Pharmacology of Nimodipine — A Review

  • A. Scriabine
Conference paper
Part of the Advances in Neurosurgery book series (NEURO, volume 18)

Abstract

Among Ca2+ antagonists (Ca2+ channel antagonists, Ca2+ entry blockers, CAs) several drugs were reported to have anti-ischemic, anticonvulsant, or other effects on the central nervous system. One Ca2+ antagonist, nimodipine, was approved in the United States for prevention of neurological deficits in patients with subarachnoid hemorrhage. Some CAs are being used for the treatment of focal and global cerebral ischemia and other disorders of the central nervous system. This article reviews pharmacological properties of nimodipine which justify its use in some disorders of the central nervous system. It updates previous reviews on the same subject [28–30].

Keywords

Cereb Blood Flow Global Cerebral Ischemia Middle Cerebral Artery Nervous System Disorder Dorsal Root Ganglion Cell 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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References

  1. 1.
    Allen GS, Ahn HS, Preziosi TJ et al. (1983) Cerebral arterial spasm — a controlled trail of nimodipine in patients with subarachnoid hemorrhage. N Engl J Med 308:619–624PubMedCrossRefGoogle Scholar
  2. 2.
    Bellemann P, Schade A, Towart R (1983) Dihydropyridine receptor in rat brain labeled with [3H]nimodipine. Proc Natl Acad Sei USA 80:2356–2360CrossRefGoogle Scholar
  3. 3.
    DeFalco FA, Bartiromo U, Majello I, DeGeronimo G, Mundo P (1989) Usefulness of calcium antagonist nimodipine in treatment of epilepsy in young patients with organic brain lesion. Abstracts of the 4th International Symposium on Ca2+ Antagonists, Florence, May 25–27, p 274Google Scholar
  4. 4.
    Deyo RA, Straube KT, Disterhoft JF (1989) Nimodipine facilitates trace conditioning of the eye-blink response in aging rabbits. Science 243:809–811PubMedCrossRefGoogle Scholar
  5. 5.
    Freedman SB, Miller RJ (1984) Effects of nitrendipine on voltage sensitive calcium channels in brain and neuronal cultured cells. In: Scriabine A, Vanov S, Deck K (eds) Nimodipine. Urban and Schwarzenberg, Baltimore, pp 79–90Google Scholar
  6. 6.
    Fry HK, McCarthy RT (1988) Nimodipine block of L-type calcium channels in freshly dispersed rabbit DRG neurons. Soc Neurosci Abstr 14, 134Google Scholar
  7. 7.
    Gelmers HJ, Gorter K, deWeerdt CJ, Wierer HJA (1988) A controlled trial of nimodip- ine in acute ischemic stroke. N Engl J Med 318:203–207PubMedCrossRefGoogle Scholar
  8. 8.
    Germano IM, Bartkowski HM, Pitts LH (1987) The therapeutic value of nimodipine in experimental cerebral ischemia: neurological outcome and histopathologic findings. J Neurosurg 67:81–87PubMedCrossRefGoogle Scholar
  9. 9.
    Hadley MN, Spetzler RF, Fifield MS, Bichard WD, Hodak JA (1987) The effect of nimodipine on intracranial pressure — volume-pressure studies in a primate model. J Neurosurg 67:387–393PubMedCrossRefGoogle Scholar
  10. 10.
    Hakim A, Hogan M, Berger M, Gjedde A (1989) Activation of the Ca channels in focal cerebral ischemia. J Cereb Blood Flow Metab 9 [Suppl 1]:S14Google Scholar
  11. 11.
    Hoffmeister F, Kazda S, Krause HP (1979) Influence of nimodipine (BAY E 9736) on the postischemic changes of brain function. Acta Neurol Scand 72:358–359Google Scholar
  12. 12.
    Hoffmeister F, Benz U, Heise A, Krause HP, Neuser V (1982) Behavioral effects of nimodipine in animals. Arzneimittelforschung 32:347–360PubMedGoogle Scholar
  13. 13.
    Kazda S, Garthoff B, Krause HP, Schlossmann K (1982) Cerebrovascular effects of the calcium antagonistic dihydropyridine derivative, nimodipine, in animal experiments. Arzneimittelforschung 32:331–338PubMedGoogle Scholar
  14. 14.
    Kazda S, Garthoff B, Luckhaus G, Nash G (1982) Prevention of cerebrovascular lesions and mortality in stroke-prone spontaneously hypertensive rats by the calcium antagonist nimodipine. In: Godfraind T, Albertini A, Paoletti R (eds) Calcium modulators. Elsevier Biomedical, Amsterdam, pp 155–167Google Scholar
  15. 15.
    Kerckhoff W van den, Ehrewes LR (1985) Transfer of the Ca-antagonists nifedipine and nimodipine across the blood-brain barrier and their regional distribution in vivo. J Cereb Blood Flow Metab 5 [Suppl I]:S459-S460Google Scholar
  16. 16.
    McCarthy RT (1989) Nimodipine block of L-type calcium channels in dorsal root ganglion cells. In: Gispen WH, Traber J (eds) Nimodipine and central nervous system function: new vistas. Schattauer, StuttgartGoogle Scholar
  17. 17.
    Meyer H, Wehinger E, Bossert F, Scherling D (1983) Nimodipine: synthesis and metabolic pathway. Arzneimittelforschung 33:106–112PubMedGoogle Scholar
  18. 18.
    Meyer FB, Anderson RE, Yaksh TL, Sundt TM (1986) Effect of nimodipine on intracellular brain pH, cortical blood flow, and EEG in experimental focal cerebral ischemia. J Neurosurg 64:617–626PubMedCrossRefGoogle Scholar
  19. 19.
    Meyer FB, Anderson RE, Sundt TM, Sharbrough FW (1986) Selective central nervous system calcium channel blockers — a new class of anticonvulsant agents. Mayo Clin Proc 61:239–247PubMedGoogle Scholar
  20. 20.
    Meyer FB, Tally PW, Anderson RE, Sundt TM Jr, Yaksh TL (1986) Inhibition of electrically induced seizures by a dihydropyridine calcium channel blocker. Brain Res 384:180–183PubMedCrossRefGoogle Scholar
  21. 21.
    Morocutti C, Pierelli F, Sanarelli L, Stefano E, Peppe A, Mattioli GL (1986) Antiepilep- tic effects of calcium antagonist (nimodipine) on cefazolin-induced epileptogenic foci in rabbits. Epilepsia 27:498–503PubMedCrossRefGoogle Scholar
  22. 22.
    Mossakowski MJ, Gadamski R (1987) Influence of the calcium channel blocker on the ischemic changes in sector CAi pyramidal neurons of Ammon’s horn in Mongolian gerbils. Neuropatol Pol 25:439–450PubMedGoogle Scholar
  23. 23.
    Peroutka SJ, Allen GS (1983) Calcium channel antagonist binding sites labeled by [3H]nimodipine in human brain. J Neurosurg 59:933–937PubMedCrossRefGoogle Scholar
  24. 24.
    Philippon J, Grob R, Dagreou F, Guggiari M, Rivierez M, Vials P (1986) Prevention of vasospasm in subarachnoid hemorrhage. A controlled study with nimodipine. Acta Neurochir (Wien) 82:110–114Google Scholar
  25. 25.
    Pickard JD, Murray GD, Illingworth R et al. (1989) Effects of oral nimodipine on cerebral infarction and outcome after subarachnoid haemorrhage: British aneurysm nimodipine trial. Br Med J 298:636–642CrossRefGoogle Scholar
  26. 26.
    Quirion R (1985) Characterization of binding sites for two classes of calcium channel antagonists in human forebrain. Eur J Pharmacol 117:139–142PubMedCrossRefGoogle Scholar
  27. 27.
    Schuurman T, Klein H, Beneke M, Traber J (1987) Nimodipine and motor deficits in the aged rat. Neurosci Res Commun 1:9–15Google Scholar
  28. 28.
    Scriabine A, Battye R, Hoffmeister F et al. (1985) Nimodipine. In: Scriabine A (ed) New cardiovascular drugs. Raven, New York, pp 197–218Google Scholar
  29. 29.
    Scriabine A, Kerckhoff van den W (1988) Pharmacology of nimodipine, a review. Ann NY Acad Sei 522:698–706CrossRefGoogle Scholar
  30. 30.
    Scriabine A, Schuurman T, Traber J (1989) Pharmacological basis for the use of nimodipine in central nervous system disorders. FASEB J 3:1799–1806PubMedGoogle Scholar
  31. 31.
    Steen PA, Gisvold SE, Milde JH, Newberg LA, Scheithauer BW, Lanier WL, Michenfelder JD (1985) Nimodipine improves outcome when given after complete cerebral ischemia in primates. Anesthesiology 62:406–411PubMedCrossRefGoogle Scholar
  32. 32.
    Towart R (1981) The selective inhibition of serotonin-induced contractions of rabbit cerebral vascular smooth muscle by calcium-antagonistic dihydropyridines. An investigation of the mechanism of action of nimodipine. Circ Res 48:650–657PubMedGoogle Scholar
  33. 33.
    Young W, DeCrescito V (1989) Nimodipine reduces brain ionic and water shifts at 24 hours after MCAO. (in preparation)Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 1990

Authors and Affiliations

  • A. Scriabine
    • 1
  1. 1.Miles Institute for Preclinical PharmacologyWest HavenUSA

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