lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Oral solution
CAUTIONARY AND ADVISORY LABELS10 ELECTROLYTES:May contain Phosphate, sodium
▶Fleet Phospho-soda(Casen Recordati S.L.)
Disodium hydrogen phosphate dodecahydrate 240 mg per 1 ml, Sodium dihydrogen phosphate dihydrate 542 mg per 1 mlFleet Phospho-soda oral solution sugar-free|90mlp £4.79 Enema
▶Sodium acid phosphate with sodium phosphate (Non-proprietary)
Disodium hydrogen phosphate dodecahydrate 80 mg per 1 ml, Sodium dihydrogen phosphate dihydrate 100 mg per 1 mlPhosphates enema (Formula B)128ml long tube|1enemap
£27.93DT price = £27.93
Phosphates enema (Formula B)128ml standard tube|1enemap
£3.98DT price = £3.98
▶Fleet Ready-to-use(Casen Recordati S.L.)
Disodium hydrogen phosphate dodecahydrate 80 mg per 1 ml, Sodium dihydrogen phosphate dihydrate 181 mg per 1 mlCleen Ready-to-use133ml enema|1enemap£0.68
LAXATIVES
›
SELECTIVE 5-HT4RECEPTOR AGONISTSPrucalopride
24-Feb-2016▶Adult:Up to500mg daily in divided doses, adjusted according to response
▶BY RECTUM
▶Adult:120mg for1dose
Adjunct in abdominal radiological procedures
▶BY MOUTH
▶Adult:400mg, to be administered with barium meal
▶BY RECTUM
▶Adult:120mg for1dose PHARMACOKINETICS
Oral preparations act within1–2days; response to rectal administration usually occurs within20minutes.
lUNLICENSED USEAdult oral solution and capsulesnot licensed for use in children under12years.
lCONTRA-INDICATIONSAvoid in intestinal obstruction lCAUTIONSDo not give with liquid paraffin
.
excessive useof stimulant laxatives can cause diarrhoea and related effects such as hypokalaemia
.
rectal preparations not indicated if haemorrhoids or analfissurelINTERACTIONS→Appendix1: docusate sodium lSIDE-EFFECTSAbdominal cramp
.
diarrhoea (excessiveuse)
.
hypokalaemia.
rashlPREGNANCYNot known to be harmful—manufacturer advises caution.
lBREAST FEEDING
▶With oral usePresent in milk following oral administration—manufacturer advises caution.
▶With rectal use Rectal administration not known to be harmful.
lDIRECTIONS FOR ADMINISTRATION
▶With oral use in childrenFor administrationby mouth, solution may be mixed with milk or squash.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Oral solution
▶Docusate sodium (Non-proprietary)
Docusate sodium 2.5 mg per 1 mlDocusate12.5mg/5ml oral solution sugar free sugar-free|300mlp£7.79DT price = £5.29 Docusate sodium 10 mg per 1 mlDocusate50mg/5ml oral solution sugar free sugar-free|300mlp £7.99DT price = £7.99
▶Docusol(Typharm Ltd)
Docusate sodium 2.5 mg per 1 mlDocusol Paediatric12.5mg/5ml oral solution sugar-free|300mlp £5.29DT price = £5.29 Enema
▶Norgalax(Essential Pharma Ltd)
Docusate sodium 12 mg per 1 gramNorgalax120mg/10g enema| 6enemap £28.00
Capsule
▶Dioctyl(UCB Pharma Ltd)
Docusate sodium 100 mgDioctyl100mg capsules|30capsulep
£2.09DT price = £2.09|100capsulep£6.98
▶DulcoEase(Boehringer Ingelheim Self-Medication Division) Docusate sodium 100 mgDulcoEase100mg capsules|30 capsuleG £3.20DT price = £2.09
Combinations available:Co-danthrusate,p.60
Liquid paraffin
12-Apr-2016 lINDICATIONS AND DOSEConstipation
▶BY MOUTH
▶Adult:10–30mL daily if required, to be administered at night
lCONTRA-INDICATIONSChildren under3years lCAUTIONSAvoid prolonged use
lSIDE-EFFECTSAnal irritation after prolonged use
.
anal seepage of paraffin after prolonged use.
granulomatousreactions caused by absorption of small quantities of liquid paraffin (especially from the emulsion)
.
interference with the absorption of fat-soluble vitamins.
lipoid pneumonia lPRESCRIBING AND DISPENSING INFORMATIONWhenprepared extemporaneously, the BP states Liquid Paraffin Oral Emulsion, BP consists of liquid paraffin5mL, vanillin 5mg, chloroform0.025mL, benzoic acid solution0.2mL, methylcellulose-20 200mg, saccharin sodium 500micrograms, water to10mL.
lPATIENT AND CARER ADVICEOral emulsion should not be taken immediately before going to bed.
lLESS SUITABLE FOR PRESCRIBINGLiquid Paraffin Oral Emulsion BP is less suitable for prescribing.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Liquid
▶Liquid paraffin (Non-proprietary)
Liquid paraffin 1 ml per 1 mlLiquid paraffin liquid|150mlp
£1.49
Liquid paraffin with magnesium hydroxide
The properties listed below are those particular to the combination only. For the properties of the components please consider, liquid paraffin above, magnesium hydroxide p.57.
lINDICATIONS AND DOSE Constipation
▶BY MOUTH
▶Adult:5–20mL as required
lPRESCRIBING AND DISPENSING INFORMATIONLiquid paraffin and magnesium hydroxide preparations are on sale to the public.
When prepared extemporaneously, the BP states Liquid Paraffin and Magnesium Hydroxide Oral Emulsion, BP consists of25% liquid paraffin in aqueous suspension containing6% hydrated magnesium oxide.
lLESS SUITABLE FOR PRESCRIBINGLiquid paraffin with magnesium hydroxide is less suitable for prescribing.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
No licensed medicines listed.
LAXATIVES
›
STIMULANT LAXATIVESBisacodyl
lINDICATIONS AND DOSE Constipation
▶BY MOUTH
▶Child 4–17 years:5–20mg once daily, adjusted according to response, dose to be taken at night
▶Adult:5–10mg once dailyIncreased if necessary up to 20mg once daily, dose to be taken at night
▶BY RECTUM
▶Child 2–17 years:5–10mg once daily, adjusted according to response
▶Adult:10mg once daily, dose to be taken in the morning
Bowel clearance before radiological procedures and surgery
▶INITIALLY BY MOUTH
▶Adult:10mg twice daily, does to be taken in the morning and evening on the day before continued
→
BNF74
Constipation 59
Gastro-intestinalsystem
1
procedure and (by rectum)10mg, to be administered 1–2hours before procedure the following day PHARMACOKINETICS
Tablets act in10–12hours; suppositories act in 20–60minutes.
lCONTRA-INDICATIONSAcute abdominal conditions (in children)
.
acute inflammatory bowel disease.
acute surgical abdominal conditions (in adults).
intestinal obstruction.
severe dehydrationlCAUTIONSExcessive use of stimulant laxatives can cause diarrhoea and related effects such as hypokalaemia
.
risk of electrolyte imbalance with prolonged use (in children) lINTERACTIONS→Appendix1: bisacodyllSIDE-EFFECTS GENERAL SIDE-EFFECTS
Abdominal cramp
.
colitis.
nausea.
vomiting SPECIFIC SIDE-EFFECTS▶With rectal useLocal irritation
lPREGNANCYMay be suitable for constipation in pregnancy, if a stimulant effect is necessary.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug. Forms available from special-order manufacturers include: oral suspension, suppository, enema Gastro-resistant tablet
CAUTIONARY AND ADVISORY LABELS5, 25
▶Bisacodyl (Non-proprietary)
Bisacodyl 5 mgBisacodyl5mg gastro-resistant tablets|60 tabletp £3.25DT price = £1.96|100tabletp£5.40|500 tabletp £25.73|1000tabletp £51.45
▶Dulco-Lax (bisacodyl)(Boehringer Ingelheim Self-Medication Division)
Bisacodyl 5 mgDulcolax5mg gastro-resistant tablets|40tabletp
£2.44|100tabletp£3.60 Enema
▶Bisacodyl (Non-proprietary)
Bisacodyl 333.333 microgram per 1 mlFleet Bisacodyl10mg/30ml enema|1enemaP no price available
Suppository
▶Bisacodyl (Non-proprietary)
Bisacodyl 10 mgBisacodyl10mg suppositories|12suppositoryp
£3.53DT price = £3.53
▶Dulco-Lax (bisacodyl)(Boehringer Ingelheim Self-Medication Division)
Bisacodyl 5 mgDulcolax5mg suppositories for children|5 suppositoryp £1.04DT price = £1.04
Bisacodyl 10 mgDulcolax10mg suppositories|12suppositoryp
£2.35DT price = £3.53
Co-danthramer
lINDICATIONS AND DOSE
Constipation in terminally ill patients (standard strength capsules)
▶BY MOUTH USING CAPSULES
▶Child 6–11 years:1capsule once daily, dose should be taken at night
▶Child 12–17 years:1–2capsules once daily, dose should be taken at night
▶Adult:1–2capsules once daily, dose should be taken at night
Constipation in terminally ill patients (strong capsules)
▶BY MOUTH USING CAPSULES
▶Child 12–17 years:1–2capsules once daily, dose should be given at night
▶Adult:1–2capsules once daily, dose should be given at night
Constipation in terminally ill patients (standard strength suspension)
▶BY MOUTH USING ORAL SUSPENSION
▶Child 2–11 years: 2.5–5mL once daily, dose should be taken at night
▶Child 12–17 years:5–10mL once daily, dose should be taken at night
▶Adult:5–10mL once daily, dose should be taken at night
Constipation in terminally ill patients (strong suspension)
▶BY MOUTH USING ORAL SUSPENSION
▶Child 12–17 years:5mL once daily, dose should be taken at night
▶Adult:5mL once daily, dose should be taken at night DOSE EQUIVALENCE AND CONVERSION
▶Co-danthramer (standard strength) capsules contain dantron25mg with poloxamer‘188’200mg per capsule.
▶Co-danthramer (standard strength) oral suspension contains dantron25mg with poloxamer‘188’200mg per5mL.
▶Co-danthramerstrongcapsules contain dantron 37.5mg with poloxamer‘188’500mg.
▶Co-danthramerstrongoral suspension contains dantron75mg with poloxamer‘188’1g per5mL.
▶Co-danthramer suspension5mL = one co-danthramer capsule,butstrong co-danthramer suspension5mL = two strong co-danthramer capsules.
lCONTRA-INDICATIONSAcute abdominal conditions (in children)
.
acute inflammatory bowel disease.
acute surgical abdominal conditions (in adults).
intestinalobstruction
.
severe dehydrationlCAUTIONSExcessive use of stimulant laxatives can cause diarrhoea and related effects such as hypokalaemia
.
may cause local irritation.
rodentstudies indicate potential carcinogenic riskCAUTIONS, FURTHER INFORMATION
▶Local irritationAvoid prolonged contact with skin (as in incontinent patients or infants wearing nappies—risk of irritation and excoriation).
lINTERACTIONS→Appendix1: dantron
lSIDE-EFFECTSAbdominal cramp
.
urine may be coloured redlPREGNANCYManufacturers advise avoid—limited information available.
lBREAST FEEDINGManufacturers advise avoid—no information available.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug. No licensed capsule preparations identified.
Oral suspension
CAUTIONARY AND ADVISORY LABELS14(urine red)
▶Co-danthramer (Non-proprietary)
Dantron 5 mg per 1 ml, Poloxamer 188 40 mg per 1 ml Co-danthramer25mg/200mg/5ml oral suspension sugar free sugar-free
|300mlP£146.39DT price = £146.39
Dantron 15 mg per 1 ml, Poloxamer 188 200 mg per 1 ml Co-danthramer75mg/1000mg/5ml oral suspension sugar free sugar-free
|300mlP£293.63DT price = £293.63
Co-danthrusate
20-Apr-2016 lINDICATIONS AND DOSEConstipation in terminally ill patients
▶BY MOUTH USING CAPSULES
▶Child 6–11 years:1capsule once daily, to be taken at night
60 Constipation and bowel cleansing
BNF74Gastro-intestinalsystem
1
▶Child 12–17 years:1–3capsules once daily, to be taken at night
▶Adult:1–3capsules once daily, to be taken at night
▶BY MOUTH USING ORAL SUSPENSION
▶Child 6–11 years:5mL once daily, to be taken at night
▶Child 12–17 years:5–15mL once daily, to be taken at night
▶Adult:5–15mL once daily, to be taken at night DOSE EQUIVALENCE AND CONVERSION
▶Co-danthrusate suspension contains dantron50mg and docusate60mg per5mL.
▶Co-danthrusate capsules contain dantron50mg and docusate60mg per capsule.
lCONTRA-INDICATIONSAcute abdominal conditions (in children)
.
acute inflammatory bowel disease.
acute surgical abdominal conditions (in adults).
intestinal obstruction.
severe dehydrationlCAUTIONSExcessive use of stimulant laxatives can cause diarrhoea and related effects such as hypokalaemia
.
may cause local irritation.
rodentstudies indicate potential carcinogenic riskCAUTIONS, FURTHER INFORMATION
▶Local irritationAvoid prolonged contact with skin (as in incontinent patients or infants wearing nappies—risk of irritation and excoriation).
lINTERACTIONS→Appendix1: dantron, docusate sodium lSIDE-EFFECTSAbdominal cramp
.
urine may be colouredred
lPREGNANCYManufacturers advise avoid—limited information available.
lBREAST FEEDINGManufacturers advise avoid—no information available.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Oral suspension
CAUTIONARY AND ADVISORY LABELS14(urine red)
▶Co-danthrusate (Non-proprietary)
Dantron 10 mg per 1 ml, Docusate sodium 12 mg per 1 ml Co-danthrusate50mg/60mg/5ml oral suspension sugar free sugar-free| 200mlP £89.92DT price = £89.92
Capsule
CAUTIONARY AND ADVISORY LABELS14(urine red)
▶Co-danthrusate (Non-proprietary)
Dantron 50 mg, Docusate sodium 60 mgCo-danthrusate 50mg/60mg capsules|63capsuleP no price available DT price =
£52.50
Glycerol
(Glycerin)
lINDICATIONS AND DOSE Constipation
▶BY RECTUM
▶Child 1–11 months:1g as required
▶Child 1–11 years:2g as required
▶Child 12–17 years:4g as required
▶Adult:4g as required
lINTERACTIONS→Appendix1: glycerol
lDIRECTIONS FOR ADMINISTRATIONMoisten suppositories with water before insertion.
lPRESCRIBING AND DISPENSING INFORMATIONWhen prepared extemporaneously, the BP states Glycerol Suppositories, BP consists of gelatin140mg, glycerol 700mg, purified water to1g.
lPATIENT AND CARER ADVICE
Medicines for Children leaflet: Glycerin (glycerol) suppositories for constipation www.medicinesforchildren.org.uk/glycerin-glycerol-suppositories-for-constipation
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug. Forms available from special-order manufacturers include: suppository
Suppository
▶Glycerol (Non-proprietary)
Gelatin 140 mg per 1 gram, Glycerol 700 mg per 1 gramGlycerol 2g suppositories|12suppositoryG £1.75DT price = £1.67 Glycerol1g suppositories|12suppositoryG£1.69DT price =
£1.04
Glycerol4g suppositories|12suppositoryG£1.31DT price =
£1.16
Senna
13-Jun-2016lDRUG ACTIONSenna is a stimulant laxative. After metabolism of sennosides in the gut the anthrone component stimulates peristalsis thereby increasing the motility of the large intestine.
lINDICATIONS AND DOSE Constipation
▶BY MOUTH USING TABLETS
▶Child 6–17 years:7.5–30mg once daily, adjusted according to response
▶Adult:7.5–15mg daily (max. per dose30mg daily), dose usually taken at bedtime; initial dose should be low then gradually increased, higher doses may be prescribed under medical supervision
▶BY MOUTH USING SYRUP
▶Child 1 month–3 years: 3.75–15mg once daily, adjusted according to response
▶Child 4–17 years:3.75–30mg once daily, adjusted according to response
▶Adult:7.5–15mg once daily (max. per dose30mg daily), dose usually taken at bedtime, higher doses may be prescribed under medical supervision
PHARMACOKINETICS Onset of action8–12hours.
lUNLICENSED USETabletsnot licensed for use in children under6years.Syrupnot licensed for use in children under 2years.
Doses in BNF adhere to national guidelines and may differ from those in product literature.
lCONTRA-INDICATIONSIntestinal obstruction
.
undiagnosed abdominal pain lINTERACTIONS→Appendix1: senna
lSIDE-EFFECTSAbdominal spasm
.
discoloration of urine.
pruritus
SIDE-EFFECTS, FURTHER INFORMATION
Prolonged or excessive use of stimulant laxatives can cause diarrhoea and related effects such as hypokalaemia.
lPREGNANCYgSpecialist sources indicate suitable for use in pregnancy.k
lBREAST FEEDINGgSpecialist sources indicate suitable for use in breast-feeding in infants over1month.k
lPATIENT AND CARER ADVICE
Medicines for Children leaflet: Senna for constipation www.medicinesforchildren.org.uk/senna-for-constipation lNATIONAL FUNDING/ACCESS DECISIONS
NHS restrictionsSenokot®tablets.
lEXCEPTIONS TO LEGAL CATEGORYSenna is on sale to the public for use in children over12years; doses on packs may vary from those in BNF Publications.
BNF74
Constipation 61
Gastro-intestinalsystem
1
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Oral solution
▶Senokot(Forum Health Products Ltd, Reckitt Benckiser Healthcare (UK) Ltd)
Sennoside B (as Sennosides) 1.5 mg per 1 mlSenokot7.5mg/5ml Syrup Pharmacy sugar free sugar-free|500mlp £4.76DT price =
£4.76 Tablet
▶Senna (Non-proprietary)
Sennoside B (as Sennosides) 7.5 mgSenna7.5mg tablets|20 tabletp £1.00|60tabletp £2.50DT price = £2.01|100 tabletp £2.13
▶Ex-Lax Senna(Novartis Consumer Health UK Ltd)
Sennoside B (as Sennosides) 12 mgEx-Lax Senna12mg pills|20 tabletG £1.54
▶Senokot(Reckitt Benckiser Healthcare (UK) Ltd, Forum Health Products Ltd)
Sennoside B (as Sennosides) 7.5 mgSenokot7.5mg tablets|20 tabletG £1.61|60tabletG £4.20DT price = £2.01|100 tabletG £5.49|500tabletG £12.50
Sennoside B (as Sennosides) 15 mgSenokot Max Strength15mg tablets|24tabletG£3.23|48tabletG £5.69DT price =
£5.69
Senna with ispaghula husk
24-Feb-2016 The properties listed below are those particular to the combination only. For the properties of the components please consider, senna p.61, ispaghula husk p.53.lINDICATIONS AND DOSE Constipation
▶BY MOUTH
▶Child 12–17 years:5–10g once daily, to be taken at night,5g equivalent to one level spoonful of granules
▶Adult:5–10g once daily, to be taken at night,5g equivalent to one level spoonful of granules lINTERACTIONS→Appendix1: senna
lSIDE-EFFECTSUrine coloured yellow or red-brown lPREGNANCYManufacturer advises avoid duringfirst
trimester. To be used only intermittently and only if dietary and lifestyle changes fail.
lDIRECTIONS FOR ADMINISTRATIONTake at night with at least150mL liquid..
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Granules
CAUTIONARY AND ADVISORY LABELS25 EXCIPIENTS:May contain Sucrose
▶Manevac(Meda Pharmaceuticals Ltd)
Senna fruit 124 mg per 1 gram, Ispaghula 542 mg per 1 gramManevac granules|400gramp£9.50DT price = £9.50
Sodium picosulfate
06-May-2016(Sodium picosulphate)
lDRUG ACTIONSodium picosulfate is a stimulant laxative.
After metabolism in the colon it stimulates the mucosa thereby increasing the motility of the large intestine.
lINDICATIONS AND DOSE Constipation
▶BY MOUTH
▶Child 1 month–3 years:2.5–10mg once daily, adjusted according to response
▶Child 4–17 years:2.5–20mg once daily, adjusted according to response
▶Adult:5–10mg once daily, dose to be taken at bedtime PHARMACOKINETICS
Onset of action6–12hours.
lUNLICENSED USESodium picosulfate doses in BNF Publications adhere to national guidelines and may differ from those in product literature.
lCONTRA-INDICATIONSIntestinal obstruction
.
undiagnosed abdominal pain
lINTERACTIONS→Appendix1: sodium picosulfate lSIDE-EFFECTS
▶Common or very commonAbdominal cramp
▶UncommonDizziness
.
nausea.
vomiting▶Frequency not knownAngioedema
.
pruritus.
rash.
syncope
SIDE-EFFECTS, FURTHER INFORMATION
Prolonged or excessive use can cause diarrhoea and related effects such as hypokalaemia.
lPREGNANCYManufacturer states evidence limited but not known to be harmful.
lBREAST FEEDINGgSpecialist sources indicate suitable for use in breast-feeding in infants over1month—not known to be present in milk.k
lPATIENT AND CARER ADVICE
Medicines for Children leaflet: Sodium picosulfate for constipation www.medicinesforchildren.org.uk/sodium-picosulfate-for-constipation
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Oral solution
EXCIPIENTS:May contain Alcohol
▶Sodium picosulfate (Non-proprietary)
Sodium picosulfate 1 mg per 1 mlSodium picosulfate5mg/5ml oral solution sugar free sugar-free|100mlp £2.37sugar-free|300 mlp£7.10DT price = £7.10
▶Dulco-Lax (sodium picosulfate)(Boehringer Ingelheim Self-Medication Division)
Sodium picosulfate 1 mg per 1 mlDulcolax Pico5mg/5ml liquid sugar-free|100mlp £1.94sugar-free|300mlp£4.62DT price
= £7.10
OPIOID RECEPTOR ANTAGONISTS
Methylnaltrexone bromide
12-Dec-2016 lDRUG ACTIONMethylnaltrexone bromide is a peripherallyacting opioid-receptor antagonist. It therefore blocks the gastro-intestinal (constipating) effects of opioids without altering their central analgesic effects.
lINDICATIONS AND DOSE
Opioid-induced constipation in patients with chronic pain (except palliative care patients with advanced illness)
▶BY SUBCUTANEOUS INJECTION
▶Adult:12mg once daily if required, to be given as 4–7doses weekly
Adjunct to other laxatives in opioid-induced constipation in advanced illness (palliative care patients)
▶BY SUBCUTANEOUS INJECTION
▶Adult (body-weight up to 38 kg):150micrograms/kg once daily on alternate days for maximum duration of treatment4months, two consecutive doses may be given24hours apart if no response to treatment on the preceding day
▶Adult (body-weight 38–61 kg):8mg once daily on alternate days for maximum duration of treatment 4months, two consecutive doses may be given 24hours apart if no response to treatment on the preceding day
▶Adult (body-weight 62–114 kg):12mg once daily on alternate days for maximum duration of treatment 4months, two consecutive doses may be given 24hours apart if no response to treatment on the preceding day
62 Constipation and bowel cleansing
BNF74Gastro-intestinalsystem
1
▶Adult (body-weight 115 kg and above):150micrograms/kg once daily on alternate days for maximum duration of treatment4months, two consecutive doses may be given24hours apart if no response to treatment on the preceding day
PHARMACOKINETICS May act within30–60minutes.
lCONTRA-INDICATIONSAcute surgical abdominal conditions
.
gastro-intestinal obstruction lCAUTIONSDiverticular disease (when active).
faecalimpaction
.
gastro-intestinal tract lesions (known or suspected).
patients with colostomy.
patients with peritoneal catheterlSIDE-EFFECTS
▶Common or very commonAbdominal pain
.
diarrhoea.
dizziness
.
flatulence.
injection site reactions.
nausea.
opioid withdrawal symptoms (usually mild to moderate)
.
vomiting
▶Frequency not knownGastro-intestinal perforation Overdose
Symptoms of overdosage include orthostatic hypotension.
lPREGNANCYManufacturer advises avoid unless essential—toxicity at high doses inanimalstudies.
lBREAST FEEDINGManufacturer advises use only if potential benefit outweighs risk—present in milk inanimal studies.
lHEPATIC IMPAIRMENTManufacturer advises avoid in severe impairment—no information available.
lRENAL IMPAIRMENTIf eGFR less than
30mL/minute/1.73m2, reduce dose as follows: body-weight under62kg,75micrograms/kg on alternate days;
body-weight62–114kg,8mg on alternate days; body-weight over114kg,75micrograms/kg on alternate days.
lDIRECTIONS FOR ADMINISTRATIONRotate injection site.
lPRESCRIBING AND DISPENSING INFORMATION Palliative care
For further information on the use of methylnaltrexone in palliative care, seewww.palliativedrugs.com/formulary/en/
opioid-antagonists.html.
lHANDLING AND STORAGEProtect from light.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Solution for injection
▶Relistor(Swedish Orphan Biovitrum Ltd)
Methylnaltrexone bromide 20 mg per 1 mlRelistor12mg/0.6ml solution for injection vials|1vialP £21.05|7vialP £147.35
Naloxegol
20-Jun-2016lDRUG ACTIONNaloxegol is a peripherally acting opioid receptor antagonist. It therefore decreases the constipating effects of opioids without altering their central analgesic effects.
lINDICATIONS AND DOSE
Opioid-induced constipation when response to laxatives inadequate
▶BY MOUTH
▶Adult:25mg once daily, to be taken in the morning DOSE ADJUSTMENTS DUE TO INTERACTIONS
Manufacturer advises reduce initial dose to12.5mg daily with concurrent use of moderate inhibitors of CYP3A4, increasing to25mg daily if well tolerated.
lCONTRA-INDICATIONSGastro-intestinal or peritoneum malignancy (risk of gastro-intestinal perforation)
.
known or suspected gastro-intestinal obstruction.
patients at riskof recurrent gastro-intestinal obstruction
.
recurrent or advanced ovarian cancer (risk of gastro-intestinal perforation).
vascular endothelial growth factor (VEGF) inhibitor treatment (risk of gastro-intestinal perforation) lCAUTIONSAlzheimer’s disease (advanced).
cardiovasculardisease
.
CNS metastases.
congestive heart failure (symptomatic).
Crohn’s disease.
diverticulitis (active or recurrent).
multiple sclerosis (active).
peptic ulcer disease (severe).
primary brain malignancies.
QT interval over 500 milliseconds.
recent history of myocardial infarction (within 6 months)CAUTIONS, FURTHER INFORMATION
▶Disruptions to blood-brain barrierManufacturer advises caution in patients with clinically important disruptions to the blood-brain barrier (e.g. advanced Alzheimer’s disease, active multiple sclerosis, primary brain malignancies)—
risk of uptake into the CNS.
▶Cardiovascular disordersSafety and efficacy has not been established in patients with these conditions.
lINTERACTIONS→Appendix1: naloxegol lSIDE-EFFECTS
▶Common or very commonAbdominal pain (discontinue treatment if severe or persistent)
.
flatulence.
headache.
nausea
.
sweating.
vomiting▶UncommonOpioid withdrawal syndrome (discontinue treatment)
SIDE-EFFECTS, FURTHER INFORMATION
▶Gastro-intestinal effectsManufacturer advises that gastro-intestinal side-effects typically occur shortly after initiation of treatment—consider reducing the dose.
lPREGNANCYManufacturer advises avoid—limited data available but toxicity at high doses inanimalstudies;
theoretical risk of opioid withdrawal in foetus.
lBREAST FEEDINGManufacturer advises avoid—present in milk inanimalstudies and theoretical risk of opioid withdrawal in breast-fed infants.
lHEPATIC IMPAIRMENTManufacturer advises avoid in severe impairment—safety and efficacy not established.
lRENAL IMPAIRMENTManufacturer advises lower initial dose in moderate to severe impairment—initially12.5mg daily, increase to25mg if well tolerated.
lDIRECTIONS FOR ADMINISTRATIONManufacturer advises tablets can be crushed, mixed with120mL of water and taken immediately if patients are unable to swallow tablets whole. The mixture may be administered via a nasogastric tube, if required.
lPATIENT AND CARER ADVICEManufacturer advises patients report severe, persistent or worsening gastro-intestinal effects (such as abdominal pain) to their prescriber.
lNATIONAL FUNDING/ACCESS DECISIONS NICE technology appraisals (TAs)
▶Naloxegol for treating opioid induced constipation (July 2015)NICE TA345
Naloxegol is recommended as a possible treatment for opioid induced constipation in patients whose response to laxatives is inadequate.
www.nice.org.uk/TA345 lMEDICINAL FORMS
There can be variation in the licensing of different medicines containing the same drug.
Tablet
CAUTIONARY AND ADVISORY LABELS23
▶Moventig(Kyowa Kirin Ltd)A
Naloxegol (as Naloxegol oxalate) 12.5 mgMoventig12.5mg tablets
|30tabletP£55.20DT price = £55.20
Naloxegol (as Naloxegol oxalate) 25 mgMoventig25mg tablets| 30tabletP£55.20DT price = £55.20
BNF74
Constipation 63
Gastro-intestinalsystem