RT Book, Section
A1 FUDIN, JEFFREY
A1 PERKINS, RUTH J.
A1 LIPMAN, ARTHUR G.
A2 Cohen, Henry
SR Print(0)
ID 1112258274
T1 Opioids
T2 Casebook in Clinical Pharmacokinetics and Drug Dosing
YR 2015
FD 2015
PB McGraw-Hill Education
PP New York, NY
SN 9780071628358
LK accesspharmacy.mhmedical.com/content.aspx?aid=1112258274
RD 2024/04/18
AB Opioids  are  among  the  oldest  documented  medications  used  by  humans.  All  opioids  are  derivatives  of  pharmacologically  active  alkaloids  from  the  milky  exudate  of  the  opium  poppy.  These  drugs  act  by  binding  at  opioid  receptors  found  in  the  CNS,  the  colon,  and  to  a  lesser  extent,  the  periphery.  Mu  and  kappa  opioid  receptors  have  clinical  utility  and  delta  opioid  receptors  offer  promise,  but  no  delta  agonist  has  been  found  acceptable  for  human  use  to  date.  However,  new  work  with  biased  legends  offers  promise  of  a  possible  future  delta  opioid  agonist  analgesic.  Most  clinically  useful  opioids  are  mu  agonists  that  also  have  varying  agonist  activity  at  kappa  receptors.  The  mu-1  aspect  of  the  receptor  is  responsible  primarily  for  analgesia  and  the  mu-2  for  other,  largely  adverse,  opioid  effects.  Numerous  subtypes  of  the  mu-1  receptors  have  been  isolated  and  cloned,  clearly  indicating  genetic  polymorphism.  Recent  work  on  opioid  agonist  G  protein  coupled  receptors,  and  specifically  beta  arrestin,  has  elucidated  our  understanding  of  biased  ligands  that  helps  explain  the  mechanisms  by  which  opioids  cause  some  adverse  effects.  This  offers  promise  of  new  agents  which  offer  full  analgesia  with  fewer  adverse  effects.1,  2,  3,  4,  and  5