Nitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary hypertension.
ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Nitrendipine is absorbed through gut and metabolized by liver before it goes into the systemic circulation and reaches the cells of the smooth muscles and cardiac muscle cells.
It binds more effectively with L-type calcium channels in smooth muscle cells because of its lower resting membrane potential. The Nitrendipine diffuses into the membrane and binds to its high affinity binding site on the inactivated L-type calcium channel that’s located in between each of the 4 intermembrane components of the α1 subunit. The exact mechanism of action of Nitrendipine is unknown, but it is believed to have important tyrosine and threonine residues in its binding pocket and its binding interferes with the voltage sensor and gating mechanism of the channel. Thought to have a domain-interface model of binding. In hypertension, the binding of Nitrendipine causes a decrease in the probability of open L-type calcium channels and reduces the influx of calcium. The reduced levels of calcium prevent smooth muscle contraction within these muscle cells. Prevention of muscle contraction enables smooth muscle dilation. Dilation of the vasculature reduces total peripheral resistance, which decreases the workload on the heart and prevents scarring of the heart or heart failure.
INDICATION AND DOSE
Hypertension
Adult: 20 mg daily as a single dose or in 2 divided doses; may be increased to 20 mg bid as necessary to control resistant hypertension.
Elderly: Initially, 10 mg daily.
Hepatic impairment: Initially, 5-10 mg once daily.
OVERDOSAGE
Symptoms: Flushing, headache, BP reduction with circulatory collapse, changes in heart rate (tachycardia, bradycardia). Management: Initially, gastric lavage with subsequent activated charcoal. Dopamine or noradrenaline may be used for excessive hypotension. Atropine or orciprenaline may be used for bradycardia.
ADVERSE DRUG REACTIONS
Hypotension, flushing, oedema, dizziness, palpitation, fatigue, headache, nausea, bloating, diarrhoea, paraesthesias, tachycardia, asthenia, drowsiness, angina, MI, irritability, respiratory disorders, hypersensitivity reactions, increased urine output, elevated LFTs, myalgia, tremor, blood count changes, gingival hyperplasia.
DRUG INTERACTIONS
Effects may be enhanced by other antihypertensives. Increased sodium excretion with diuretics at the start of treatment. May prolong effects of pancuronium, vecuronium. May increase digoxin levels. Reduced levels/effects with rifampicin, phenytoin, carbamazepine or phenobarbitone. Levels/effects may be increased with cimetidine, valproic acid, erythromycin, troleandomycin, clarithromycin, roxithromycin, ketoconazole, itraconazole, fluconazole, nefazodone, protease inhibitors, quinupristin or dalfopristin.
Potentially Fatal: Effects may be enhanced by other antihypertensives. Increased sodium excretion with diuretics at the start of treatment. May prolong effects of pancuronium, vecuronium. May increase digoxin levels. Reduced levels/effects with rifampicin, phenytoin, carbamazepine or phenobarbitone. Levels/effects may be increased with cimetidine, valproic acid, erythromycin, troleandomycin, clarithromycin, roxithromycin, ketoconazole, itraconazole, fluconazole, nefazodone, protease inhibitors, quinupristin or dalfopristin.
FOOD INTERACTIONS - Concentration may be increased with grapefruit juice.
BRANDS - COMPANY - COUNTRY
Balodipine Taiyo Pharmaceutical, Japan
Balotein Medisa Shinyaku, Japan
Baylotensin Tanabe Mitsubishi Pharma, Japan
Bayniroad Taisho Yakuhin, Japan
Bayotensin Bayer Vital, Germany
Bayotensin mite Bayer Vital, Germany
Baypresol Bayer, Spain
Baypress Bayer, Austria; Bayer, Belgium; Bayer, Switzerland; Bayer, Colombia; Bayer, Czech Republic; Bayer, Denmark; Bayer, Greece; Bayer, Hungary; Bayer, Italy; Bayer, South Korea; Bayer, Netherlands; Bayer, Thailand; Bayer, Turkey; Bayer Animal Health, Luxembourg; Bayer Santé, France
Baypress mite Bayer, Switzerland
Caltren Libbs, Brazil
Cardiazem Sanitas, Chile
Cenipres (Nitrendipine and Enalapril)- Ferrer, Austria
Cobatensin Kobayashi Kako, Japan
Ditrenil Siam Bheasach, Thailand
Dosperopin Towa Yakuhin, Japan
Ecatelisin Zensei Yakuhin, Japan
Ellenal Sanwa Kagaku, Japan
Eneas (Nitrendipine and Enalapril) - Abbott, Turkey; Dream Pharma, South Korea; Ferrer, Dominican Republic; Ferrer, Guatemala; Ferrer, Honduras; Ferrer, Luxembourg; Ferrer, Nicaragua; Ferrer, El Salvador; Ferrer Farma, Spain; Galenica, Greece; Galenica, Romania
ENEAS (Nitrendipine and Enalapril)- Ferrer, Germany; Merck, Germany
Enit (Nitrendipine and Enalapril) - Adeka, Turkey; Ferrer, Luxembourg; Ferrer Farma, Spain; Gap, Greece
Gericin Seid, Spain
Grifonitren Chile, Chile
Jutapress Juta, Germany; Q-Pharm, Germany
Leonitren Mentinova, Greece
Lisba Rafarm, Greece
Lostradyl Chrispa, Greece
Lusopress Berlin-Chemie, Bulgaria; Berlin-Chemie, Estonia; Instituto Luso Farmaco, Czech Republic; Luso, Latvia; Lusofarmaco, Lithuania; Lusofarmaco, Romania; Lusofarmaco, Slovakia; Lusofarmaco, Tunisia
Miniten Utopian, Thailand
Nelconil Pharmathen, Greece
Nian Ying Yuan, Taiwan
Nidrel UCB Pharma, France
Nifecard Bros, Greece
Nilzipin Kyorin Rimedio, Japan
Niprina Esteve, Spain
Nirapel Ivax, Argentina
Nitopress Kyowa Yakuhin, Japan
Nitotelocin Choseido Pharmaceutical, Japan
Nitregamma Wörwag Pharma, Germany
Nitren Lich Winthrop, Germany
Nitren Siu Guan, Taiwan
Nitren-acis Acis, Germany
Nitrencord Biosintética, Brazil
Nitrend KSK KSK-Pharma, Germany
Nitrendil Bagó, Argentina; Elmor, Venezuela
Nitrendilat Medilat, Greece
Nitrendipin - 1 A Pharma 1A Pharma, Germany
Nitrendipin AbZ AbZ-Pharma, Germany
Nitrendipin Actavis Actavis, Germany; Balkanpharma, Bulgaria
Nitrendipin AL Aliud, Bulgaria; Aliud, Germany
Nitrendipin Aristo Aristo Pharma, Germany
Nitrendipin Basics Basics, Germany
Nitrendipin beta Betapharm, Germany
Nitrendipin dura Mylan dura, Germany
Nitrendipin Heumann Heumann, Germany
Nitrendipin JENAPHARM mibe, Germany
Nitrendipin Lindopharm Lindopharm, Germany
Nitrendipin Sandoz Sandoz, Germany
Nitrendipin STADA STADA, Germany
Nitrendipin-corax Corax, Germany
Nitrendipin-CT CT Arzneimittel, Germany
Nitrendipine - Pacific Pharm - Pacific, China
Nitrendipine Myla Mylan, France
Nitrendipine Teva Teva Santé, France
Nitrendipine Xinhua Pharm - Xinhua, China
Nitrendipine-Xinhua Pharm - Xinhua, China
Nitrendipino Andromaco Andromaco, Chile
Nitrendipino L.CH. Chile, Chile
Nitrendipino Mintlab Mintlab, Chile
Nitrendipino Ratiopharm Ratiopharm, Spain
Nitrendipino Rider Rider, Chile
Nitrendipino Stada STADA, Spain
Nitrendipin-ratiopharm Ratiopharm, Germany; Ratiopharm, Czech Republic
Nitrendypina Anpharm Anpharm, Poland
Nitrensal TAD, Germany
Nitrepin Zdravlje, Serbia
Nitrepress Hexal, Czech Republic; Hexal, Germany; Hexal, Lithuania
Nitre-Puren Actavis, Germany
Nitresan Pro.Med., Poland; Pro.Med.CS, Czech Republic; Pro.Med.CS, Estonia; Pro.Med.CS, Lithuania; Pro.Med.CS, Slovakia
Nitrezic Ohara Yakuhin, Japan
Nivitron Coup, Greece
Potional Kleva, Greece
Ravena STADA, Bulgaria
Shetlazorna Nisshin Seiyaku - Yamagata, Japan
Shu Mai Te Great Wall Pharmaceutical Factory, China
Spidox Finixfarm, Greece
Tensogradal Kern, Spain
Tepanil - Norma Hellas, Greece
Unipres - Krka, Czech Republic; Krka, Hungary; Krka, Lithuania; Krka, Slovenia
Unipress - Krka, Slovakia
Vastensium - Salvat, Spain
Vipres (Nitrendipine and Enalapril) - Ferrer Farma, Spain
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