scholarly journals Granisetron Transdermal System in the Management of Chemotherapy-Induced Nausea and Vomiting

2016 ◽  
Vol 8 ◽  
pp. CMT.S10240 ◽  
Author(s):  
Hiromitsu Kitayama
Keyword(s):  
Population Analysis ◽  
Pharmacokinetic Profile ◽  
Average Concentration ◽  
Benign Disease ◽  
Receptor Antagonists ◽  
Oral Formulations ◽  
Maximal Plasma ◽  
The One ◽  
Transdermal Granisetron ◽  
Type 3

Serotonin-type 3 receptor antagonists have been available as intravenous and oral formulations. Recently, granisetron transdermal system has won a firm position in the antiemesis of cancer chemotherapy. Its pharmacokinetic profile has been shown by pooled population analysis incorporation data. The 52 cm2 patch, which contains 34.3 mg granisetron, releases 3.3 mg daily and reaches the maximal plasma concentration after 48 hours, maintaining a 2.2 ng/mL stable average concentration over six days. This level is similar to the one obtained with daily oral 2 mg of granisetron. Three randomized clinical studies evaluating its efficacy have been published. Transdermal granisetron showed noninferiority to other formulations of serotonin-type 3 receptor antagonists for highly and moderately emetogenic – including multiday – chemotherapy. The adverse effects were not significantly different from other formulations. The system has possible applications in oral chemotherapy, radiotherapy, dexamethasone sparing, palliative care, and refractory emesis due to benign disease.

scholarly journals Review of Pharmacokinetics and Pharmacogenetics in Atypical Long-Acting Injectable Antipsychotics

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 935
Author(s):  
Francisco José Toja-Camba ◽  
Nerea Gesto-Antelo ◽  
Olalla Maroñas ◽  
Eduardo Echarri Arrieta ◽  
Irene Zarra-Ferro ◽  
...  
Keyword(s):  
Plasma Concentrations ◽  
Pharmacokinetic Profile ◽  
Therapeutic Drug ◽  
Population Pharmacokinetic ◽  
Antipsychotic Therapy ◽  
Oral Formulations ◽  
Risk Balance ◽  
The One ◽  
Long Acting

Over the last two decades, pharmacogenetics and pharmacokinetics have been increasingly used in clinical practice in Psychiatry due to the high variability regarding response and side effects of antipsychotic drugs. Specifically, long-acting injectable (LAI) antipsychotics have different pharmacokinetic profile than oral formulations due to their sustained release characteristics. In addition, most of these drugs are metabolized by CYP2D6, whose interindividual genetic variability results in different metabolizer status and, consequently, into different plasma concentrations of the drugs. In this context, there is consistent evidence which supports the use of therapeutic drug monitoring (TDM) along with pharmacogenetic tests to improve safety and efficacy of antipsychotic pharmacotherapy. This comprehensive review aims to compile all the available pharmacokinetic and pharmacogenetic data regarding the three major LAI atypical antipsychotics: risperidone, paliperidone and aripiprazole. On the one hand, CYP2D6 metabolizer status influences the pharmacokinetics of LAI aripiprazole, but this relation remains a matter of debate for LAI risperidone and LAI paliperidone. On the other hand, developed population pharmacokinetic (popPK) models showed the influence of body weight or administration site on the pharmacokinetics of these LAI antipsychotics. The combination of pharmacogenetics and pharmacokinetics (including popPK models) leads to a personalized antipsychotic therapy. In this sense, the optimization of these treatments improves the benefit–risk balance and, consequently, patients’ quality of life.

Spacer conformation in biologically active molecules

2004 ◽  
Vol 76 (5) ◽  
pp. 959-964 ◽  
Author(s):  
J. Karolak-Wojciechowska ◽  
A. Fruzinski
Keyword(s):  
Statistical Data ◽  
Population Analysis ◽  
Cambridge Structural Database ◽  
Biologically Active ◽  
Aliphatic Chain ◽  
X Ray ◽  
Flexible Spacer ◽  
Conformational Preferences ◽  
Structural Database ◽  
The One

Based on our contemporary studies on the structures of biologically active molecules, we focus our attention on the aliphatic chain and its conformation. That flexible spacer definitely influenced the balanced position of all pharmacophoric points in molecules of biological ligands. The one atomic linker and two or three atomic spacers with one heteroatom X =O, S, CH2, NH have been taken into account. The conformational preferences clearly depend on the heteroatom X. In the discussion, we utilize our own X-ray data, computation chemistry methods, population analysis, and statistical data from the Cambridge Structural Database (CSD).

Rapid rituximab infusion is safe and well tolerated in malignant and benign disease

2020 ◽  
pp. 107815522097845
Author(s):  
Sorana G Ursu ◽  
Derek L Rinchuse ◽  
John Lister
Keyword(s):  
Medical Records ◽  
Malignant Disease ◽  
Benign Disease ◽  
P Value ◽  
Infusion Time ◽  
Benign Diseases ◽  
Secondary Objective ◽  
The Mean ◽  
The One ◽  
Related Reaction

Introduction Although the safety and feasibility of rapid rituximab administration has been demonstrated for B-cell malignancies, there is scant data in the literature to support its use in patients with benign diseases. Objective To identify the incidence of infusion-related reaction with rapid rituximab administration in malignant and benign disease. Secondary objective was to determine the infusion time saved between standard administration and rapid rituximab administration. Methods A retrospective cohort study was conducted by reviewing electronic medical records from December 2018 to April 2020. Adult patients who received at least one dose of rapid rituximab were included. Results A total of 63 patents were included. The incidence of an infusion-related reaction with rapid rituximab was 1.6%. The one patient who reacted had a diagnosis of neuromyelitis optica. The mean infusion time saved was 2.9 hours (95% CI: 2.7-3.1; P-value <0.001). Conclusion The use of the rapid rituximab administration is safe and well tolerated in both benign and malignant disease.

Numerical analysis of the convection and diffusion of solutes to roots

Soil Research ◽  
1967 ◽  
Vol 5 (2) ◽  
pp. 149 ◽  
Author(s):  
JB Passioura ◽  
MH Frere
Keyword(s):  
Differential Equation ◽  
Partial Differential Equation ◽  
Porous Medium ◽  
Diffusion Coefficient ◽  
Numerical Analysis ◽  
Average Concentration ◽  
Soil System ◽  
Dry Soil ◽  
The One ◽  
And Diffusion

A numerical method is given for solving a partial differential equation describing the radial movement of solutes through a porous medium to a root. Computer programmes based on the method were prepared and used to obtain solutions of the equation for an idealized root-soil system in which a solute is transported to the root by convection but is not taken up by the root. Various patterns of water uptake were considered, the most complex being a diurnally varying uptake from soil in which the water content is decreasing. The solutions suggest that the maximum build-up of solute at the surface of a root is trivial if the root is growing in a medium such as agar, in which the diffusion coefficient of the solute is high, but may be considerable, with a concentration up to 10 times higher than the average concentration in the soil solution, when the root is growing in a fairly dry soil. The application of the method to systems other than the one considered in detail is discussed.

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