page95
quate;
it
should be used as
an adjunct
to existing
laxative therapy.
Methylnaltrexone does not
alter
the
central analgesic effect of opioids. For the prevention of
opioid-induced constipation in palliative care, see p.
22.
METHYLNALTREXONE BROMIDE
Indications
opioid-induced constipation in terminally
ill patients,
when response to other laxatives is
inadequate
Cautions
diverticular disease; faecal impaction;
patients with colostomy or peritoneal catheter
Contra-indications
gastro-intestinal obstruction;
acute surgical abdominal conditions
Hepatic impairment
manufacturer advises avoid in
severe hepatic impairment—no information available
Renal impairment
if eGFR less than 30 mL/minute/
1.73 m
2
,
reduce dose as follows: body-weight under
62 kg,
75 micrograms/kg on alternate days; body-
weight 62–114 kg, 8 mg on alternate days; body-
weight over 114 kg,
75 micrograms/kg on alternate
days
Pregnancy
toxicity at high doses in
animal
studies—
manufacturer advises avoid unless essential
Breast-feeding
manufacturer advises use only if
potential benefit outweighs risk—present in milk in
animal
studies
Side-effects
abdominal pain,
nausea,
diarrhoea,
flatulence;
dizziness;
injection site reactions,
hyper-
hidrosis;
also reported gastro-intestinal perforation
Dose
. By subcutaneous injection,
ADULT
over 18 years, body-
weight under 38 kg,
150 micrograms/kg on alternate
days; body-weight 38–62 kg,
8 mg on alternate days;
body-weight 62–114 kg,
12 mg on alternate days;
body-weight over 114 kg,
150 micrograms/kg on
alternate days; may be given less frequently depend-
ing on response; 2 consecutive doses may be given 24
hours apart if no response to treatment on the pre-
ceding day; rotate sites of injection;
max.
duration of
treatment 4 months
Note
May act within 30–60 minutes
Relistor
c
(Wyeth) T A
Injection
,
methylnaltrexone bromide 20 mg/mL,
net
price 0.6-mL vial = £21.05, 7-vial pack (with syringes
and needles) = £147.35
1.6.7
5HT
4
-receptor agonists
Prucalopride is
a selective serotonin 5HT
4
-receptor
agonist with prokinetic properties.
It is licensed for the
treatment of chronic constipation in women, when other
laxatives have failed to provide an adequate response.
Headache and gastro-intestinal
symptoms
(including
abdominal
pain,
nausea,
and diarrhoea)
are the most
frequent side-effects. The side-effects generally occur at
the start of treatment and are usually transient.
PRUCALOPRIDE
Indications
chronic constipation in women when
other laxatives fail to provide an adequate response
Cautions
history of arrhythmias or ischaemic heart
disease; concomitant use with drugs that prolong QT
interval; severe,
unstable chronic illness
Contra-indications
intestinal perforation or obstruc-
tion; severe inflammatory conditions of the intestinal
tract (such as Crohn’s disease,
ulcerative colitis,
and
toxic megacolon)
Hepatic impairment
max.
1 mg daily in severe
impairment
Renal impairment
max.
1 mg daily if eGFR less than
30 mL/minute/1.73 m
2
Pregnancy
manufacturer advises avoid and recom-
mends effective contraception during treatment
Breast-feeding
manufacturer advises avoid—present
in milk
Side-effects
nausea,
vomiting,
abdominal pain,
dys-
pepsia,
flatulence,
diarrhoea,
rectal bleeding;
head-
ache,
dizziness,
fatigue;
polyuria;
less commonly
anorexia,
palpitation,
tremor,
and fever
Dose
.
ADULT
over 18 years, 2 mg once daily;
ELDERLY
over 65
years, initially 1 mg once daily, increased if necessary
to 2 mg once daily
Note
Review treatment if no response after 4 weeks
Resolor
c
(Movetis) T A
Tablets
, f/c, prucalopride (as succinate) 1 mg (white),
net price 28-tab pack = £38.69;
2 mg (pink),
28-tab
pack = £59.52
1.7
Local preparations for
anal and rectal disorders
1.7.1 Soothing haemorrhoidal preparations
1.7.2 Compound haemorrhoidal
preparations with corticosteroids
1.7.3 Rectal sclerosants
1.7.4 Management of anal fissures
Anal and perianal pruritus, soreness, and excoriation are
best
treated by application of
bland ointments
and
suppositories (section 1.7.1).
These conditions occur
commonly in patients
suffering from haemorrhoids,
fistulas,
and proctitis.
Cleansing with attention to any
minor faecal soiling, adjustment of the diet to avoid hard
stools,
the use of
bulk-forming materials such as bran
(section 1.6.1)
and a high residue diet
are helpful.
In
proctitis
these measures
may supplement
treatment
with corticosteroids or sulfasalazine (see section 1.5).
When necessary,
topical
preparations containing local
anaesthetics (section 1.7.1) or corticosteroids (section
1.7.2)
are used,
provided perianal
thrush has
been
excluded.
Perianal thrush is treated with a topical anti-
fungal preparation (section 13.10.2).
For the management of
anal fissures
,
see section 1.7.4.
1.7.1
Soothing haemorrhoidal
preparations
Soothing preparations containing mild astringents such
as bismuth subgallate,
zinc oxide,
and hamamelis may
give symptomatic relief in haemorrhoids. Many proprie-
tary
preparations
also
contain
lubricants,
vaso-
constrictors,
or mild antiseptics.
Local anaesthetics are used to relieve pain associated
with
haemorrhoids
and
pruritus ani
but good evidence
BNF 61
1.6.7 5HT
4
-receptor agonists
75
1
Gastro-intestinal system