TY  - CHAP
M1  - Book, Section
TI  - NALOXONE
A1  - Go, Joyce
A2  - Olson, Kent R.
A2  - Anderson, Ilene B.
A2  - Benowitz, Neal L.
A2  - Blanc, Paul D.
A2  - Clark, Richard F.
A2  - Kearney, Thomas E.
A2  - Kim-Katz, Susan Y.
A2  - Wu, Alan H. B.
PY  - 2018
T2  - Poisoning & Drug Overdose, 7e
AB  - Pharmacology.  Naloxone  is  a  synthetic  N-allyl  derivative  with  pure  opioid  antagonist  activity  that  competitively  blocks  mu-,  kappa-,  and  delta-opiate  receptors  within  the  CNS.  It  has  no  opioid  agonist  properties  and  can  be  given  safely  in  large  doses  without  producing  respiratory  or  CNS  depression.  Take-home  naloxone  programs  are  being  developed  in  which  opiate  users  and  their  families  are  supplied  naloxone  for  use  on  the  scene  in  case  of  accidental  overdose.  The  most  common  routes  of  administration  for  this  purpose  are  intranasal  and  intramuscular  or  subcutaneous  by  autoinjector  or  syringe.Naloxone  undergoes  extensive  first-pass  metabolism  and  is  not  effective  orally  but  may  be  given  by  intravenous,  intramuscular,  subcutaneous,  nebulized,  intranasal,  and  intraosseous  routes.  After  intravenous  administration,  opioid  antagonism  occurs  within  1–2  minutes  and  persists  for  approximately  30–120  minutes.  The  plasma  half-life  ranges  from  30  to  81  minutes.  Table  III–11  is  a  comparison  of  the  routes  of  administration  for  naloxone.Nalmefene  is  a  pure  opioid  antagonist  that  has  been  used  to  treat  acute  opioid  intoxication.  It  has  a  longer  elimination  half-life  and  duration  of  action  than  naloxone.  However,  its  production  was  discontinued  in  2008  and  is  no  longer  available  in  the  United  States.Naltrexone  is  another  potent  competitive  opioid  antagonist  that  is  active  orally  and  used  to  prevent  recidivism  in  patients  detoxified  after  opioid  abuse.  It  has  also  been  used  to  reduce  craving  for  alcohol.  It  is  not  used  for  the  acute  reversal  of  opioid  intoxication.IndicationsReversal  of  acute  opioid  intoxication  manifested  by  coma,  respiratory  depression,  or  hypotension.Empiric  therapy  for  stupor  or  coma  suspected  to  be  caused  by  opioid  overdose.Anecdotal  reports  suggest  that  high-dose  naloxone  may  partially  reverse  the  CNS  and  respiratory  depression  associated  with  clonidine,  ethanol,  benzodiazepine,  or  valproic  acid  overdoses,  although  these  effects  are  inconsistent.Contraindications.  Do  not  use  in  patients  with  a  known  hypersensitivity  to  naloxone  or  nalmefene  (may  have  cross-sensitivity).Adverse  effects.  Human  studies  have  documented  an  excellent  safety  record  for  naloxone.Use  in  opiate-dependent  patients  may  precipitate  acute  withdrawal  syndrome.  Neonates  of  addicted  mothers  may  have  more  severe  withdrawal  symptoms,  including  seizures.  Aggressive  use  of  opiate  antagonists  in  so-called  rapid  opioid  detoxification  (ROD)  and  ultra-rapid  opioid  detoxification  (UROD)  has  been  associated  with  marked  increases  in  plasma  corticotropin,  cortisol,  and  catecholamine  levels  and  in  sympathetic  activity;  pulmonary  edema;  acute  renal  failure;  ventricular  bigeminy;  psychosis;  delirium;  and  death.Pulmonary  edema  or  ventricular  fibrillation  occasionally  has  occurred  shortly  after  naloxone  administration  in  opioid-intoxicated  patients.  Pulmonary  edema  has  also  been  associated  with  postanesthetic  use  of  naloxone,  especially  when  catecholamines  and  large  fluid  volumes  have  been  administered.Reversing  the  sedative  effects  of  an  opioid  may  amplify  the  toxic  effects  of  other  drugs.  For  example,  agitation,  hypertension,  and  ventricular  irritability  have  occurred  after  naloxone  administration  to  persons  high  on  a  "speedball"  (heroin  plus  cocaine  or  methamphetamine).There  has  been  one  case  report  of  hypertension  after  naloxone  administration  in  a  patient  with  clonidine  overdose.  Hypertension  has  been  associated  with  postoperative  use  of  naloxone.  Use  caution  in  patients  with  cardiovascular  risk  factors,  especially  patients  with  a  previous  history  of  uncontrolled  hypertension.Use  in  pregnancy.  FDA  Category  B  (Introduction).  Naloxone  may  produce  an  acute  opioid  withdrawal  syndrome  in  both  mother  ...
SN  - 
PB  - McGraw-Hill Education
CY  - New York, NY
Y2  - 2024/04/20
UR  - accessmedicine.mhmedical.com/content.aspx?aid=1179993007
ER  -