Nisoldipine

(BAN, USAN, rINN)
Nisoldipine Chemical formula
Synonyms: Bay-k-5552; Nisoldipiini; Nisoldipin; Nisoldipino; Nisoldipinum. Isobutyl methyl 1,4-dihydro-2,6dimethyl-4-(2-nitrophenyl)pyridine-3,5-dicarboxylate.
Cyrillic synonym: Низольдипин.

💊 Chemical information

Chemical formula: C20H24N2O6 = 388.4.
CAS — 63675-72-9.
ATC — C08CA07.
ATC Vet — QC08CA07.

💊 Adverse Effects, Treatment, and Precautions

As for dihydropyridine calcium-channel blockers.

💊 Interactions

As for dihydropyridine calcium-channel blockers.

💊 Pharmacokinetics

Nisoldipine is well absorbed from the gastrointestinal tract after oral doses but undergoes rapid and extensive first-pass metabolism in the gut wall and liver and bioavailability has been reported to be only about 4 to 8%. About 60 to 80% of an oral dose is excreted in the urine and the remainder in the faeces, mainly as metabolites. The terminal elimination half-life is about 7 to 12 hours. Nisoldipine is more than 99% bound to plasma proteins.
Peak plasma concentrations occurred 1 hour after a single oral dose, and varied greatly between the patients. The mean plasma elimination half-life was 11.4 hours after a single dose and 14.0 hours after repeated dosing, which was longer than had been previously reported, perhaps reflecting the greater sensitivity of the assay. In another study oral, but not intravenous, nisoldipine increased liver blood flow in 10 healthy subjects and thus affected its own systemic availability.2 Variations in liver blood flow may account for the interindividual variation in the pharmacokinetics of nisoldipine.
1. Ottosson A-M, et al. Analysis and pharmacokinetics of nisoldipine in hypertensive patients. Curr Ther Res 1989; 45: 347–58
2. van Harten J, et al. Variability in the pharmacokinetics of nisoldipine as caused by differences in liver blood flow response. J Clin Pharmacol 1989; 29: 714–21.

💊 Uses and Administration

Nisoldipine is a dihydropyridine calcium-channel blocker with actions and uses similar to those of nifedipine. It is used in the management of hypertension and angina pectoris. Nisoldipine is given orally usually as a modified-release preparation. Absorption is affected by food and the modified-release preparation should be taken on an empty stomach; it should not be taken with high fat meals. Doses are similar for both hypertension and angina. The initial dose is 10 mg once daily and the usual maintenance dose is 20 to 40 mg once daily.
1. Mitchell J, et al. Nisoldipine: a new dihydropyridine calciumchannel blocker. J Clin Pharmacol 1993; 33: 46–52
2. Plosker GL, Faulds D. Nisoldipine coat-core: a review of its pharmacology and therapeutic efficacy in hypertension. Drugs 1996; 52: 232–53
3. Langtry HD, Spencer CM. Nisoldipine coat-core; a review of its pharmacodynamic and pharmacokinetic properties and clinical efficacy in the management of ischaemic heart disease. Drugs 1997; 53: 867–84.

💊 Preparations

Proprietary Preparations

Arg.: Nisodipen†; Austria: Syscor; Belg.: Sular; Syscor; Braz.: Syscor; Chile: Nivas; Cz.: Syscor†; Fin.: Syscor; Ger.: Baymycard; Gr.: Syscor; Hung.: Baymycard; Ital.: Syscor; NZ: Syscor; S.Afr.: Syscor†; Spain: Cornel†; Sular; Syscor; Switz.: Syscor†; UK: Syscor; USA: Sular.
Published May 08, 2019.