Quinupristin/dalfopristin

From Wikipedia, the free encyclopedia
Quinupristin/dalfopristin
Combination of
Quinupristin Antibiotic
Dalfopristin Antibiotic
Clinical data
Pregnancy cat. B (U.S.)
Legal status ℞-only (U.S.)
Routes IV
Identifiers
CAS number 126602-89-9 N
ATC code J01FG02
PubChem CID 23724510
ChemSpider 21106373 YesY
 N (what is this?)  (verify)

Quinupristin/dalfopristin (trade name Synercid) is a combination of two antibiotics used to treat infections by staphylococci and by vancomycin-resistant Enterococcus faecium.

Quinupristin and dalfopristin are both streptogramin antibiotics, derived from pristinamycin. Quinupristin is derived from pristinamycin IA; dalfopristin from pristinamycin IIA. They are combined in a weight-to-weight ratio of 30% quinupristin to 70% dalfopristin.

Administration

Intravenous, usually 7.5 mg/kg every 8–12 hours

Mechanism of action

Quinupristin and dalfopristin are protein synthesis inhibitors in a synergistic manner. While each of the two is only a bacteriostatic agent, the combination shows bactericidal activity.

  • Dalfopristin binds to the 23S portion of the 50S ribosomal subunit, and changes the conformation of it, enhancing the binding of quinupristin[1] by a factor of about 100. In addition, it inhibits peptidyl transfer.[1]
  • Quinupristin binds to a nearby site on the 50S ribosomal subunit and prevents elongation of the polypeptide,[1] as well as causing incomplete chains to be released.[1]

Pharmacokinetics

Clearance by the liver, half-life 1–3 hours (with persistence of effects for 9–10 hours).

Side effects

  1. Joint aches (arthralgia) or muscle aches (myalgia)
  2. Nausea, diarrhea or vomiting
  3. Rash or itching
  4. Headache
  5. Phlebitis
  6. Hyperbilirubinemia

Drug interactions

Inhibits P450 and enhances the effects of terfenadine, astemizole, indinavir, midazolam, Ca channel blockers, warfarin, cisapride and cyclosporine.

References

  1. ↑ 1.0 1.1 1.2 1.3 Page 212 in: Title: Hugo and Russell's pharmaceutical microbiology Authors: William Barry Hugo, Stephen P. Denyer, Norman A. Hodges, Sean P. Gorman Edition: 7, illustrated Publisher: Wiley-Blackwell, 2004 ISBN 0-632-06467-6, ISBN 978-0-632-06467-0 Length: 481 pages

Further reading

  • Allington, DR, Rivey, MP. (Jan 2001). "Quinupristin/dalfopristin: a therapeutic review". Clin Ther. 23 (1): 24–44. doi:10.1016/S0149-2918(01)80028-X. PMID 11219478. 
  • "Quinupristin/dalfopristin: a review of its use in the management of serious gram-positive infections". Drugs 58 (6): 1061–97. December 1999. PMID 10651391. .
  • "Quinupristin-dalfopristin: a new antibiotic for severe gram-positive infections". Am Fam Physician 64 (11): 1863–6. December 2001. PMID 11764864. .
  • "Antistaphylococcal (MSSA, MRSA, MSSE, MRSE) antibiotics". Med. Clin. North Am. 85 (1): 1–17. January 2001. PMID 11190346. .
  • http://www.fda.gov/cder/consumerinfo/druginfo/SYNERCID.HTM
Antibacterials: protein synthesis inhibitors (J01A, J01B, J01F, J01G, QJ01XQ)
30S
Aminoglycosides
(initiation inhibitors)
-mycin (Streptomyces)
  • Streptomycin#
  • Dihydrostreptomycin
  • Neomycin#
    • Framycetin
    • Paromomycin
    • Ribostamycin
  • Kanamycin#
    • Amikacin
    • Arbekacin
    • Bekanamycin
    • Dibekacin
    • Tobramycin
  • Spectinomycin#
  • Hygromycin B
  • Paromomycin
-micin (Micromonospora)
  • Gentamicin#
    • Netilmicin
    • Sisomicin
    • Isepamicin
  • Verdamicin
  • Astromicin
Tetracycline antibiotics
(tRNA binding)
Tetracyclines
  • Doxycycline#
  • Chlortetracycline
  • Clomocycline
  • Demeclocycline
  • Lymecycline
  • Meclocycline
  • Metacycline
  • Minocycline
  • Oxytetracycline
  • Penimepicycline
  • Rolitetracycline
  • Tetracycline
Glycylcyclines
  • Tigecycline
50S
Oxazolidinone
(initiation inhibitors)
  • Eperezolid
  • Linezolid
  • Posizolid
  • Radezolid
  • Ranbezolid
  • Sutezolid
  • Tedizolid
Peptidyl transferase
Amphenicols
  • Chloramphenicol#
  • Azidamfenicol
  • Thiamphenicol
  • Florfenicol
Pleuromutilins
  • Retapamulin
  • Tiamulin
  • Valnemulin
MLS (transpeptidation/translocation)
Macrolides
  • Azithromycin#
  • Clarithromycin
  • Dirithromycin
  • Erythromycin#
  • Flurithromycin
  • Josamycin
  • Midecamycin
  • Miocamycin
  • Oleandomycin
  • Rokitamycin
  • Roxithromycin
  • Spiramycin
  • Troleandomycin
  • Tylosin
  • Ketolides
    • Telithromycin
    • Cethromycin
    • Solithromycin†
Lincosamides
  • Clindamycin#
  • Lincomycin
  • Pirlimycin
Streptogramins
  • Pristinamycin
  • Quinupristin/dalfopristin
  • Virginiamycin
EF-G
Steroid antibacterials
  • Fusidic acid
  • #WHO-EM
  • ‡Withdrawn from market
  • Clinical trials:
    • †Phase III
    • §Never to phase III

M: BAC

bact (clas)

gr+f/gr+a (t)/gr-p (c)/gr-o

drug (J1p, w, n, m, vacc)

This article is issued from Wikipedia. The text is available under the Creative Commons Attribution/Share Alike; additional terms may apply for the media files.