scholarly journals On Quantitative Relationships Between Drug-Like Compound Lipophilicity and Plasma Free Fraction in Monkey and Human

2012 ◽  
Vol 101 (3) ◽  
pp. 1028-1039 ◽  
Author(s):  
Sami S. Zoghbi ◽  
Kacey B. Anderson ◽  
Kimberly J. Jenko ◽  
David A. Luckenbaugh ◽  
Robert B. Innis ◽  
...  
Keyword(s):  
Free Fraction ◽  
Plasma Free Fraction

Functional change of the auditory cortex related to brain serotonergic neurotransmission in type 1 diabetic adolescents with and without depression

2011 ◽  
Vol 26 (S2) ◽  
pp. 323-323
Author(s):  
G. Manjarrez ◽  
R. Herrera ◽  
J. Manjarrez ◽  
S. Mejenes ◽  
J. Hernandez-R
Keyword(s):  
Auditory Cortex ◽  
Auditory Evoked Potentials ◽  
Free Fraction ◽  
Functional Change ◽  
Diabetic Patients ◽  
Serotonergic Activity ◽  
Serotonergic Neurotransmission ◽  
Poor Treatment ◽  
Plasma Free Fraction

ObjectiveThe aim of this study was to determine whether diabetic patients who were depressed present a decrease of brain serotonergic activity compared to diabetic patients without depression or patients with depression but without diabetes. Determination was made with plasma free fraction of l-tryptophan (FFT) and intensity-dependent auditory-evoked potentials (IDAEPs).MethodsThirty seven adolescents were studied (20 type 1 diabetic subjects: 9 with depression, 11 without depression), 9 controls and 8 subjects with only depression. FFT, glucose, glycated hemoglobin, free fatty acids, albumin and IDAEPs were determined.ResultAll diabetic patients showed a significant decrease of FFT. The group diabetic subjects with depression presented a steeper slope of the amplitude-intensity function of N1/P2 component, suggesting a higher reactivity of the auditory cortex in comparison to diabetic subjects without depression, subjects with only depression, and controls. This was associated with lower plasma FFT. Diabetic subjects with depression had a deficiency of metabolic control due to poor treatment adherence.ConclusionsThese findings suggest an enhanced deterioration of brain serotonergic neurotransmission in diabetic subjects with depression with abnormal responses of the auditory cortex. The N1/P2 component of IDAEP is proposed as a noninvasive indicator of brain serotonergic tone that differentiates depressed from nondepressed diabetic patients.

On the quantitative relationship between radiotracer lipophilicity and plasma free fraction

NeuroImage ◽  
2010 ◽  
Vol 52 ◽  
pp. S221 ◽  
Author(s):  
Sami S. Zoghbi ◽  
Kacey B. Anderson ◽  
Kimberley J. Jenko ◽  
Robert B. Innis ◽  
Victor W. Pike
Keyword(s):  
Quantitative Relationship ◽  
Free Fraction ◽  
Plasma Free Fraction

scholarly journals Low Frequency of Intermittent HIV-1 Semen Excretion in Patients Treated with Darunavir-Ritonavir at 600/100 Milligrams Twice a Day plus Two Nucleoside Reverse Transcriptase Inhibitors or Monotherapy

2010 ◽  
Vol 54 (11) ◽  
pp. 4910-4913 ◽  
Author(s):  
Sidonie Lambert-Niclot ◽  
Gilles Peytavin ◽  
Claudine Duvivier ◽  
Catherine Poirot ◽  
Michèle Algarte-Genin ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Genital Tract ◽  
Low Frequency ◽  
Free Fraction ◽  
Male Genital Tract ◽  
Reverse Transcriptase Inhibitors ◽  
Good Penetration ◽  
Plasma Free Fraction ◽  
Hiv 1 ◽  
Male Genital

ABSTRACT HIV-1 RNA level and darunavir concentration in the genital tract were measured in 45 men receiving darunavir-ritonavir mono- or tritherapy. At week 48, a low frequency (3/45) of HIV-1 RNA shedding was observed in patients (1 on monotherapy and 2 on triple therapy), although they had undetectable HIV-1 RNA in plasma. The median darunavir seminal plasma concentration was close to the blood plasma free fraction, demonstrating a good penetration of darunavir into the male genital tract.

scholarly journals Standards of laboratory practice: cardiac drug monitoring

1998 ◽  
Vol 44 (5) ◽  
pp. 1096-1109 ◽  
Author(s):  
Roland Valdes ◽  
Saeed A Jortani ◽  
Mihai Gheorghiade
Keyword(s):  
Heart Failure ◽  
Congestive Heart Failure ◽  
Drug Monitoring ◽  
Free Fraction ◽  
Therapeutic Index ◽  
Therapeutic Monitoring ◽  
Therapeutic Drug ◽  
Laboratory Practice ◽  
Clinical Complications ◽  
The Impact

Abstract In this Standard of Laboratory Practice we recommend guidelines for therapeutic monitoring of cardiac drugs. Cardiac drugs are primarily used for treatment of angina, arrhythmias, and congestive heart failure. Digoxin, used in congestive heart failure, is widely prescribed and therapeutically monitored. Monitoring and use of antiarrhythmics such as disopyramide and lidocaine have been steadily declining. Immunoassay techniques are currently the most popular methods for measuring cardiac drugs. Several reasons make measurement of cardiac drugs in serum important: their narrow therapeutic index, similarity in clinical complications and presentation of under- and overmedicated patients, need for dosage adjustments, and confirmation of patient compliance. Monitoring may also be necessary in other circumstances, such as assessment of acetylator phenotypes. We present recommendations for measuring digoxin, quinidine, procainamide (and N-acetylprocainamide), lidocaine, and flecainide. We discuss guidelines for measuring unbound digoxin in the presence of an antidote (Fab fragments), for characterizing the impact of digoxin-like immunoreactive factor (DLIF) and other cross-reactants on immunoassays, and for monitoring the unbound (free fraction) of drugs that bind to α1-acid glycoprotein. We also discuss logistic, clinical, hospital, and laboratory practice guidelines needed for implementation of a successful therapeutic drug monitoring service for cardiac drugs.

The relevance of therapeutic drug monitoring in plasma and erythrocytes in anti-cancer drug treatment

2004 ◽  
Vol 42 (11) ◽  
Author(s):  
Herlinde Dumez ◽  
Gunther Guetens ◽  
Gert De Boeck ◽  
Martin S. Highley ◽  
Robert A. A. Maes ◽  
...  
Keyword(s):  
Therapeutic Drug Monitoring ◽  
Drug Monitoring ◽  
Drug Transport ◽  
Free Fraction ◽  
The Body ◽  
Cancer Drug ◽  
Therapeutic Drug ◽  
Anti Cancer ◽  
Plasma Compartment ◽  
Made In

AbstractTherapeutic drug monitoring generally focuses on the plasma compartment only. Differentiation between the total plasma concentration and the free fraction (plasma water) has been described for a number of limited drugs. Besides the plasma compartment, blood has also a cellular fraction which has by far the largest theoretical surface and volume for drug transport. It is with anti-cancer drugs that major progress has been made in the study of partition between the largest cellular blood compartment, i.e., erythrocytes, and the plasma compartment. The aim of the present review is to detail the progress made in predicting what a drug does in the body, i.e., pharmacodynamics including toxicity and plasma and/or red blood cell concentration monitoring. Furthermore, techniques generally used in anti-cancer drug monitoring are highlighted. Data for complex Bayesian statistical approaches and population kinetics studies are beyond the scope of this review, since this is generally limited to the plasma compartment only.

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