D2 receptor blockade by flunarizine and cinnarizine explains extrapyramidal side effects. A SPECT study

J Cereb Blood Flow Metab. 1995 May;15(3):513-8. doi: 10.1038/jcbfm.1995.63.

Abstract

Twenty-six patients under treatment with the calcium channel blockers flunarizine (Fz) or cinnarizine (Cz) were examined-with single-photon emission computed tomography using [123I]iodobenzamide as a ligand. The striatal dopamine D2 receptor-binding potential was determined and found to be reduced by 14 to 63% (39.5 +/- 15.0%; p < 0.0001) in patients compared with age-matched control values. This reduction was larger in 12 patients with extrapyramidal symptoms and was only slowly reversible after discontinuation of treatment. Patients treated for > 6 months had significantly larger reductions than patients treated for a shorter period. Parkinsonian symptoms were only seen in patients older than 50 years. Our findings prove a neuroleptic-like action of Fz and Cz, which seems to be the major reason for their extrapyramidal side effects. Older age and long-term treatment are predisposing factors for these effects.

MeSH terms

  • Adult
  • Aged
  • Brain Diseases / drug therapy
  • Brain Diseases / metabolism
  • Cinnarizine / adverse effects*
  • Cinnarizine / therapeutic use
  • Dopamine D2 Receptor Antagonists*
  • Female
  • Flunarizine / adverse effects*
  • Flunarizine / therapeutic use
  • Humans
  • Male
  • Middle Aged
  • Parkinson Disease / drug therapy
  • Parkinson Disease / metabolism
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Dopamine D2 Receptor Antagonists
  • Cinnarizine
  • Flunarizine