Ofloxacin

J01M - Quinolone antibacterials ATC J01MA01 Small molecule approved 1990 Oral Parenteral Topical Black-box warning

🧬 Cross-allergy: Fluoroquinolones

JFDA label: Oflacin-200mg F.C Tablets

⚠ Black-Box Warning

neurotoxicity — ChEMBL drug_warning (Black Box Warning) | United States
musculoskeletal toxicity — ChEMBL drug_warning (Black Box Warning) | United States
SERIOUS ADVERSE REACTIONS INCLUDING TENDINITIS, TENDON RUPTURE, PERIPHERAL NEUROPATHY, CENTRAL NERVOUS SYSTEM EFFECTS AND EXACERBATION OF MYASTHENIA GRAVIS Fluoroquinolones, including ofloxacin, have

Mechanism of Action

Inhibitor of Bacterial DNA gyrase — Bacterial DNA gyrase inhibitor

Target	Action	Gene / class
Bacterial DNA gyrase efficacy	INHIBITOR

Indications

Approved

Acne Vulgaris — acne
Bacterial Infections — bacterial disease
Bronchitis, Chronic — chronic bronchitis
Corneal Ulcer — keratitis
Eye Infections — eye infection
Infections — infection
Otitis Externa — otitis externa

Off-label

Conjunctivitis, Bacterial
Diabetic Foot
Glaucoma
Glaucoma, Open-Angle
Ocular Hypertension
Otitis Media
Pelvic Inflammatory Disease
Urinary Tract Infections

Antimicrobial Spectrum

Expected / intrinsic spectrum (EUCAST breakpoints & labels) — not local resistance. Source: EUCAST v16 · openfda-label.

Bacteria

Organism	Activity	MIC
Acinetobacter calcoaceticus	Active	—
Chlamydia pneumoniae	Active	—
Chlamydia trachomatis	Active	—
Citrobacter diversus	Active	—
Citrobacter freundii	Active	—
Clostridium perfringes	Active	—
Enterobacter aerogenes	Active	—
Enterobacter cloacae	Active	—
Enterobacterales	Susceptible	0.25 mg/L
Escherichia coli	Active	—
Haemophilus ducreyi	Active	—
Haemophilus influenzae	Susceptible	0.06 mg/L
Klebsiella oxytoca	Active	—
Klebsiella pneumoniae	Active	—
Legionella pneumophila	Active	—
Moraxella catarrhalis	Susceptible	0.25 mg/L
Morganella morganii	Active	—
Mycoplasma hominis	Active	—
Mycoplasma pneumoniae	Active	—
Neisseria gonorrhoeae	Susceptible	0.125 mg/L
Proteus mirabilis	Active	—
Proteus vulgaris	Active	—
Providencia rettgeri	Active	—
Providencia stuartii	Active	—
Pseudomonas aeruginosa	Active	—
Serratia marcescens	Active	—
Staphylococcus aureus	Active	—
Staphylococcus epidermidis	Active	—
Staphylococcus saprophyticus	Active	—
Streptococcus pneumoniae	Active	—
Streptococcus pyogenes	Active	—
Treponema pallidum	Active	—

Class profile

gramStatus	Both
spectrumBreadth	Moderate
atypicalCoverage	Yes
isBactericidal	1
moaCategory	DNA synthesis inhibitor (topoisomerase II/IV)
pdIndex	Concentration-dependent
postAntibioticEffect	Prolonged
mrsaCoverage	0
resistanceMechanisms	Target site mutations (gyrA,parC),Active efflux

Contraindications

Source: openFDA

Ofloxacin tablets are contraindicated in persons with a history of hypersensitivity associated with the use of ofloxacin or any member of the quinolone group of antimicrobial agents. Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (3)

Rare Cardiac disorder · Electrocardiogram QT prolonged · Tachycardia

Vascular disorders (4)

Uncommon Ear haemorrhage

Rare Ecchymosis · Haemorrhage · Hypotension

Nervous system disorders (13)

Common Dizziness · Paraesthesia

Uncommon Headache

Rare Aphasia · Ataxia · Benign intracranial hypertension · Cerebral thrombosis · Encephalopathy · Loss of consciousness · Myasthenia gravis · Neuropathy peripheral · Nystagmus · Syncope

Hepatobiliary disorders (6)

Rare Hepatic failure · Hepatic function abnormal · Hepatic necrosis · Hepatitis · Hepatobiliary disease · Jaundice

Renal and urinary disorders (6)

Rare Haematuria · Nephrolithiasis · Polyuria · Renal failure · Renal failure acute · Urinary tract disorder

Blood and lymphatic system disorders (9)

Rare Agranulocytosis · Anaemia · Aplastic anaemia · Eosinophilia · Haemoglobin · Haemolytic anaemia · Leukopenia · Pancytopenia · Thrombocytopenia

Immune system disorders (5)

Rare Alveolitis allergic · Anaphylactic shock · Hypersensitivity · Immune system disorder · Serum sickness

Metabolism and nutrition disorders (2)

Rare Diabetes mellitus · Hypoglycaemia

Gastrointestinal disorders (10)

Uncommon Diarrhoea · Dry mouth · Nausea · Vomiting

Rare Colitis · Dyspepsia · Gastrointestinal haemorrhage · Hiccups · Intestinal perforation · Pseudomembranous colitis

Skin and subcutaneous tissue disorders (19)

Common Dermatitis · Pruritus · Rash

Rare Angioedema · Dermatitis bullous · Dermatitis exfoliative · Erythema multiforme · Erythema nodosum · Petechiae · Photosensitivity reaction · Purpura · Rash maculo-papular · Rash pustular · Skin disorder · Skin hyperpigmentation · Stevens-Johnson syndrome · Thrombotic thrombocytopenic purpura · Toxic epidermal necrolysis · Vascular purpura

Musculoskeletal and connective tissue disorders (6)

Rare Connective tissue disorder · Muscle enzyme increased · Muscle injury · Rhabdomyolysis · Tendon rupture · Tendonitis

Psychiatric disorders (11)

Rare Aggression · Agitation · Anxiety · Disorientation · Mania · Mental disorder · Mood swings · Nightmare · Paranoia · Phobia · Suicidal ideation

Eye disorders (7)

Rare Conjunctivitis · Diplopia · Eye disorder · Uveitis · Vision blurred · Visual acuity reduced · Visual impairment

Ear and labyrinth disorders (5)

Common Ear pain · Vertigo

Uncommon Tinnitus

Rare Deafness · Hearing impaired

Reproductive system and breast disorders (1)

Rare Vulvovaginal candidiasis

Infections and infestations (1)

Rare Vulvovaginal mycotic infection

Investigations (6)

Common Blood glucose decreased

Uncommon Body temperature increased

Rare Coordination abnormal · Electroencephalogram abnormal · Prothrombin level increased · Urine output increased

General disorders and administration site conditions (32)

Very Common Application site reaction

Common Dysgeusia

Rare Acidosis · Affect lability · Ageusia · Albuminuria · Anaphylactoid reaction · Angiopathy · Anosmia · Anuria · Asthenia · Candiduria · Cataract · Contusion · Drug interaction · Dysphonia · Extrapyramidal disorder · Hostility · Lenticular opacities · Leukocytoclastic vasculitis · Mediastinal disorder · Multi-organ failure · Nervous system disorder · Parosmia · Psychotic disorder · Scotoma · Shock · Stridor · Suicide attempt · Torsade de pointes · Urethral disorder · Vasodilation procedure

Respiratory, thoracic and mediastinal disorders (4)

Rare Bronchospasm · Dyspnoea · Pulmonary oedema · Tubulointerstitial nephritis

Dosing

Source: openFDA

The usual dose of ofloxacin tablets is 200 mg to 400 mg orally every 12 h as described in the following dosing chart. These recommendations apply to patients with normal renal function (i.e., creatinine clearance > 50 mL/min). For patients with altered renal function (i.e., creatinine clearance ≤ 50 mL/min), see the Patients With Impaired Renal Function subsection. Infection DUE TO THE DESIGNATED PATHOGENS (see INDICATIONS AND USAGE ). Unit Dose Frequency Duration Daily Dose Acute Bacterial Exacerbation of Chronic Bronchitis 400 mg q12h 10 days 800 mg Comm. Acquired Pneumonia 400 mg q12h 10 days 800 mg Uncomplicated Skin and Skin Structure Infections 400 mg q12h 10 days 800 mg Acute, Uncomplicated Urethral and Cervical Gonorrhea 400 mg single dose 1 day 400 mg Nongonococcal Cervicitis/Urethritis due to C. trachomatis 300 mg q12h 7 days 600 mg Mixed Infection of the Urethra and Cervix due to C. trachomatis and N. gonorrhoeae 300 mg q12h 7 days 600 mg Acute Pelvic Inflammatory Disease 400 mg q12h 10 to 14 days 800 mg Uncomplicated Cystitis due to E. coli or K. pneumoniae 200 mg q12h 3 days 400 mg Uncomplicated Cystitis due to Other Approved Pathogens 200 mg q12h 7 days 400 mg Complicated UTI's 200 mg q12h 10 days 400 mg Prostatitis due to E. coli 300 mg q12h 6 weeks 600 mg Antacids containing calcium, magnesium, or aluminum; sucralfate; divalent or trivalent cations such as iron; or multivitamins containing zinc; or didanosine, chewable/buffered tablets or the pediatric powder for oral solution should not be taken within the two-hour period before or within the two-hour period after taking ofloxacin (see PRECAUTIONS ). Patients With Impaired Renal Function Dosage should be adjusted for patients with a creatinine clearance ≤ 50 mL/min. After a normal initial dose , dosage should be adjusted as follows: Creatinine Clearance Maintenance Dose Frequency 20 to 50 mL/min the usual recommended unit dose q24h < 20 mL/min ½ the usual recommended unit dose q24h When only the serum creatinine is known, the following formula may be used to estimate creatinine clearance. Women: 0.85 × the value calculated for men. The serum creatinine should represent a steady-state of renal function. Figure Patients With Cirrhosis The excretion of ofloxacin may be reduced in patients with severe liver function disorders (e.g., cirrhosis with or without ascites). A maximum dose of 400 mg of ofloxacin per day should therefore not be exceeded.

Warnings & Precautions

Source: openFDA

Boxed Warning

SERIOUS ADVERSE REACTIONS INCLUDING TENDINITIS, TENDON RUPTURE, PERIPHERAL NEUROPATHY, CENTRAL NERVOUS SYSTEM EFFECTS AND EXACERBATION OF MYASTHENIA GRAVIS Fluoroquinolones, including ofloxacin, have been associated with disabling and potentially irreversible serious adverse reactions that have occurred together, including: Tendinitis and tendon rupture Peripheral neuropathy Central nervous system effects (see WARNINGS ). Discontinue ofloxacin immediately and avoid the use of fluoroquinolones, including ofloxacin, in patients who experience any of these serious adverse reactions (see WARNINGS ). Fluoroquinolones, including ofloxacin, may exacerbate muscle weakness in persons with myasthenia gravis. Avoid ofloxacin in patients with a known history of myasthenia gravis (See WARNINGS ). Because fluoroquinolones, including ofloxacin, have been associated with serious adverse reactions (see WARNINGS ), reserve ofloxacin for use in patients who have no alternative treatment options for the following indications: Acute exacerbation of chronic bronchitis Uncomplicated cystitis (see INDICATIONS and USAGE )

Warnings & Precautions

Disabling and Potentially Irreversible Serious Adverse Reactions Including Tendinitis and Tendon Rupture, Peripheral Neuropathy, and Central Nervous System Effects Fluoroquinolones, including ofloxacin, have been associated with disabling and potentially irreversible serious adverse reactions from different body systems that can occur together in the same patient. Commonly seen adverse reactions include tendinitis, tendon rupture, arthralgia, myalgia, peripheral neuropathy, and central nervous system effects (hallucinations, anxiety, depression, insomnia, severe headaches, and confusion). These reactions can occur within hours to weeks after starting ofloxacin. Patients of any age or without pre-existing risk factors have experienced these adverse reactions (see Warnings ) Discontinue ofloxacin immediately at the first signs or symptoms of any serious adverse reaction. In addition, avoid the use of fluoroquinolones, including ofloxacin, in patients who have experienced any of these serious adverse reactions associated with fluoroquinolones. Tendinitis and Tendon Rupture Fluoroquinolones, including ofloxacin, have been associated with an increased risk of tendinitis and tendon rupture in all ages. This adverse reaction most frequently involves the Achilles tendon, and rupture of the Achilles tendon and has been reported with the rotator cuff (the shoulder), the hand, the biceps, the thumb, and other tendons. Tendinitis or tendon rupture can occur within hours or days of starting ofloxacin, or as long as several months after completion of fluoroquinolone therapy. Tendinitis and tendon rupture can occur bilaterally. The risk of developing fluoroquinolone-associated tendinitis and tendon rupture is increased in patients over 60 years of age, in those taking corticosteroid drugs, and in patients with kidney, heart or lung transplants. Other factors that may independently increase the risk of tendon rupture include strenuous physical activity, renal failure, and previous tendon disorders such as rheumatoid arthritis. Tendinitis and tendon rupture have been reported in patients taking fluoroquinolones who do not have the above risk factors. Discontinue ofloxacin immediately if the patient experiences pain, swelling, inflammation or rupture of a tendon. Avoid fluoroquinolones, including ofloxacin, in patients who have a history of tendon disorders or have experienced tendinitis or tendon rupture (see Adverse Reactions ). Patients should be advised to rest at the f

Pregnancy & Lactation

Pregnancy

Lactation

Caution Hale L3

Maternal use of an ear drop or eye drop that contains

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	C18H20FN3O4
Molecular weight	361.37 g/mol
IUPAC name	7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
CAS	82419-36-1
PubChem CID	4583
InChIKey	`GSDSWSVVBLHKDQ-UHFFFAOYSA-N`
logP	1.54 (XLogP -0.4)
Polar surface area	75.01 Å²
H-bond acceptors / donors	6 / 1
Drug-likeness (QED)	0.87
Lipinski violations	0

SMILES

CC1COc2c(N3CCN(C)CC3)c(F)cc3c(=O)c(C(=O)O)cn1c23

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes (logBB -0.76)

Transporters

BCRP (Inhibitor)BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MATE1 (Inhibitor)MCT1 (Inhibitor)MCT4 (Inhibitor)MRP (Inhibitor)MRP1 (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OAT1 (Inhibitor)OAT3 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)OATP2B1 (Inhibitor)OCT1 (Inhibitor)OCTN1 (Inhibitor)OCTN2 (Inhibitor)P-gp (Inhibitor)BCRP (Substrate)MDR1 (Substrate)MRP1 (Substrate)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drug	Severity	Management
Acetohexamide	major
Aminolevulinic acid	major
Anagrelide	major
Arsenic trioxide	major
Betamethasone	major
Bupropion	major
Cabozantinib	major
Ceritinib	major
Chloroquine	major
Chlorpropamide	major
Cisapride	major
Crizotinib	major
Deflazacort	major
Dexamethasone	major
Dicoumarol	major
Dolasetron	major
Fingolimod	major
Fludrocortisone	major
Glimepiride	major
Glipizide	major
Glyburide	major
Halofantrine	major
Hydrocortisone	major
Hydroxychloroquine	major
Insulin aspart (aspart protamine)	major
Insulin aspart (aspart)	major
Insulin degludec	major
Insulin detemir	major
Insulin glargine	major
Insulin glulisine	major
Insulin human	major
Insulin human (inhalation, rapid acting)	major
Insulin human (isophane)	major
Insulin human (regular)	major
Insulin human (zinc extended)	major
Insulin human (zinc)	major
Insulin lispro	major
Insulin lispro (protamine)	major
Iohexol	major
Iopamidol	major

Showing 40 of 100+.

Registered Products (9)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Oflocol	Solution 0.3 %	5 ml	Land Of Medicine Drug Store	1.850
OFLOX E/D	Ophthalmic Solution 3 mg/ml	5 ml	Arab Company for Medical & Agricultural Products	2.310
Optiflox eye drops	Ophthalmic Solution 0.3 %	10 ml	Amman Pharmaceutical Indusries	2.500
Novecin Tablets	Tablet 200 mg	10 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	8.000
Oflacin-200mg F.C Tablets	Film-Coated Tablet 200 mg	10 tab pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	8.000
Novecin Tablet	Tablet 400 mg	10 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	11.900
Novecin Tablet	Tablet 400 mg	500 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	535.280
Novecin Tablets	Tablet 200 mg	1000 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	608.000
Oflacin-200mg F.C Tablets	Film-Coated Tablet 200 mg	1000 tab pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	680.000