Ebastine has not only an antihistamine effect


Pharmacological properties of the drug Ebastine

Long-acting antihistamine. Has a pronounced affinity for H1 receptors; when it is re-prescribed, no tachyphylaxis is observed. It does not have anticholinergic activity and does not have a sedative effect. The effect develops 1 hour after administration and lasts about 48 hours. After a 5-day course of treatment, the antihistamine effect of ebastine persists for 72 hours. When taken orally, it is quickly absorbed in the digestive tract and metabolized. The maximum concentration in blood plasma is reached after 2.6–4 hours. The half-life is 15–19 hours; in patients with renal and hepatic insufficiency it increases. Ebastine is excreted in the urine.

Evaluation of the effectiveness and safety of ebastine (Kestin) for allergic diseases

Among the second generation antihistamines, Ebastine stands out, being different in its structure. The difference is based on the structure of oxypiperidine, the prototype of one of the first generation antihistamines (diphenylpyraline). Ebastine has the chemical formula C32fl3NO2, its molecular weight is 469.64.

In fact, the main active drug substance exhibiting pharmacological activity is the carboxylated metabolite of ebastine - carebastine.

To create ebastine through the nitrogen atom in the structure of diphenylpyralin, a long aliphatic side chain was attached to the piperidine ring, which provided a long duration of action, low stimulating activity towards central H-histamine receptors, and safety for the cardiovascular system.

Pharmacodynamic characteristics

Features of binding to the receptor. According to the results of the study, ebastine (10 mg orally) binds to approximately 10% of histamine H1 receptors in the brain, therefore rarely causing sedation, while chlorpheniramine binds to 50%, which correlates with the concentration of chlorpheniramine in the blood [8 ].

Antihistamine activity. Single dose efficacy studies have shown that ebastine at doses of 3, 10 and 30 mg significantly reduces histamine-induced wheals compared to placebo. Ebastine statistically significantly suppressed histamine-induced whealing (p<0.001) and hyperemia (p<0.002) reactions at 24 hours after a 10 mg dose.

There is a direct relationship between the time of onset of antihistamine action after taking the drug and the level of carbastine in the blood plasma. Peak plasma concentrations of carebastine coincide with maximum wheal suppression and occur 2 hours after dosing of ebastine.

According to the results of one study, ebastine and astemizole, used for 7 days at a dose of 10 mg/day, equally suppressed the histamine-induced reaction over 24 hours, while loratadine, cetirizine and terfenadine at a dose of 120 mg/day demonstrated , according to the results of the same study, noticeable fluctuations in antihistamine potential [10].

In addition, there is evidence that ebastine has the ability to prevent the development of bronchospasm induced by histamine.

Antiallergic activity. Ebastine suppresses allergen-induced reactions during both intradermal and intranasal provocative tests. When conducting an intradermal test, ebastine at a dose of 1-10 mg was significantly more effective than placebo, and the effect lasted 24 hours. With an intranasal test, 20 mg of ebastine increased the threshold dose of pollen that causes an allergic reaction, much more effectively than placebo [10].

Anticholinergic activity. Ebastine at a dose of 50 mg (five times the therapeutic dose) has no effect on blood pressure, heart rate and salivation.

Effect on the activity of the central nervous system, psychomotor state and the occurrence of sedation. Taking ebastine at a daily dose of 10-30 mg did not affect the ability to drive a car, and at a dose of 50 mg, according to subjective assessment, caused some sedation compared to taking a lower dose of ebastine 10 mg and placebo.

When comparing single doses of ebastine and clemastine, 10 and 20 mg of ebastine were found to be positively different from clemastine in their effects on the ability to visually track a target, subjective assessment of drowsiness and the ability to cause general discomfort [10].

Pharmacokinetic characteristics

Absorption. Ebastine begins to be absorbed immediately after administration, with the concentration of the active metabolite in plasma reaching a maximum 4-6 hours after administration of a dose of 5-40 mg. Evidence of the predictability of the duration and potency of ebastine is the lack of significant differences in the time to reach maximum concentrations between doses. After reaching the maximum concentration, the plasma level of carebastine begins to decrease monoexponentially. Approximately 83% of ebastine is absorbed in the intestine. There were no statistically significant differences in the maximum concentration ^max), time to reach it, area under the plasma concentration-time curve, or half-life for two groups of subjects: those taking ebastine on an empty stomach and not on an empty stomach [10].

During the “first pass” after oral administration, ebastine is extensively metabolized and is almost completely converted to the active metabolite. The conversion occurs mainly in the small intestine. Ebastine is rapidly converted to an active metabolite, has a half-life of approximately 15 hours and a duration of action of at least 24 hours [7].

Distribution and elimination. After taking a single dose (10 mg), the volume of distribution of ebastine ranges from 32.4 to 43.9 l.

Carebastine is approximately 98% bound to human serum proteins, which determines the significant duration of action of the drug.

The half-life of the drug (T^2), apparently independent of the dose used, is 15-18 hours, with 66% of the drug excreted in the urine mainly in the form of a bound metabolite.

With subsequent daily administration of the drug at a dose of 10 mg, a steady-state steady-state concentration is achieved after 3-5 days with a peak plasma concentration of 130 to 160 ng/ml [10].

The use of ebastine at a daily dose of 20 mg for 7 days did not cause any changes in the pharmacokinetic profile of ebastine and carebastine, and the plasma levels of carebastine reached a stable level on the fourth day of therapy. Plasma clearance and half-life are likely similar to those observed after a single dose, as evidenced by the linear pharmacokinetics of carebastine during multiple doses.

The half-life of ebastine makes it advisable to use it once a day for histamine-induced diseases [10].

The half-life of ebastine for both single and multiple doses is approximately 14 hours.

Age characteristics, patients with renal and hepatic insufficiency and ebastine pharmacokinetics. In elderly patients, the volume of distribution does not change significantly, but it increases significantly (up to 74.6 l) in patients with liver cirrhosis, which accounts for the longer average half-life of carebastine in these patients.

In patients suffering from severe renal and hepatic insufficiency, ebastine should be prescribed with caution, only for strict indications, since in these cases the pharmacokinetic profile of carebastine changes due to slower elimination. Thus, in case of renal failure, the half-life increases to 23-26 hours, in case of liver failure - up to 27 hours.

There is no need to change the dosage regimen when treating elderly patients, since there is no difference in the pharmacokinetics of a single dose of ebastine and its equilibrium concentration in elderly people (over 65 years of age) who do not have pathologies of the liver and kidneys, and in young volunteers [10].

According to research results, ebastine can be prescribed to adult patients without any significant clinical differences in the pharmacokinetics of ebastine associated with the age and gender of the patient [1].

Clinical use

It has been proven that the response to the allergen after stopping ebastine continues for another 4 days and then reaches values ​​comparable to those when taking placebo. Therefore, patients should not take ebastine for 4 days before undergoing skin prick tests [2].

Efficiency and safety. Data on the effectiveness and safety of ebastine are based on the results of more than 20 clinical trials.

Two of them assessed the possibility of long-term treatment with ebastine for chronic urticaria. One of them covered 211 patients and lasted 3 months, the other included 101 patients and provided for long-term assessment (up to 1 year).

Although other antihistamines are recommended for clinical use in fixed doses, ebastine was evaluated in phase III trials at both 10 and 20 mg doses, based on the results of preliminary studies to select the optimal dose and compare the effectiveness of different doses. The research results are given below.

  1. In a pilot study to determine the effective dose for allergic rhinitis, 40 patients with pollen allergy received different (ranging from 10-40 mg) doses of ebastine for 4 weeks. All patients noted significant clinical improvement, and there was no significant difference in adverse effects.
  2. In three studies, covering 750 patients (two of them included 487 patients with allergic rhinitis, the third - 263 patients with chronic urticaria) and lasting from 1 to 4 weeks, it was shown
  3. the advantage of a daily dose of ebastine 10 mg compared to doses of 1 and 5 mg per day.
  4. In a study of 101 patients with chronic rhinitis (17 of whom also suffered from chronic conjunctivitis) caused by pollen, there was no dose-response relationship with regard to side effects in patients treated for 7 weeks. ebastine in doses of 10 and 20 mg/day; both doses were effective.
  5. Similar data were obtained in a dose-testing study that included 459 patients with ragweed pollen allergy, a strict indication for ebastine. When compared with daily doses of 1, 3, 10 and 30 mg, the optimal dose was 20 mg/day. It provided symptom relief for 24 hours without causing dose-dependent adverse effects [10].

Allergic rhinitis/rhinoconjunctivitis. Efficacy criteria in clinical trials of ebastine were generally based on patient and/or investigator assessment of both symptoms and overall effectiveness. Four main symptoms were recorded - nasal discharge, nasal congestion, sneezing and itching, and eye symptoms. In a number of studies, the four main symptoms of pathology of the nasal mucosa were combined and assessed using a common scale [19].

A 12-week placebo-controlled, multicenter study was undertaken to evaluate the efficacy and safety of ebastine 10 and 20 mg once daily for the treatment of perennial allergic rhinitis. Patients received:

  • 10 mg ebastine once a day (88 patients);
  • 20 mg ebastine once a day (102);
  • placebo (100).

Symptom severity was rated on a scale of 0–3 points twice daily for the entire 12 weeks of the study.

Both patients and physicians reported a significant clinical benefit of ebastine over placebo at both doses. No serious side effects were observed. All patients tolerated the treatment well and showed low levels of nervous system and headache side effects. The study concluded that ebastine, given at doses of 10 and 20 mg, had a rapid effect on reducing the symptoms of perennial allergic rhinitis (PAR) in adults and adolescents; Subsequently, results were also obtained about additional benefits of the 20 mg dose of ebastine [3, 17].

Comparison with terfenadine and placebo. In three major clinical trials lasting 2 or 3 weeks, 874 patients with seasonal allergic rhinitis, some of whom had concomitant conjunctivitis, received:

  • 10 mg ebastine once a day daily (318 patients);
  • 20 mg ebastine once a day daily (157);
  • 60 mg terfenadine 2 times a day daily (159);
  • placebo (240).

Ebastine at a daily dose of 10 mg over a two-week period provided a rapid and statistically significant reduction in symptoms, including symptoms of conjunctivitis. Ebastine at this dose was significantly more effective than placebo, and comparable in effectiveness in patients with allergic rhinitis and pollen-induced conjunctivitis to terfenadine at a dose of 60 mg 2 times a day. However, ebastine at a daily dose of 20 mg, taken in the morning, achieved more significant improvement in patients with severe symptoms. Patients tolerated ebastine well at both doses (10 and 20 mg/day) during the three-week study period; the frequency of adverse events in the group of patients receiving ebastine was the same as in the placebo group.

The first clinical trial for perennial allergic rhinitis included 151 patients who received:

  • 10 mg ebastine once a day daily (76);
  • placebo (75).

Treatment with ebastine in the form of a single daily dose of 10 mg of the drug for a week allowed most symptoms to be controlled; the overall effectiveness of treatment was higher than in the group of patients receiving placebo. Both researchers and patients rated the overall effectiveness of ebastine as significantly higher than the effectiveness of placebo (in both cases (p < 0.01). Patients tolerated ebastine well; there were no statistically significant differences between groups in the frequency and nature of adverse effects. Frequency dry mouth and drowsiness were almost the same in patients of both groups [10].

In a later two- to three-week placebo-controlled study, 385 patients with perennial allergic rhinitis received:

  • 10 mg ebastine once a day daily (79);
  • 10 mg ebastine 2 times a day daily (74);
  • 20 mg ebastine 1 time per day daily (318);
  • placebo (155).

The differences in the overall assessment of effectiveness between the groups receiving ebastine 10 mg/day and placebo after 7 days from the start of treatment turned out to be statistically significant (p <0.01). In addition, the use of ebastine in a daily dose of 20 mg (in 1 or 2 doses) reduced the severity of the main symptoms of allergic rhinitis compared to placebo.

Comparison with cetirizine. The efficacy and safety of ebastine in relieving symptoms of pollen-induced allergic rhinitis was compared with that of the second generation antihistamine cetirizine.

Over a three-week period, 343 patients received:

  • 10 mg ebastine daily once (116);
  • 20 mg ebastine daily once (111);
  • 10 mg cetirizine once daily (116).

Allergic rhinitis was combined with conjunctivitis in 60% of patients. On the 8th day, discomfort in the nose and eyes decreased in 50% of patients, this decrease persisted until the end of the study. In general, researchers observed a decrease in discomfort in the nose and eyes both in groups of patients receiving ebastine in doses of 10 and 20 mg/day, and in the group receiving cetirizine in a daily dose of 10 mg [20].

However, the higher dose of ebastine was, as judged by patients and investigators, to be significantly more effective than the dose of cetirizine used, and the difference was statistically significant (P = 0.048), according to the investigators. From the patients' point of view, ebastine 20 mg/day was also more effective in reducing discomfort in the nose and eyes than cetirizine 10 mg, the difference being statistically significant after the first week of treatment (p=0.048). In addition, the effects of ebastine 20 mg peaked faster than ebastine 10 mg or cetirizine 10 mg, but the differences were not statistically significant. The safety of treatment was generally equally high in all three groups of patients [16].

This study identified a subgroup of 158 patients with severe symptoms. Symptomatic improvement in this subgroup was significantly more often observed when using ebastine at a dose of 20 mg/day than at a dose of 10 mg/day (p<0.03).

Comparison with loratadine. A comparative study was conducted on the use of ebastine 20 mg and 10 mg, loratadine 10 mg and placebo in the treatment of seasonal allergic rhinitis. Patients received treatment for 4 weeks. The study found that ebastine 20 mg once daily was significantly superior to loratadine 10 mg once daily in reducing rhinitis symptoms throughout the day and over a 4-week period [5,20].

A study has also been conducted on the use of ebastine in the treatment of perennial allergic rhinitis.

The aim of the study was to compare the effectiveness and tolerability of ebastine (10 and 20 mg) with the standard drug loratadine (10 mg) in the daily treatment of PAR [11, 20].

The trial was conducted on 317 patients (aged 12-68 years) with severe symptoms of CAD. Symptoms were rated for severity (0-3) every day and compared with the patients' initial symptoms in a randomized, double-blind study over 4 weeks.

Symptoms including both the year-round index (CI = sneezing + nasal itching + nasal discharge) and the total nasal index (NII = CI + nasal congestion) showed a statistically much greater improvement with ebastine 10 and 20 mg compared with loratadine at a dose of 10 mg for all parameters except sneezing, itching and eye symptoms. Over 4 weeks, the average NRI was reduced by 44, 47 and 32%, respectively, while the difference in treatment effectiveness was evident already 1 week after the start of treatment. The final conclusion of patients and physicians (percentage of patients with improvement) was in favor of ebastine (79 to 85%) compared with loratadine (65 to 66%). The treatment was well tolerated and no adverse effects were observed.

This study showed that ebastine at doses of 10 or 20 mg was more effective than loratadine at a dose of 10 mg for the treatment of PAR [11].

Chronic urticaria. The criteria for the effectiveness of treatment of chronic urticaria were changes in three indicators: itching, number of wheals and their size - compared with those recorded during the initial period of the study.

Comparison with terfenadine and placebo. The effectiveness of ebastine in relieving the symptoms of chronic urticaria in adults was compared with the effectiveness of terfenadine, an established drug for the treatment of urticaria, and placebo in a three-month trial in 211 patients. Patients received:

  • 10 mg ebastine once daily (69);
  • 60 mg terfenadine twice daily (78);
  • placebo (64).

In 204 patients with chronic urticaria with a history of at least 3 months, itching significantly decreased on the 7th and 14th days of treatment in the group of patients taking ebastine at a dose of 10 mg/day, compared with the group taking placebo. The number of blisters also decreased significantly in patients receiving ebastine. The overall incidence of side effects in the group of patients receiving ebastine did not differ significantly from the frequency in the group receiving placebo.

The intensity of itching and the number of blisters per day significantly decreased in the group of patients receiving ebastine, compared with similar indicators in the group receiving placebo. Moreover, once daily use of ebastine has been shown to be as effective as twice daily dosing of terfenadine.

Patients tolerated both ebastine and terfenadine well throughout the study [10].

Tolerance and side effects

The incidence of side effects was assessed during the baseline trial period and during the treatment period. It was not possible to detect any relationship between the dose of ebastine and the frequency of side effects; The safety profile for 10 and 20 mg ebastine was comparable. Other second-generation antihistamines do not have a similar breadth of therapeutic action: exceeding the recommended therapeutic dose is associated with a significant increase in the frequency of side effects.

7 clinical trials were conducted to study the incidence of side effects when using different doses of ebastine. A total of 1452 patients with allergic rhinitis (1329) and chronic urticaria (133) participated in these studies. An overall analysis of the results of all trials showed that the most common adverse events were:

  • headache;
  • dry mouth;
  • sedative effect.

Adverse events were mostly minor or moderate in severity, and no differences in their frequency and severity could be detected in the groups of patients receiving ebastine and placebo.

According to a comparative study, ebastine at a dose of 10 mg/day is comparable to cetirizine at an equivalent dose in terms of the incidence of side effects, which did not increase when the dose of ebastine was increased to 20 mg/day. However, the incidence of sedation in patients receiving cetirizine at a dose of 10 mg/day was higher (7.8%) than in patients receiving ebastine at the same dose (4.3%).

In 101 patients with chronic urticaria, the safety and tolerability of ebastine at a dose of 20 mg/day with long-term use was assessed. Sixty-six patients completed the one-year course of treatment, 12 of whom (18%) experienced 18 adverse reactions, none of which were considered serious by the investigators.

Ebastine has a flexible dosing regimen, combined with a wide range of safety when used.

The dependence of the frequency of adverse reactions on the dose of ebastine has not been established; The safety profile for doses of 20 and 10 mg is comparable. The occurrence of side effects was tested using subjective measures - questionnaires and visual analogue scales. Sedation was noted in a small number of patients when using high doses of the drug. When prescribing therapeutic doses of the drug in the treatment of seasonal or year-round allergic rhinitis, or chronic idiopathic urticaria, no side effects from the central nervous system were noted [6].

In addition, a study was conducted to examine the occurrence of systemic side effects with ebastine.

Cardiotropic effect. The cardiac safety of ebastine has been extensively studied, evaluated, and characterized in phases I-III clinical trials. Ebastine alone at recommended doses of 10 and 20 mg does not have any clinically significant effect on the QT interval in adults or in various special populations (the elderly, children, or patients with impaired renal or hepatic function). Ebastine, used at a dose of 60-100 mg/day, did not cause a clinically significant prolongation of the QT interval [12, 13].

Five 2- to 3-week studies assessed electrocardiographic data, including 12-lead ECG and 24-hour Holter monitoring. An analysis of the duration of the QT interval was carried out in 1202 subjects.

These studies did not detect a dose-dependent increase in the QT interval, nor did they demonstrate an increase in the QT interval by more than 25% of the baseline value. In all those examined, the value of the studied indicator did not exceed 500 m/s. Only 79 (7%) of 1202 patients had a QT interval greater than 444 m/s. The mean maximum QT interval was compared between the ebastine-treated group and the placebo group. It was not possible to detect statistically significant differences in this indicator in any of the groups, except that the average maximum value of the QT interval in the placebo group was significantly higher compared to the group receiving ebastine at a dose of 10 mg/day. There was also no relationship between QT prolongation and ebastine dose. Holter monitoring performed in 226 patients did not reveal any clinically significant data. None of the patients experienced serious side effects.

Change in the duration of the QT interval from baseline in 224 patients receiving:

  • ebastine 10 mg 2 times a day (74);
  • ebastine 20 mg once daily (77);
  • placebo (73).

The mean deviations (as a percentage) of the duration of the QT interval from baseline in both groups of patients receiving ebastine and in the placebo group were not statistically different [10, 12, 13].

Thus, the overall cardiac safety profile of ebastine is very favorable. Based on the information currently available, these findings imply that ebastine, as well as loratadine and cetirizine, are less likely to cause alterations in ventricular repolarization than terfenadine or astemizole [18].

Biological and biochemical safety. None of the clinical studies revealed any tendency towards pathological changes in biochemical and hematological parameters (including the number of red blood cells, leukocytes and platelets).

Dosage and indications for use

The use of ebastine for therapeutic purposes is indicated for:

  • allergic rhinitis and allergic conjunctivitis;
  • hives;
  • itching caused by the release of histamine.

The recommended dose of ebastine for adults and children over 12 years of age is 1 tablet daily (ebastine is available in the form of round white tablets, each containing 10 mg of the drug, 89 mg of lactose and excipients). For the treatment of patients with more severe symptoms, the dose may be increased to 2 tablets (20 mg/day) daily. There are no changes in the frequency and nature of side effects with increasing doses of the drug.

The clinical effect of ebastine does not depend on food intake: the drug can be taken both on an empty stomach and after meals [14].

Drug interactions

According to the study, blood alcohol content did not change after taking 20 mg of ebastine, and the usual pharmacokinetics of carebastine in blood plasma was maintained. In addition, ebastine did not change the level of diazepam in the blood plasma and did not enhance the effect of this sedative drug, and diazepam, in turn, did not affect the pharmacokinetics of carebastine.

Ebastine in a single dose of 20 mg in 12 healthy individuals did not interact with cimetidine after repeated use of the latter. Cimetidine did not affect the conversion of ebastine to carebastine and its subsequent elimination.

Taking ebastine at a dose of 20 mg/day for 10 days, accompanied on the 5th day by a single dose of warfarin at a dose of 25 mg, had no effect on prothrombin time and did not cause clinically significant manifestations. The pharmacokinetic parameters of carebastine and mirror isomers of warfarin also did not change.

No significant changes in the pharmacokinetics of theophylline and carebastine were found with the combined use of ebastine and theophylline.

Chronic administration of ketoconazole alters the metabolism of single dose ebastine, leading to its accumulation as an unmetabolized compound.

Repeated doses of erythromycin have been shown to alter the metabolism of a single dose (20 mg) of ebastine, leading to its accumulation as an unmetabolized substance.

The interaction of ebastine with ketoconazole and erythromycin (which can prolong the QT interval) has been studied. In both cases of combination therapy, there was a pharmacokinetic and pharmacodynamic interaction: there was a prolongation of the QT interval by 18-19 m/s (4.7-5%).

There was no interaction between ebastine and theophylline, warfarin, cimetidine, diazepam and alcohol.

In the case of taking ebastine with food, an increase in the concentration of carebastine in plasma and the area under the curve by 1.5-2 times was observed. At the same time, the time to reach maximum concentration did not increase. Taking ebastine with food does not affect the clinical effect of the drug.

Overdose

There is no specific antidote for an overdose of antihistamines. Taking excessive doses of the drug requires immediate medical intervention. Adults and children who have taken a large dose of the drug are usually monitored at home, but they should still be monitored for 2-3 hours, especially for sedation [9].

The place of ebastine in clinical practice

Ebastine is a new selective H2-histamine receptor antagonist without anticholinergic and sedative effects in therapeutic doses. Ebastine combines the effectiveness of first-generation antihistamines with the improved safety profile of second-generation antihistamines [15]. When using ebastine, a rapid onset and long duration of action are observed [4]. Ebastine, when administered orally at a dose of 10-20 mg/day, causes rapid, effective and long-lasting blockade of histamine H1 receptors, having an excellent safety profile, regardless of the dose.

Conveniently administered once daily, ebastine relieves symptoms of allergic rhinitis, associated or not associated with conjunctivitis and chronic urticaria, and has a high efficacy/safety ratio in the treatment of these diseases. According to clinical studies, the effectiveness of ebastine at a dose of 10 mg/day in the treatment of patients with allergic rhinitis is comparable to terfenadine at a dose of 60 mg 2 times a day. For the treatment of patients with chronic urticaria, ebastine represents a safe and well-tolerated alternative to other non-sedating antihistamines. No interactions of ebastine with alcohol and diazepam were found. Ebastine can be safely recommended to elderly patients.

Ebastine is the only second-generation antihistamine with a wide spectrum of therapeutic action. This allows it to be used in two dosages (10 or 20 mg once daily), and no differences in the frequency of adverse events are observed. Since ebastine in a daily dose of 20 mg is effective for treating severe symptoms of rhinitis, it can be used for both mild and severe forms of allergic rhinitis.

In case of renal failure, the half-life of the drug increases to 23-26 hours, and in case of liver failure - up to 27 hours.

However, greater therapeutic latitude does not lead to an increase in the frequency and severity of side effects. Contraindications to taking the drug are pregnancy and lactation.

On the other hand, there are undeniable advantages of ebastine compared to other antihistamines:

  • binding to plasma proteins is 95-98%;
  • the therapeutic dose of the drug (20 mg) is more effective compared to fexofenadine;
  • the effectiveness of the drug does not depend on food intake. When administered simultaneously with food
  • the level of carebastine in the blood increases 1.6 - 2 times;
  • pharmacokinetics do not change due to the age and gender of the patient;
  • the effect on the duration of the QT interval is not clinically significant even at a dose of 100 mg (significantly - 5-10 times - higher than the therapeutic dose);
  • lack of anticholinergic effects;
  • does not potentiate the effect of alcohol and benzodiazepines;
  • does not have a sedative effect;
  • does not affect the ability to drive a car;
  • flexible dosage of the drug.

After 5 days of use of ebastine, activity remains for 72 hours due to the action of active metabolites, which is significant for high compliance with treatment, since it makes it possible to skip a dose of the drug without the risk of developing allergic reactions.

Thus, ebastine can be considered the optimal or one of the optimal drugs for the treatment of allergies.

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