Solantra cream 1%, 30 g

Treatment of inflammatory skin lesions in rosacea (papulopustular form) in adult patients.

For external use only.

Apply Solantra cream 1 time per day every day throughout the course of treatment - up to 4 months. If necessary, the course of treatment can be repeated.

If there is no improvement after 3 months of using the drug, treatment should be discontinued.

Apply a small amount of cream (about the size of a pea) to the skin of each of the five areas of the face: forehead, chin, nose and cheeks. Distribute the drug in a thin layer over the entire face, avoiding contact with eyes, lips and mucous membranes.

Solantra should only be applied to the face.

In patients with impaired renal function and elderly patients, dose adjustment is not required.

1 g of cream contains:

Active ingredient: ivermectin 10.0 mg.

Excipients: glycerol 40.0 mg, isopropyl palmitate 40.0 mg, carbomer copolymer type B 2.0 mg, dimethicone 20 Cst 5.0 mg, disodium edetate 0.5 mg, citric acid monohydrate 0.5 mg, cetyl alcohol 35 , 0 mg, stearyl alcohol 25.0 mg, macrogol cetostealic ester 30.0 mg, sorbitan stearate 20.0 mg, methyl parahydroxybenzoate 2.0 mg. propyl parahydroxybenzoate 1.0 mg, phenoxyethanol 10.0 mg, propylene glycol 20.0 mg, oleyl alcohol 20.0 mg, sodium hydroxide solution 10% to pH 6.3 ± 0.3, purified water to 1000 mg.

Х Hypersensitivity to the active substance or any other component of the drug;

Х Pregnancy;

Х Breastfeeding period;

Х Children under 18 years of age (the safety and efficacy of the drug for this age group has not been studied).

Carefully:

Х Abnormal liver function

Trade name of the drug:

Solantra

International non-proprietary name:

Ivermectin

Dosage form:

cream for external use

Composition:

1 g of cream contains:

Active ingredient: ivermectin 10.0 mg.

Excipients: glycerol 40.0 mg, isopropyl palmitate 40.0 mg, carbomer copolymer type B 2.0 mg, dimethicone 20 Cst 5.0 mg, disodium edetate 0.5 mg, citric acid monohydrate 0.5 mg, cetyl alcohol 35 , 0 mg, stearyl alcohol 25.0 mg, macrogol cetostealic ester 30.0 mg, sorbitan stearate 20.0 mg, methyl parahydroxybenzoate 2.0 mg. propyl parahydroxybenzoate 1.0 mg, phenoxyethanol 10.0 mg, propylene glycol 20.0 mg, oleyl alcohol 20.0 mg, sodium hydroxide solution 10% to pH 6.3 ± 0.3, purified water to 1000 mg.

Description:

Cream from white to light yellow.

Pharmacotherapeutic group:

antimicrobial and antiprotozoal agent. ATX code: D11AX22.

Pharmacological properties

Pharmacodynamics

Ivermectin belongs to the avermectin group. which has an anti-inflammatory effect by suppressing the production of inflammatory cytokines induced by lipopolysaccharides. The anti-inflammatory properties of topical ivermectin have been observed in animal models of inflammatory skin processes. Ivermectin also causes the death of parasites, mainly through selective binding and high affinity for glutamate-regulated chlorine channels found in the nerve and muscle cells of invertebrates. The mechanism of action of Solantra in the treatment of inflammatory skin lesions in rosacea is not known, but it may be associated with both the anti-inflammatory effects of ivermectin and the ability of ivermectin to kill Demodex mites, which, in turn, are a factor causing skin inflammation.

Pharmacokinetics

Suction

The absorption of ivermectin contained in Solantra was evaluated in a clinical study involving adult patients with severe papulopustular rosacea who used the maximum permissible dose of the drug. In steady state (after 2 weeks of treatment), the highest mean (± standard deviation) plasma ivermectin concentrations were observed within 10 ± 8 hours after drug administration (Cmax 2.1 ± 1.0 ng / ml, range: 0.7 -4.0 ng / ml), and the highest mean (± standard deviation) AUC0-244 was 36 ± 16 ngh / ml, range: 14-75 ngh / ml). Systemic exposure to ivermectin reached a plateau by the end of the second week of treatment under steady state conditions. With longer treatment in the Phase 3 studies, the systemic exposure to ivermectin remained the same as after 2 weeks of treatment.Under conditions of equilibrium concentration, the levels of systemic exposure to ivermectin (AUC0-244: 36 ± 16 ng h / ml) were lower than after a single oral dose of 6 mg ivermectin in healthy volunteers (AUC0-244: 134 ± 66 ng h / ml).

Distribution

An in vitro study showed that the binding of ivermectin to blood plasma proteins (mainly albumin) is more than 99%. No significant binding of ivermectin to erythrocytes was observed.

Metabolism

In in vitro studies using human liver microsomes and recombinant CYP450 enzymes, it was noted that ivermectin is metabolized mainly by CYP3A4 inhibitors.

In vitro studies have shown that ivermectin does not inhibit CYP450 isoenzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, ZA4, 4A11 or 2E1. Ivermectin does not induce the expression of CYP450 enzymes (1A2, 2B6, 2C9, or 3A4) in cultured human hepatocytes. The two main metabolites of ivermectin (3 '-0-demethyl ivermectin and 4a-hydroxy ivermectin) were identified in a clinical pharmacokinetic study using the maximum allowable dose of the drug and studied during phase 2 clinical trials. Like the parent compound, the metabolites reached an equilibrium state by the end of the second week of treatment, with no signs of accumulation observed up to 12 weeks. In addition, systemic exposures to metabolites (assessed using Cmax and AUC) obtained at steady state were much lower than those after oral ivermectin.

Withdrawal

The terminal elimination half-life averaged 6 days (approximately 145 hours, range: 92-238 hours) in patients who applied the drug to the skin once daily for 28 days in a clinical pharmacokinetic study using the maximum allowable dose of the drug. Excretion from the body depends on the degree of absorption after external application of Solantra cream. The pharmacokinetics of ivermectin have not been studied in patients with impaired liver and kidney function.

Indications

Treatment of inflammatory skin lesions in rosacea (papulopustular form) in adult patients.

Contraindications

Х Hypersensitivity to the active substance or any other component of the drug;

Х Pregnancy;

Х Breastfeeding period;

Х Children under 18 years of age (the safety and efficacy of the drug for this age group has not been studied).

Carefully:

Х Abnormal liver function

Application during pregnancy and during breastfeeding

Pregnancy

Data on the use of ivermectin in pregnant women are limited or absent. Reproductive toxicity studies when taking ivermectin orally showed that the drug has teratogenic potential in rats and rabbits, however, due to the low systemic exposure when applied externally at the recommended dosage, the drug has a low risk of fetotoxicity in humans. The use of Solantra during pregnancy is not recommended.

Breastfeeding period

After oral administration, low concentrations of ivermectin are excreted into breast milk. With external use of the drug, the release of ivermectin into breast milk has not been studied. Pharmacokinetic and toxicological data from animal studies also indicate the excretion of ivermectin in breast milk. The risk to the nursing infant cannot be excluded. If it is necessary to use the drug, you should consult with your doctor to make a decision to stop breastfeeding.

Method of administration and dosage

For external use only.

Apply Solantra cream 1 time per day every day throughout the course of treatment - up to 4 months. If necessary, the course of treatment can be repeated.

If there is no improvement after 3 months of using the drug, treatment should be discontinued.

Apply a small amount of cream (about the size of a pea) to the skin of each of the five areas of the face: forehead, chin, nose and cheeks. Distribute the drug in a thin layer over the entire face, avoiding contact with eyes, lips and mucous membranes.

Solantra should only be applied to the face.

In patients with impaired renal function and elderly patients, dose adjustment is not required.

Side effect

The most common adverse reactions, such as burning sensation, skin irritation, itching and dry skin, were reported in less than 1% of drug-treated patients in clinical trials.

Typically, these reactions are mild to moderate and usually diminish with continued therapy.

There were no significant differences in the safety profile between patients aged 18 to 65 years and patients over the age of 65 years.

Overdose

Overdose cases of Solantra have not been reported.

In case of accidental or significant exposure of a person to unknown amounts of veterinary dosage forms of ivermectin (ingestion, inhalation, parenteral administration or contact with the body surface), the following symptoms were most often observed: skin rash, facial edema, eyelid edema, headache, dizziness, asthenia, nausea , vomiting and diarrhea. Other reported adverse reactions include seizures, ataxia, shortness of breath, abdominal pain, paresthesia, urticaria, and contact dermatitis.

In case of accidental ingestion of the drug, symptomatic therapy is carried out, including parenteral administration of fluids and electrolytes, respiratory support (providing oxygen and, if necessary, artificial ventilation of the lungs) and vasopressors (in the presence of a pronounced decrease in blood pressure). To prevent the absorption of the ingested drug, provoking vomiting and / or urgent gastric lavage may be shown, followed by the use of laxatives and other measures to eliminate intoxication.

Interaction with other medicinal products

Studies on the study of drug interactions with other drugs have not been conducted. The simultaneous use of Solantra cream with other drugs for external and systemic use for the treatment of rosacea has not been studied. Caution should be exercised with the simultaneous use of ivermectin with potent inhibitors of CYP3A4, since the concentration of the drug in the blood plasma can increase significantly.

special instructions

The medicinal product contains:

- cetyl alcohol and stearic alcohol, which can cause local skin reactions (e.g. contact dermatitis),

- methyl parahydroxybenzoate (E218) and propyl parahydroxybenzoate (E216), which can cause allergic reactions (including delayed type),

- propylene glycol, which can irritate the skin.

Wash your hands after applying the drug.

After the drug has dried, cosmetics can be applied. Influence on the ability to drive vehicles and work with mechanisms

Solantra drug does not affect or slightly affects the ability to drive vehicles and work with mechanisms.

Release form

Cream for external use 1%.

15 g or 30 g of cream in a laminated (PE / Alu / PE) tube with a PE head and a PP / PE closure system with child protection; 1 tube with instructions for use in a cardboard box.

Vacation conditions

On prescription.

Storage conditions

At a temperature not higher than 30 ? C.

Keep out of the reach of children.

Shelf life is 2 years.

Do not use after the expiration date.