Medical Genetics Summaries [Internet].
View in own window. Table is adapted from a FDA-approved drug label for aripiprazole 2. Aripiprazole is an atypical antipsychotic primarily used in the treatment of abilify patient information sheet kansas and bipolar disorder. The first antipsychotics to be discovered abilify patient the s information sheet kansas information sheet kansas and chlorpromazine.
However, prominent adverse effects included extrapyramidal side effects such as tardive dyskinesia, muscle rigidity, tremors, and Parkinsonian-like symptoms. However, many have serious metabolic effects.
Coumadin dosage 4 mg is an atypical antipsychotic that is noted for abilify patient information sheet kansas fewer metabolic side effects than other atypicals, such as clozapine, olanzapine, risperidone, and quetiapine. Other atypicals currently approved by the FDA information sheet kansas asenapine, brexpiprazole, cariprazine, lurasidone, paliperidone, and ziprasidone.
The main action of both first-generation and second-generation antipsychotics is thought to be the post-synaptic blockade of D2 dopamine receptors. All antipsychotics, with the exception of aripiprazole, are D2 antagonists.
Aripiprazole is a partial D2 agonist. Aripiprazole binds to the D2 receptor with a high affinity similar to dopamine.
However, because it has low intrinsic activity, it causes much lower activation of the receptor abilify patient information sheet kansas to dopamine. Overactivity in this region is thought to abilify patient information sheet kansas psychosis and abilify patient information sheet kansas positive symptoms of schizophrenia.
In addition, the preservation of some D2 receptor activity click here other dopamine-rich pathways in the brain mesocortical and nigrostriatal areas may provide more protection against extrapyramidal side effects 3, 4.
Aripiprazole also has a high affinity for the serotonin 5-HT 2A receptors, where it acts as an antagonist and it moderately blocks the alpha 1 adrenergic and histamine H1 receptors, which may account abilify patient information the lower incidence of orthostatic hypotension and sedation compared to other antipsychotics 5. Adverse events to aripiprazole include increased mortality in elderly patients with psychosis abilify patient information sheet kansas by dementia, suicidal thoughts and behavior in sheet kansas and young adults, neuroleptic malignant syndrome, and tardive dyskinesia 2.
Aripiprazole activity is thought to be primarily due to the parent drug, information sheet kansas to a lesser extent its major metabolite, dehydro-aripiprazole.
The mean elimination half-life is about 75 hours for aripiprazole, but in individuals who have no appreciable CYP2D6 activity poor metabolizersthe mean elimination half-life for aripiprazole is abilify patient information sheet kansas hours.
Genetic variations in the CYP2D6 gene abilify patient information sheet kansas been found to impact serum levels of aripiprazole 6, 7. Because standard doses of aripiprazole lead to higher plasma levels of aripiprazole and dehydro-aripiprazole, the dose of aripiprazole should be adjusted in subjects carrying two nofunction alleles causing poor metabolizer status. The FDA recommends that patients who are known to be CYP2D6 poor metabolizers should receive half the standard dose of aripiprazole, or a quarter of the standard dose if they are also taking medicines that strongly inhibit CYP3A4 e.
This study also suggested that individuals with /methotrexate-and-infections-lung-disease.html CYP2D6 activity ultrarapid metabolizers may need to take an alternative antipsychotic not metabolized by CYP2D6 because of reduced drug levels 8.
The cytochrome P superfamily Abilify patient information sheet kansas is a large and diverse group of enzymes that form the major system for metabolizing abilify patient, hormones, toxins, and drugs. The CYP genes are highly polymorphic and can result in no, decreased, normal or increased enzyme activity.
For a detailed abilify patient information sheet kansas of CYP2D6 alleles, abilify patient information sheet kansas see abilify patient information sheet kansas.
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