Prophylaxis of Plasmodium falciparumInfection in a Human Challenge Model with WR 238605, a New 8-Aminoquinoline Antimalarial

ABSTRACT The prophylactic efficacy of WR 238605, a primaquine analog, was studied with a human Plasmodium falciparum challenge model. A single oral dose of 600 mg, administered 1 day prior to challenge, successfully protected three of four subjects. The fourth subject developed mild, oligosymptomatic malaria on day 31, with drug concentrations one-half of those in the protected individuals. WR 238605 appears to be a promising prophylactic drug for P. falciparum malaria.

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Food–Drug Interaction between the Adlay Bran Oil and Drugs in Rats

Nutrients ◽

10.3390/nu11102473 ◽

2019 ◽

Vol 11 (10) ◽

pp. 2473 ◽

Cited By ~ 2

Author(s):

Hsien-Tsung Yao ◽

Jia-Hsuan Lin ◽

Yun-Ta Liu ◽

Mei-Ling Li ◽

Wenchang Chiang

Keyword(s):

Oral Dose ◽

Drug Interactions ◽

Single Oral Dose ◽

Plasma Concentrations ◽

Oral Drug ◽

Drug Cocktail ◽

Intestinal Drug Absorption ◽

Drug Concentrations ◽

Plasma Theophylline ◽

Term Administration

Adlay (Coix lachryma-jobi L. var. ma-yuen Stapf) contains various phytonutrients for treating many diseases in Asia. To investigate whether orally administered adlay bran oil (ABO) can cause drug interactions, the effects of ABO on the pharmacokinetics of five cytochrome P450 (CYP) probe drugs were evaluated. Rats were given a single oral dose (2.5 mL/kg BW) of ABO 1 h before administration of a drug cocktail either orally or intravenously, and blood was collected at various time points. A single oral dose of ABO administration did not affect the pharmacokinetics of five probe drugs when given as a drug cocktail intravenously. However, ABO increased plasma theophylline (+28.4%), dextromethorphan (+48.7%), and diltiazem (+46.7%) when co-administered an oral drug cocktail. After 7 days of feeding with an ABO-containing diet, plasma concentrations of theophylline (+45.4%) and chlorzoxazone (+53.6%) were increased after the oral administration of the drug cocktail. The major CYP enzyme activities in the liver and intestinal tract were not affected by ABO treatment. Results from this study indicate that a single oral dose or short-term administration of ABO may increase plasma drug concentrations when ABO is given concomitantly with drugs. ABO is likely to enhance intestinal drug absorption. Therefore, caution is needed to avoid food–drug interactions between ABO and co-administered drugs.

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Randomized Controlled Trial of Fosmidomycin-Clindamycin versus Sulfadoxine-Pyrimethamine in the Treatment of Plasmodium falciparum Malaria

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.01448-06 ◽

2007 ◽

Vol 51 (5) ◽

pp. 1869-1871 ◽

Cited By ~ 49

Author(s):

Sunny Oyakhirome ◽

Saadou Issifou ◽

Peter Pongratz ◽

Fortune Barondi ◽

Michael Ramharter ◽

...

Keyword(s):

Randomized Controlled Trial ◽

Plasmodium Falciparum ◽

Oral Dose ◽

Randomized Trial ◽

Single Oral Dose ◽

Uncomplicated Malaria ◽

Controlled Trial ◽

Plasmodium Falciparum Malaria ◽

Randomized Controlled ◽

High Degree

ABSTRACT Fosmidomycin-clindamycin therapy given every 12 h for 3 days was compared with a standard single oral dose of sulfadoxine-pyrimethamine. The two treatments showed comparably good tolerabilities and had an identical high degree of efficacy of 94% in a randomized trial carried out with 105 Gabonese children aged 3 to 14 years with uncomplicated malaria. These antimalarials merit further clinical exploration.

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Pharmacokinetics of gatifloxacin after a single oral dose in healthy young adult subjects and adult patients with chronic bronchitis, with a comparison of drug concentrations obtained by bronchoscopic microsampling and bronchoalveolar lavage

Clinical Therapeutics ◽

10.1016/j.clinthera.2007.01.005 ◽

2007 ◽

Vol 29 (1) ◽

pp. 123-130 ◽

Cited By ~ 15

Author(s):

Junko Kikuchi ◽

Koichi Yamazaki ◽

Eiki Kikuchi ◽

Akitoshi Ishizaka ◽

Masaharu Nishimura

Keyword(s):

Young Adult ◽

Oral Dose ◽

Bronchoalveolar Lavage ◽

Single Oral Dose ◽

Chronic Bronchitis ◽

Adult Patients ◽

Healthy Young Adult ◽

Drug Concentrations ◽

Bronchoscopic Microsampling

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Measurement of clomipramine, N-desmethyl-clomipramine, imipramine, and dehydroimipramine in biological fluids by selective ion monitoring, and pharmacokinetics of clomipramine.

Clinical Chemistry ◽

10.1093/clinchem/22.6.892 ◽

1976 ◽

Vol 22 (6) ◽

pp. 892-897 ◽

Cited By ~ 24

Author(s):

J P Dubois ◽

W Küng ◽

W Theobald ◽

B Wirz

Keyword(s):

Oral Dose ◽

Single Oral Dose ◽

Whole Blood ◽

Biological Fluids ◽

Tricyclic Antidepressant ◽

Renal Elimination ◽

Drug Concentrations ◽

Selective Ion Monitoring ◽

Spectrometer System

Abstract To quantitatively determine tricyclic antidepressant agents, we used a combined gas chromatograph/mass spectrometer system, and deuterium-labeled internal standards. Recovery exceeds 95% and the coefficient of variation is less than 4% for human whole-blood samples supplemented with 5 to 15 ng of clomipramine hydrochloride or 20 to 60 ng of dehydroimipramine hydrogen fumarate per milliliter. For both amines, the detection limit is 0.3 mug/liter; Six healthy volunteers who received a single oral dose of 50 mg of clomipramine hydrochloride showed peak drug concentrations in the blood 3 to 5 h after administration, ranging between 14.4 and 30.1 mug/liter. Plasma/whole blood concentration ratios varied from 0.70 to 1.20, and the cumulative renal elimination from 0 to 72 h is less than 0.2% of the dose. This method is suitable for in vivo bioavailability studies of unchanged clomipramine, dehydroimipramine, and imipramine after a single oral dose of as little as 25 mg.

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Pharmacokinetic Interactions between Primaquine and Pyronaridine-Artesunate in Healthy Adult Thai Subjects

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.03829-14 ◽

2014 ◽

Vol 59 (1) ◽

pp. 505-513 ◽

Cited By ~ 27

Author(s):

Podjanee Jittamala ◽

Sasithon Pukrittayakamee ◽

Elizabeth A. Ashley ◽

François Nosten ◽

Borimas Hanboonkunupakarn ◽

...

Keyword(s):

Oral Dose ◽

Single Oral Dose ◽

Geometric Mean ◽

Maximum Plasma ◽

Geometric Mean Ratio ◽

Pharmacokinetic Interactions ◽

Drug Concentrations ◽

Pharmacokinetic Properties ◽

To Receive ◽

Noncompartmental Approach

ABSTRACTPyronaridine-artesunate is a newly introduced artemisinin-based combination treatment which may be deployed together with primaquine. A single-dose, randomized, three-sequence crossover study was conducted in healthy Thai volunteers to characterize potential pharmacokinetic interactions between these drugs. Seventeen healthy adults received a single oral dose of primaquine alone (30 mg base) and were then randomized to receive pyronaridine-artesunate alone (540−180 mg) or pyronaridine-artesunate plus primaquine in combination, with intervening washout periods between all treatments. The pharmacokinetic properties of primaquine, its metabolite carboxyprimaquine, artesunate, its metabolite dihydroartemisinin, and pyronaridine were assessed in 15 subjects using a noncompartmental approach followed by a bioequivalence evaluation. All drugs were well tolerated. The single oral dose of primaquine did not result in any clinically relevant pharmacokinetic alterations to pyronaridine, artesunate, or dihydroartemisinin exposures. There were significantly higher primaquine maximum plasma drug concentrations (geometric mean ratio, 30%; 90% confidence interval [CI], 17% to 46%) and total exposures (15%; 6.4% to 24%) during coadministration with pyronaridine-artesunate than when primaquine was given alone. Pyronaridine, like chloroquine and piperaquine, increases plasma primaquine concentrations. (This study has been registered at ClinicalTrials.gov under registration no. NCT01552330.)

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Antimalarial Iron Chelator, FBS0701, Shows Asexual and Gametocyte Plasmodium falciparum Activity and Single Oral Dose Cure in a Murine Malaria Model

PLoS ONE ◽

10.1371/journal.pone.0037171 ◽

2012 ◽

Vol 7 (5) ◽

pp. e37171 ◽

Cited By ~ 25

Author(s):

Patricia Ferrer ◽

Abhai K. Tripathi ◽

Martha A. Clark ◽

Carla Cerami Hand ◽

Hugh Young Rienhoff ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Oral Dose ◽

Single Oral Dose ◽

Iron Chelator ◽

Malaria Model

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Evaluation of Artemisone Combinations in Aotus Monkeys Infected with Plasmodium falciparum

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00471-09 ◽

2009 ◽

Vol 53 (8) ◽

pp. 3592-3594 ◽

Cited By ~ 18

Author(s):

Nicanor Obaldia ◽

Barbara M. Kotecka ◽

Michael D. Edstein ◽

Richard K. Haynes ◽

Burkhard Fugmann ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Body Weight ◽

Oral Dose ◽

Single Oral Dose

ABSTRACT Artemisone (single oral dose, 10 mg/kg of body weight) cured nonimmune Aotus monkeys of their Plasmodium falciparum infections when combined with mefloquine (single oral dose, 5 and 10 mg/kg but not 2.5 mg/kg). In combination with amodiaquine (20 mg/kg/day), artemisone (10 mg/kg/day) given orally for 3 days cured all infected monkeys. Three days of treatment with artemisone (30 mg/kg/day) and clindamycin (100 mg/kg/day) was also curative.

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A Rapid (48 hours) Thyroid Suppression Test using a Single Oral Dose of 100 of Triiodothyronine

Nuklearmedizin ◽

10.1055/s-0038-1624823 ◽

1973 ◽

Vol 12 (03) ◽

pp. 218-224

Author(s):

Elli Lakka - Papadodima ◽

Constantin Ntalles ◽

Denis Ikkos

Keyword(s):

Oral Dose ◽

Single Oral Dose ◽

Suppression Test

Des mesurages répétés de la fixation thyroïdienne de 10 minutes du 132I injecté intraveineusement on été effectués sur 55 malades euthyroïdiens sans et avec goitre et sur 16 malades hyperthyreoïdiens par 4 jours consécutifs. Immédiatement après le premier mesurage tous les malades recevaient une dose unique oral de 100 μg de Triiodothyronine (T3). Les valeurs de fixation 24, 48 et 72 heures après le T3 (moyen ± déviation standard) étaient de 75 ± 1,7, 64 ± 1,8, et 67 ± 1,9 dans le groupe euthyroïdien et le 106 ± 2,6, 104 ± 2,2 et 108 ± 4,0 dans le groupe hyperthyroïdien, exprimés en pourcentage du groupe controle. 48 heures après T3 tous les personnes euthyroïdiens, sauf une, avaient des valeurs en dessous de 88% tandis que la valeur la plus basse des personnes hyperthyroïdiens ce jour était de 93%. La séparation des valeurs 48 heures des deux groupes était complète après avoir respecté l’influence de la première fixation sur la valeur 48 heures. On peut donc supposer q’un test thyroïdien de suppression utilisable en clinique peut-être effectué en 48 heures après une administration oral de 100 μg de T3 et mesurage de la fixation 10 minutes après l’injection du radioisotope.

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Effect of Aspirin on the Thrombelastogram of Human Blood

Thrombosis and Haemostasis ◽

10.1055/s-0038-1649127 ◽

1973 ◽

Vol 30 (03) ◽

pp. 494-498 ◽

Cited By ~ 1

Author(s):

G de Gaetano ◽

J Vermylen

Keyword(s):

Oral Dose ◽

Single Oral Dose ◽

Platelet Function ◽

Human Blood ◽

Platelet Rich Plasma ◽

Plasma Samples ◽

Release Reaction ◽

Platelet Release

SummaryThrombelastograms of both native blood and re-calcified platelet-rich plasma samples taken from subjects given a single oral dose of aspirin (1 gram) were not significantly different from the pretreatment recordings. Aspirin also did not modify the thrombelastogram when preincubated in vitro with platelet-rich plasma at concentrations inhibiting the platelet “release reaction” by collagen. Thrombelastography therefore cannot evaluate the effect of aspirin on platelet function.

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