ciprofloxacin (Rx)

1-10%

Nausea (3%)

Abdominal pain (2%)

Diarrhea (2% adults; 5% children)

Increased aminotransferase levels (2%)

Vomiting (1% adults; 5% children)

Headache (1%)

Increased serum creatinine (1%)

Rash (2%)

Restlessness (1%)

<1%

Acidosis

Allergic reaction

Angina pectoris

Anorexia

Arthralgia

Ataxia

Back pain

Bad taste

Blurred vision

Breast pain

Bronchospasm

Diplopia

Dizziness

Drowsiness

Dysphagia

Dyspnea

Flushing

Foot pain

Hallucinations

Hiccups

Hypertension

Hypotension

Insomnia

Irritability

Joint stiffness

Lethargy

Migraine

Nephritis

Nightmares

Oral candidiasis

Palpitation

Photosensitivity

Polyuria

Syncope

Tachycardia

Tinnitus

Tremor

Urinary retention

Vaginitis

Postmarketing Reports

Acute generalized exanthematous pustulosis (AGEP), erythema multiforme, exfoliative dermatitis, fixed eruption, photosensitivity/phototoxicity reaction

Agitation, confusion, delirium

Agranulocytosis, albuminuria, serum cholesterol and TG elevations, blood glucose disturbances, hemolytic anemia, marrow depression (life threatening), pancytopenia (life threatening or fatal outcome), potassium elevation (serum)

Anaphylactic reactions (including life-threatening anaphylactic shock), serum sickness like reaction, Stevens-Johnson syndrome

Anosmia, hypesthesia

Constipation, dyspepsia, dysphagia, flatulence, hepatic failure (including fatal cases), hepatic necrosis, jaundice, pancreatitis

Hypertonia, hypotension (postural), increased INR (in patients treated with Vitamin K antagonists), QT prolongation, torsade de pointes, ventricular arrhythmia

Methemoglobinemia

Myasthenia, exacerbation of myasthenia gravis, myoclonus, nystagmus, peripheral neuropathy that may be irreversible, phenytoin alteration (serum), polyneuropathy, psychosis

Myalgia, tendinitis, tendon rupture, toxic epidermal necrolysis (Lyell’s Syndrome), twitching

Infections: Candiduria, vaginal candidiasis, moniliasis (oral, gastrointestinal, vaginal), pseudomembranous colitis

Renal calculi

Vasculitis

Aortic aneurysm and dissection

Contraindications

Documented hypersensitivity; concurrent tizanidine administration

Cautions

Use in pregnancy, though generally contraindicated for all quinolones, is allowed for life-threatening situations; limited data from use of ciprofloxacin in pregnancy show no higher rate of birth defects than background

Do not use oral suspension in nasogastric tube; to prepare, add microcapsules to diluent

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 therapy, including in patients of any age or without pre-existing risk factors; discontinue therapy immediately at first signs or symptoms of any serious adverse reaction; in addition, avoid use of fluoroquinolones, in patients who have experienced any serious adverse reactions associated with fluoroquinolones (see Black Box Warnings)

Peripheral neuropathy: sensory or sensorimotor axonal polyneuropathy affecting small and/or large axons resulting in paresthesias, hypoesthesias, dysesthesias, and weakness reported; peripheral neuropathy may occur rapidly after initiating and may potentially become permanent

In prolonged therapy, perform periodic evaluations of organ system functions (eg, renal, hepatic, hematopoietic); adjust dose in renal impairment; superinfections may occur with prolonged or repeated antibiotic therapy; discontinue use immediately if signs and symptoms of hepatitis occur

Not first drug of choice in pediatrics (except in anthrax), because of increased incidence of adverse events in comparison with control subjects, including arthropathy; no data exist on dosing for pediatric patients with renal impairment (ie, CrCl <50 mL/min)

Crystalluria may occur; urine alkalinity may increase risk; ensure adequate hydration during therapy

Serious and sometimes fatal hypoglycemia reported with fluoroquinolone use; hyperglycemia also reported; monitor patients closely for signs/symptoms of abnormal glucose levels; if hypoglycemic reaction occurs in a patient being treated discontinue therapy and initiate appropriate treatment immediately

Moderate-to-severe phototoxicity reactions reported; avoid excessive sunlight and take precautions to limit exposure; discontinue use if phototoxicity occurs

Acute onset of retinal detachment increased 4.5-fold with oral fluoroquinolones in a single case-controlled study - JAMA 2012;307(13):1414-1419; another study disputes these findings (relative risk, 1.29) - JAMA 2013;310(20):2184-2190

Clostridium difficile-associated diarrhea (CDAD) reported; if CDAD suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued; appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated

Prescribing antibiotics in absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to patient and increases risk of development of drug-resistant bacteria

Fluoroquinolones may exacerbate muscle weakness in patients with myasthenia gravis; postmarketing serious adverse reactions, including deaths and requirement for ventilatory support, have been associated with fluoroquinolone use in patients with myasthenia gravis; avoid in patients with known history of myasthenia gravis

Mechanism of Action

Inhibits relaxation of DNA; inhibits DNA gyrase in susceptible organisms; promotes breakage of double-stranded DNA

Absorption

Bioavailability (PO): ~50-85%

Peak plasma time (PO): Immediate-release, 0.5-2 hr; extended-release, 1-2.5 hr

Distribution

Distributed widely throughout body; tissue concentrations often exceed serum concentrations, especially in kidneys, gallbladder, liver, lungs, gynecologic tissue, and prostatic tissue; cerebrospinal fluid (CSF) concentration is 10% in noninflamed meninges and 14-37% in inflamed meninges; crosses placenta; enters breast milk

Protein bound: 20-40%

Vd: 2.1-2.7 L/kg

Metabolism

Metabolized in liver

Enzyme inhibitor: CYP1A2

Elimination

Half-life: 2-5 hr (children); 3-5 hr (adults)

Excretion: Urine (30-50%), feces (15-43%)

IV Incompatibilities

Additive: Aminophylline, amoxicillin, amoxicillin-clavulanate, amphotericin, ampicillin-sulbactam, ceftazidime, cefuroxime, clindamycin, floxacillin, heparin, piperacillin, sodium bicarbonate, ticarcillin

Y-site: Aminophylline, ampicillin-sulbactam, azithromycin, cefepime, dexamethasone sodium phosphate, furosemide, heparin, hydrocortisone sodium succinate, magnesium sulfate(?), methylprednisolone sodium succinate, phenytoin, potassium phosphates, propofol, sodium bicarbonate(?), sodium phosphates, total parenteral nutrition formulations, warfarin

IV Compatibilities

Solution: Compatible with most IV fluids

Additive: Amikacin, aztreonam, dobutamine, dopamine, fluconazole, gentamicin, lidocaine, linezolid, metronidazole (ready-to-use form is compatible; hydrochloride form in vial is incompatible), midazolam, potassium chloride, tobramycin

Y-site: Amiodarone, calcium gluconate, clarithromycin, digoxin, diphenhydramine, dobutamine, dopamine, linezolid, lorazepam, midazolam, promethazine, quinupristin/dalfopristin, tacrolimus

IV Administration

Infuse 1-2 mg/mL (diluted in D5W or NS) into large vein over 60 minutes

When administering intermittently through Y-site, temporarily discontinue primary solution

Stability

Stable at concentration of 0.5-2 mg/mL in D5W or NS for 14 days at room temperature or refrigerated