Haloperidol decanoate steady state

Haloperidol is a typical butyrophenone type antipsychotic that exhibits high affinity dopamine D 2 receptor antagonism and slow receptor dissociation kinetics. [42] It has effects similar to the phenothiazines . [17] The drug binds preferentially to D 2 and α 1 receptors at low dose (ED 50 = and  mg/kg, respectively), and 5-HT 2 receptors at a higher dose (ED 50 =  mg/kg). Given that antagonism of D 2 receptors is more beneficial on the positive symptoms of schizophrenia and antagonism of 5-HT 2 receptors on the negative symptoms, this characteristic underlies haloperidol's greater effect on delusions, hallucinations and other manifestations of psychosis. [43] Haloperidol's negligible affinity for histamine H 1 receptors and muscarinic M 1 acetylcholine receptors yields an antipsychotic with a lower incidence of sedation, weight gain, and orthostatic hypotension though having higher rates of treatment emergent extrapyramidal symptoms .

Given these considerations, antipsychotic drugs should be prescribed in a manner that is most likely to minimize the occurrence of tardive dyskinesia. Chronic antipsychotic treatment should generally be reserved for patients who suffer from a chronic illness that 1) is known to respond to antipsychotic drugs, and 2) for whom alternative, equally effective, but potentially less harmful treatments are not available or appropriate. In patients who do require chronic treatment, the smallest dose and the shortest duration of treatment producing a satisfactory clinical response should be sought. The need for continued treatment should be reassessed periodically.

Decanoic acid acts as a non-competitive AMPA receptor antagonist at therapeutically relevant concentrations, in a voltage- and subunit-dependent manner, and this is sufficient to explain its antiseizure effects. [12] This direct inhibition of excitatory neurotransmission by decanoic acid in the brain contributes to the anticonvulsant effect of the MCT ketogenic diet . [12] Decanoic acid and the AMPA receptor antagonist drug perampanel act at separate sites on the AMPA receptor, and so it is possible that they have a cooperative effect at the AMPA receptor, suggesting that perampanel and the ketogenic diet could be synergistic. [12]

Haloperidol decanoate steady state

haloperidol decanoate steady state

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