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Antisecretory drugs and mucosal protectants

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1 Gastro-intestinal system

1.3 Antisecretory drugs and mucosal protectants

Motility stimulants

Domperidone and metoclopramide (section 4.6) are dopamine receptor antago-nists which stimulate gastric emptying and small intestinal transit, and enhance the strength of oesophageal sphincter contraction. Metoclopramide and occa-sionally domperidone can cause acute dystonic reactions—for further details of this and other side-effects, see section 4.6.

A low dose oferythromycin stimulates gastro-intestinal motility and may be used on the advice of a paediatric gastroenterologist to promote tolerance of enteral feeds; erythromycin may be less effective as a prokinetic drug in preterm neonates than in older children.

DOMPERIDONE

Cautions see under Domperidone (section 4.6) Side-effects see under Domperidone (section

4.6); also QT-interval prolongation reported Licensed use not licensed for use in

gastro-intes-tinal stasis; not licensed for use in children for gastro-oesophageal reflux disease

Indication and dose

Gastro-oesophageal reflux disease (but efficacy not proven, see section 1.1), gastro-intestinal stasis

. By mouth

Neonate100–300 micrograms/kg 4–6 times daily before feeds

Child 1 month–12 years200–400 micrograms/

kg (max. 20 mg) 3–4 times daily before food Child 12–18 years10–20 mg, 3–4 times daily before food

Nausea and vomitingsection 4.6

Preparations Section 4.6

ERYTHROMYCIN

Cautions see section 5.1.5; interactions: Appen-dix 1 (macrolides)

Side-effects see section 5.1.5

Licensed use not licensed for use in gastro-intes-tinal stasis

Indication and dose Gastro-intestinal stasis . By mouth

Neonate3 mg/kg 4 times daily

Child 1 month–18 years3 mg/kg 4 times daily

. By intravenous infusion Neonate3 mg/kg 4 times daily

Child 1 month–1 year3 mg/kg 4 times daily

Preparations Section 5.1.5

The management of H. pylori infection and of NSAID-associated ulcers is dis-cussed below.

Helicobacter pylori infection

Eradication of Helicobacter pylori reduces the recurrence of gastric and duodenal ulcers and the risk of rebleeding. The presence of H. pylori should be confirmed before starting eradication treatment. If possible, the antibacterial sensitivity of the organism should be established at the time of endoscopy and biopsy. Acid inhibition combined with antibacterial treatment is highly effective in the eradica-tion of H. pylori; reinfeceradica-tion is rare. Antibiotic-associated colitis is an uncommon risk.

Treatment to eradicate H. pylori infection in children should be initiated under specialist supervision. One-week triple-therapy regimens that comprise ome-prazole, amoxicillin, and either clarithromycin or metronidazole are recom-mended. Resistance to clarithromycin or to metronidazole is much more common than to amoxicillin and can develop during treatment. A regimen containing amoxicillin and clarithromycin is therefore recommended for initial therapy and one containing amoxicillin and metronidazole for eradication failure. There is usually no need to continue antisecretory treatment (with a proton pump inhibitor or H2-receptor antagonist), however, if the ulcer is large, or complicated by haemorrhage or perforation then antisecretory treatment is continued for a further 3 weeks. Lansoprazole may be considered if omeprazole is unsuitable.

Treatment failure usually indicates antibacterial resistance, poor compliance, or familial reinfection.

Two-week triple-therapy regimens offer the possibility of higher eradication rates compared to one-week regimens, but adverse effects are common and poor compliance is likely to offset any possible gain.

Two-week dual-therapy regimens using a proton pump inhibitor and a single antibacterial produce low rates of H. pylori eradication and arenot recommended.

For the role of H. pylori eradication therapy in children starting or taking NSAIDs, see NSAID-associated ulcers, below.

Recommended regimens for Helicobacter pylori eradication

Eradication therapy Age range Oral dose

(to be used in combination with omeprazole, section 1.3.5) Amoxicillin 1–6 years 250 mg twice daily (with clarithromycin)

125 mg 3 times daily (with metronidazole) 6–12 years 500 mg twice daily (with clarithromycin)

250 mg 3 times daily (with metronidazole) 12–18 years 1 g twice daily (with clarithromycin)

500 mg 3 times daily (with metronidazole)

Clarithromycin 1–12 years 7.5 mg/kg (max. 500 mg) twice daily (with metronidazole or amoxicillin)

12–18 years 500 mg twice daily (with metronidazole or amoxicillin) Metronidazole 1–6 years 100 mg twice daily (with clarithromycin)

100 mg 3 times daily (with amoxicillin) 6–12 years 200 mg twice daily (with clarithromycin)

200 mg 3 times daily (with amoxicillin) 12–18 years 400 mg twice daily (with clarithromycin)

400 mg 3 times daily (with amoxicillin)

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Test for Helicobacter pylori

13C-Urea breath test kits are available for confirming the presence of gastro-duodenal infection with Helicobacter pylori. The test involves collection of breath samples before and after ingestion of an oral solution of13C-urea; the samples are sent for analysis by an appropriate laboratory. The test should not be performed within 4 weeks of treatment with an antibacterial or within 2 weeks of treatment with an antisecretory drug. A specific 13C-Urea breath test kit for children is available (Helicobacter Test INFAI for children of the age 3–11c). However the appropriateness of testing for H. pylori infection in children has not been established. Breath, saliva, faecal, and urine tests for H. pylori are frequently unreliable in children; the most accurate method of diagnosis is endoscopy with biopsy.

Helicobacter Test INFAI for children of the age 3-11c(Infai)A

Oral powder,13C-urea 45 mg, net price 1 kit (including 4 breath sample containers, straws) =

£19.20 (spectrometric analysis included)

Helicobacter Test INFAIc(Infai)A Oral powder,13C-urea 75 mg, net price 1 kit (including 4 breath-sample containers, straws) =

£19.20 (spectrometric analysis included); 1 kit (including 2 breath bags) = £14.20 (spectroscopic analysis not included); 50-test set = £855.00 (spectrometric analysis included)

NSAID-associated ulcers

Gastro-intestinal bleeding and ulceration can occur with NSAID use (section 10.1.1). In adults, the risk of serious upper gastro-intestinal side-effects varies between individual NSAIDs (see Gastro-intestinal side-effects, p. 602). Whenever possible, NSAIDs should bewithdrawn if an ulcer occurs.

Children at high risk of developing gastro-intestinal complications include those with a history of peptic ulcer disease or serious upper gastro-intestinal complica-tion, those taking other medicines that increase the risk of upper gastro-intestinal side-effects, or those with serious co-morbidity. In children at risk of ulceration, a proton pump inhibitor (section 1.3.5) or an H2-receptor antagonist, such as ranitidine, may be considered for protection against gastric and duodenal ulcers associated with non-selective NSAIDs.

NSAID use and H. pylori infection are independent risk factors for gastro-intes-tinal bleeding and ulceration. In children already taking a NSAID, eradication of H.

pylori is unlikely to reduce the risk of NSAID-induced bleeding or ulceration.

However, in children about to start long-term NSAID treatment who are H. pylori positive and have dyspepsia or a history of gastric or duodenal ulcer, eradication of H. pylori may reduce the overall risk of ulceration.

If the NSAID can be discontinued in a child who has developed an ulcer, a proton pump inhibitor usually produces the most rapid healing, alternatively the ulcer can be treated with an H2-receptor antagonist.

If NSAID treatment needs to continue, the ulcer is treated with a proton pump inhibitor (section 1.3.5).

1.3.1

H2-receptor antagonists

Histamine H2-receptor antagonists heal gastric and duodenal ulcers by reducing gastric acid output as a result of histamine H2-receptor blockade; they are also used to relieve symptoms of dyspepsia and gastro-oesophageal reflux disease (section 1.1). H2-receptor antagonists should not normally be used for Zollinger–Ellison syndrome because proton pump inhibitors (section 1.3.5) are more effective.

Maintenance treatment with low doses has largely been replaced in Helicobacter pylori positive children by eradication regimens (section 1.3).

H2-receptor antagonist therapy can promote healing of NSAID-associated ulcers (section 1.3).

Treatment with a H2-receptor antagonist has not been shown to be beneficial in haematemesis and melaena, but prophylactic use reduces the frequency of bleeding from gastroduodenal erosions in hepatic coma, and possibly in other

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1.3.1 H2-receptor antagonists BNFC 2009

1Gastro-intestinalsystem

conditions requiring intensive care. Treatment also reduces the risk of acid aspiration in obstetric patients at delivery (Mendelson’s syndrome).

H2-receptor antagonists are also used to reduce the degradation of pancreatic enzyme supplements (section 1.9.4) in children with cystic fibrosis.

Side-effects Side-effects of the H2-receptor antagonists include diarrhoea and other gastro-intestinal disturbances, altered liver function tests (rarely liver damage), headache, dizziness, rash, and tiredness. Rare side-effects include acute pancreatitis, bradycardia, AV block, confusion, depression, and hallucina-tions particularly in the very ill, hypersensitivity reachallucina-tions (including fever, arthr-algia, myarthr-algia, anaphylaxis), blood disorders (including agranulocytosis, leuco-penia, pancytoleuco-penia, thrombocytopenia), and skin reactions (including erythema multiforme and toxic epidermal necrolysis). There have been occasional reports of gynaecomastia and impotence.

RANITIDINE

Cautions acute porphyria; interactions: Appen-dix 1 (histamine H2-antagonists)

Renal impairment use half normal dose if esti-mated glomerular filtration rate less than 50 mL/

minute/1.73 m2

Pregnancy manufacturer advises avoid unless essential, but not known to be harmful Breast-feeding significant amount present in milk, but not known to be harmful

Side-effects see notes above; also rarely tachy-cardia, agitation, visual disturbances, alopecia;

very rarely interstitial nephritis

Licensed use oral preparations not licensed for use in children under 3 years; injection not licensed for use in children under 6 months Indication and dose

Reflux oesophagitis, benign gastric and duo-denal ulceration, prophylaxis of stress ulcer-ation, other conditions where gastric acid reduction is beneficial(see notes above and section 1.9.4)

. By mouth

Neonate2 mg/kg 3 times daily but absorption unreliable; max. 3 mg/kg 3 times daily Child 1–6 months1 mg/kg 3 times daily; max.

3 mg/kg 3 times daily

Child 6 months–3 years2–4 mg/kg twice daily Child 3–12 years2–4 mg/kg (max. 150 mg) twice daily; increased up to 5 mg/kg (max.

300 mg) twice daily in severe gastro-oeso-phageal reflux disease

Child 12–18 years150 mg twice daily or 300 mg at night; increased if necessary, to 300 mg twice daily or 150 mg 4 times daily for up to 12 weeks in moderate to severe gastro-oesophageal reflux disease

NoteIn fat malabsorption syndrome, give 1–2 hours before food to enhance effects of pancreatic enzyme replacement

. By slow intravenous injection Neonate0.5–1 mg/kg every 6–8 hours Child 1 month–18 years1 mg/kg (max. 50 mg) every 6–8 hours (may be given as an intermit-tent infusion at a rate of 25 mg/hour)

Zollinger–Ellison syndrome(but see notes above)

. By mouth

Child 12–18 years150 mg 3 times daily (doses up to 6 g daily in divided doses have been used) Administration For slow intravenous injection dilute

to a concentration of 2.5 mg/mL with Glucose 5%, Sodium Chloride 0.9%, or Compound Sod-ium Lactate. Give over at least 3 minutes

1Ranitidine(Non-proprietary)A

Tablets, ranitidine (as hydrochloride) 150 mg, net price 60-tab pack = £1.27; 300 mg, 30-tab pack =

£1.32

Brands include Raniticc

Effervescent tablets, ranitidine (as hydrochloride) 150 mg, net price 60-tab pack = £10.74; 300 mg, 30-tab pack = £11.25. Label: 13

Excipientsmay include sodium (check with supplier) Oral solution, ranitidine (as hydrochloride) 75 mg/

5 mL, 100 mL = £7.44, 300 mL = £21.43 Excipientsmay include alcohol (check with supplier) 1.Ranitidine can be sold to the public for children over 16

years (provided packs do not contain more than 2 weeks’ supply) for the short-term symptomatic relief of heartburn, dyspepsia, and hyperacidity, and for the prevention of these symptoms when associated with consumption of food or drink (max. single dose 75 mg, max. daily dose 300 mg)

Zantacc(GSK)A

Tablets, f/c, ranitidine (as hydrochloride) 150 mg, net price 60-tab pack = £1.30; 300 mg, 30-tab pack

= £1.30

Effervescent tablets, pale yellow, ranitidine (as hydrochloride) 150 mg (contains 14.3 mmol Na+/ tablet), net price 60-tab pack = £25.94; 300 mg (contains 20.8 mmol Na+/tablet), 30-tab pack =

£25.51. Label: 13

Excipientsinclude aspartame (section 9.4.1) Syrup, sugar-free, ranitidine (as hydrochloride) 75 mg/5 mL. Net price 300 mL = £20.76 Excipientsinclude alcohol 8%

Injection, ranitidine (as hydrochloride) 25 mg/mL.

Net price 2-mL amp = 60p

BNFC 2009 1.3.1 H2-receptor antagonists

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1.3.2

Selective antimuscarinics

Classification not used in BNF for Children.

1.3.3

Chelates and complexes

Sucralfate is a complex of aluminium hydroxide and sulphated sucrose that appears to act by protecting the mucosa from acid-pepsin attack; it has minimal antacid properties. Sucralfate can be used to prevent stress ulceration in children receiving intensive care. It should be used with caution in this situation (impor-tant: reports of bezoar formation, see CSM advice below).

SUCRALFATE

Cautions administration of sucralfate and enteral feeds should be separated by 1 hour; interac-tions: Appendix 1 (sucralfate)

Renal impairment use with caution; aluminium is absorbed and may accumulate

Breast-feeding amount probably too small to be harmful

Bezoar formationFollowing reports of bezoar formation associated with sucralfate, theCSM has advised caution in seriously ill patients, especially those receiving conco-mitant enteral feeds or those with predisposing conditions such as delayed gastric emptying

Side-effects constipation; less frequently diarr-hoea, nausea, indigestion, flatulence, gastric dis-comfort, back pain, dizziness, headache, drowsi-ness, bezoar formation (see above), dry mouth, and rash

Licensed use not licensed for use in children under 15 years; tablets not licensed for prophy-laxis of stress ulceration

Indication and dose

Prophylaxis of stress ulceration in child under intensive care

. By mouth

Child 1 month–2 years250 mg 4–6 times daily Child 2–12 years500 mg 4–6 times daily

Child 12–15 years1 g 4–6 times daily Child 15–18 years1 g 6 times daily; max. 8 g daily

Benign gastric and duodenal ulceration . By mouth

Child 1 month–2 years250 mg 4–6 times daily Child 2–12 years500 mg 4–6 times daily Child 12–15 years1 g 4–6 times daily Child 15–18 years2 g twice daily (on rising and at bedtime) or 1 g 4 times daily (1 hour before meals and at bedtime) taken for 4–6 weeks, or in resistant cases up to 12 weeks; max. 8 g daily Administration for administration by mouth,

sucralfate should be given 1 hour before meals, see also Cautions, above; oral suspension blocks fine-bore feeding tubes; crushed tablets may be dispersed in water.

Antepsinc(Chugai)A

Tablets, scored, sucralfate 1 g, net price 50-tab pack

= £4.81. Label: 5

Suspension, sucralfate, 1 g/5 mL, net price 250 mL (aniseed- and caramel-flavoured) = £4.81. Label: 5

1.3.4

Prostaglandin analogues

Classification not used in BNF for Children.

1.3.5

Proton pump inhibitors

The proton pump inhibitorsomeprazole and lansoprazole inhibit gastric acid secretion by blocking the hydrogen-potassium adenosine triphosphatase enzyme system (the ‘proton pump’) of the gastric parietal cell. Omeprazole is currently only licensed in children for the treatment of gastro-oesophageal reflux disease with severe symptoms. Lansoprazole is not licensed for use in children, but may be considered when the available formulations of omeprazole are unsuitable. Proton pump inhibitors are effective short-term treatments for gastric and duodenal ulcers;

they are also used in combination with antibacterials for the eradication of Helicobacter pylori (see p. 59 for specific regimens). An initial short course of a proton pump inhibitor is the treatment of choice in gastro-oesophageal reflux disease with severe symptoms; children with endoscopically confirmed erosive, ulcerative, or stricturing oesophagitis usually need to be maintained on a proton pump inhibitor.

Proton pump inhibitors are also used for the prevention and treatment of NSAID-associated ulcers (see p. 60). In children who need to continue NSAID treatment after an ulcer has healed, the dose of proton pump inhibitor should not normally be reduced because asymptomatic ulcer deterioration may occur.

Proton pump inhibitors are effective in the treatment of the Zollinger-Ellison syndrome (including cases resistant to other treatment). They are also used to

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1.3.3 Chelates and complexes BNFC 2009

1Gastro-intestinalsystem

reduce the degradation of pancreatic enzyme supplements (section 1.9.4) in children with cystic fibrosis.

Side-effects Side-effects of the proton pump inhibitors include gastro-intestinal disturbances (including nausea, vomiting, abdominal pain, flatulence, diarrhoea, constipation), and headache. Less frequent side-effects include dry mouth, per-ipheral oedema, dizziness, sleep disturbances, fatigue, paraesthesia, arthralgia, myalgia, rash, and pruritus. Other side-effects reported rarely or very rarely include taste disturbance, stomatitis, hepatitis, jaundice, hypersensitivity reactions (including anaphylaxis, bronchospasm), fever, depression, hallucinations, confu-sion, gynaecomastia, interstitial nephritis, hyponatraemia, blood disorders (including leucopenia, leucocytosis, pancytopenia, thrombocytopenia), visual disturbances, sweating, photosensitivity, alopecia, Stevens-Johnson syndrome, and toxic epidermal necrolysis. By decreasing gastric acidity, proton pump inhi-bitors may increase the risk of gastro-intestinal infections (including Clostridium difficile infection).

LANSOPRAZOLE

Cautions interactions: Appendix 1 (proton pump inhibitors)

Hepatic impairment may accumulate in severe impairment

Pregnancy manufacturer advises avoid Breast-feeding present in milk in animal stu-dies—manufacturer advises avoid

Side-effects see notes above; also glossitis, pan-creatitis, anorexia, restlessness, tremor, impo-tence, petechiae, and purpura; very rarely colitis, raised serum cholesterol or triglycerides Licensed use not licensed for use in children Indication and dose

Gastro-oesophageal reflux disease, acid-related dyspepsia, treatment of duodenal and benign gastric ulcer including those compli-cating NSAID therapy, fat malabsorption despite pancreatic enzyme replacement ther-apy in cystic fibrosis

. By mouth

Child body-weight under 30 kg0.5–1 mg/kg (max. 15 mg) once daily in the morning

Child body-weight over 30 kg15–30 mg once daily in the morning

Administration for administration by a nasogastric tube or an oral syringe, Zoton FasTabccan be dispersed in a small amount of water Zotonc(Wyeth)A

FasTabc(= orodispersible tablet), lansoprazole 15 mg, net price 28-tab pack = £5.97; 30 mg, 14-tab pack = £5.47, 28-tab pack = £11.00. Label: 5, 22, counselling, administration

Excipientsinclude aspartame (section 9.4.1) CounsellingTablets should be placed on the tongue, allowed to disperse and swallowed, or may be swallowed whole with a glass of water.

OMEPRAZOLE

Cautions interactions: Appendix 1 (proton pump inhibitors)

Hepatic impairment no more than 700 micr-ograms/kg (max. 20 mg) once daily Pregnancy not known to be harmful

Breast-feeding present in milk but not known to be harmful

Side-effects see notes above; also agitation and impotence

Licensed use capsules and tablets not licensed for use in children except for severe ulcerating reflux oesophagitis in children over 1 year; injection not licensed for use in children under 12 years

Indication and dose

Gastro-oesophageal reflux disease, acid-related dyspepsia, treatment of duodenal and benign gastric ulcers including those compli-cating NSAID therapy, prophylaxis of acid aspiration, Zollinger-Ellison syndrome, fat malabsorption despite pancreatic enzyme replacement therapy in cystic fibrosis . By mouth

Neonate700 micrograms/kg once daily, increased if necessary after 7–14 days to 1.4 mg/kg; some neonates may require up to 2.8 mg/kg once daily

Child 1 month–2 years700 micrograms/kg once daily, increased if necessary to 3 mg/kg (max. 20 mg) once daily

Child body-weight 10–20 kg10 mg once daily increased if necessary to 20 mg once daily (in severe ulcerating reflux oesophagitis, max. 12 weeks at higher dose)

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Child body-weight over 20 kg20 mg once daily increased if necessary to 40 mg once daily (in severe ulcerating reflux oesophagitis, max. 12 weeks at higher dose)

. By intravenous injection over 5 minutes or by intravenous infusion

Child 1 month–12 yearsinitially 500 micr-ograms/kg (max. 20 mg) once daily, increased to 2 mg/kg (max. 40 mg) once daily if necessary Child 12–18 years40 mg once daily

Helicobacter pylori eradication (in combination with antibacterials see p. 59)

. By mouth

Child 1–12 years1–2 mg/kg (max. 40 mg) once daily

Child 12–18 years40 mg once daily

Administration for administration by mouth, swal-low whole, or disperse Losec MUPSctablets in water, or mix capsule contents or Losec MUPSc tablets with fruit juice or yoghurt. Preparations consisting of an e/c tablet within a capsule shouldnot be opened.

For administration through an enteral feeding tube, use Losec MUPScor the contents of a capsule containing omeprazole dispersed in a large volume of water, or in 10 mL Sodium Bicarbonate 8.4% (1 mmol Na+/mL) (allow to stand for 10 minutes before administration).

For intermittent intravenous infusion, dilute recon-stituted solution to a concentration of 400 micr-ograms/mL with Glucose 5% or Sodium Chloride 0.9%; give over 20–30 minutes

Omeprazole(Non-proprietary)A

Capsules, enclosing e/c granules, omeprazole 10 mg, net price cap pack = £1.87; 20 mg, cap pack = £1.75; 40 mg, 7-cap pack = £2.04, 28-cap pack = £58.00. Counselling, administration NoteSome preparations consist of an e/c tablet within a capsule; brands include Mepradecc

Dental prescribing on NHSGastro-resistant omeprazole capsules may be prescribed

Tablets, e/c, omeprazole 10 mg, net price 28-tab pack = £6.13; 20 mg, 28-tab pack = £5.37; 40 mg, 7-tab pack = £5.08. Label: 25

Intravenous infusion, powder for reconstitution, omeprazole (as sodium salt), net price 40-mg vial =

£5.21

Losecc(AstraZeneca)A

MUPSc(multiple-unit pellet system = dispersible tablets), f/c, omeprazole 10 mg (light pink), net price 28-tab pack = £19.34; 20 mg (pink), 28-tab pack = £29.22; 40 mg (red-brown), 7-tab pack =

£14.61. Counselling, administration Capsules, enclosing e/c granules, omeprazole 10 mg (pink), net price 28-cap pack = £19.34; 20 mg (pink/brown), 28-cap pack = £29.22; 40 mg (brown), 7-cap pack = £14.61. Counselling, administration

Intravenous infusion, powder for reconstitution, omeprazole (as sodium salt), net price 40-mg vial =

£5.41

Injection, powder for reconstitution, omeprazole (as sodium salt), net price 40-mg vial (with solvent)

= £5.41

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