Chloroquine serum concentration and side effects: Evidence for dose‐dependent kinetics

Frisk-Holmberg, M; Bergkvist, Yngve; Domeij-Nyberg, B; Hellström, Laila; Jansson, Folke

doi:10.1002/cpt1979253345

Cited by 128 publications

(51 citation statements)

References 2 publications

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“…Symptoms were present when blood concentrations were high and disappeared when the blood concentrations fell below 4 ,u mol/l. This is in agreement with our previous report (Frisk-Holmberg et al, 1979). Above serum concentrations of 2.5 umol/l 80% of chronically treated patients experienced side effects but below 1.3 ,Lmol/l no side effects were demonstrated.…”

Section: Case Reportsupporting

confidence: 94%

“…Chloroquine on the other hand was eliminated at a rate almost six times slower than reported previously (Frisk-Holmberg et al, 1979;McChesney et al, 1967). This could be of practical importance in the Sodium valproate (VPA), a broad spectrum antiepileptic drug, is now widely used in the treatment of epilepsy.…”

Section: Case Reportmentioning

confidence: 48%

“…During the treatment of rheumatoid diseases most side effects are reversible but occur frequently and are related to the blood concentration of the drug (Frisk-Holmberg et al, 1979). Irreversible side effects occur when higher total doses are given.…”

Section: Chloroquine Intoxicationmentioning

confidence: 99%

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Chloroquine intoxication [letter]

Frisk-Holmberg¹,

Bergqvist²,

Englund³

1983

Brit J Clinical Pharma

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Section: Case Reportsupporting

confidence: 94%

Section: Case Reportmentioning

confidence: 48%

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Chloroquine intoxication [letter]

Frisk-Holmberg¹,

Bergqvist²,

Englund³

1983

Brit J Clinical Pharma

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“…A multiexponential concentration-time curve is therefore obtained if the plasma concentration is followed long enough thus giving higher values for the terminal half-life (Frisk-Holmberg et al, 1979;Gustafsson etal., 1983).…”

Section: Discussionmentioning

confidence: 99%

Plasma chloroquine and desethylchloroquine concentrations in children during and after chloroquine treatment for malaria.

Walker¹,

Dawodu²,

Adeyokunnu³

et al. 1983

Brit J Clinical Pharma

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1 Twelve children with acute falciparum malaria were treated with 25 mg/kg chloroquine orally in three divided doses at 24 h intervals. 2 Concentrations of chloroquine and its metabolite, desethylchloroquine, were measured in plasma from the beginning of treatment for up to 7 days using a high pressure liquid chromatography (h.p.l.c.) technique. 3 Chloroquine was detectable in plasma within 30 min of giving the drug. Peak level was reached in 1-8 h after the first dose of 10 mg/kg and the peak concentrations ranged between 65 and 263 ng/ml. 4 Chloroquine concentration declined slowly in plasma after stopping drug administration so that the concentration at the seventh day was 37.5% of the concentration on the third day. The apparent half-life was 3-4 days. 5 Desethylchloroquine was detectable in plasma within 30 min of giving chloroquine and peak levels were reached in 2-12 h. Peak concentration after the first dose of chloroquine ranged between 9 and 62 ng/ml. 6 Desethylchloroquine was also slowly cleared from plasma and mean concentration at the end of 7 days was 49% of the mean concentration at the end of 3 days.

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“…It is difficult to make direct comparisons between blood and plasma concentrations, especially in acute dosage, but an estimate would put the blood concentration as being [4][5][6][7][8] times the plasma concentration.5 Such an estimate would make this the highest ever recorded concentration of chloroquine in a surviving overdose patient. It is certainly the highest recorded concentration in the United Kingdom.…”

Section: Discussionmentioning

confidence: 99%