TY  - CHAP
M1  - Book, Section
TI  - ESMOLOL
A1  - Kearney, Thomas E.
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.
Y1  - 2018
N1  - 
T2  - Poisoning & Drug Overdose, 7e
AB  - Pharmacology.  Esmolol  is  a  short-acting,  IV,  cardioselective  beta-adrenergic  blocker  with  no  intrinsic  sympathomimetic  or  membrane-depressant  activity.  In  usual  therapeutic  doses,  it  causes  little  or  no  bronchospasm  in  patients  with  asthma.  Esmolol  produces  peak  effects  within  6–10  minutes  of  administration  of  an  intravenous  bolus.  It  is  hydrolyzed  rapidly  by  red  blood  cell  esterases,  with  an  elimination  half-life  of  9  minutes;  therapeutic  and  adverse  effects  disappear  within  30  minutes  after  the  infusion  is  discontinued.IndicationsRapid  control  of  supraventricular  and  ventricular  tachyarrhythmias  and  hypertension,  especially  if  caused  by  excessive  sympathomimetic  activity  (eg,  stimulant  drugs,  hyperthyroid  state).Reversal  of  hypotension  and  tachycardia  caused  by  excessive  beta-adrenergic  activity  resulting  from  theophylline  or  caffeine  overdose.Control  of  ventricular  tachyarrhythmias  caused  by  excessive  myocardial  catecholamine  sensitivity  (eg,  chloral  hydrate  and  chlorinated  hydrocarbon  solvents).ContraindicationsContraindications  include  hypotension,  bradycardia,  and  congestive  heart  failure  secondary  to  intrinsic  cardiac  disease  or  cardiac-depressant  effects  of  drugs  and  toxins  (eg,  cyclic  antidepressants  and  barbiturates).Hypertension  caused  by  alpha-adrenergic  or  generalized  stimulant  drugs  (eg,  cocaine,  amphetamines),  unless  esmolol  is  coadministered  with  a  vasodilator  (eg,  nitroprusside  or  phentolamine).  Paradoxic  hypertension  may  result  from  an  unopposed  alpha  effect,  although  it  is  less  likely  than  that  associated  with  the  use  of  a  nonspecific  beta-adrenergic  blocker  (propranolol).Adverse  effectsHypotension,  bradycardia,  and  cardiac  arrest  may  occur,  especially  in  patients  with  intrinsic  cardiac  disease  or  cardiac-depressant  drug  overdose.Bronchospasm  may  occur  in  patients  with  asthma  or  chronic  bronchospasm,  but  it  is  less  likely  than  with  propranolol  or  other  nonselective  beta-blockers  and  is  rapidly  reversible  after  the  infusion  is  discontinued.Esmolol  may  mask  physiologic  responses  to  hypoglycemia  (tremor,  tachycardia,  and  glycogenolysis)  and,  therefore,  should  be  used  with  caution  in  patients  with  diabetes.Avoid  extravasation.  Infusion  site  reactions  include  irritation  as  well  as  necrosis  and  thrombophlebitis.Use  in  pregnancy.  FDA  Category  C  (indeterminate).  This  does  not  preclude  its  short-term  use  for  a  seriously  symptomatic  patient  (Introduction).  High-dose  infusion  may  contribute  to  placental  ischemia.Drug  or  laboratory  interactionsEsmolol  may  transiently  increase  the  serum  digoxin  level  by  10-20%,  but  the  clinical  significance  of  this  is  unknown.Esmolol  may  increase  the  risk  of  hypotension,  bradycardia,  AV  conduction  impairment  if  used  concurrently  with  calcium  channel  antagonists,  sympatholytics  (clonidine),  or  amiodarone.Recovery  from  succinylcholine-induced  neuromuscular  blockade  may  be  delayed  slightly  (5-10  minutes).  Similarly,  esmolol  metabolism  may  be  inhibited  by  anticholinesterase  agents  (eg,  organophosphates).Esmolol  is  not  compatible  with  sodium  bicarbonate  solutions.Dosage  and  method  of  administrationDilute  before  intravenous  injection  to  a  final  concentration  of  10  mg/mL  with  5%  dextrose,  lactated  Ringer  injection,  or  saline  solutions.Give  as  an  intravenous  infusion,  starting  at  0.025-0.05  mg/kg/min  and  increasing  as  needed  up  to  0.2  mg/kg/min  (average  dose,  0.1  mg/kg/min).  Steady-state  concentrations  are  reached  approximately  30  minutes  after  each  infusion  adjustment.  A  loading  dose  of  0.5-1.0  mg/kg  should  be  given  over  30  seconds  to  1  minute  if  more  rapid  onset  of  clinical  effects  (5-10  minutes)  is  desired.Infusion  rates  greater  than  0.2  mg/kg/min  are  likely  to  produce  excessive  hypotension.  At  rates  greater  than  0.3  mg/kg/min,  the  beta-blocking  effects  lose  their  beta1  selectivity.FormulationsParenteral.  Esmolol  hydrochloride  (Brevibloc,  others),  2.5  g  in  10-mL  ampules  (250  mg/mL),  100  mg  in  10-mL  vials  (10  mg/mL),  and  20  mg/mL  (double  strength)  in  5-mL  vials  and  100-mL  ...
SN  - 
PB  - McGraw-Hill Education
CY  - New York, NY
Y2  - 2024/04/19
UR  - accessmedicine.mhmedical.com/content.aspx?aid=1174607428
ER  -