The pharmacokinetics of para‐aminosalicylic acid and its relationship to efficacy and intolerance

Abulfathi, Ahmed A.; Donald, Peter R.; Adams, Kim; Svensson, Elin M; Diacon, Andreas H.; Reuter, Helmuth

doi:10.1111/bcp.14395

Cited by 18 publications

(17 citation statements)

References 48 publications

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“…PAS, discovered in 1944, is available in an oral formulation; it should be administered with acid food to increase its absorption ( Abulfathi et al., 2020 ).…”

Section: Methodsmentioning

confidence: 99%

Tuberculosis and pharmacological interactions: A narrative review

Riccardi

Canetti

Rodari

et al. 2021

Current Research in Pharmacology and Drug Discovery

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Even if major improvements in therapeutic regimens and treatment outcomes have been progressively achieved, tuberculosis (TB) remains the leading cause of death from a single infectious microorganism. To improve TB treatment success as well as patients' quality of life, drug-drug-interactions (DDIs) need to be wisely managed. Comprehensive knowledge of anti-TB drugs, pharmacokinetics and pharmacodynamic (PK/PD) parameters, potential patients’ changes in absorption and distribution, possible side effects and interactions, is mandatory to built effective anti-TB regimens. Optimization of treatments and adherence to international guidelines can help bend the curve of TB-related mortality and, ultimately, decrease the likelihood of treatment failure and drop-out during anti-TB treatment. Aim of this paper is to describe the most relevant DDIs between anti-TB and other drugs used in daily clinical practice, providing an updated and “easy-to-use” guide to minimize adverse effects, drop-outs and, in the long run, increase treatment success.

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“…PAS, discovered in 1944, is available in an oral formulation; it should be administered with acid food to increase its absorption ( Abulfathi et al., 2020 ).…”

Section: Methodsmentioning

confidence: 99%

Tuberculosis and pharmacological interactions: A narrative review

Riccardi

Canetti

Rodari

et al. 2021

Current Research in Pharmacology and Drug Discovery

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show abstract

“…47 In contrast, limited clinical data suggest high peaks may produce better effects. 48 Penetration into human lung lesions is unknown. GI upset and diarrhea are the main adverse effects.…”

Section: Reserve Drugsmentioning

confidence: 99%

“…Based on limited in vitro activity, time above MIC can be suggested 47 . In contrast, limited clinical data suggest high peaks may produce better effects 48 . Penetration into human lung lesions is unknown.…”

Section: Beta‐lactamsmentioning

confidence: 99%

The Treatment of Tuberculosis

Peloquin

Davies

2021

Clin Pharma and Therapeutics

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Tuberculosis (TB) remains a leading cause of infectious death worldwide, and poverty is a major driver. Clinically, TB presents as “latent” TB and active TB disease, and the treatment for each is different. TB drugs can display “early bactericidal activity (EBA)” and / or “sterilizing activity” (clearing persisters). Isoniazid is excellent at the former, and rifampin is excellent at the latter. Pyrazinamide and ethambutol complete the first‐line regimen for drug‐susceptible TB, each playing a specific role. Drug‐resistant TB is an increasing concern, being met, in part, with repurposed drugs (including moxifloxacin, levofloxacin, linezolid, clofazimine, and beta‐lactams) and new drugs (including bedaquiline, pretomanid, and delamanid). One challenge is to select drugs without overlapping adverse drug reaction profiles. QTc interval prolongation is one such concern, but to date, it has been manageable. Drug penetration into organism sanctuaries, such as the central nervous system, bone, and pulmonary TB cavities remain important challenges. The pharmacodynamics of most TB drugs can be described by the area under the curve (AUC) divided by the minimal inhibitory concentration (MIC). The hollow fiber infection model (HFIM) and various animal models (especially mouse and macaque) allow for sophisticated pharmacokinetic/pharmacodynamic experiments. These experiments may hasten the selection of the most potent, shortest possible regimens to treat even extremely drug resistant TB. These findings can be translated to humans by optimizing drug exposure in each patient, using therapeutic drug monitoring and dose individualization.

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Section: Adverse Effectsmentioning

confidence: 99%

“…The most common ADEs in patients treated with PAS are hypothyroidism (when administered concomitantly with Eto); gastrointestinal manifestations such as diarrhoea, nausea, vomiting and anorexia; hepatitis; and malabsorption syndrome (45). Eosinophilic pneumonia, encephalopathy and optic neuritis are adverse effects that need to be carefully monitored (22,45). Also, during therapy with PAS, haematological changes (haemolytic anaemia, agranulocytosis, leukopenia, thrombocytopenia and methemoglobinemia) and allergic reactions (pruritus and fever) can occur (26,45,46).…”

Section: Adverse Effectsmentioning

confidence: 99%

Adverse effects induced by second-line antituberculosis drugs: an update based on last WHO treatment recommendations for drug-resistant tuberculosis

et al. 2021

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Introduction: Tuberculosis (TB), a common condition worldwide, is still among the main infectious diseases with high mortality rates, both in adults and infants. Drug-resistant tuberculosis (DR-TB) drugs, revised by the World Health Organization (WHO) in 2018, are a prolonged and complex therapy associated with many adverse drug effects (ADEs). Aim: To systematically review the ADEs of second-line anti-TB drugs reported in multicentric studies published after the latest WHO guidelines, compared with those from clinical trials published before 2018. Material and methods: A PubMed search, using keywords (TB OR DR-TB) AND (adverse effects) AND “second-line anti-TB drugs”, resulted in 56 studies. Only two studies, published after the last update of WHO guidelines in 2018, reported ADEs. Results: A total of 223 participants were included in the two selected studies. The use of multidrug regimens has been associated with an increased incidence of ADEs: 42 ADEs were recorded in 30 patients (26.3%) in the first study, while all patients had at least one ADE that occurred or worsened during treatment; and 19 (17%) had severe ADEs in the second study. However, both studies had a good favourable outcome rate (90% and 79.8%, respectively). Gastrointestinal disturbances, hepatotoxicity, headache and dizziness are the most common ADEs induced by a majority of second-line DR-TB treatments. A special attention should be given in the case of association of drugs determining QT interval (QT) prolongation on electrocardiogram, or psychiatric disorders. Conclusions: Proper strategies about ADE management have to be planned for timely detection of the possible ADEs that can be induced by second-line anti-TB therapy.

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The pharmacokinetics of para‐aminosalicylic acid and its relationship to efficacy and intolerance

Cited by 18 publications

References 48 publications

Tuberculosis and pharmacological interactions: A narrative review

Tuberculosis and pharmacological interactions: A narrative review

The Treatment of Tuberculosis

Adverse effects induced by second-line antituberculosis drugs: an update based on last WHO treatment recommendations for drug-resistant tuberculosis

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