1 What is this medicine
and what is it used for?
Naltrexone is a potent, long-acting, competitive opioid
receptor antagonist — it blocks mu-, kappa-, and delta-opioid receptors,
preventing opioids and endogenous opioid peptides (endorphins, enkephalins)
from exerting their effects. In addiction medicine, blocking the rewarding and
reinforcing effects of opioids and alcohol removes the positive reinforcement
that drives addiction.
It is used for:
• Opioid use disorder (OUD) —
prevention of relapse to opioid dependence after detoxification (opioid-free
period). Naltrexone blocks the euphoric effects of opioids, removing the
incentive to use.
• Alcohol use disorder (AUD) — reduces
alcohol craving and the reinforcing effects of alcohol. Shown in RCTs to reduce
heavy drinking days and total alcohol consumption.
It is also used off-label at very low doses (LDN — 1–4.5
mg/day) for various inflammatory, immune, and pain conditions, but this is
investigational and not within the licensed indication of this 50 mg tablet.
2 How to take this
medicine
Standard dose: 50 mg once daily. Take with food to reduce
nausea. Swallow whole with water. Alternatively, 100 mg may be prescribed every
other day, or 150 mg three times weekly, for supervised dosing programmes.
|
CRITICAL — OPIOID-FREE STATUS MUST BE
CONFIRMED BEFORE STARTING: Naltrexone MUST NOT be given to anyone who is
currently dependent on opioids or has taken opioids recently. Starting naltrexone in an opioid-dependent
patient precipitates ACUTE OPIOID WITHDRAWAL — which is extremely distressing
and can be dangerous. A minimum opioid-free period must be confirmed:
at least 7–10 days for short-acting opioids (heroin, codeine, morphine); at
least 7–14 days for long-acting opioids (methadone requires at least 10–14
days minimum). A naloxone challenge test can be performed by
the clinical team to confirm opioid-free status before the first dose. The patient must carry a NALTREXONE TREATMENT
CARD at all times informing medical staff that opioid pain relief will be
ineffective. |
3 Possible side effects
|
Frequency |
Side Effect |
What to Do |
|
Very Common (>10%) |
Nausea / vomiting |
Take with food;
usually improves after first week. |
|
Very Common (>10%) |
Fatigue / malaise |
Usually transient. |
|
Very Common (>10%) |
Abdominal pain |
Take with food;
usually mild. |
|
Very Common (>10%) |
Headache |
Paracetamol if needed. |
|
Common (1–10%) |
Decreased appetite |
Monitor weight; ensure
adequate nutrition. |
|
Common (1–10%) |
Anxiety / insomnia |
Monitor; usually
settles. Refer to psychological support. |
|
Common (1–10%) |
Joint and muscle pain
(arthralgia, myalgia) |
Paracetamol or NSAID
(note: opioid analgesics will be ineffective). |
|
Uncommon |
Hepatotoxicity (at
high doses > 50 mg/day) |
LFT monitoring
required. Report jaundice or dark urine. |
|
Serious risk |
Opioid overdose after
treatment discontinuation |
Tolerance to opioids
is greatly reduced after naltrexone — any post-treatment opioid use carries a
very high risk of fatal overdose. |
|
FATAL OVERDOSE RISK AFTER STOPPING
NALTREXONE: Naltrexone significantly reduces tolerance to
opioids. After stopping naltrexone (especially after long-term use), if a
patient resumes opioid use at their previous dose, they have a very high risk
of fatal overdose — their tolerance is much lower than before treatment. ALL patients and caregivers must be warned
about this risk at every treatment review. Naloxone (Narcan) rescue kits should be
prescribed to all patients and caregivers. |
||
4 Contraindications
Naltrexone is contraindicated in: patients currently using
opioids or in acute opioid withdrawal; patients who have failed the naloxone
challenge test; patients with acute hepatitis or liver failure; known
hypersensitivity; and patients requiring opioid analgesia (opioid pain
medicines will be ineffective).
Use with caution in: hepatic impairment (hepatotoxic at high
doses — monitor LFTs); renal impairment; depression (psychological support
essential alongside pharmacotherapy); and pregnancy/breastfeeding.
5 Drug interactions
• All opioid medications (morphine,
codeine, tramadol, oxycodone, methadone, fentanyl, buprenorphine): completely
blocked by naltrexone — no analgesic, sedative, or euphoric effect. Non-opioid
analgesia (NSAIDs, paracetamol, regional anaesthesia) must be used for pain
management.
• Thioridazine: additive lethargy and
somnolence — avoid.
• Yohimbine: may cause rapid heart rate
in combination — avoid.
6 Storage
Store below 25°C. Original packaging. Keep out of reach of
children.
7 Prescription
requirement
|
PRESCRIPTION ONLY MEDICINE (POM) — Addiction
medicine / substance use disorder specialist, or GP with specialist
support/training. Monitoring: LFTs at baseline and monthly for
first 3–6 months (high-dose hepatotoxicity risk); urine drug screen before
and during treatment; mood and psychological wellbeing. Patient must carry Naltrexone Treatment Card. |
8 Guidance for patients
& caregivers
Naltrexone is an important pharmacological tool in recovery
from opioid or alcohol dependence. It blocks the 'reward' of using — removing
the high or buzz that drives the cycle of addiction. It works best as part of a
comprehensive recovery programme that includes psychological therapy, social
support, and relapse prevention counselling.
Carry your naltrexone treatment card at all times. If you
need pain treatment (for surgery, injury, or medical procedures), tell every
healthcare provider you are on naltrexone — opioid pain medicines will not work
effectively. Regional anaesthesia, paracetamol, ketamine, or other non-opioid
analgesics will need to be used instead.
After stopping naltrexone, your tolerance to opioids is
greatly reduced. If you or your loved one relapses to opioid use after stopping
naltrexone, a much smaller amount of opioid than before can cause a fatal
overdose. Keep naloxone (Narcan) nasal spray or auto-injector at home and make
sure a family member knows how to use it.
9 Pharmacist &
prescriber notes
Naltrexone 50 mg/day is the standard licensed dose for both
OUD and AUD. The hepatotoxicity risk is dose-related — first described at
investigational doses of 300 mg/day; at 50 mg/day the risk is low but warrants
monitoring. LFTs at baseline, monthly for first 3 months, then every 3 months.
The 28-tablet pack covers one month of daily 50 mg dosing.
Supervised consumption dosing: some programmes use 100 mg on Monday, 100 mg on
Wednesday, 150 mg on Friday — total 350 mg/week, dispensed 3x weekly; confirm
which schedule is prescribed. Injectable extended-release naltrexone (Vivitrol
— 380 mg IM monthly) is available for patients with poor oral adherence.
The Sinclair Method (naltrexone 50 mg taken 1 hour before
each drinking occasion rather than daily) is used for AUD in some centres —
this is off-label dosing.
10 Frequently asked
questions
What if I stop naltrexone and then use opioids?
This is life-threatening. Naltrexone reduces your tolerance
to opioids. If you stop naltrexone and use opioids at a dose you previously
tolerated, you could die of overdose because your body is now much more
sensitive. This risk is highest in the first month after stopping. Please have
naloxone (Narcan) at home as a safety net.
Will naltrexone stop me from wanting to drink or use drugs?
Naltrexone reduces the craving and the reinforcing 'reward'
effect of alcohol and opioids — but it does not completely eliminate cravings.
It works best combined with psychological therapy and strong support networks.
I need surgery — what should I tell the anaesthetist?
Tell every healthcare provider: 'I am on naltrexone — opioid
pain medicines will not work.' Your anaesthetist will plan non-opioid pain
control. In extreme emergencies, very high doses of opioids can partially
overcome the block — this must only be managed by experienced anaesthetic staff
in monitored settings.
How long do I need to stay on naltrexone?
For OUD: typically at least 6–12 months; some patients
benefit from longer-term use. For AUD: duration is variable, guided by your
response and clinical judgement. Discuss with your addiction medicine
specialist.
Does naltrexone cause withdrawal symptoms?
Naltrexone itself does not cause dependence or withdrawal.
However, starting it while any opioids are still in your system will
precipitate immediate, severe opioid withdrawal — which is why you must be
completely opioid-free before the first dose.