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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 Y |
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.
Contents
- 1 Administration
- 2 Mechanism of action
- 3 Pharmacokinetics
- 4 Side effects
- 5 Drug interactions
- 6 References
- 7 Further reading
Administration[edit]
Intravenous, usually 7.5 mg/kg every 8–12 hours
Mechanism of action[edit]
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[edit]
Clearance by the liver, half-life 1–3 hours (with persistence of effects for 9–10 hours).
Side effects[edit]
- Joint aches (arthralgia) or muscle aches (myalgia)
- Nausea, diarrhea or vomiting
- Rash or itching
- Headache
- Phlebitis
- Hyperbilirubinemia
Drug interactions[edit]
Inhibits P450 and enhances the effects of terfenadine, astemizole, indinavir, midazolam, Ca channel blockers, warfarin, cisapride and cyclosporine.
References[edit]
- ^ a b c d 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[edit]
- 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
|
|
-micin (Micromonospora) |
- Gentamicin#
- Netilmicin
- Sisomicin
- Isepamicin
|
|
|
Tetracycline antibiotics
(tRNA binding) |
Tetracyclines |
- Doxycycline#
- Chlortetracycline
- Clomocycline
- Demeclocycline
- Lymecycline
- Meclocycline
- Metacycline
- Minocycline
- Oxytetracycline
- Penimepicycline
- Rolitetracycline
- Tetracycline
|
|
Glycylcyclines |
|
|
|
|
50S |
Oxazolidinone
(initiation inhibitors) |
- Linezolid
- Torezolid
- Eperezolid
- Posizolid
- Radezolid
- Ranbezolid
- Sutezolid
|
|
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 |
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
gr+f/gr+a (t)/gr-p (c)/gr-o
|
drug (J1p, w, n, m, vacc)
|
|
|
|
UpToDate Contents
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English Journal
- Prevalence of antimicrobial resistance in faecal enterococci from vet-visiting pets and assessment of risk factors.
- Leite-Martins L1, Mahú MI2, Costa AL3, Bessa LJ4, Vaz-Pires P3, Loureiro L5, Niza-Ribeiro J6, de Matos AJ7, Martins da Costa P4.
- The Veterinary record.Vet Rec.2015 Jun 27;176(26):674. doi: 10.1136/vr.102888. Epub 2015 Jun 15.
- The objective of this study was to determine the prevalence of antimicrobial resistance (AMR) exhibited by enterococci isolated from faeces of pets and its underlying risk factors. From September 2009 to May 2012, rectal swabs were collected from 74 dogs and 17 cats, selected from the population of
- PMID 26078332
- Prevalence, species distribution and antimicrobial resistance patterns of methicillin-resistant staphylococci in Lithuanian pet animals.
- Ruzauskas M1, Couto N2, Kerziene S3, Siugzdiniene R4, Klimiene I5, Virgailis M6, Pomba C7.
- Acta veterinaria Scandinavica.Acta Vet Scand.2015 Jun 2;57:27. doi: 10.1186/s13028-015-0117-z.
- BACKGROUND: The bacterial genus Staphylococcus consists of many species that causes infections in pet animals. Antimicrobial resistant staphylococci cause infections that are difficult to treat and they are important from the point of one health perspective. The aim of this study was to determine th
- PMID 26032539
- Genotyping of community-associated methicillin resistant Staphylococcus aureus (CA-MRSA) in a tertiary care centre in Mysore, South India: ST2371-SCCmec IV emerges as the major clone.
- Rajan V1, Schoenfelder S2, Ziebuhr W2, Gopal S3.
- Infection, genetics and evolution : journal of molecular epidemiology and evolutionary genetics in infectious diseases.Infect Genet Evol.2015 Jun 1. pii: S1567-1348(15)00231-2. doi: 10.1016/j.meegid.2015.05.032. [Epub ahead of print]
- The burden of community-associated methicillin resistant Staphylococcus aureus (CA-MRSA) is on the rise in population and clinical settings on account of the adaptability and virulence traits of this pathogen. We characterized 45 non-duplicate CA-MRSA strains implicated mainly in skin and soft tissu
- PMID 26044198
Japanese Journal
- バンコマイシン耐性腸球菌 (特集 外科領域における耐性菌)
- Isolation and Molecular Characterization of Methicillin-Resistant Staphylococci from Horses, Personnel and Environmental Sites at an Equine Hospital in Turkey
- 各種抗菌薬に対する2004年臨床分離好気性グラム陽性球菌および嫌気性菌の感受性サーベイランス
Related Links
- Quinupristin / Dalfopristin [QPR/DPR] キヌプリスチン/ダルホプリスチン, ストレプトグラミン系 1. 商品名 先発品 注射用シナシッド 【アステラス製薬】 2. 日本における発売年 2003(平成15)年 3. 特長 世界で初めてのストレプトグラミン系 ...
- Quinupristin/dalfopristin should be used with extreme caution in CHILDREN younger than 16 years old; safety and effectiveness in these children have not been confirmed. PREGNANCY and BREAST-FEEDING: If you become ...
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キヌプリスチン・ダルホプリスチン耐性腸球菌
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