Monograph: |
Nicardipine Hydrochloride
Incompatibilities. The manufacturers recommend that a
solution containing nicardipine hydrochloride 0.1 mg per mL
is used for intravenous infusion. Suitable diluents are solu-
tions of glucose or sodium chloride; sodium bicarbonate and
lactated Ringer's are incompatible with nicardipine infusion.
Adverse Effects, Treatment, and Precautions
As for dihydropyridine calcium-channel blockers
(see Nifedipine).
Interactions
As tor dihydropyridine calcium-channel blockers
(see Nifedipine).
Pharmacokinetics
Nicardipine is rapidly absorbed from the gastro-in-
testinal tract but is subject to saturable first-pass he-
patic metabolism. Bioavailability of about 35% has
been reported following a 30-mg dose at steady
state. The pharmacokinetics of nicardipine are non-
linear due to the saturable first-pass hepatic metabo-
lism and an increase in dose may produce a dispro-
portionate increase in plasma concentration. There
is also considerable interindividual variation in plas-
ma-nicardipine concentrations. Nicardipine is high-
ly bound to plasma proteins (more than 95%).
Nicardipine is extensively metabolised in the liver
and is excreted in the urine and faeces, mainly as
inactive metabolites. The terminal plasma half-life
is about 8.6 hours, thus steady-state plasma concen-
trations are achieved after 2 to 3 days of dosing three
times a day.
Uses and Administration
Nicardipine hydrochloride is a dihydropyridine cal
cium-channel blocker with actions and uses similar
to nifedipine. It is used in the management
of hypertension and angina pectoris.
Nicardipine hydrochloride is generally given
mouth although the intravenous route has been em-
ployed for the short-term treatment of hypertension
Oral doses of nicardipine hydrochloride are similar
for both hypertension and angina. An initial dose
of 20 mg by mouth three times a day is recommend-
ed. The dose may be increased at intervals of 3 days
until the required effect is achieved. The effective
dose range is between 60 and 120 mg per day, the
usual dose being 30 mg three times a day; in hyper
tensive patients a maintenance dose of 30 or 40 mg
twice daily may be possible. Modified-release prep
arations of nicardipine hydrochloride for adminis-
tration twice daily are also available.
Nicardipine hydrochloride may be administered
slow intravenous infusion as a 0.1 mg per mL so
tion in the short-term treatment of hypertension.
initial infusion rate of 5 mg per hour is recommed
ed, increased, as necessary, up to a maximum
15 mg per hour and subsequently reduced to 3
mg per hour.
Reduced doses of nicardipine hydrochloride
And longer dosing intervals may be necessary in patients with impaired liver function.
Administration in neonates. Intravenous infusion of
nicardipine was used successfully in 8 preterm infants (gesta-
tional age 28 to 36 weeks) for the management of hyperten-
sion. Infusions were continued for periods of 3 to 36 days.
No hypotension, oedema, or tachycardia were observed.
Cerebrovascular disorders: Nicardipine ha5 been report-
ed to increase cerebral blood flow' and has been investigated
for possible benefit in haemorrhagic and ischaemic stroke
although nimodipine is the dihydropyridine
calcium-channel blocker usually used. Nicardipine has also
been tried' in patients with cerebrovascular insufficiency.
However, studies have produced inconclusive results.
Renal transplantation. Like other calcium-channel block-
nicardipine increases blood-cyclosporine concentrations
when the 2 drugs are given concurrently However, in con-
trast to reports of benefit from the concurrent use of nifed-
ipine and cyclosporine, Kessler and colleagues did not
note any improvement in renal function when nicardipine and
cyclosporine were given together in renal transplant patients'
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