Chlorpheniramine Maleate Tablet Uses, Side Effects and Mechanism of Action

What is Chlorpheniramine Maleate Tablet

Chlorpheniramine Maleate tablet is a first-generation antihistamine commonly used to relieve the symptoms associated with allergic conditions, such as allergic rhinitis (hay fever) and cold and flu symptoms.

It is a member of the alkylamine class of antihistamines and acts by blocking the effects of histamine, a naturally obtained substance in the body involved in allergic reactions.

Chlorpheniramine is available in various dosage forms, including tablets, capsules, syrups, and as an ingredient in combination products.

Historical Context and Discovery Of Chlorpheniramine Maleate Tablet

Chlorpheniramine was first synthesized in the 1940s by chemists at the University of Cincinnati as part of their research on antihistamines.

It was initially developed as a cough suppressant, but its antihistaminic properties were later discovered by researchers at the Merrell-National Laboratories. Chlorpheniramine was first marketed under “Chlor-Trimeton” by Merrell in the 1950s.

It was one of the first antihistamines widely used to relieve allergy symptoms.

Chlorpheniramine Maleate Tablet Uses

Chlorpheniramine has been an actual allergy and respiratory medicine medication for many years.

It is widely used for the symptomatic relief of various allergic conditions, such as allergic rhinitis, urticaria (hives), and itching. It also alleviates cold and flu symptoms, such as sneezing, runny nose, and congestion.

Chlorpheniramine effectively reduces the severity of these symptoms and improves the quality of life for patients suffering from allergic conditions. It is commonly used as a first-line treatment option and is over-the-counter in many countries, making it easily accessible to patients.

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Chemical Properties and Synthesis of Chlorpheniramine Maleate Tablet

A. Chemical Structure and Molecular Formula

Chlorpheniramine belongs to the alkylamine class of antihistamines and has the chemical name 2-[p-chloro-α-(2-dimethylamino ethyl)benzyl]pyridine. Its molecular formula is C16H19ClN2, and its molecular weight is 274.8 g/mol. Chlorpheniramine is a white or almost white crystalline powder freely soluble in water and alcohol.

B. Physical Properties

Chlorpheniramine has a melting point of 132-135°C and a boiling point of 358-359°C. It has a pKa value of 9.4, indicating a weak base. Chlorpheniramine is stable under normal conditions of storage and use, but it may undergo degradation when exposed to light, air, or moisture. Storing Chlorpheniramine in a cool, dry place and protecting it from sunlight is essential to maintain its stability.

C. Synthesis and Manufacturing Process

Chlorpheniramine can be synthesized through several methods, including reducing the corresponding nitro compound or by N-alkylation of 2-[(4-chlorophenyl)methyl]pyridine with N, N-dimethylethanolamine. The synthesis of Chlorpheniramine involves multiple steps and requires careful control of reaction conditions and purification processes to obtain a pure and stable product. Commercially, pharmaceutical companies manufacture Chlorpheniramine using Good Manufacturing Practices (GMP) to ensure the final product’s quality, safety, and efficacy.

Pharmacology and Mechanism of Action Chlorpheniramine Maleate Tablet

A. Pharmacokinetics

Chlorpheniramine is well absorbed after oral administration, with peak plasma concentrations reached within 1-3 hrs. It is extensively metabolized in to the liver and excreted primarily in the urine as metabolites. The half-life of Chlorpheniramine is approximately 20 hours, meaning it has a relatively long duration of action and may only need to be taken once or twice a day, depending on the dosage and formulation.

B. Mechanism of Action

Chlorpheniramine acts by blocking the effects of histamine, a naturally occurring substance in the body that is released during an allergic reaction. Histamine is responsible for causing various symptoms associated with allergic conditions, such as itching, sneezing, runny nose, and congestion. Chlorpheniramine works by competitively binding to the histamine H1 receptors, thereby preventing histamine from binding to these receptors and exerting its effects. This results in a reduction of allergic symptoms and relief of discomfort.

C. Pharmacodynamic Properties

Chlorpheniramine has antihistaminic, anticholinergic, and sedative properties. Its antihistaminic properties are responsible for its ability to relieve allergic symptoms. The anticholinergic properties of Chlorpheniramine contribute to its drying effects, such as reducing nasal secretions and relieving symptoms of a runny nose. The soothing properties of Chlorpheniramine can cause drowsiness. They may be beneficial in alleviating symptoms such as sneezing and coughing at night, but they can also cause sleepiness during the day, which can be a side effect of the medication.

Clinical Uses and Dosage Of Chlorpheniramine Maleate Tablet

A. Clinical Indications

Chlorpheniramine is indicated to relieve symptoms associated with allergic conditions, such as (hay fever) allergic rhinitis , urticaria (hives), and itching. It also alleviates cold and flu symptoms, including sneezing, runny nose, and congestion. Chlorpheniramine is commonly used as a first-line treatment option for mild to moderate allergic conditions and is often over-the-counter in many countries. Depending on the patient’s needs, it may also be prescribed by a healthcare provider for more severe symptoms or in combination with other medications.

B. Dosage and Administration

The dosage of Chlorpheniramine varies depending on the patient’s age, weight, and severity of symptoms. It is available in different dosage forms, including tablets, capsules, and syrups, with varying strengths. The recommended dose for adults is usually 4 mg to 8 mg every 4 to 6 hours, not exceeding a total daily dose of 32 mg. For children, the dosage is usually based on their weight and age, and it is important to follow the dosing information provided by the healthcare provider or the package insert.

C. Special Populations

Chlorpheniramine should be used with caution in specific populations, including elderly individuals, pregnant and breastfeeding women, and patients with certain medical conditions such as liver or kidney impairment, glaucoma, asthma, or urinary retention. The dosages may need to be adjusted in these populations, or alternative medications may be considered, and it is essential to consult with a healthcare provider for appropriate dosing and monitoring.

Medical Uses and Indications

Chlorpheniramine is an antihistamine medication that is commonly used for various medical purposes due to its ability to alleviate allergy and respiratory symptoms.

This article explores the medical uses and indications of chlorpheniramine, highlighting its effectiveness in treating allergies, cold and flu symptoms, as well as other conditions such as itching, urticaria, and motion sickness.

A. Allergy and Respiratory Conditions: Chlorpheniramine is highly effective in managing allergy-related symptoms, particularly allergic rhinitis and hay fever.

It works by blocking histamine receptors, which helps reduce nasal congestion, sneezing, itching, and runny nose associated with allergies.

The medication can provide relief from symptoms caused by environmental allergens, such as pollen, dust mites, and pet dander.

B. Cold and Flu Symptoms Relief: Chlorpheniramine is often included in over-the-counter cold and flu medications due to its ability to alleviate symptoms such as sneezing, watery eyes, and nasal congestion.

By targeting the histamine response in the body, chlorpheniramine can provide temporary relief from the discomfort caused by respiratory infections.

C. Other Medical Uses: Apart from its primary applications in allergy and respiratory conditions, chlorpheniramine has demonstrated efficacy in addressing other medical issues.

It is commonly prescribed to relieve itching associated with various skin conditions like urticaria (hives), insect bites, and contact dermatitis.

Additionally, chlorpheniramine can be used as a preventive measure against motion sickness, as it helps reduce nausea and dizziness caused by motion-related activities such as travelling or sailing.

Safety and Side Effects Chlorpheniramine Maleate Tablet

A. Safety Profile

Chlorpheniramine is generally considered to be safe and well-tolerated when used as directed. However, like any medication, it can cause side effects in some individuals.

Chlorpheniramine’s most common side effects include drowsiness, dry mouth, blurred vision, constipation, and urinary retention. These side effects are usually mild and temporary but can be more severe in elderly individuals or patients with certain medical conditions.

B. Drug Interactions

Chlorpheniramine may interact with other medications, and it is vital to inform your healthcare provider or pharmacist if you are taking any other medicines, including over-the-counter medications, herbal supplements, or vitamins.

Some follow drugs that may interact with Chlorpheniramine include sedatives, tranquillizers, opioids, anticholinergic medications, and monoamine oxidase inhibitors (MAOIs).

These interactions can increase the risk of side effects, such as excessive drowsiness or respiratory depression, and may require dosage adjustments or avoidance of certain medications.

C. Special Precautions

There are some special precautions to keep in mind when using Chlorpheniramine.

It should be used with caution in elderly individuals, as they may be more susceptible to the medication’s sedative effects. Pregnant and breastfeeding women should consult their doctors before using Chlorpheniramine, as its safety during pregnancy and lactation is not well-established.

Patients with certain medical conditions, such as liver or kidney impairment, glaucoma, asthma, or urinary retention, should also use Chlorpheniramine with caution, and dosages may need to be adjusted or alternative medications considered.

D. Overdose and Emergency Situations

In case of an overdose of Chlorpheniramine, it is important to seek immediate medical attention. Symptoms of an overdose may include severe sleepiness, confusion, difficulty breathing, blurred vision, increased heart rate, and loss of consciousness. Call your local emergency services or poison control centre for assistance in emergencies.

Conclusion Of Chlorpheniramine Maleate Tablet Uses

Chlorpheniramine is a commonly used antihistamine medication that effectively relieves symptoms associated with allergic conditions, such as hay fever, hives, and itching.

It works by blocking the effects of histamine, a naturally occurring substance in the body that is released during an allergic reaction. Chlorpheniramine is generally safe and well-tolerated when used as directed, but it can cause side effects, especially drowsiness, dry mouth, and blurred vision.

It is essential to follow the dosing instructions provided by your healthcare provider or the package insert and to inform your healthcare provider or pharmacist of any other medications you are taking chlorpheniramine to avoid potential drug interactions.

If you have any questions or concerns about chlorpheniramine use, consult your healthcare provider for appropriate guidance.

FAQs Of Chlorpheniramine Maleate Tablet Uses