Antispasmodics and other drugs altering gut motility

1 Gastro-intestinal system

1.2 Antispasmodics and other drugs altering gut motility

Other compound alginate preparations Gastrocote^c(Actavis)

Tablets, alginic acid 200 mg, dried aluminium hydroxide 80 mg, magnesium trisilicate 40 mg, sodium bicarbonate 70 mg. Contains about 1 mmol Na⁺/tablet. Net price 100-tab pack = £3.51 Cautions diabetes mellitus (high sugar content) Dose

. By mouth

Child 6–18 years1–2 tablets chewed 4 times daily (after meals and at bedtime)

Liquid, sugar-free, peach-coloured, dried alumin-ium hydroxide 80 mg, magnesalumin-ium trisilicate 40 mg, sodium alginate 220 mg, sodium bicarbonate 70 mg/5 mL. Contains 2.13 mmol Na⁺/5 mL. Net price 500 mL = £2.67

Dose . By mouth

Child 6–18 years5–15 mL 4 times daily (after meals and at bedtime)

Gaviscon^cAdvance(R&C)

Tablets, sugar-free, sodium alginate 500 mg, potassium bicarbonate 100 mg. Contains 2.25mmol Na⁺, 1 mmol K⁺/tablet. Net price 60–tab pack (peppermint-flavour) = £3.24

Excipientsinclude aspartame (section 9.4.1) Dose

. By mouth

Child 6–12 years1 tablet to be chewed after meals and at bedtime (under medical advice only) Child 12–18 years1–2 tablets to be chewed after meals and at bedtime

Suspension, sugar-free, aniseed- or peppermint-flavour, sodium alginate 500 mg, potassium bicarbonate 100 mg/5 mL. Contains 2.3 mmol Na⁺, 1 mmol K⁺/5 mL, net price 250 mL = £2.70, 500 mL

= £5.40 Dose

. By mouth

Child 2–12 years2.5–5 mL after meals and at bedtime (under medical advice only)

Child 12–18 years5–10 mL after meals and at bed-time

Gaviscon^cInfant(R&C)

Oral powder, sugar-free, sodium alginate 225 mg, magnesium alginate 87.5 mg, with colloidal silica and mannitol/dose (half dual-sachet). Contains 0.92 mmol Na⁺/dose. Net price 15 dual-sachets (30 doses) = £2.46

Dose . By mouth

Neonate body-weight under 4.5 kg1 ‘dose’ (half dual-sachet) mixed with feeds (or water, for breast-fed infants) when required (max. 6 times in 24 hours) Neonate body-weight over 4.5 kg2 ‘doses’ (1 dual-sachet) mixed with feeds (or water, for breast-fed infants) when required (max. 6 times in 24 hours) Child 1 month–2 years

Body-weight under 4.5 kgdose as for neonate Body–weight over 4.5 kg2 ‘doses’ (1 dual-sachet) mixed with feeds (or water, for breast-fed infants) when required (max. 6 times in 24 hours) NoteNot to be used in preterm neonates, or where excessive water loss likely (e.g. fever, diarrhoea, vomiting, high room temperature), or if intestinal obstruction. Not to be used with other preparations containing thickening agents

Safe PracticeEach half of the dual-sachet is identified as

‘one dose’. To avoid errors prescribe as ‘dual-sachet’

with directions in terms of ‘dose’

Rennie^cDuo(Roche Consumer Health)

Suspension, sugar-free, calcium carbonate 600 mg, magnesium carbonate 70 mg, sodium alginate 150 mg/5 mL. Contains 2.6 mmol Na⁺/5 mL. Net price 500 mL (mint flavour) = £2.67

Dose . By mouth

Child 12–18 years10 mL after meals and at bedtime;

an additional 10 mL may be taken between doses for heartburn if necessary, max. 80 mL daily Excipientsinclude propylene glycol

Topal^c(Fabre)

Tablets, alginic acid 200 mg, dried aluminium hydroxide 30 mg, light magnesium carbonate 40 mg with lactose 220 mg, sucrose 880 mg, sod-ium bicarbonate 40 mg (low Na⁺). Net price 42-tab pack = £1.67

Cautions diabetes mellitus (high sugar content) Dose

. By mouth

Child 12–18 years1–3 tablets chewed 4 times daily (after meals and at bedtime)

indications for antimuscarinic drugs include asthma and airways disease (section 3.1.2), motion sickness (section 4.6), urinary frequency and enuresis (section 7.4.2), mydriasis and cycloplegia (section 11.5), premedication (section 15.1.3), palliative care (p. 26), and as an antidote to organophosphorus poisoning (p. 47).

Antimuscarinics that are used for gastro-intestinal smooth muscle spasm include the tertiary aminedicycloverine hydrochloride (dicyclomine hydrochloride) and the quaternary ammonium compoundspropantheline bromide and hyoscine butylbromide. The quaternary ammonium compounds are less lipid soluble than atropine and so are less likely to cross the blood-brain barrier; they are also less well absorbed from the gastro-intestinal tract.

Dicycloverine hydrochloride may also have some direct action on smooth muscle.

Hyoscine butylbromide is advocated as a gastro-intestinal antispasmodic, but it is poorly absorbed; the injection may be useful in endoscopy and radiology.

Cautions Antimuscarinics should be used with caution in children (especially children with Down’s syndrome) due to increased risk of side-effects; they should also be used with caution in hypertension, conditions characterised by tachy-cardia (including hyperthyroidism, tachy-cardiac insufficiency, tachy-cardiac surgery), pyrexia, pregnancy, and in children susceptible to angle-closure glaucoma. Antimusca-rinics are not used in children with gastro-oesophageal reflux disease, diarrhoea or ulcerative colitis.Interactions: Appendix 1 (antimuscarinics).

Contra-indications Antimuscarinics are contra-indicated in myasthenia gravis (but may be used to decrease muscarinic side-effects of anticholinesterases—

section 10.2.1), paralytic ileus, and pyloric stenosis.

Side-effects Side-effects of antimuscarinics include constipation, transient bradycardia (followed by tachycardia, palpitation and arrhythmias), reduced bronchial secretions, urinary urgency and retention, dilatation of the pupils with loss of accommodation, photophobia, dry mouth, flushing and dryness of the skin. Side-effects that occur occasionally include nausea, vomiting, and giddiness.

DICYCLOVERINE HYDROCHLORIDE

(Dicyclomine hydrochloride) Cautions see notes above

Contra-indications see notes above; child under 6 months

Breast-feeding avoid—present in milk; apnoea reported in infant

Side-effects see notes above Indication and dose

Symptomatic relief of gastro-intestinal disor-ders characterised by smooth muscle spasm . By mouth

Child 6 months–2 years5–10 mg 3–4 times daily 15 minutes before feeds

Child 2–12 years10 mg 3 times daily Child 12–18 years10–20 mg 3 times daily

Merbentyl^c(Sanofi-Aventis)A

Tablets, dicycloverine hydrochloride 10 mg, net price 20 = £1.01; 20 mg (Merbentyl 20^c), 84-tab pack

= £8.47

Syrup, dicycloverine hydrochloride 10 mg/5 mL, net price 120 mL = £1.84

NoteDicycloverine hydrochloride can be sold to the public provided that max. single dose is 10 mg and max. daily dose is 60 mg

Compound preparations Kolanticon^c(Peckforton)

Gel, sugar-free, dicycloverine hydrochloride 2.5 mg, dried aluminium hydroxide 200 mg, light magnes-ium oxide 100 mg, simeticone 20 mg/5 mL, net price 200 mL = £2.21, 500 mL = £2.79 Dose

Child 12–18 years10–20 mL every 4 hours when required

HYOSCINE BUTYLBROMIDE

Cautions see notes above; also intestinal and urinary outlet obstruction

Pregnancy manufacturer advises use only if potential benefit outweighs risk

Breast-feeding amount too small to be harmful Contra-indications see notes above

Side-effects see notes above

Licensed use tablets not licensed for use in chil-dren under 6 years; injection not licensed for use in children (age range not specified by manufac-turer)

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Indication and dose

Symptomatic relief of gastro-intestinal or gen-ito-urinary disorders characterised by smooth muscle spasm

. By mouth

Child 6–12 years10 mg 3 times daily Child 12–18 years20 mg 4 times daily Excessive respiratory secretions and bowel colic in palliative care(see also p. 28) . By mouth

Child 1 month–2 years300–500 micrograms/

kg (max. 5 mg) 3–4 times daily Child 2–5 years5 mg 3–4 times daily Child 5–12 years10 mg 3–4 times daily Child 12–18 years10–20 mg 3–4 times daily . By intramuscular or intravenous injection

Child 1 month–4 years300–500 micrograms/

kg (max. 5 mg) 3–4 times daily

Child 5–12 years5–10 mg 3–4 times daily Child 12–18 years10–20 mg 3–4 times daily

Acute spasm, spasm in diagnostic procedures . By intramuscular or intravenous injection

Child 2–6 years5 mg repeated after 30 minutes if necessary (may be repeated more frequently in endoscopy), max. 15 mg daily

Child 6–12 years5–10 mg repeated after 30 minutes if necessary (may be repeated more frequently in endoscopy), max. 30 mg daily Child 12–18 years20 mg repeated after 30 minutes if necessary (may be repeated more frequently in endoscopy), max. 80 mg daily Administration for intravenous injection, may be

diluted with Glucose 5% or Sodium Chloride 0.9%; give over at least 1 minute.

For administration by mouth, injection solution may be used; content of ampoule may be stored in a refrigerator for up to 24 hours after opening Buscopan^c(Boehringer Ingelheim)A

Tablets,coated, hyoscine butylbromide 10 mg, net price 56-tab pack = £2.59

NoteHyoscine butylbromide tablets can be sold to the public provided single dose does not exceed 20 mg, daily dose does not exceed 80 mg, and pack does not contain a total of more than 240 mg

Injection, hyoscine butylbromide 20 mg/mL. Net price 1-mL amp = 20p

PROPANTHELINE BROMIDE

Cautions see notes above

Hepatic impairment manufacturer advises cau-tion

Renal impairment manufacturer advises caution Pregnancy manufacturer advises avoid Breast-feeding may suppress lactation Contra-indications see notes above Side-effects see notes above

Licensed use tablets not licensed for use in chil-dren under 12 years

Indication and dose

Symptomatic relief of gastro-intestinal disor-ders characterised by smooth muscle spasm . By mouth

Child 1 month–12 years300 micrograms/kg (max. 15 mg) 3–4 times daily at least one hour before food

Child 12–18 years15 mg 3 times daily at least one hour before meals and 30 mg at night (max.

120 mg daily)

Pro-Banthine^c(Concord)A

Tablets, pink, s/c, propantheline bromide 15 mg, net price 112-tab pack = £15.32. Label: 23 Extemporaneous formulations available see Extemporaneous Preparations, p. 8

Other antispasmodics

Alverine, mebeverine, and peppermint oil are believed to be direct relaxants of intestinal smooth muscle and may relieve pain in irritable bowel syndrome and primary dysmenorrhoea. They have no serious adverse effects; peppermint oil occasionally causes heartburn.

ALVERINE CITRATE

Cautions

Pregnancy caution

Breast-feeding little information available—

manufacturer advises avoid Contra-indications paralytic ileus

Side-effects nausea; headache, dizziness; pru-ritus, rash; hepatitis also reported

HYOSCINE BUTYLBROMIDE (continued)

56

1.2 Antispasmodics and other drugs altering gut motility BNFC 2009

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Indication and dose

Adjunct in gastro-intestinal disorders charac-terised by smooth muscle spasm, dysmenorr-hoea

. By mouth

Child 12–18 years60–120 mg 1–3 times daily

Spasmonal^c(Norgine)

Capsules, alverine citrate 60 mg (blue/grey), net price 100-cap pack = £11.95; 120 mg (Spasmonal^c Forte, blue/grey), 60-cap pack = £13.80

MEBEVERINE HYDROCHLORIDE

Cautions avoid in acute porphyria (section 9.8.2) Pregnancy not known to be harmful—manufac-turers advise caution

Contra-indications paralytic ileus

Side-effects rarely allergic reactions (including rash, urticaria, angioedema)

Licensed use tablets and liquid not licensed for use in children under 10 years; granules not licensed for use in children under 12 years; mod-ified-release capsules not licensed for use in chil-dren under 18 years

Indication and dose

Adjunct in gastro-intestinal disorders charac-terised by smooth muscle spasm

. By mouth

Child 3–4 years25 mg 3 times daily, preferably 20 minutes before meals

Child 4–8 years50 mg 3 times daily, preferably 20 minutes before meals

Child 8–10 years100 mg 3 times daily, prefer-ably 20 minutes before meals

Child 10–18 years135–150 mg 3 times daily, preferably 20 minutes before meals

1Mebeverine Hydrochloride(Non-proprietary)A Tablets, mebeverine hydrochloride 135 mg, net price 20 = £2.21

Oral suspension, mebeverine hydrochloride (as mebeverine embonate) 50 mg/5 mL. Contains Na⁺ 0.87 mmol/5 mL. Net price 300 mL = £107.00 1.Mebeverine hydrochloride can be sold to the public for

children over 10 years, for symptomatic relief of irritable bowel syndrome, provided that max. single dose is 135 mg and max. daily dose is 405 mg

Colofac^c(Solvay)A

Tablets, s/c, mebeverine hydrochloride 135 mg.

Net price 20 = £1.50

Modified release Colofac^cMR(Solvay)A

Capsules, m/r, mebeverine hydrochloride 200 mg, net price 60-cap pack = £6.67. Label: 25 Dose

Irritable bowel syndrome . By mouth

Child 12–18 years1 capsule twice daily preferably 20 minutes before food

Compound preparations

1Fybogel^cMebeverine(R&C)A

Granules, buff, effervescent, ispaghula husk 3.5 g, mebeverine hydrochloride 135 mg/sachet. Con-tains 2.5 mmol K⁺/sachet, net price 10 sachets =

£2.50. Label: 13, 22, counselling, see below Excipientsinclude aspartame (section 9.4.1) Dose

Irritable bowel syndrome . By mouth

Child 12–18 years1 sachet in water, morning and evening 30 minutes before food; an additional sachet may also be taken before the midday meal if necessary CounsellingPreparations that swell in contact with liquid should always be carefully swallowed with water and should not be taken immediately before going to bed 1.10-sachet pack can be sold to the public for use in

children over 12 years

PEPPERMINT OIL

Cautions sensitivity to menthol

Breast-feeding significant levels of menthol in breast milk unlikely

Side-effects heartburn, perianal irritation; rarely, allergic reactions (including rash, headache, bradycardia, muscle tremor, ataxia)

Local irritationCapsules should not be broken or chewed because peppermint oil may irritate mouth or oesophagus

Indication and dose

Relief of abdominal colic and distension, par-ticularly in irritable bowel syndrome . By mouth

Child 15–18 years1–2 capsules, swallowed whole with water, 3 times daily for up to 3 months if necessary

Colpermin^c(McNeil)

Capsules, e/c, light blue/dark blue, blue band, peppermint oil 0.2 mL. Net price 100-cap pack =

£12.05. Label: 5, 25

Excipientsinclude arachis (peanut) oil

ALVERINE CITRATE (continued)

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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