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Chlorpheniramine Maleate CAS 113-92-8

113-92-8
Chlorpheniramine Maleate
Chlorpheniramine Maleate
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  • Appearance: White powder
  • Purity: 99. 0%min
  • Stock: In stock
  • Sample: Available
  • Zhishang Chemical: Chlorpheniramine Maleate Supplier & Manufacturer
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Chlorpheniramine Maleate: The Complete Guide

Chlorpheniramine Maleate for Sale

Basic Info of Chlorpheniramine Maleate

What is Chlorpheniramine Maleate?

Chlorpheniramine molecular formula C20H23ClN2O4, molecular weight 390.86. The taxonomic name is chlorpheniramine maleate. White crystalline powder. No odor and also bitter taste. Melting point 130 ~ 135 ℃. Soluble in water, ethanol and chloroform, the aqueous service is acidic. Perishable when revealed to light. It can be acquired by the condensation of pyridine, p-chlorotoluene and also dimethylamide, and so on and then treated with maleic acid.

Chlorpheniramine is one of the greatest antihistamines with resilient effect, reduced dose and couple of side effects. It can generally competitively block histamine H1 receptors on allergic reaction target cells, to make sure that histamine can not bind to H1 receptors, thus preventing the allergic reactions brought on by it. It is suitable for different allergic diseases, medication allergies, and so on. Dental absorption is fast and total, as well as the occurrence of unfavorable reactions is reduced. The sedative result is weaker than that of promethazine, as well as it additionally has a particular anticholinergic effect. It is similar to diphenhydramine, but with much less central restraint. It can cause epilepsy and also is contraindicated in people with epilepsy. It should be utilized with caution in lactating females, glaucoma, hypertension, hyperthyroidism, and also clients with benign prostatic hypertrophy. During the period of taking the medication, it is not enabled to drive car such as vehicles, watercrafts, and also planes or operate makers.

Chlorpheniramine has numerous side effects on the main nervous system as well as heart as well as has a brief duration of activity, so clinicians in significant medical facilities at home and also abroad seldom use chlorpheniramine. However, because of its low cost, chlorpheniramine is still among the anti-allergic medications typically made use of in rural areas or main clinical institutions in China. The main damaging reactions of chlorpheniramine are much more obvious drowsiness, palpitations, and so on, especially the side effects on the heart and also kidney have triggered individuals’s caution, and also youngsters and also senior people should use chlorpheniramine with care.

Chlorpheniramine Maleate Uses

Antihistamines. Comparable to clotrimide, brompheniramide is additionally an antihistamine.

Chlorpheniramine maleate made use of for colds and sensitive illness of skin as well as mucous membrane layers. Its functions are generally used for urticaria, eczema, dermatitis, medication eruption, skin pruritus, neurodermatitis, insect bites, solar dermatitis, as well as likewise for allergic dermatitis and vasomotor rhinitis., medication as well as food allergies. Along with the solid competitive barring of histamine H1 receptors on allergy target cells, it has an anti-allergic impact by antagonizing H1 receptors, and additionally has an anti-M choline receptor impact. Signs and symptoms such as dry mouth, constipation, thickened spit, and also completely dry nasal mucosa take place.

(±) – Chlorphenamine maleate has been used in:

  • Determine receptor function as H1 receptor antagonist
  • Effect of blocking compound 48 / 80 on plasma IGF-I
  • As a standard for rapid sensing and measurement by sequential injectors coupled to potentiometers

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The Mechanism of Action of Chlorpheniramine Maleate

Antihistamines are a class of drugs that can counteract various pathological reactions caused by histamine. This class of drugs reversibly occupies histamine receptors and competitively blocks the binding of histamine to the receptors, thereby exhibiting antihistamine effects.

There are two types of histamine receptors, H1 and H2, which have different effects when activated. When the H1 receptor is excited, it can cause bronchial and gastrointestinal smooth muscle contraction, vascular smooth muscle relaxation, enhanced atrial muscle contraction, and slow atrioventricular conduction. H2 receptor stimulation can cause gastric parietal cells to secrete gastric acid and so on. These two types of effects are each antagonized by different drugs. H1 receptor antagonists replace histamine in the body and competitively antagonize its action. It cannot inactivate histamine, nor does it inhibit its synthesis and release. Therefore, it is mainly used to relieve the symptoms of allergic reactions, such as urticaria, angioedema, rhinitis, conjunctivitis, and itching caused by skin diseases; some traditional H1 receptor antagonists can antagonize acetylcholine, 5-HT, adrenal glands H1 receptor antagonists such as diphenhydramine, diphenhydramine, and promethazine have antiemetic properties and can be used to treat nausea, vomiting and diarrhea in Meniere’s disease and related diseases symptom.

Some drugs also have anti-vertigo and sedative effects. Promethazine can be used for preoperative anesthesia and short-term treatment of insomnia due to its sedative effect. H1 receptor antagonists can enhance the effects of ethanol, barbiturates, hypnotics, analgesics, anxiolytics, tranquilizers and other central depressants. Monoamine oxidase inhibitors may enhance their anticholinergic effects. The drug can also synergize with atropine and tricyclic antidepressants. It can mask the ototoxicity of aminoglycosides, so that the skin test is false positive and the drug is stopped early. Before using antihistamines, their incompatibilities should be fully understood. Combined with sedatives, hypnotics, tranquilizers or alcoholic beverages, it can strengthen the central inhibitory effect. Delay the intrahepatic metabolism of phenytoin sodium and increase its blood concentration.

Difference Between Chlorpheniramine and Ketotifen

  1. Pharmacological effects are different
    Chlorpheniramine and ketotifen both have H1 receptor antagonistic effects and have good curative effects on urticaria, hay fever and allergic rhinitis. Because they can pass through the blood-brain barrier, they can cause side effects such as drowsiness; both have anticholinergic effects It can relieve rhinorrhea caused by colds, but it can cause dry mouth and urinary retention.
  2. Ketotifen can be used for the prevention of asthma
    In addition to its antihistamine effect, ketotifen also has the activity of stabilizing mast cells similar to sodium cromoglycate. It can be used for the prevention of asthma, but it takes several weeks to achieve the best effect, so it cannot be used for the treatment of acute asthma. attack. It should be reminded that domestic and foreign guidelines do not recommend ketotifen for the routine treatment of asthma.
    Chlorpheniramine is ineffective in the treatment of asthma and is generally not recommended for asthmatics.
    Special reminder: Ketotifen has both anti-serotonin effects, and a small number of patients taking ketotifen can cause weight gain.
  3. Chlorpheniramine can be used for pregnant women
    In the U.S. Food and Drug Administration (FDA) pregnancy safety classification, chlorpheniramine, cyproheptadine, diphenhydramine, loratadine, and cetirizine belong to category B, which can be used in pregnant women.
    Ketotifen belongs to category C, and some animal experiments have shown that ketotifen has adverse effects on the fetus, so pregnant women should avoid using ketotifen.
  4. Avoid using ketotifen in combination with oral hypoglycemic drugs
    Clinical studies have found that when ketotifen is used in combination with oral hypoglycemic drugs, it can cause reversible thrombocytopenia. Therefore, the drug instructions clearly stipulate that ketotifen should not be used in combination with oral hypoglycemic drugs.
    Domestic animal experiments have found that ketotifen can accelerate the metabolic rate of theophylline and reduce the blood concentration of theophylline. When ketotifen is used in combination with aminophylline, the dosage of theophylline should be adjusted according to the clinical manifestations of the patient and the blood concentration of theophylline.
    Special reminder: Both chlorpheniramine and ketotifen have respiratory depressant effects, and neither can be used in combination with other central nervous system depressants or alcohol.
  5. Ketotifen comes in a variety of dosage forms
    In addition to oral tablets, ketotifen is available as nasal spray, nasal drops, and eye drops.
    Chlorpheniramine is only available by injection and as an oral tablet.
    Special reminder: Although chlorpheniramine is very effective for allergic skin diseases, chlorpheniramine should not be used topically because of the risk of causing allergic dermatitis.

Reference

  1. Chlorpheniramine maleate – PubChem
  2. Good doctor online: the role and precautions of chlorpheniramine

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