Quinupristin/dalfopristin: Difference between revisions

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{{drugbox
#REDIRECT [[Quinupristin-Dalfopristin]]
| IUPAC_name = '''quinupristine'''  N-[(6''R'',9''S'',10''R'',13''S'',15a''S'',18''R'',22''S'',24a''S'')-22-<br>[p-(dimethylamino)benzyl]-6-ethyldocosahydro-
10,23-dimethyl-5,8,12,15,17,21,24-heptaoxo-13-phenyl-18-<br><nowiki>[[</nowiki>"(3''S'')-3-quinuclidinylthio]methyl]-
12H-pyrido[2,1-''f'']pyrrolo-[2,1-''l''][1,4,7,10,13,16] oxapentaazacyclononadecin-9-yl]-3-hydroxypicolinamide
 
'''dalfopristin'''  (3''R'',4''R'',5''E'',10''E'',12''E'',14''S'',26''R'',26a''S'')-26-<br><nowiki>[[</nowiki>2-(diethylamino)ethyl]sulfonyl]-8,9,14,15,24,25,26,26a- octahydro-14-hydroxy-3-<br>isopropyl-4,12-dimethyl-3H-21,18-nitrilo-1H,22H-pyrrolo[2,1-''c''][1,8,4,19]-
dioxadiazacyclotetracosine-1,7,16,22(4H,17H)-tetrone
| image =
| CAS_number = 120138-50-3
| CAS_supplemental={{CAS|112362-50-2}}
| ATC_prefix = J01
| ATC_suffix = FG02
| PubChem = 6435782
| DrugBank =
| synonyms =
| chemical_formula= '''quinupristin''' C53H67N9O10S1 <br>'''dalfopristin''' C34H50N4O9S
| molecular_weight = '''quinupristin''' 1022.24 g/mol <br>'''dalfopristin''' 690.85 g/mol
| bioavailability =
| protein_bound = moderate
| metabolism =
| elimination_half-life =  '''quinupristin'''  3.1 hours <br>'''dalfopristin'''  1 hour
| excretion = 75% fecal, 15-19% urinary
| pregnancy_category = B <small>([[United States|U.S.]])</small>
| legal_status = ℞-only <small>(U.S.)</small>
| routes_of_administration = [[Intravenous|IV]]
}}
{{SI}}
{{CMG}}
 
{{EH}}
 
'''Quinupristin/dalfopristin''' (Synercid&reg;) is a combination of two [[antibiotic]]s used to treat [[infection]]s by [[staphylococcus|staphylococci]] and by [[vancomycin]]-resistant ''[[Enterococcus|Enterococcus faecium]]''. It is not effective against ''[[Enterococcus|Enterococcus faecalis]]'' infections.
 
Quinupristin and dalfopristin are both [[streptogramin]] antibiotics, derived from [[pristinamycin]]. Quinupristin is derived from pristinamycin I; 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==
Dalfopristin inhibits the early phase of [[protein]] synthesis in the bacterial [[ribosome]] and quinupristin inhibits the late phase of protein synthesis. The combination of the two components acts [[synergy|synergistically]] and is more effective [[in vitro]] than each component alone.
 
==Pharmacokinetics==
Clearance by the [[liver]], [[half-life]] 1-3 hours (with persistence of effects for 9-10 hours).
 
==Side effects==
#[[arthralgia|Joint]] or [[myalgia|muscle]] aches
#[[Nausea]], [[diarrhea]] or vomiting
#[[Rash]] or [[pruritus|itching]]
#[[Headache]]
 
==References==
*Allington DR, Rivey MP., "Quinupristin/dalfopristin: a therapeutic review.", Clin Ther. 2001 Jan;23(1):24-44. PMID 11219478.
*Lamb HM, Figgitt DP, Faulds D., "Quinupristin/dalfopristin: a review of its use in the management of serious gram-positive infections.", Drugs. 1999 Dec;58(6):1061-97. PMID 10651391.
*Manzella JP., "Quinupristin-dalfopristin: a new antibiotic for severe gram-positive infections.", Am Fam Physician. 2001 Dec 1;64(11):1863-6. PMID 11764864.
*Paradisi F, Corti G, Messeri D., "Antistaphylococcal (MSSA, MRSA, MSSE, MRSE) antibiotics.", Med Clin North Am. 2001 Jan;85(1):1-17. PMID 11190346.
*http://www.fda.gov/cder/consumerinfo/druginfo/SYNERCID.HTM
 
{{Macrolides, lincosamides and streptogramins}}
[[Category: Combination antibiotics]]
{{SIB}}
[[fr:quinupristine-dalfopristine]]
 
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