Rozonix solopharm (Gel) Instructions for Use

Marketing Authorization Holder

Grotex, LLC (Russia)

ATC Code

D11AX21 (Brimonidine)

Active Substance

Brimonidine (Rec.INN registered by WHO)

Dosage Form

Rozonix solopharm

Gel for external use 0.5%

Dosage Form, Packaging, and Composition

Gel for external use

10 g – tubes – cardboard packs – By prescription
30 g – tubes – cardboard packs – By prescription

Clinical-Pharmacological Group

Selective alpha₂-adrenergic agonist used for rosacea

Pharmacotherapeutic Group

Other drugs used in dermatology

Pharmacological Action

An agent for external use, a highly selective agonist of α₂-adrenergic receptors. Its affinity for α₂-adrenergic receptors is 1000 times greater than its affinity for α₁-adrenergic receptors.

Application of a highly selective α₂-adrenergic receptor agonist to the facial skin reduces erythema through direct vasoconstriction of the small blood vessels of the dermis.

Pharmacokinetics

With daily application to the facial skin once a day for 29 days, no accumulation of brimonidine in the blood plasma was observed.

Brimonidine is actively metabolized in the liver. Brimonidine and its metabolites are excreted primarily by the kidneys.

Indications

Treatment of facial erythema in rosacea.

ICD codes

Dosage Regimen

For external use only.

Apply a thin layer to the skin of each of the five facial areas (forehead, chin, nose, each cheek) once daily.

The maximum recommended daily dose is 1 g of gel, approximately equivalent to the size of five match heads.

Apply only to intact skin; avoid application to irritated skin, open wounds, or the immediate eye area.

Ensure the gel has dried completely before applying any other topical medicinal or cosmetic products.

Strictly adhere to the recommended dose and frequency of application; do not exceed one application per day.

Avoid increasing the daily dose or application frequency, as the safety of such use has not been established.

If severe skin irritation or an allergic reaction occurs, discontinue treatment immediately.

In case of worsening erythema or severe flushing, suspend use; symptomatic relief may include cooling compresses, NSAIDs, or antihistamines.

Before resuming treatment after a break, perform a trial application to a small area of facial skin at least one day prior to full-face application.

Adverse Reactions

Nervous system disorders: uncommon – headache, paresthesia.

Eye disorders: uncommon – eyelid edema.

Cardiovascular system disorders: common – flushing; rare – arterial hypotension.

Respiratory system disorders: uncommon – nasal congestion.

Gastrointestinal system disorders: uncommon – dry mouth.

Skin and subcutaneous tissue disorders: common – redness, itching, burning sensation of the skin, skin blanching at the application site; uncommon – rosacea, dermatitis, skin irritation, sensation of heat, contact dermatitis, allergic contact dermatitis, dry skin, skin pain, skin discomfort, papular rash, acne, facial swelling, urticaria; rare – angioedema.

General and local reactions: uncommon – feeling of heat, feeling of cold at the application site.

Contraindications

Hypersensitivity to brimonidine; children and adolescents under 18 years of age; concurrent use with MAO inhibitors (e.g., selegiline or moclobemide), and tricyclic (imipramine) and tetracyclic (maprotiline, mianserin and mirtazapine) antidepressants that affect noradrenergic transmission.

With caution

Pregnancy; impaired liver and kidney function.

Use in Pregnancy and Lactation

Data on the use of brimonidine during pregnancy are limited or absent.

It is not known whether Brimonidine and its metabolites are excreted in breast milk. In this regard, the risk for newborns and infants cannot be ruled out. The decision to discontinue breastfeeding or use this agent should be made, taking into account the importance of treatment for the mother.

Use in Hepatic Impairment

Use with caution in case of impaired liver function.

Use in Renal Impairment

Use with caution in case of impaired kidney function.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

Should not be applied to irritated skin or open wounds, or to the area around the eyes. In case of severe irritation or allergy, treatment with brimonidine should be discontinued.

Brimonidine can be used in combination with other medicinal products used to treat inflammatory elements in rosacea, and with cosmetic products. They can be applied to the skin only after this agent has dried, and not immediately before it.

The effect of brimonidine begins to weaken several hours after application. In some patients, recurrence of erythema and flushing in a more severe form than observed before treatment has been described. Most such cases were noted within the first 2 weeks after starting treatment.

Some patients receiving brimonidine therapy experienced flushing. In most cases, erythema and flushing resolved after discontinuation of the drug.

In case of worsening erythema, the use of brimonidine should be suspended. Symptomatic measures, such as cooling compresses, taking NSAIDs and antihistamines, may alleviate the symptoms.

After resuming brimonidine use, cases of exacerbation of erythema and flushing with a more severe course were noted. After a temporary break in treatment, resumption of brimonidine use should begin with a trial application of this agent to a small area of facial skin at least 1 day before transitioning to treatment with the drug when applied to the entire facial skin surface.

The recommended dose and frequency of application should be strictly observed: once a day, in a very thin layer.

Avoid increasing the maximum daily dose and/or frequency of use, as the safety of increased daily doses or multiple daily applications has not been established.

Concomitant use with systemic α-adrenergic receptor agonists may enhance the side effects of this class of drugs in patients with severe or uncontrolled, or unstable cardiovascular diseases; with depression, cerebrovascular or coronary insufficiency, Raynaud’s disease, orthostatic hypotension, obliterating thromboangiitis, scleroderma or Sjögren’s syndrome.

Drug Interactions

MAO inhibitors can theoretically interfere with the absorption of brimonidine and potentially lead to an increase in systemic side effects, such as arterial hypotension, and also affect the metabolic process and absorption of circulating amines.

The possibility of additive or potentiating action should be considered when using brimonidine concomitantly with drugs that depress the CNS (alcohol, barbiturates, opiates, sedatives or anesthetics).

There are no data on the effect of brimonidine on the level of circulating catecholamines. Nevertheless, caution is recommended when prescribing brimonidine to patients receiving drugs that can affect the metabolism of amines and increase their concentration in the blood, such as chlorpromazine, methylphenidate, reserpine.

Caution is recommended at the start of treatment or when changing the dose of co-administered systemic drugs (regardless of their dosage form) that may interact with α-adrenergic receptor agonists or affect their action, i.e., are agonists or antagonists of α-adrenergic receptors (e.g., isoprenaline, prazosin).

In some patients, Brimonidine can cause a clinically insignificant decrease in blood pressure, so caution should be exercised when using antihypertensive agents and/or cardiac glycosides concomitantly with brimonidine.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.