page128
Pregnancy
avoid (teratogenic in
animal
studies);
effective contraception required during and for at
least 3 months after administration (hormonal
contraception not considered effective); monthly
pregnancy tests advised
Breast-feeding
manufacturer advises avoid—no
information available
Side-effects
gastro-intestinal disturbances,
dry
mouth,
rectal haemorrhage,
hepatic impairment (see
Cautions,
above); flushing,
hypotension,
palpitation,
oedema,
chest pain;
dyspnoea;
headache,
dizziness,
fatigue;
back pain and pain in extremities; anaemia;
hypersensitivity reactions (including rash,
pruritus,
and anaphylaxis)
Dose
. Pulmonary arterial hypertension,
initially 62.5 mg
twice daily increased after 4 weeks to 125 mg twice
daily; max.
250 mg twice daily;
CHILD
under 12 years
see
BNF for Children
. Systemic sclerosis with ongoing digital ulcer disease,
initially 62.5 mg twice daily increased after 4 weeks to
125 mg twice daily
Tracleer
c
(Actelion) T A
Tablets
,
f/c,
orange,
bosentan (as monohydrate)
62.5 mg,
net price 56-tab pack = £1510.21;
125 mg,
56-tab pack = £1510.21
DIAZOXIDE
Indications
hypertensive emergency including severe
hypertension associated with renal disease (but no
longer recommended—see section 2.5);
hypoglyc-
aemia (section 6.1.4)
Cautions
ischaemic heart disease; interactions:
Appendix 1 (diazoxide)
Renal impairment
dose reduction may be required
Pregnancy
prolonged use may produce alopecia,
hypertrichosis,
and impaired glucose tolerance in
neonate;
inhibits uterine activity during labour
Side-effects
tachycardia, hypotension,
hyperglyc-
aemia,
sodium and water retention;
rarely
cardiome-
galy,
hyperosmolar non-ketotic coma,
leucopenia,
thrombocytopenia,
and hirsuitism
Dose
. By rapid intravenous injection (less than 30 seconds),
1–3 mg/kg to max. single dose of 150 mg (see below);
may be repeated after 5–15 minutes if required
Note
Single doses of
300 mg have been associated with
angina and with myocardial and cerebral infarction
Eudemine
c
(Goldshield) A U
Injection
, diazoxide 15 mg/mL, net price 20-mL amp
= £30.00
Tablets
,
see section 6.1.4
HYDRALAZINE HYDROCHLORIDE
Indications
moderate to severe hypertension
(adjunct);
heart failure (with long-acting nitrate,
but
see section 2.5.5);
hypertensive emergencies (includ-
ing during pregnancy) (see section 2.5)
Cautions
coronary artery disease (may provoke
angina,
avoid after myocardial infarction until stabi-
lised),
cerebrovascular disease;
occasionally blood
pressure reduction too rapid even with low parenteral
doses; manufacturer advises test for antinuclear factor
and for proteinuria every 6 months and check acet-
ylator status before increasing dose above 100 mg
daily,
but evidence of clinical value unsatisfactory;
interactions: Appendix 1 (hydralazine)
Contra-indications
idiopathic systemic lupus erythe-
matosus, severe tachycardia, high output heart failure,
myocardial insufficiency due to mechanical obstruc-
tion, cor pulmonale, dissecting aortic aneurysm; acute
porphyria (section 9.8.2)
Hepatic impairment
reduce dose
Renal impairment
reduce dose if eGFR less than
30 mL/minute/1.73 m
2
Pregnancy
neonatal thrombocytopenia reported,
but
risk should be balanced against risk of uncontrolled
maternal hypertension;
manufacturer advises avoid
before third trimester
Breast-feeding
present in milk but not known to be
harmful;
monitor infant
Side-effects
tachycardia, palpitation,
flushing,
hypo-
tension, fluid retention, gastro-intestinal disturbances;
headache,
dizziness;
systemic lupus erythematosus-
like syndrome after long-term therapy with over
100 mg daily (or less in women and in slow acetylator
individuals) (see also notes above); rarely rashes,
fever,
peripheral neuritis,
polyneuritis,
paraesthesia,
arthralgia, myalgia,
increased lacrimation,
nasal con-
gestion, dyspnoea, agitation, anxiety,
anorexia; blood
disorders (including leucopenia,
thrombocytopenia,
haemolytic anaemia),
abnormal liver function,
jaun-
dice,
raised plasma creatinine,
proteinuria and hae-
maturia reported
Dose
. By mouth, hypertension, 25 mg twice daily, increased
to usual max.
50 mg twice daily (see notes above)
Heart failure (initiated in hospital) 25 mg 3–4 times
daily,
increased every 2 days if necessary;
usual
maintenance dose 50–75 mg 4 times daily
. By slow intravenous injection,
hypertensive emer-
gencies and hypertension with renal complications,
5–10 mg diluted with 10 mL sodium chloride 0.9%;
may be repeated after 20–30 minutes (see Cautions)
.
By intravenous infusion,
hypertensive emergencies
and hypertension with renal complications,
initially
200–300 micrograms/minute;
maintenance usually
50–150 micrograms/minute
Hydralazine
(Non-proprietary) A
Tablets
,
hydralazine hydrochloride 25 mg,
net price
56 = £9.32;
50 mg,
56 = £16.84
Apresoline
c
(Amdipharm) A
Tablets
, yellow, s/c, hydralazine hydrochloride 25 mg,
net price 84-tab pack = £3.38
Excipients
include gluten
Injection
,
powder for reconstitution,
hydralazine
hydrochloride,
net price 20-mg amp = £2.22
ILOPROST
Indications
idiopathic or familial pulmonary arterial
hypertension
Cautions
unstable pulmonary hypertension with
advanced right heart failure;
hypotension (do not
initiate if systolic blood pressure below 85 mmHg);
acute pulmonary infection; chronic obstructive
pulmonary disease; severe asthma;
interactions:
Appendix 1 (iloprost)
Contra-indications
unstable angina;
within 6 months
of myocardial infarction;
decompensated cardiac
failure (unless under close medical supervision);
108
2.5.1 Vasodilator antihypertensive drugs
BNF 61
2
Cardiovascular system