Allertek

Allertek is a systemic antihistamine drug, a derivative of piperazine.

Cetirizine, which is the metabolic unit of hydroxyzine, is a potent, selective antagonist of peripheral H1 histamine terminals. In vitro synthesis tests with terminals have shown no significant affinity for terminals other than H1.[ 1 ]

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

Indications Allertek

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

Release form

The drug is produced in tablets - 7 or 20 pieces in a blister pack. There is 1 such pack in a box.

Pharmacodynamics

In addition to its antagonist effect on H1 endings, cetirizine exhibits antiallergic activity: in individuals with intolerance caused by the action of an allergen, a dose of 10 mg taken 1-2 times a day slows the influx of eosinophils into the conjunctiva and epidermis.

In a placebo-controlled trial using a large dose of cetirizine (60 mg) for 7 days, no statistically significant prolongation of QT interval was observed.[ 2 ]

Pharmacokinetics

Elderly people.

In 16 elderly subjects, when a single 10 mg dose was administered, the half-life increased by approximately 50% and the clearance rate decreased by 40% compared to other patients. It is suggested that the decrease in 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 the drug in mild renal dysfunction (creatinine clearance level is less than 40 ml per minute) were similar to those observed in healthy people. In moderate renal dysfunction, the half-life was prolonged threefold, and the clearance rate was reduced by 70%.

In individuals undergoing hemodialysis (creatinine clearance values are less than 7 ml per minute), when using a single dose of 10 mg cetirizine, the half-life was three times longer and the clearance value was 70% lower. Hemodialysis poorly excretes cetirizine from plasma. Individuals with severe or moderate renal dysfunction require a change in the dosage of the drug.

Persons with liver dysfunction.

In patients with chronic liver pathologies (biliary cirrhosis and liver diseases caused by cholestasis), who used 10 or 20 mg of Allertek once, the half-life was prolonged by 50%, and the clearance rate decreased by 40%. Dosage adjustments are required only if the patient has both kidney and liver dysfunction.

Dosing and administration

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

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

Persons with severe or moderate renal dysfunction.

Since cetirizine is excreted through the kidneys, if alternative methods of therapy are not possible, the intervals between drug administrations should be individually selected (taking into account the degree of renal dysfunction).

Dosage adjustment for an adult with renal dysfunction:

No violations (CC level ≥80 ml per minute) – 10 mg of the drug once a day;

Mild dysfunction (creatinine clearance in the range of 50-79 ml per minute) – 10 mg of the substance once a day;

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

Severe dysfunction (CC values <30 ml per minute) – 5 mg of the drug with 1-time administration after 2 days;

Terminal phase of renal failure (in individuals undergoing dialysis; CC level <10 ml per minute) – prohibited for use.

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

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

• Application for children

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

Use Allertek during pregnancy

There is insufficient information regarding the effects of the drug on pregnant women. Animal testing does not demonstrate direct or indirect effects on the course of pregnancy, fetal and embryonic development, as well as the process of birth or postnatal development. The drug should be used very carefully during pregnancy - only in situations where the doctor determines that the benefit of administering the drug is more likely than the risks of complications for the fetus.

Cetirizine can be excreted in breast milk in amounts that make up 25-90% of the plasma level (depending on the length of time that has passed since taking the drug). Because of this, the drug is used with extreme caution during breastfeeding.

Contraindications

Main contraindications:

• severe intolerance associated with the active ingredient or auxiliary components of the drug, as well as with hydroxyzine or any derivative of piperazine;
• those with severe renal dysfunction (creatinine clearance level is below 10 ml per minute);
• rare forms of galactose intolerance (hereditary), Lapp lactase deficiency or glucose-galactose malabsorption (these contraindications apply to the drug in the form of coated tablets).

Side effects Allertek

Side effects include:

• disorders affecting the blood system and lymph: thrombocytopenia is observed occasionally;
• immune disorders: intolerance is observed occasionally. Anaphylaxis develops occasionally;
• problems with nutritional regimen and metabolic processes: possible increase in appetite;
• Mental disorders: sometimes agitation is observed, accompanied by anxiety. Depression, insomnia, confusion, aggression and hallucinations are occasionally observed. A nervous tic occurs sporadically. Suicidal thoughts may appear;
• problems with the functioning of the nervous system: sometimes paresthesia occurs. Movement disorders or seizures occur occasionally. Dyskinesia, syncope, dysgeusia, dystonia or tremor develop occasionally. Memory disorders or amnesia may occur;
• lesions affecting the visual organs: occasional blurred vision, accommodation disorder or movement disorder affecting the eyeballs;
• disturbances of the auditory organs and balance: vertigo may occur;
• problems with cardiac activity: tachycardia occasionally appears;
• gastrointestinal disorders: sometimes diarrhea is observed;
• symptoms from the hepatobiliary system: liver dysfunction is occasionally observed (increased levels of alkaline phosphatase, bilirubin, transaminases and GGT);
• lesions in the epidermis and subcutaneous layer: sometimes rashes or itching develop. Urticaria occurs rarely. Fixed drug erythema or Quincke's edema is observed isolated;
• disorders affecting the kidneys and urethra: enuresis or dysuria are observed sporadically. Urinary retention may develop;
• systemic problems: sometimes there is malaise or asthenia. Occasionally, swelling appears;
• changes in diagnostic and laboratory test results: weight increases occasionally.

Overdose

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

In severe overdoses (at least five times the standard daily dose), diarrhea, mydriasis, stupor, confusion, headaches, anxiety, severe fatigue, tachycardia, and dizziness have been observed. In addition, malaise, itching, tremors, drowsiness, urinary retention, and sedation have been reported.

The drug 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 are taken. The dialysis procedure will not be effective.

Interactions with other drugs

When testing multiple doses of theophylline (0.4 g once daily) together with cetirizine, an insignificant (16%) decrease in the clearance level of the latter was observed. At the same time, no changes in the theophylline values occurred with this combination.

In tests with multiple doses of ritonavir (0.6 g twice daily) and cetirizine (10 mg daily), the duration of exposure to cetirizine increased by approximately 40%. Similar values for ritonavir showed a decrease of 11%.

The absorption volume of cetirizine is not reduced when taken with food, although the rate of absorption is slowed by 60 minutes.

Storage conditions

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

Shelf life

Allertek is approved for use within a 4-year period from the date of manufacture of the pharmaceutical substance.

Analogues

The medicine's analogues are Zirtek, Cetrilev, Allergolik, Zodak with Aleron, Analergin and Xizal with Alercetin. In addition, the list includes Letizen, Amertil, Lazin with Contrahist Allergy, Cetirinax and Glencet with Levzirin, Cetrin, Egizin and Cetirizine with Cetrinal.