TARGINACT Prolonged release tablet Ref.[50554] Active ingredients: Naloxone Oxycodone Oxycodone and Naloxone

Posology

TarginAct is for oral administration and must be swallowed whole and not broken or chewed. It may be taken with or without food with sufficient liquid.

Pain

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

TarginAct is taken at the determined dosage, twice daily according to a fixed time schedule. While symmetric administration (the same dose mornings and evenings) subject to a fixed time schedule (every 12 hours) is appropriate for the majority of patients, some patients, depending on the individual pain situation, may benefit from asymmetric dosing tailored to their pain pattern. In general, the lowest effective analgesic dose should be selected.

Unless otherwise prescribed, TarginAct should be administered as follows:

Adults:

The usual starting dose for an opioid naïve patient is 10 mg/5 mg of oxycodone hydrochloride/naloxone hydrochloride at 12 hourly intervals.

Patients already receiving opioids may be started on higher doses of TarginAct, depending on their previous opioid experience. Patients requiring higher doses are recommended TarginAct 20 mg/10 mg or TarginAct 40 mg/20 mg.

TarginAct 5 mg/2,5 mg is intended for dose titration when initiating opioid therapy and individual dose adjustment. The maximum daily dose of TarginAct is 80 mg oxycodone hydrochloride and 40 mg naloxone hydrochloride.

Patients taking TarginAct according to a regular time schedule may require immediaterelease analgesics as “rescue” medication for breakthrough pain. TarginAct is a prolongedrelease formulation and therefore not intended for the treatment of breakthrough pain. For the treatment of breakthrough pain, a single dose of “rescue medication” should approximate 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 TarginAct requires upward adjustment. This adjustment should be made every 1-2 days in steps of twice daily 5 mg/2,5 mg, or where demanded 10 mg/5 mg, oxycodone hydrochloride/naloxone hydrochloride until a stable dose is reached.

The aim is to establish a patient-specific, twice daily dose that will maintain adequate analgesia and make use of as little rescue medication as possible for as long as pain therapy is necessary.

Restless Legs Syndrome

TarginAct is indicated for patients suffering from Restless Legs Syndrome (RLS) for at least 6 months. RLS symptoms should be present daily and during daytime (≥ 4 days/week). TarginAct should be used after failure of previous dopaminergic treatment. Dopaminergic treatment failure is defined as inadequate initial response, a response that has become inadequate with time, occurrence of augmentation or unacceptable tolerability despite adequate doses. Previous treatment with at least one dopaminergic medicinal product should have lasted in general 4 weeks.

A shorter period might be acceptable in case of unacceptable tolerability with dopaminergic therapy.

The dosage should be adjusted to the sensitivity of the individual patient. Treatment of patients with RLS with TarginAct should be under the supervision of a clinician with experience in the management of RLS.

There is no clinical experience with TarginAct in the long-term treatment of RLS beyond 1 year.

TarginAct should be administered as follows:

Adults:

The usual starting dose is 5 mg/2,5 mg of 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 20 mg/10 mg oxycodone hydrochloride/naloxone hydrochloride. Some patients may benefit from higher daily doses up to a maximum of 60 mg/30 mg oxycodone hydrochloride/naloxone hydrochloride.

TarginAct is taken at the determined dosage twice daily according to a fixed time schedule. While symmetric administration (the same dose mornings and evenings) subject to a fixed time schedule (every 12 hours) is appropriate for the majority of patients, some patients, depending on the individual situation, may benefit from asymmetric dosing tailored to the individual patient. In general, the lowest effective dose should be selected.

Special populations

Elderly patients

As for younger adults the dosage should be adjusted to the intensity of the pain and the sensitivity of the individual patient.

Duration of use: TarginAct should not be administered for longer than absolutely necessary. If long-term pain treatment is necessary in view the nature and severity of the illness, careful and regular monitoring is required to establish whether and to what extent further treatment is necessary. When the patient no longer requires opioid therapy, it may be advisable to taper the dose gradually (see section 4.4).

Adult patients with impaired hepatic function

A clinical trial has shown that plasma concentrations of both oxycodone and naloxone are elevated in patients with hepatic impairment. Naloxone concentrations were affected to a higher degree than oxycodone (see section 5.2). The clinical relevance of a relative high naloxone exposure in hepatic impaired patients is yet not known. Caution must be exercised when administering TarginAct to patients with mild hepatic impairment (see section 4.4). In patients with moderate and severe hepatic impairment TarginAct is contraindicated (see section 4.3).

Adult patients with impaired renal function

A clinical trial has shown that plasma concentrations of both oxycodone and naloxone are significantly elevated in patients with renal impairment and is contraindicated (see section 5.2 and section 4.3). Naloxone concentrations were affected to a higher degree than oxycodone. The clinical relevance of a relative high naloxone exposure in renal impaired patients is yet not known. TarginAct is contraindicated in moderate to severe renal impairment. Caution should be exercised when administering TarginAct to patients with mild renal impairment (see section 4.3).

Paediatric population

Children and adolescents under 18 years

The safety and efficacy of TarginAct in patients below the age of 18 years of age has not been established. TarginAct should not be used in children below the age of 18.

Method of administration

TarginAct is for oral administration and must be swallowed whole and not broken or chewed. It may be taken with or without food with sufficient liquid.

Symptoms of intoxication

Depending on the history of the patient, an overdose of TarginAct may be manifested by symptoms that are either triggered by oxycodone (opioid receptor agonist) or by naloxone (opioid receptor antagonist).

Symptoms of oxycodone overdose include miosis, respiratory depression, somnolence progressing to stupor, skeletal muscle flaccidity, bradycardia as well as hypotension. Coma, non-cardiogenic pulmonary oedema and circulatory failure may occur in more severe cases and may lead to a fatal outcome.

Symptoms of a naloxone overdose alone are unlikely.

Therapy of intoxication

Withdrawal symptoms due to an overdose of naloxone should be treated symptomatically in a closely-supervised environment.

Clinical symptoms suggestive of an oxycodone overdose may be treated by the administration of opioid antagonists (e.g. naloxone 0,4-2 mg intravenously). Administration should be repeated at 2-3 minute intervals, as clinically necessary. It is also possible to apply an infusion of 2 mg naloxone in 500 ml of 0,9% sodium chloride or 5% dextrose (0,004 mg/ml naloxone). The infusion should run at a rate aligned to the previously administered bolus doses and to the patient’s response.

Consideration may be given to gastric lavage.

Supportive measures (artificial ventilation, oxygen, vasopressors and infusions) should be employed, as necessary, to manage the circulatory shock accompanying an overdose. Cardiac arrest or dysrhythmias may require cardiac massage or defibrillation. Artificial ventilation should be applied if necessary. Fluid and electrolyte metabolism should be maintained.

36 months.

Store at or below 25°C.

Do not remove from the outer carton until required for use.

TarginAct is supplied in clear PVC and silver aluminium foil blister packs of 28, which are enclosed in a cardboard carton.