effects on memory retention. Therefore, considering flurothyl induced seizures in modern anesthesia facilities is encouraged to relieve medication treatment resistant patients with psychiatric illnesses like mood disorders and catatonia.[10]
Risks/Complications
Convulsants like
pentylenetetrazol and
flurothyl were effective in psychiatric treatment but difficult to administer. Flurothyl was not widely being used due to the persistence of the ethereal aroma and fears in the professional staff that they might seize.[10]
History
In 1934, camphor-induced and pentylenetetrazol-induced brain seizures were first used to relieve psychiatric illnesses. But camphor was found ineffective. In 1957, inhalant anesthetic flurothyl was tested and found to be clinically effective in the induction of seizures, even though certain risks persisted.[10]
^Calabrese EJ (2008). "Modulation of the epileptic seizure threshold: implications of biphasic dose responses". Critical Reviews in Toxicology. 38 (6): 543–56.
doi:
10.1080/10408440802014261.
PMID18615309.
S2CID5081215.
^de Araujo Furtado M, Rossetti F, Chanda S, Yourick D (December 2012). "Exposure to nerve agents: from status epilepticus to neuroinflammation, brain damage, neurogenesis and epilepsy". Neurotoxicology. 33 (6): 1476–1490.
doi:
10.1016/j.neuro.2012.09.001.
PMID23000013.
^Galland, M. C.; Griguer, Y.; Morange-Sala, S.; Jean-Pastor, M. J.; Rodor, F.; Jouglard, J. (1992). "Convulsions fébriles : faut-il contre-indiquer certains médicaments ?" [Febrile convulsions: should some drugs be contraindicated?]. Thérapie (in French). 47 (5): 409–414.
PMID1363740.
INIST3915621.
^
abcdCooper, Kathryn; Fink, Max (October 2014). "The Chemical Induction of Seizures in Psychiatric Therapy: Were Flurothyl (Indoklon) and Pentylenetetrazol (Metrazol) Abandoned Prematurely?". Journal of Clinical Psychopharmacology. 34 (5): 602–607.
doi:
10.1097/JCP.0000000000000173.
PMID25029329.
S2CID23735035.
^Löscher W (June 2002). "Animal models of epilepsy for the development of antiepileptogenic and disease-modifying drugs. A comparison of the pharmacology of kindling and post-status epilepticus models of temporal lobe epilepsy". Epilepsy Research. 50 (1–2): 105–23.
doi:
10.1016/s0920-1211(02)00073-6.
PMID12151122.
S2CID5930079.
^Löscher W (May 2009). "Preclinical assessment of proconvulsant drug activity and its relevance for predicting adverse events in humans". European Journal of Pharmacology. 610 (1–3): 1–11.
doi:
10.1016/j.ejphar.2009.03.025.
PMID19292981.
^Rubio C, Rubio-Osornio M, Retana-Márquez S, Verónica Custodio ML, Paz C (December 2010). "In vivo experimental models of epilepsy". Central Nervous System Agents in Medicinal Chemistry. 10 (4): 298–309.
doi:
10.2174/187152410793429746.
PMID20868357.