Ofloxacin (Tarivid, Floxin) is a broad-spectrum antibiotic that is used to treat a variety of bacterial infections including pneumonia, enteric infections, eye, and ear infections.

Ofloxacin Uses:

• Acute exacerbations of chronic bronchitis
• Community-acquired pneumonia
• Uncomplicated Skin & skin structure infections
• nongonococcal urethritis & cervicitis due to Chlamydia trachomatis infection
• Mixed infections of the urethra and cervix
• Acute pelvic inflammatory disease
• Acute uncomplicated Urethral & cervical gonorrhea.
• Uncomplicated Cystitis
• Complicated Urinary tract infections
• Prostatitis

Note:

• The CDC no longer advises using fluoroquinolones to treat gonococcal illness as of April 2007.

• Off Label Use of Ofloxacin in Adults:

  • Epididymitis.
  • Leprosy (multibacillary).
  • Leprosy (paucibacillary).
  • Treatment of spontaneous bacterial peritonitis.
  • Traveler's diarrhea.

Ofloxacin Dose in Adults

Ofloxacin Dose in the treatment of Cervicitis and urethritis:

P/O:

• Nongonococcal (due to Chlamydia trachomatis):

  • For 7 days, 300 mg every 12 hours

• Gonococcal (acute, uncomplicated):

  • 400 mg as a single dose.

Note:

• • The CDC no longer advises the use of fluoroquinolones for the treatment of simple gonococcal illness as of April 2007.

Ofloxacin Dose in the treatment of acute exacerbation Chronic bronchitis, community-acquired pneumonia, skin, and uncomplicated skin structure infections:

P/O:

• For 10 days, 400 mg every 12 hours

Ofloxacin Dose in the treatment of acute Pelvic inflammatory disease:

• Manufacturer's labeling:

  • For 10-14 days, 400 mg every 12 hours.

Note:

• • The CDC advises against using it unless it is impossible to treat patients with severe cephalosporin allergies with normal cephalosporin medication and there is a low prevalence of quinolone-resistant gonococcal pathogens in the population.
  • The CDC advises using metronidazole in combination.
    Confirmation of follow-up, culture, and sensitivity (CDC [Workowski 2015]).

Ofloxacin Dose in the treatment of Prostatitis:

P/O:

•  For 6 weeks, 300 mg every 12 hours

Ofloxacin Dose in the treatment of UTI:

P/O:

• Uncomplicated:

  • Every 12 hours, 200 mg for 3 to 7 days,

• Complicated:

  • Every 12 hours, 200 mg for 10 days,

Ofloxacin Dose in the treatment of Epididymitis (off-label):

P/O

• Likely caused by enteric organisms:

  • 300 mg two times daily for 10 days
  • 200 mg two times daily for 14 days (Canadian STI Guidelines 2008 [Update 2014])

• Men who engage in insertive anal intercourse are more likely affected by sexually transmitted chlamydia, gonorrhoea, and enteric pathogens.:

  • Combining ceftriaxone with 300 mg twice daily for 10 days is recommended (CDC [Workowski 2015])

Ofloxacin Dose in the treatment of Leprosy (multibacillary) (off-label):

P/O:

• Alternatively, 400 mg once every 30 days (in conjunction with monthly rifampin and minocycline) for 24 months, or 400 mg once every 24 hours (in combination with dapsone and rifampin) for 12 months (WHO 2012).

Ofloxacin Dose in the treatment of Leprosy (paucibacillary) (off-label):

Multiple-dose regimen:

• • For 4 weeks, 400 mg orally once 24 hours (in combination with rifampin).

Single-dose regimen:

• • A single dose of 400 mg (in combination with single doses of rifampin & minocycline).

Note:

• • It was discovered to be less efficient than the typical WHO multiple drug therapy (WHO-MDT) for paucibacillary leprosy.
    only be used if relapse careful monitoring is possible

Ofloxacin Dose in the treatment of Spontaneous bacterial peritonitis (off-label):

P/O:

• 400 mg two times every 24 hours.

Ofloxacin Dose in the treatment of Traveler's diarrhea (off-label):

P/O:

• 400 mg once every 24 hours for three days, with or without loperamide, or 200 mg twice every 24 hours for one to three days.
• If symptoms do not go away after 24 hours, continue with a 3-day therapy cycle.
• A 3-day course of therapy is advised for individuals who have dysentery or fever.
• Shigella dysenteriae enteric infection is an exception, and a 5-day treatment course is preferable than single-dose or 3-day regimens.

Note:

• Resistance to fluoroquinolones is rising.
• Particularly in areas with a high frequency of Campylobacter, such Southeast Asia or India, azithromycin may be preferable (ACG [Riddle 2016]).

Ofloxacin Dose in Children

Ofloxacin Dose in the treatment of Susceptible infections in children:

P/O:

• • Rvery 12 hours 15 mg/kg/day in divided doses.

Pregnancy Risk Factor C

• Animal reproduction studies revealed certain unfavourable outcomes.
• Ofloxacin is present in the amniotic fluid and passes through the placenta.
• Pregnant women's blood levels of ofloxacin may be lower than those of non-pregnant women.
• According to available data, there is no evidence that ofloxacin can cause an increase in teratogenic effects during pregnancy.

Ofloxacin use during breastfeeding:

• Ofloxacin is produced in breast milk.
• The manufacturer advises making a decision regarding whether to cease nursing or stop using the medication.
• This consideration should be taken in light of the possibility of serious adverse reactions in the infant while nursing.

Ofloxacin Dose in Kidney Disease:

P/O:

• After a normal initial dose, adjust as follows:

  • CrCl >50 mL/min:

    • Dosage adjustment is not necessary.

  • CrCl 20-50 mL/min:

    • Give the typical dose as directed every 24 hours.

  • CrCl <20 mL/minute:

    • Give half of the regular dose advised every 24 hours.

  • Intermittent hemodialysis (IHD):

    • After dialysis, 100-200 mg.

  • Peritoneal dialysis:

    • Every 24 hours, 200 mg.

  • Continuous renal replacement therapy (CRRT):

    • Every 24 hours, 300 mg.

Ofloxacin Dose in Liver Disease:

• Mild to moderate impairment:

  • In the manufacturer’s labeling, there are no dosage adjustments provided.
  • use cautiously.

• Severe impairment (eg, cirrhosis with or without ascites):

  • Max dose:
  • 400 mg per day

Side Effects of Ofloxacin:

• Cardiovascular:

  • Chest Pain

• Central Nervous System:

  • Headache
  • Insomnia
  • Dizziness
  • Fatigue
  • Drowsiness
  • Sleep Disorder
  • Nervousness
  • Pain

• Dermatologic:

  • Pruritus
  • Skin Rash
  • Genital Pruritus

• Gastrointestinal:

  • Nausea
  • Diarrhea
  • Vomiting
  • Abdominal Cramps
  • Constipation
  • Decreased Appetite
  • Dysgeusia
  • Flatulence
  • Gastrointestinal Distress
  • Xerostomia

• Genitourinary:

  • Vaginitis

• Ophthalmic:

  • Visual Disturbance

• Respiratory:

  • Pharyngitis

• Miscellaneous:

  • Fever

Contraindications to Ofloxacin:

• Intolerance to ofloxacin, other quinolones, or any other ingredient in the formulation

Warnings and precautions

• Modified cardiac conduction

  • The QTc interval may be prolonged by fluoroquinolones.
  • Avoid administering Class Ia and Class III antiarrhythmics, cisapride, erythromycin, antipsychotics, or tricyclic antidepressants to patients who have a history of QTc prolongation, uncorrected hypokalemia, hypomagnesemia, or concurrent administration of other medications known to prolong the QT interval.

• Aneurysm of the aorta and dissection

  • The use of fluoroquinolones has been associated with aortic aneurysm ruptures in older people.
  • Patients who have a history of aneurysms or who are at higher risk, such as those with hypertension, peripheral atherosclerotic diseases, hypertension, and patients with genetic disorders affecting blood vessels (such as Marfan syndrome, Ehlers Danlos syndrome), should avoid taking fluoroquinolones unless there is no effective alternative.
  • Extended therapy (e.g., more than 14 days) may raise the risk (Lee 2018)

• CNS effects

  • The use of fluoroquinolones has been associated with an increased risk of CNS side effects, including tremors, high intracranial pressure (including pseudotumor cerebri), disorientation, and seizures.
  • Patients should exercise caution if they have any CNS problems, such as severe cerebral arteriosclerosis, epilepsy, or any other risk factors.

• Regulation of Glucose

  • Fluoroquinolones have been connected to problems with the regulation of glucose, including hypo- and hyperglycemia.
  • Patients who are also taking insulin or oral hypoglycemic drugs have been most affected by these events.
  • There have been several cases of severe hypoglycemia including death and coma.
  • Patients with diabetes should have a thorough examination to look for indications of poor glucose regulation.
  • Stop taking the medication if you experience hypoglycemia.

• Hypersensitivity reactions

  • Anaphylaxis and severe hypersensitivity reactions can occur with quinolone therapy.
  • These reactions may have a wide spectrum.
  • Itching, urticaria and rash may be the most common reactions after one dose. However, severe idiosyncratic dermatologic symptoms may also occur after multiple doses.
  • You should immediately stop taking any drugs if you experience a skin rash, or other symptoms.

• Peripheral neuropathy:

  • It  has been rarely reported.
  • The effects of therapy can be immediate and irreversible.
  • Stop taking medication if you experience symptoms of sensorimotor or sensory neuropathy.

• Phototoxicity:

  • Avoid too much sun and take safety precautions (e.g., wearing loose-fitting clothes, using sunscreen).
  • Phototoxicity reactions may range from mild to severe.
  • If you experience photosensitivity, stop using the product.

• Psychiatric reactions

  • Fluoroquinolones are linked to a higher incidence of psychiatric side effects. Hallucinations and toxic psychosis are examples of this.
  • Additionally, it can lead to agitation, delirium, confusion, disorientation, anxiety, concentration deficits, and memory loss.
  • Patients with depression history or other risk factors should be cautious.
  • Stop using the medication if you experience a reaction.

• Superinfection

  • Prolonged use of the medicine might result in fungal and bacterial superinfections, such as pseudomembranous collitis and C. difficile-associated diarrhoea (CDAD).
  • Several months after receiving antibiotics, CDAD was monitored.

• Tendon rupture/ inflammation: [US Boxed Warn]

  • Reports of tendon inflammation and rupture have been reported after using quinolone antibiotics.
  • For patients over 60 and those undergoing organ transplants, concurrent corticosteroids may raise the risk.
  • Achilles tendon ruptures are most frequently treated surgically. Other tendon locations, like the rotator cuff and biceps, have been documented, nevertheless.
  • Tendonitis can be caused by strenuous exercise.
  • Stop using the medication immediately if there is any tendon inflammation.
  • This may occur even after therapy is stopped.

• Hepatic impairment

  • Hepatic patients need to exercise caution.

• Myasthenia gravis: [US Boxed Warning]:

  • Can make myasthenia gravis-related muscular weakness worse.
  • Both fatalities and severe exacerbations have occurred.
  • Patients with myasthenia gravis should not use.

• Renal impairment

  • Patients with impaired renal function should be cautious.
  • Adjustment of dosage is required.
  • Increased risk of tendon rupture.

• Rheumatoid arthritis:

  • Patients with rheumatoid arthritis should be cautious.
  • Tendon rupture risk is more. 

• Seizures:

  • When giving medication to patients who are at high risk for seizures, exercise caution (CNS disorders, or concurrent therapy with medications that may lower the seizure threshold).
  • Despite the rarity of seizures, they can be made worse by concurrent NSAID therapy.

• Syphilis:

  • Syphilis should be checked on all patients at the time they are diagnosed with gonorrhea and three months later. Ofloxacin is not effective in treating syphilis, and can mask symptoms.

Note:

• The CDC no longer advises using fluoroquinolones to treat simple gonococcal illness as of April 2007.

Ofloxacin (systemic): Drug Interaction

Monitoring Parameters:

• If therapy is prolonged, examine CBC, renal, and hepatic function periodically.
• Signs and symptoms of disordered glucose regulation.

How to administer Ofloxacin?

• Both with and without food, administer.
• Sucralfate, didanosine, iron, zinc, and antacids made of magnesium, calcium, or aluminium shouldn't be taken within two hours of each other.

Mechanism of action of Ofloxacin:

• A DNA-gyrase inhibitor is ofloxacin.
• The DNA's superhelical shape is preserved by the essential bacterial enzyme DNA gyrase.
• DNA replication, DNA transposition, and DNA repair and transcription all require DNA gyrase.
• Bactericidal.

Absorption:

• Well absorbed

Distribution:

• Widely disseminated throughout body fluids and tissues, including sputum, skin, prostatic tissue, lung, cervix, blister fluid, and ovary.

Protein binding:

• 20%-32 %

Bioavailability:

• 98 %

Half-life elimination:

• Nine hours (biphasic: four to five hours [6.4 to seven hours in older patients] and twenty to twenty-five hours [accounts for about 5%]).
  with renal impairment extended

Time to peak serum concentration:

• 1-2 hours

Excretion:

• Urine:
  • 65 %-80 % (as unchanged drug).
• Feces:
  • 4 %-8 %.
  • <10 % is metabolized.

International Brands of Ofloxacin:

• Akilen
• Avaflox
• Biloxcin
• Cilox 200
• Cinaflox
• Danoflox
• Evaflox
• Flobacin
• Flogirax
• Floksan
• Flotavid
• Flovid
• Floxil
• Floxitop
• Floxstat
• Fugacin
• Hyflox
• Kinflocin
• Kinoxacin
• Loxinter
• Loxwin
• Medofloxine
• Mefoxa
• Menazin
• Microbac
• Novecin
• Nufafloqo
• Ofcin
• Ofla
• Oflacin
• Oflamed
• Oflin
• Oflobid
• Oflocee
• Oflocet
• Oflocin
• Oflodal
• Oflodex
• Oflodura
• Oflovir
• Ofloxin
• Ofloxol
• Oltrex
• Onexacin
• Orivid
• Orocin
• Oxacid
• Oxacin
• Pharflox
• Quotavil
• Rilox
• Sinflo
• Tabrin
• Tafloc
• Taravid
• Tariflox
• Tarivid
• Taroflex
• Telbit
• Uro Tarivid
• Vioflox
• Vioson
• Viotisone
• Zanocin

Ofloxacin Brand Names in Pakistan: