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Nadifloxacin: Wikis

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Nadifloxacin
Systematic (IUPAC) name
(RS)-9-Fluoro-8-(4-hydroxy-piperidin-1-yl)-5-methyl-1-oxo-6,7-dihydro-1 H,5H-pyrido[3,2,1-ij]quinoline-2-carboxylic acid
Identifiers
CAS number 124858-35-1
ATC code none
PubChem 4410
Chemical data
Formula C 19H21FN2O4  
Mol. mass 360.379 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes topical (epicutaneous)

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

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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 107ng./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

  1. ^ Murata K, Tokura Y (March 2007). "[Anti-microbial therapies for acne vulgaris: anti-inflammatory actions of anti-microbial drugs and their effectiveness]" (in Japanese). J. UOEH 29 (1): 63–71. PMID 17380730.  
  2. ^ Steinhilber; Schubert-Zsilavecz, Roth (2004). Medizinische Chemie: Targets und Arzneistoffe. WVG Stuttgart.  

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