CIPRO

Clinical safety rating: caution

Comprehensive clinical and safety monograph for CIPRO (CIPRO).

How it works

Ciprofloxacin inhibits bacterial DNA gyrase and topoisomerase IV, preventing DNA replication and transcription, leading to bacterial cell death.

What the body does with it

Metabolism	Ciprofloxacin is metabolized in the liver via CYP1A2, producing 4 metabolites: desethylene ciprofloxacin (major), N-acetyl ciprofloxacin, oxo-ciprofloxacin, and formyl ciprofloxacin. Approximately 40-50% of the dose is excreted unchanged in urine via glomerular filtration and tubular secretion.
Excretion	Renal (50-70% unchanged via glomerular filtration and tubular secretion); biliary/fecal (15-20%, primarily as metabolites); small amount metabolized to 4 metabolites (oxo-, sulfo-, and desethylene-ciprofloxacin).
Half-life	Terminal elimination half-life: 3-5 hours (normal renal function), extended to 8-10 hours in mild-to-moderate renal impairment (CrCl 30-50 mL/min) and up to >10 hours in severe impairment (CrCl <30 mL/min); half-life in elderly may be 5-8 hours due to reduced clearance.
Protein binding	20-40% bound to serum proteins (primarily albumin).
Volume of Distribution	2.1-2.8 L/kg (extensive, indicating penetration into tissues; high concentrations in lung, prostate, bone, and urogenital tissues; crosses blood-brain barrier with inflamed meninges).
Bioavailability	Oral: 70-80% (range 50-85%); decreased by 25-30% with concurrent antacids or calcium, iron, zinc supplements. Intravenous: 100%.
Onset of Action	Oral: 30-90 minutes (peak serum concentration 1-2 hours). Intravenous: immediate (peak at end of infusion). Topical (ophthalmic/otic): within 15-30 minutes.
Duration of Action	Antibacterial effect persists for approximately 12 hours post-dose (based on serum levels above MIC for most susceptible organisms); recommended dosing interval is 12 hours. Prolonged in renal impairment.

Classification & Brands

Action Class	Quinolones/ Fluroquinolones
Brand Substitutes	Wocipflo 500mg Tablet, Strox 500mg Tablet, Ciprodac 500 Tablet, Alciflox 500mg Tablet, Cifran OD 500mg Tablet, Cyprine FC 250mg Tablet, Cyprine 250mg Tablet, Ciprokind 250mg Tablet, Floxip 250 Tablet, Ciprodac 250 Tablet

Dosing & administration

Ciprofloxacin 500 mg PO q12h or 400 mg IV q12h for uncomplicated infections; 750 mg PO q12h or 400 mg IV q8h for severe/complicated infections.

Dosage form	FOR SUSPENSION
Renal impairment	CrCl 30-50 mL/min: 250-500 mg PO q12h or 200-400 mg IV q12h; CrCl 5-29 mL/min: 250-500 mg PO q18h or 200-400 mg IV q18-24h; hemodialysis: 250-500 mg PO q24h post-dialysis or 200-400 mg IV q24h.
Liver impairment	No dose adjustment required for mild-moderate hepatic impairment (Child-Pugh A/B). Use with caution in severe impairment (Child-Pugh C) due to limited data; monitor for adverse effects.
Pediatric use	Complicated UTI/pyelonephritis: 10-20 mg/kg IV q8h (max 400 mg/dose) or 10-20 mg/kg PO q12h (max 750 mg/dose); inhalational anthrax: 15 mg/kg IV q12h (max 400 mg/dose) or 15 mg/kg PO q12h (max 500 mg/dose).
Geriatric use	Start at lower end of dosing range due to age-related renal decline; monitor renal function and adjust dose per renal adjustment; increased risk of tendonitis/tendon rupture and CNS effects (dizziness, confusion).

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for CIPRO (CIPRO).

Breastfeeding	Ciprofloxacin excreted into breast milk (M/P ratio ~0.83). Safety not established; use caution due to potential arthropathy in nursing infants. American Academy of Pediatrics: usually compatible, but alternatives preferred.
Teratogenic Risk	Ciprofloxacin is contraindicated in pregnancy due to arthropathy risk in juvenile animals. First trimester: limited human data; animal studies show cartilage damage; avoid. Second/third trimesters: potential fetal cartilage toxicity; avoid use.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Fluoroquinolones, including ciprofloxacin, are associated with an increased risk of tendinitis and tendon rupture in all ages. This risk is further increased in patients over 60 years of age, those taking corticosteroids, and those with kidney, heart, or lung transplants. Fluoroquinolones may exacerbate muscle weakness in persons with myasthenia gravis. Avoid in patients with a history of myasthenia gravis.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to ciprofloxacin or any fluoroquinolone","Concurrent use with tizanidine (due to CYP1A2 inhibition)","History of tendinitis or tendon rupture with fluoroquinolone use","Myasthenia gravis"]

Clinical Precautions

Precautions

["Tendinitis and tendon rupture (black box warning)","Exacerbation of myasthenia gravis","CNS effects including seizures, dizziness, and confusion","Peripheral neuropathy","QT prolongation","Clostridium difficile-associated diarrhea","Photosensitivity","Hepatotoxicity","Renal impairment (dose adjustment required)","Hypersensitivity reactions","Aortic aneurysm and dissection (rare)"]

Clinical Tips & Counseling

Drug interactions

Loading safety data…

CIPRO

Clinical safety rating: caution

Comprehensive clinical and safety monograph for CIPRO (CIPRO).

How it works

Ciprofloxacin inhibits bacterial DNA gyrase and topoisomerase IV, preventing DNA replication and transcription, leading to bacterial cell death.

What the body does with it

Metabolism	Ciprofloxacin is metabolized in the liver via CYP1A2, producing 4 metabolites: desethylene ciprofloxacin (major), N-acetyl ciprofloxacin, oxo-ciprofloxacin, and formyl ciprofloxacin. Approximately 40-50% of the dose is excreted unchanged in urine via glomerular filtration and tubular secretion.
Excretion	Renal (50-70% unchanged via glomerular filtration and tubular secretion); biliary/fecal (15-20%, primarily as metabolites); small amount metabolized to 4 metabolites (oxo-, sulfo-, and desethylene-ciprofloxacin).
Half-life	Terminal elimination half-life: 3-5 hours (normal renal function), extended to 8-10 hours in mild-to-moderate renal impairment (CrCl 30-50 mL/min) and up to >10 hours in severe impairment (CrCl <30 mL/min); half-life in elderly may be 5-8 hours due to reduced clearance.
Protein binding	20-40% bound to serum proteins (primarily albumin).
Volume of Distribution	2.1-2.8 L/kg (extensive, indicating penetration into tissues; high concentrations in lung, prostate, bone, and urogenital tissues; crosses blood-brain barrier with inflamed meninges).
Bioavailability	Oral: 70-80% (range 50-85%); decreased by 25-30% with concurrent antacids or calcium, iron, zinc supplements. Intravenous: 100%.
Onset of Action	Oral: 30-90 minutes (peak serum concentration 1-2 hours). Intravenous: immediate (peak at end of infusion). Topical (ophthalmic/otic): within 15-30 minutes.
Duration of Action	Antibacterial effect persists for approximately 12 hours post-dose (based on serum levels above MIC for most susceptible organisms); recommended dosing interval is 12 hours. Prolonged in renal impairment.

Classification & Brands

Action Class	Quinolones/ Fluroquinolones
Brand Substitutes	Wocipflo 500mg Tablet, Strox 500mg Tablet, Ciprodac 500 Tablet, Alciflox 500mg Tablet, Cifran OD 500mg Tablet, Cyprine FC 250mg Tablet, Cyprine 250mg Tablet, Ciprokind 250mg Tablet, Floxip 250 Tablet, Ciprodac 250 Tablet

Dosing & administration

Ciprofloxacin 500 mg PO q12h or 400 mg IV q12h for uncomplicated infections; 750 mg PO q12h or 400 mg IV q8h for severe/complicated infections.

Dosage form	FOR SUSPENSION
Renal impairment	CrCl 30-50 mL/min: 250-500 mg PO q12h or 200-400 mg IV q12h; CrCl 5-29 mL/min: 250-500 mg PO q18h or 200-400 mg IV q18-24h; hemodialysis: 250-500 mg PO q24h post-dialysis or 200-400 mg IV q24h.
Liver impairment	No dose adjustment required for mild-moderate hepatic impairment (Child-Pugh A/B). Use with caution in severe impairment (Child-Pugh C) due to limited data; monitor for adverse effects.
Pediatric use	Complicated UTI/pyelonephritis: 10-20 mg/kg IV q8h (max 400 mg/dose) or 10-20 mg/kg PO q12h (max 750 mg/dose); inhalational anthrax: 15 mg/kg IV q12h (max 400 mg/dose) or 15 mg/kg PO q12h (max 500 mg/dose).
Geriatric use	Start at lower end of dosing range due to age-related renal decline; monitor renal function and adjust dose per renal adjustment; increased risk of tendonitis/tendon rupture and CNS effects (dizziness, confusion).

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for CIPRO (CIPRO).

Breastfeeding	Ciprofloxacin excreted into breast milk (M/P ratio ~0.83). Safety not established; use caution due to potential arthropathy in nursing infants. American Academy of Pediatrics: usually compatible, but alternatives preferred.
Teratogenic Risk	Ciprofloxacin is contraindicated in pregnancy due to arthropathy risk in juvenile animals. First trimester: limited human data; animal studies show cartilage damage; avoid. Second/third trimesters: potential fetal cartilage toxicity; avoid use.
Fetal Monitoring