EXOCIN - PACKAGE LEAFLET - LEAFLETS

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Exocin - Package Leaflet

Indications Contraindications Precautions for use Interactions Warnings Dosage and method of use Overdose Undesirable Effects Shelf life and Storage Composition and pharmaceutical form

Active ingredients: Ofloxacin

EXOCIN 3 mg / ml eye drops, solution

Exocin package inserts are available for pack sizes:

EXOCIN 3 mg / ml eye drops, solution
EXOCIN 0.3% ointment

Why is Exocin used? What is it for?

PHARMACOTHERAPEUTIC CATEGORY

Ophthalmologicals, other antimicrobials

THERAPEUTIC INDICATIONS

EXOCIN 3 mg / ml eye drops is indicated for the treatment of external ocular infections caused by germs sensitive to ofloxacin, such as blepharitis, conjunctivitis, blepharoconjunctivitis, keratoconjunctivitis, dacryocystitis, keratitis, infectious corneal ulcers of bacterial origin, meibomitis, and for post prophylaxis -operative.

Contraindications When Exocin should not be used

Hypersensitivity to the active substance, to any of the excipients of the product or to other quinolones

Precautions for use What you need to know before taking Exocin

Ophthalmic Use: Do not use for injections or intraocular use. The use of contact lenses is not recommended in patients receiving therapy for ocular infection. The use of EXOCIN should be monitored in patients who have shown sensitivity to other quinolones.

The safety and efficacy of the product in infants less than one year of age have not been established therefore its use is not recommended.

Babies

The information on the use of EXOCIN in neonates in the treatment of conjunctivitis is very limited. The use of EXOCIN in neonates with ophthalmia neonatorum caused by Neisseria gonorrhoeae or Chlamydia trachomatis has not been evaluated as the use of the product in such patients. Therefore, it is necessary to consult the physician in order to determine the advisability of a treatment of the newborn with EXOCIN.

Interactions Which drugs or foods may change the effect of Exocin

Tell your doctor or pharmacist if you have recently taken any other medicines, even those without a prescription.

You should tell your doctor if you are taking other medicines that can alter the heart rhythm: medicines that belong to the class of anthythmics (for example quinidine, hydroquinidine, disopyramide, amiodarone, sotalol, dofetilite, ibutilide), tricyclic antidepressants, some antimicrobials (which belong to the macrolide class), some antipsychotics.

Systemic administration of some quinolones has been shown to inhibit the metabolic elimination of caffeine and theophylline. Drug interaction studies conducted with systemic ofloxacin have shown that the metabolic elimination of caffeine and theophylline are not significantly affected. from ofloxacin.

Although there have been reports of an "increased prevalence of CNS toxicity at systemic doses of fluoroquinolones when used concomitantly with non-steroidal anti-inflammatory drugs (NSAIDs), this has not been reported in the concomitant systemic use of NSAIDs and ofloxacin.

Warnings It is important to know that:

Severe and sporadic hypersensitivity reactions (anaphylactic / anaphylactoid) with fatal outcome, some following the first dose, have been reported in patients receiving systemic quinolones, including ofloxacin. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, angioedema (including laryngeal, pharyngeal, or facial edema), airway obstruction, dyspnoea, hives, and pruritus.

If an allergic reaction to ofloxacin occurs, discontinue administration of the drug. Patients who have shown sensitivity to other quinolone antibacterial agents should use EXOCIN with caution.

Prolonged use may cause a new bacterial infection which cannot be sufficiently treated with EXOCIN.

When using EXOCIN, the risk of nasopharyngeal passage which may contribute to the occurrence and spread of bacterial resistance must be considered. Like any other antibiotic, prolonged use can cause excessive development of non-sensitive microorganisms, in this case and if no improvement is noticed after a reasonable period of time, discontinue use and consult your eye doctor.

Stevens-Johnson syndrome has been reported in patients who received topical ophthalmic ofloxacin, but no causal relationship with the drug has been demonstrated.

Clinical and non-clinical publications have reported the occurrence of corneal perforation in patients with pre-existing corneal epithelial defect or corneal ulcer following topical treatment with fluoroquinolone antibiotics. However, significant elements of confusion were found in many of these reports, such as advanced age, presence of large ulcers, concomitant eye conditions (e.g. severe dry eye), systemic inflammatory conditions (e.g. rheumatoid arthritis), and concomitant use of steroids. ocular or non-steroidal anti-inflammatory drugs. However, care should be taken regarding the risk of corneal perforation when using the product for the treatment of patients with corneal epithelial defects or corneal ulcers.

Corneal precipitates have been reported during treatment with ofloxacin for topical ophthalmic use. However, a causal relationship has not been demonstrated.

EXOCIN potentially increases sensitivity to sunlight. Exposure to the sun or direct sunlight should be avoided when using EXOCIN.

Before taking EXOCIN:

Heart problems

Particular care should be taken when using this type of medicine, if you were born with or have a family history of prolonged QT interval (displayed on the ECG, an electrical recording of the heart), have a saline imbalance in the blood (especially a low level blood potassium or magnesium), have a very slow heart rhythm (called "bradycardia"), have a weak heart (heart failure), have a history of heart attack (myocardial infarction), if you are a woman or patient elderly or if you are taking other medicines which may cause abnormal changes in the ECG (see section "Interactions").

Before taking this medicine, tell your doctor:

If there is any imperfection or ulceration on the surface of the eye, as the use of the product may increase the risk of corneal perforation.

Pregnancy and breastfeeding

As there are inadequate and well-controlled clinical studies in pregnant women and since systemic use of quinolones has caused arthropathy in immature animals, it is not recommended to use the drug during pregnancy. Since ofloxacin and other systemically administered quinolones are excreted in breast milk , there may be a risk to the infant, therefore it is necessary to evaluate whether to discontinue breastfeeding or therapy, bearing in mind the importance of the drug for the mother.

Effects on ability to drive and use machines:

No studies on the ability to drive and use machines have been performed.

You may experience transient blurring of vision immediately after using EXOCIN. In this case, do not drive or operate machinery until your vision is clear again.

Important information about some excipients:

The preservative (benzalkonium chloride) present in EXOCIN can cause eye irritation and is also known to discolour soft contact lenses. Therefore, avoid contact with soft contact lenses; if you wear soft contact lenses, remove your lenses before using these eye drops and wait 15 minutes after using EXOCIN before re-applying them

Dosage and method of use How to use Exocin: Dosage

The dosage is 1-2 drops 4-6 times a day, or according to medical prescription.

For the treatment of keratitis, infectious corneal ulcers of bacterial origin: for the first two days, 1-2 drops every 30 minutes, during the day.

In the following week, 1-2 drops every hour initially and then gradually reduce the dosage (1-2 drops 4 times a day) until the treatment is complete.

Treatment with EXOCIN should be limited to the time needed to achieve clinical recovery.

Overdose What to do if you have taken too much Exocin

In the event of a topical overdose, rinse the eye with water.

In case of accidental intake of an excessive dose of EXOCIN, notify your doctor immediately or go to the nearest hospital.

If you have any questions about the use of EXOCIN, ask your doctor or pharmacist.

Side Effects What are the side effects of Exocin

Like all medicines, EXOCIN can cause side effects, although not everybody gets them.

The following categories describe the possibility of having a side effect

Not known: frequency cannot be estimated from the available data

Very common: occurs in more than 1 in 10 patients

Common: occurs in less than 1 in 10 patients

Uncommon: occurs in less than 1 in 100 patients Rare: occurs in less than 1 in 1000 patients

Very Rare: Occurs in less than 1 in 10,000 patients

The following side effects may occur with the use of this medicine:

Common side effects

Ocular pathologies

eye irritation,
ocular discomfort

Undesirable effects with frequency not known

Ocular pathologies

keratitis,
conjunctivitis,
blurred vision,
photophobia,
ocular edema,
foreign body sensation in the eye,
increased lacrimation,
dry eye,
eye pain,
allergic reactions (including eye itch and eyelid itching)
eye redness

Nervous system disorders

Dizziness

Gastrointestinal disorders

Nausea

Skin and subcutaneous tissue disorders

Periorbital edema
Facial edema

Heart problems

Not known: normal fast heart rhythm, life-threatening irregular heart rhythm, altered heart rhythm (called "QT interval prolongation", displayed on ECG, electrical activity of the heart).

Side effects with very rare frequency

Disorders of the immune system

Allergic reactions (including swelling under the skin which can occur in areas such as the face, lips or other parts of the body; rash, itching or hives on the skin; swelling of the mouth, tongue or throat and may block the airways, which may cause wheezing, difficulty in swallowing, breathing or shortness of breath; sudden, severe, life-threatening allergic reaction)

Rare serious reactions have been observed after systemic use of ofloxacin and most symptoms are reversible. As a small amount of ofloxacin may be absorbed systemically following topical administration, other undesirable effects reported in systemic use may appear.

Compliance with the instructions contained in the package leaflet reduces the risk of undesirable effects.

Reporting of side effects

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. Undesirable effects can also be reported directly via the national reporting system at “www.agenziafarmaco.gov.it/it/responsabili.” By reporting side effects you can help provide more information on the safety of this medicine.

Expiry and Retention

Expiry: see the expiry date indicated on the package.

The expiry date indicated refers to the product in intact packaging, correctly stored.

Warning: do not use the medicine after the expiry date indicated on the package.

Throw away the bottle 28 days after first opening, even if there is still some solution left.

Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. This will help protect the environment.

KEEP THE MEDICINAL PRODUCT OUT OF THE SIGHT AND REACH OF CHILDREN

Composition and pharmaceutical form

COMPOSITION

100 ml of solution contain:

Active ingredient: ofloxacin 0.3 g

Excipients: benzalkonium chloride, sodium chloride, purified water.

PHARMACEUTICAL FORM AND CONTENT

Eye drops, solution; bottle of 10 ml

Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.

Further information on Exocin can be found in the "Summary of Characteristics" tab. 01.0 NAME OF THE MEDICINAL PRODUCT 02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION 03.0 PHARMACEUTICAL FORM 04.0 CLINICAL PARTICULARS 04.1 Therapeutic indications 04.2 Posology and method of administration 04.3 Contraindications 04.4 Special warnings and appropriate precautions for use 04.5 Interactions with other medicinal products and other forms of interaction 04.6 Pregnancy and lactation 04.7 Effects on ability to drive and use machines 04.8 Undesirable effects 04.9 Overdose 05.0 PHARMACOLOGICAL PROPERTIES 05.1 Pharmacodynamic properties 05.2 Pharmacokinetic properties 05.3 Preclinical safety data 06.0 PHARMACEUTICAL PARTICULARS 06.1 Excipients 06.2 Incompatibilities 06.3 Shelf life 06.4 Special precautions for storage 06.5 Nature of the immediate packaging and contents of the package 06.6 Instructions for use and handling 07.0 MARKETING AUTHORIZATION HOLDER 08.0 MARKETING AUTHORIZATION NUMBER O 09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION 10.0 DATE OF REVISION OF THE TEXT 11.0 FOR RADIO DRUGS, COMPLETE DATA ON INTERNAL RADIATION DOSIMETRY 12.0 FOR RADIO DRUGS, ADDITIONAL DETAILED INSTRUCTIONS AND QUALITY CONTROLS

01.0 NAME OF THE MEDICINAL PRODUCT

EXOCIN

02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION

EXOCIN 3 mg / ml eye drops, solution

100 ml of solution contain

Active ingredient: Ofloxacin 0.3 g

Excipients: Benzalkonium chloride

EXOCIN 0.3% ointment

100 g of ointment contain

Active ingredient: Ofloxacin 0.3 g

Excipients: Lanolin

For the full list of excipients, see section 6.1

03.0 PHARMACEUTICAL FORM

Eye drops, solution

Ointment

04.0 CLINICAL INFORMATION

04.1 Therapeutic indications

EXOCIN is indicated for the treatment of external ocular infections caused by germs sensitive to ofloxacin, such as blepharitis, conjunctivitis, blepharoconjunctivitis, keratoconjunctivitis, dacryocystitis, keratitis, meibomites, and for post-operative prophylaxis.

EXOCIN is also indicated, limited to the 3 mg / ml eye drops form, for the treatment of infectious corneal ulcers of bacterial origin.

04.2 Posology and method of administration

Eye drops: The dosage is 1-2 drops 4-6 times a day, or according to medical prescription.

For the treatment of keratitis, infectious corneal ulcers of bacterial origin:

for the first two days, 1-2 drops every 30 minutes, during the day.

In the following week, 1-2 drops every hour initially and then gradually reduce the dosage (1-2 drops 4 times a day) until the treatment is complete.

Ointment: 1 application 3-4 times a day, or according to medical prescription.

Treatment with EXOCIN should be limited to the time needed to achieve clinical recovery.

04.3 Contraindications

Hypersensitivity to the active substance, to any of the excipients or to other quinolones.

04.4 Special warnings and appropriate precautions for use

Ophthalmic Use: Do not use for injections or intraocular use.

The safety and efficacy of the product in infants less than one year of age have not been established.

Particular care should be taken when using fluoroquinolones, including EXOCIN, in patients with known risk factors for QT interval prolongation such as, for example:

• Congenital long QT syndrome

• Concomitant use of drugs that are known to prolong the QT interval (for example, class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics)

• Incorrect electrolyte imbalance (eg hypokalaemia, hypomagnesaemia)

• Heart disease (for example heart failure, myocardial infarction, bradycardia)

• Elderly patients and women may be more sensitive to QT prolonging drugs.

Therefore, special care should be taken when administering fluoroquinolones, including EXOCIN, to these populations (see sections 4.5, 4.8 and 4.9).

If an allergic reaction to ofloxacin occurs, discontinue administration of the drug. Use EXOCIN with caution in patients who have shown sensitivity to other quinolone antibacterial agents. When using EXOCIN one must consider the risk of nasopharyngeal passage which may contribute to the occurrence and the spread of bacterial resistance. Like any other antibiotic, prolonged use can cause an excessive development of non-sensitive microorganisms; in this case and if no improvement is noticed after a reasonable period of time, discontinue use and consult your ophthalmologist.

Stevens-Johnson syndrome has been reported in patients who received topical ophthalmic ofloxacin, but no causal relationship with the drug has been demonstrated.

There are very limited data available to establish the efficacy and safety of EXOCIN in the treatment of conjunctivitis in neonates.

The use of EXOCIN in neonates with ophthalmia neonatorum caused by Neisseria gonorrhoeae or Chlamydia trachomatis is not recommended as the use of the product in such patients has not been evaluated.

Corneal precipitates have been reported during treatment with ofloxacin for topical ophthalmic use.

However, a causal relationship has not been demonstrated.

Exposure to the sun or UV rays should be avoided when using ofloxacin due to the potential risk of photosensitivity.

The use of contact lenses is not recommended in patients receiving therapy for ocular infection.

Important information about some of the ingredients

EXOCIN eye drops contain benzalkonium chloride as a preservative, which can cause eye irritation.

Avoid contact with soft contact lenses. Remove contact lenses before application and wait at least 15 minutes before reapplying them. The bleaching action of soft contact lenses is known.

EXOCIN ophthalmic ointment contains lanolin as an excipient, which may cause local skin reactions (e.g. contact dermatitis).

04.5 Interactions with other medicinal products and other forms of interaction

No interaction studies have been performed with EXOCIN eye drops or ointment.

Drugs known to prolong the QT interval.

EXOCIN, like other fluoroquinolones, should be used with caution in patients taking drugs known to prolong the QT interval (eg Class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics) (see section 4.4).

Systemic administration of some quinolones has been shown to inhibit the metabolic clearance of caffeine and theophylline. Drug interaction studies conducted with systemic ofloxacin have shown that the metabolic clearance of caffeine and theophylline are not significantly affected by ofloxacin.

04.6 Pregnancy and lactation

Use in pregnancy: As there are no adequate and well controlled clinical studies in pregnant women and since the systemic use of quinolones has caused arthropathy in immature animals, it is recommended not to use the drug during pregnancy.

Use during lactation: Since ofloxacin and other systemically administered quinolones are excreted in breast milk, there may be a risk to the infant, therefore it is necessary to evaluate whether to discontinue breastfeeding or therapy, bearing in mind the importance of the drug for the mother.

04.7 Effects on ability to drive and use machines

No studies on the ability to drive and use machines have been performed.

Transient blurring of vision may occur soon after using the product. Do not drive or operate machinery until symptoms have disappeared.

04.8 Undesirable effects

General

Serious reactions after systemic use of ofloxacin are rare and most symptoms are reversible.

Since a small amount of ofloxacin can be absorbed systemically following topical administration, other undesirable effects reported in systemic use may appear.

Adverse events observed with ofloxacin, documented through both spontaneous events and clinical studies, are classified within the body systems and listed below as Very common (≥1 / 10); Common (≥1 / 100 to

Disorders of the immune system

Very rare: Hypersensitivity * (including angioedema, dyspnoea, anaphylactic reaction / shock, oropharyngeal swelling and tongue swelling)

* Serious and occasionally fatal hypersensitivity (anaphylactic / anaphylactoid) reactions, some of which after the first dose, have been reported in patients treated with systemic quinolones, including ofloxacin. See section 4.4.

Nervous system disorders

not known: Vertigo

Ocular pathologies

Common: Eye irritation; Eye discomfort

not known: Keratitis; Conjunctivitis; Blurred vision Photophobia; Ocular edema; Foreign body sensation in the eye; Increased lacrimation; Dry eye; Eye pain; Ocular hyperaemia; Hypersensitivity (including eye itch and eyelid itching)

Gastrointestinal disorders

not known: Nausea

Skin and subcutaneous tissue disorders

not known: Periorbital edema, Facial edema

Heart ailments

not known: ventricular arrhythmia and torsades de pointes (reported mainly in patients with known risk factors for QT prolongation), prolonged QT on ECG (see sections 4.4. and 4.9)

Reporting of suspected adverse reactions

Reporting of suspected adverse reactions that occur after authorization of the medicinal product is important, as it allows continuous monitoring of the benefit / risk ratio of the medicinal product.

Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system at "www.agenziafarmaco.gov.it/it/responsabili".

04.9 Overdose

No cases of overdose have been reported.

In the event of an overdose, symptomatic treatment should be taken. ECG monitoring should be performed because of the possibility of QT interval prolongation.

In the event of a topical overdose, rinse the eye with water.

05.0 PHARMACOLOGICAL PROPERTIES

05.1 Pharmacodynamic properties

Pharmacotherapeutic group: Ophthalmologicals, anti-infectives, fluoroquinolones

ATC code: S01AE01

EXOCIN contains as active ingredient ofloxacin, a synthetic broad spectrum antibiotic from the fluoroquinolone family. It is active against a large number of Gram + and Gram- bacteria, including Staphylococci, Streptococci, Enterobacteria, Pseudomonas aeruginosa, Haemophilus influenzae, Neisseria gonorrhoeae and Chlamydia tracomatis.

Ofloxacin exerts its bactericidal activity by specifically inhibiting the microbial DNA-gyrase enzyme.

The bactericidal action is very rapid, with 90% of the bacteria eliminated after 19-55 minutes. The growth inhibiting effect of the bacteria persists for 6-8 hours after the drug is removed.

Furthermore, the particular mechanism of action reduces the appearance of bacterial resistance.

EXOCIN demonstrated activity in vitro against bacteria resistant to other antibiotics, including penicillin, aminoglycosides, macrolides, tetracyclines.

This seems to be due to the different mechanism of action of ofloxacin which also acts in the stationary phase of bacterial growth.

05.2 Pharmacokinetic properties

The spread of EXOCIN in ocular tissues affected by external ocular infections always reaches concentrations above the MICs and MBCs.

05.3 Preclinical safety data

Orally, the LD 50 showed values of approximately 5400 mg / kg in the mouse, 3500 mg / kg in the rat, over 200 mg / kg in the dog. Via e.v. LD 50 is about 200 mg / kg in mice and rats, and over 70 mg / kg in dogs. In systemic studies, the most important harmful effect observed was that on the articular cartilage in immature animals, an effect common to all quinolones. In ophthalmic use, tolerability was found to be very good.