Drugs List

Therapeutic Indications

Uses

Treatment of opioid-induced constipation

Administration

Naloxegol tablet can be crushed to a powder and mixed in half a glass of water (120ml) and drunk immediately in patients who are unable to swallow the tablet whole. The glass should be rinsed with a further half glass(120ml) of water and the contents drunk. A nasogastric tube can also be used to administer the mixture in patients unable to swallow the tablet whole. It is important to flush the nasogastric tube through with water after administration of the mixture.

Contraindications

Children under 18 years
Predisposition to gastrointestinal obstruction
Predisposition to gastrointestinal perforation
Breastfeeding
Gastrointestinal malignancy
Gastrointestinal obstruction
Ovarian carcinoma
Pregnancy
Severe hepatic impairment

Precautions and Warnings

Acute peptic ulcer
Advanced Alzheimer's disease
Brain neoplasm
Central nervous system metastasis
Congestive cardiac failure
Crohn's disease
Diverticulitis
Moderate renal impairment
Multiple sclerosis
Tumour infiltration of the gastrointestinal tract
Within 6 months of a myocardial infarction

Reduce dose in patients with moderate renal impairment
Advise patient to take 30 minutes before or 2 hours after breakfast
Advise patient to stop and contact Dr if severe/persistent abdominal pain
Advise patient to inform physician if severe diarrhoea occurs
Advise patient to stop medication & contact GP if signs of opioid toxicity
Advise patient not to take St John's wort concurrently
Grapefruit juice should not be taken simultaneously

Due to limited clinical experience, use naloxegol with caution in patients with cancer-related pain.

Patients with clinically significant disturbances to the blood-brain barrier for example primary brain malignancies, CNS metastases and other inflammatory conditions, active multiple sclerosis, Alzheimer's disease etc. were excluded from clinical trials. These patients may be at risk of naloxegol entry into the CNS and therefore caution should be used.

Patients taking methadone as a primary therapy for their pain had a higher incidence of gastrointestinal adverse reactions in clinical trials. In a few cases symptoms suggestive of opioid withdrawal when taking naloxegol 25mg were observed in patients taking methadone for their pain condition.

Patients taking methadone for the treatment of opioid addiction were excluded from the clinical development programme therefore caution should be used.

Pregnancy and Lactation

Pregnancy

Naloxegol is contraindicated in pregnancy. Limited data exists from the use of naloxegol in pregnant women. There is a theoretical potential for provoking opioid withdrawal in the foetus with use of an opioid receptor antagonist in the mother, who is being treated with a concurrent opioid.

Studies in animals have shown reproductive toxicity where systemic exposures were several times above the therapeutic exposure level.

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

Naloxegol is contraindicated in breastfeeding. It is unknown whether naloxegol is excreted in human milk. Available toxicological data in rats have shown naloxegol is excreted in milk.

At therapeutic doses, most opioids are excreted into breast milk in minimal amounts. There is a theoretical possibility that naloxegol could provoke opioid withdrawal in a breast-fed neonate whose mother is taking an opioid receptor agonist.

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 pain
Diarrhoea
Flatulence
Headache
Hyperhidrosis
Hypersensitivity reactions
Nasopharyngitis
Nausea
Opioid withdrawal syndrome
Vomiting

Presentation

Oral formulations containing naloxegol oxalate.

Drugs List

Therapeutic Indications

Uses

Treatment of opioid-induced constipation

Dosage

Adults

Patients with Renal Impairment

Administration

Naloxegol tablet can be crushed to a powder and mixed in half a glass of water (120ml) and drunk immediately in patients who are unable to swallow the tablet whole. The glass should be rinsed with a further half glass(120ml) of water and the contents drunk. A nasogastric tube can also be used to administer the mixture in patients unable to swallow the tablet whole. It is important to flush the nasogastric tube through with water after administration of the mixture.

Contraindications

Children under 18 years
Predisposition to gastrointestinal obstruction
Predisposition to gastrointestinal perforation
Breastfeeding
Gastrointestinal malignancy
Gastrointestinal obstruction
Ovarian carcinoma
Pregnancy
Severe hepatic impairment

Precautions and Warnings

Acute peptic ulcer
Advanced Alzheimer's disease
Brain neoplasm
Central nervous system metastasis
Congestive cardiac failure
Crohn's disease
Diverticulitis
Moderate renal impairment
Multiple sclerosis
Tumour infiltration of the gastrointestinal tract
Within 6 months of a myocardial infarction

Reduce dose in patients with moderate renal impairment
Advise patient to take 30 minutes before or 2 hours after breakfast
Advise patient to stop and contact Dr if severe/persistent abdominal pain
Advise patient to inform physician if severe diarrhoea occurs
Advise patient to stop medication & contact GP if signs of opioid toxicity
Advise patient not to take St John's wort concurrently
Grapefruit juice should not be taken simultaneously

Due to limited clinical experience, use naloxegol with caution in patients with cancer-related pain.

Patients with clinically significant disturbances to the blood-brain barrier for example primary brain malignancies, CNS metastases and other inflammatory conditions, active multiple sclerosis, Alzheimer's disease etc. were excluded from clinical trials. These patients may be at risk of naloxegol entry into the CNS and therefore caution should be used.

Patients taking methadone as a primary therapy for their pain had a higher incidence of gastrointestinal adverse reactions in clinical trials. In a few cases symptoms suggestive of opioid withdrawal when taking naloxegol 25mg were observed in patients taking methadone for their pain condition.

Patients taking methadone for the treatment of opioid addiction were excluded from the clinical development programme therefore caution should be used.

Pregnancy and Lactation

Pregnancy

Naloxegol is contraindicated in pregnancy. Limited data exists from the use of naloxegol in pregnant women. There is a theoretical potential for provoking opioid withdrawal in the foetus with use of an opioid receptor antagonist in the mother, who is being treated with a concurrent opioid.

Studies in animals have shown reproductive toxicity where systemic exposures were several times above the therapeutic exposure level.

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

Naloxegol is contraindicated in breastfeeding. It is unknown whether naloxegol is excreted in human milk. Available toxicological data in rats have shown naloxegol is excreted in milk.

At therapeutic doses, most opioids are excreted into breast milk in minimal amounts. There is a theoretical possibility that naloxegol could provoke opioid withdrawal in a breast-fed neonate whose mother is taking an opioid receptor agonist.

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

Counselling

Advise patient that naloxegol should be taken in the morning, for patient convenience to avoid bowel movements in the middle of the night.

The tablets may be crushed to a powder and mixed in half a glass of water for patients unable to swallow. The mixture should be used immediately after preparation. The glass should then be rinsed with a further half glass of water and the contents drunk.

Advise patient to take on an empty stomach at least 30 minutes before the first meal or 2 hours after the first meal of the day.

Advise patient to avoid grapefruit products.

Advise patient not to take St John's wort concurrently.

Advise patient to stop medication and contact doctor if signs of opioid toxicity.

Advise patient to stop medication and contact doctor if severe and/or persistent abdominal pain.

Advise patient to inform doctor if severe diarrhoea occurs.

Side Effects

Abdominal pain
Diarrhoea
Flatulence
Headache
Hyperhidrosis
Hypersensitivity reactions
Nasopharyngitis
Nausea
Opioid withdrawal syndrome
Vomiting

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: November 2018

Reference Sources

Summary of Product Characteristics: Moventig 12.5mg and 25mg tablets. Kyowa Kirin Ltd. Revised September 2018.