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Chlorpheniramine maleate is available in tablets and injections, also known as paracetamol, an antihistamine, which exerts an anti-allergic effect through antagonism of H1 receptors. It is mainly used for rhinitis, skin and mucous membrane allergy and relief of cold symptoms such as tearing, sneezing and runny nose.
Uses and functions of Chloropheniramine maleate.
Indications for colds and allergic diseases of the skin and mucous membranes, the function of urticaria, eczema,dermatitis, drug rash, pruritus, neurodermatitis, insect bites, solar dermatitis, can also be used for allergic dermatitis, vasodilatory rhinitis, drug and food allergies.
In addition to a strong competitive blockade of the role of histamine H1 receptors on the target cells of the allergic reaction, through the antagonism of the H1 receptor to play an anti-allergic effect, but also has the effect of anti-M cholinergic receptors, so after taking the drug can be dry mouth, constipation, sputum thickening, nasal mucous membrane dryness and other symptoms.
Pharmacological Effect of Chloropheniramine maleate.
Chlorpheniramine is an H1 receptor antagonist, and its chemical structure belongs to hydrocarbons and amines.Chlorpheniramine can competitively block the histamine H1 receptor on the target cells of allergic reactions, so that histamine can not bind to the H1 receptor, thus inhibiting the allergic reactions caused by it.
However, chlorpheniramine does not affect the metabolism of histamine, nor does it prevent the release of histamine in the body.
Chlorpheniramine also has central inhibition and anticholinergic effects, so after taking the drug, there is a feeling of drowsiness, dry mouth, constipation, sputum thickening and nasal mucous membrane dryness.After a long time of clinical practice, it is believed that chlorpheniramine has a strong antihistamine effect, small dosage and few side effects.
The antihistamine effect of chlorpheniramine is stronger than that of diphenhydramine and ipratropium, while the central inhibitory effect is weaker, and the anticholinergic effect is also weaker.
Because of the mild adverse effects such as drowsiness, it is suitable for children and patients who need to work during the day.
Chlorpheniramine also has the effect of reducing tracheal secretion and gastric acid secretion. It was the most commonly used antihistamine in the clinic before the introduction of the new generation of antihistamines.
Poduction Method of Bulk Chloropheniramine maleate Powder.
Obtained by two-step condensation of 2-p-chlorobenzylpyridine. In a dry reaction pot, add sodium ammonia,anhydrous toluene, heating to reflux, 2-p-chlorobenzylpyridine and bromoacetaldehyde diethyl acetal drop at the same time. After adding, reflux reaction 8h.Cooling static, take the toluene solution, the solids with a small amount of water to dissolve and then extracted with toluene. The extract was combined with toluene solution, washed to neutral, recycled toluene, obtained 3-p-chlorobenzene-3-(2-pyridyl)-propionaldehyde diethyl acetal. It was mixed with DMF and added to the reaction pot,and a mixture of formic acid and water was added with stirring.
Heating to 110-120 ° C reaction 2h, 150-160 ° C reaction 3h. Cooling, decompression recovery of DMF, diluted with heated water, adjusted with alkali to pH 14.Then extract with toluene, wash the extract with water to neutral, recover the toluene and distill under reduced pressure, collect the 150-190 ℃ fractions to get clodermeton.
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