Drugs List

Therapeutic Indications

Uses

Pain - moderate to severe

Moderate to severe acute pain that can only be controlled by opioid analgesics.

Administration

The oral solution may be administered via external tubes, e.g. nasogastric or percutaneous endoscopic gastrostomy (PEG) tubes.

Contraindications

Acute alcohol intoxication
Children under 2 years
Drug intoxication
Impaired consciousness
Risk of paralytic ileus
Weight below 16kg
Within 2 weeks of discontinuing MAOIs
Acute asthma
Breastfeeding
Head trauma
Hepatic impairment in children under 18 years
Paralytic ileus
Pregnancy
Raised intracranial pressure
Renal impairment in children under 18 years
Severe asthma
Severe hepatic impairment
Severe hypercapnia
Severe renal impairment
Severe respiratory depression

Precautions and Warnings

Children aged 2 to 18 years
Elderly
Predisposition to seizures
Acute pancreatitis
Biliary tract disorder
Brain neoplasm
Coma
Drug misuse
Galactosaemia
Glucose-galactose malabsorption syndrome
History of seizures
Lactose intolerance
Moderate hepatic impairment
Respiratory depression
Respiratory impairment

Reduce dose and/or alter dose interval in patients with hepatic impairment
Advise ability to drive/operate machinery may be affected by side effects
Advise patient not to drive until they know how the medicine affects them
Advise patient this medicine may be subject to driving restrictions
Children under 18 years: For hospital use only
Not all available products are licensed for all age groups
Oral liquid contains propylene glycol
Some formulations contain lactose
May cause respiratory depression
Monitor patients for signs and symptoms of Serotonin Syndrome
Monitor patients with a history of alcoholism and drug abuse
Monitor patients with pulmonary insufficiency
Potential for drug abuse
May cause dependence
Avoid abrupt withdrawal
Discontinue if paralytic ileus is suspected
Maintain treatment at the lowest effective dose
Advise patient to avoid alcohol during treatment
Advise that effects are potentiated by CNS depressants (including alcohol)

If dose related respiratory depression occurs it should be treated as any opioid induced respiratory depression.

Paediatric patients with obesity should be extensively monitored and the recommended maximum dose for the age should not be exceeded.

Pregnancy and Lactation

Pregnancy

Tapentadol is contraindicated in pregnancy.

At the time of writing there is limited published information regarding use during pregnancy. The manufacturer recommends using tapentadol only when the potential benefit to the mother outweighs the risk to the foetus. Animal studies have not shown any teratogenic effect, however, delayed development and embryotoxicity were observed.

The effect of tapentadol in labour and delivery in humans is unknown, therefore tapentadol is not recommended for use in women during or immediately before labour or delivery. Due to the opioid activity of tapentadol, newborn infants whose mothers have been taking tapentadol should be monitored for respiratory depression.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Tapentadol is contraindicated in breastfeeding.

At the time of writing there is limited published information regarding use during breastfeeding.

There is no information on the excretion of tapentadol in human milk. Studies in animals have shown that tapentadol is excreted in breast milk therefore a risk to the child can not be excluded. Schaefer (2015) states that a single dose does not require any breastfeeding limitation, but repeated use is not recommended.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Abdominal discomfort
Abnormal thinking
Addiction
Agitation
Allergic reaction
Altered temperature sensation
Anxiety
Asthenia
Ataxia
Attention disturbances
Confusion
Constipation
Convulsions
Decrease in blood pressure
Decrease in heart rate
Decreased appetite
Depressed mood
Diarrhoea
Disorientation
Dizziness
Dream abnormalities
Dry mouth
Dysarthria
Dyspepsia
Dyspnoea
Euphoria
Faintness
Fatigue
Feeling abnormal
Feeling drunk
Flushing
Gastric disorders
Hallucinations
Headache
Hyperhidrosis
Hypersensitivity reactions
Hypoaesthesia
Impaired co-ordination
Impaired consciousness
Impaired memory
Increased heart rate
Involuntary muscle contractions
Irritability
Muscle spasm
Nausea
Nervousness
Oedema
Oxygen saturation decreased
Paraesthesia
Pollakiuria
Pruritus
Rash
Respiratory depression
Restlessness
Sedation
Sensation of heaviness
Serotonin syndrome
Sleep disturbances
Somnolence
Tremor
Urinary hesitancy
Urticaria
Visual disturbances
Vomiting
Withdrawal symptoms

Presentation

Standard release oral formulations of tapentadol (as hydrochloride).

Drugs List

Therapeutic Indications

Uses

Pain - moderate to severe

Moderate to severe acute pain that can only be controlled by opioid analgesics.

Dosage

Dosing should be individualised according to the severity of pain.

Adults

Children

Patients with Hepatic Impairment

Administration

The oral solution may be administered via external tubes, e.g. nasogastric or percutaneous endoscopic gastrostomy (PEG) tubes.

Contraindications

Acute alcohol intoxication
Children under 2 years
Drug intoxication
Impaired consciousness
Risk of paralytic ileus
Weight below 16kg
Within 2 weeks of discontinuing MAOIs
Acute asthma
Breastfeeding
Head trauma
Hepatic impairment in children under 18 years
Paralytic ileus
Pregnancy
Raised intracranial pressure
Renal impairment in children under 18 years
Severe asthma
Severe hepatic impairment
Severe hypercapnia
Severe renal impairment
Severe respiratory depression

Precautions and Warnings

Children aged 2 to 18 years
Elderly
Predisposition to seizures
Acute pancreatitis
Biliary tract disorder
Brain neoplasm
Coma
Drug misuse
Galactosaemia
Glucose-galactose malabsorption syndrome
History of seizures
Lactose intolerance
Moderate hepatic impairment
Respiratory depression
Respiratory impairment

Reduce dose and/or alter dose interval in patients with hepatic impairment
Advise ability to drive/operate machinery may be affected by side effects
Advise patient not to drive until they know how the medicine affects them
Advise patient this medicine may be subject to driving restrictions
Children under 18 years: For hospital use only
Not all available products are licensed for all age groups
Oral liquid contains propylene glycol
Some formulations contain lactose
May cause respiratory depression
Monitor patients for signs and symptoms of Serotonin Syndrome
Monitor patients with a history of alcoholism and drug abuse
Monitor patients with pulmonary insufficiency
Potential for drug abuse
May cause dependence
Avoid abrupt withdrawal
Discontinue if paralytic ileus is suspected
Maintain treatment at the lowest effective dose
Advise patient to avoid alcohol during treatment
Advise that effects are potentiated by CNS depressants (including alcohol)

If dose related respiratory depression occurs it should be treated as any opioid induced respiratory depression.

Paediatric patients with obesity should be extensively monitored and the recommended maximum dose for the age should not be exceeded.

Pregnancy and Lactation

Pregnancy

Tapentadol is contraindicated in pregnancy.

At the time of writing there is limited published information regarding use during pregnancy. The manufacturer recommends using tapentadol only when the potential benefit to the mother outweighs the risk to the foetus. Animal studies have not shown any teratogenic effect, however, delayed development and embryotoxicity were observed.

The effect of tapentadol in labour and delivery in humans is unknown, therefore tapentadol is not recommended for use in women during or immediately before labour or delivery. Due to the opioid activity of tapentadol, newborn infants whose mothers have been taking tapentadol should be monitored for respiratory depression.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Tapentadol is contraindicated in breastfeeding.

At the time of writing there is limited published information regarding use during breastfeeding.

There is no information on the excretion of tapentadol in human milk. Studies in animals have shown that tapentadol is excreted in breast milk therefore a risk to the child can not be excluded. Schaefer (2015) states that a single dose does not require any breastfeeding limitation, but repeated use is not recommended.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

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 discomfort
Abnormal thinking
Addiction
Agitation
Allergic reaction
Altered temperature sensation
Anxiety
Asthenia
Ataxia
Attention disturbances
Confusion
Constipation
Convulsions
Decrease in blood pressure
Decrease in heart rate
Decreased appetite
Depressed mood
Diarrhoea
Disorientation
Dizziness
Dream abnormalities
Dry mouth
Dysarthria
Dyspepsia
Dyspnoea
Euphoria
Faintness
Fatigue
Feeling abnormal
Feeling drunk
Flushing
Gastric disorders
Hallucinations
Headache
Hyperhidrosis
Hypersensitivity reactions
Hypoaesthesia
Impaired co-ordination
Impaired consciousness
Impaired memory
Increased heart rate
Involuntary muscle contractions
Irritability
Muscle spasm
Nausea
Nervousness
Oedema
Oxygen saturation decreased
Paraesthesia
Pollakiuria
Pruritus
Rash
Respiratory depression
Restlessness
Sedation
Sensation of heaviness
Serotonin syndrome
Sleep disturbances
Somnolence
Tremor
Urinary hesitancy
Urticaria
Visual disturbances
Vomiting
Withdrawal symptoms

Overdosage

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 ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: February 2018

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.

Summary of Product Characteristics: Palexia film coated tablets. Grunenthal Ltd. Revised November 2018.

Summary of Product Characteristics: Palexia 20 mg/ml oral solution. Grunenthal Ltd. Revised June 2019.

Gov.uk. 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: https://www.gov.uk Last accessed: 6 January 2015
New drug driving offence implications for medicines packaging. Medicines Regulatory News. 10 December 2013. Available at: https://www.mhra.gov.uk Last accessed: 6 January 2015

MHRA Drug Safety Update January 2019
Available at: https://www.mhra.gov.uk
Last accessed: 07 March 2019