Factors Influencing the Absorption and Disposition of Mecillinam and Pivmecillinam in Man

Andrews, J. M.; Kendall, M. J.; Mitchard, M.

doi:10.1111/j.1365-2125.1976.tb04886.x

Cited by 10 publications

(3 citation statements)

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“…From these studies, it emerged that the absorption of orally administered pivmecillinam is delayed and reduced in the supine position compared with the orthostatic position. A slight reduction of drug bioavailability was observed in the supine position, as shown by the pivmecillinam serum AUC (Andrews et al, 1976). No significant differences were detected in mean plasma concentrations when similar antibiotic drugs were administered intravenously.…”

Section: Drug Pk Studies In Space and In Surrogate Models Of Microgra...mentioning

confidence: 99%

Physiological adaptations affecting drug pharmacokinetics in space: what do we really know? A critical review of the literature

Russo

Bandiera

Monici

et al. 2022

British J Pharmacology

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As human spaceflight progresses with extended mission durations, the demand for effective and safe drugs will necessarily increase. To date, the accepted medications used during missions (for space motion sickness, sleep disturbances, allergies, pain, and sinus congestion) are administered under the assumption that they act as safely and efficaciously as on Earth. However, physiological changes have been documented in human subjects in spaceflight involving fluid shifts, muscle and bone loss, immune system dysregulation, and adjustments in the gastrointestinal tract and metabolism. These alterations may change the pharmacokinetics (PK) and pharmacodynamics of commonly used medications. Frustratingly, the information gained from bed rest studies and from in‐flight observations is incomplete and also demonstrates a high variability in drug PK. Therefore, the objectives of this review are to report (i) the impact of the space environmental stressors on human physiology in relation to PK; (ii) the state‐of‐the‐art on experimental data in space and/or in ground‐based models; (iii) the validation of ground‐based models for PK studies; and (iv) the identification of research gaps.

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Section: Drug Pk Studies In Space and In Surrogate Models Of Microgra...mentioning

confidence: 99%

Physiological adaptations affecting drug pharmacokinetics in space: what do we really know? A critical review of the literature

Russo

Bandiera

Monici

et al. 2022

British J Pharmacology

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“…Mecillinam is poorly absorbed from the gastrointestinal tract but pivmecillinam is well absorbed. Pivmecillinam reaches serum concentrations of 3ug/ml 1.5 h after 200 mg taken orally [31]. …”

Section: Discussionmentioning

confidence: 99%

Characteristics of gram-negative urinary tract infections caused by extended spectrum beta lactamases: pivmecillinam as a treatment option within South Dublin, Ireland

et al. 2016

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BackgroundThe prevalence of urinary tract infections (UTIs) caused by extended-spectrum β-lactamase (ESBL)-producing Enterobacteriaceae is increasing and the therapeutic options are limited, especially in primary care. Recent indications have suggested pivmecillinam to be a suitable option. This pilot study aimed to assess the viability of pivmecillinam as a therapeutic option in a Dublin cohort of mixed community and healthcare origin.MethodsA prospective measurement of mean and fractional inhibitory concentrations of antibiotic use in 95 patients diagnosed with UTI caused by ESBL-producing Enterobacteriaceae was carried out. 36 % patients were from general practice, 40 % were admitted to hospital within south Dublin, and 25 % samples arose from nursing homes. EUCAST breakpoints were used to determine if an isolate was sensitive or resistant to antibiotic agents.ResultsSixty-nine percent of patients (N = 66) with urinary ESBL isolates were female. The mean age of females was 66 years compared with a mean age of 74 years for males. Thirty-six percent of isolates originated from primary care, hospital inpatients (26 %), and nursing homes (24 %). The vast majority of ESBL isolates were E. coli (80 %). The E tests for mecillinam and co-amoxiclav had concentration ranges from 0.16 mg/L up to 256 mg/L. The mean inhibitory concentration (MIC) of mecillinam ranged from 0.25 to 256 mg/L, while co-amoxiclav MICs ranged from 6 to 256 mg/L. The percentage of isolates resistant to mecillinam and co-amoxiclav was found to be 5.26 and 94.74 % respectively.ConclusionsThis is the first study exploring the use of pivmecillinam in an Irish cohort and has demonstrated that its use in conjunction with or without co-amoxiclav is an appropriate and useful treatment for urinary tract infections caused by ESBL-producing organisms.

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“…Peak serum levels are significantly lower in supine, resting subjects than in moderately active ones . Mean serum levels of mecillinam double following co-administration of probenecid (ROHOLT et al 1975;ANDREWS et al 1976). …”

Section: Mecillinammentioning

confidence: 98%

Pharmacokinetics of β-Lactam Antibiotics

Kwan¹

1983

Antibiotics

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Factors Influencing the Absorption and Disposition of Mecillinam and Pivmecillinam in Man

Cited by 10 publications

References 10 publications

Physiological adaptations affecting drug pharmacokinetics in space: what do we really know? A critical review of the literature

Physiological adaptations affecting drug pharmacokinetics in space: what do we really know? A critical review of the literature

Characteristics of gram-negative urinary tract infections caused by extended spectrum beta lactamases: pivmecillinam as a treatment option within South Dublin, Ireland

Pharmacokinetics of β-Lactam Antibiotics

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