![]() ![]() haloperidol and quetiapine) may retain significant efficacy.Īntidepressants and mood stabilizers However, an antipsychotic with a substantial disparity in pharmacology (e.g. Having been on one or more antipsychotics for any appreciable amount of time results in dramatically reduced sensitivity to others with similar mechanisms of action. These drugs block dopamine receptors and some also block serotonin receptors (such as chlorpromazine, the first antipsychotic used clinically). As a result, somebody who is tolerant to benzodiazepines is more sensitive to barbiturates than vice versa. However, the barbiturates are also AMPA receptor blockers, and in addition interact with the nAChR and voltage-gated calcium channels. Convergence upon the GABA A receptor is why tolerance for one drug in the group will most likely cause cross-tolerance for the other drugs in the group. ![]() When these drugs are taken together, especially with ethanol (drinking alcohol), there is a disproportionate increase in toxicity because the effects of both occur simultaneously and add up since they act on the same receptor at different sites. Both of these mechanisms allow for influx of chloride ions. Benzodiazepine binding increases the binding of GABA and barbiturates maximize the time the pore is open. In addition to gamma-Aminobutyric acid (GABA) itself, the GABA A receptor can also bind barbiturates and benzodiazepines. Morphine, oxycodone, heroin, fentanyl, endogenous opioids ( endomorphins, enkephalins, dynorphins)Ĭocaine, amphetamine, methylphenidate, ephedrineĮxcitation of the GABA receptor produces an influx of negatively charged chloride ions, which hyperpolarizes the neuron and makes it less likely to give rise to an action potential. MAO inhibitors ( tranylcypromine, phenelzine, selegiline) tricyclic antidepressants ( imipramine), SSRIs ( fluoxetine, sertraline, paroxetine) Phenothiazines ( chlorpromazine), butyrophenones ( haloperidol), clozapine, aripiprazole
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