High Blood Pressure / Hypertension

Nicardipine Hydrochloride

By Cardiologist on September 30th, 2010

Drug Nomenclature

Pharmacopoeias. In China, and Japan.

Incompatibility. The manufacturers recommend that a solution containing nicardipine hydrochloride 100 micrograms/mL is used for intravenous infusion. Suitable diluents are solutions of glucose or sodium chloride. Sodium bicarbonate and lactated Ringer’s are incompatible with nicardipine infusion. Nicardipine hydrochloride (1 mg/mL in glucose 5%) has also been reported to be visually incompatible with furosemide, heparin, and thiopental.

Adverse Effects, Treatment, and Precautions

As for dihydropyridine calcium-channel blockers (see Nifedipine).

Interactions

As for dihydropyridine calcium-channel blockers (see Nifedipine).

Pharmacokinetics

Nicardipine is rapidly and completely absorbed from the gastrointestinal tract but is subject to saturable first-pass hepatic metabolism. Bioavailability of about 35% has been reported after a 30-mg dose at steady state. The pharmacokinetics of nicardipine are non-linear due to the saturable first-pass hepatic metabolism and an increase in dose may produce a disproportionate increase in plasma concentration. There is also considerable interindividual variation in plasma-nicardipine concentrations. Nicardipine is more than 95% bound to plasma proteins. 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 concentrations are achieved after 2 to 3 days of dosing three times daily.

Uses and Administration

Nicardipine is a dihydropyridine calcium-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 orally although the intravenous route has been used for the short-term treatment of hypertension.

Oral doses of nicardipine hydrochloride are similar for both hypertension and angina. The initial dose is 20 mg three times daily and may be increased at intervals of at least 3 days until the required effect is achieved. The usual maintenance dose is 30 mg three times daily, but daily doses of between 60 and 120 mg in divided doses may be given. Modified-release preparations of nicardipine hydrochloride for dosage twice daily are also available.

Nicardipine hydrochloride may be given by slow intravenous infusion as a 100 micrograms/mL solution in the short-term treatment of hypertension. An initial infusion rate of 5 mg/hour is recommended, increased, as necessary, up to a maximum of 15 mg/hour and subsequently reduced to 3 mg/hour. For use in children, see below.

Reduced doses of nicardipine hydrochloride and longer dosing intervals may be necessary in patients with hepatic or renal impairment (see below).

Administration in children. Intravenous infusion of nicardipine has been used in both infants and children for the management of hypertension. In studies in children aged between 2 days and 17 years, initial doses ranged from 0.2 to 5 micrograms/kg per minute, with maintenance infusions of 0.15 to 6 micrograms/kg per minute. Adverse effects were rare; one study reported adverse effects in 5 of 31 treatment courses, including tachycardia, flushing, palpitations, and hypotension. There has also been a report of the successful use of intravenous infusion of nicardipine in 8 preterm infants (gestational age 28 to 36 weeks). Infusions were given at a dose of 0.5 to 2 micrograms/kg per minute and continued for periods of 3 to 36 days. No hypotension, oedema, or tachycardia were observed. The BNFC suggests that neonates and children up to age 18 years may be given nicardipine hydrochloride by continuous intravenous infusion for the management of hypertensive crises. The initial dose is 500 nanograms/kg per minute, adjusted according to response; the usual maintenance dose is 1 to 4 micrograms/kg per minute, with a maximum dose of 250 micrograms/minute.

Administration in hepatic or renal impairment. Reduced doses of nicardipine hydrochloride and longer dosing intervals may be necessary in patients with hepatic or renal impairment. The US manufacturers recommend an initial dose of 20 mg twice daily by mouth in patients with hepatic impairment.

Cerebrovascular disorders. Nicardipine has been reported to increase cerebral blood flow and use by various routes 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.

Proprietary Preparations

Austria: Karden;

Belgium: Rydene;

France: Loxen;

Germany: Antagonil;

Indonesia: Perdipine;

Ireland: Cardene †;

Italy: Bionicard; Cardioten; Cardip; Cordisol †; Lisanirc; Neucor; Nicant †; Nicapress; Nicardal; Nicarpin; Nicaven; Nimicor; Niven †; Perdipina; Ranvil †; Vasodin;

Japan: Perdipine;

Malaysia: Cardepine;

The Netherlands: Cardene;

Philippines: Cardepine;

Portugal: Nerdipina;

Singapore: Cardibloc;

Spain: Dagan; Flusemide; Lecibral; Lincil; Lucenfal; Nerdipina; Vasonase;

Thailand: Cardepine; Nerdipine †;

Turkey: Loxen;

United Kingdom (UK): Cardene;

United States of America (US and USA): Cardene.

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