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Oxycodone hydrochloride and naloxone hydrochloride oral modified release

Updated 2 Feb 2023 | Opioid analgesics


Modified release tablets of oxycodone hydrochloride and naloxone hydrochloride

Drugs List

  • MYLOXIFIN 10mg+5mg modified release tablet
  • MYLOXIFIN 20mg+10mg modified release tablet
  • MYLOXIFIN 40mg+20mg modified release tablet
  • MYLOXIFIN 5mg+2.5mg modified release tablet
  • OXYARGIN 10mg+5mg modified release tablet
  • OXYARGIN 20mg+10mg modified release tablet
  • OXYARGIN 40mg+20mg modified release tablet
  • OXYARGIN 5mg+2.5mg modified release tablet
  • oxycodone hydrochloride 10mg and naloxone 5mg modified release tablet
  • oxycodone hydrochloride 20mg and naloxone 10mg modified release tablet
  • oxycodone hydrochloride 40mg and naloxone 20mg modified release tablet
  • oxycodone hydrochloride 5mg and naloxone 2.5mg modified release tablet
  • TARGINACT 10mg+5mg modified release tablet
  • TARGINACT 20mg+10mg modified release tablet
  • TARGINACT 40mg+20mg modified release tablet
  • TARGINACT 5mg+2.5mg modified release tablet
  • Therapeutic Indications


    Pain - severe
    Severe to very severe idiopathic Restless Leg Syndrome: Secondary treatment

    Severe pain, which can be adequately managed only with opioid analgesics.

    Second line symptomatic treatment of patients with severe to very severe idiopathic restless legs syndrome (RLS) after failure of dopaminergic therapy.

    Oxycodone and naloxone is indicated for patients suffering from RLS for at least 6 months. RLS symptoms should be present daily and during daytime. Previous treatment with at least one dopaminergic drug should have lasted in general 4 weeks.

    The opioid antagonist naloxone is added to counteract opioid-induced constipation by blocking the action of oxycodone at opioid receptors locally in the gut.


    Symmetric administration (the same dose mornings and evenings) subject to a fixed time schedule (every 12 hours) is appropriate for the majority of patients. However, some patients may benefit from asymmetric dosing tailored to the individual patient, depending on the individual situation. In general, the lowest effective dose should be selected.

    The dosage should be adjusted to the intensity of the pain and the sensitivity of the individual patient.

    Oxycodone and naloxone modified release tablets are not intended for the 'rescue' treatment of breakthrough pain. A single dose of an immediate release analgesics should be used, amounting to one sixth of the equivalent daily dose of oxycodone hydrochloride. The need for more than two 'rescues' per day is usually an indication that the dose of oxycodone and naloxone modified release tablet requires upward adjustment. Adjustment should be made every 1 to 2 days in steps of 5mg/2.5mg tablets twice daily, or where necessary 2.5mg/1.25mg or 10mg/5mg until a stable dose is reached, with the aim of establishing a patient-specific twice daily dose that will maintain adequate analgesia and use as little rescue medication as possible for as long as pain therapy is necessary.

    Restless Leg Syndrome
    The dosage should be adjusted to the sensitivity of the individual patient and should be under the supervision of a clinician with experience in the management of restless legs syndrome.


    Opioid naive patients
    The usual starting dose is 10mg/5mg at 12 hourly intervals.

    Patients already receiving opioids
    May be started on higher doses, depending on their previous opioid experience.

    The maximum daily dose is 160mg oxycodone hydrochloride and 80mg naloxone hydrochloride. Patients requiring higher doses should be administered supplemental modified-release oxycodone at the same time intervals. The analgesic efficacy of the oxycodone and naloxone modified release tablets is equivalent to oxycodone alone modified release preparations. The maximum daily dose of modified release oxycodone hydrochloride is 400mg.

    Oxycodone and naloxone modified release tablets should not be administered for longer than necessary.

    Restless Leg Syndrome
    The usual starting dose is 5mg/2.5mg oxycodone hydrochloride/naloxone hydrochloride at 12 hourly intervals. Titration on a weekly basis is recommended in case higher doses are required. The mean daily dose in the pivotal study was 10mg/5mg every 12 hours. Some patients may benefit from higher daily doses up to a maximum of 30mg/15mg every 12 hours.

    Prior to continuation of treatment beyond 1 year a discharge regimen by gradually tapering down of oxycodone and naloxone over a period of approximately one week should be considered to establish if continued treatment is indicated.


    24 hours post-operatively
    Acute abdomen
    Children under 18 years
    Pre-operative administration
    Risk of paralytic ileus
    Within 2 weeks of discontinuing MAOIs
    Cardiac failure secondary to pulmonary disorder
    Chronic constipation
    Delayed gastric emptying
    Head trauma
    Moderate hepatic impairment
    Paralytic ileus
    Raised intracranial pressure
    Severe asthma
    Severe chronic obstructive pulmonary disease
    Severe respiratory depression

    Precautions and Warnings

    Predisposition to seizures
    Adrenal insufficiency
    Benign prostatic hyperplasia
    Biliary tract disorder
    Cardiovascular disorder
    Delirium tremens
    Epileptic disorder
    Glucose-galactose malabsorption syndrome
    History of alcohol abuse
    History of drug misuse
    Inflammatory bowel disease
    Lactose intolerance
    Mild hepatic impairment
    Mild renal impairment
    Myasthenia gravis
    Opioid dependence
    Partial gastrointestinal obstruction
    Respiratory impairment
    Sleep apnoea
    Toxic psychosis

    Advise patient ability to drive or operate machinery may be impaired
    Advise patient not to drive until they know how the medicine affects them
    Advise patient this medicine may be subject to driving restrictions
    Not all available brands are licensed for all indications
    Some formulations contain lactose
    Monitor patients with renal impairment
    Neonate exposed in utero: Monitor for neonatal withdrawal syndrome
    Patients on long-term therapy should be regularly reviewed
    Potential for drug abuse
    Restless Leg Syndrome: Evaluate continuation of treatment every 3 months
    Restless Leg Syndrome: Review therapy by controlled withdrawal after 1 year
    Restless Leg Syndrome: Treatment to be supervised by a specialist
    Tolerance and dependence may occur
    Consider dose reduction if sleep-related breathing disorders occur
    Increased risk of central sleep apnoea and sleep-related hypoxemia
    Neonate exposed in labour: Risk of respiratory depression
    Prolonged use at high doses may result in hyperalgesia
    Withdrawal symptoms after long-term normal use on abrupt cessation
    May affect results of some laboratory tests
    Progressive withdrawal recommended
    Consider dose reduction or alternative opioid in cases of hyperalgesia
    Advise patient not to take St John's wort concurrently
    Advise patient to avoid alcohol during treatment
    Advise that effects are potentiated by CNS depressants (including alcohol)
    Advise patient grapefruit products may increase plasma level
    Advise patients that empty tablet/capsule may be observed in stools

    Oxycodone and naloxone is contraindicated in patients with a history of opioid abuse for the treatment of RLS.

    Oxycodone and naloxone is not recommended within the first 12 to 24 hours post-operatively. Depending on the type and extent of surgery, the anaesthetic procedure selected, other co-medication and the individual condition of the patient, the exact timing for initiating post-operative treatment with oxycodone and naloxone depends on a careful risk benefit assessment for each individual patient.

    There is no clinical experience in patients with cancer associated to peritoneal carcinomatosis or with sub-occlusive syndrome in advanced stages of digestive and pelvic cancers. The treatment with oxycodone and naloxone in this population is not recommended.

    After complete discontinuation of therapy with oxycodone and naloxone with a subsequent switch to another opioid a worsening of the bowel function is expected.

    In patients under long-term opioid treatment with higher doses of opioids, the switch to oxycodone and naloxone can initially provoke withdrawal symptoms. Such patients may require specific attention. Oxycodone and naloxone is not suitable for the treatment of withdrawal symptoms.

    Pregnancy and Lactation


    Use oxycodone and naloxone with caution during pregnancy.

    The manufacturer concludes that oxycodone and naloxone modified release tablets should only be used during pregnancy if the benefit outweighs the possible risk to foetus or neonate. At the time of writing, there are no data from the use of oxycodone and naloxone modified release tablets in pregnant women and during childbirth. Both oxycodone and naloxone pass into the placenta. No animal studies have currently been performed with oxycodone and naloxone in combination, but animal studies with administration of the single drugs have not revealed any teratogenic or embryotoxic effects. The limited data on the use of oxycodone during pregnancy reveal no evidence of an increased risk of congenital abnormalities.

    Schaefer (2015) indicates that the use of oxycodone is acceptable in pregnancy under strict indication. Long-term use is limited to special situations only. Depending upon dose, timing and duration of exposure, the newborn may suffer from respiratory depression and withdrawal symptoms.


    Oxycodone and naloxone is contraindicated during breastfeeding.

    The manufacturer recommends that breastfeeding should be discontinued during treatment with oxycodone and naloxone modified release tablets. Oxycodone passes into breast milk with a milk-plasma concentration ratio of 3.4:1. Oxycodone effects in the infant are therefore conceivable, including drowsiness in particular. In a case of six exposed neonates, no effects were observed in the nursing infants. It is not known whether naloxone also passes into the breast milk. However, after taking these tablets systemic naloxone levels are very low. A risk to the infant cannot be excluded.

    Schaefer (2015) indicates that oxycodone should not be undertaken during breastfeeding and should be critically viewed, especially in the first postpartum weeks.

    Effects on Ability to Drive and Operate Machinery

    This class of medicine is in the list of drugs included in regulations under 5a of the Road Traffic Act 1988 (England and Wales). When prescribing this medicine: Advise patient the medicine can affect cognitive function and is likely to affect ability to drive. Advise patient not to drive until they know how the medicine affects them.

    Side Effects

    Abdominal distension
    Abdominal pain
    Abnormal thinking
    Accidental injury
    Anaphylactic reaction
    Angina pectoris
    Attention disturbances
    Biliary colic
    Changes of blood pressure
    Chest pain
    Disturbances of appetite
    Dry mouth
    Dry skin
    Erectile dysfunction
    Gingival disorder
    Hearing disturbances
    Herpes simplex
    Hot flushes
    Hypersensitivity reactions
    Impaired co-ordination
    Impaired concentration
    Increases in hepatic enzymes
    Involuntary muscle contractions
    Micturition disorders
    Mood changes
    Mouth ulcers
    Muscle spasm
    Muscle twitch
    Perceptual disturbances
    Peripheral oedema
    Personality change
    Psychomotor hyperactivity
    Reduced libido
    Respiratory depression
    Skin reactions
    Speech disturbances
    Tooth disorder
    Urinary retention
    Visual disturbances
    Weight changes
    Withdrawal symptoms

    Effects on Laboratory Tests

    Athletes must be aware that this medicine may cause a positive reaction to 'anti-doping' tests.


    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last Full Review Date: September 2020

    Reference Sources

    Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 3rd edition (2015) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.

    Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 10th edition (2015) ed. Briggs, G., Freeman, R. Wolters Kluwer Health, Philadelphia.

    Summary of Product Characteristics: Myloxifin 5mg/2.5mg, 10mg/5mg, 20mg/10mg and 40mg/20mg prolonged release tablets. Zentiva. Revised September 2019.

    Summary of Product Characteristics: Oxyargin 5mg/2.5mg, 10mg/5mg, 20mg/10mg and 40mg/20mg prolonged release tablets. Mylan. Revised February 2020.

    Summary of Product Characteristics: Targinact 5mg/2.5mg, 10mg/5mg, 20mg/10mg and 40mg/20mg prolonged release tablets. Napp Pharmaceuticals Ltd. Revised March 2021. Government departments. Department for Transport. Publications. Drug driving and medicine: Advice for healthcare professionals. Drug driving: Guidance for healthcare professionals on drug driving. Available at: Last accessed: 16 September 2020

    New drug driving offence: implications for medicines packaging. Medicines Regulatory News. 10 December 2013. Available at: Last accessed: 16 September 2020

    NICE Evidence Services Available at: Last accessed: 22 February 2021

    US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
    Available at:
    Naloxone Last revised: 20 July 2020
    Last accessed: 16 September 2020

    US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
    Available at:
    Oxycodone Last revised: 20 July 2020
    Last accessed: 16 September 2020

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