Pharmacology 3620 Lecture Notes - Lecture 16: Prodrug, Nociceptor, Enkephalin
6 Jan 2021
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Analgesia and anesthesia: pain unpleasant sensory and emotional experience associated with an actual or potential tissue damage. Opiod receptors: endogenous opioids can be released from neurons and immune cells, 3 main types: mu, kappa, delta, mus b-endorphins, *used for analgesia, kappa dynorphin, delta enkephalins, mu receptors are gpcrs with gi alpha subunit. Impact permeability to ca++ and k: however, there are also other effects. Increased opening, leading to increased hyperpolarization: recall: k+ is involved in hyperpolarization because it is a positive ion leaving the cell (high conc inside, low conc outside) Important to note that even in chronic users, there is significant levels of respiratory depression, which is important when considering overdose. Bottom line: tolerance develops for many of the effects of opioids, but it is different for the different effects (constipation, apnea, analgesia) Naloxone: competitive antagonist for the mu receptor.
