What Is Levocetirizine?

Levocetirizine chemical name is R-(-)-2- [2- [4-[(4-chlorophenyl) benzyl] -1-piperazinyl] ethoxy] acetic acid, The molecular formula is C21H25ClN2O3, the molecular weight is 388.888800, the density is 1.237g / cm3, and the boiling point is 542.1ºC at 760mmHg. Levocetirizine hydrochloride tablet with its main ingredients is used to treat allergic-related symptoms of the following diseases: allergic rhinitis (including seasonal persistent allergic rhinitis and perennial persistent allergic rhinitis) and chronic idiopathic Sexual urticaria.

Chinese name: Levocetirizine
Foreign name: Levocetirizine

CAS number: 130018-77-8
Molecular formula: C21H25ClN2O3

Levocetirizine compound profile

Levocetirizine Basic Information

Chinese name:

Chinese alias: (R) -cetirizine dihydrochloride; 2- [2- [4-[(4-chlorophenyl) -phenylmethyl] piperazin-1-yl] ethoxy] acetic acid ;

English name: Levocetirizine

English alias: Vardenafil; Vivanza; levocarnitine; vardenafilH;

CAS number: 130018-77-8

Molecular formula: C ₂₁ H ₂₅ ClN ₂ O ₃

Molecular weight: 388.888800

Structural formula:

Exact mass: 388.15500

PSA: 53.01000

LogP: 3.02400 ^[1]

Physiochemical Properties of Levocetirizine

Density: 1.237g / cm ³

Boiling point: 542.1ºC at 760mmHg

Flash point: 281.6ºC

Vapor pressure: 1.39E-12mmHg at 25 ° C ^[1]

Levocetirizine compound related drug detailed introduction

Levocetirizine drug name:

[Common name] Levocetirizine hydrochloride tablets

[English name] Levocetirizine Hydrochoride Tablets

[Chinese Pinyin] Yan Suan Zuo Xi Ti Li Qin Pian ^[2]

Levocetirizine Ingredients:

The main ingredient of this product is Levocetirizine Hydrochloride, the chemical name is: R-(-)-2- [2- [4-[(4-chlorophenyl) benzyl] -1-piperazinyl] ethyl Oxy] acetic acid dihydrochloride ^[2]

Levocetirizine belongs to the category:

Chemicals & Biological Products >> Anti-Allergic Drugs >> H1 Receptor Blockers >> Piperazines

Chemical drugs and biological products >> Anti-allergic drugs >> H1 receptor blockers >> Second-generation H1 receptor blockers ^[2]

Levocetirizine traits:

This product is a white film-coated tablet, which appears white or almost white after removing the film coating. ^[2]

Levocetirizine Pharmacology and Toxicology

Pharmacological action

This product is an oral selective histamine H1 receptor antagonist. There is no obvious anticholinergic and antiserotonin effects, and the central inhibitory effect is small.
Toxicology research

Genotoxicity: The results of Ames test, chromosome aberration test of human lymphocytes, mouse lymphoma test and rat micronucleus test were all negative.

Reproductive toxicity: The results of mouse fertility and general reproductive toxicity tests indicate that when cetirizine is administered orally at a dose of 64 mg / kg (based on body surface area, which is equivalent to approximately 25 times the maximum daily oral dose recommended by adults), No damage to fertility. Mice, rats, and rabbits received oral doses of 96, 225, and 135 mg / kg (based on body surface area, which are approximately equivalent to 40, 180, and 220 times the maximum daily oral doses recommended by adults, respectively). See teratogenic effects. However, there are no adequate and strictly controlled clinical research data on pregnant women. Because animal reproduction studies do not always predict the effects of the drug on humans, this product should only be taken during pregnancy if it is really needed. Oral administration of lactating mice (female mice) at a dose of 96 mg / kg (converted by body surface area, which is equivalent to about 40 times the daily oral dose of adult clinically recommended doses) can cause delayed weight gain in pups. Studies in Beagle dogs have shown that approximately 3% of the dose is excreted in milk.

Carcinogenicity: In carcinogenicity tests administered orally for 2 consecutive years in rats, the dose reached 20 mg / kg (based on body surface area, which is equivalent to approximately 15 times the maximum daily oral dose recommended by adults, or the maximum daily dose recommended by children in clinical practice). 10 times), no carcinogenicity was seen. In the carcinogenicity test of oral administration in mice for 2 consecutive years, the dose reached 16mg / kg (based on body surface area, which is equivalent to approximately 6 times the maximum daily oral dose recommended for adults, or 4 times the maximum daily dose recommended for children. ), It can cause an increase in the incidence of benign liver tumors in male animals; when the dose is 4mg / kg (converted according to body surface area, which is equivalent to approximately twice the maximum daily oral dose recommended by adults, or the maximum daily dose recommended by children) No increase in the incidence of liver tumors was seen. The clinical significance of these findings is unclear. ^[2]

Levocetirizine Pharmacokinetics

The pharmacokinetics of levocetirizine are characterized by a linear relationship between plasma concentration levels and doses, with small differences between individuals.

Levocetirizine is rapidly and completely absorbed in the human body. Eating may cause the absorption rate of levectirizine to decrease, but the total absorption will not decrease. The extent of levoctirizine absorption has nothing to do with the dosage. The results of clinical trials show that the relative bioavailability of 5mg levectirizine tablets is nearly 100%, and the blood concentration reaches a peak about 0.9 hours after administration by adults; levoctirizine and plasma proteins are firmly bound, and the plasma protein binding rate is about 90%, apparent volume of distribution is 0.4L / kg; plasma elimination half-life is 7.9 ± 1.9 hours, 5mg once a day, the plasma concentration reaches steady state after 2 consecutive days; peak plasma concentration after 5mg single dose It was 270 ng / ml, and the steady-state peak of blood concentration after administering 5 mg again was 308 ng / ml. Levocetirizine has no first-pass metabolism, and its metabolic rate in humans is less than 14% of the administered dose. Therefore, it is speculated that the individual differences in liver enzymes or the combined use of liver enzyme inhibitors have little effect on it, and other It is unlikely that matter will interact. On average, 85.4% of levoctirizine was excreted by the urine as a prototype, and 12.9% was excreted by the feces. Levocetirizine is not converted to dextrocetirizine during absorption and elimination. ^[2]

Levocetirizine indications

Treats allergy-related symptoms of the following: allergic rhinitis (including seasonal persistent allergic rhinitis and perennial persistent allergic rhinitis) and chronic idiopathic urticaria. ^[2]

Levocetirizine Usage and Dosage:

Adults, children 6 years and over: Take 1 tablet (5mg) orally daily, which can be taken on an empty stomach, during or after a meal.

Patients with renal impairment: Patients with mild renal impairment do not need to adjust the dosage, and dosages of patients with moderate to severe renal impairment are adjusted according to the following table:

Creatinine clearance rate (ml / min) in patients with renal function statusa dose and number of medications

Moderate renal impairment 30-49 once every 2 days, 5mg

Moderate renal impairment <30 once every 3 days, 5mg

Advanced nephropathy-patients using dialysis <10 Contraindications a. Serum creatinine clearance (CLcr mL / min) = [140-age (years)] × weight (kg) / [72 × serum creatinine (mg / dl)] × 0.85 (female patient coefficient)

Patients with impaired liver function: Only patients with impaired liver function need not adjust the dosage;
For patients with renal impairment, please refer to the "Dosage and Administration of Renal Impairment". ^[2]

Levocetirizine adverse reactions

This product can cause headache, drowsiness, dry mouth, fatigue, weakness, abdominal pain and other adverse reactions in individual patients. ^[2]

Levocetirizine Contraindications

It is forbidden to those who are allergic to any component of this product or those who are allergic to piperazine derivatives. Disabled in patients with advanced renal disease with creatinine clearance <10ml / min. It is contraindicated in patients with special genetic diseases, including rare galactose intolerance, primary lapplactase, or glucose-galactose malabsorption. ^[2]

Levocetirizine Precautions

This product is not recommended for children under 6 years of age, as the film-coated tablets of the product currently available do not allow for dose adjustment.
Although no research data are available at present, some sensitive patients may have effects on the central nervous system when they are taking levecitorizine hydrochloride with alcohol or a central nervous system inhibitor.
Impact on the ability to drive and operate machinery: Controlled clinical trials have shown that levoctirizine does not impair alertness, responsiveness, and driving ability at the recommended dose. If patients need to drive, engage in potentially dangerous activities or operate machinery, do not overdo it and consider their response to this product; co-administration of alcohol or other central nervous system inhibitors may lead to reduced alertness and impaired operating ability . ^[2]