Nitrendipine

(BAN, USAN, rINN)
Nitrendipine Chemical formula
Synonyms: Bay-e-5009; Nitrendipiini; Nitrendipin; Nitrendipinas; Nitrendipino; Nitrendipinum. Ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(3nitrophenyl)pyridine-3,5-dicarboxylate.
Cyrillic synonym: Нитрендипин.

💊 Chemical information

Chemical formula: C18H20N2O6 = 360.4.
CAS — 39562-70-4.
ATC — C08CA08.
ATC Vet — QC08CA08.

Pharmacopoeias.

In Chin., Eur., and Jpn.

Ph. Eur. 6.2

(Nitrendipine). A yellow crystalline powder. It exhibits polymorphism. Practically insoluble in water; sparingly soluble in dehydrated alcohol and in methyl alcohol; freely soluble in ethyl acetate. Exposure to ultraviolet light leads to formation of a nitrophenylpyridine derivative. Solutions should be prepared in the dark or under light of wavelength greater than 420 nm, immediately before use. Protect from light.

💊 Adverse Effects, Treatment, and Precautions

As for dihydropyridine calcium-channel blockers.

💊 Interactions

As for dihydropyridine calcium-channel blockers.

💊 Pharmacokinetics

Nitrendipine is reported to be well absorbed after oral doses but undergoes extensive first-pass metabolism; the absolute oral bioavailability is reported to range from about 10 to 20%, depending in part on the dosage form. Nitrendipine is about 98% bound to plasma proteins. It is extensively metabolised in the liver and is excreted as metabolites, mainly in urine, with small amounts in the faeces. Although early studies reported a terminal elimination half-life of about 2 to 4 hours, later studies, using more sensitive assay procedures, have recorded values between about 10 and 22 hours.
1. Soons PA, Breimer DD. Stereoselective pharmacokinetics of oral and intravenous nitrendipine in healthy male subjects. Br J Clin Pharmacol 1991; 32: 11–16.

💊 Uses and Administration

Nitrendipine is a dihydropyridine calcium-channel blocker with actions similar to those of nifedipine. It is used in the treatment of hypertension. The usual dose is 20 mg daily as a single oral dose or as 2 divided doses. The dose may be increased to 20 mg twice daily if necessary for the control of resistant hypertension. In the elderly, an initial dose of 10 mg daily should be used. The dose should also be reduced in hepatic impairment (see below).
1. Santiago TM, Lopez LM. Nitrendipine: a new dihydropyridine calcium-channel antagonist for the treatment of hypertension. DICP Ann Pharmacother 1990; 24: 167–75.

Administration in hepatic impairment.

The initial dose of nitrendipine should be reduced to 5 to 10 mg once daily in patients with hepatic impairment.

💊 Preparations

Proprietary Preparations

Arg.: Nirapel; Nitrendil; Tocrat†; Austria: Baypress; Belg.: Baypress; Braz.: Caltren; Nitrencord; Chile: Cardiazem; Grifonitren; Nitrendicor†; Presabet†; Tensofar; Cz.: Baypress; Lusopress; Nitrepress; Nitresan; Unipres; Denm.: Baypress; Fr.: Baypress; Nidrel; Ger.: Bayotensin; Jutapress; Nitre; Nitre-Puren; Nitregamma; Nitren Lich; Nitren†; Nitrendepat†; Nitrendidoc; Nitrendimerck†; Nitrensal; Nitrepress; Gr.: Aroselin; Baypress; Crivion; GPress; Lanocardique†; Leonitren; Lisba; Lostradyl; Midonat†; Nelconil; Nifecard; Nivitron; Pallohyman†; Potional; Pressodipin; Spidox; Tepanil†; Ufocard; Hong Kong: Baypress; Hung.: Baypress; Unipres; Ital.: Baypress; Deiten; Jpn: Baylotensin; Mex.: Baypress†; Neth.: Baypress; Port.: Baypress; Farnitran; Hiperdipina; Hipertenol†; Spain: Balminil†; Baypresol; Gericin; Niprina; Sub Tensin; Tensogradal; Trendinol†; Vastensium; Switz.: Baypress; Thai.: Baypress; Ditrenil; Miniten; Turk.: Baypress; Venez.: Baypress; Nitrendil; Retencal†. Multi-ingredient: Ger.: Eneas; Gr.: Eneas; Enit; India: Cardif Beta; Port.: Eneas; Enit; Spain: Eneas; Enit; Vipres; Zorail.
Published May 08, 2019.