Nadifloxacin

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Nadifloxacin
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration		topical (epicutaneous)
ATC code
Identifiers
  • (RS)-9-Fluoro-8-(4-hydroxy-piperidin-1-yl)-5-methyl-1-oxo-6,7-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-2-carboxylic acid
JSmol)
ChiralityRacemic mixture
Melting point245 to 247 °C (473 to 477 °F) (dec.)
  • CC1CCc2c(N3CCC(O)CC3)c(F)cc3c(=O)c(C(=O)O)cn1c23
  • InChI=1S/C19H21FN2O4/c1-10-2-3-12-16-13(18(24)14(19(25)26)9-22(10)16)8-15(20)17(12)21-6-4-11(23)5-7-21/h8-11,23H,2-7H2,1H3,(H,25,26) ☒N
  • Key:JYJTVFIEFKZWCJ-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Nadifloxacin (

acne vulgaris.[1]
It is also used to treat bacterial skin infections.

Pharmacology

Antibacterial spectrum

In vitro studies of nadifloxacin showed potent and broad-spectrum antibacterial activity against aerobic

methicillin-sensitive Staphylococcus aureus (MSSA). The drug was also active against new quinolone-resistant MRSA. Nadifloxacin does not show cross-resistance with other new fluoroquinolones.[citation needed
]

Mechanism of action

Nadifloxacin

inhibits the enzyme DNA gyrase
that is involved in bacterial DNA synthesis and replication, thus inhibiting the bacterial multiplication. Nadifloxacin in addition to determine a therapeutic antibacterial action, can have a sebostatic and anti-inflammatory action, thus contributing to the improvement of the clinical condition of the patient.[2][3][4]

Pharmacokinetics

Following a single topical application of 10 g nadifloxacin 1% cream to normal human back skin, the highest plasma concentration was determined to be 107 ng/mL with an elimination half-life of 19.4 hours. Approximately 0.09% of the administered dose was excreted in the urine over 48 hours post- dosing. The plasma concentration reached a steady state on Day 5 of repeated administration study when nadifloxacin 1% cream was applied at 5 g twice daily to normal healthy individuals for a period of 7 days. The plasma concentration reached a peak of 4.1 ng/ml at 8 hours post-final dosing with an elimination half-life of 23.2 hours. The urinary excretion rate reached 0.16% on Day 7.

Clinical use

In some European countries, the drug has been approved for the treatment of acne vulgaris.[5] In a 2013 multicenter, randomized clinical study with a total of 184 Japanese patients with moderate to severe acne, adapalene 0.1% gel plus nadifloxacin 1% cream (combination therapy) showed a significant efficacy in decrement of inflammatory papulopustular lesions.[6] In patients with skin lesions, topical application of nadifloxacin can result in plasma concentrations of 1 to 3 ng/ml. Consequently, some authors argued that it should not be used to treat relatively harmless diseases like acne vulgaris, risking the development of quinolone

resistances.[7]

Adverse effects

During the treatment some patients may develop some adverse effects predominantly of the skin and subcutaneous tissue: burning and

itching (in absolute the most common side effect), contact dermatitis, dryness and skin irritation.[8]

References

  1. PMID 17380730
    .
  2. PMID 15795123
    .
  3. S2CID 22232885
    .
  4. PMID 17380730
    .
  5. PMID 16436342
    . Retrieved 2014-09-28.
  6. S2CID 31595559
    .
  7. ISBN 978-3-7692-3483-1
    .
  8. PMID 25212256
    .
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