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acid sequestrants
effectively reduce LDL-cholesterol
but can aggravate hypertriglyceridaemia.
Cautions
Bile acid sequestrants
interfere with the
absorption of fat-soluble vitamins; supplements of vita-
mins A,
D,
K,
and folic acid may be required when
treatment is prolonged.
Interactions: Appendix 1 (bile
acid sequestrants)
Pregnancy and breast-feeding
Bile acid seques-
trants should be used with caution as although the drugs
are not
absorbed,
they may cause fat-soluble vitamin
deficiency on prolonged use.
Side-effects
As
bile
acid
sequestrants
are
not
absorbed,
gastro-intestinal
side-effects
predominate.
Constipation is common,
but
diarrhoea has occurred,
as have nausea, vomiting, and gastro-intestinal discom-
fort.
Hypertriglyceridaemia
may
be
aggravated.
An
increased bleeding tendency has been reported due to
hypoprothrombinaemia associated with vitamin K defi-
ciency.
Counselling
Other drugs should be taken at least 1
hour before (4 hours before colesevelam), or 4–6 hours
after bile acid sequestrants to reduce possible interfer-
ence with absorption.
Colesevelam can be taken at the
same time as a statin or ezetimibe.
COLESEVELAM HYDROCHLORIDE
Indications
primary hypercholesterolaemia as an
adjunct to dietary measures,
either alone or with a
statin; primary and familial hypercholesterolaemia, in
combination with ezetimibe,
either with or without a
statin
Cautions
see notes above; also gastro-intestinal moti-
lity disorders,
major gastro-intestinal surgery,
inflammatory bowel disease; patients receiving
ciclosporin should have their blood-ciclosporin con-
centration monitored before,
during,
and after treat-
ment with colesevelam;
interactions: Appendix 1
(colesevelam)
Contra-indications
bowel or biliary obstruction
Hepatic impairment
manufacturer advises caution
Pregnancy
see notes above
Breast-feeding
see notes above
Side-effects
see notes above; also headache; myalgia
Dose
. Monotherapy, 3.75 g daily in 1–2 divided doses; max.
4.375 g daily
. Combination therapy with a statin,
or ezetimibe,
or
both,
2.5–3.75 g daily in 1–2 divided doses
Cholestagel
c
(Genzyme) T A
Tablets
,
f/c,
colesevelam hydrochloride 625 mg,
net
price 180-cap pack = £87.36.
Label:
21,
counselling,
avoid other drugs at same time (see notes above)
COLESTYRAMINE
(Cholestyramine)
Indications
hyperlipidaemias,
particularly type IIa,
in
patients who have not responded adequately to diet
and other appropriate measures;
primary prevention
of coronary heart disease in men aged 35–59 years
with primary hypercholesterolaemia who have not
responded to diet and other appropriate measures;
pruritus associated with partial biliary obstruction and
primary biliary cirrhosis (section 1.9.2);
diarrhoeal
disorders (section 1.9.2)
Cautions
see notes above; interactions:
Appendix 1
(colestyramine)
Contra-indications
complete biliary obstruction (not
likely to be effective)
Pregnancy
see notes above
Breast-feeding
see notes above
Side-effects
see notes above;
intestinal obstruction
reported rarely and hyperchloraemic acidosis
reported on prolonged use
Dose
. Lipid reduction,
initially 4 g daily increased by 4 g at
weekly intervals to 12–24 g daily in 1–4 divided doses,
then adjusted as required;
max.
36 g daily
. Pruritus,
see section 1.9.2
. Diarrhoeal disorders,
see section 1.9.2
.
CHILD
6–12 years,
see
BNF for Children
Note
The contents of each sachet should be mixed with at least
150 mL of water or other suitable liquid such as fruit juice,
skimmed milk, thin soups, and pulpy fruits with a high moisture
content
Colestyramine
(Non-proprietary) A
Powder
,
sugar-free,
colestyramine (anhydrous) 4 g/
sachet,
net price 50-sachet pack = £18.34.
Label:
13,
counselling, avoid other drugs at same time (see notes
above)
Excipients
may include aspartame (see section 9.4.1)
Questran
c
(Bristol-Myers Squibb) A
Powder
,
colestyramine (anhydrous) 4 g/sachet,
net
price 50-sachet pack = £10.76. Label: 13, counselling,
avoid other drugs at same time (see notes above)
Excipients
include sucrose 3.79 g/sachet
Questran Light
c
(Bristol-Myers Squibb) A
Powder
,
sugar-free,
colestyramine (anhydrous) 4 g/
sachet,
net price 50-sachet pack = £16.15.
Label:
13,
counselling, avoid other drugs at same time (see notes
above)
Excipients
include aspartame (see section 9.4.1)
COLESTIPOL HYDROCHLORIDE
Indications
hyperlipidaemias,
particularly type IIa,
in
patients who have not responded adequately to diet
and other appropriate measures
Cautions
see notes above; interactions: Appendix 1
(colestipol)
Pregnancy
see notes above
Breast-feeding
see notes above
Side-effects
see notes above
Dose
. Initially 5 g 1–2 times daily in liquid increased if
necessary in 5-g increments at intervals of 1 month to
max.
30 g daily (in 1–2 divided doses)
Note
The contents of each sachet should be mixed with at least
100 mL of water or other suitable liquid such as fruit juice,
skimmed milk, thin soups, yoghurt, and pulpy fruits with a high
moisture content
Colestid
c
(Pharmacia) A
Granules
, yellow, colestipol hydrochloride 5 g/sachet,
net price 30 sachets = £15.05. Label:
13, counselling,
avoid other drugs at same time (see notes above)
Colestid Orange
,
granules, yellow/orange,
colestipol
hydrochloride 5 g/sachet,
with aspartame, net price
30 sachets = £15.05.
Label:
13,
counselling,
avoid
other drugs at same time (see notes above)
BNF 61
2.12 Lipid-regulating drugs
165
2
Cardiovascular system