Sucralfate + Sodium Alginate Tablets

(500 mg + 20 mg)

1. Formulation
I. Sucralfate ...............................................500 g
Sodium alginate ........................................20 g
Corn starch [3] ..........................................70 g
II. Kollidon 30 [1] ...........................................20 g
Ethanol 95% ...........................................80 ml
III. Kollidon CL [1] ..........................................30 g
Magnesium stearate [2] ...............................3 g

2. Manufacturing (Wet granulation)

Granulate mixture I with solution II, pass through a sieve, mix the dry
granules with III and press with low compression force.

3. Tablet properties
Weight .................................................660 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness..................................................90 N
Disintegration .....................................3 4 min
Friability...................................................0.3%

Use
Cimetidine inhibits gastric acid secretion. Rather fewer side effects have been
reported for the closely related drug
ranitidine (q.v.).
Pharmacology
Cimetidine is a safe and widely used drug, a low dose formulation of which is
now available over the counter
without prescription for the short term management of indigestion and heartburn
in adults. The drug, first synthesised
in 1972, was designed to work by blocking the H2 histamine receptors in the
stomach that control the release of gastric
acid, thereby also reducing pepsin output. High dose treatment has been shown
to speed the healing of peptic ulcers
in the oesophagus, stomach, and duodenum, and low dose maintenance
treatment can be used to prevent a recurrence
in vulnerable patients. Omeprazole (q.v.) may be effective when cimetidine is not.
Cimetidine and ranitidine have also
been widely used to treat acute non-specific gastrointestinal bleeding, especially
in patients undergoing intensive care
(where acute haematemesis is often seen to be a sign of stress ulceration), but
such haemorrhage frequently stops
rapidly without specific treatment, and the 27 trials that have been carried out in
adult patients fail to show clear
evidence of benefit. Only one small trial has yet been attempted in the neonatal
period.
Cimetidine is rapidly absorbed when taken by mouth and mostly excreted
unchanged in the urine, the plasma
elimination half life being about 2 hours in adults, but rather more than this in the
neonatal period. Side effects are
rare, although dizziness, somnolence, and fatigue have been reported.
Arrhythmia has been seen both in adults and in
neonates, especially with rapid IV administration. Cimetidine has mild, dose
related, antiandrogenic properties and
reversible gynaecomastia has been reported.
Cimetidine crosses the placenta and should be used with caution in early
pregnancy, although teratogenicity has
not been reported. It has been widely used in mothers during delivery (as
discussed in the monograph on ranitidine)
without adverse effects being noted in the neonate. Use during lactation will
result in the baby receiving (on a weight
for weight basis) a dose equivalent to 57% of the maternal dose. This does not
seem to have caused problems. There
is not enough experience with its use for the manufacturers to recommend the
use of this drug in children under
1 year old.
Drug interactions
Cimetidine (unlike ranitidine) binds very strongly to cytochrome P450, inhibiting
the breakdown of those drugs that
are metabolised by this enzyme in the liver. Erythromycin, lidocaine, midazolam,
nifedipine, phenytoin, suxamethonium,
theophylline (or aminophylline), and warfarin are amongst the drugs most notably
affected.
Treatment
Give 5 mg/kg by mouth every 6 hours if there is evidence of active ulceration.
Half this dose may be adequate when
the drug is given prophylactically. Treatment can be given IV when necessary, but
must be given slowly over at least
10 minutes. A continuous infusion of ranitidine may be preferred. Dosage must
be halved or treatment stopped when
there is renal failure.
Supply
2 ml ampoules for IV or IM use containing 200 mg of cimetidine cost 36p. The IV
preparation must be diluted at least
fivefold, and is most conveniently diluted 10-fold, before use. Take 1 ml of
cimetidine from the ampoule and dilute to
10 ml with 09% sodium chloride to provide a preparation containing 10 mg/ml
suitable for IV (or oral) use. Rapid IV
administration can cause arrhythmia. An oral syrup containing 40 mg/ml of
cimetidine is also available from the
pharmacy (100 ml costs 470) and this can be diluted with syrup BP to give a
preparation containing 10 mg/ml on
request.
CIMETIDINE
Neonatal folmulary codex