Pefloxacin

J01M - Quinolone antibacterials ATC J01MA03 Small molecule

JFDA label: Peflox- 400 f/c tablets

Mechanism of Action

Inhibitor of Bacterial DNA gyrase — Bacterial DNA gyrase inhibitor; Inhibitor of Topoisomerase IV — Topoisomerase IV inhibitor

Target	Action	Gene / class
Bacterial DNA gyrase efficacy	INHIBITOR
Topoisomerase IV efficacy	INHIBITOR

Indications

Approved

Bacterial Infections — bacterial disease

Class profile

gramStatus	Both
spectrumBreadth	Moderate
atypicalCoverage	No
isBactericidal	1
moaCategory	DNA synthesis inhibitor (topoisomerase II/IV)
pdIndex	Concentration-dependent
postAntibioticEffect	Prolonged
mrsaCoverage	0
resistanceMechanisms	Target site mutations (gyrA,parC),Active efflux

Pregnancy & Lactation

Pregnancy

Monitoring

Efficacy	Culture and susceptibility testing; clinical resolution (temperature, WBC, CRP, procalcitonin)
Toxicity	Renal function (dose adjustment in renal impairment); hepatic function for hepatically cleared agents; signs of C. difficile infection (diarrhoea)
Clinical pearl	Culture results guide de-escalation to narrower-spectrum therapy. Review antibiotic appropriateness at 48–72 h (antimicrobial stewardship).
Counseling	Complete the full course. Report persistent diarrhoea, rash, or lack of improvement after 48–72 h.

Chemistry & Properties

Formula	C17H20FN3O3
Molecular weight	333.36 g/mol
IUPAC name	1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
CAS	70458-92-3
PubChem CID	51081
InChIKey	`FHFYDNQZQSQIAI-UHFFFAOYSA-N`
logP	1.61 (XLogP 0.3)
Polar surface area	65.78 Å²
H-bond acceptors / donors	5 / 1
Drug-likeness (QED)	0.92
Lipinski violations	0

SMILES

CCn1cc(C(=O)O)c(=O)c2cc(F)c(N3CCN(C)CC3)cc21

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes (logBB -0.16)

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (3)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Pefloquin Tab	Tablet 400 mg	2 tab pack varies	Hayat Pharmaceutical Industries CO.PLC/JORDAN	1.080
Pefloquin Tab	Tablet 400 mg	10 tab pack varies	Hayat Pharmaceutical Industries CO.PLC/JORDAN	4.970
Peflox- 400 f/c tablets	Tablet 400 mg	10 tab	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	5.420