farmacos colinergicos papa
TRANSCRIPT
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FARMACOS FARMACOS COLINERGICOSCOLINERGICOS
LUIS FUJITA ALARCONLUIS FUJITA ALARCON
HOSPITAL EL CARMENHOSPITAL EL CARMEN
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Sintesis de AcetilcolinaSintesis de Acetilcolina
ColinaAcCoA
Acetilcolina
Vesícula
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MetabolismoMetabolismo
Acetilcolina RECEPTORRECEPTOR
Colina Acetato
Acetilcolinoesterasa(eritrocito,mus.esqueletico, snc)
(Butirilcolinoesterasa) (Plasma, musculo liso, glandulas, higado, piel)
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Agonista ColinergicosAgonista Colinergicos
• Mimetizan a los efectos de la acetil colina
• Parasimpaticomimeticos• Colinomemeticos• Agonista colinergicos
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Agonista colinergicosAgonista colinergicos
• Subtipos de receptores Muscarinicos Nicotinico
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Tipos de receptores Tipos de receptores NicotinicoNicotinico
• Nicotínico neural (Nn) Ganglio Autonomo ----- Despolizacion Neurona postganglionar
Medula suprerenal ----- Secreción de catecolamina
• Nicotínico muscular (Nm) Placa mioneural ----- Desporalizacion de la placa
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Mecanismo de acciónMecanismo de acciónNicotinicoNicotinico
• Canal iónico• Respuesta excitatoria• Despolarización de conductos de
Na+
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NICOTINANICOTINA
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¡¡¡Son ¡¡¡Son heterogeniheterogeni
o¡¡¡o¡¡¡
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M1 M3M1 M3
• Activacion de Fosfolipasa C• Activa IP3, DAG• Aumento de Ca++
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Efectos farmacológicosEfectos farmacológicos
• Placa mioneural
Fase 1 Fasciculaciones Fase 2 Parálisis
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• Toxina botulinica : Bloquea liberación de Ach
• Viuda negra: Movilizacion y fusión
vesicular y liberacion de Ach
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TIPOS DE RECEPTORES TIPOS DE RECEPTORES MUSCARINICOSMUSCARINICOS
• Muscarinicos 1 Ganglio de glandulas secretorias
• Muscarinicos 2 Miocardio Musculo liso • Muscarinicos 3 Músculo liso • Muscarinicos 4 SNC
Muscarinicos 5 SNC
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Mecanismo de acciónMecanismo de acción
• M1 Fosfolipasa C, IP3, Cascada DAG
• M3
• M2 Adenilciclasa, Inhibición de cAMP
Activación de los conductos
de K
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M2M2• Hiperpolarizacion• Cierre canales de Ca++• Inhibición de adenil ciclasa
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ClasificacionClasificacion
• Acción directa: Unión a receptores
Esteres de la colina
Alcaloides naturales
• Acción indirecta: Inactivacion de Enzima
Anticolinestasa reversible
Anticolinestesa irreversible
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Esteres de la colinaEsteres de la colina
• Acetil Colina• Metacolina• Carbacol• Betanecol
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Alcaloides NaturalesAlcaloides Naturales
• Pilocarpina• Arecolina• Oxotremorina• Muscarina
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Mecanismo de acciónMecanismo de acción
Muscarinico Nicotínico
Arecolina Terciario + +++
Pilocarpina Terciario +++ +
Muscarina Cuaternario +++ +
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Esteres de la colina
Susceptibilad a Che
Acciones Farmacológicos
CV GI Urinaria Ojo ANTG. ATROPINA
NICOTINIC
Ach +++ ++ ++ ++ + +++ ++
Metacolina + +++ ++ ++ + +++ +
Carbacol - + +++ +++ ++ + ++
Betanecol - +/- +++ +++ ++ +++ -
Muscralina - ++ +++ +++ ++ +++ -
Pilocarpina - + +++ +++ ++ +++ -
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Colinergicos de acción Colinergicos de acción indirectaindirecta
• AntiChE reversible Alcaloides naturales: Fisostigmina
Derivados sinteticos: Neostigmina Piridostigmina
Edrofonio Ambenonio
• AntiChE irreversible Organos fosforado
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Efectos farmacológicosEfectos farmacológicos
•Cardiovascular Vasos sanguíneos carecen de inervación colinergicas
Ventrículos tienes escasa innervación colinergicas Efecto a dosis dependiente:
Dosis Baja: Vasodilatacion Taquicardia refleja Dosis Mayores: Vasodilatacion,Bradicardia
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PPILOCARPINAILOCARPINA
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Efectos farmacológicosEfectos farmacológicos
• Cardiovascular Vasodilatacion ----- Oxido nitrico y FRDE
Cronotropo negativo ---- Hiperporalizacion Disminución desporalizacion SA
Inotropico negativo Dromotropico negativo
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Efectos farmacológicosEfectos farmacológicos
• Gastrointestinal Competencia cardias Tono y amplitud contracciones Actividad peristáltica Actividad secretora gástrica Actividad secretora pancreática Nausea, vomito, colico Diarrea RELAJA ESFINTERES
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Glándulas exocrinasGlándulas exocrinas
• Lagrimal• Traqueo bronquial• Salivales• Digestivas• Sudoriparas
Ecrinas –- ParasimpaticoApocrinas-- Simpatico
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Efectos farmacológicosEfectos farmacológicos
• Respiratorio
Aumenta secreción traqueobronquial
Broncocontriccion ( GMPc )
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Efectos farmacológicosEfectos farmacológicos
• Genitourinario Peristaltismo uretral
Presión de la micción voluntaria Contracción músculo detrusor
Relajación trígono Relajación esfínteres Disminuye capacidad vesical
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Efectos farmacológicosEfectos farmacológicos
• Ojo : Miosis Espasmo del músculo ciliar Espasmo de acomodación Disminución de PIO ( vaso dilatación de plexo
coroideo)
( Apertura de canal de Schelmm
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Reacciones adversasReacciones adversas
• Bochorno• Sudoración• Calambres• Salivación• Nausea• Defecación involuntaria• Crisis asmatica• Dificultacion para vision lejana
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GRACIAS
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