Octynia

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT OCTINIA (OCTINIA)

Composition:

Active substances: octenidine dihydrochloride, phenoxyethanol;

1 ml of solution contains octenidine dihydrochloride 1 mg, phenoxyethanol 20 mg;

Excipients: glycerol, sodium gluconate, cocamidopropyl betaine, sodium chloride, sodium hydroxide, hydrochloric acid diluted, purified water.

Pharmaceutical form. Solution.

Main physicochemical properties: clear or almost clear, colorless liquid.

Pharmacotherapeutic group. Antiseptics and disinfectants. Quaternary ammonium compounds. Octenidine, combinations. ATC code D08AJ57.

Pharmacological Properties

Pharmacodynamics

The combination of octenidine dihydrochloride and phenoxyethanol is an antiseptic for the treatment of mucous membranes, skin, and wounds.

Mechanism of action

Octenidine dihydrochloride is a member of cationic-active compounds and, due to its two cationic centers, possesses pronounced surface-active properties. It interacts with components of the microbial cell wall and membrane, leading to disruption of cellular function.

The antimicrobial mechanism of action of phenoxyethanol involves, in particular, increasing the permeability of the cell membrane to potassium ions.

Pharmacodynamic properties

Antimicrobial activity includes bactericidal and fungicidal activity, as well as activity against lipophilic viruses and hepatitis B virus. The efficacy spectra of phenoxyethanol and octenidine dihydrochloride complement each other.

In quantitative and qualitative in vitro studies without protein load, a solution of octenidine dihydrochloride with phenoxyethanol applied for 1 minute demonstrated bactericidal and antifungal activity against bacteria and Candida albicans fungi, with a reduction factor (RF) of 6–7 lg.

Under conditions of adding 10% defibrinated sheep blood, 10% bovine albumin, or 1% mucin, or a mixture of 4.5% defibrinated sheep blood, 4.5% bovine albumin, and 1% mucin, the solution of octenidine dihydrochloride with phenoxyethanol caused a reduction in bacterial count with an RF of 6–7 lg and in Candida albicans fungi of >3 lg after at least 1 minute of exposure.

In quantitative and qualitative in vitro studies in the presence of 0.1% albumin, good activity was observed within 1 minute of contact with gram-positive and gram-negative bacteria, yeasts, and fungi when 50% and 75% solutions of octenidine dihydrochloride with phenoxyethanol were used.

In vitro studies evaluated the activity of the octenidine dihydrochloride and phenoxyethanol solution against specific viruses. Efficacy was demonstrated against lipophilic viruses, such as herpes simplex virus, HIV, and hepatitis B virus.

Primary resistance to the octenidine dihydrochloride and phenoxyethanol solution is not expected, nor is secondary resistance with prolonged use, due to its nonspecific mode of action.

Clinical studies on efficacy at vaginal and oral mucous membranes demonstrated a significant reduction in microbial counts with both short-term and long-term use.

Paediatric population

Efficacy and tolerability of the octenidine dihydrochloride and phenoxyethanol solution have been demonstrated in 347 children aged from 6 days to 12 years, as well as in 73 preterm infants with a gestational age of less than 36 weeks.

A study on umbilical cord stump treatment with octenidine dihydrochloride and phenoxyethanol solution in 1725 newborns demonstrated good tolerability.

Pharmacokinetics

Absorption

Animal studies with 14C-labeled material demonstrated that octenidine dihydrochloride is not absorbed through the gastrointestinal tract, skin, or mucous membranes.

Following oral administration, radiolabeled octenidine dihydrochloride was absorbed through the gastrointestinal mucosa in mice, rats, and dogs only in very small amounts (0–6%). It was established that in mice, topical application of octenidine dihydrochloride for 24 hours under occlusive dressing did not result in absorption.

Based on in vitro data, the possibility of octenidine dihydrochloride crossing the placenta can be excluded.

In rat studies, orally administered 14C-labeled phenoxyethanol was almost completely absorbed and excreted in urine as phenoxyacetic acid.

Octenidine dihydrochloride was not absorbed through the vaginal mucosa (in rabbits) or through wounds (in humans, rats).

Paediatric population

The oxidative metabolism of 2-phenoxyethanol was studied in 4 infants aged from 1 week to 11 months and in 24 preterm infants with a gestational age of less than 36 weeks. This study demonstrated that 2-phenoxyethanol is absorbed through the skin and is completely or nearly completely metabolized via oxidation to phenoxyacetic acid and excreted by the kidneys, demonstrating the safety of applying the octenidine dihydrochloride and phenoxyethanol solution.

Clinical characteristics

Indications

Used for repeated, time-limited treatment of mucous membranes and surrounding skin prior to diagnostic and surgical procedures in the anogenital area: vagina, vulva, glans penis, before urinary bladder catheterization; for oral cavity treatment; for antiseptic treatment of local bacterial and fungal infections in the vaginal area. The medicinal product is indicated for time-limited supportive therapy of interdigital mycosis and for antiseptic treatment of wounds and burns of various origins.

Use for treatment of local bacterial and fungal infections in the vaginal area is restricted to adult patients and children aged 8 years and older. For all other indications, the medicinal product Octinia can be used in adults and children without age restrictions.

Contraindications

Hypersensitivity to the active substances or to any of the excipients of the product.

Do not use in the nose, for irrigation of the abdominal cavity (e.g., during surgery), in the area of the tympanic membrane, or for instillation into the urinary bladder.

When used in the vaginal area: do not use during the first trimester of pregnancy; do not use in children under 8 years of age.

Interaction with other medicinal products and other forms of interaction

Do not apply the medicinal product Octinia to adjacent skin areas treated with antiseptics based on PVP-iodine due to the possibility of pronounced skin discoloration at contiguous sites, ranging from brown to purple.

Special precautions for use

Avoid swallowing the medicinal product Octinia or its entry into the bloodstream, for example, as a result of accidental injection.

Avoid contact of the medicinal product Octinia with the eyes. If the product comes into contact with the eyes, immediately rinse thoroughly with large amounts of water.

The use of aqueous solutions of octenidine (0.1% with/without phenoxyethanol) for skin disinfection prior to invasive procedures has been associated with serious skin reactions in premature newborns with low body weight.

Before application, remove any soaked materials, cloths, or clothing. Do not use excessive amounts and avoid accumulation of the solution in skin folds or under the patient, or dripping onto bed linen or other materials in direct contact with the patient. When an occlusive dressing is required on areas previously treated with Octinia, exercise caution to ensure that no excess product remains before applying the dressing.

Persistent edema, erythema, and tissue necrosis have been observed after irrigation of deep wounds using a syringe, in some cases requiring surgical revision (see section "Adverse reactions").

Use during pregnancy or breastfeeding

Fertility

No negative impact of octenidine dihydrochloride on fertility was observed in rats.

There are no data available on the effect of phenoxyethanol on fertility.

Pregnancy

A moderate amount of data obtained from pregnant women (from 300 to 1000 pregnancy outcomes, gestational age ≥ 12 weeks) indicates no evidence of teratogenic effects or embryotoxicity/fetotoxicity of the medicinal product Octinia.

Animal studies have not revealed signs of reproductive toxicity.

If necessary, the medicinal product Octinia may be used during pregnancy. As a precautionary measure, since clinical data for the first trimester of pregnancy are lacking, the solution of the medicinal product Octinia should not be applied to the vaginal area during the first three months of pregnancy.

Breastfeeding

Comprehensive data on the use of the medicinal product during lactation from experimental animal and clinical studies are lacking. Since octenidine dihydrochloride is absorbed in very small amounts or not absorbed at all, it is expected not to penetrate into breast milk.

Phenoxyethanol is rapidly and almost completely absorbed and is almost entirely excreted via the kidneys as oxidized metabolites. Therefore, accumulation in breast milk is unlikely.

As a precautionary measure, the medicinal product Octinia should not be applied to the breast area during breastfeeding.

Ability to influence the speed of reactions while driving or operating machinery

The medicinal product does not affect the ability to drive or operate machinery.

Method of Administration and Dosage

The solution is intended for topical use only and should not be injected into tissues, for example, using a syringe.

The medicinal product Octinia should be used undiluted, applied directly to the affected area until completely moistened. Octinia should be applied once daily to the treatment area using swabs soaked with the preparation or by spraying to reach inaccessible skin surfaces. Application using a swab is recommended.

Further procedures, such as applying a surgical dressing, may be performed no sooner than 2 minutes after application of the preparation. Mouth rinsing is also possible, but this method of administration is limited to cases where the entire oral cavity needs to be treated. In such cases, 20 mL of the preparation should be used for 20 seconds; the preparation must not be swallowed.

For maintenance therapy in cases of interdigital mycosis, the medicinal product should be sprayed onto the affected areas in the morning and evening.

To achieve the desired effect, these instructions must be strictly followed.

Since experience with continuous use does not exceed 14 days, the medicinal product Octinia should be used for a limited treatment duration.

Treatment of local bacterial and fungal infections of the vaginal area

Before first use, take the provided vaginal spray applicator and attach it to the bottle. The spray mechanism functions properly when the bottle is held vertically with the bottom facing downward. For full readiness before the first use, perform one or two test sprays over a sink. The vaginal spray applicator is mobile. For deep insertion of the applicator into the vagina, it is recommended to sit on the toilet or lie in bed. Press the spray applicator 11 times to distribute the preparation deeply into the vagina. After application, press the spray applicator one or two times, directing it, for example, over a sink, then rinse the spray applicator under running water and dry it with a clean cloth. The treatment duration should be 7 days: on the first day, apply the preparation in the morning and evening, then once daily in the evening. Before each subsequent application, press the spray applicator one or two times, directing it over a sink, and perform the procedure as described. The spray applicator may be used throughout the entire treatment course. After completion of treatment for vaginal infection, the spray applicator should be discarded.

To prevent reinfection, the patient's partner must also undergo treatment. Male genital organs should be treated with the medicinal product until completely moistened.

To achieve the desired effect, these instructions must be strictly followed.

In case of persistent or recurrent symptoms, a gynecological examination including microbiological diagnostics is mandatory. If necessary, appropriate antibacterial therapy should be initiated.

Children

The dosage of the medicinal product Octinia is the same for adults and children.

For the treatment of local bacterial and fungal infections in the vaginal area, Octinia may be used in children aged 8 years and older.

For all other indications, the medicinal product Octinia can be used in adults and children without age restrictions.

Overdose

There is no information available regarding overdose. However, the likelihood of overdose with topical application is very low. In case of local overdose, the affected area may be rinsed with a large amount of Ringer's solution.

Accidental ingestion of the medicinal product Octinia is not considered dangerous. Oxytenidine dihydrochloride is not absorbed and is excreted in feces. However, oral ingestion of a large amount of Octinia cannot exclude irritation of the gastrointestinal mucosa.

Oxytenidine dihydrochloride is more toxic when administered intravenously than orally. Therefore, entry of a large amount of the medicinal product Octinia into the bloodstream, for example, due to accidental injection, should be avoided. However, since Octinia contains oxytenidine dihydrochloride at a concentration of only 0.1%, intoxication is highly unlikely.

Side effects

The evaluation of adverse effects is based on the following frequency of occurrence: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), rare (≥ 1/10000 to < 1/1000), very rare (< 1/10000), frequency not known (cannot be estimated from the available data).

General disorders and application site reactions

Rare: burning, redness, itching, sensation of warmth at the application site.

Very rare: allergic contact reaction, for example transient redness at the application site.

Frequency not known: following irrigation of deep wounds using a syringe, persistent swelling, erythema, and tissue necrosis have been observed, which in some cases required surgical revision (see section "Special precautions for use").

A bitter taste may occur when rinsing the oral cavity.

Other possible adverse effects include swelling, induration, pain, blisters, and eczema at the site of application.

Paediatric population

The frequency, type, and severity of adverse reactions in children are the same as in adults.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorization of the medicinal product is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report any suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua/.

Shelf life

2 years.

Shelf life after first opening of the container: 2 years.

Storage conditions

Store in the original packaging at a temperature not exceeding 25 °C.

For 200 ml, 300 ml, and 500 ml containers, do not freeze.

Keep out of the reach of children.

Packaging

30 ml in a plastic bottle closed with a pump dispenser with spray nozzle.

50 ml in a plastic bottle closed with a pump dispenser, supplied with a spray nozzle in an individual package.

200 ml, 300 ml, or 500 ml in a Type III hydrolytic glass bottle closed with a plastic cap.

One bottle per carton.

Or one 200 ml or 300 ml bottle, without carton packaging.

Availability category: Over-the-counter (without prescription).

Manufacturer: JSC "Farmak".

Manufacturer's address and place of business

74, Kyrylivska Street, Kyiv, 04080, Ukraine.