Solantra (Soolantra)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceIvermectinIvermectin
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  • Solantra
    cream externally 
    Galderma S.A.     Switzerland
    • Dosage form: & nbspTOfor external use.
    Composition:

    1 g cream contains:

    Active substance: 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, stearic alcohol 25.0 mg, macrogol cetostearyl 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, water purified to 1000 mg.

    Description:

    Cream from white to light yellow color.

    Pharmacotherapeutic group:antimicrobial and antiprotozoal agent
    ATX: & nbsp

    D.11.A.X.22   Ivermectin

    Pharmacodynamics:

    Ivermectin belongs to the avermectin group, which has an anti-inflammatory effect by suppressing the production of inflammatory cytokines induced by lipopolysaccharides. Anti-inflammatory properties of ivermectin for external use have been observed in models of skin inflammatory processes in animals. Ivermectin also causes the death of the parasite, mainly via the selective binding and high affinity to a glutamate-gated chloride channel located 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 it can be associated with both the anti-inflammatory effects of ivermectin and the ability of ivermectin to kill mites Demodex, which, in turn, are a factor that causes inflammation of the skin.

    Pharmacokinetics:

    Suction

    The absorption of ivermectin contained in the preparation of Solantra was evaluated in a clinical study with the participation of adult patients with a severe degree of papulo-pustular rosacea form, using the maximum permissible dose of the drug. In the equilibrium state (after 2 weeks of treatment), the highest mean ± standard deviation of ivermectin concentration in the blood plasma was observed within 10 ± 8 hours after the drug was administered (CmOh: 2.1 ± 1.0 ng / ml, range: 0.7-4.0 ng / ml), and the highest mean (± standard deviation) AUC0-24 h was 36 ± 16 ng h / ml, range: 14-75 ng / ml). Systemic exposure of ivermectin reached a plateau by the end of the second week of treatment under equilibrium conditions. With longer treatment in the 3-phase studies, the system exposure index of ivermectin remained the same as after a two-week treatment. In conditions of equilibrium concentration, the levels of systemic exposure of ivermectin (AUC0-24 h: 36 ± 16 ng h / ml) were lower than after single ingestion of 6 mg ivermectin in healthy volunteers (AUC0-24 h: 134 ± 66 ng h / ml).

    Distribution

    Study in vitro showed that the binding of ivermectin to plasma proteins (predominantly albumin) is more than 99%. Significant binding of ivermectin with erythrocytes was not observed.

    Metabolism

    In studies in vitro using human liver microsomes and recombinant enzymes CYP450 it was noted that ivermectin metabolized, mainly by inhibitors CYP3 A4.

    Research in vitro showed that ivermectin does not inhibit isoenzymes CYP450 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4, 4A11 or 2E1. Ivermectin does not induce the expression of enzymes CYP450 (1A2, 2B6, 2C9 or 3A4) in human hepatocyte culture. 2 major metabolites of ivermectin (3 "-O-demethyl ivermectin and 4a-hydroxy ivermectin) were detected during the clinical study of pharmacokinetics with the application of the maximum permissible dose of the drug and were studied during the phase 2 clinical trials. Like the initial compound, the metabolites reached the equilibrium state by the end of the second week of treatment, no signs of accumulation were observed in the period up to 12 weeks.In addition, system exposures of metabolites (estimated using CmOh and AUC), obtained at an equilibrium state, were much lower than those after ingestion of ivermectin.

    Excretion

    The final half-life period 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 study of pharmacokinetics 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 hepatic and renal function.
    Indications:

    Treatment of inflammatory skin lesions with rosacea (papule-pustular form) in adult patients.

    Contraindications:

    - Hypersensitivity to the active ingredient or any other component of the drug;

    - pregnancy;

    - the period of breastfeeding;

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

    Carefully:

    Violation of the function of the liver.

    Pregnancy and lactation:

    Pregnancy

    Data on the use of ivermectin in pregnant women are limited or absent. Reproductive toxicity studies with oral ivermectin have shown that the drug has a teratogenic potential in rats and rabbits, but due to low systemic exposure to external application in 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 application of the drug, the isolation of ivermectin in breast milk has not been studied. Pharmacokinetic and toxicological data obtained by the results of animal studies also indicate the isolation of ivermectin in breast milk. The risk for an infant can not be ruled out. If it is necessary to use the drug, you should consult your doctor to make a decision to stop breastfeeding.

    Dosing and Administration:

    For external use only.

    Apply Solantra cream once a day daily throughout the course of treatment - up to 4 months. If necessary, the course of treatment can be repeated.

    In the absence of improvement after 3 months of treatment, treatment should be discontinued.

    A small amount of cream (the size of a pea) to apply to the skin of each of the five areas of the face: the forehead, chin, nose and cheeks. Distribute the drug thinly throughout the face, avoiding contact with the eyes, lips and mucous membranes.

    Solantra should be applied only on the face.

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

    Side effects:

    The most frequent adverse reactions, such as burning sensation, skin irritation, pruritus and dry skin, were noted in less than 1% of patients who received medication in clinical trials.

    Typically, these reactions are mild or moderate and usually weaken with continued therapy.

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

    Undesirable reactions obtained during clinical trials of the Solantra preparation are presented in Table 1. These reactions are classified according to organ systems and development frequency as follows: very often (≥ 1/10), often (from ≥ 1/100 to <1/10) , infrequently (from ≥ 1/1 000 to <1/100), rarely (from ≥ 1/10 000 to <1/1 000), very rarely (<1/10 000), it is unknown (it is impossible to estimate, based on available data).

    Table 1.

    System of organs

    Frequency emergence

    Undesirable reactions

    Infringements from skin and subcutaneous fabrics

    Often

    Burning sensation of the skin

    Infrequently

    Skin irritation, itching, dry skin

    Unknown

    Contact dermatitis, allergic

    reactions
    Overdose:

    No reports of cases of drug overdose Solantra have been recorded.

    In case of accidental or significant exposure to unknown quantities of veterinary medicinal forms of ivermectin per person (ingestion, inhalation, parenteral administration or exposure to the body surface), the most common symptoms are: skin rash, face swelling, eyelid edema, headache, dizziness, asthenia, nausea , vomiting and diarrhea. Other reported adverse reactions include: convulsions, ataxia, dyspnea, 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, support of breathing (providing oxygen supply and, if necessary, artificial ventilation) and vasopressors (with a marked decrease in blood pressure). To prevent absorption of ingested medication, vomiting and / or urgent gastric lavage may be indicated, followed by the use of laxatives and other measures to eliminate intoxication.

    Interaction:

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

    Simultaneous application of Solantra cream with other drugs for external and systemic use for the treatment of rosacea has not been studied.

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

    Special instructions:

    The medicinal preparation contains:

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

    - methyl parahydroxybenzoate (E218) and propyl parahydroxybenzoate (E216), 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, cosmetic products can be applied.
    Effect on the ability to drive transp. cf. and fur:

    Solantra's preparation does not influence or slightly affects the ability to drive vehicles and work with machinery.

    Form release / dosage:

    Cream for external use, 1%.

    Packaging:

    For 15 g or 30 grams of cream in a laminated (PE / Al / PE) tube with a PE head and a closure system made of PP / PE with protection from opening by children; 1 tube with instructions for use in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003692
    Date of registration:20.06.2016
    Expiration Date:20.06.2021
    The owner of the registration certificate: Galderma S.A. Galderma S.A. Switzerland
    Manufacturer: & nbsp
    Representation: & nbspGALDERMA, LLCGALDERMA, LLCRussia
    Information update date: & nbsp18.08.2016
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