Nimodipin

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

• Sicherheit

  P264：Nach Gebrauch gründlich waschen.

  P264：Nach Gebrauch gründlich waschen.

  P270：Bei Gebrauch nicht essen, trinken oder rauchen.

  P301+P312：BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

  P501：Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Nimodipine Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.

• S-Sätze Betriebsanweisung:

  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

• Beschreibung

  Nimodipine is a cerebral vasodilating calcium antagonist related to nifedipine. It is indicated for the prophylaxis and treatment of neurological deficits due to cerebral vasospasm after subarachnoid hemorrhage.

• Chemische Eigenschaften

  Crystalline Solid

• Originator

  Bayer (W. Germany)

• Verwenden

  provitamin, antixerophthalamic

• Verwenden

  Nimodipine has been used:
  
  • as a L-type calcium channel (LTCC) inhibitor, to evaluate its neuroprotective activity in the vibrosections
  • as a standard, in the enantioseparation of chiral drugs by high performance liquid chromatography (HPLC)
  • in the pharmacological studies for the measurement of spine voltage escape
  
  

• Verwenden

  Used as a cerebral vasodilator. A dihydropyridine calcium channel blocker

• Verwenden

  A dihydropyridine calcium channel blocker. It is used as a vasodilator (cerebral).

• Definition

  ChEBI: A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm.

• Manufacturing Process

  After 8 hours boiling of solution of 3.8 g of 3'-nitro-benzylideneacetoacetic acid isopropylester, 8 grams of acetoacetic acid β-metoxyethyl ester and 6 ml conc ammonia in 80 ml ethanol under reflux, 2,6-dimethyl-4-(3'-nitrophenyl)- 1,4-dihydropyridine 3-β-methoxyethyl ester 5-isopropyl ester of melting point 125°C (petroleum ether/ acetic ester) was obtained. Yield 49% of theory.

• Trademarks

  Nimotop (Bayer).

• Therapeutic Function

  Vasodilator

• Allgemeine Beschreibung

  Nimodipine, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)- 3,5-pyridinedicarboxylic acid 2-methoxyethyl1-methylethyl ester (Nimotop), is another dihydropyridinecalcium channel blocker but differs in that it dilatesthe cerebral blood vessels more effectively than do the otherdihydropyridine derivatives. This drug is indicated for treatmentof subarachnoid hemorrhage-associated neurologicaldeficits.

• Biologische Aktivität

  L-type Ca 2+ channel blocker.

• Biochem/physiol Actions

  Nimodipine enhances the survival of dopaminergic substantia nigra neurons.

• Clinical Use

  Calcium-channel blocker:
  Prevention and treatment of ischaemic neurological deficits following subarachnoid haemorrhage

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Aminophylline: possibly increases aminophylline concentration.
  Anaesthetics: enhanced hypotensive effect.
  Antibacterials: metabolism accelerated by rifampicin; metabolism possibly inhibited by clarithromycin, erythromycin and telithromycin.
  Antidepressants: enhanced hypotensive effect with MAOIs .
  Antiepileptics: effect reduced by carbamazepine,
  barbiturates, phenytoin and primidone.
  Antifungals: metabolism possibly inhibited by itraconazole and ketoconazole; negative inotropic effect possibly increased with itraconazole.
  Antihypertensives: enhanced hypotensive effect, increased risk of first dose hypotensive effect of post synaptic alpha-blockers.
  Antivirals: concentration possibly increased by ritonavir; use telaprevir with caution.
  Grapefruit juice: concentration increased - avoid.
  Theophylline: possibly increased theophylline concentration.

• Stoffwechsel

  Nimodipine is extensively metabolised in the liver via the cytochrome P450 isoenzyme CYP3A4. It is eliminated as metabolites, mainly by dehydrogenation of the dihydropyridine ring and oxidative O-demethylation. Oxidative ester cleavage, hydroxylation of the 2- and 6-methyl groups, and glucuronidation as a conjugation reaction are other important metabolic steps. The three primary metabolites occurring in plasma show no or only therapeutically negligible residual activity. The metabolites are excreted about 50% renally and 30% in faeces via the bile.

• Lager

  Store at RT

• Einzelnachweise

  1) Cohen and McCarthy (1987),?Nimodipine block of calcium channels in rat anterior pituitary cells; J. Physiol.,?387?195 2) Batuecas?et al.?(1998),?Effects of chronic nimodipine on working memory of old rats in relation to defects in synaptosomal calcium homeostasis; Eur. J. Pharmacol.,?350?141 3) LeVere?et al.?(1989),?Recovery of function after brain damage: facilitation by the calcium entry blocker nimodipine; Behav. Neurosci.,?103?561 4) Herzfeld?et al.?(2014),?Investigation of the neuroprotective impact of nimodipine on Neuro2a cells by means of a surgery-like stress model; Int. J. Mol. Sci.,?15?18453 5) Schampel?et al.?(2017),?Nimodipine fosters remyelination in a mouse model of multiple sclerosis and induces microglia-specific apoptosis; Proc. Natl. Acad. Sci. USA,?114?E3295 6) Allen?et al.?(1983),?Cerebral arterial spasm – a controlled trial of nimodipine in patients with subarachnoid hemorrhage; N. England J. Med.,?308?619

Nimodipine Upstream-Materialien And Downstream Produkte

Nimodipin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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