3.4 Opioid toxicity
OPIOID RECEPTOR ANTAGONISTS
Naloxone hydrochloride
lINDICATIONS AND DOSE
Overdosage with opioids
▶BY INTRAVENOUS INJECTION
▶Neonate:Initially 100 micrograms/kg, if no response,
repeat at intervals of 1 minute to a max. of 2 mg, then
review diagnosis; further doses may be required if
respiratory function deteriorates, doses can be given by
subcutaneous or intramuscular routes but only if
intravenous route is not feasible; intravenous
administration has more rapid onset of action.▶Child 1 month–11 years:Initially 100 micrograms/kg
(max. per dose 2 mg), if no response, repeat at intervals
of 1 minute to a max. of 2 mg, then review diagnosis;
further doses may be required if respiratory function
deteriorates, doses can be given by subcutaneous or
intramuscular routes but only if intravenous route is
not feasible; intravenous administration has more
rapid onset of action
▶Child 12–17 years:Initially 400 micrograms, then
800 micrograms for up to 2 doses at 1 minute intervals
if no response to preceding dose, then increased to
2 mg for 1 dose if still no response ( 4 mg dose may be
required in seriously poisoned patients), then review
diagnosis; further doses may be required if respiratory
function deteriorates, doses can be given by
subcutaneous or intramuscular routes but only if
intravenous route is not feasible; intravenous
administration has more rapid onset of action
▶BY CONTINUOUS INTRAVENOUS INFUSION
▶Neonate:Using an infusion pump, adjust rate according
to response (initially, rate may be set at 60 %ofthe
initial resuscitative intravenous injection dose per
hour). The initial resuscitativeintravenous injectiondose
is that which maintained satisfactory ventilation for at
least 15 minutes.▶Child:Using an infusion pump, adjust rate according to
response (initially, rate may be set at 60 % of the initial
resuscitative intravenous injection dose per hour). The
initial resuscitativeintravenous injectiondose is that
which maintained satisfactory ventilation for at least
15 minutes
Reversal of postoperative respiratory depression
▶INITIALLY BY INTRAVENOUS INJECTION
▶Neonate: 1 microgram/kg, repeated every 2 – 3 minutes if
required.▶Child 1 month–11 years: 1 microgram/kg, repeated every
2 – 3 minutes if required
▶Child 12–17 years:Initially 100 – 200 micrograms,
alternatively (by intravenous injection) initially
1. 5 – 3 micrograms/kg, if response inadequate, give
subsequent doses, (by intravenous injection)
100 micrograms every 2 minutes, alternatively (by
intramuscular injection) 100 micrograms every
1 – 2 hours
Reversal of respiratory and CNS depression resulting from
opioid administration to mother during labour
▶BY INTRAMUSCULAR INJECTION
▶Neonate: 200 micrograms, alternatively
60 micrograms/kg, to be given as a single dose at birth.▶BY INTRAVENOUS INJECTION, OR BY SUBCUTANEOUS INJECTION
▶Neonate: 10 micrograms/kg, repeated every 2 – 3 minutes
if required.PHARMACOKINETICS
▶Naloxone has a short duration of action; repeated doses
or infusion may be necessary to reverse effects of
opioids with longer duration of action.lUNLICENSED USENaloxone doses in BNF may differ from
those in product literature.IMPORTANT SAFETY INFORMATION
SAFE PRACTICE
Doses used in acute opioid overdosage may not be
appropriate for the management of opioid-induced
respiratory depression and sedation in those receiving
palliative care and in chronic opioid use.lCAUTIONSCardiovascular disease or those receiving
cardiotoxic drugs (serious adverse cardiovascular effects
reported).maternal physical dependence on opioids (may
precipitate withdrawal in newborn).pain.physical
dependence on opioids (precipitates withdrawal)
CAUTIONS, FURTHER INFORMATION
▶Titration of doseIn postoperative use, the dose should be
titrated for each patient in order to obtain sufficient
respiratory response; however, naloxone antagonises
analgesia.
lSIDE-EFFECTS
▶Common or very commonArrhythmias.dizziness.
headache.hypertension.hypotension.nausea.vomiting
▶UncommonDiarrhoea.dry mouth.hyperhidrosis.
hyperventilation.pain.tremor
▶Rare or very rareAnxiety.cardiac arrest.erythema
multiforme.pulmonary oedema.seizure
▶Frequency not knownAnalgesia reversed.asthenia.chills.
death.dyspnoea.fever.irritability.nasal complaints.
piloerection.withdrawal syndrome.yawning
lPREGNANCYUse only if potential benefit outweighs risk.
lBREAST FEEDINGNot orally bioavailable.
lDIRECTIONS FOR ADMINISTRATIONForcontinuous
intravenous infusion, dilute to a concentration of up to
200 micrograms/mL with Glucose 5 % or Sodium Chloride
0. 9 %.lMEDICINAL FORMS
There can be variation in the licensing of different medicines
containing the same drug.
Solution for injection
▶Naloxone hydrochloride (Non-proprietary)
Naloxone hydrochloride 20 microgram per 1 mlNaloxone
40 micrograms/ 2 ml solution for injection ampoules|
10 ampouleP£ 55. 00
Naloxone hydrochloride 400 microgram per 1 mlNaloxone
400 micrograms/ 1 ml solution for injection ampoules|
10 ampouleP£ 41. 00 – £ 53. 70
Naloxone hydrochloride 1 mg per 1 mlNaloxone 2 mg/ 2 ml solution
for injection pre-filled syringes| 1 pre-filled disposable
injectionP£ 16. 80842 Drug toxicity BNFC 2018 – 2019
Emergency treatment of poisoning16