Allertek

Allertek is a systemic antihistamine medication, a piperazine derivative.

Cetirizine, which is a metabolic element of hydroxyzine, is a potent selective antagonist of peripheral H1-terminations of histamine. When tested in vitro for synthesis with endings, no noticeable affinity for endings other than H1 was found. [1]

The use of standard servings of cetirizine leads to an improvement in quality and health in people with seasonal or chronic rhinitis with allergic etiology.

Indications Allertek

It is used to eliminate eye and nasal signs of year-round or seasonal rhinitis (allergic origin), as well as to eliminate the symptoms of idiopathic urticaria (chronic stage).

Release form

The drug is produced in tablets - 7 or 20 pieces inside a cell pack. The box contains 1 such pack.

Pharmacodynamics

In addition to the antagonistic effect on the H1 endings, cetirizine demonstrates antiallergic activity: in persons with intolerance caused by the action of an allergen, a 10 mg portion taken 1-2 times a day slows down the influx of eosinophils into the conjunctiva and epidermis.

During placebo-controlled testing, in which a large dose of cetirizine (60 mg) was used for 7 days, there was no statistically significant prolongation of the QT interval. [2]

Pharmacokinetics

Aged people.

In 16 elderly people, when a single 10 mg dose was administered, the half-life increased by approximately 50%, and the clearance rate decreased by 40% in comparison with other patients. There is an assumption that the decrease in the level of drug clearance in elderly volunteers was caused by renal dysfunction.

Children, including babies.

In the period of 6-12 years, the half-life of cetirizine is approximately 6 hours, and in the age subgroup of 2-6 years - 5 hours. In children under 2 years of age, this figure decreases to 3.1 hours.

Persons with renal dysfunction.

Pharmacokinetic characteristics of drugs with mild renal dysfunction (CC level - less than 40 ml per minute) were similar to those observed in healthy people. With moderate renal dysfunction, the half-life term was threefold prolonged, and the clearance rate decreased by 70%.

In individuals who are on hemodialysis (CC values are less than 7 ml per minute), when using a 1-fold portion of 10 mg of cetirizine, the half-life was three times longer, and the clearance value was 70% less. Hemodialysis weakly excretes cetirizine from plasma. People with severe or moderate renal dysfunction may need to adjust the dosage of the medication.

Individuals with hepatic dysfunction.

In people with chronic hepatic pathologies (cirrhosis of the biliary type and liver disease caused by cholestasis), who once used 10 or 20 mg of Allertek, the half-life term was prolonged by 50%, and the level of clearance fell by 40%. A dosage change is required only with the simultaneous presence of dysfunctions of both the kidneys and the liver in the patient.

Dosing and administration

The tablet is taken orally with plain water - swallowed without chewing.

The age subgroup 6-12 years old should take 0.5 tablets (5 mg) 2 times a day. Persons over 12 years old and adults - 1 tablet 1 time per day.

Individuals with severe or moderate renal dysfunction.

Because the excretion of cetirizine is realized through the kidneys, in the absence of the possibility of using alternative methods of therapy, the intervals between the use of drugs should be personally selected (taking into account the degree of renal dysfunction).

Dosage change for an adult with renal dysfunction:

Absence of violations (CC level ≥80 ml per minute) - 10 mg of drugs 1 time per day;

Mild dysfunction (CC indicator in the range of 50-79 ml per minute) - 10 mg of the substance 1 time per day;

Moderate dysfunction (CC value within 30-49 ml per minute) - 5 mg of the drug 1 time per day;

Severe dysfunction (CC indicators <30 ml per minute) - 5 mg of drugs with 1 application after 2 days;

Terminal phase of renal failure (in persons undergoing dialysis; CC level <10 ml per minute) - it is forbidden to use.

For children with renal dysfunction, the portion is selected personally, taking into account the age and weight, as well as the child's QC indicators.

The duration of the therapeutic course is selected by the doctor personally, taking into account the nature of the pathology.

• Application for children

Allertek is not used in persons under the age of 6, because with this form of drug release, it is impossible to find a dosage suitable for the child.

Use Allertek during pregnancy

There is not enough information regarding the effect of the medication on pregnant women. Animal testing does not show direct or indirect effects on pregnancy, fetal and embryonic development, labor, or postnatal development. It is necessary to use the medicine very carefully during pregnancy - only in situations where the doctor determines that the benefits of drug administration are more likely than the risks of complications for the fetus.

Cetirizine can be excreted in mother's milk in values that are 25-90% of the plasma indicator (depending on the length of the time interval that has passed since the drug was taken). Because of this, with hepatitis B, the drug is used with extreme caution.

Contraindications

The main contraindications:

• severe intolerance associated with the active element or auxiliary components of the drug, and in addition to hydroxyzine or any piperazine derivative;
• severe renal dysfunction (CC level - below 10 ml per minute);
• rare forms of galactose intolerance (hereditary), Lapp lactase deficiency or glucose-galactose malabsorption (these contraindications refer to the drug in the form of coated tablets).

Side effects Allertek

Among the side signs:

• disorders affecting the blood system and lymph: thrombocytopenia is observed singly;
• immune lesions: rarely, intolerance is observed. Anaphylaxis develops singly;
• problems with the nutritional regimen and metabolic processes: possibly increased appetite;
• mental disorders: sometimes there is agitation, accompanied by anxiety. Depression, insomnia, confusion, aggression, and hallucinations are rare. A single nervous tic develops. Perhaps the appearance of thoughts of suicide;
• problems with the work of the NA: sometimes there are paresthesias. Occasionally, movement disorders or seizures appear. Dyskinesia, syncope, dysgeusia, dystonia or tremor develop singly. Perhaps a memory disorder or the appearance of amnesia;
• lesions affecting the visual organs: visual blurring, accommodation disorder or movement disorder that affects the eyeballs appears;
• dysfunction of the auditory organs and balance: vertigo may occur;
• heart problems: occasionally tachycardia appears;
• disorders in the digestive tract: diarrhea is sometimes observed;
• symptoms from the hepatobiliary system: hepatic dysfunction is occasionally noted (an increase in the values of alkaline phosphatase, bilirubin, transaminases and GGT);
• lesions in the epidermis and subcutaneous layer: sometimes rashes or itching develop. Occasionally, urticaria occurs. A single fixed medical erythema or Quincke's edema is observed;
• disorders affecting the kidneys and urethra: enuresis or dysuria is singly noted. Development of urinary retention is possible;
• systemic problems: sometimes malaise or asthenia occurs. Puffiness occasionally appears;
• change in the indications of diagnostics and laboratory tests: occasionally, weight increases.

Overdose

Signs of intoxication with cetirizine are mainly associated with effects on the central nervous system or with symptoms that are similar to the anticholinergic effect.

With a very severe overdose (exceeding the standard daily portion at least five times), diarrhea, mydriasis, stupor, confusion, headaches, anxiety, severe fatigue, tachycardia and dizziness were observed. In addition, malaise, itching, tremors, drowsiness, urinary retention, and sedation.

The medicine has no antidote. In case of poisoning, gastric lavage is performed (in situations where less than 60 minutes have passed since the drug was taken) and symptomatic actions. The dialysis procedure will not be effective.

Interactions with other drugs

In tests with multiple use of theophylline (0.4 g once a day) together with cetirizine, an insignificant (by 16%) decrease in the level of the latter's clearance was noted. At the same time, changes in theophylline values with such a combination occurred.

During tests with repeated administration of ritonavir (0.6 g 2 times per day) together with cetirizine (10 mg per day), the exposure duration of the latter increased by approximately 40%. Ritonavir showed a decrease of 11%.

The absorption volume of cetirizine does not decrease when consumed with food, while the absorption rate slows down by 60 minutes.

Storage conditions

Allertek must be stored in a place protected from sunlight, moisture and small children. Temperature level - maximum 25 ° C.

Shelf life

Allertek is allowed to be used within a 4-year period from the date of manufacture of the pharmaceutical substance.

Analogs

The analogs of the medication are the drugs Zirtek, Tsetrilev, Alergolik, Zodak with Aleron, Analergin and Ksizal with Alercetin. In addition, the list includes Letizen, Amertil, Lazin with Contrahist Alerji, Cetirinax and Glenzet with Levzirin, Cetrin, Egizin and Cetirizin with Cetrinal.