Isotrexin (Gel) Instructions for Use

Marketing Authorization Holder

Stiefel Laboratories (UK) Limited (United Kingdom)

Manufactured By

Stiefel Laboratories (Ireland) Limited (Ireland)

Exclusive Representative

Representative Office DELTA MEDICAL (Ukraine)

ATC Code

D10AD54 (Isotretinoin in combination with other drugs)

Active Substances

Erythromycin (Rec.INN registered by WHO)

Isotretinoin (Rec.INN registered by WHO)

Dosage Form

Isotrexin

Gel for external use 500 mcg+20 mg/1 g: tube 6 g, 25 g, 30 g, 40 g or 50 g

Dosage Form, Packaging, and Composition

Gel for external use light yellow in color.

Excipients : hydroxypropylcellulose, butylated hydroxytoluene, ethanol.

6 g – aluminum tubes (1) – cardboard packs.
25 g – aluminum tubes (1) – cardboard packs.
30 g – aluminum tubes (1) – cardboard packs.
40 g – aluminum tubes (1) – cardboard packs.
50 g – aluminum tubes (1) – cardboard packs.

Clinical-Pharmacological Group

Acne treatment drug

Pharmacotherapeutic Group

Acne treatment agent

Pharmacological Action

A combined drug for the treatment of acne.

Isotretinoin is one of the biologically active forms of vitamin A; it has a regulatory effect on the growth of epithelial cells and their differentiation.

It inhibits the terminal differentiation of sebocytes and the hyperproliferation of the epithelium of the sebaceous gland ducts, normalizes the composition of their secretion and facilitates its evacuation. Due to this, the production of sebum is reduced and the inflammatory reaction around the glands is decreased.

Isotretinoin affects comedogenesis, inhibits follicular keratinization, and suppresses acne caused by Propionebacterium acnes.

It has antiseborrheic, anti-inflammatory, and keratolytic effects.

Erythromycin is an antibiotic of the macrolide group; it has an inhibitory effect on protein synthesis in bacteria by reversibly binding to ribosomal subunits.

In the treatment of acne, the efficacy of erythromycin is manifested in the reduction of the Propionebacterium acnes population.

Isotretinoin as a component of Isotrexin is effective in the comedonal phase of the disease, while Erythromycin is effective in the treatment of mild to moderate inflamed acne.

Pharmacokinetics

The percutaneous absorption of isotretinoin and erythromycin is insignificant.

During the study of the local absorption of the two components of Isotrexin in the treatment of patients with acne, only a slight increase in isotretinoin levels compared to baseline levels was noted (Isotretinoin is usually detected in blood plasma).

The levels remained below 5 ng/ml and did not increase in the presence of erythromycin.

Erythromycin levels in blood plasma were not detected.

Indications

• Treatment of mild to moderate acne.

ICD codes

Dosage Regimen

Apply the gel externally only.

Wash and thoroughly dry the affected skin areas prior to each application.

Apply a thin layer of gel to the affected skin twice daily, in the morning and in the evening.

Avoid contact with eyes, nostrils, mouth, and all mucous membranes.

Use caution when applying to sensitive skin areas, such as the neck and skin around the eyes.

Do not apply to broken, sunburned, or eczematous skin.

Wash hands immediately after application.

The full therapeutic effect typically requires 6 to 8 weeks of continuous treatment.

If excessive skin irritation occurs during the first two weeks, interrupt treatment for a few days.

Resume application once irritation subsides.

Discontinue use if adverse reactions persist.

Minimize sun exposure and use sunscreen during treatment due to potential for photosensitivity.

Adverse Reactions

Dermatological reactions sensations of slight tingling, burning and irritation, erythema and peeling of the skin at the site of application of the drug, photosensitivity.

Contraindications

• Children under 12 years of age;
• Pregnancy;
• Hypersensitivity to the components of the drug.

Use in Pregnancy and Lactation

The use of Isotrexin during planned and confirmed pregnancy is contraindicated.

The percutaneous absorption of isotretinoin is insignificant.

However, since it is not known whether the components of the drug are excreted in breast milk, Isotrexin should not be prescribed during lactation (breastfeeding).

Special Precautions

Contact with the mucous membranes of the mouth, nose and eyes, as well as with areas of skin with damaged or ulcerated surfaces, should be avoided.

The drug should be applied with caution to sensitive areas of the skin (the area around the eyes and the neck).

Since Isotrexin can cause increased sensitivity to sunlight, deliberate or prolonged exposure to the sun should be minimized.

If side effects occur, which usually appear in the 1st-2nd week of treatment, therapy should be interrupted for several days and the drug should be resumed after the symptoms of irritation disappear.

If the side effects do not disappear, treatment should be discontinued.

Overdose

Accidental overdose is unlikely because the drug is intended for external use.

Drug Interactions

Concomitant use of other drugs with keratolytic or exfoliative properties, including those from the retinoid group, is not recommended.

The effect of the drug is weakened with the simultaneous administration of tetracycline group antibiotics, as well as with the topical use of glucocorticosteroids.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is approved for use as an over-the-counter product.

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.