NITRENDIPINE

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