Afлubin® penciclovir

I N S T R U C T I O N for medical use of the medicinal product AФLUBIN® PENCICLOVIR

Composition:

Active substance: penciclovir;

1 g of cream contains penciclovir 0.01 g (10 mg);

Excipients: propylene glycol, white soft paraffin, cetostearyl alcohol, mineral oil, cetomacrogol 1000, purified water.

Pharmaceutical form. Cream.

Main physicochemical properties: homogeneous white cream.

Pharmacotherapeutic group. Chemotherapeutic agents for topical use. Antiviral agents. ATC code D06B B06.

Pharmacological Properties.

Pharmacodynamics.

Penciclovir demonstrates high selectivity in vivo and in vitro against human herpes viruses Herpes simplex (types 1 and 2), including acyclovir-resistant strains with altered DNA polymerase, Varicella zoster virus, as well as Epstein-Barr virus and cytomegalovirus. In virus-infected cells, penciclovir is rapidly converted into its triphosphate form (with the participation of virus-induced thymidine kinase). Penciclovir triphosphate is retained within virus-infected cells for over 12 hours, where it inhibits viral DNA replication—significantly longer than acyclovir. By suppressing viral replication, penciclovir considerably shortens healing time, even after the development of papules and vesicles, reduces pain sensations, and shortens the duration of crust desquamation caused by viral activity. The half-life is 9, 10, and 20 hours in cells infected with Varicella zoster, Herpes simplex type 1, and Herpes simplex type 2, respectively. In uninfected cells treated with penciclovir, the concentration of penciclovir triphosphate is practically undetectable. Thus, penciclovir does not affect uninfected cells.

Pharmacokinetics.

After topical application of 1% cream, the concentration of penciclovir in blood plasma and urine is not quantitatively detectable.

Clinical characteristics.

Indications. Labial herpes (Herpes labialis).

Contraindications.

Hypersensitivity to penciclovir, famciclovir, or other components of the medicinal product (e.g. propylene glycol).

Interaction with other medicinal products and other forms of interaction.

No interactions have been observed during concomitant administration of other medicinal products (local or systemic) when the medicinal product was used in clinical studies.

Special precautions for use

The cream should only be applied to herpes-affected areas on the lips or skin around the mouth. Application of the cream to mucous membranes (e.g., eyes, mouth, nose, or genital organs) is not recommended. Particular care should be taken to avoid contact of the cream with the eyes or the surrounding areas.

If symptoms of the disease have not resolved after 4 days of treatment with the cream, medical advice should be sought.

To prevent the spread of the virus to other parts of the body and to avoid infecting other people, the following precautions should be observed:

• always wash hands before and after touching the affected area;
• store the tube of cream in its original packaging and do not allow other people to use it;
• avoid rupturing blisters formed as a result of prolonged viral activity;
• avoid touching the eyes (the virus may infect the cornea);
• avoid kissing, especially children;
• avoid sharing items through which the virus may spread: towels, cups, cutlery, cigarettes.

The cream contains cetyl stearyl alcohol, which may cause local skin reactions (e.g., contact dermatitis). Each 1 g of cream contains 416 mg of propylene glycol, which may cause skin irritation.

Patients with immunodeficiency (e.g., AIDS patients or bone marrow transplant recipients) should consult their physician, who will determine whether systemic oral therapy is required.

Use during pregnancy or breastfeeding

Since clinical studies have shown minimal systemic absorption of penciclovir following topical application, there are no major concerns regarding the use of the cream during pregnancy or breastfeeding. However, because the safety of penciclovir during pregnancy or breastfeeding has not been established, the product should only be used during these periods after consultation with a physician, and only when the expected benefit to the mother outweighs the potential risk to the fetus/infant.

There is no information available on the excretion of penciclovir in human breast milk.

Fertility

There are no data on the effect of penciclovir on fertility in humans. Studies in animals have not shown any effect on fertility following topical application of penciclovir.

Effect on ability to drive and use machines

The medicinal product has no influence on the ability to drive or operate machinery.

Dosage and Administration.

For adults (including elderly patients) and children aged 12 years and older.

The cream should be applied every 2 hours (except during sleep). The treatment course lasts 4 days. Treatment should be initiated as early as possible upon the first signs of infection. Hands should be washed before applying the cream.

The cream should be applied with a clean finger or a single-use applicator (for packages containing applicators) in an amount sufficient to cover the affected area of skin.

Children. The safety and efficacy of the drug in children under 12 years of age have not been established.

Overdose.

Overdose is unlikely with topical use. Even in case of accidental oral ingestion of the entire contents of the package, adverse effects are not expected due to the low oral absorption of penciclovir. However, some irritation of the oral mucosa may occur. There is no need for specific therapeutic measures in case of accidental oral ingestion of the entire contents of the package.

Adverse Reactions

The frequency of adverse reactions is classified as follows:

very common (≥ 1/10);
common (from ≥ 1/100 to < 1/10);
uncommon (from ≥ 1/1000 to < 1/100);
rare (from ≥ 1/10,000 to < 1/1,000);
very rare (< 1/10,000);
frequency not known (cannot be estimated from available data).

Aflubin® Penciclovir cream was well tolerated in clinical trials. The most commonly reported adverse reactions were local reactions at the site of application.

General disorders and administration site conditions:
common (≥ 1/100, < 1/10): application site reactions (including pain at application site, hypoesthesia, burning sensation, tingling, numbness).

During post-marketing surveillance, the following adverse reactions have been reported (all reactions were local or generalized). The frequency of adverse reactions based on post-marketing data is difficult to estimate; therefore, the frequency of these reactions is considered as not known.

Immune system disorders:
frequency not known: urticaria, hypersensitivity reactions.

Skin and subcutaneous tissue disorders:
frequency not known: allergic dermatitis (including rash, pruritus, blisters, and swelling).

Additionally, cases of contact dermatitis (as a reaction to cetyl stearyl alcohol) and irritation at the application site (as a reaction to propylene glycol) are possible. No cases of increased photosensitivity (pigmentation due to exposure of cream-treated skin areas to ultraviolet radiation) were observed during clinical trials of Aflubin® Penciclovir cream.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after medicine authorization is important. It allows continuous monitoring of the benefit-risk balance of the medicine. Healthcare professionals and patients, as well as their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy through the automated pharmacovigilance information system at the following link: https://aisf.dec.gov.ua/.

Shelf life: 3 years.

Storage conditions: Store out of reach and sight of children at a temperature not exceeding 30 °C. Do not freeze.

Packaging: 2 g of cream in aluminum tubes with a membrane. 1 tube per cardboard box.

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

Manufacturer:
Medgenix Benelux NV / Medgenix Benelux NV.

Manufacturer's address and place of business:
Vliegveld 21, Wevelgem, 8560, Belgium / Vliegveld 21, Wevelgem, 8560, Belgium.