Pharmacokinetics of oxatomide given percutaneously to healthy volunteers

Benvenuti, Claudio; Broggini, M.; Botta, V.; Valenti, M.; Broccali, G; Li, Bo

doi:10.1002/bdd.2510130703

Cited by 4 publications

(2 citation statements)

References 2 publications

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“…L'assorbimento percutaneo di oxatomide è piuttosto scarso, con concentrazioni plasmatiche che non superano i 5 ng/ml dopo una settimana di applicazioni quotidiane di un gel al 5% [12], per cui l'uso topico risulta virtualmente privo di effetti sistemici.…”

Section: Farmacocineticaunclassified

Profilo clinico ed economico di oxatomide

Pradelli

Eandi

2003

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Oxatomide is an antiallergic drug with a double mechanism of action: it possesses antagonistic activity on the H 1 histaminergic receptor and it inhibits the production and release of flogistic and allergic mediators by effector cells, presumably acting as a selective calcium channel blocker on these cellular types. The efficacy and safety of oxatomide have been evaluated in many studies conducted on patients affected by different clinical conditions, demonstrating remarkable flexibility. It proved to be safe and effective also in extreme ages, i.e. children under 3 months of age and elderly over 80 years. Approved indications include rhinitis, asthma, conjunctivitis, urticaria, atopic and allergic dermatitis and food allergy and intolerance. In direct comparisons, oxatomide consistently proved superior than placebo and equally or more effective than other consolidated antiallergics. The drug tolerability is good, its main side effects are drowsiness and weight gain, usually transient. Cardiac and hepatic safety data are very reassuring, as is the case for drug interaction potential. Form an economical point of view, the drug acquisition cost is acceptable, being among the lowest in its class, at equally effective doses. Overall, the efficacy in several clinical conditions, the good tolerability in most patients and the reasonable purchase cost suggest that oxatomide is characterized by excellent risk-to-benefit and cost-to-benefit ratios in the treatment of allergic pathologies. Farmeconomia e percorsi terapeutici 2003; 4 (4): 217-230Profilo clinico ed economico di oxatomide Lorenzo Pradelli*, Mario Eandi* INTRODUZIONELe malattie allergiche sono tra le patologie più diffuse nei paesi occidentali, dove la loro prevalenza e gravità è in costante aumento. Per quanto nella maggioranza dei casi le patologie ad eziologia allergica non costituiscano una minaccia per la sopravvivenza, esse sono tuttavia in grado di peggiorare gravemente la qualità di vita dei pazienti e del loro nucleo familiare, esordendo spesso in età infantile.La migliorata conoscenza della fisiopatologia della malattia allergica, con il riconoscimento del ruolo fondamentale del processo flogistico nella patogenesi e nella progressione dei fenomeni allergici, ha accresciuto l'interesse per i farmaci antiallergici cosiddetti "dual action", che all'efficacia antistaminica H 1 uniscono un'azione inibente sui mediatori cellulari dell'infiammazione.Scopo del presente lavoro è delineare un profilo farmacologico clinico e farmacoeconomico dell'oxatomide, un farmaco appartenente alla classe degli antiallergici "dual action".La revisione dei principali lavori scientifici pubblicati sull'oxatomide verrà utilizzata come base per condurre un'analisi dei valori clinici ed economici del suo utilizzo, condotta dal punto di vista di tutti i soggetti coinvolti nella pratica clinica. FarmacodinamicaOxatomide è un farmaco in grado di contrastare la reazione allergica agendo in diverse fasi del suo sviluppo. Il primo meccanismo d'azione studiato consiste nell'a...

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Section: Farmacocineticaunclassified

Profilo clinico ed economico di oxatomide

Pradelli

Eandi

2003

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“…Few high-performance liquid chromatographic methods employing fluorescence detection have been established for the determination of oxatomide in human plasma (Benavenuti et al, 1992;Dani et al, 2002) and rat plasma (Kikuchi et al, 2002). However, the sample preparation and extraction procedures of the methods mentioned above are complex and timeconsuming.…”

Section: Introductionmentioning

confidence: 99%

Determination of oxatomide in human plasma by high‐performance liquid chromatography–electrospray ionization mass spectrometry

She

Hui-lin

et al. 2008

Biomedical Chromatography

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A rapid, sensitive and specific high-performance liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS) method has been developed and validated for the determination of oxatomide in human plasma. Flunarizine hydrochloride was employed as the internal standard (IS). The analytes were chromatographically separated on a Shimadzu Shim-pack VP-ODS C18 column (250 x 2.0 mm i.d.) with a mobile phase consisting of methanol and aqueous ammonium acetate solution (10 mm, pH 4.0; 85:15, v/v). Detection was performed on a single quadrupole mass spectrometer using an electrospray ionization interface with the selected-ion monitoring (SIM) mode. The method showed excellent linearity (r = 0.9995) over the concentration range of 0.5-500 ng/mL with good accuracy and precision. The intra- and inter-batch precisions were within 10% relative standard deviation. The recoveries were more than 90%. The validated method was successfully applied to a preliminary pharmacokinetic study of oxatomide in Chinese healthy male volunteers.

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Bioanalysis of antihistamines for clinical or forensic purposes

Katselou

Papoutsis

Νικολάου

et al. 2016

Biomedical Chromatography

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Antihistamines are a class of drugs that inhibit the action of histamine and are used to alleviate symptoms associated with allergic reactions, but some of them can cause side effects, the most unpleasant and dangerous of which are the sedative effects that may hinder important psychological functions and impair skilled performance. These side effects could decrease safety in certain common and critical tasks, such as driving or operating machinery, leading to accidents. Antihistamines can also cause intoxications, sometimes lethal, especially when co-administered with alcohol or other sedative drugs. Thus, the development of analytical methods for their determination in biological fluids is considered to be useful for the investigation of clinical and forensic cases. These methodologies could also be used for pharmacokinetic studies. Several liquid and a few gas chromatographic methods have been developed for the determination of antihistamines in biological matrices after proper pretreatment procedures. This article reviews the published analytical methodologies that were gathered through the search in PubMed database and the recent developments on isolation or determination of antihistamines in biological materials. Current trends and future perspectives on bioanalysis of antihistamines are also discussed. Copyright © 2016 John Wiley & Sons, Ltd.

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Pharmacokinetics of oxatomide given percutaneously to healthy volunteers

Cited by 4 publications

References 2 publications

Profilo clinico ed economico di oxatomide

Profilo clinico ed economico di oxatomide

Determination of oxatomide in human plasma by high‐performance liquid chromatography–electrospray ionization mass spectrometry

Bioanalysis of antihistamines for clinical or forensic purposes

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