Antepsin 1g/5ml Oral Suspension
SUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Antepsin 1g/5ml Oral Suspension
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each 5 mL dose contains 1 gram sucralfate.
For the full list of excipients, see section 6.1
3 PHARMACEUTICAL FORM
Oral Suspension
White to off-white viscous suspension with an odour of aniseed/caramel.
4.1 Therapeutic indications
Antepsin is indicated in adults and adolescents over 14 years old for treatment of duodenal ulcer, gastric ulcer, chronic gastritis, and the prophylaxis of gastrointestinal haemorrhage from stress ulceration in seriously ill patients.
4.2 Posology and method of administration
For oral administration.
Antepsin must not be administered intravenously.
Duodenal ulcer, gastric ulcer, chronic gastritis:
Adults: The usual dose is 2 grams twice daily to be taken on rising and at bedtime, or 1 gram 4 times a day to be taken 1 hour before meals and at bedtime. Maximum daily dose: 8 grams.
Four to six weeks’ treatment is usually needed for ulcer healing, but up to twelve weeks may be necessary in resistant cases.
Antacids may be used as required for relief of pain, but should not be taken half an hour before or after Antepsin.
Paediatric population: The safety and efficacy of Antepsin in children under 14 years of age has not been established. Currently available data are described in section 5.1 but no recommendation on posology can be made.
Elderly: see below
Prophylaxis of gastrointestinal haemorrhage from stress ulceration:
Adults: The usual dose is 1 gram six times a day. A maximum dose of 8 grams daily should not be exceeded. Antacids may be used as required for relief of pain, but should not be taken half an hour before or after Antepsin.
Elderly: There are no special dosage requirements for elderly patients but as with all medicines, the lowest effective dose should be used.
Paediatric population: The safety and efficacy of Antepsin in children under 14 years of age has not been established. Currently available data are described in section 5.1.
4.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.
4.4 Special warnings and precautions for use
Antepsin must not be administered intravenously. Inadvertent intravenous administration of insoluble sucralfate and its insoluble excipients may induce fatal complications, including pulmonary and cerebral emboli. Other severe complications including aluminium intoxication are reported after intravenous administration.
The product should only be used with caution in patients with renal dysfunction, due to the possibility of increased aluminium absorption.
Sucralfate is not recommended for use in individuals on dialysis.
In patients with severe or chronic renal impairment, Antepsin should be used with extreme caution and only for short-term treatment. Small amounts of aluminium are absorbed through the gastrointestinal tract and aluminium may accumulate. Aluminium osteodystrophy, osteomalacia, encephalopathy, and anaemia have been reported in patients with chronic renal impairment. For patients with impairment of renal function, laboratory testing such as aluminium, phosphate, calcium, and alkaline phosphatase is recommended to be periodically performed due to excretion impairment.
The concomitant use of other aluminium containing medications is not recommended in view of the enhanced potential for aluminium absorption and toxicity.
Contains sodium methyl parahydroxybenzoate (E219) and sodium propyl parahydroxybenzoate (E217) which may cause allergic reactions (possibly delayed). Bezoars have been reported after administration of sucralfate mainly to severely ill patients in intensive care units. The majority of these patients (including neonates in whom sucralfate is not recommended) had underlying medical conditions that may predispose to bezoar formation (such as delayed gastric emptying due to surgery, drug therapy or diseases that reduce motility), or were receiving concomitant enteral tube feeding.
Paediatric Population:
Antepsin is not recommended for use in children under 14 years of age due to insufficient data on safety and efficacy.
4.5 Interactions with other medicinal products and other forms of interaction
Concomitant administration of Antepsin may reduce the bioavailability of certain drugs including fluoroquinolones such as ciprofloxacin and norfloxacin, tetracycline, ketoconazole, sulpiride, digoxin, warfarin, phenytoin, theophylline, levothyroxine, quinidine and H2 antagonists. The bioavailability of these agents may be restored by separating the administration of these agents from Antepsin by two hours. This interaction appears to be non systemic in origin presumably resulting from these agents being bound by Antepsin in the gastrointestinal tract. Because of the potential of Antepsin to alter the absorption of some drugs from the gastrointestinal tract, the separate administration of Antepsin from that of other agents should be considered when alterations in bioavailability are felt to be critical for concomitantly administered drugs.
Sucralfate should not be co-administered with citrate preparations. Co-administration of citrate preparations with sucralfate may increase the blood concentrations of aluminium. The mechanism may be due to chelation of aluminium, which is assumed to increase its absorption.
The administration of Antepsin Suspension and enteral feeds by nasogastric tube should be separated by one hour in patients receiving Antepsin Suspension for the prophylaxis of stress ulceration. In rare cases bezoar formation has been reported when Antepsin and enteral feeds have been given too closely together.
4.6 Fertility, pregnancy and lactation
Pregnancy
Teratogenicity studies in mice, rats and rabbits at doses up to 50 times the human dose have revealed no evidence of harm to the foetus. Safety in pregnant women has not been established and Antepsin should be used during pregnancy only if clearly needed.
Lactation
It is not known whether this drug is excreted in human milk. Caution should be exercised when Antepsin is administered to breast-feeding women.
4.7 Effects on ability to drive and use machines
Do not drive if you feel dizzy or drowsy.
4.8 Undesirable effects
Tabulated list of adverse reactions
|
Immune system disorders |
Not known (cannot be estimated from the available data) |
Anaphylactic reaction including pruritus, urticaria, oedema, dyspnoea |
|
Nervous system disorders |
Not known (cannot be estimated from the available data) |
Dizziness, headache, drowsiness |
|
Ear and labyrinth disorders |
Not known (cannot be estimated from the available data) |
Vertigo |
|
Gastrointestinal disorders |
Common (> 1% and < 10%); |
Constipation |
|
Uncommon (> 0.1% and <1%) |
Dry mouth, nausea, | |
|
Rare (> 0.01% and <0.1%) |
Bezoar formation1 | |
|
Not known (cannot be estimated from the available data) |
Diarrhoea, vomiting, gastric discomfort, indigestion, flatulence | |
|
Skin and subcutaneous tissue disorders |
Rare (> 0.01% and <0.1%) |
Rash |
|
Musculoskeletal and connective tissue disorders |
Not known (cannot be estimated from the available data) |
Back pain |
|
Injury, poisoning and procedural |
Not known (cannot be estimated from the available |
Osteodystrophy2, osteomalacia2, |
complications
data)
encephalopathy2
2
anaemia
'Reported in patients with impaired gastric emptying, patients with enteral tube feeding or low birth weight infants
2Reported in patients with chronic renal impairment
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.
4.9 Overdose
In a clinical trial on healthy men of overdose with sucralfate, most cases remained asymptomatic, but symptoms of abdominal pain, nausea, and vomiting were reported in a few cases. Acute oral toxicity studies in animals, using doses up to 12 g/kg body weight, could not find a lethal dose. Risks associated with overdose, should, therefore, be minimal.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Alimentary tract and metabolism, ATC code: A02B X02
The action of Antepsin is non-systemic as the drug is only minimally absorbed from the gastro-intestinal tract. The small amounts that are absorbed are excreted primarily in the urine. Antepsin exerts a generalised cytoprotective effect by preventing gastrointestinal mucosal injury.
Studies in humans and animal models show that Antepsin forms an ulcer adherent complex with the proteinaceous exudate of the ulcer site. This property enables Antepsin to form a protective barrier over the ulcer lesion giving sustained protection against the penetration and action of gastric acid, pepsin and bile.
Studies both in humans and animals demonstrate that Antepsin protects the gastric mucosa against various irritants such as alcohol, acetylsalicyclic acid and sodium taurocholate.
Antepsin also directly inhibits pepsin activity and absorbs bile salts. It has only weak antacid activity. It does not alter gastric emptying time, nor normal digestive function. Antepsin has no demonstrated pharmacological effect on the cardiovascular or central nervous systems.
Paediatric population
In the literature, there are limited clinical data on the use of sucralfate in children, mainly for stress ulcer prophylaxis, reflux oesophagitis, and mucositis. The dose used in these studies was 0.5 - 1 g four times a day, depending on the children’s age and the severity of the underlying disease, and was applied without major safety concerns.
In view of the limited data, use of sucralfate in children under 14 years of age is currently not recommended.
5.2 Pharmacokinetic properties
Sucralfate is only minimally absorbed from the gastro-intestinal tract. The small amounts that are absorbed are excreted primarily in the urine. Absorption of aluminium from sucralfate may be increased in patients on dialysis or with renal dysfunction (see also "other special warnings and precautions").
5.3 Preclinical safety data
There was no evidence of carcinogenesis in mice and rats receiving oral sucralfate in dosages of up to 1 gm/kg daily (12 times the usual human dosage) for 2 years. In animal studies there was no effect evidence of impaired fertility. The effect of sucralfate on human fertility is not known.
6 PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Saccharin sodium
Sodium dihydrogen phosphate dihydrate
Purified water
Glycerol
Sodium propyl hydroxybenzoate (E217)
Sodium methyl hydroxybenzoate (E219)
Xanthan gum Aniseed flavour Caramel flavour
6.2 Incompatibilities
Not applicable
6.3 Shelf life
3 years
After first opening: 28 days.
6.4 Special precautions for storage
Store below 25°C.
6.5 Nature and contents of container
Glass bottle (pack size 250 ml)
6.6 Special precautions for disposal
No special requirements
7 MARKETING AUTHORISATION HOLDER
Chugai Pharma UK Limited
Mulliner House
Flanders Road
Turnham Green
London
W4 1NN
UK
8 MARKETING AUTHORISATION NUMBER
PL 12185/0010
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
12/10/1998 / 29/09/2005
10 DATE OF REVISION OF THE TEXT
08/11/2013