Alpizarin^® (Tablets, Ointment) Instructions for Use

ATC Code

J05AX (Other antiviral drugs)

Clinical-Pharmacological Group

Herbal preparation with antiviral action

Pharmacotherapeutic Group

Systemic antiviral agents; direct-acting antiviral agents; other antiviral agents

Pharmacological Action

Alpizarin^® possesses antiviral activity against the following viruses: Herpes simplex types 1 and 2, Herpes zoster, Varicella zoster, and cytomegaloviruses. In vitro experiments have shown an inhibitory effect of tetrahydroxyglucopyranosylxanthene against the human immunodeficiency virus.

The inhibitory effect of the drug on virus reproduction is particularly evident in the early stages of its development. Alpizarin^® does not affect the activity of viral neuraminidase.

Alpizarin^® has immunostimulating properties regarding cellular and humoral immunity, and the ability to induce the production of gamma-interferon in blood cells.

Alpizarin^® inhibits the growth of gram-negative (Escherichia coli) and gram-positive (Staphylococcus aureus, Mycobacterium tuberculosis) bacteria, fungi (Microsporum canis), and pathogenic protozoa (Entamoeba histolytica, Trichomonas vaginalis). The mechanism of action of the drug is based on its ability to suppress bacterial nuclease activity. Alpizarin^® has a moderate anti-inflammatory effect.

Pharmacokinetics

The drug is rapidly absorbed from the gastrointestinal tract when taken orally.

Unchanged Tetrahydroxyglucopyranosylxanthene is detected in blood plasma within 0.5-5 hours after administration.
The maximum concentration of tetrahydroxyglucopyranosylxanthene – 4.5 µg/ml – is reached 1 hour after its administration.

Tetrahydroxyglucopyranosylxanthene is largely bound to blood proteins (90-70%).

Extarenal pathways of tetrahydroxyglucopyranosylxanthene elimination predominate. The excretion of unchanged tetrahydroxyglucopyranosylxanthene by the kidneys within 24 hours does not exceed 0.1%.

Indications

• As part of combination therapy for acute and recurrent infections caused by the herpes simplex virus of various localizations (including genital);
• Viral diseases of the oral mucosa (aphthous stomatitis);
• Herpes zoster (shingles);
• Kaposi’s varicelliform eruption;
• Cytomegalovirus infection;
• Chickenpox.

ICD codes

Dosage Regimen

Ointment

Externally, topically.

The ointment is applied externally/topically 4-6 times a day: for skin lesions, adults are prescribed 5% ointment, children – 2%; for mucous membranes, adults and children – 2% ointment. The ointment is applied in a thin layer and gently rubbed in.

The therapeutic effect of the drug is most pronounced when prescribed in the initial period of the disease or relapse. The duration of treatment depends on the form and severity of the disease.

For acute and recurrent forms of simple herpes of extragenital localization with single eruptions, the ointment is applied to the lesion for 3-5 days. In case of widespread eruptions, as well as in the presence of fever, lymphadenopathy and other general phenomena, the ointment is used for 5-14 days.

For Kaposi’s varicelliform eruption and cytomegalovirus infection, the ointment is used in the same age-specific dosages for 7-21 days as part of complex therapy.

For genital herpes, 2% ointment is applied to the affected areas 4 to 6 times a day for 7-10 days.

For viral diseases of the oral mucosa (aphthous stomatitis), the ointment is applied to the affected areas for 5-15 days; for the erosive-ulcerative form of oral lichen planus of the oral mucosa – for 2-4 weeks.

For diseases caused by Herpes zoster (shingles) and Varicella zoster (chickenpox), 2% ointment (for children) or 5% ointment (for adults) is applied topically to the lesion for 5-21 days.

In case of relapses, repeated courses of treatment with the drug are carried out.

Tablets

Adults and children over 12 years are prescribed orally (regardless of food intake) 100-200 mg 3-4 times/day for 5-10 days; children 6-12 years – 0.1 g 2-3 times/day; children 1-6 years – 0.05-0.1 g 2-3 times/day.

Simultaneously, local applications of 5% ointment on the skin and 2% ointment on the mucous membranes are prescribed. The ointment is applied to the affected skin areas without a bandage 2-6 times a day.

The therapeutic action is more pronounced when used early in the disease. The duration of treatment is 10-30 days. In case of relapse, the course is repeated.

For acute and recurrent forms of Herpes simplex of extragenital localization with single eruptions, the ointment is applied to the lesion 2-3 times a day for 3-5 days. In case of widespread eruptions, as well as in the presence of fever, lymphadenopathy, the drug is prescribed simultaneously orally and as an ointment for 5-14 days.

For Kaposi’s varicelliform eruption, it is used as part of complex therapy for 7-21 days; for genital herpes, 2% ointment is applied to the affected areas 4-6 times a day for 7-10 days; in case of recurrent disease – additionally orally for 5-14 days.

For viral diseases of the oral mucosa, it is prescribed orally in the same doses and simultaneously 2% ointment is applied to the affected areas for 5-15 days; for erosive-ulcerative form of oral lichen planus of the oral mucosa – for 2-4 weeks.

For diseases caused by Varicella zoster, combined therapy is carried out, including oral administration and topical application of 2% (for children) or 5% (for adults) ointment to the affected area for 5-21 days.

For prevention of Herpes simplex relapses, an oral course is prescribed 1 month after the end of treatment and then during inter-relapse periods in courses of 10-14 days.

Adverse Reactions

Allergic reactions are possible.

Contraindications

• Pregnancy;
• Children under 3 years of age;
• Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• Hypersensitivity to the components of the drug;

With caution during breastfeeding.

Use in Pregnancy and Lactation

There are no data on the excretion of tetrahydroxyglucopyranosylxanthene into breast milk, therefore the use of the drug during breastfeeding is possible only for vital indications, if the expected benefit to the mother outweighs the potential risk to the child. Consultation with a doctor is necessary.

With caution during breastfeeding.

Pediatric Use

Contraindicated in children under 3 years of age. Can be used in children over 3 years of age according to indications.

Special Precautions

In case of widespread eruptions, as well as in the presence of fever, lymphadenopathy and other general phenomena, the drug Alpizarin^® tablets 100 mg is used in combination with the drug Alpizarin^® ointment for external and topical use 2% and 5%.

1 tablet of the drug contains 0.1 g of milk sugar (lactose) and 0.0475 g of potato starch, which corresponds to 0.01 XE (bread units). The maximum daily dose of the drug for children from 3 to 12 years old contains 0.03 XE; for children over 12 years old and adults – 0.08 XE.

Effect on ability to drive vehicles and mechanisms

The drug does not affect the performance of potentially hazardous activities or those requiring increased concentration and speed of psychomotor reactions (driving vehicles and working with moving mechanisms).

Overdose

To date, no cases of overdose have been reported. The occurrence of an overdose is unlikely.

Drug Interactions

Not described.

Storage Conditions

In a place protected from light at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life – 5 years.

Dispensing Status

By prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.