Pyrazinamide
From Proteopedia
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Pyrazinamide is a medication used to treat tuberculosis.<ref name="a2">[https://www.drugs.com/monograph/pyrazinamide.html "Pyrazinamide".] The American Society of Health-System Pharmacists. Archived from the original on 20 December 2016. Retrieved 8 December 2016.</ref> For active tuberculosis, it is often used with rifampicin, isoniazid, and either streptomycin or ethambutol.<ref name="a3">World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary. World Health Organization. pp. 136, 140, 594, 608. hdl:10665/44053. ISBN 978-9241547659.</ref> It is not generally recommended for the treatment of latent tuberculosis.<ref name="a2">[https://www.drugs.com/monograph/pyrazinamide.html "Pyrazinamide".] The American Society of Health-System Pharmacists. Archived from the original on 20 December 2016. Retrieved 8 December 2016.</ref> See also [https://en.wikipedia.org/wiki/Pyrazinamide Pyrazinamide]. | Pyrazinamide is a medication used to treat tuberculosis.<ref name="a2">[https://www.drugs.com/monograph/pyrazinamide.html "Pyrazinamide".] The American Society of Health-System Pharmacists. Archived from the original on 20 December 2016. Retrieved 8 December 2016.</ref> For active tuberculosis, it is often used with rifampicin, isoniazid, and either streptomycin or ethambutol.<ref name="a3">World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary. World Health Organization. pp. 136, 140, 594, 608. hdl:10665/44053. ISBN 978-9241547659.</ref> It is not generally recommended for the treatment of latent tuberculosis.<ref name="a2">[https://www.drugs.com/monograph/pyrazinamide.html "Pyrazinamide".] The American Society of Health-System Pharmacists. Archived from the original on 20 December 2016. Retrieved 8 December 2016.</ref> See also [https://en.wikipedia.org/wiki/Pyrazinamide Pyrazinamide]. | ||
| - | Pyrazinamide diffuses into the granuloma of M. tuberculosis, where the tuberculosis enzyme pyrazinamidase converts pyrazinamide to the active form pyrazinoic acid.<ref name="a15">PMID:26218737</ref> Under acidic conditions of pH 5 to 6, the pyrazinoic acid that slowly leaks out converts to the protonated conjugate acid, which is thought to diffuse easily back into the bacilli and accumulate. The net effect is that more pyrazinoic acid accumulates inside the bacillus at acid pH than at neutral pH.ref name="a15">PMID:26218737</ref><ref name="a16">PMID:12701830</ref> | + | Pyrazinamide diffuses into the granuloma of M. tuberculosis, where the tuberculosis enzyme pyrazinamidase converts pyrazinamide to the active form pyrazinoic acid.<ref name="a15">PMID:26218737</ref> Under acidic conditions of pH 5 to 6, the pyrazinoic acid that slowly leaks out converts to the protonated conjugate acid, which is thought to diffuse easily back into the bacilli and accumulate. The net effect is that more pyrazinoic acid accumulates inside the bacillus at acid pH than at neutral pH.<ref name="a15">PMID:26218737</ref><ref name="a16">PMID:12701830</ref> |
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== References == | == References == | ||
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Revision as of 13:28, 1 January 2024
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References
- ↑ 1.0 1.1 "Pyrazinamide". The American Society of Health-System Pharmacists. Archived from the original on 20 December 2016. Retrieved 8 December 2016.
- ↑ World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary. World Health Organization. pp. 136, 140, 594, 608. hdl:10665/44053. ISBN 978-9241547659.
- ↑ 3.0 3.1 Whitfield MG, Soeters HM, Warren RM, York T, Sampson SL, Streicher EM, van Helden PD, van Rie A. A Global Perspective on Pyrazinamide Resistance: Systematic Review and Meta-Analysis. PLoS One. 2015 Jul 28;10(7):e0133869. PMID:26218737 doi:10.1371/journal.pone.0133869
- ↑ Zhang Y, Mitchison D. The curious characteristics of pyrazinamide: a review. Int J Tuberc Lung Dis. 2003 Jan;7(1):6-21 PMID:12701830
