Cerebrospinal fluid and plasma concentrations of dipyrone metabolites after a single oral dose of dipyrone

1998 ◽  
Vol 54 (7) ◽  
pp. 549-553 ◽  
Author(s):  
O. Cohen ◽  
E. Zylber-Katz ◽  
Y. Caraco ◽  
L. Granit ◽  
M. Levy
1967 ◽  
Vol 5 (2) ◽  
pp. 6-7

Corticosteroids are well absorbed from the gut: plasma concentrations of prednisolone or hydrocortisone are at a maximum about 2 hours after a single oral dose.1 An intramuscular dose acts no more quickly. Intravenous corticosteroid acts at once and is required for severe acute adrenal failure, for example in the crises of Addison’s disease, after adrenalectomy, after sudden cessation of corticosteroid therapy and sometimes in severe hypopituitarism. A sudden increase in the requirement of patients who are taking or have taken corticosteroids may also demand intravenous therapy.


2019 ◽  
Vol 2019 ◽  
pp. 1-10
Author(s):  
Nathathai Temyingyong ◽  
Nut Koonrungsesomboon ◽  
Nutthiya Hanprasertpong ◽  
Mingkwan Na Takuathung ◽  
Supanimit Teekachunhatean

Soy isoflavones have several potential benefits related to postmenopausal health. Isoflavone glycosides, found predominantly in nonfermented soy products, e.g., soy milk, require conversion by gut microbiota to their respective bioavailable aglycones prior to absorption into portal circulation. Use of short-course oral ciprofloxacin for the treatment of acute uncomplicated cystitis, the incidence of which is increasing among postmenopausal women, might adversely affect gut microbiota. The objective of this one-group pre-post treatment study was to determine the effect of short-course oral ciprofloxacin on isoflavone pharmacokinetics in healthy postmenopausal women. Eleven postmenopausal subjects were assigned to consume a single oral dose of 375 mL UHT soy milk (SOY phase). Blood samples were collected immediately before soy milk ingestion and at specific times for 32 hours after soy milk ingestion. Following a washout period of at least seven days, subjects were assigned to take 250 mg oral ciprofloxacin after breakfast and dinner for three days, followed by a single oral dose of 375 mL UHT soy milk the next day (CIPRO/SOY phase). Blood samples were collected at the same time points as in the SOY phase. Plasma samples were treated withβ-glucuronidase/sulfatase and plasma concentrations of aglycones (genistein and daidzein) were determined using high-performance liquid chromatography.Cmax,AUC0-t, andAUC0-∞of both aglycones andTmaxof genistein obtained from the CIPRO/SOY phase were significantly lower than those obtained from the SOY phase, whileTmaxof daidzein and t1/2of both aglycones in the two phases were not significantly different.


Nutrients ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 2473 ◽  
Author(s):  
Hsien-Tsung Yao ◽  
Jia-Hsuan Lin ◽  
Yun-Ta Liu ◽  
Mei-Ling Li ◽  
Wenchang Chiang

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.


2009 ◽  
Vol 43 (5) ◽  
pp. 944-949 ◽  
Author(s):  
Lan Fan ◽  
Gong-You Tao ◽  
Guo Wang ◽  
Yao Chen ◽  
Wei Zhang ◽  
...  

Background Ginkgo biloba extract (GBE), the best selling herbal medicine in the world, has been reported to inhibit P-glycoprotein in vitro. However, the effects of GBE on P-glycoprotein activity in humans have not been clarified. Objective To investigate the effects of single and repeated GBE ingestion on the oral pharmacokinetics of talinolol, a substrate drug for P-glycoprotein in humans. Methods Ten unrelated healthy male volunteers were selected to participate in a 3-stage sequential study. Plasma concentrations of talinolol from 0 to 24 hours were measured by high-performance liquid chromatography after talinolol 100 mg was administrated alone, with a single oral dose of GBE (120 mg), and after 14 days of repeated GBE ingestion (360 mg/day). Results A single oral dose of GBE did not affect the pharmacokinetics of talinolol. Repeated ingestion of GBE increased the talinolol maximum plasma concentration (Cmax) by 36% (90% CI 10 to 68; p = 0.025), the area under the concentration-time curve (AUC)0-24 by 26% (90% CI 11 to 43; p = 0.008) and AUC0-∞ by 22% (90% CI 8 to 37; p = 0.014), respectively, without significant changes in elimination half-life and the time to Cmax. Conclusions Our results suggest that long-term use of GBE significantly influenced talinolol disposition in humans, likely by affecting the activity of P-glycoprotein and/or other drug transporters.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Jackelyn Murray ◽  
Robert J. Hogan ◽  
David E. Martin ◽  
Kathy Blahunka ◽  
Fred D. Sancilio ◽  
...  

AbstractEffective vaccines are slowing the COVID-19 pandemic, but SARS-CoV-2 will likely remain an issue in the future making it important to have therapeutics to treat patients. There are few options for treating patients with COVID-19. We show probenecid potently blocks SARS-CoV-2 replication in mammalian cells and virus replication in a hamster model. Furthermore, we demonstrate that plasma concentrations up to 50-fold higher than the protein binding adjusted IC90 value are achievable for 24 h following a single oral dose. These data support the potential clinical utility of probenecid to control SARS-CoV-2 infection in humans.


Xenobiotica ◽  
2001 ◽  
Vol 31 (12) ◽  
pp. 891-901 ◽  
Author(s):  
J. M. M. Van Amelsvoort ◽  
K. H. Van Het Hof ◽  
J. N. J. J. Mathot ◽  
T. P. J. Mulder ◽  
A. Wiersma ◽  
...  

2019 ◽  
Vol 63 (6) ◽  
Author(s):  
Amit V. Desai ◽  
David Han ◽  
Donna L. Kowalski ◽  
Christopher Lademacher ◽  
Helene Pearlman ◽  
...  

ABSTRACT This phase 1, open-label, single-dose, parallel-group study evaluated the pharmacokinetics (PK) of isavuconazole after a single oral dose of the prodrug isavuconazonium sulfate in healthy nonelderly (age, 18 to 45 years) and elderly (age, ≥65 years) males and females. Overall, 48 subjects were enrolled in the study (n = 12 each in groups of nonelderly males and females and elderly males and females). All subjects received a single oral dose of 372 mg of isavuconazonium sulfate (equivalent to 200 mg isavuconazole). PK samples were collected for analysis of isavuconazole plasma concentrations from the predose time point up to 336 h postdose. Data were analyzed using population pharmacokinetic (PPK) analysis. The resulting PPK model included two compartments with Weibull absorption function as well as interindividual variability with respect to clearance, intercompartment clearance, volumes of central and peripheral compartments, and two Weibull absorption parameters, RA and KAMAX. The PPK analysis showed that elderly females had the highest exposure versus males (ratio of total area under the time-concentration curve [AUC], 138; 90% confidence interval [CI], 118 to 161) and versus nonelderly females (ratio of AUC, 147; 90% CI, 123 to 176). Higher exposures in elderly females were not associated with significant toxicity or treatment-emergent adverse events, as measured in this study. No dose adjustments appear to be necessary based on either age group or sex even with an increase in exposure for elderly females. (This study has been registered at ClinicalTrials.gov under registration no. NCT01657890.)


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