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| Clinical data | |
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | topical (epicutaneous) |
| ATC code | |
| Identifiers | |
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| UNII | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.166.530 |
| Chemical and physical data | |
| Formula | C19H21FN2O4 |
| Molar mass | 360.385 g·mol−1 |
| 3D model (JSmol) | |
| Chirality | Racemic mixture |
| Melting point | 245 to 247 °C (473 to 477 °F) (dec.) |
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Nadifloxacin (INN, brand namesAcuatim,Nadiflox,Nadoxin,Nadixa,Activon) is a topicalfluoroquinoloneantibiotic for the treatment ofacne vulgaris.[1] It is also used to treat bacterial skin infections.
In vitro studies of nadifloxacin showed potent and broad-spectrum antibacterial activity against aerobicGram-positive,Gram-negative andanaerobic bacteria, includingCutibacterium acnes andStaphylococcus epidermidis. Nadifloxacinshowed potent antibacterial activity againstmethicillin-resistantStaphylococcus aureus (MRSA), which was similar to potency againstmethicillin-sensitiveStaphylococcus aureus (MSSA). The drug was also active against new quinolone-resistant MRSA. Nadifloxacin does not show cross-resistance with other new fluoroquinolones.[citation needed]
Nadifloxacininhibits the enzymeDNA 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]
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 eliminationhalf-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.
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 quinoloneresistances.[7]
During the treatment some patients may develop some adverse effects predominantly of the skin and subcutaneous tissue: burning anditching (in absolute the most common side effect),contact dermatitis,dryness and skin irritation.[8]