Chemical formula: C₁₇H₁₈FN₃O₃ Molecular mass: 331.342 g/mol PubChem compound: 2764
Ciprofloxacin interacts in the following cases:
Ciprofloxacin, like other fluoroquinolones, should be used with caution in patients receiving drugs known to prolong QT interval (e.g. Class IA and III anti-arrhythmics, tricyclic antidepressants, macrolides, antipsychotics).
Caution should be taken when using fluoroquinolones, including ciprofloxacin in patients with known risk factors for prolongation of the QT interval such as congenital long QT syndrome.
Recommended starting and maintenance doses for patients with impaired renal function: 200-400 mg every 12h intravenous and 250-500 mg every 12h pos.
Recommended starting and maintenance doses for patients with impaired renal function: 200-400 mg every 24h intravenous and 250-500 mg every 24h pos.
Simultaneous administration of ciprofloxacin with a vitamin K antagonist may augment its anti-coagulant effects. The risk may vary with the underlying infection, age and general status of the patient so that the contribution of ciprofloxacin to the increase in INR (international normalised ratio) is difficult to assess. The INR should be monitored frequently during and shortly after co-administration of ciprofloxacin with a vitamin K antagonist (e.g. warfarin, acenocoumarol, phenprocoumon, or fluindione).
It is recommended not to use opioids during the perioperative period in patients receiving ciprofloxacin.
Azlocillin given intravenously causes an increase in ciprofloxacin concentrations.
On concurrent administration of ciprofloxacin and caffeine or pentoxifylline (oxpentifylline), raised serum concentrations of these xanthine derivatives were reported.
A transient rise in the concentration of serum creatinine was observed when ciprofloxacin and cyclosporin containing medicinal products were administered simultaneously. Therefore, it is frequently (twice a week) necessary to control the serum creatinine concentrations in these patients.
Following concomitant administration of 250 mg ciprofloxacin with clozapine for 7 days, serum concentrations of clozapine and N-desmethylclozapine were increased by 29% and 31%, respectively. Clinical surveillance and appropriate adjustment of clozapine dosage during and shortly after co-administration with ciprofloxacin are advised.
In clinical studies, it was demonstrated that concomitant use of duloxetine with strong inhibitors of the CYP450 1A2 isozyme such as fluvoxamine, may result in an increase of AUC and Cmax of duloxetine. Although no clinical data are available on a possible interaction with ciprofloxacin, similar effects can be expected upon concomitant administration.
In particular cases, concurrent administration of ciprofloxacin and glibenclamide containing medicinal products can intensify the action of glibenclamide (hypoglycaemia).
It was demonstrated in healthy subjects that concomitant use of lidocaine containing medicinal products with ciprofloxacin, a moderate inhibitor of CYP450 1A2 isozyme, reduces clearance of intravenous lidocaine by 22%. Although lidocaine treatment was well tolerated, a possible interaction with ciprofloxacin associated with side effects may occur upon concomitant administration.
Renal tubular transport of methotrexate may be inhibited by concomitant administration of ciprofloxacin, potentially leading to increased plasma levels of methotrexate and increased risk of methotrexate-associated toxic reactions. The concomitant use is not recommended.
Metoclopramide accelerates the absorption of ciprofloxacin (oral) resulting in a shorter time to reach maximum plasma concentrations. No effect was seen on the bioavailability of ciprofloxacin.
Concomitant administration of ciprofloxacin and omeprazole containing medicinal products results in a slight reduction of Cmax and AUC of ciprofloxacin.
Simultaneous administration of ciprofloxacin and phenytoin may result in increased or reduced serum levels of phenytoin such that monitoring of drug levels is recommended.
Probenecid interferes with renal secretion of ciprofloxacin. Co-administration of probenecid and ciprofloxacin increases ciprofloxacin serum concentrations.
It was shown in a clinical study that concomitant use of ropinirole with ciprofloxacin, a moderate inhibitor of the CYP450 1A2 isozyme, results in an increase of Cmax and AUC of ropinirole by 60% and 84%, respectively. Monitoring of ropinirole-related side effects and dose adjustment as appropriate is recommended during and shortly after co-administration with ciprofloxacin.
Cmax and AUC of sildenafil were increased approximately twofold in healthy subjects after an oral dose of 50 mg given concomitantly with 500 mg ciprofloxacin. Therefore, caution should be used prescribing ciprofloxacin concomitantly with sildenafil taking into consideration the risks and the benefits.
Concurrent administration of ciprofloxacin and theophylline can cause an undesirable increase in serum theophylline concentration. This can lead to theophylline-induced side effects that may rarely be life threatening or fatal. During the combination, serum theophylline concentrations should be checked and the theophylline dose reduced as necessary.
Co-administration ciprofloxacin may increase blood levels of zolpidem, concurrent use is not recommended.
Haemolytic reactions have been reported with ciprofloxacin in patients with glucose-6-phosphate dehydrogenase deficiency. Ciprofloxacin should be avoided in these patients unless the potential benefit is considered to outweigh the possible risk. In this case, potential occurrence of haemolysis should be monitored.
Psychiatric reactions may occur even after the first administration of ciprofloxacin. In rare cases, depression or psychosis can progress to suicidal ideations/thoughts culminating in attempted suicide or completed suicide. In the occurrence of such cases, ciprofloxacin should be discontinued.
Ciprofloxacin should generally not be used in patients with a history of tendon disease/disorder related to quinolone treatment. Nevertheless, in very rare instances, after microbiological documentation of the causative organism and evaluation of the risk/benefit balance, ciprofloxacin may be prescribed to these patients for the treatment of certain severe infections, particularly in the event of failure of the standard therapy or bacterial resistance, where the microbiological data may justify the use of ciprofloxacin.
Tendinitis and tendon rupture (especially Achilles tendon), sometimes bilateral, may occur with ciprofloxacin, even within the first 48 hours of treatment. Inflammation and ruptures of tendon may occur even up to several months after discontinuation of ciprofloxacin therapy The risk of tendinopathy may be increased in elderly patients or in patients concomitantly treated with corticosteroids.
At any sign of tendinitis (e.g. painful swelling, inflammation), ciprofloxacin treatment should be discontinued. Care should be taken to keep the affected limb at rest.
Ciprofloxacin should be used with caution in patients with myasthenia gravis.
The occurrence of severe and persistent diarrhoea during or after treatment (including several weeks after treatment) may indicate an antibiotic-associated colitis (life-threatening with possible fatal outcome), requiring immediate treatment. In such cases, ciprofloxacin should immediately be discontinued, and an appropriate therapy initiated. Anti-peristaltic drugs are contraindicated in this situation.
Cases of hepatic necrosis and life-threatening hepatic failure have been reported with ciprofloxacin. In the event of any signs and symptoms of hepatic disease (such as anorexia, jaundice, dark urine, pruritus, or tender abdomen), treatment should be discontinued.
Crystalluria related to the use of ciprofloxacin has been reported. Patients receiving ciprofloxacin should be well hydrated and excessive alkalinity of the urine should be avoided.
Epidemiologic studies report an increased risk of aortic aneurysm and dissection after intake of fluoroquinolones, particularly in the older population.
Therefore, fluoroquinolones should only be used after careful benefit-risk assessment and after consideration of other therapeutic options in patients with positive family history of aneurysm disease, or in patients diagnosed with pre-existing aortic aneurysm and/or aortic dissection, or in presence of other risk factors or conditions predisposing for aortic aneurysm and dissection (e.g. Marfan syndrome, vascular Ehlers-Danlos syndrome, Takayasu arteritis, giant cell arteritis, Behcet’s disease, hypertension, known atherosclerosis).
Ciprofloxacin has been shown to cause photosensitivity reactions. Patients taking ciprofloxacin should be advised to avoid direct exposure to either extensive sunlight or UV irradiation during treatment.
Cases of polyneuropathy (based on neurological symptoms such as pain, burning, sensory disturbances or muscle weakness, alone or in combination) have been reported in patients receiving ciprofloxacin. Ciprofloxacin should be discontinued in patients experiencing symptoms of neuropathy, including pain, burning, tingling, numbness, and/or weakness in order to prevent the development of an irreversible condition.
Ciprofloxacin like other quinolones are known to trigger seizures or lower the seizure threshold. Cases of status epilepticus have been reported. Ciprofloxacin should be used with caution in patients with CNS disorders which may be predisposed to seizure. If seizures occur ciprofloxacin should be discontinued.
The data that are available on administration of ciprofloxacin to pregnant women indicates no malformative or foeto/neonatal toxicity of ciprofloxacin. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. In juvenile and prenatal animals exposed to quinolones, effects on immature cartilage have been observed, thus, it cannot be excluded that the drug could cause damage to articular cartilage in the human immature organism/foetus.
As a precautionary measure, it is preferable to avoid the use of ciprofloxacin during pregnancy.
There are no adequate data from the use of ciprofloxacin in pregnant woman. Animal studies do not indicate direct harmful effects with respect to reproductive toxicity. Systemic exposure to ciprofloxacin after topical use is expected to be low.
As a precautionary measure, it is preferable to avoid the use of ciprofloxacin during pregnancy, unless the therapeutic benefit is expected to outweigh the potential risk to the fetus.
There are no data on the use of ciprofloxacin otic solution 0.2% in pregnant women. There are moderate amount of data from the use oral ciprofloxacin in pregnant women. No reproductive toxicity has been performed after otic administration. However after systemic exposure, animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity.
Since systemic exposure to ciprofloxacin is negligible after otic administration, thus no effects are anticipated during pregnancy. Ciprofloxacin can be used during pregnancy.
Ciprofloxacin is excreted in breast milk. Due to the potential risk of articular damage, ciprofloxacin should not be used during breast-feeding.
Orally administered ciprofloxacin is excreted in the human milk. It is unknown whether ciprofloxacin is excreted in human breast milk following topical ocular or otic administration. A risk to the suckling child cannot be excluded. Therefore, caution should be exercised when ciprofloxacin is administered to nursing women.
Ciprofloxacin is excreted in human milk after systemic use. It is not known whether ciprofloxacin is excreted in human milk after otic use. No effects on the breast-fed newborn are anticipated since the systemic exposure of the breast-feeding woman to ciprofloxacin is negligible. Cetraxal can be used during breast-feeding.
Studies have not been performed in humans to evaluate the effect of topical administration of ciprofloxacin on fertility. Oral administration in animals does not indicate direct harmful effects with respect to fertility.
Due to its neurological effects, ciprofloxacin may affect reaction time. Thus, the ability to drive or to operate machinery may be impaired.
This product has no or negligible influence on the ability to drive or use machines.
Temporarily blurred vision or other visual disturbances may affect the ability to drive or use machines. If transient blurred vision occurs upon instillation, the patient must wait until the vision clears before driving or using machinery.
Ciprofloxacin has no or negligible influence on the ability to drive and use machines.
The most commonly reported adverse drug reactions (ADRs) are nausea, diarrhoea, vomiting, transient increase in transaminases, rash, and injection and infusion site reactions.
ADRs derived from clinical studies and post-marketing surveillance with Ciprofloxacin (oral, intravenous and sequential therapy) sorted by categories of frequency are listed below. The frequency analysis takes into account data from both oral and intravenous administration of ciprofloxacin.
Common ≥1/100 to <1/10, Uncommon ≥1/1,000 to <1/100, Rare ≥1/10,000 to <1/1,000, Very Rare <1/10,000, Frequency not known (cannot be estimated from available data)
Uncommon: Mycotic superinfections
Uncommon: Eosinophilia
Rare: Leukopenia, Anaemia, Neutropenia, Leukocytosis, Thrombocytopenia, Thrombocytaemia
Very Rare: Haemolytic anaemia, Agranulocytosis, Pancytopenia (life-threatening), Bone marrow depression (life-threatening)
Rare: Allergic reaction, Allergic oedema/angio-oedema
Very Rare: Anaphylactic reaction, Anaphylactic shock (life-threatening), Serum sickness-like reaction
Uncommon: Decreased appetite
Rare: Hyperglycaemia, Hypoglycaemia
Uncommon: Psychomotor hyperactivity/agitation
Rare: Confusion and disorientation, Anxiety reaction, Abnormal dreams, Depression (potentially culminating in suicidal ideations/thoughts or suicide attempts and completed suicide), Hallucinations
Very Rare: Psychotic reactions (potentially culminating in suicidal ideations/thoughts or suicide attempts and completed suicide)
Frequency not known: Mania, hypomania
Uncommon: Headache, Dizziness, Sleep disorders, Taste disorders
Rare: Par- and Dysaesthesia, Hypoaesthesia, Tremor, Seizures (incl. status epilepticus), Vertigo
Very Rare: Migraine, Disturbed coordination, Gait disturbance, Olfactory nerve disorders, Intracranial hypertension and pseudomotor cerebri
Frequency not known: Peripheral neuropathy and polyneuropathy
Rare: Visual disturbances e.g. diplopia
Very Rare: Visual colour distortions
Rare: Tinnitus, Hearing loss/Hearing impaired
Rare: Tachycardia
Frequency not known: Ventricular arrhythmia and torsades de pointes* (reported predominantly in patients with risk factors for QT prolongation), ECG QT prolongation
Rare: Vasodilatation, Hypotension, Syncope
Very Rare: Vasculitis
Rare: Dyspnoea (including asthmatic condition)
Common: Nausea, Diarrhoea
Uncommon: Vomiting, Gastrointestinal and abdominal pains, Dyspepsia, Flatulence
Rare: Antibiotic associated diarrhoea including pseudomembraneous colitis
Very Rare: Pancreatitis
Increase in transaminases
Increased bilirubin
Rare: Hepatic impairment, Cholestatic icterus, Hepatitis
Very Rare: Liver necrosis (very rarely progressing to life-threatening hepatic failure)
Uncommon: Rash, Pruritus, Urticaria
Rare: Photosensitivity reactions
Very Rare: Petechiae, Erythema multiforme, Erythema nodosum, Stevens-Johnson syndrome (potentially life-threatening), Toxic epidermal necrolysis (potentially life-threatening)
Frequency not known: Acute generalised exanthematous pustulosis (AGEP); Drug reaction with Eosinophilia and Systemic Symptoms (DRESS)
Uncommon: Musculoskeletal pain (e.g. extremity pain, back pain, chest pain), Arthralgia
Rare: Myalgia, Arthritis, Increased muscle tone and cramping
Very Rare: Muscular weakness, Tendinitis, Tendon rupture (predominantly Achilles tendon), Exacerbation of symptoms of myasthenia gravis
Uncommon: Renal impairment
Rare: Renal failure Haematuria, Crystalluria, Tubulointerstitial nephritis
Common: Injection and infusion site reactions (only intravenous administration)
Uncommon: Asthenia, Fever
Rare: Oedema, Sweating (hyperhidrosis)
Frequency not known: Syndrome of inappropriate secretion of antidiuretic hormone (SIADH)
Uncommon: Increase in blood alkaline phosphatase
Rare: Prothrombin level abnormal, Increased amylase
Frequency not known: International normalised ratio increased (in patients treated with Vitamin K antagonists)
* These events were reported during the postmarketing period and were observed predominantly among patients with further risk factors for QT prolongation
The following undesirable effects have a higher frequency category in the subgroups of patients receiving intravenous or sequential (intravenous to oral) treatment:
Common: Vomiting, Transient increase in transaminases, Rash
Uncommon: Thrombocytopenia, Thrombocytaemia, Confusion and disorientation, Hallucinations, Par- and dysaesthesia, Seizures, Vertigo, Visual disturbances, Hearing loss, Tachycardia, Vasodilatation, Hypotension, Transient hepatic impairment, Cholestatic icterus, Renal failure, Oedema
Rare: Pancytopenia, Bone marrow depression, Anaphylactic shock, Psychotic reactions, Migraine, Olfactory nerve disorders, Hearing impaired, Vasculitis, Pancreatitis, Liver necrosis, Petechiae, Tendon rupture
The incidence of arthropathy, mentioned above, is referring to data collected in studies with adults. In children, arthropathy is reported to occur commonly.
In clinical trials, the most frequently reported adverse drug reactions were ocular discomfort, dysgeusia and corneal deposits occurring approximately in 6%, 3% and 3% of patients respectively.
The adverse reactions listed below are classified according to the following convention: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000), or not known (cannot be estimated from the available data). Within each frequency-grouping, adverse reactions are presented in order of decreasing seriousness. The adverse reactions have been observed during clinical trials and post-marketing experience.
The following undesirable effects were reported in association with the ophthalmic use of ciprofloxacin:
Rare: hypersensitivity
Uncommon: headache
Rare: dizziness
Common: corneal deposits, ocular discomfort, ocular hyperaemia
Uncommon: keratopathy, punctate keratitis, corneal infiltrates, photophobia, visual acuity reduced, eyelid oedema, blurred vision, eye pain, dry eye, eye swelling, eye pruritus, lacrimation increased, eye discharge, eyelid margin crusting, eyelid exfoliation, conjunctival oedema, erythema of eyelid
Rare: ocular toxicity, keratitis, conjunctivitis, corneal epithelium defect, diplopia, hypoaesthesia eye, asthenopia, eye irritation, eye inflammation, hordeolum
Rare: ear pain
Rare: paranasal sinus hypersecretion, rhinitis
Common: dysgeusia
Uncommon: nausea
Rare: diarrhoea, abdominal pain
Rare: dermatitis
Not known: tendon disorder
With locally applied fluoroquinolones (generalized) rash, toxic epidermolysis, dermatitis exfoliative, Stevens-Johnson syndrome and urticaria occur very rarely.
Serious and occasionally fatal hypersensitivity (anaphylactic) reactions, some following the first dose, have been reported in patients receiving systemic quinolone therapy. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, tingling, pharyngeal or facial oedema, dyspnoea, urticaria, and itching.
Ruptures of the shoulder, hand, Achilles, or other tendons that required surgical repair or resulted in prolonged disability have been reported in patients receiving systemic fluoroquinolones. Studies and post marketing experience with systemic fluoroquinolones indicate that the risk of these ruptures may be increased in patients receiving corticosteroids, especially geriatric patients and in tendons under high stress, including the Achilles tendon. To date, clinical and post marketing data have not demonstrated a clear association between ciprofloxacin and musculoskeletal and connective tissue adverse reactions.
In isolated cases blurred vision, decreased visual acuity and medication residue have been observed with ophthalmic ciprofloxacin.
Moderate to severe phototoxicity has been observed in patients treated with systemic quinolones. Nevertheless, phototoxic reactions to ciprofloxacin are uncommon.
Safety and effectiveness of ciprofloxacin 3mg/ml eye drops were determined in 230 children between the ages of 0 and 12 years of age. No serious adverse drug reaction was reported in this group of patients.
In a Phase III clinical trial, a total of 319 patients were treated with ciprofloxacin.
The most commonly reported adverse reactions are: ear pruritus occurring in 0.9% of patients treated with ciprofloxacin, and headache and application site pain, both occurring in approximately 0.6% of patients.
All treatment related adverse reactions are uncommon (≥1/1000 to <1/100) and are listed below.
Uncommon: Ear pruritus, tinnitus
Uncommon: Dizziness, headache
Uncommon: Dermatitis
Uncommon: Application Site Pain
With locally applied fluoroquinolones (generalized) rash, toxic epidermolysis, dermatitis exfoliative, Stevens-Johnson syndrome, and urticaria occur very rarely.
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