What Is Cetirizine Dihydrochloride?

Cetirizine is a potent H1 receptor antagonist that is taken orally into the body and quickly binds to the histamine H1 receptor on the target cell membrane, blocking histamine from activating target cells. Cetirizine has no significant anticholinergic and serotonin effects. At normal doses, it is not easy to penetrate the blood-brain barrier. This product can inhibit the transmission of histamine in the early stage of allergy, reduce the migration activity of inflammatory cells and the release of transmitters in the late stage of allergy, so it is also effective for the late stage allergy. This product is a highly selective H1 receptor antagonist, so far no adverse effects on cardiac electrical activity have been found.

Cetirizine hydrochloride

Cetirizine is a powerful

Common name: Cetirizine hydrochloride

English name: Cetirizine Hydrochloride

English alias Cetrizine Di-HCl; Cetirizine Hydrochloride; 2- (2- {4-[(4-Chlorophenyl) (phenyl) -methyl] piperazino} ethoxy) acetic acid dihydrochloride; Cetrizine dihydrochloride; (2- {4-[(4 -chlorophenyl) (phenyl) methyl] piperazin-1-yl} ethoxy) acetic acid dihydrochloride

The chemical name is: (±) -2- [2- [4-[(4-chlorophenyl) benzyl] -1-piperazinyl] ethoxy] acetic acid dihydrochloride

CAS Registry Number: 83881-52-1

Molecular formula: C21H25ClN2O3 · 2HCl

Molecular weight: 461.81 ^[1]

Seasonal and perennial allergic rhinitis, nasal conjunctivitis,

Adults 10mg 1 time / day. Elderly people with renal dysfunction should reduce the dosage, 10 mg once / day or 5 mg twice daily for children 6-12 years old, and 5 mg once daily for children 2-6 years old.

Cetirizine is a metabolite of hydroxyzine in humans, and animal experiments have proven that cetirizine hydrochloride is a peripheral

Acute toxicity: The LD50 of Kunming mice is 758.1mg / kg (95% confidence limit is 712.1 ~ 806.9mg / kg), and the LD50 of tail vein injection is 131.1mg / kg (95% confidence limit is 120.8 ~ 142.1mg / kg).

Identification:

(1) Take about 10mg of this product, add 2ml of sulfuric acid, place in warm water, the solution will be yellow, and the yellow will disappear after dilution with water. National Medicine of the People's Republic of China

Histamine H1 receptor antagonist. For seasonal or perennial

This product is suitable for allergic diseases of the respiratory system, skin and eyes, including perennial allergic diseases, such as allergic skin diseases,

Cetirizine hydrochloride is a second-generation H1 antihistamine, which is a long-acting, selective oral strong anti-allergic drug. H1

10mgqd for adults. Elderly people with renal dysfunction should reduce the dosage, 10mgqd or 5mgbid for children aged 6-12, 5mgqd for children aged 2-6.

Occasionally mild drowsiness, headache, dizziness, dry mouth and gastrointestinal discomfort.

Avoid co-administration or drinking with sedatives.

After oral administration of 10 mg, the blood concentration was reached in 30-60 minutes, and the peak blood concentration at 1 hour was 257 ug / L (980 ug / L in children). Food factors have no effect on the extent of absorption, but can slightly affect the rate of absorption. This product

Improve the literature to synthesize cetirizine and optimize industrial production. Method to

Establishing Cetirizine Hydrochloride Tablets

The human pharmacokinetics and relative bioavailability of domestic cetirizine hydrochloride tablets were studied. Methods: Eight male healthy volunteers were selected, and single-dose (10mg) oral domestic cetirizine hydrochloride tablets and imported cetirizine hydrochloride tablets were measured by reversed-phase high performance liquid chromatography with ultraviolet 229nm as the detection wavelength. Cetirizine concentration in the human body. Results: The in vivo dynamic process of cetirizine hydrochloride was a two-compartment open model of first-order absorption. The cmax of domestic and imported tablets was (316.71 ± 39.66) and (314.80 ± 31.79) ng / ml, and the tmax was (0.72). ± 0.09) and (0.72 ± 0.09) h, t1 / 2 is (10.71 ± 3.06) and (9.95 ± 2.41) h, and AUC0 are (2728.52 ± 356.06) and (2753.01 ± 360.33) ng * h / ml . Conclusion: The relative bioavailability of domestic cetirizine hydrochloride tablets is (99.50 ± 8.89)%; cmax and AUC0 were selected for three-way analysis of variance and two-sided and one-sided t test. The results showed that domestic tablets and imported tablets The formulation is bioequivalent.