Failure to detect amodiaquine in the blood after oral administration.

Salako, L.A.; Idowu, O A

doi:10.1111/j.1365-2125.1985.tb05068.x

Cited by 10 publications

(11 citation statements)

References 6 publications

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“…The drug became detectable at 0.25 h, and reached a peak concentration of 31.9 ± 3.1 ng ml[' (mean ± s.e. mean) at 0.5 ± 0.03 h. The mean apparent terminal half-life of AQ was 5.2 ± 1.7 h. Like Salako & Idowu (1985), we found much higher plasma concentrations of AQm than AQ. The peak AQm concentration was 181.4 ± 25.8 ng ml-, reached at 3.4 ± 0.8 h. Sampling continued until 96 h at which time no AQ was detectable, but the mean AQm concentration was 29.1 ± 8.4 ng m-1'.…”

supporting

confidence: 65%

“…We wish to reply to the recent publication by Salako & Idowu (1985) entitled Failure to detect amodiaquine in the blood after oral administration. We have reported a high performance liquid chromatographic method for the measurement of amodiaquine (AQ) in plasma.…”

mentioning

confidence: 99%

“…In addition, we have conducted a single dose study in seven healthy male Caucasians (aged 22-45 years) given 600 mg AQ orally after an overnight fast (Winstanley et al, 1986). In contrast to the findings of Salako & Idowu (1985), we were able to measure plasma concentrations of AQ for up to 8 h after dosing. The drug became detectable at 0.25 h, and reached a peak concentration of 31.9 ± 3.1 ng ml[' (mean ± s.e.…”

mentioning

confidence: 99%

“…Since Salako & Idowu (1985) sampled blood at 0.5, 0.75, 1, 1.5 h and thereafter, it is surprising that they did not detect AQ in plasma. This could be due to one or more of the following reasons:…”

mentioning

confidence: 99%

“…(c) The method described by Salako & Idowu (1985) is reminiscent of that of Churchill et al (1985), which uses no internal standard and therefore provides little safeguard against failure of extraction of the compounds, or an indication when this has occurred.…”

mentioning

confidence: 99%

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The detection of amodiaquine in blood after oral administration [letter]

Winstanley¹,

Edwards²,

Orme³

et al. 1986

Brit J Clinical Pharma

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supporting

confidence: 65%

mentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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The detection of amodiaquine in blood after oral administration [letter]

Winstanley¹,

Edwards²,

Orme³

et al. 1986

Brit J Clinical Pharma

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Antimalarial Agents

Casteel¹

2003

Burger's Medicinal Chemistry and Drug Discovery

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Malaria continues to be a major global health problem and seems to be increasing in some parts of the world. By way of an introduction, relevant aspects of the disease, including incidence and resistance, and of the parasite and its biochemistry and genetics are presented. The chemotherapeutic agents now available to prevent and treat malaria are discussed individually. Some of these drugs have been in use for decades or even centuries, such as quinine, chloroquine, and primaquine. Other agents are of more recent origin including mefloquine, halofantrine, atovaquone, and the artemisinins. Chloroquine had been the drug of first resort for many years. It is inexpensive, well‐tolerated, and extremely effective where parasites remain sensitive. But the development of resistance to chloroquine has emphasized the need for new agents and strategies to treat malaria. New information on the genetic basis of chloroquine resistance and on the overall mechanism of action of chloroquine holds promise for advances in therapy. Another important tactic in dealing with infection by resistant parasites is the use of drug combinations. The combination of pyrimethamine and sulfadoxine has been very successful, but resistance is developing. Newer, highly effective combinations include atovaquone with proguanil, lumefantrine with artemether, and chlorproguanil with dapsone. The artemisinin group of compounds has made a powerful positive impact on malaria chemotherapy although their use in monotherapy is not recommended. Details of the mechanism of action of these drugs are becoming clearer. Knowledge about action should assist in addressing issues of possible toxicity. Great progress has been made in sequencing the genome of Plasmodium falciparum . New molecular targets have been identified as a result and efforts are underway to develop antimalarial agents based on these targets. Researchers around the world are also exploring natural products for yet another lead in antimalarial chemotherapy. “If we take as our standard of importance the greatest harm to the greatest number, then there is no question that malaria is the most important of all infectious diseases 1 .” “Ah, poor heart! he is so shaked of a burning quotidian tertian, that it is most lamentable to behold [2].”

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Disposition of monodesethylamodiaquine after a single oral dose of amodiaquine and three regimens for prophylaxis againstPlasmodium falciparum malaria

Pussard

Verdier

Faurisson

et al. 1987

Eur J Clin Pharmacol

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The disposition of monodesethylamodiaquine was studied in four healthy subjects after a single oral dose of 10 mg/kg amodiaquine base. Amodiaquine was not found in any sample, but the major metabolite monodesethylamodiaquine was detected and was assumed to be the sole derivative that contributed significantly to antimalarial activity in the blood. The best fit for the decay of the metabolite was obtained with a three-compartment model. The half-lives of the first two phases were 3.2 to 11.4 h for t1/2 alpha 1 and 22.7 to 50.3 h for t1/2 alpha 2 in plasma. The half-life of the terminal phase (t1/2 beta) was between 9 and 18.2 days. The concentration in whole blood was 4- to 6-times higher than in plasma. Three schedules (alternate days, weekly, daily) of the conventional prophylactic dose of 10 mg/kg per week were compared in six other healthy subjects. There were significant differences in the plasma monodesethylamodiaquine levels between the three schedules.

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Failure to detect amodiaquine in the blood after oral administration.

Cited by 10 publications

References 6 publications

The detection of amodiaquine in blood after oral administration [letter]

The detection of amodiaquine in blood after oral administration [letter]

Antimalarial Agents

Disposition of monodesethylamodiaquine after a single oral dose of amodiaquine and three regimens for prophylaxis againstPlasmodium falciparum malaria

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