Farmacos Autacoidespdf PDF
Farmacos Autacoidespdf PDF
Farmacos Autacoidespdf PDF
AUTACOIDES
Por:
Dr.
Jonathan
Arauz
AUTACOIDES
Autacoides
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alfabtico no exhaustivoBG(
Adenosina
Histamina
Prostaglandinas
Cininas
Leucotrienos
Serotonina
Factores quimiotcticos
xido Ntrico
Tromboxanos
Prostaciclina
HISTAMINA
/"(7%*3"$%&"('*(,&"($.1A+,1"(4'(2"=.(0'*.($.1'+,1"#(.23'&%4"("(0"#3%#(4'(1"(/H7%*3%4%&"9(;#"+%"*("(1"(
Respuesta celular:
Estimulacin de la liberacin de mediadores
Acumulacin de leucocitos en tejidos
Fagocitosis y destruccin de microorganismos
RESPUESTA INMUNE
Histamina
UESTAHINMUNE
ISTAMINA
/"(7%*3"$%&"('*(,&"($.1A+,1"(4'(2"=.(0'*.($.1'+,1"#(.23'&%4"("(0"#3%#(4'(1"(/H7%*3%4%&"9(;#"+%"*("(1"(
'&-%$"(7%*3%4%&"(4'*+"#2.I%1"*"C(*'(+.&*%4'#"(J,'('*(,&"("$%&"(2%.;A&%+"9('&('1(*'&3%4.(4'(J,'(*'(3#"3"(
4'( ,&( 3#"&*$%*.#( J,'( &.( 5.#$"( 0"#3'( 4'( <F"*( $'3"2:1%+"*( ;'&'#"1'*( 4'( 1"( +A1,1"D( /"( 7%*3"$%&"( '*3?(
HISTAMINA
0#'*'&3'('&('1(K%*3'$"(L'#<%.*.(!'&3#"19(1"*(+A1,1"*(0"#%'3"1'*(4'(1"($,+.*"(;?*3#%+"9(1.*($"*3.+%3.*9(1.*(
2"*:5%1.*(>($,+7"*(.3#"*(+A1,1"*D( piel,
Mastocitos, basofilos,
mucosa
gastrointestinal,
histidina
histaminocitos,
pulmones, mdula sea
M0"#'&3'$'&3'9(1"(7%*3"$%&"('*(,&($'4%"4.#($,>("&3%;,.(4'*4'('1(0,&3.(4'(<%*3"(5%1.;'&A3%+.9(0.#(1.(
neuronas histaminrgicas
Histidin
HISTAMINA
decarboxilasa
..................................
piel,
J,'( 0,'4'( '&+.&3#"#*'( '&( 4%<'#*.*(
.#;"&%*$.*9( 5.#$"&4.( 0"#3'( 4'( $N13%01'*( 3.I%&"*( >( "0"#'+%'&4.(
Mastocitos, basofilos,
mucosa gastrointestinal,
Estmulos que liberan Histamina
histaminocitos,
%&+1,*.('&(2"+3'#%"*(>(01"&3"*D(
pulmones,
mdula sea
CH2CH
2NH2
neuronas
histaminrgicas
Antgeno-anticuerpo
..................................
os
dina
cin
CH2CH2NH2
C3a y
Estmulos que liberan Histamina:
HN Antgeno-anticuerpo
N
C3a y C5b
C5b complemento
Agentes citotxicos
Enzimas proteolticas
complemento
Polisacaridos
histamina
Agentes citotxicos
HISTAMINA
CH2NH2
H4
histaminocitos,
neuronas histaminrgicas
Antgeno-anticuerpo
C3a y C5b complemento
Agentes citotxicos
Enzimas proteolticas
Polisacaridos
BK, sustancia P
Polimixina B, protamina,
tubocurarina, morfina...
ewis
n
CH2CH2NH2
HN
H4?
histamina
H1
H2 H3
Frmacos
antihistamnicos H1
Inhibidores de la
degranulacin de mastocitos:
Cromoglicato (Tema
Farmacos
antihistamnicos H2
Efectos
de
la
Histamina
Efectos de la Histamina
Sistema cardiovascular
-Vasodilatacin (H1, H2)
-Aumento de la permeabilidad (H1)
Triple respuesta de Lewis
-Aumento de la frecuencia, fuerza de contraccin
y gasto cardaco (H2)
Msculo liso
Contraccin de bronquios, bronquiolos, leo
y tero (H1)
Glndulas
Incremento secrecin gstrica (H2) y otras (H1)
Terminaciones sensitivas: prurito (H1)
SNC
F
an
Receptores
de
Histamina
Receptores
H1:
estn
ubicados
en
el
msculo
liso
del
leon,
el
endotelio
y
bronquios.
Responden
a
los
anThistamnicos
convencionales
uTlizados
para
tratar
las
alergias,
los
cuales
bloquean
a
receptores
H1,
por
lo
que
se
llaman
antagonistas
H1.
Receptores
H2:
estn
situados
sobre
las
clulas
parietales
del
estmago,
esTmulan
principalmente
la
secrecin
de
cido
gstrico.
Responden
a
los
antagonistas
H2,
como
la
cimeTdina,
que
inhiben
la
secrecin
de
cido
gstrico
y
se
uTlizan
para
ayudar
a
curar
la
gastriTs.
Receptores
de
Histamina
Receptores
H3:
se
encuentran
en
el
sistema
nervioso
central
y
en
menor
medida
en
los
tejidos
del
sistema
nervioso
perifrico.
Disminuyen
la
liberacin
de
neurotransmisores:
histamina,
aceTlcolina,
norepinefrina
y
serotonina.
Receptores
H4:
estn
ubicados
principalmente
en
los
baslos
y
en
la
mdula
sea.
Tambin
se
encuentran
en
el
Tmo,
el
intesTno
delgado,
el
bazo
y
el
colon.
Juegan
un
papel
en
la
quimiotaxis.
primarily mast cells, eosinophils, and basophils. H4 receptors share 40% homology with H3 receptors and bind many
H3 receptor agonists, although with lower affinity. Coupling
A Initial exposure
Allergen
B cell
IgE
Mast cell
Mast cell
Capillary
Granules
IgE
B Subsequent exposure
Allergen
Edema fluid
Crosslinked IgE
Histamine
Degranulated
mast cell
FIGURE 43-2.
Pathophysiology of the IgE-mediated hypersensitivity reaction. Allergen-induced mast cell degranulation requires two separate exposures
to the allergen. A. On initial exposure, the allergen must penetrate mucosal surfaces so that it can encounter cells of the immune system. Activation of the immune
response causes B lymphocytes to secrete allergen-specific IgE antibodies. These IgE molecules bind to Fc receptors on mast cells, leading to sensitization of the
mast cells. B. On subsequent exposure, the multivalent allergen cross-links two IgE/Fc receptor complexes on the mast cell surface. Receptor cross-linking causes
the mast cell to degranulate. Local histamine release results in an inflammatory response, shown here as edema.
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FARMACOLOGA HISTAMINRGICA
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Frmacos antihistamnicos H1
Aumento permeabilidad (H1)
Prurito (H1)
Contraccin de bronquios,
bronquiolos, leo y tero (H1)
Reflejo axnico (H1)
Efecto dilatador ((H1, H2)
Aumento secreciones bronquiales,
salivares, nasales, lacrimales (H1)
difenhidramina...
Grupo eTlamina
+
Histamina
Depresin SNC
Accin anticolinrgica
Accin anestsica local
Clasificacin
Qumica
Alquilaminas
Piperazinas
Piperidinas
Clasificacin Funcional
!
Primera Generacin
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Segunda Generacin
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Etanolaminas
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Fenotiazinas
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Otras
;#?&9'$(+Daccin H1 y H2E+
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Etilenodiaminas
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Antihistamnicos H1
Sedacin
Primera generacin
Difenhidramina
Dimenhidrinato
Clorfeniramina
Tripolidina
Hidroxicina
Promeatazina
Segunda generacin
Cetirazina
Astemizol (retirado)
Ebastina
Loratadina
Terfenadina (retirado)
Bloqueo
colinrgico
Duracin de
accin (h)
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ACCIONES FARMACOLGICAS
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Indicaciones teraputicas
Antihistamnicos H1
es,
Efectos adversos
Antihistamnicos H1
Sedacin (somnolencia, incordinacin motor, cansancio)
Efectos anticolinrgicos (sequedad de boca, visin
borrosa, dificultades en la miccin...)
terfenadina y astemizol