FARMACOS

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"(

La INFLAMACIN es la respuesta defensiva del organismo

ante la invasin de un patgeno o la presencia de un agente
externo fsico o qumico nocivo
RESPUESTA INNATA (no inmunolgica)
Respuesta vascular:
Vasodilatacin
Aumento del flujo sanguneo
Aumento de la permeabilidad vascular
Exudacin de lquidos

Respuesta celular:
Estimulacin de la liberacin de mediadores
Acumulacin de leucocitos en tejidos
Fagocitosis y destruccin de microorganismos
RESPUESTA INMUNE

timulacin de la liberacin de mediadores

Prostaciclina
umulacin de leucocitos en tejidos
gocitosis y destruccin de microorganismos

Histamina

UESTAHINMUNE
ISTAMINA

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'&-%$"(7%*3%4%&"(4'*+"#2.I%1"*"C(*'(+.&*%4'#"(J,'('*(,&"("$%&"(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

nes, mdula sea

........................

CH2NH2

H4

histaminocitos,
neuronas histaminrgicas

Estmulos que liberan Histamina:

Antgeno-anticuerpo
C3a y C5b complemento

Agentes citotxicos
Enzimas proteolticas
Polisacaridos
BK, sustancia P
Polimixina B, protamina,
tubocurarina, morfina...

Estrs fsico (trmico, mecnico)

Triple Respuesta de Lewis

1. RUBOR - Enrojecimiento como consecuencia de la vasodilatacin
directa.
2. PICOR - Causado por reejo axnico.
3. EDEMA - Hinchazn producida por aumento de la presin capilar

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

quent exposure to the allergen. Upon such an exposure, the

allergen binds to and cross-links the IgE/Fc receptor complexes, triggering cell degranulation (Fig. 43-2).

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

Mast cell degranulation

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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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
!"#$%&$'"()'$(*+,-#"%&$'"()'$(*+
.&$'"()'$(+
!40-'5'$(*+6&0-'5'$(*+,'0-'5'$(+
/5(3(8'$(*+,'9"#:&93(8'$(*+
;'%&$'-9'"(-'$(*+<&3#3'%&$#+

Segunda Generacin
/0"'1(23'$(+
,&3'"'5'$(*+7&1#0&3'"'5'$(+
/23&)'5#-*+;&2-#"(3(8'$(*+=>(23'$(*+
.&?#%&$(8'$(*+7&1#0(>(23'$(*+7#"(3(8'$(*+
@&"%&$(8'$(*+A-#9(3(8'$(*+6'5#-(23'$(+

,(>'$#?()'$(*+,-&)(23'$(*+
Etanolaminas

;')&$:'8"'$(3#*+;'%&$:'8"()'$(*+

B+

;#?'-()'$(*+.&$'-3#-#?()'$(+
/$3(5#-'$(*+C'"'-()'$(++

B+

Fenotiazinas

6&38'-(5'$(*+C"#)&3(5'$(+

B+

Otras

;#?&9'$(+Daccin H1 y H2E+

/5&-(23'$(*+=)&8(23'$(*+=9'$(23'$(+

Etilenodiaminas

640:#2+ (F&$3&2+ 2#$+ &$+ "&(-'8(8+ )&3(>#-'3#2+ #+ )#-G04-(2+ )4H+ "&-(0'#$(8(2+ 0#$+ #3"(2+ 9"&B&?'23&$3&2I+
/4$J4&+$#+2&+(0&93(+()9-'()&$3&*+2&+:(+--&F(8#+(+42("+&-+3G")'$#+8&+K(F&$3&2+8&+3&"0&"(+F&$&"(0'L$M+
&$+"&-(0'L$+0#$+(F&$3&2+$#+2&8($3&2+0#$+)&N#"+9&"%'-+8&+&%&03#2+(81&"2#2+0("8O(0#2I+

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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&$+"&-(0'L$+0#$+(F&$3&2+$#+2&8($3&2+0#$+)&N#"+9&"%'-+8&+&%&03#2+(81&"2#2+0("8O(0#2I+
ACCIONES FARMACOLGICAS
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(00'L$+($&23G2'0(+-#0(-+8&+0'&"3#2+(F&$3&2EI+/4$J4&+&23#2+(F&$3&2+$#+9"&2&$3($+&%&03#+(-F4$#+2#>"&+-(+
2&0"&0'L$+ FR23"'0(*+ 94&8&$+ )#8'%'0("+ :(23(+ 0'&"3#+ 94$3#+ -(+ 9"&2'L$+ 2($F4O$&(+ 9#"+ 9("3'0'9(0'L$+ 8&+
"&0&93#"&2+PQ+H+PVI+/4$J4&+-(+)(H#"O(+8&+&23(2+(00'#$&2+94&8&$+0#$2'8&"("2&+0#)#+($3''$%-()(3#"'(2*+
-#2+($3':'23()O$'0#2+2#$+0#$2'23&$3&)&$3&+249&"(8#2+9#"+-#2+F-40#0#"3'0#'8&2+(+&23&+"&29&03#I+
=-+"&23#+8&+-(2+(00'#$&2+%(")(0#-LF'0(2+8&+-#2+($3':'23()O$'0#2+8&9&$8&+8&+8#2+(29&03#2+>R2'0#2W+

Indicaciones teraputicas
Antihistamnicos H1

es,

Rinitis y conjuntivitis alrgica

Urticaria
Cinetosis

Efectos adversos
Antihistamnicos H1
Sedacin (somnolencia, incordinacin motor, cansancio)
Efectos anticolinrgicos (sequedad de boca, visin
borrosa, dificultades en la miccin...)

Fotosensibilizacin, dermatitis alrgica

(va tpica)

Alteraciones hematolgicas (leucopenia,

agranulocitosis, anemia hemoltica)

Cardiotoxicidad (prolongacin QT, torsades de pointes y

fibrilacin ventricular)

terfenadina y astemizol