[Ca++ ion transport blockers as reversants of the drug resistance of malarial parasites. 1. The effect of verapamil on the resistance to chloroquine in vivo of Plasmodium berghei and in vitro of Plasmodium falciparum].
The reversing action of verapamil on the effect of chloroquine was found in in vivo experiments by using a model P. berghei resistant to chloroquine, an LNK65 isolate having a naturally lower resistance to the agent, and its polyresistant strain with the acquired resistance to chloroquine and fansidar, as well as by employing the chlorine-resistant P. falciparum isolates from the south of the Socialist Republic of Vietnam. The magnitude of this effect was related to the dose of verapamil, the frequency of administration of a combination of the agents in vivo, while that was associated to the concentration of verapamil and the level of isolate resistance to chloroquine in vitro which was the most pronounced. Taking into account the dose-dependent effect of verapamil, it can be suggested that increasing its concentration in combination with chloroquine can provide a more marked reversing action with lower chloroquine concentrations. The parameters accepted by the authors in evaluating the combined effect enable the effect of the verapamil/chloroquine concentration to be regarded as potentiation.
Rabinovich
S A
SA
Orlov
V S
VS
Dadasheva
N R
NR
Bukhtin
B A
BA
Maksakovskaia
E V
EV
Shcherbakov
A M
AM
Nguyen
V K
VK
Nguyen
D S
DS
Vu
T T
TT
D000818:Animals; D000962:Antimalarials / Q000037:antagonists & inhibitors* / Q000627:therapeutic use; D002121:Calcium Channel Blockers / Q000494:pharmacology* / Q000627:therapeutic use; D002738:Chloroquine / Q000037:antagonists & inhibitors* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004347:Drug Interactions; D004351:Drug Resistance; D004359:Drug Therapy, Combination; D006801:Humans; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D016778:Malaria, Falciparum / Q000469:parasitology; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects* / Q000302:isolation & purification; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000302:isolation & purification; D014700:Verapamil / Q000494:pharmacology* / Q000627:therapeutic use
D000962:Antimalarials; D002121:Calcium Channel Blockers; D002738:Chloroquine; D014700:Verapamil
Blokatory transporta ionov Ca++, kak reversanty lekarstvennoĭ ustoĭchivosti maliariĭnykh parazitov. Soobshchenie 1. Vliianie verapamila na ustoĭchivost' k khlorokhinu in vivo u Plasmodium berghei i in vitro u Plasmodium falciparum.