Nadifloxacin
| 200px | |
| Systematic (IUPAC) name | |
|---|---|
|
(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 | |
| Clinical data | |
| Routes of administration | topical (epicutaneous) |
| Identifiers | |
| CAS Number | 124858-35-1 |
| ATC code | none |
| PubChem | CID 4410 |
| Chemical data | |
| Formula | C19H21FN2O4 |
| Molar mass | 360.379 g/mol[[Script error: No such module "String".]] |
Nadifloxacin (INN, brand names Acuatim, Nadiflox, Nadoxin, Nadixa) is a topical fluoroquinolone antibiotic for the treatment of acne vulgaris.[1]
It is also used to treat bacterial skin infections.
In patients with skin lesions, topical application of nadifloxacin can result in plasma concentrations of 1 to 3 ng/ml. Consequently, it has been argued that it should not be used to treat relatively harmless diseases like acne vulgaris, risking the development of quinolone resistances.[2]
Contents
Pharmacology
Antibacterial spectrum
In vitro studies of nadifloxacin showed potent and broad-spectrum antibacterial activity against aerobic Gram-positive, Gram-negative and anaerobic bacteria, including Propionibacterium acnes and Staphylococcus epidermidis. Nadifloxacin showed potent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), which was similar to potency against methicillin-sensitive Staphylococcus aureus (MSSA). The drug was also active against new quinolone-resistant MRSA. Nadifloxacin does not show cross-resistance with other new quinolones.
Mechanism of action
Nadifloxacin inhibits the enzyme DNA gyrase that is involved in bacterial DNA synthesis and replication, thus inhibiting the bacterial multiplication.
Pharmacokinetics
Following a single topical application of 10gm 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 gm 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.
See also
References
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- 2Fix
- Fluoroquinolone antibiotics
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