Solantra cream for external use 1%, 30g

Composition

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of 1 g of cream contains:  

Active ingredient:

Ivermectin 10.0 mg.

Auxiliary substances:  

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,

Stearic alcohol 25.0 mg,

Macrogol cetostealer ether 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 up to 1000 mg

Pharmacological action

Antimicrobial and antiprotozoal agents.

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 ivermectin for external use have been observed in animal models of skin inflammation. Ivermectin also causes the death of parasites, mainly through selective binding and high affinity for glutamate-regulated chlorine channels found in 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 may be associated with both the anti-inflammatory effects of ivermectin and the ability of ivermectin to cause the death of Demodex mites, which, in turn, are a factor that causes skin inflammation.

Pharmacokinetics

Suction

The absorption of ivermectin contained in Solantra was evaluated in a clinical study involving adult patients with severe papulo-pustular rosacea who used the maximum allowable dose of the drug.

At steady state (after 2 weeks of treatment), the highest mean (± standard deviation) plasma concentrations of ivermectin were observed within 10 ± 8 hours after use of the drug (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 at steady state. With longer-term treatment in phase 3 studies, the systemic exposure to ivermectin remained the same as after two weeks of treatment.

At steady state, systemic exposure to ivermectin (AUC0-244: 36 ± 16 ng h / ml) was lower than after a single oral dose of 6 mg of ivermectin in healthy volunteers (AUC0-244: 134 ± 66 ng h/ml).

Distribution

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

Metabolism

In vitro studies using human liver microsomes and recombinant CYP450 enzymes have shown that ivermectin is mainly metabolized 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 (1 A 2,2 B 6,2 C 9 or ZA 4) in human hepatocyte culture. Two major metabolites of ivermectin (3”-0-demethyl ivermectin and 4a-hydroxy ivermectin) were identified in a clinical pharmacokinetic study with the maximum allowable dose of the drug and studied during phase 2 clinical trials.

Similar to the parent compound, the metabolites reached an equilibrium state by the end of the second week of treatment, and no signs of accumulation were observed for up to 12 weeks. In addition, systemic exposures to metabolites (estimated using Cmax and AUC) obtained at steady state were much lower than those after oral use of ivermectin.

Deduction

The final elimination half-life averaged 6 days (approximately 145 hours, range: 92-238 hours). in patients who applied the drug to the skin once a day for 28 days during a clinical pharmacokinetic study when using the maximum allowable dose of the drug.

Elimination 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 (papulo-pustular form) in adult patients.

Use during pregnancy and lactation

Pregnancy

Data on the use of ivermectin in pregnant women are limited or absent. Studies of reproductive toxicity when taking ivermectin orally have shown that the drug has a 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.

Breast-feeding period

After oral use, low concentrations of ivermectin are excreted in breast milk. With external use of the drug, the release of ivermectin into breast milk has not been studied.

Pharmacokinetic and toxicological data obtained from animal studies also indicate the release of ivermectin into breast milk. The risk to an children cannot be excluded. If it is necessary to use the drug, you should consult with your doctor to make a decision on stopping breastfeeding.

Contraindications

– Hypersensitivity to the Active ingredient or any other component of the drug;

– pregnancy;

– breast-feeding period;

– children under 18 years of age (the safety and effectiveness of the drug for this age category has not been studied).

With caution:

Impaired liver function.

Side effects

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

As a rule, these reactions are mild or moderate in nature and usually weaken with continued therapy.

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

Interaction

Studies on the interactions of the drug with other drugs have not been conducted.

The concomitant use of Solantra cream with other topical and systemic medications for the treatment of rosacea has not been studied.

Caution should be exercised when concomitantly using ivermectin with potent CYP3A4 inhibitors, since the concentration of the drug in the blood plasma can significantly increase.

How to take, course of use and dosage

For external use only.

Apply Solantra cream 1 time a day daily for the entire 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 (the size of a pea) to each of the five areas of the face: forehead, chin, nose and cheeks. Spread the drug in a thin layer over the entire face, avoiding contact with the eyes, lips and mucous membranes.

Solantra should only be applied to the face.

In patients with impaired renal function and elderly patients, no dose adjustment is required.

Overdose

No cases of overdose of Solantra have been reported.

If a person has been exposed to unknown amounts of veterinary medicinal forms of ivermectin accidentally or significantly (ingestion, inhalation, parenteral use, or contact with the body surface), the most common symptoms were 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 performed, including parenteral use of fluids and electrolytes, respiratory support (providing oxygen supply and, if necessary, artificial ventilation of the lungs) and vasopressors (in the presence of a pronounced decrease in blood pressure).

To prevent absorption of the ingested drug, provoking vomiting and/or urgent gastric lavage may be indicated, followed by the use of laxatives and other measures to eliminate intoxication.

Special instructions

The medicinal product contains:

– cetyl alcohol and stearyl alcohol, which can cause local skin reactions (for example, contact dermatitis),

– methyl parahydroxybenzoate (E 218) and propyl parahydroxybenzoate (E 216), which can cause allergic reactions (including delayed type),

– propylene glycol, which can cause skin irritation.

After applying the drug, you should wash your hands.

After the drug has dried, cosmetics can be applied.

Form of production

Cream from white to light yellow color

Active ingredient

Ivermectin

Conditions of release from pharmacies

By prescription

Dosage form

cream