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Aripiprazole

Antipsychotic Agents
CATEGORIES

Antipsychotic Agents


ALIASES

ABILIFY MAINTENA, Abilify, Abilify Maintena Kit, Aripiprazol Krka, Aripiprazol STADA, Aripiprazole Accord, Aripiprazole Amneal, Aripiprazole Medical Valley, Aripiprazole Sandoz, Aripiprazole Teva, Lemilvo


SUBSTANCES

aripiprazole, aripiprazole monohydrate


ENVIRONMENTAL CONCERN: MODERATE
Aripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.

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MODERATE
No measurements of aripripazole have been reported from wastewater or the external environment, either in Sweden or abroad. However, the reason may be that no one has specifically searched for the substance. Aripiprazole is slowly degraded in the environment.

In the literature there are contradictory fat solubility data for alimemazine reported. However, several independent sources report an estimated fat solubility (logPow) above 4, indicating that the substance has a high potential for bioaccumulation.

Comparison with flupentixol, haloperidol and risperidone
Both haloperiodol and risperidone have been reported in wild Swedish fish at levels above therapeutic concentrations in humans, which is also reasonable based on their high fat solubility and measured concentrations in Swedish wastewater. There is also a risk that flupentixol may accumulate in fish close to therapeutic concentration. Flupentixol, haloperidol and risperidone are all included in the Stockholm County Council's table of pharmaceuticals with risk for negative environmental impact according to the environmental program 2017-2021. The risk of aripripazole accumulating in fish at potent levels is estimated to be lower.

The risk classification insignificant, according to Fass.se, is based on total sold amount (kg) of the substance in Sweden during the year 2015 and the toxicity of the substance.

REFERENCES

  1. UBA, The Umweltbundesamt. Database - Pharmaceuticals in the environment.
  2. Stockholms läns landsting. Förteckning över miljöbelastande läkemedel inklusive åtgärdsförslag framtagen inom ramen för SLL:s miljöprogram 2017–2021.
  3. Schulz M, Schmoldt A. Therapeutic and toxic blood concentrations of more than 800 drugs and other xenobiotics. Pharmazie. 2003;58:447-74.
  4. DrugBank-aripiprazol. Canada.
  5. Fick J, Lindberg RH, Tysklind M, Larsson DG. Predicted critical environmental concentrations for 500 pharmaceuticals. Regul Toxicol Pharmacol. 2010;58:516-23.
  6. Fass.se för vårdpersonal