Palexia retard

Package leaflet: Information for the patient

Palexia retard, 50 mg, prolonged-release tablets
Palexia retard, 100 mg, prolonged-release tablets
Palexia retard, 150 mg, prolonged-release tablets
Palexia retard, 200 mg, prolonged-release tablets
Palexia retard, 250 mg, prolonged-release tablets
Tapentadol
Please read carefully the entire leaflet before using this medicine, as it contains important information for you.

• Keep this leaflet for future reference.
• If you have any questions, please consult your doctor, pharmacist, or nurse.
• This medicine has been prescribed for a specific individual. Do not share it with others. This medicine may harm others, even if their symptoms are similar.
• If you experience any adverse reactions, including any not listed in this leaflet, inform your doctor, pharmacist, or nurse. See section 4.

Table of contents

1. What Palexia retard is and what it is used for
2. Important information before taking Palexia retard
3. How to take Palexia retard
4. Possible side effects
5. How to store Palexia retard
6. Contents of the pack and other information

1. What Palexia retard is and what it is used for

Tapentadol – the active substance in Palexia retard – is an analgesic belonging to the group of strong opioids. Palexia retard is indicated for the treatment of:

• chronic severe pain in adults, when only an opioid analgesic therapy is expected to be adequate for pain management;
• chronic severe pain in children above 6 years of age and adolescents, which can be properly managed only by opioid analgesics.

2. Important information before using Palexia retard

When not to use Palexia retard:

• if the patient is allergic to tapentadol or any of the other ingredients of this medicine (listed in section 6),
• in patients with asthma or dangerously slow and shallow breathing (respiratory depression, elevated carbon dioxide levels in the blood),
• in patients with intestinal obstruction,
• in cases of acute alcohol, sedative, analgesic or other psychotropic drug intoxication (drugs affecting mood and emotions) (see "Palexia retard and other medicines").

Warnings and precautions
Before starting treatment with Palexia retard, discuss the following with your doctor or pharmacist:

• if you have slow or shallow breathing,
• if you have increased intracranial pressure or disturbances of consciousness up to coma,
• in patients after head injury or with brain tumours,
• in patients with liver or kidney disease (see "How to take Palexia retard"),
• in patients with diseases of the pancreas or biliary tract, including pancreatitis,
• in patients taking medicines with mixed agonist-antagonist properties at the mu-opioid receptors (e.g. pentazocine, nalbuphine) or medicines that are partial agonists of the mu-opioid receptor (e.g. buprenorphine),
• in patients with a tendency to seizures or convulsions, or when taking other medicines that increase the risk of seizures and may increase seizure risk.

Tolerance, dependence and abuse
This medicine contains tapentadol, which is an opioid medicine. Repeated use of opioid-containing medicines may lead to reduced effectiveness of the medicine (the body becomes accustomed to it, known as tolerance). Repeated use of Palexia retard may lead to dependence, abuse and addiction, which may result in life-threatening overdose. The risk of such adverse effects may increase with higher doses and prolonged duration of use. Dependence or addiction may lead to loss of control over the amount or frequency of medicine intake. The risk of developing dependence or addiction varies among individuals. Increased risk of developing abuse or dependence on Palexia retard may occur in individuals with the following conditions:

• the patient or any family member has ever abused or been dependent on alcohol, prescription medicines or illicit drugs ("addiction"),
• the patient is a smoker,
• the patient has ever had mood disorders (depression, anxiety or personality disorders) or has been treated by a psychiatrist for other mental disorders.

If any of the following symptoms occur during treatment with Palexia retard, this may indicate developing dependence or addiction:

• need to take the medicine longer than prescribed by the doctor,
• need to take a higher dose than recommended,
• feeling the need to continue taking the medicine even if it does not help relieve pain,
• using the medicine for reasons other than recommended, e.g. "to calm down" or "to help fall asleep",
• repeated unsuccessful attempts to stop or control medicine use,
• feeling unwell after stopping the medicine and feeling better after resuming it ("withdrawal effect").

If any of these symptoms are observed, the patient should consult a doctor to discuss the best treatment plan, including the appropriate timing and safe way to discontinue treatment (see section 3 Discontinuation of Palexia retard).

Children and adolescents
Children and adolescents with obesity should be closely monitored, and the maximum recommended dose should not be exceeded. Palexia retard should not be given to children under 6 years of age.

Sleep-related breathing disorders
Palexia retard may cause sleep-related breathing disorders such as sleep apnoea (pauses in breathing during sleep) and hypoxaemia (low blood oxygen levels). Symptoms may include breathing pauses during sleep, nocturnal awakenings due to breathlessness, difficulty maintaining sleep or excessive daytime sleepiness. If the patient or someone else observes such symptoms, contact a doctor. The doctor may consider reducing the dose.

Palexia retard and other medicines
Tell your doctor or pharmacist about all medicines you are currently taking, have recently taken or plan to take.

The risk of adverse effects increases if the patient takes medicines that may cause seizures (epileptic fits), such as antidepressants or antipsychotics. The risk of seizures may increase if the patient takes Palexia retard at the same time. Your doctor will advise whether Palexia retard is appropriate for you.

Concomitant use of Palexia retard and sedative medicines such as benzodiazepines or benzodiazepine-like drugs [e.g. certain sleeping tablets or sedatives (e.g. barbiturates) or analgesics such as opioids, morphine and codeine (also used as cough suppressants), antipsychotics, H1 antihistamines, alcohol] increases the risk of drowsiness, breathing difficulties (respiratory depression), coma and may be life-threatening. Therefore, concomitant use of such medicines should only be considered when no other treatment options are available.

If your doctor prescribes Palexia retard together with sedative medicines, the dose and duration of concomitant treatment should be limited.

Concomitant use of opioids and medicines used to treat epilepsy, neuropathic pain or anxiety (gabapentin and pregabalin) increases the risk of opioid overdose, respiratory depression and may be life-threatening.

Inform your doctor if you are taking gabapentin or pregabalin or any sedative medicine and strictly follow your doctor's dosage instructions. It may be helpful to inform friends or family members so they are aware of the above-mentioned objective and subjective symptoms. If such symptoms occur, contact your doctor.

If you are taking medicines that affect serotonin levels (e.g. certain medicines used to treat depression), consult your doctor before taking Palexia retard due to the risk of "serotonin syndrome". Serotonin syndrome is rare but may be life-threatening. Symptoms include: uncontrolled, rhythmic muscle contractions, including those affecting eye movements, agitation, excessive sweating, tremor, increased reflexes including increased muscle tone and body temperature above 38°C. If this occurs, seek medical advice.

The concomitant use of Palexia retard with mixed mu-opioid receptor agonist/antagonist medicines (e.g. pentazocine, nalbuphine) or partial mu-opioid receptor agonists (e.g. buprenorphine) has not been studied. Palexia retard may not work properly if used simultaneously with the above-mentioned medicines.

Inform your doctor immediately if you are currently taking any of the medicines listed above.

Concomitant use of Palexia retard with strong inhibitors or inducers (e.g. rifampicin, phenobarbital, St. John's wort) of enzymes necessary for the elimination of tapentadol from the body may affect the action of tapentadol or may cause adverse effects, especially when starting or stopping their administration. Inform your doctor about all medicines currently being taken.

Palexia retard must not be used concomitantly with MAO inhibitors (medicines used to treat depression). Inform your doctor if these medicines have been used within the last 14 days.

The risk of adverse effects may increase if the patient takes Palexia retard together with the following medicines with anticholinergic effects:

• antidepressants
• medicines used to treat allergies, motion sickness or nausea (antihistamines and antiemetics)
• medicines used to treat psychiatric disorders (antipsychotics or neuroleptics)
• muscle relaxants
• medicines used to treat Parkinson's disease

Palexia retard with food, drink and alcohol
Do not drink alcohol while taking Palexia retard, as some adverse effects such as drowsiness may be intensified. The medicine can be taken regardless of meals.

Pregnancy, breastfeeding and fertility
If you are pregnant, breastfeeding, think you may be pregnant, or are planning to have a baby, consult your doctor or pharmacist before using this medicine.

Do not use Palexia retard:

• during pregnancy, unless your doctor decides it is necessary. Long-term use of tapentadol during pregnancy may cause withdrawal symptoms in newborns, which may be life-threatening if not recognised and treated by a doctor.
• during childbirth, as it may cause dangerous slowing or shallowing of the newborn's breathing (respiratory depression),
• during breastfeeding, as the medicine may be excreted in breast milk.

Driving and operating machinery
Palexia retard may cause drowsiness, dizziness, blurred vision and affect reaction ability. These symptoms may occur especially at the beginning of treatment with Palexia retard, after a dose change recommended by the doctor, or when alcohol or sedative medicines are taken concomitantly. Ask your doctor whether driving and operating machinery are permitted after taking the medicine.

Palexia retard contains lactose
If the patient has previously been diagnosed with intolerance to certain sugars, the patient should contact the doctor before taking the medicine.

3. How to use Palexia retard

This medicine should always be used as directed by the physician. In case of doubt, consult your doctor or pharmacist.
Before starting treatment and regularly during treatment, your doctor will discuss with you what to expect from using Palexia retard, when and for how long it should be taken, when to contact your doctor, and when the medicine should be discontinued (see also section "Stopping Palexia retard").

Dosage should be adjusted according to the intensity of pain and individual patient sensitivity. The lowest effective dose that adequately relieves pain should be used.

Adults
The usual starting dose is 50 mg every 12 hours.
Your doctor may recommend a different dose or dosing interval if necessary.
If you feel the medicine's effect is too strong or too weak, consult your doctor or pharmacist.
Total daily doses exceeding 500 mg of tapentadol are not recommended.

Elderly patients
Dosage adjustment is usually not required in elderly patients (over 65 years of age).
Drug elimination may be prolonged in patients in this age group, and therefore your doctor may recommend an alternative dosing regimen.

Patients with impaired liver or kidney function
This medicine should not be used in patients with severe liver impairment.
In cases of moderate liver impairment, your doctor will recommend an alternative dosing regimen.
Patients with mild liver impairment do not require dose adjustment.
This medicine should not be used in patients with severe kidney impairment.
Dose adjustment is not required in patients with mild or moderate kidney impairment.

Use in children and adolescents
The dose of Palexia retard in children and adolescents aged 6 years to less than 18 years depends on age and body weight.
The appropriate dose will be determined by the doctor. The total daily dose should not exceed 500 mg, i.e. 250 mg administered every 12 hours.
This medicine should not be used in children and adolescents with kidney or liver impairment.
Palexia retard should not be used in children under 6 years of age.

Method of administration
Palexia retard should be taken orally.
The tablet should be swallowed whole with an adequate amount of liquid.
Do not chew, break, or crush the tablet, as this may lead to overdose due to too rapid release of the active substance into the body.
The medicine may be taken with or without food.
The empty tablet shell may pass undigested and may be visible in the stool. This is not a cause for concern, as the active substance has already been absorbed by the body and only the tablet shell remains in the stool.

Duration of treatment
Do not use the tablets for longer than recommended by your doctor.

Overdose of Palexia retard
After taking very large doses, the following symptoms may occur:

• Pinpoint pupils, vomiting, drop in blood pressure, rapid heartbeat, collapse, disturbances of consciousness or coma (deep unconsciousness), seizures, dangerously slow or shallow breathing or respiratory arrest, which may lead to death. In such cases, seek immediate medical attention!

Missed dose of Palexia retard
If you miss a dose, your pain symptoms may return. Do not take a double dose to make up for the missed dose.
Resume your regular dosing schedule.

Stopping Palexia retard
If you stop or discontinue Palexia retard before the end of the prescribed treatment period, your pain symptoms may return. Contact your doctor before stopping the medicine.
Generally, no adverse effects are observed upon discontinuation of the medicine. However, in rare cases, patients who have been taking the medicine for some time and who stop it abruptly may experience general malaise.
The following symptoms may occur:

• Restlessness, lacrimation, runny nose, yawning, sweating, chills, muscle pain, and dilated pupils,
• Irritability, restlessness, back pain, joint pain, weakness, abdominal cramps, difficulty sleeping, nausea, loss of appetite, vomiting, diarrhoea, increased blood pressure, respiratory rate, and heart rate.
  If any of these symptoms occur, consult your doctor immediately. Do not stop taking the medicine abruptly unless instructed by your doctor. Your doctor will advise you on how to discontinue the medicine. Discontinuation may involve gradually reducing the dose.
  If you have any further doubts about using this medicine, consult your doctor or pharmacist.

4. Possible adverse effects

Like all medicines, this medicine can cause adverse effects, although not everybody will experience them. In children and adolescents, no additional adverse effects have been observed compared to those occurring in adults.

Important adverse effects or symptoms to watch for and what to do if they occur:

This medicine may cause allergic reactions. Symptoms may include wheezing, difficulty breathing, swelling of the eyelids, face or lips, rash or itching, particularly affecting the whole body.

Another serious adverse effect is excessive slowing and shallowness of breathing. This most commonly occurs in elderly and weakened patients.

If any of these serious adverse effects affect you, contact your doctor immediately.

Other adverse effects that may occur:

Very common (may affect more than 1 in 10 people): nausea, constipation, dizziness, somnolence, headache.

Common (may affect less than 1 in 10 people): loss of appetite, anxiety, depressed mood, sleep disturbances, nervousness, motor restlessness, difficulty concentrating, tremor, muscle spasms, facial flushing, shortness of breath, vomiting, diarrhoea, indigestion, itching, excessive sweating, rash, feeling of weakness, fatigue, sensation of body temperature change, dryness of mucous membranes, fluid retention (oedema).

Uncommon (may affect less than 1 in 100 people): allergic reactions to the medicine (including skin swelling, urticaria, and in severe cases difficulty breathing, low blood pressure, collapse or shock), weight loss, disorientation, confusion, agitation, perceptual disturbances, unusual dreams, euphoric mood, impaired level of consciousness, memory impairment, psychiatric disturbances, fainting, excessive sedation, balance disorders, speech disorders, paraesthesia, abnormal skin sensations (e.g. tingling, pricking), visual disturbances, increased heart rate, decreased heart rate, palpitations, decreased arterial blood pressure, abdominal discomfort, urticaria, difficulty in urination, increased frequency of urination, sexual dysfunction, withdrawal syndrome (see "Discontinuation of Palexia retard"), feeling of abnormality, irritability.

Rare (may affect less than 1 in 1000 people): drug dependence, thought disorders, seizures, feeling of impending fainting, coordination disorders, dangerously slow or shallow breathing (respiratory depression), delayed gastric emptying, sensation of alcohol intoxication, feeling of relaxation.

Frequency not known (frequency cannot be estimated from available data): delirium.

Generally, the likelihood of suicidal thoughts and behaviours is higher in patients with chronic pain. Additionally, medicines used in the treatment of depression (which affect the neurotransmitter system in the brain) may increase this risk, especially at the beginning of treatment. Although tapentadol also affects neurotransmitters, data obtained from its use in humans have not provided evidence of an increased risk.

Reporting of adverse effects

If any adverse effects occur, including any not listed in this leaflet, tell your doctor, pharmacist or nurse. Adverse effects can be reported directly to the Department of Monitoring Adverse Drug Reactions of the Office for Registration of Medicinal Products, Medical Devices and Biocidal Products, Al. Jerozolimskie 181C, 02-222 Warsaw, Tel.: +48 22 49 21 301, Fax: +48 22 49 21 309, Website: https://smz.ezdrowie.gov.pl

Adverse effects can also be reported to the marketing authorisation holder.

Reporting adverse effects helps to provide more information on the safety of the medicine.

5. How to store Palexia retard

Keep this medicine out of sight and reach of children.
Do not use this medicine after the expiry date stated on the cardboard box and blister.
The expiry date refers to the last day of the stated month.
No special precautions regarding storage of this medicine are required.
Medicines must not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer in use. This will help protect the environment.

6. Contents of the pack and other information

What Palexia retard contains

• The active substance is tapentadol.
  Palexia retard 50 mg prolonged-release tablets: Each tablet contains 50 mg of tapentadol (as hydrochloride).
  Palexia retard 100 mg prolonged-release tablets: Each tablet contains 100 mg of tapentadol (as hydrochloride).
  Palexia retard 150 mg prolonged-release tablets: Each tablet contains 150 mg of tapentadol (as hydrochloride).
  Palexia retard 200 mg prolonged-release tablets: Each tablet contains 200 mg of tapentadol (as hydrochloride).
  Palexia retard 250 mg prolonged-release tablets: Each tablet contains 250 mg of tapentadol (as hydrochloride).

• Other ingredients are:
  Palexia retard 50 mg prolonged-release tablets
  Tablet core: hypromellose, microcrystalline cellulose, colloidal anhydrous silica, magnesium stearate.
  Tablet coating Opadry II white 33G28488: hypromellose, lactose monohydrate, talc, macrogol, propylene glycol, titanium dioxide (E 171).
  Palexia retard 100 mg prolonged-release tablets
  Tablet core: hypromellose, microcrystalline cellulose, colloidal anhydrous silica, magnesium stearate.
  Tablet coating Opadry II yellow 33G32826: hypromellose, lactose monohydrate, talc, macrogol, propylene glycol, titanium dioxide (E 171), iron oxide yellow (E 172).
  Palexia retard 150 mg prolonged-release tablets
  Tablet core: hypromellose, microcrystalline cellulose, colloidal anhydrous silica, magnesium stearate.
  Tablet coating Opadry II pink 33G34210: hypromellose, lactose monohydrate, talc, macrogol, propylene glycol, titanium dioxide (E 171), iron oxide yellow (E 172), iron oxide red (E 172).
  Palexia retard 200 mg prolonged-release tablets
  Tablet core: hypromellose, microcrystalline cellulose, colloidal anhydrous silica, magnesium stearate.
  Tablet coating Opadry II orange 33G23931: hypromellose, lactose monohydrate, talc, macrogol, propylene glycol, titanium dioxide (E 171), iron oxide yellow (E 172), iron oxide red (E 172).
  Palexia retard 250 mg prolonged-release tablets
  Tablet core: hypromellose, microcrystalline cellulose, colloidal anhydrous silica, magnesium stearate.
  Tablet coating Opadry II red 33G35200: hypromellose, lactose monohydrate, talc, macrogol, propylene glycol, titanium dioxide (E 171), iron oxide yellow (E 172), iron oxide red (E 172), iron oxide black (E 172).

What Palexia retard looks like and contents of the pack
Palexia retard 50 mg prolonged-release tablets: White, prolonged-release coated tablets, elongated in shape (6.5 mm x 15 mm), marked with the Grünenthal logo on one side and "H1" on the other side.
Palexia retard 100 mg prolonged-release tablets: Pale yellow, prolonged-release coated tablets, elongated in shape (6.5 mm x 15 mm), marked with the Grünenthal logo on one side and "H2" on the other side.
Palexia retard 150 mg prolonged-release tablets: Pale pink, prolonged-release coated tablets, elongated in shape (6.5 mm x 15 mm), marked with the Grünenthal logo on one side and "H3" on the other side.
Palexia retard 200 mg prolonged-release tablets: Pale orange, prolonged-release coated tablets, elongated in shape (7 mm x 17 mm), marked with the Grünenthal logo on one side and "H4" on the other side.
Palexia retard 250 mg prolonged-release tablets: Brownish-red, prolonged-release coated tablets, elongated in shape (7 mm x 17 mm), marked with the Grünenthal logo on one side and "H5" on the other side.
Palexia retard prolonged-release tablets are packed in blisters and cardboard boxes containing 20, 24, 30, 54 or 60 tablets.
Not all pack sizes may be marketed.

Marketing Authorisation Holder and Manufacturer
Grünenthal GmbH
Zieglerstrasse 6
52078 Aachen
Germany

This medicinal product is authorised in the European Economic Area and in the United Kingdom (Northern Ireland) under the following names:
Austria, Belgium, Croatia, Cyprus, Czech Republic, Germany, Greece, Luxembourg, Netherlands, Poland, Portugal, Slovakia, Spain: PALEXIA retard.
Denmark, Norway, Sweden: PALEXIA Depot.
Ireland, Slovenia, United Kingdom (Northern Ireland): PALEXIA SR.
Italy: PALEXIA.

For further information about this medicinal product, please contact the local representative of the Marketing Authorisation Holder:
Stada Pharm Sp. z o.o.
ul. Krakowiaków 44
02-255 Warsaw
Tel. +48 22 737 79 20