One of the most popular tools from allergies is cetirizine. Based on this active substances created many anti-allergic drugs in different forms of production. The first time I discovered this drug, and why it is considered one of the best Allergy drugs?
- HISTORY OF DISCOVERY
- CERTIFICATE OF SUBSTANCE
- WHAT IS THE SAFETY OF THE DRUG
- EFFECTIVENESS IS PROVEN
Cetirizine, the active substance of a number of antihistamines. Is competitive antagonist of histamine by blocking H1-histamine receptors. The drug included in the list of vital and essential medicines. Since 2007, in the United States cetirizine approved for use without a prescription.
In the instruction it is specified that, in addition, the antihistamine effect of cetirizine prevents and facilitates the development of a number of allergic reactions.
History of discovery
In the 20-ies of the last century scientists have found that the most important mediator of allergic reactions is histamine. This substance is considered to be the main intermediary in the implementation of such allergic reactions as rhinitis, pruritus, urticaria, asthma and anaphylactic shock.
Since histamine it has become evident that drugs that will suppress the activity of this substance, will allow to stop or prevent the development of allergic reactions. 20 years later was created the first antihistamines.
In the mid 60-ies it was found that external allergic manifestations are due to the fact that histamine binds to histamine receptors of the first type (H1 receptors). Then the question arose about the development of better antihistamines which selectively block the H1 receptors.
In 1987 was created the drug is cetirizine a highly selective blocker of H1-receptors. After binding to the receptor, the histamine is not able to communicate with them. This prevents the implementation of allergic symptoms, which in some cases can be fatal to humans.
Cetirizine is an antihistamine of the second generation. Unlike the previous generation of drugs, antiallergic drugs of the second generation do not have sedative action.
Research conducted in 1999 (Grant A. J., Danielson L. A., Rihoux J.-P., DeVos S.,) and in 2002 (Purohit A., Duvernelle C., Melac m, Pauli G., Frossard N., 2001; Frossard N., Purohit A., Melac m, Pauli G.,) showed that cetirizine copes well with skin itching and redness due to its ability to penetrate the skin.
Certificate of substance
Cetirizine is a metabolite gidroxizina. The chemical name of the drug [2-[(4-chlorophenyl) phenylmethyl]-1-piperazinyl] ethoxy] acetic acid.
From gidroxizina cetirizine is characterized in that in the side chain are attached hydroxyl (-OH) group. It would seem that such a minor change should not affect the chemical and physical properties of the drug, but it is not. Attaching a hydroxyl group to the side chain gidroxizina provides cetirizine negative charge at physiological values of pH (pH). Such a property drastically reduces the ability of molecules to enter the brain through the blood-brain barrier. This removes the effects of the drug on the Central histamine receptors in the brain.
The chemical formula of the preparation ensures a high affinity for peripheral H1-receptors, thereby locking the latter to histamine. The positive moment is the fact that even at high concentrations of cetirizine does not block serotonin receptors, adrenergic receptors, dopamine and cholinergic receptors. Therefore, cetirizine is devoid of side effects associated with impacts on these groups of receptors.
What is the safety of the drug
Randomized placebo-controlled trials have shown the safety of cetirizine for adults and children. The study was conducted as a dose 5, 10 mg / day and 60 mg per day.
Children have a normal reaction of the skin to histamine was restored for three days after discontinuation of the drug. Studies with the use of cetirizine in infants aged 6 to 11 months have shown its safety in this age group. In the instructions to the drug indicated that children aged 6-12 months should take the drug under medical supervision.
It is noteworthy that studies with cetirizine are now. One recent study dates back to July 26, 2018, where we investigated the effect of cetirizine and other antihistamines on cognitive abilities of the patient. In the study, researchers from Hungary indicates that cetirizine may have a negative impact on cognitive abilities of the patient.
Effectiveness is proven
The efficacy and safety of cetirizine, proven, and indisputable. The drug is used to relieve some allergic symptoms, mainly nasal and ocular. Also, the drug effectively cope with the symptoms of urticaria and allergic dermatitis.
Our database PubMed on request Cetirizine issued about 1,800 scientific articles. The drug was conducted fairly randomized studies that showed its safety. Therefore, in the present anti-allergic drugs on the basis of cetirizine are one of the primary means relieves and prevents Allergy symptoms.
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