Pristinamycin

Pristinamycin
Combination of
Pristinamycin IAStreptogramin B antibiotic
Pristinamycin IIAStreptogramin A antibiotic
Clinical data
AHFS/Drugs.comInternational Drug Names
MedlinePlusa603007
ATC code
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
 NY (what is this?)  (verify)

Pristinamycin (INN), also spelled pristinamycine, is an antibiotic used primarily in the treatment of staphylococcal infections, and to a lesser extent streptococcal infections. It is a streptogramin group antibiotic, similar to virginiamycin, derived from the bacterium Streptomyces pristinaespiralis. It is marketed in Europe by Sanofi-Aventis under the trade name Pyostacine.

Pristinamycin is a mixture of two components that have a synergistic antibacterial action. Pristinamycin IIA is a macrolide, and results in pristinamycin's having a similar spectrum of action to erythromycin. Pristinamycin IA (streptogramin B) is a depsipeptide.[1] PI and PII are coproduced by S. pristinaespiralis in a ratio of 30:70. Each compound binds to the bacterial 50 S ribosomal subunit and inhibits the elongation process of the protein synthesis, thereby exhibiting only a moderate bacteriostatic activity. However, the combination of both substances acts synergistically and leads to a potent bactericidal activity that can reach up to 100 times that of the separate components.

The pristinamycin biosynthetic gene cluster is the largest antibiotic supercluster known so far, with a size of ~210 kb, wherein the PI and PII biosynthetic genes are not clustered individually but are scattered across the complete sequence region.[2] Furthermore, this biosynthetic gene region is interrupted by a cryptic type II PKS gene cluster.

Medical use

Despite the macrolide component, it is effective against erythromycin-resistant staphylococci and streptococci.[3][4] It is active against methicillin-resistant Staphylococcus aureus (MRSA). Its usefulness for severe infections, however, may be limited by the lack of an intravenous formulation owing to its poor solubility.[5] Nevertheless, it is sometimes used as an alternative to rifampicin+fusidic acid or linezolid for the treatment of MRSA.

The lack of an intravenous formulation led to the development of the pristinamycin-derivative quinupristin/dalfopristin (i.e., Synercid), which may be administered intravenously for more severe MRSA infections.

See also

Footnotes

  1. ^ Hamilton-Miller JM (June 1991). "From foreign pharmacopoeias: 'new' antibiotics from old?". The Journal of Antimicrobial Chemotherapy. 27 (6): 702–705. doi:10.1093/jac/27.6.702. PMID 1938680.
  2. ^ Mast Y, Weber T, Gölz M, Ort-Winklbauer R, Gondran A, Wohlleben W, Schinko E (March 2011). "Characterization of the 'pristinamycin supercluster' of Streptomyces pristinaespiralis". Microbial Biotechnology. 4 (2): 192–206. doi:10.1111/j.1751-7915.2010.00213.x. PMC 3818860. PMID 21342465.
  3. ^ Weber P (December 2001). "[Streptococcus pneumoniae: lack of emergence of pristinamycin resistance]". Pathologie-Biologie. 49 (10): 840–845. doi:10.1016/S0369-8114(01)00255-3. PMID 11776696.
  4. ^ Leclercq R, Soussy CJ, Weber P, Moniot-Ville N, Dib C (September 2003). "[In vitro activity of the pristinamycin against the isolated staphylococci in the french hospitals in 1999-2000]". Pathologie-Biologie. 51 (7): 400–404. doi:10.1016/S0369-8114(03)00054-3. PMID 12948760.
  5. ^ Sean C. Sweetman, ed. (November 30, 2004). Martindale: The complete drug reference (34th ed.). London: Pharmaceutical Press. ISBN 0-85369-550-4.