Sunday , 7 August 2022

Overview of Chlorpheniramine maleate – An effective Antihistamine

Y.N. Sujitha*, P.M.Sowndarya, M.V.SaiLalithkumar, Y.Sarath, K.Siva
Narayana Pharmacy College, Chinthareddypalem, Nellore, Andhra Pradesh, India.
E-mail: [email protected]

Chlorpheniramine maleate is an antihistamine. It blocks the effects of a chemical which causes symptoms of allergy such as itching. It can be used to treat many types of allergies such as hay fever, food or medicine allergies, rhinitis, urticaria or insect bites. Chlorpheniramine maleate is also used to treat itching that is caused by chicken pox. This medication works by blocking a certain natural substance (histamine) that your body makes during an allergic reaction. By blocking another natural substance made by your body (acetylcholine), it helps dry up some body fluids to relieve symptoms such as watery eyes and runny nose.Chlorpheniramine maleate causes drowsiness in animals just as it does in people and can be used as a mild tranquilizer. Some argue that it is the drowsiness side effect that makes this medication appear to be helpful in itch management (i.e., patients scratch less because they are sleeping more.)
Key words: Antihistamine, Hay fever, Rhinitis,Acetylcholine, Tranquilizers
Chlorpheniramine (Maleate) is the maleate salt of chlorpheniramine. Chlorpheniramine is an antihistaminic agent derived from pheniramine. Chemically it is gamma-(4-chlorophenyl)-N, N-dimethyl-2-pyridinepropanamin. Chlorphenamine maleate which isa potent histamine. Histamine is an inflammatory biochemical that causes skin redness, swelling, pain, increased heart rate, and blood pressure drop when it binds to one of many H1 receptors throughout the body. Histamine is a very important mediator of allergy in humans; hence a spectacular array of different antihistamines has proliferated. Chlorpheniramine maleate is typically administered 2 to 3 times daily. The drug is readily and rapidly absorbed from the G.I. tract and is usually effective within an hour.The half-life may be as long as 24 hours. The drug is largely inactivated in the liver and excreted as metabolites in the urine. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. That doesn’t mean it works for everybody. People over 60 are especially likely to suffer from side effects. It’s a good idea not to mix Chlorpheniramine with alcohol or any other drug that produces a drowsy effect. This includes sedatives such as Valium,andopiates. This hasn’t stopped the pharmaceutical industry from marketing a blend of Chlorpheniramine) and Hydrocodone (codeine for particularly severe colds.
Mechanism of action:
Chlorpheniramine is an anticholinergic  antihistamine. It also is effective against nausea and motion sickness, with its primary mechanism of action being its ability to reduce acetylcholine levels in the brain. Acetylcholine is a neurotransmitter. In the brain, acetylcholine and dopamine have antagonistic effects on each other, so a proper balance is necessary for a healthy, functioning body and mind. Many antihistamines (Benadryl) work the same way; by reducing (or inhibiting the effects of) the level of acetylcholine in the brain, histamine levels decrease throughout the body, alleviating the symptoms of an allergic reaction. The decrease in acetylcholine gives the dopamine more influence within the brain, which is why anticholinergic drugs are often used to alleviate the symptoms of Parkinson’s disease. Anticholinergic also tend to promote urine retention via temporary swelling of the Prostate, making them useful as anti-incontinence drugs.
Adverse effects:
The symptomatic adverse reactions produced by Chlorpheniramine maleate are more or less tolerable and if they become severe, they can be treated symptomatically, these include Drowsiness, Nausea, Vomiting, Restlessness, Palpitation, Constipation, Abdominal pain, Dry mouth, Blurred vision, Sedation, Facial dyskinesia’s, Blood dyscrasias, Xerostomia.
In the treatment of allergic skin disease, antihistamines are felt to synergize with omega 3 fatty acid supplements and, as a general rule for this condition, it is best to use these medications together. Chlorpheniramine maleate should not be used with additional tranquilizing medications. This antihistamine is used in an assortment of human products where it is combined with pain relievers and antihistamines. Chlorpheniramine maleate is available in 2 mg, 4 mg, 8 mg & 12 mg tablets as well as oral syrup and injectable.
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2. Hellbom, E. (2006). “Chlorpheniramine, selective serotonin-reuptake inhibitors (SSRIs) and over-the-counter (OTC) treatment”. Medical Hypotheses 66 (4): 689–690.
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