Pharmacological properties of the drug Erius
Desloratadine is a selective blocker of peripheral histamine H1 receptors that does not have a sedative effect. Desloratadine is the primary active metabolite of loratadine. In preclinical studies of desloratadine and loratadine, no qualitative or quantitative differences in the toxicity of the 2 drugs at comparative doses (taking into account the concentration of desloratadine) were identified. After oral administration, Erius selectively blocks peripheral H1-histamine receptors and does not penetrate the BBB. Numerous studies have shown that in addition to antihistamine activity, Erius has antiallergic and anti-inflammatory effects. It has been established that Erius inhibits a cascade of various reactions underlying the development of allergic inflammation, namely:
- release of pro-inflammatory cytokines, including interleukins (IL): IL-4, IL-6, IL-8, IL-13;
- release of pro-inflammatory chemokines such as RANTES;
- production of superoxide anion by activated polymorphonuclear neutrophil granulocytes;
- adhesion and chemotaxis of eosinophilic granulocytes;
- expression of adhesion molecules such as P-selectin;
- IgE-dependent release of histamine, prostaglandin D2 and leukotriene C4;
- acute allergic bronchospasm in animal studies.
In clinical studies, daily intake of Erius at a dose of up to 20 mg for 14 days was not accompanied by statistically significant clinically significant changes in the cardiovascular system. Its use at a dose of 45 mg/day (9 times higher than the therapeutic dose) for 10 days did not cause an increase in the QT . Erius does not penetrate the BBB. When used at the recommended dose of 5 mg, the incidence of drowsiness did not exceed that in the placebo group. In clinical studies, Erius had no effect on psychomotor reactions when taken at a dose of up to 7.5 mg/day. Pharmacokinetics. Desloratadine is determined in blood plasma within 30 minutes after administration. The maximum concentration in the blood plasma is reached after 3 hours, the half-life is on average 27 hours. The degree of accumulation of desloratadine corresponds to its half-life (about 27 hours) and the frequency of use (1 time per day). The bioavailability of desloratadine is proportional to the dose, ranging from 5 to 20 mg. Desloratadine is moderately (83–87%) bound to plasma proteins. When used at a dose of 5–20 mg once a day for 14 days, no clinically significant accumulation of the drug was detected. When conducting cross-comparative studies with the same dose of the drug, the bioequivalence of the drug in the form of tablets and syrup was proven. The results of the studies showed that desloratadine does not inhibit CYP 3A4 or CYP 2D6 and is neither a substrate nor an inhibitor of P-glycoprotein. A single dose of desloratadine 7.5 mg with food (a high-fat, high-calorie breakfast or grapefruit juice) did not affect the distribution of desloratadine.
Erius
Erius (desloratadine) is a long-acting antihistamine. Histamine is a biologically active substance that is abundantly released into the intercellular space during allergic diseases. Traditional histamine receptor blockers suppress the activity of histamine, but do not affect other pathogenetic mechanisms underlying the development of the allergic inflammatory response. In addition, they have a number of undesirable side effects that significantly limit their use (for example, sedation due to the lack of selectivity of action on histamine receptors). Erius is a new generation antihistamine that affects all key parts of the allergic reaction and does not have a negative effect on the central nervous system or the cardiovascular system. Today, this drug has essentially replaced Claritin, which until recently was the most prescribed antihistamine in the world. Erius, in turn, has a higher affinity for H1-histamine receptors while maintaining a favorable safety profile and the virtual absence of clinically significant side effects that could lead to discontinuation of the drug or limit its use. In addition, Erius is endowed with anti-inflammatory and anti-edematous effects, the development mechanism of which is not associated with inactivation of histamine receptors. Desloratadine, the active ingredient of the drug, is a metabolite of loratadine, an order of magnitude more active than its predecessor. Thanks to this, the therapeutic dose of Erius is half that of drugs based on loratadine. Among all antihistamines known today, Erius has the highest selectivity and degree of affinity for H1-histamine receptors, which gives it the most favorable safety profile.
The drug has additional antiallergic properties that are not associated with antihistamine activity - it suppresses the expression of cell adhesion molecules, prevents the release of other mediators of inflammatory reactions, and inhibits the formation of superoxide anion. This ability of the drug significantly expands the scope of its use and opens up new opportunities for the relief of acute allergic reactions and the treatment of chronic diseases of an allergic nature. Unlike antihistamines of earlier generations, Erius does not affect cardiac conduction parameters and does not have a negative effect on the digestive tract. Fatty foods, grapefruit juice and other specific foods do not reduce the bioavailability of the drug and do not affect its pharmacokinetic and pharmacodynamic characteristics. The drug can be taken regardless of meals, incl. and on an empty stomach. It is quickly absorbed into the gastrointestinal tract and begins to act within half an hour from the moment of administration. The peak action of Erius is observed 1-2 hours after administration. Therapeutic concentrations of the drug in the blood are maintained for 24 hours. Severe renal failure is a limiting factor in treatment with Erius and requires special caution when prescribing the drug. Erius does not affect cognitive performance, attention and concentration and does not potentiate the effects of ethanol. The drug is contraindicated during pregnancy and breastfeeding. It can be used in pediatric practice in patients older than 2 years.
Use of the drug Erius
To eliminate symptoms associated with allergic rhinitis (including intermittent and persistent) and chronic idiopathic urticaria, Erius in the form of tablets or syrup is taken orally, regardless of food intake, in the following doses. Tablets Adults and adolescents (over 12 years of age) - 1 tablet (5 mg) 1 time per day. The tablet should be swallowed whole with water. It is advisable to take the drug regularly at the same time of day. The duration of treatment is determined by the severity and course of the disease. Treatment of intermittent allergic rhinitis is carried out taking into account the patient's medical history and can be stopped after the symptoms disappear and resumed when they reappear. Continuous treatment may be recommended for patients with persistent allergic rhinitis throughout the period of exposure to the allergen. Syrup Children aged 6–11 months - 2.0 ml (1 mg) 1 time per day; 1 year–5 years - 2.5 ml (1.25 mg) 1 time per day; 6–11 years - 5.0 ml (2.5 mg) 1 time per day. Adults and adolescents (over 12 years of age) are prescribed 10.0 ml of syrup once a day. The drug is taken regardless of meals.
ERIUS TAB 5MG N10
In children 12–17 years old, according to the results of clinical studies, the most common side effect was headache (5.9%), the frequency of which was no higher than when taking placebo (6.9%).
Information on side effects is presented based on the results of clinical studies and observations of the post-registration period.
According to WHO, side effects are classified according to their frequency as follows: very common (≥1/10); often (from ≥1/100 to <1/10); uncommon (from ≥1/1000 to <1/100); rare (from ≥1/10000 to <1/1000); very rare (<1/10000); frequency unknown (it was not possible to determine the frequency of occurrence based on available data).
From the mental side:
very rarely - hallucinations.
From the nervous system:
often - headache, insomnia (children under 2 years of age); very rarely - dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.
From the liver and biliary tract:
very rarely - increased activity of liver enzymes, increased bilirubin concentration, hepatitis; frequency unknown - jaundice.
From the digestive system:
often - dry mouth, diarrhea (children under 2 years of age); very rarely - abdominal pain, nausea, vomiting, dyspepsia, diarrhea.
From the SSS side:
very rarely - tachycardia, palpitations; frequency unknown - prolongation of the QT interval.
From the musculoskeletal system:
very rarely - myalgia.
For the skin and subcutaneous tissues:
frequency unknown - photosensitivity.
Common disorders:
often - increased fatigue, fever (children under 2 years of age); very rarely - anaphylaxis, angioedema, shortness of breath, itching, rash, incl. hives; frequency unknown - asthenia.
Post-registration period.
Children: frequency unknown - QT interval prolongation, arrhythmia, bradycardia.
If any of the side effects indicated in the description worsen, or the patient notices any other side effects not listed in the description, the doctor should be informed.
Film-coated tablets
The most common side effects (≥1/100 to <1/10), the frequency of which was slightly higher than with placebo (“dummy”): increased fatigue (1.2%), dry mouth (0.8% ) and headache (0.6%).
Syrup
In children from 6 to 23 months, the following side effects were observed, the frequency of which was slightly higher than with placebo: diarrhea (3.7%), increased body temperature (2.3%), insomnia (2.3%).
In children aged 2 to 11 years, when using the drug Erius® in the form of syrup, the frequency of side effects was the same as when using placebo.
According to the results of clinical studies, no side effects were identified in children from 6 to 11 years of age when taking the drug in recommended doses (2.5 mg/day).
In adults and adolescents (12 years and older), according to the results of clinical studies, side effects were recorded in 3% of patients compared to the group of patients using placebo, of which the most common were: increased fatigue (1.2%), dryness during mouth (0.8%), headache (0.6%).
Side effects of the drug Erius
In clinical studies, when using the drug Erius according to indications for use, including allergic rhinitis and chronic idiopathic urticaria at the recommended dose of 5 mg/day, the incidence of side effects was 3% higher than when using placebo. When using the drug Erius, the most common side effects (compared to placebo) were fatigue (1.2%), dry mouth (0.8%), headache (0.6%). Very rarely - hypersensitivity reactions (including anaphylactic reaction and rash), tachycardia, palpitations, increased activity of liver enzymes, bilirubin, hepatitis. When using syrup in children aged 6 to 23 months, diarrhea (3.7%), chills (2.3%) and insomnia (2.3%) were most often noted; in other age categories - increased fatigue (1.2%), dry mouth (0.8%), headache (0.6%).
Aerius®
The most common side effects (≥1/100 to <1/10), the frequency of which was slightly higher than with placebo (“dummy”): increased fatigue (1.2%), dry mouth (0.8% ) and headache (0.6%).
In children aged 12-17 years, according to the results of clinical studies, the most common side effect was headache (5.9%), the frequency of which was no higher than when taking placebo (6.9%).
Information on side effects is presented based on the results of clinical studies and observations of the post-registration period.
According to the World Health Organization (WHO), side effects are classified according to their frequency as follows: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 up to <1/100), rare (from ≥1/10000 to <1/1000), very rare (<1/10000); frequency unknown - based on available data, it was not possible to determine the frequency of occurrence.
From the mental side: very rarely - hallucinations; frequency unknown - abnormal behavior, aggression.
From the nervous system: often - headache; very rarely dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.
From the liver and biliary tract: very rarely - increased activity of liver enzymes, increased bilirubin concentration, hepatitis; frequency unknown - jaundice.
From the digestive system: often - dry mouth; very rarely - abdominal pain, nausea, vomiting, dyspepsia, diarrhea, increased appetite.
From the cardiovascular system: very rarely - tachycardia, palpitations; frequency unknown - prolongation of the QT interval.
From the musculoskeletal system: very rarely - myalgia.
From the skin and subcutaneous tissues: frequency unknown - photosensitivity.
General disorders: often - increased fatigue; very rarely - anaphylaxis, angioedema, shortness of breath, itching, rash, including urticaria; frequency unknown - asthenia.
Laboratory and instrumental data: increased body weight.
Post-registration period
Children: frequency unknown - QT prolongation, arrhythmia, bradycardia, abnormal behavior, aggression.
If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.
Special instructions for the use of the drug Erius
The effectiveness and safety of using syrup in children under 6 months of age and tablets in children under 12 years of age has not been fully established. In clinical and pharmacological studies, Erius did not enhance the effects of alcohol such as impaired psychomotor function and drowsiness. Psychomotor test results did not differ significantly between patients who received Erius and placebo alone or with alcohol. During pregnancy and breastfeeding. Erius is not recommended for use during pregnancy, since the safety of the drug in pregnant women has not been established. Desloratadine passes into breast milk, so it is recommended to stop breastfeeding during treatment with the drug. effects on the ability to drive vehicles or operate complex machinery .
