Consumer medicine information

Palexia IR

Tapentadol

BRAND INFORMATION

Brand name

Palexia IR

Active ingredient

Tapentadol

Schedule

S8

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Palexia IR.

What is in this leaflet

This leaflet answers some common questions about PALEXIA® IR.

It does not contain all the available information.

It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you having PALEXIA® IR against the benefits they expect it will have for you.

If you have any concerns about this medicine, ask your doctor, nurse or pharmacist.

Keep this leaflet with the medicine. You may need to read it again.

What PALEXIA® IR is used for

PALEXIA® (tapentadol) IR is used to relieve severe pain. This strong pain reliever belongs to a group of medicines known as opioid analgesics.

This medicine is available only with a doctor’s prescription.

Your doctor may have prescribed PALEXIA® IR for another reason.

Ask your doctor if you have any questions about why PALEXIA® IR has been prescribed for you.

Before you take PALEXIA® IR

When you must not take it

You must not take PALEXIA® IR if you:

  • are allergic to tapentadol or any of the ingredients listed at the end of this leaflet. Signs of allergic reaction may include a skin rash, itching, shortness of breath or swelling of the face, lips or tongue
  • have asthma or if your breathing is dangerously slow or shallow (respiratory depression, hypercapnia)
  • have paralysis of the gut
  • have acute poisoning with alcohol, sleeping pills, pain relievers or other psychotropic medicines (medicines that affect mood and emotions)
  • are taking medicine for depression containing a monoamine oxidase inhibitor (MAOI) medicine (such as Nardil, Parnate) or have taken a MAOI within the last 14 days. Ask your doctor or pharmacist if any of your medicines is an MAOI.

Do not take PALEXIA® IR if the packaging is torn or shows signs of tampering or the tablets do not look quite right.

Do not take PALEXIA® IR if the expiry date on the pack has passed.

You should only start taking PALEXIA® IR under direct supervision of your doctor due to the following risks:

Addiction
You can become addicted to PALEXIA® IR even if you take it exactly as prescribed. PALEXIA® IR may become habit forming causing mental and physical dependence. If abused it may become less able to reduce pain.

Dependence
As with all other opioid containing products, your body may become used to you taking PALEXIA® IR. Taking it may result in physical dependence. Physical dependence means that you may experience withdrawal symptoms if you stop taking PALEXIA® IR suddenly, so it is important to take it exactly as directed by your doctor.

Tolerance
Tolerance to PALEXIA® IR may develop, which means that the effect of the medicine may decrease. If this happens, more may be needed to maintain the same effect.

Withdrawal
Continue taking your medicine for as long as your doctor tells you. If you stop having this medicine suddenly, your pain may worsen and you may experience some or all of the following withdrawal symptoms:

  • nervousness, restlessness, agitation, trouble sleeping or anxiety
  • body aches, weakness or stomach cramps
  • loss of appetite, nausea, vomiting or diarrhoea
  • increased heart rate, breathing rate or pupil size
  • watery eyes, runny nose, chills or yawning
  • increased sweating.

If you are not sure whether you should start taking this medicine, talk to your doctor.

Before you start to take it

Tell your doctor if you:

  • have slow or shallow breathing
  • have sleep-related breathing disorders
  • suffer from increased pressure in the brain or disturbed consciousness up to coma
  • have had a head injury or a brain tumour
  • have had an epileptic fit or seizure or if you have an increased risk of having epileptic fits or seizures
  • suffer from a liver or kidney disease
  • suffer from a pancreatic or biliary tract disease including pancreatitis
  • are breastfeeding
  • are pregnant, or planning to become pregnant
  • have an addiction or history of abuse of alcohol, opioids or other drugs
  • have been told that you have an intolerance to some sugars. Lactose is an ingredient in these tablets.

Tell your doctor if you are pregnant or planning to become pregnant. You should not take PALEXIA® IR during pregnancy unless your doctor has told you to do so. Taking PALEXIA® IR during pregnancy may lead to withdrawal symptoms in the newborn baby. You should not take PALEXIA® IR during labour as it can cause breathing problems and signs of withdrawal in the newborn. Your doctor will discuss the risks and benefits of using PALEXIA® IR.

Tell your doctor if you are breastfeeding. You should not take PALEXIA® IR if you are breastfeeding as it may pass into your breast milk.

Taking other medicines

Tell your doctor if you are using any other medicines, including any that you buy without a prescription from a pharmacy, supermarket or health food shop.

Some medicines and PALEXIA® IR may interfere with each other. These medicines include:

  • medicines for depression, sleeplessness or mental conditions such as selective serotonin reuptake inhibitors (SSRI’s), serotonin-norephinephrine reuptake inhibitors (SNRI’s), tricyclic anti-depressants (TCAs), monoamine oxidase inhibitor (MAOIs) and triptans
  • other pain relievers such as morphine or codeine
  • some cough medicines
  • general anaesthetics such as propofol or midazolam (examples are Propofol™ or Midazolam™)
  • medicines that slow the brain activity (central nervous system (CNS) depressants or phenothiazines). These medicines can be used to treat anxiety, muscle tension, pain, insomnia, acute stress reactions, panic attacks or seizure disorders such as sleeping pills, tranquilizers, hypnotics or sedatives (examples are Stelazine™, Largactil™, Valium™, Temaze™, or Xanax™).

Taking these medicines with PALEXIA® IR may increase the risk of possible side effects (see Side Effects). Your breathing may become seriously slow or shallow (respiratory depression) and your blood pressure may decrease. Your consciousness may be decreased, you may feel drowsier or feel that you might faint. If this happens tell your doctor.

Do not take PALEXIA® IR with alcohol. Some side effects such as drowsiness may be increased.

Other medications can also interfere with PALEXIA® IR and make you feel drowsy (see Warning information at the start of this document). Ask your doctor or pharmacist for more information.

How to take PALEXIA® IR

You should only start taking PALEXIA® IR under the direct supervision of your doctor.

Your doctor will tell you how much you should take, when and how often. It is important that you take this medicine as directed by your doctor.

If you are unsure ask your doctor or pharmacist.

How much to take

The usual dose is 1 tablet every 4 to 6 hours.

Your doctor may prescribe a different, more appropriate dose or interval of dosing, if this is necessary for you.

If you feel that the effect of these tablets is too strong or too weak, talk to your doctor or pharmacist.

PALEXIA® IR is not suitable for children and adolescents below the age of 18 years.

In elderly patients (above 65 years) usually no dose adjustment is necessary. However, the excretion of tapentadol may be delayed in some patients of this age group. If this applies to you, your doctor may recommend a different dosage regimen.

Patients with severe liver problems should not take these tablets. If you have moderate problems, your doctor will recommend a different dosage regimen.

Patients with severe kidney problems should not take these tablets.

Carefully follow all directions given to you by your doctor and pharmacist. These directions may differ from the information in this leaflet.

When and how should you take the tablets

PALEXIA® IR tablets should be swallowed whole with water. They may be taken, before, with, or after food.

Do not chew, divide or break the tablets. Chewing, dividing or breaking the tablets will release the medicine quickly and side effects may then occur.

How long to take it

This differs between individuals depending on how severe your pain is, how you respond to PALEXIA® IR and the cause of your pain. Ask your doctor for advice on how long you need to take PALEXIA® IR.

Carefully follow all directions given to you by your doctor and pharmacist. These directions may differ from the information contained in this leaflet.

If you forget to take it

If you forget to take a dose, you can take it as soon as you remember. The next dose should be taken after four or six hours, or as prescribed by your doctor.

Do not take a double dose to make up for the dose that you missed.

If you take too much (overdose)

If you or someone else receive too much (overdose), and experience one or more of the symptoms below, call triple zero (000) for an ambulance. Keep the person awake by talking to them or gently shaking them every now and then. You should follow the above steps even if someone other than you have accidentally used PALEXIA® IR that was prescribed for you. If someone takes an overdose, they may experience one or more of the following symptoms:

  • Slow, unusual or difficult breathing
  • Drowsiness, dizziness or unconsciousness
  • Slow or weak heartbeat
  • Nausea or vomiting
  • Convulsions or fits

If you think you or someone else may have taken too much PALEXIA® IR, you should immediately:

  • phone the Poisons Information Centre (by calling 13 11 26), or
  • contact your doctor, or
  • go to the Emergency Department at your nearest hospital.

You should do this even if there are no signs of discomfort or poisoning.

When seeking medical attention, take this leaflet and remaining medicine with you to show the doctor. Also tell them about any other medicines or alcohol which have been taken.

While you are taking PALEXIA® IR

Things you must do

Be sure to keep all of your doctor’s appointments so that your progress can be checked.

If you are about to be started on any new medicine, tell your doctor and pharmacist that you are taking PALEXIA® IR.

Tell your doctor if you believe that PALEXIA® IR is not helping your condition.

Tell your doctor if, for any reason, you have not taken your medicine exactly as prescribed. Otherwise your doctor may think it is not working effectively and change your treatment unnecessarily.

If you become pregnant while you are taking PALEXIA® IR, tell your doctor immediately.

If you plan to have surgery, even at the dentist’s, tell your doctor, anaesthetist or dentist that you are taking this medicine. It may affect other medicines used during surgery.

Things you must not do

If you wish to stop treatment, please tell your doctor first before stopping treatment. Do not stop taking this medicine unless your doctor tells you to. If your doctor wants you to stop taking your tablets, he/she will tell you how to do this. This may include a gradual reduction in the dose.

Some people may feel unwell if they suddenly stop taking PALEXIA® IR. If you suddenly stop taking PALEXIA® IR you may experience withdrawal symptoms (see Withdrawal section above).

Do not give PALEXIA® IR to anyone else, even if they have the same condition as you.

Do not take PALEXIA® IR for any other complaints unless your doctor tells you to.

Things to be careful of

Do not drive or operate heavy machinery until you know how PALEXIA® IR affects you. PALEXIA® IR can make you sleepy, dizzy, or lightheaded.

Do not drink alcohol while you are taking PALEXIA® IR tablets. Drinking alcohol while taking PALEXIA® IR may make you feel more sleepy and increase the risk of serious side effects, such as shallow breathing, with the risk of stopping breathing and loss of consciousness.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking PALEXIA® IR.

Like all medicines, PALEXIA® IR can cause some unwanted side effects in some people. Sometimes they are serious, most of the time they are not. Side effects not listed in this leaflet may occur in some patients. You may need to get medical attention if you get some of the side effects.

Ask your doctor or pharmacist to answer any questions you may have.

Very common:

  • nausea
  • vomiting
  • dizziness
  • drowsiness
  • headache.

Common:

  • decreased appetite
  • anxiety
  • confusion
  • hallucination
  • difficulty sleeping
  • abnormal dreams
  • trembling
  • flushing or reddening of the face and neck
  • constipation
  • diarrhoea
  • indigestion
  • dry mouth
  • itching
  • increased sweating
  • rash
  • muscle cramps
  • feeling of weakness
  • fatigue
  • feeling of body temperature change.

Uncommon:

  • depressed mood
  • disorientation
  • excitability (agitation)
  • nervousness
  • restlessness
  • euphoric mood
  • disturbance in attention
  • memory impairment
  • near fainting
  • sedation
  • difficulty in controlling movements
  • difficulty in speaking
  • numbness
  • abnormal sensations of the skin (e.g. tingling, prickling)
  • muscle twitches
  • abnormal vision
  • faster or irregular heart beat
  • decreased blood pressure
  • dangerously slow or shallow breathing
  • shortness of breath
  • abdominal discomfort
  • hives
  • sensation of heaviness
  • delay in passing urine
  • frequent urination
  • drug withdrawal syndrome (see “Things you must not do”)
  • accumulation or retention of water in the tissues (oedema)
  • feeling abnormal
  • feeling drunk
  • irritability
  • feeling of relaxation.

Rare:

  • allergic reaction
  • thinking abnormal thoughts
  • epileptic fit
  • depressed level of consciousness
  • abnormal coordination
  • slower heart beat
  • impaired gastric emptying.

If any of the following happen, tell your doctor or go to accident and emergency at your nearest hospital immediately:

  • skin rash (red spots or patches), itching, hives
  • swelling of the face, lips, mouth or throat which may cause difficulty in swallowing or breathing
  • chest tightness, wheezing or pain in the chest
  • heart palpitations
  • faintness or collapse
  • hallucinations
  • seizures, fits or convulsions.

These are very serious side effects. If you have them, you may have had a serious allergic reaction to PALEXIA® IR. You may need urgent medical attention or hospitalisation.

If you notice any unwanted effects not mentioned in this leaflet, please inform your doctor, or pharmacist.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

After using PALEXIA® IR

Storage

Keep PALEXIA® IR tablets in the blister pack until it is time to take them.

Keep your tablets in a cool, dry place where the temperature stays below 30°C.

Do not store PALEXIA® IR in the bathroom or near a sink.

Do not leave them in a car or on a window sill Heat and dampness can destroy some medicines.

Keep PALEXIA® IR tablets where children cannot reach them. A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Disposal

If you no longer need to use this medicine or it is out of date, take it to any pharmacy for safe disposal.

Do not use this medicine after the expiry date.

Product Description

There are 3 distinct strengths of PALEXIA® IR tablets:

PALEXIA® IR 50 mg tablets
White round shaped film-coated tablets of 7 mm diameter, marked with Grünenthal logo on one side and “H6” on the other side.

PALEXIA® IR 75 mg tablets
Pale yellow round shaped film-coated tablets of 8 mm diameter, marked with Grünenthal logo on one side and “H7” on the other side.

PALEXIA® IR 100 mg tablets
Pale pink round shaped film-coated tablets of 9 mm diameter, marked with Grünenthal logo on one side and “H8” on the other side.

The registered pack sizes for PALEXIA® IR tablets are:5, 10, 14, 20, 28, 30, 40, 50, 56, 60, 90 and 100 tablets.

All strengths and pack sizes may not be available.

PALEXIA® IR tablets are sealed in a blister foil pack.

Ingredients

Active ingredients

PALEXIA® IR 50 mg tablets - each tablet contains 50 mg tapentadol (as hydrochloride).

PALEXIA® IR 75 mg tablets - each tablet contains 75 mg tapentadol (as hydrochloride).

PALEXIA® IR 100 mg tablets - each tablet contains 100 mg tapentadol (as hydrochloride).

Inactive ingredients

PALEXIA® IR tablets also contain the following inactive ingredients:

  • microcrystalline cellulose
  • lactose monohydrate
  • croscarmellose sodium
  • povidone (K30)
  • magnesium stearate
  • polyvinyl alcohol
  • titanium dioxide (E171)
  • macrogol 3350
  • purified talc
  • iron oxide yellow (E172) (75 and 100 mg tablets only)
  • iron oxide red (E172) (75 and 100 mg tablets only)
  • iron oxide black (E172) (100 mg tablets only).

PALEXIA® IR contains lactose.

PALEXIA® IR does not contain:

  • gluten
  • preservative.

Further information

You can obtain more information from your doctor or pharmacist.

Australian sponsor:

Seqirus Pty Ltd
ABN 26 160 735 035
63 Poplar Road
Parkville, VIC 3052
Australia

PALEXIA® IR is distributed in Australia by:

Seqirus(Australia) Pty Ltd
ABN 66 120 398 067
63 Poplar Road
Parkville, VIC 3052
Australia

PALEXIA® IR is manufactured by:

Grünenthal GmBH, Germany

Australian Registration Numbers:

PALEXIA® IR 50 mg tablets
AUST R 165310

PALEXIA® IR 75 mg tablets
AUST R 165317

PALEXIA® IR 100 mg tablets
AUST R 165318

This leaflet was prepared in September 2020.

PALEXIA® is a registered trademark of Grünenthal GmBH, used under licence.

Published by MIMS December 2020

BRAND INFORMATION

Brand name

Palexia IR

Active ingredient

Tapentadol

Schedule

S8

 

Boxed Warnings

Limitations of use. Because of the risks associated with the use of opioids, Palexia IR should only be used in patients for whom other treatment options, including non-opioid analgesics, are ineffective, not tolerated or otherwise inadequate to provide appropriate management of pain (see Section 4.4 Special Warnings and Precautions for Use).
Hazardous and harmful use. Palexia IR poses risks of hazardous and harmful use which can lead to overdose and death. Assess the patient's risk of hazardous and harmful use before prescribing and monitor the patient regularly during treatment (see Section 4.4 Special Warnings and Precautions for Use).
Life threatening respiratory depression. Serious, life-threatening or fatal respiratory depression may occur with the use of Palexia IR. Be aware of situations which increase the risk of respiratory depression, modify dosing in patients at risk and monitor patients closely, especially on initiation or following a dose increase (see Section 4.4 Special Warnings and Precautions for Use).
Concomitant use of benzodiazepines and other central nervous system (CNS) depressants, including alcohol. Concomitant use of opioids with benzodiazepines, gabapentinoids, antihistamines, tricyclic antidepressants, antipsychotics, cannabis or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death. Limit dosages and durations to the minimum required; and monitor patients for signs and symptoms of respiratory depression and sedation. Caution patients not to drink alcohol while taking Palexia IR.

1 Name of Medicine

Tapentadol (as hydrochloride).

2 Qualitative and Quantitative Composition

Palexia IR tablets contain 50, 75 or 100 mg tapentadol (as hydrochloride).
Palexia IR tablets contain lactose.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Palexia IR 50 mg tapentadol (as hydrochloride) immediate release tablets. White round shape biconvex film-coated tablets with Grünenthal logo embossed on one side and "H6" engraving on the other side.
Palexia IR 75 mg tapentadol (as hydrochloride) immediate release tablets. Pale yellow round shape biconvex film-coated tablets with Grünenthal logo embossed on one side and "H7" engraving on the other side.
Palexia IR 100 mg tapentadol (as hydrochloride) immediate release tablets. Pale pink round shape biconvex film-coated tablets with Grünenthal logo embossed on one side and "H8" engraving on the other side.

4 Clinical Particulars

4.9 Overdose

Experience with Palexia IR overdose is very limited. Preclinical data suggest that symptoms similar to those of other centrally acting analgesics with mu-opioid receptor agonist activity are to be expected upon intoxication with tapentadol. In the clinical setting, these symptoms may include miosis, vomiting, cardiovascular collapse, consciousness disorders up to coma, convulsions and respiratory depression up to respiratory arrest.
Management of overdose should be focused on treating symptoms of mu-opioid receptor agonism. Primary attention should be given to re-establishment of a patent airway and institution of assisted or controlled ventilation when overdose of Palexia IR is suspected. Pure opioid antagonists such as naloxone, are specific antidotes to respiratory depression resulting from opioid overdose. Respiratory depression following an overdose may outlast the duration of action of the opioid antagonist. Administration of an opioid antagonist is not a substitute for continuous monitoring of airway, breathing, and circulation following an opioid overdose. If the response to opioid antagonists is suboptimal or only brief in nature, an additional antagonist should be administered as directed by the manufacturer of the product.
Gastrointestinal decontamination may be considered in order to eliminate unabsorbed drug. Gastrointestinal decontamination with activated charcoal may be considered within 2 hours after intake. Before attempting gastrointestinal decontamination, care should be taken to secure the airway.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Tapentadol did not induce gene mutations in bacteria, but was clastogenic at cytotoxic concentrations in an in vitro chromosomal aberration test with metabolic activation in Chinese hamster V79 cells in 1 of 2 assays. The one positive result for tapentadol was not confirmed in vivo in rats, using the two endpoints of chromosomal aberration and unscheduled DNA synthesis, at extrapolated exposures (AUC) similar to the maximum anticipated human exposure. The weight of evidence indicates that tapentadol presents no significant genotoxic potential at clinical doses.
Carcinogenicity. Tapentadol was administered to rats (diet) and mice (oral gavage) for two years. A significant trend towards increased hepatocellular tumours (adenoma and carcinoma) was observed in mice at oral doses of 100 mg/kg/day or greater. A dose related increased incidence of hepatocellular hypertrophy (but not tumours) was observed in rats at dietary doses of 125 mg/kg/day or greater. Exposures (plasma AUC) in both species were less than that at the maximum recommended clinical dose. These findings may derive from adaptive changes following hepatic enzyme induction. The potential clinical relevance is unknown.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Palexia IR immediate release tablets contain tapentadol hydrochloride (HCl) which is a centrally acting synthetic analgesic combining mu-agonist and noradrenaline re-uptake inhibition activity in a single molecule. Tapentadol is a white to off-white powder; freely soluble in water and methanol, and soluble in ethanol. The pKa1 is 9.36 and pKa2 is 10.37 determined in 0.15 M KCl solution. The partition coefficient is defined as the ratio of the equilibrium concentrations of a single neutral molecular species in a 1-octanol/aqueous buffered solution 2-phase system. The value of log P for tapentadol hydrochloride in 1-octanol/water is 2.89 ± 0.01. The chemical name for tapentadol HCl is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl] phenol monohydrochloride. The molecular weight of tapentadol HCl is 257.80, and the empirical formula is C14H23NO.HCl.
Chemical structure. The structural formula of tapentadol HCl (CAS number: 175591-09-0) is:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSTAPHYD.gif CAS number. (CAS number: 175591-09-0).

7 Medicine Schedule (Poisons Standard)

Controlled Drug, S8.

Summary Table of Changes

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