Quinupristin/dalfopristin

Quinupristin/dalfopristin
Combination of

Quinupristin (top) and dalfopristin (bottom)
Quinupristin	Streptogramin antibiotic
Dalfopristin	Streptogramin antibiotic
Clinical data
Pregnancy category	B (U.S.)
Routes of administration	IV
ATC code	J01FG02 (WHO)
Legal status
Legal status	℞-only (U.S.)
Identifiers
CAS Number	126602-89-9^N
PubChem (CID)	23724510
ChemSpider	21106373^Y
^NY (what is this?) (verify)

Quinupristin/dalfopristin (pronunciation: kwi NYOO pris tin / dal FOE pris tin) (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

Joint aches (arthralgia) or muscle aches (myalgia)
Nausea, diarrhea or vomiting
Rash or itching
Headache
Phlebitis
Hyperbilirubinemia

Drug interactions

The drug inhibits P450 and enhances the effects of terfenadine, astemizole, indinavir, midazolam, calcium channel blockers, warfarin, cisapride and ciclosporin.

References

1 2 3 4 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

Allington DR, Rivey M (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. doi:10.2165/00003495-199958060-00008. 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. doi:10.1016/s0025-7125(05)70302-3. PMID 11190346. .
http://web.archive.org/web/20070618100658/http://www.fda.gov:80/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 Plazomicin^† Isepamicin Verdamicin Astromicin

Tetracycline antibiotics
(tRNA binding)

Tetracyclines	Doxycycline^# Chlortetracycline Clomocycline Demeclocycline Lymecycline Meclocycline Metacycline Minocycline Oxytetracycline Penimepicycline Rolitetracycline Tetracycline

Glycylcyclines	Tigecycline

Fluorocyclines	Eravacycline^†

50S

Oxazolidinone
(initiation inhibitors)

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

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