North South University

“Chlorpheniramine”
PHR215 : Medicinal Pharmacy 1
Section - 01

Submitted by – Submitted to –
MD. Sakib Talukder Dr. Murad Hossain
(2011945649) (Associate Professor)
North South University

11th June,Introduction
2023 –
Antihistamines like chlorpheniramine are frequently used to treat allergic responses and their
accompanying symptoms. It functions by obstructing the effects of histamine, a chemical the
body produces in response to an allergic reaction. Sneezing, itching, watery eyes and a runny
nose are reduced as a result. Although chlorpheniramine comes in a variety of quantities and
forms, it's crucial to be aware of any possible adverse effects, including sleepiness and dry
mouth. It is advised to adhere to the recommendations made by medical specialists and seek their
individualized advice on its usage.

Classification –
H1 antihistamines have historically been divided into six chemical groups -
1. Alkylamines
(Bromopheniramine, Chlorpheniramine, Dexchlorpheniramine, Pheniramine,
Dimethindene, Triprolidine, Acrivastine)
2. Ethanolamines
(Carbinoxamine, Clemastine, Dimenhydrinate, Diphenhydramine, Doxylamine,
Phenyltoxamine)
3. Ethylenediamines
(Antazoline, Pyrilamine, Trpelenamine)
4. Phenothiazines
(Promethazine, Mequitazine, Trimepazine)
5. Piperazines
(Buclizine, Cyclizine, Meclizine, Oxatomide, Hydroxyzine, Cetrizine, Levocetrizine)
6. Piperidines
(Azatadine, Cyproheptadine, Ketotifen, Loratadine, Desloratadine,Bilastine, Ebastine,
Terfenadine, Fexofenadine, Levocabastine, Mizolastine, Rupatadine)

Mechanism of Action –
Chlorpheniramine works by competitively blocking the body's H1 histamine receptors, which is
the exact mechanism of action. The body releases the chemical histamine during an allergic
reaction, which is what causes symptoms like runny nose, itching, and sneezing.
As a first-generation antihistamine, chlorpheniramine binds to the H1 histamine receptors found
in a variety of tissues, including the blood vessels, respiratory system, and nasal passages.
Chlorpheniramine efficiently prevents the binding of histamine molecules to the receptors by
attaching to these receptors, deactivating the allergic reaction.
The production of inflammatory chemicals, vasodilation, increased vascular permeability, and
the recognizable allergy symptoms are all prevented by blocking the H1 receptors. This lessens
allergy-related symptoms such nasal congestion, sneezing, itching, and watery eyes.
It's crucial to remember that the mechanism of action of chlorpheniramine is not just restricted to
H1 receptors. It also has some anticholinergic capabilities, which means it has the ability to
inhibit the action of the neurotransmitter acetylcholine. Additionally, this leads to the drying of
secretions, which has the potential to cause side effects including dry mouth, impaired vision,
and constipation.
It's important to note that while chlorpheniramine is efficient in treating allergy symptoms, due
to its capacity to pass the blood-brain barrier and affect the central nervous system, it may make
you feel sleepy. This calming effect is frequently utilized as a benefit in specific circumstances,
such as to treat evening allergies or as a light sleep aid.
For more information on the mechanism of action, dosage, and any possible drug interactions or
side effects related to chlorpheniramine, it is crucial to speak with a healthcare provider or read
the medication's instructions.

Indications –
Chlorpheniramine is used for a number of ailments including allergy-related symptoms. Its
general indicators consist of :

1) Allergic rhinitis –
 Sneezing, itching, runny nose, and other allergic rhinitis symptoms can all be helped by
chlorpheniramine.
2) Allergic conjunctivitis –
Redness, irritation, and watery eyes are among the symptoms of allergic conjunctivitis
that it is used to treat.
3) Urticaria (hives) –
Chlorpheniramine can be used to treat allergic reactions' hives and itching.
4) Pruritus (itching) –
It can ease widespread itchiness brought on by allergies or other illnesses.
5) Common cold symptoms –
Chlorpheniramine can be used to treat cold-related symptoms such runny nose, sneezing,
and nasal congestion.
6) Dermatographism –
Chlorpheniramine can treat his illness, which is characterized by the development of
wheals or welts in reaction to physical pressure or scratching.

Dosage and Administration –

Depending on the formulation, the patient's age, health, and reaction to therapy, the dosage and
administration of chlorpheniramine may change. It is crucial that you adhere to the guidelines set
out by your healthcare provider or the details listed on the product label. The following are basic
recommendations for administering and dosing chlorpheniramine :
Oral tablets or capsules :
 Adults and children 12 years and older : Typically, the recommended dose is 4 mg to 8
mg every 4 to 6 hours, not exceeding 32 mg in a 24-hour period.
 Children 6 to 12 years old : The usual dose is 2 mg to 4 mg every 4 to 6 hours, not
exceeding 24 mg in a 24-hour period.
 Children 2 to 6 years old : The recommended dose is 1 mg to 2 mg every 4 to 6 hours, not
exceeding 12 mg in a 24-hour period.
 Children under 2 years old : The use of chlorpheniramine in this age group should be
done under the guidance of a healthcare professional.
Oral liquid :
Depending on the chlorpheniramine content, different dosages of oral liquid formulations may be
required. It is crucial to accurately measure the dosage with a syringe or other calibrated
measurement tool.
For the correct dosage depending on age and weight, we must adhere to the detailed instructions
given by the healthcare provider or the product label.
Extended-release formulations :
Extended-release formulations may have distinct dose guidelines and are intended to offer relief
for a longer period of time.
We must abide by the precise directions given by the medical expert or the product label on the
right dosage and dosing schedule.

Side Effects –
Like any drug, chlorpheniramine has potential negative effects. Some of the typical negative
effects of using chlorpheniramine include the following :
1) Drowsiness :
Sedation or sleepiness is one of the most prominent adverse effects of chlorpheniramine.
It may make you feel sleepy or exhausted, which may make it difficult for you to carry
out activities that call for attention, including operating machinery or a vehicle.
2) Dry mouth and throat :
The effects of chlorpheniramine might include dry mouth and throat. It may also make
you more thirsty and impact your ability to swallow and speak clearly.
3) Blurred vision :
While using chlorpheniramine, some people may suffer impaired vision or trouble
focusing. When performing tasks that call for sharp eyesight, it's crucial to exercise
caution.
4) Urinary retention :
Urinary retention brought on by chlorpheniramine might make it challenging to
completely empty the bladder. This may lead to more frequent urination or trouble
peeing.
5) Constipation :
Chlorpheniramine may occasionally result in constipation, which makes it difficult to
pass feces.
6) Gastrointestinal disturbances :
Vomiting, nausea, and an upset stomach are among additional gastrointestinal side effects
that may occur.

7) Dizziness :
Dizziness or lightheadedness brought on by chlorpheniramine may impair balance and
coordination.
 8) Allergic reactions :
Chlorpheniramine allergies are possible but uncommon. Rash, itching, swelling, very
lightheadedness, or breathing difficulties are all indications of an allergic response. If we
encounter any of these symptoms, might get help right once.

Conclusion –
Chlorpheniramine is a first-generation antihistamine used to treat allergies and related symptoms.
It works by blocking histamine effects in the body. It is effective in treating allergic rhinitis, hay
fever, itching, and common cold symptoms. However, it can cause side effects such as
drowsiness and dry mouth. Proper dosage and following healthcare professional's instructions
are important. Special precautions may be necessary for specific populations. Overall,
Chlorpheniramine is a valuable tool for managing allergy symptoms.

References –
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B., ... & Sturm, G. J. (2018). The EAACI/GA2LEN/EDF/WAO guideline for the
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1414.
2) Schroeck, J. L., Ford, J., Conway, E. L., Kurtzhalts, K. E., Gee, M. E., Vollmer, K. A., ...
& Mergenhagen, K. A. (2016). Review of safety and efficacy of sleep medicines in older
adults. Clinical therapeutics, 38(11), 2340-2372.
3) Pichichero, M. E., & McLinn, S. E. (2003). An update on the use of antihistamines in
allergic disorders. Expert opinion on pharmacotherapy, 4(12), 2131-2140.
4) European Medicines Agency. (2009). Chlorphenamine (chlorpheniramine maleate):
summary of product characteristics.
5) UpToDate. (2022). Chlorpheniramine (Systemic): Drug information.