Antimalarial primaquine for spinal sensory and motor blockade in rats

J Pharm Pharmacol. 2021 Oct 7;73(11):1513-1519. doi: 10.1093/jpp/rgab054.

Abstract

Objectives: The purpose of the experiment was to estimate whether intrathecal antimalarial drugs could provoke spinal block, and their comparison with lidocaine.

Methods: Rats were intrathecally administrated with antimalarial agents (primaquine, chloroquine, hydroxychloroquine and amodiaquine) and lidocaine, and neurobehavioural examinations (nociception, proprioception and motor function) were assessed; n = 8 per group. One-way and two-way analysis of variance were designed to analyse data.

Key findings: At a concentration of 20 mM, primaquine (0.46 mg/rat) exhibited the longest duration and the most potent effect of nociceptive, proprioceptive and motor blockade (P < 0.01) among five drugs, whereas the other antimalarial drugs displayed a lesser or similar potency of spinal blockade compared with lidocaine (0.29 mg/rat). In dose-dependent studies, primaquine was more potent (P < 0.01) than lidocaine for spinal block. At ED25, ED50 and ED75 equipotent doses, primaquine produced a greater duration of spinal motor, proprioceptive and nociceptive blockade when compared with lidocaine (P < 0.01).

Conclusions: Primaquine, chloroquine, hydroxychloroquine and amodiaquine produced spinal blockade. Primaquine was more potent and displayed a prolonged life of local anaesthetic effect compared with lidocaine, whereas the other antimalarial drugs displayed a lesser or similar potency compared with lidocaine.

Keywords: antimalarial medications; lidocaine; motor function; nociception; primaquine; spinal block.

MeSH terms

  • Aminoquinolines / pharmacology
  • Anesthesia, Spinal / methods*
  • Anesthetics, Local / pharmacology*
  • Animals
  • Antimalarials / pharmacology*
  • Dose-Response Relationship, Drug
  • Injections, Spinal
  • Lidocaine / pharmacology
  • Male
  • Motor Activity / drug effects*
  • Nerve Block / methods
  • Nociception / drug effects*
  • Primaquine / pharmacology*
  • Proprioception / drug effects*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Aminoquinolines
  • Anesthetics, Local
  • Antimalarials
  • Lidocaine
  • Primaquine

Grants and funding