Quinupristin-Dalfopristin: Difference between revisions

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Created page with "{{drugbox | 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-..."
 
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{{drugbox
__NOTOC__
| 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-
{{Quinupristin dalfopristin}}
10,23-dimethyl-5,8,12,15,17,21,24-heptaoxo-13-phenyl-18-<br><nowiki>[[</nowiki>"(3''S'')-3-quinuclidinylthio]methyl]-
{{CMG}}; {{AE}} {{chetan}}
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]-
==Overview==
dioxadiazacyclotetracosine-1,7,16,22(4H,17H)-tetrone
'''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.
| 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}}


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.




'''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.
==Category==
Streptogramin
==US Brand Names==


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.
==FDA Package Insert==


==Administration==
'''  [[Quinupristin dalfopristin description|Description]]'''
[[Intravenous]], usually 7.5 mg/kg every 8-12 hours
'''| [[Quinupristin dalfopristin clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Quinupristin dalfopristin microbiology|Microbiology]]'''
'''| [[Quinupristin dalfopristin indications and usage|Indications and Usage]]'''
'''| [[Quinupristin dalfopristin contraindications|Contraindications]]'''
'''| [[Quinupristin dalfopristin warnings and precautions|Warnings and Precautions]]'''
'''| [[Quinupristin dalfopristin adverse reactions|Adverse Reactions]]'''
'''| [[Quinupristin dalfopristin drug interactions|Drug Interactions]]'''
'''| [[Quinupristin dalfopristin overdosage|Overdosage]]'''
'''| [[Quinupristin dalfopristin clinical studies|Clinical Studies]]'''
'''| [[Quinupristin dalfopristin dosage and administration|Dosage and Administration]]'''
'''| [[Quinupristin dalfopristin how supplied|How Supplied]]'''
'''| [[Quinupristin dalfopristin labels and packages|Labels and Packages]]'''


==Mechanism of action==
==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.
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==
==References==
*Allington DR, Rivey MP., "Quinupristin/dalfopristin: a therapeutic review.", Clin Ther. 2001 Jan;23(1):24-44. PMID 11219478.
{{Reflist|2}}
*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]]
 
[[fr:quinupristine-dalfopristine]]


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Revision as of 05:19, 9 January 2014

Quinupristin dalfopristin
SYNERCID ® FDA Package Insert
Description
Clinical Pharmacology
Microbiology
Indications and Usage
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Overdosage
Dosage and Administration
How Supplied
Labels and Packages

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Chetan Lokhande, M.B.B.S [2]

Overview

Quinupristin/dalfopristin (Synercid®) is a combination of two antibiotics used to treat infections by staphylococci and by vancomycin-resistant Enterococcus faecium. It is not effective against 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.


Category

Streptogramin

US Brand Names

FDA Package Insert

Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages

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 synergistically and is more effective in vitro than each component alone.

References

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