Neurofarmacología; Analgésicos (2da parte) Opioides I Dr. José Renán Pérez P. 14.10.12

Introducción Opiode: Compuesto relacionado con el opio Opiáceo: Papaver somniferum Opiáceo: Derivados del opio (codeína, tabaína) Endorfina: Péptidos opioides endógenos. Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Historia Teofrasto III Ac 1680 Sydenham 1810 Aislamiento de la morfina 1970 Naloxona 1975 Encefalina 1976 receptores μ,δ,κ 1994 Receptors FQ Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Opiodes endógenos

POMC proencefalina Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Receptores κ μ δ

Acoplamiento Desensibilización Tolerancia Aguda Crónica Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Crisis epileptiformes Efectos clínicos Recompensa μ Analgesia Termoregulación Localización: Talámica Sustancia gris PA Rafé Hasta Posterior GRD Miosis Neuroendócrinos Crisis epileptiformes Respiración Tos Eméticos κ Antianalgesia Cardiovascular Gastrointestinal Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Morfina Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Levorfanol Agonista de receptores de morfina Dextrorfano (isómero-D) Inhibe NMDAr Famarmacocinética similar a morfina t1/2 of 12-16 h Mejor tolerado Nalbufina* Butorfanol* Yaksh TL, Wallace MS. Opioids, Analgesia, and Pain Management. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011

Meperidina Agonistas de receptores μ Efecto principal en SNC y elementos neurales en GI. Analgesia. Congéneres: Trastornos GI

Fentanilo

Tramadol Análogo sintético de Codeína Agonista débil μ Inhibidor de recaptura de Na y 5HT Absorción IM Biodisponibiliad 100% Pico 3 h Distribución Metabolismo CYP2D6 CYP3A4 conjugación acido meperidinico, 2/3 Proteínas Plasmáticas t1/2 6 h Interacción con IMAOs Excreción Renal 10% circulación enterohepática

Agonistas paciales Agonistas μ y κ Pentazocina Nalbufina Butorfanol Buprenorfina

Fin de 2da parte