Uso del Aripiprazol

en Nios y
Adolescentes
Dra. Rhodis Pea
Psiquiatra
30 de julio 2016

Aripri

Aripiprazol

Objetivos
Breve historia

Mecanismo de accion.
Efectos secundarios
Interacciones medicamentosas
Indicaciones
Dosis

Aripri

Aripiprazol

Hola!

Aprobaciones en adultos
Aprobado en 2002 por la FDA para la
esquizofrenia.
En 2004 para el trastorno bipolar.
En el 2005 presentacin en solucin oral.
En el 2006 tabletas dispersables,
En el 2007 se lanza una inyeccin IM para la
agitacin, y la FDA lo aprueba como tratamiento
adjunto para el trastorno depresivo mayor.
En el 2015 se aprueba inyeccin de liberacin
extendida.

Soy Aripiprazol
Aprobaciones en nios y adolescentes
Derivado de la quinolinona.

U.S. Food and Drug Administration

En el 2007 fue aprobada su uso en

adolescentes de 13-17 aos con esquizofrenia.
En el 2008 en nios y adolescentes de 10-17
para el tratamiento agudo del trastorno bipolar.
Es aprobado en 2009 para la irritabilidad
asociada al trastorno del espectro autista de 617 aos.
En el 2014 para el Trastorno de Tourrete.

Porque es llamado antipsictico

atpico de tercera generacin?
Perfil farmacolgico algo singular
Llamado tambin el atpico de los
antipsicticos atpicos.
Aripiprazol es un agonista que acta en
varias reas cerebrales.

Aripri

Agonista parcial D2

Agonista parcial 5-HT1A

Antagonista 5-HT2A

Aripri

Aripiprazol

El aripiprazol tiene afinidad por una

amplia gama de receptores relevantes
del SNC:
Receptores
dopaminrgicos:
Alta afinidad
D2
D3
Receptores
serotoninrgicos:
Alta afinidad
5-HT1A
5-HT2A
5-HT2B
Moderada
5-HT7
afinidad

5-HT1D

Receptores
adrenrgicos:
Moderada
1A
afinidad
1B
2A
2C
Moderada
Receptores
afinidad

histamnicos:
H1

Bartolomeis A. et al. Update on the Mechanism of Action of Aripiprazole. CNS Drugs (2015) 29:773799

Que es un agonista
parcial?

Cuales son las implicaciones del agonismo

parcial D2?
Unin al receptor D2 con la misma
afinidad que dopamina, pero con
menor eficacia intrnseca.
La respuesta que detona es menor que
la dopamina pero mayor que un
antagonista.
Modula la neurotransmisin de vas
dopaminrgicas.
Puede disminuir la actividad en la va
mesolmbica, lo que reducira los sntomas
positivos.

Guzman F. Psychopharmacology Institute

Se postula que tiene habilidad para

aumentar la actividad dopaminrgica desde
un nivel subnormal a una actividad normal en
la va mesocortical mejorando los sntomas
negativos y cognitivos.

Accin molecular del aripiprazol en receptores D2

de dopamina: De agonismo parcial a selectividad
funcional
Los mltiples
funcionales
mediadosmediados
por los receptores
ha permitido
un
Los mltiples
efectos efectos
funcionales
del aripiprazol
por los D2
receptores
D2 ha
progresivo
en en
la conceptualizacin
del
de este
este
permitidocambio
un cambio
progresivo
la conceptualizacin
delmecanismo
mecanismode
de accin
accin de
fortaleciendo
la hiptesis
de una
modulacin
selectivafuncional
funcional
frmaco,frmaco,
fortaleciendo
la hiptesis
de una
modulacin
selectiva
dependiente
dependiente
de D2. de D2.
Puede actuar como un agonista completo o antagonista completo dependiendo al
contexto en el cual su funcin es investigada; estas caractersticas son nicas
comparados
con otros
agonistasthat
parciales.
However,
the observation
aripiprazole elicits multiple
D2R-mediated functional effects encompassing the
Por lo tanto,
sidoofconsiderado
como
unhas
ligando
funcionalmente
selectivo; esto es un
wholeharange
pharmacological
traits
enabled
a progressive
farmaco shift
queinpuede
mostrar actividad
intrinsecaofdiferente en diferentes subclases de
the conceptualization
of the mechanism
receptores
enoflathis
sinapsis,o
que puede
efectos
action
drug, strengthening
thecausar
hypothesis
of a funcionales multiples, aun cuando
interactua
con el mismo
functional
selectiverecptor.
modulation of D2R-dependent specific
downstream signaling pathways [45, 46].
Aripiprazole may act as a complete
full agonist or a full antagonist according to the context in
Bartolomeis A. et al. Update on the Mechanism of Action of Aripiprazole. CNS Drugs (2015) 29:773799
which its functions are investigated; these features are

 Numerosas evidencias sugieren que el aripiprazol

actua en los receptores D2 impactando el sistema
dopaminergico en diferentes formas, dependiendo
en las condiciones del sujeto en el cual el sistema
biologico es examinado. Por lo tanto, aripiprazol ha
sido descrito como un antagonista completo, un
antagonista moderado o un agonista parcial en los
receptores
D2
en
diferentes
paradigmas
preclinicos, consistente en caracteristicas de
ligando parciales del compuesto.

1
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Lets review some concepts

Yellow
Is the color of gold,
butter and ripe
lemons. In the
spectrum of visible
light, yellow is found
between green and
orange.

Blue
Is the colour of the
clear sky and the deep
sea. It is located
between violet and
green on the optical
spectrum.

Red
Is the color of blood,
and because of this it
has historically been
associated with
sacrifice, danger and
courage.

Yellow
Is the color of gold,
butter and ripe
lemons. In the
spectrum of visible
light, yellow is found
between green and
orange.

Blue
Is the colour of the
clear sky and the deep
sea. It is located
between violet and
green on the optical
spectrum.

Red
Is the color of blood,
and because of this it
has historically been
associated with
sacrifice, danger and
courage.

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