Desloratadin
The most common adverse reactions (>1/100 to <1/10), the frequency of which was slightly higher than with placebo: 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 adverse reaction was headache (5.9%), the frequency of which was no higher than when taking placebo (6.9%).
Information on adverse reactions is presented based on the results of clinical studies and observations of the post-registration period.
According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: very often (>1/10), often (from ≥1/100 to <1/10), infrequently (from ≥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 adverse reactions indicated in the instructions worsen, or you notice any other adverse reactions not listed in the instructions, tell your doctor.
DESLORATADINE (tablets)
I'm an allergy sufferer, I succumbed to the influence of a not very experienced allergy sufferer - my mother: “We need to take DEZloratadine!
Because DEZ doesn’t make you sleepy. Pebble drinks it and generally feels good." Pebble is a neighbor who is a prophet from a foreign country. Frets. Let's listen to Pebble. And although in my very, very close circle of friends I have three respected allergists in the city (even four!), I have already heeded all their advice at one time. Picking my eyes out of their sockets every day, I agree to listen to Galkin’s advice.
I bought two DEZloratadins. And by order. One is from the manufacturer BIOCOM, the other is from another. I don't know if I'll get to the point of comparison. Maybe the allergy will go away on its own if you manage to change the climate in the next couple of days.
Biosynthetic DEZloratadine is coated tablets. This means that they will not be absorbed in the stomach. This means they will act more slowly. A simple logic chain. All that remains is to check how long this effect will last and how many bumps on my forehead I will get with a cloudy head.
The first experiment was scheduled for a working day. Dangerous! Well, what if people look at me, and I scratch my nose, then my eyebrow, or pick my ear, or even wink at the wrong time, because my eye itches, but you can’t scratch it - it’s made up. They come to me for treatment, but I myself look like I’m sick. God forbid that revenues will fall because of this and people will go to another clinic where the administrators don’t bother. Then the bosses will kill me.
Half of this tablet was not enough for me to relieve scabies. I restrained my awkward movements with my arms, shoulders and facial muscles as best I could. But at the same time, the whole working day I felt as if I was watching a movie about myself. I am not me, especially the one who works. But I, being me, held my head in my hands all day so that it wouldn’t fall on the table. Damn, you can even break your nose. In short, a complete zombie, no worse than from suprastin. I don’t know how I made it to the end of the working day. Lived - that's a big word. More precisely, it pre-existed. And this despite the fact that the instructions say that the drug does not have any effect on the central nervous system.
Experiment two. For the day after tomorrow. Sunday, no need to go to work. Snot - in different directions, tears - in the same direction. My eyes are itching - I would wish it on my enemy. But there are none. I decided to snatch the whole pill. An hour later, when my eyes didn’t itch any less and I really wanted to sleep, I realized that I wouldn’t drink DEZloratadine anymore. A two-hour afternoon nap (strong, with a pleasant dream) saved me a little. But my eyelids look like after a full six-hour workout in the gym. Open your eyes - how to lift a barbell in a snatch, and then throw the barbell, close your eyes, rest for sixty seconds. This is how I communicated with my people all day. I didn't look at them. I listened to them.
I have to go to work tomorrow. Let me comb my hair better. But on the other hand, I will give everyone what they ask for and give the correct change. Otherwise, then you won’t be able to justify yourself by saying that it wasn’t out of malice that I cheated by a thousand))), it’s the pills’ fault))).
I know for sure that the selection of such drugs is an individual matter. I can’t recommend it, at least from my own experience. But if you determine at random that DEZloratadine from Biosynthesis helps you well, then a big amen to you and wishes for good health.
Don't sneeze or itch! And don't cough!
Your Beauty Eleonora.
Desloratadine FT
- Pharmacodynamics Desloratadine is a long-acting, non-sedating antihistamine with selective antagonistic effects on peripheral histamine H1 receptors. After oral administration, desloratadine selectively blocks peripheral H1-histamine receptors, since it practically does not penetrate the blood-brain barrier. Desloratadine is the main active metabolite of loratadine. In vitro studies have shown that desloratadine has antiallergic effects, including inhibiting the release of proinflammatory cytokines, including IL-4, IL-6, IL-8 and IL-13, from human mast cells/basophils. Desloratadine also inhibits the expression of adhesion molecule (P-selectin) in endothelial cells. These data have no proven clinical significance. The fact that desloratadine practically does not penetrate the blood-brain barrier has been confirmed in controlled studies. When using the recommended dose of 5 mg/day of desloratadine in adults and adolescents, the incidence of somnolence was not higher than that in the placebo group. In clinical and pharmacological studies in adults, desloratadine did not increase the effects of alcohol such as impaired psychomotor function and drowsiness. The results of the psychomotor test did not reveal a significant difference in patients who received desloratadine and placebo alone or in combination with alcohol (see section "Interactions with other medicinal products and other types of interactions"). In a multiple-dose study of desloratadine in adults and adolescents with daily use of the drug in doses of up to 20 mg per day for 14 days, it was found that desloratadine did not cause clinically or statistically significant changes in the cardiovascular system. In a study in which adults and adolescents took desloratadine at a dose of 45 mg/day (9 times the recommended therapeutic dose) for 10 days, there was also no prolongation of the QTc interval on the ECG. Recommendations for dosing of desloratadine in children from 6 months are based on comparative pharmacokinetic studies. The safety of syrup containing desloratadine was studied in 3 placebo-controlled studies in 246 children aged 6 months to 11 years. Children aged 6 months to 11 years with a history of seasonal allergic rhinitis or chronic idiopathic urticaria received desloratadine at doses of 1 mg/day (age 6-11 months), 1.25 mg/day (age 1-5 years), and 2 .5 mg/day (age 6-11 years). Treatment was well tolerated as measured by clinical tests, laboratory tests, vital signs, and ECG data (measurement of changes in interwave intervals, including the QTc interval). Taking into account the recommended doses, the pharmacokinetics of desloratadine in children were comparable to the pharmacokinetics in adults. The effectiveness of oral desloratadine has not been studied in pediatric studies. However, because the pathogenesis and course of allergic rhinitis and chronic urticaria, and the pharmacokinetic profile of desloratadine are similar in children and adults, efficacy data in adults may also indicate efficacy in children. Desloratadine selectively blocks histamine H1 receptors, thereby preventing the secretion of histamine, a causative factor for all types of urticaria, regardless of etiology. It is expected that desloratadine will be effective in relieving the symptoms of not only chronic idiopathic urticaria, which was a clinical model in the study of the effectiveness of desloratadine, but also its other types, according to clinical recommendations (with the exception of acute urticaria as one of the manifestations of an anaphylactic reaction (see section "Special Instructions and Precautions"): In 2 placebo-controlled studies in patients with chronic idiopathic urticaria for 6 weeks, desloratadine was effective in relieving itching and reducing the size and number of rashes at the end of the first course of treatment. In each study, the effect was maintained for 24 hours post-dose. Studies excluded a minority of patients who were not responsive to antihistamines. Greater than 50% relief of itching was observed in 55% of patients who received desloratadine, compared with 19% of patients who received placebo. Use of desloratadine was also significant reduced the negative impact of the disease on sleep and daytime activity, which was assessed on a four-point scale.
Pharmacokinetics Absorption Desloratadine is well absorbed. Within 30 minutes after oral administration, desloratadine can be detected in the blood plasma. The maximum concentration in blood plasma is reached after approximately 3 hours. The relative bioavailability of desloratadine is proportional to the dose administered over a dose range of 5 mg to 20 mg. Absolute bioavailability is unknown. Distribution Desloratadine is moderately (83-87%) bound to plasma proteins. In patients with renal and/or hepatic insufficiency, the degree of binding of desloratadine and 3-hydroxydesloratadine to plasma proteins is not changed compared to that in patients with normal renal and hepatic function. There is no evidence of clinically significant accumulation of desloratadine following dosing of 5-20 mg once daily for 14 days. Metabolism Desloratadine is metabolized to the active metabolite 3-hydroxydesloratadine and then undergoes glucuronidation. The enzyme that is responsible for the metabolism of desloratadine has not been identified, therefore interactions of desloratadine with other drugs cannot be excluded. In vivo and in vitro studies have shown that desloratadine does not inhibit CYP3A4 and CYP2D6, and is neither a substrate nor an inhibitor of P-glycoprotein. Elimination The terminal half-life is approximately 27 hours. Administration of 14C-labeled desloratadine showed that approximately 84% of the total dose was equally excreted in urine and feces. Plasma analysis of the metabolite 3-hydroxydesloratadine showed that its Tmax and t1/2 are similar to the Tmax and t1/2 of desloratadine. Desloratadine is practically not excreted by hemodialysis (0.3%). There are no data regarding the elimination of desloratadine by peritoneal dialysis. Effect of food on pharmacokinetics A study with a single dose of desloratadine 7.5 mg found that food (high-calorie, high-fat breakfast) or grapefruit juice did not affect the pharmacokinetics of desloratadine. Special Populations Patients with Renal Impairment The pharmacokinetics of desloratadine in patients with chronic renal failure (CKD) were compared with those in healthy controls in one single-dose study and one multiple-dose study of desloratadine. In a single-dose study, the AUC of desloratadine was 2 and 2.5 times greater in patients with mild/moderate and severe renal impairment, respectively, than in healthy volunteers. In a study using repeated doses of desloratadine, steady state was achieved after the 11th day of treatment. Compared with healthy subjects, the AUC of desloratadine was approximately 1.5 times higher in patients with mild to moderate forms of chronic renal failure and approximately 2.5 times higher in patients with severe forms of chronic renal failure. In both studies, changes in Cmax and AUC of desloratadine and 3-hydroxydesloratadine were not clinically significant. Patients with Hepatic Impairment The pharmacokinetics of desloratadine after a single oral dose in patients with mild (4 patients), moderate (4 patients) and severe (4 patients) hepatic impairment (Child-Pugh classification) was compared with that in 8 subjects with normal hepatic function. . In patients with hepatic impairment, regardless of its degree, an approximately 2.4-fold increase in AUC was observed compared with healthy subjects. The clearance of desloratadine in patients with mild, moderate and severe hepatic impairment was 37%, 36% and 28%, respectively, of that in healthy study subjects. An increase in the mean half-life was also observed in patients with hepatic impairment. The mean Cmax and AUC values of 3-hydroxydesloratadine were not statistically significantly different from those in healthy subjects. The degree of plasma protein binding of desloratadine and 3-hydroxydesloratadine did not change in patients with liver disease. The incidence of adverse reactions with a maximum 10-day treatment in patients with moderate hepatic impairment (Child-Pugh class B) was not increased. Children In separate single-dose studies, the Cmax and AUC of desloratadine were comparable in children receiving age-appropriate recommended doses and in adults receiving desloratadine 5 mg syrup. Thus, in children aged 6 to 11 years, a single dose of 2.5 mg of desloratadine in the form of an internal solution and in children from 2 to 5 years of age, a single dose of 1.25 mg of desloratadine in the form of an internal solution led to concentrations of desloratadine in blood plasma comparable to that in adults who took 5 mg desloratadine tablets. However, the Cmax and AUC values of the metabolite of desloratadine (3-hydroxydesloratadine) were 1.27 and 1.61 times higher when adults took an oral solution containing 5 mg of desloratadine in a single dose, compared with the Cmax and AUC obtained in children from 2 to 11 years old, receiving 1.25-2.5 mg of desloratadine as a solution for internal use. A single dose of desloratadine oral solution containing 0.625 mg or 1.25 mg was administered to children aged 6-11 months and 12-23 months, respectively. The results of the pharmacokinetic analysis revealed that a dose of 1 mg for children aged 6-11 months and 1.25 mg for children aged 12-23 months is required to achieve plasma concentrations of desloratadine similar to those obtained when taken by adults as a single dose. doses of 5 mg desloratadine as a solution for internal use. Elderly Subjects: In elderly subjects (65 years of age or older), after repeated doses of desloratadine tablets, mean Cmax and AUC values were 20% higher than in subjects less than 65 years of age. Total clearance (Cl/F) after adjustment for body weight was similar in subjects of both age groups. The mean plasma half-life of desloratadine was 33.7 hours in subjects aged 65 years or older. Pharmacokinetic parameters for 3-hydroxydesloratadine were unchanged in older subjects compared to younger subjects. Differences in pharmacokinetic parameters associated with age are unlikely to be clinically significant, so dose adjustment is not required in elderly patients. Poor Metabolizers The conversion of desloratadine (DL) to 3-hydroxydesloratadine (3-DL) is significantly slower in a portion of the population due to phenotypic polymorphism that is not yet fully understood. The prevalence of slow metabolizers among the Caucasian population is 6% (adults and children aged 2 to 11 years), and among the Black population it is 18% (adults) and 16% (children). They have higher concentrations of desloratadine in the blood. The area under the concentration-time curve ratio of desloratadine and 3-hydroxydesloratadine is also higher (AUC DL / AUC 3-DL > 10 at normal). Similar pharmacokinetic parameters were observed in a repeated-dose study in children with slow metabolizers who were diagnosed with allergic rhinitis." Exposure (AUC) of desloratadine was approximately 6 times greater and Cmax approximately 3-4 times higher and reached after 3-6 hours compared with AUC and Cmax in children with normal metabolism of desloratadine. Half-life in children with delayed The metabolism of desloratadine is approximately 120 hours. The extent of exposure to desloratadine was similar in poor metabolizers of adults and children at age-appropriate doses. The overall safety profile in these subjects was not different from that in the general population. In children under 2 years of age with poor metabolizers the effect of desloratadine has not been studied.
