Oral solution aticizal 2.5mg/5ml An Thien treat allergic rhinitis (90ml)

ATC code: R06A E09.

Mechanism of action: Levocetirizine is the isomers (R) of Cetirizine, a strong and selective antagonist of the peripheral H1 H1 receptor, but hardly impacts on other receptors, so there is almost no acetylcholine antagonistic effect and no serotonin antagonistic effect. Levocetirizine inhibits the early stage of allergic reactions through histamine intermediaries and also reduces the relocation of inflammatory cells and reduces the release of intermediate substances at the late stage of allergic reactions.

Studies show that Levocetirizine has a high affinity for H1 receptors. Levocetirizine has an affinity for H1 receptors 2 times higher than Cetirizine. Levocetirizine separated from H1 receptor with a semi -discharged time of 115 ± 38 minutes.

Hematopological pharmacological studies in healthy volunteers prove that levocetirizine at half the dose of Cetirizine has the same activity as Cetirizine, both in the skin and nose.

Dynamic pharmacokinetics

absorption: Levocetirizine absorbs quickly and widely by oral. In adults, the peak concentration in plasma is achieved after 0.9 hours and reaches a stable state after 2 days.

The peak concentration after the single dose and the repeated dose of 5 mg are 270 ng/ml and 308 ng/ml. The level of absorption does not depend on the dose and is not changed by food, but reduces or slowly reaches the peak concentration.

distribution:

90% Levocetirizine is connected to plasma proteins.

The distribution of levocetirizine is limited, the distribution volume is 0.4 liters/kg.

transformation:

The metabolism of levocetirizine in humans is less than 14% of the dose. The metabolic path includes the process of oxidation of aromatic compounds, n and o dealers and taurin complexes, levocetirizine does not affect the activity of isenzyme CYP 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 at higher concentration than the peak concentration after taking a dose of 5 mg.

Levocetirizine is low and inability to inhibit metabolism, so there is no interaction of levocetirizine with other substances, or vice versa.

excretion:

Semi -selling time in adult plasma is 7.9 ± 1.9 hours. Shorter selling time in children. The average clearance in adults is 0.63 ml/min/kg.

levocetirizine and its metabolites are mainly eliminated through urine (85.4%), 12.9% are eliminated in feces.

levocetirizine is eliminated by glomerular filtration and excretion in the renal tubules.

kidney failure:

Levocetirizine's clearance is correlated with creatinine clearance. Therefore, the recommendation of adjusting the distance of levocetirizine dose is based on creatinine clearance in medium and severe renal impairment patients. For patients with end -stage kidney disease, the total clearance of the drug decreases by about 80% compared to normal people. The amount of levocetirizine is removed during 4 hours of hemorrhage is

liver failure:

pharmacokinetics of levocetirizine in liver failure patients have not been tested.

Elderly:

Mobile pharmacokinetic data in the elderly is limited. Levocetirizine is mainly eliminated in urine. Therefore, the dose of levocetirizine should be adjusted in accordance with the kidney function in elderly patients.

Notify the physician the unwanted effects when using the drug.

Be cautious when using

need to be very careful when taking the drug for patients in the following cases:

Be cautious when used simultaneously with alcohol.

Be cautious in patients with risk factors for urinary retention (eg spinal cord lesions, prostate hyperplasia) because levocetirizine may increase the risk of urinary retention.

Not enough data for the use of levocetirizine for infants and children under 2 years old.

Autodium warning:

The ingredient containing methyl paraben and propyl paraben, which can cause allergic reactions (bronchospasm).

The drug contains sorbitol and sucrose, patients with fructose intolerant treatment disorders, glucose absorption disorders - galactose or a deficiency of sucrose - isomaltose should not use this drug.

Colonel contains Sunset Yellow, which is at risk for allergic reactions.

The effect of the drug on driving and operating machinery

Clinical trials shows that levocetirizine at the recommended dose does not impair mental alertness, reaction ability or driving ability in healthy people. However, some patients may see drowsiness, fatigue and weakness when treating with levocetirizine. Therefore, patients intend to drive, participate in dangerous activities or operate machinery, so be cautious and pay attention to the adverse reaction when taking the drug.

Use drugs for women during pregnancy and lactation

Pregnant women:

Data studying the use of levocetirizine in pregnant women is limited. Animal research does not show direct or indirect effects on pregnancy, fetal/embryonic development, childbirth or postpartum development.

The use of levocetirizine may be considered during pregnancy if necessary.

breastfeeding women:

Cetirizine has been shown to be excreted in breast milk. Therefore, levocetirizine also has the ability to excrete in breast milk. Levocetirizine adverse reactions may be observed in breastfed babies. Therefore, be careful when prescribing levocetirizine for breastfeeding women.

Interactive drug

There is no study of interactive drugs of levocetirizine.

Studies on Cetirizine racemic isomers show that there is no interaction with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and CYP3A4.

The absorption of levocetirizine is not affected by food but the absorption rate decreases.

In sensitive patients, using Cetirizine or Levocetirizine along with alcohol or other central neurological inhibitors can reduce alertness and reduce functioning efficiency.

In the multi-dose study between Ritonavir (600 mg x 2 times a day) and Cetirizine (10 mg daily), the level of contact with Cetirizine has increased by about 40% while ritonavir changes slightly (-11%) compared to Cetirizine simultaneously.

In the multi -dose study between theophyllline (400 mg once daily) and Cetirizine, there is a slight reduction in the clearance of cetirizine (16%) while theophylline tends to not be affected by the drug used in Cetirizine.

Cavalry: Due to no studies on the correlation of the drug, do not mix this drug with other drugs.