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Drug Details

Palexia 50 mg film-coated tablets

• Drug Class Description
  opioid analgesic
• Generic Name
  Tapentadol hydrochloride
• Presentation
  Film-coated tablet (tablet) White round shaped film-coated tablets of 7 mm diameter, marked with Grünenthal logo on one side and “H6” on the other side.
• Description
  Each film-coated tablet contains 50 mg tapentadol (as hydrochloride). Excipient(s): Palexia 50 mg contains 24.74 mg lactose.
• Indications
  Palexia is indicated for the relief of moderate to severe acute pain in adults, which can be adequately managed only with opioid analgesics.
• Adult Dosage
  

  The dosing regimen should be individualised according to the severity of pain being treated, the previous treatment experience and the ability to monitor the patient. Patients should start treatment with single doses of 50 mg tapentadol as film-coated tablet administered every 4 to 6 hours. Higher starting doses may be necessary depending on the pain intensity and the patient's previous history of analgesic requirements. On the first day of dosing, an additional dose may be taken as soon as one hour after the initial dose, if pain control is not achieved. The dose should then be titrated individually to a level that provides adequate analgesia and minimises undesirable effects under the close supervision of the prescribing physician. Daily doses greater than 700 mg tapentadol on the first day of treatment and maintenance daily doses greater than 600 mg tapentadol have not been studied and are therefore not recommended. As soon as stable dosing regimen is achieved and longer treatment is anticipated, the possibility of switching the patient to therapy with the prolonged-release tablets (Palexia SR) should be considered. As with all symptomatic treatments, the continued use of tapentadol must be evaluated on an ongoing basis.   Discontinuation of treatment Withdrawal symptoms could occur after abrupt discontinuation of treatment with tapentadol (see section 4.8). When a patient no longer requires therapy with tapentadol, it may be advisable to taper the dose gradually to prevent symptoms of withdrawal.   Renal Impairment In patients with mild or moderate renal impairment a dosage adjustment is not required (see section 5.2). Palexia has not been studied in controlled efficacy trials in patients with severe renal impairment, therefore the use in this population is not recommended (see sections 4.4 and 5.2).   Hepatic Impairment In patients with mild hepatic impairment a dosage adjustment is not required (see section 5.2). Palexia should be used with caution in patients with moderate hepatic impairment. Treatment in these patients should be initiated at the lowest available dose strength, i.e. 50 mg tapentadol as film-coated tablet, and not be administered more frequently than once every 8 hours. At initiation of therapy a daily dose greater than 150 mg tapentadol as film-coated tablet is not recommended. Further treatment should reflect maintenance of analgesia with acceptable tolerability, to be achieved by either shortening or lengthening the dosing interval (see sections 4.4 and 5.2). Palexia has not been studied in patients with severe hepatic impairment and therefore, use in this population is not recommended (see sections 4.4 and 5.2).   Elderly Patients (persons aged 65 years and over) In general, a dose adaptation in elderly patients is not required. However, as elderly patients are more likely to have decreased renal and hepatic function, care should be taken in dose selection as recommended (see sections 4.2 and 5.2).   Paediatric Patients The safety and efficacy of Palexia in children and adolescents below 18 years of age has not yet been established. Therefore Palexia is not recommended for use in this population.   Method of administration Palexia should be taken with sufficient liquid. Palexia can be taken with or without food.

   

• Contra Indications
  

  Palexia is contraindicated

  • in patients with hypersensitivity to tapentadol or to any of the excipients (see section 6.1)

  • in situations where active substances with mu-opioid receptor agonist activity are contraindicated, i.e. patients with significant respiratory depression (in unmonitored settings or the absence of resuscitative equipment), and patients with acute or severe bronchial asthma or hypercapnia

  • in any patient who has or is suspected of having paralytic ileus

  • in patients with acute intoxication with alcohol, hypnotics, centrally acting analgesics, or psychotropic active substances

   

• Special Precautions
  

  Potential for Abuse and Addiction/ Dependence Syndrome Palexia has a potential for abuse and addiction. This should be considered when prescribing or dispensing Palexia in situations where there is concern about an increased risk of misuse, abuse, addiction, or diversion. All patients treated with active substances that have mu-opioid receptor agonist activity should be carefully monitored for signs of abuse and addiction.   Respiratory Depression At high doses or in mu-opioid receptor agonist sensitive patients, Palexia may produce dose-related respiratory depression. Therefore, Palexia should be administered with caution to patients with impaired respiratory functions. Alternative non-mu-opioid receptor agonist analgesics should be considered and Palexia should be employed only under careful medical supervision at the lowest effective dose in such patients. If respiratory depression occurs, it should be treated as any mu-opioid receptor agonist-induced respiratory depression (see section 4.9).   Head Injury and Increased Intracranial Pressure Palexia should not be used in patients who may be particularly susceptible to the intracranial effects of carbon dioxide retention such as those with evidence of increased intracranial pressure, impaired consciousness, or coma. Analgesics with mu-opioid receptor agonist activity may obscure the clinical course of patients with head injury. Palexia should be used with caution in patients with head injury and brain tumors.   Seizures Palexia has not been systematically evaluated in patients with a seizure disorder, and such patients were excluded from clinical trials. However, like other analgesics with mu-opioid agonist activity Palexia should be prescribed with care in patients with a history of a seizure disorder or any condition that would put the patient at risk of seizures.   Renal Impairment Palexia has not been studied in controlled efficacy trials in patients with severe renal impairment, therefore the use in this population is not recommended (see section 4.2 and 5.2).   Hepatic Impairment Subjects with mild and moderate hepatic impairment showed a 2-fold and 4.5-fold increase in systemic exposure, respectively, compared with subjects with normal hepatic function. Palexia should be used with caution in patients with moderate hepatic impairment (see section 4.2 and 5.2), especially upon initiation of treatment. Palexia has not been studied in patients with severe hepatic impairment and therefore, use in this population is not recommended (see sections 4.2 and 5.2).   Use in Pancreatic/Biliary Tract Disease Active substances with mu-opioid receptor agonist activity may cause spasm of the sphincter of Oddi. Palexia should be used with caution in patients with biliary tract disease, including acute pancreatitis.   Concomitant treatment with monoamine oxidase inhibitors (MAOI) Treatment with Palexia should be avoided in patients who are receiving monoamine oxidase (MAO) inhibitors or who have taken them within the last 14 days due to potential additive effects on synaptic noradrenaline concentrations which may result in adverse cardiovascular events, such as hypertensive crisis (see section 4.5) Palexia film-coated tablets contain lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption, should not take this medicinal product.

   

• Interactions
  

  Treatment with Palexia should be avoided in patients who are receiving monoamine oxidase (MAO) inhibitors or who have taken them within the last 14 days due to potential additive effects on synaptic noradrenaline concentrations which may result in adverse cardiovascular events, such as hypertensive crisis (see section 4.4)

  Medicinal products like benzodiazepines, barbiturates and opioids (analgesics, antitussives or substitution treatments) may enhance the risk of respiratory depression if taken in combination with Palexia. CNS depressants (e.g. benzodiazepines, antipsychotics, H1-antihistamines, opioids, alcohol) can enhance the sedative effect of tapentadol and impair vigilance. Therefore, when a combined therapy of Palexia with a respiratory or CNS depressant is contemplated, the reduction of dose of one or both agents should be considered.

  In isolated cases there have been reports of serotonin syndrome in a temporal connection with the therapeutic use of tapentadol in combination with serotoninergic medicinal products such as selective serotonin re-uptake inhibitors (SSRIs). Signs of serotonin syndrome may be for example confusion, agitation, fever, sweating, ataxia, hyperreflexia, myoclonus and diarrhoea. Withdrawal of the serotoninergic medicinal products usually brings about a rapid improvement. Treatment depends on the nature and severity of the symptoms.

  There is no clinical data on the concomitant use of Palexia with mixed mu-opioid agonist/antagonists (like pentazocine, nalbuphine) or partial mu-opioid agonists (like buprenorphine). As with pure mu-opioid agonists, the analgesic effect provided by the mu-opioid component of Palexia may be theoretically reduced in such circumstances. Therefore, care should be taken when combining Palexia with these medicinal products.

  The major elimination pathway for tapentadol is conjugation with glucuronic acid mediated via uridine diphosphate transferase (UGT) mainly UGT1A6, UGT1A9 and UGT2B7 isoforms. Thus, concomitant administration with strong inhibitors of these isoenzymes may lead to increased systemic exposure of tapentadol. Interaction studies with active substances that potentially could affect the glucuronidation (paracetamol, acetylsalicylic acid, naproxen and probenecid) did not result in any clinically relevant effect on the serum concentrations of tapentadol (see section 5.2). Interaction studies with substances that can affect absorption of tapentadol (omeprazole and metoclopramide) did not result in any clinically relevant effect on the serum concentrations of tapentadol (see section 5.2).

  For patients on tapentadol treatment, caution should be exercised if concomitant drug administration of strong enzyme inducing drugs (e.g. rifampicin, phenobarbital, St John's Wort (hypericum perforatum)) starts or stops, since this may lead to decreased efficacy or risk for adverse effects, respectively.

• Adverse Drug Reactions
  

  The adverse drug reactions that were experienced by patients in the placebo controlled trials performed with Palexia were predominantly of mild and moderate severity. The most frequent adverse drug reactions were in the gastrointestinal and central nervous system (nausea, vomiting, somnolence, dizziness and headache).

  The table below lists adverse drug reactions that were identified from clinical trials performed with Palexia. They are listed by class and frequency. Frequencies are defined as very common (1/10); common (1/100, <1/10); uncommon (1/1,000, <1/100); rare (1/10,000, <1/1,000); very rare (<1/10,000), not known (cannot be estimated from the available data).

   

  ADVERSE DRUG REACTIONS
  System Organ Class	Frequency
  	Very common	Common	Uncommon	Rare
  Immune system disorders				Hypersensitivity
  Metabolism and nutrition disorders		Decreased appetite
  Psychiatric disorders		Anxiety, Confusional state, Hallucination, Sleep disorder, Abnormal dreams	Depressed mood, Disorientation, Agitation, Nervousness, Restlessness, Euphoric mood	Thinking abnormal
  Nervous system disorders	Dizziness, Somnolence, Headache	Tremor	Disturbance in attention, Memory impairment, Presyncope, Sedation, Ataxia, Dysarthria, Hypoaesthesia, Paraesthesia, Muscle contractions involuntary	Convulsion, Depressed level of consciousness, Coordination abnormal
  Eye disorders			Visual disturbance
  Cardiac disorders			Heart rate increased	Heart rate decreased
  Vascular disorders		Flushing	Blood pressure decreased
  Respiratory, thoracic and mediastinal disorders			Respiratory depression, Oxygen saturation decreased, Dyspnoea,
  Gastrointestinal disorders	Nausea, Vomiting	Constipation, Diarrhoea, , Dyspepsia, Dry mouth	Abdominal discomfort	Impaired gastric emptying
  Skin and subcutaneous tissue disorders		Pruritus, Hyperhidrosis, Rash	Urticaria
  Musculoskeletal and connective tissue disorder		Muscle spasms	Sensation of heaviness
  Renal and urinary disorders			Urinary hesitation, Pollakiuria
  General disorders and administration site conditions		Asthenia, Fatigue, Feeling of body temperature change	Drug withdrawal syndrome, Oedema, Feeling abnormal, Feeling drunk, Irritability, Feeling of relaxation

  Clinical trials performed with Palexia with patient exposure up to 90 days have shown little evidence of withdrawal symptoms upon abrupt discontinuations and these were generally classified as mild, when they occurred. Nevertheless, physicians should be vigilant for symptoms of withdrawal (see section 4.2) and treat patients accordingly should they occur.

  The risk of suicidal ideation and suicides committed is known to be higher in patients suffering from chronic pain. In addition, substances with a pronounced influence on the monoaminergic system have been associated with an increased risk of suicidality in patients suffering from depression, especially at the beginning of treatment. For tapentadol data from clinical trials and post-marketing reports do not provide evidence for an increased risk