Active Ingredients

Chlorphenamine – Effect, Application & Risks


Chlorphenamine is an antihistamine used to treat allergic conditions . It inhibits the effect of the messenger substance histamine and thus counteracts allergic symptoms such as itching , reddening and skin reactions . Chlorphenamine also has antidepressant and sedative effects. It is on the market under various trade names as a monopreparation and also as a substance in combination preparations. Possible side effects include tiredness , nervousness , dry mouth and sleep disorders .

What is chlorphenamine?

Chlorphenamine belongs to the chemical group of alkylamines. It is a first-generation antihistamine. The drug is used in human and veterinary medicine to treat allergic reactions.

The drug is available under the trade names Trimeton® and Balkis Dr. Henk® snuff capsules known. It is also contained in various combination preparations such as Solmucalm®, Rhinopront®, Pecto-Baby®, Migräne-Kranit® and Benical®. Chlorphenamine is present in medical products as so-called chlorphenamine maleate. Chlorphenamine maleate is a white, crystalline powder and soluble in water.

Pharmacological action

Chlorphenamine is a histamine receptor antagonist. These active ingredients reduce the effect of the body’s own messenger histamine or even completely neutralize it. Histamine is a biogenic amine and an important mediator in the human body. It plays a role in gastric acid production and in the central nervous system . It is also responsible for allergic reactions.

Upon contact with an allergen, histamine is released in granulocytes and mast cells and binds to the receptor . This can lead to redness, edema and itching.

Chlorphenamine acts on the so-called H1 receptor. The H1 receptors are located on endothelial cells. After activation, nitric oxide is released due to increased calcium levels. This results in a relaxation of the vascular muscles. This circumstance leads to the so-called vasodilatation . The blood vessels dilate.

Due to the release of histamine, this process can lead to symptoms of an allergy such as itching, reddening of the skin or anaphylactic shock . The latter is life-threatening.

In addition to its effect on the messenger substance histamine, chlorphenamine has other properties. It has an antidepressant effect because it reduces the reuptake of norepinephrine and serotonin at nerve endings. So far, however, there have been no human studies on this possible area of ​​application. In addition, chlorphenamine has a tiring (sedating) effect.

Medical Application & Use

Due to its inhibitory effect on the histamine receptor, chlorphenamine is used to treat allergic diseases. Indication areas are therefore diseases of the respiratory tract such as hay fever , colds , allergic rhinitis, chronic runny nose and sinusitis . It can also be used to treat colds and flu-like effects. The drug can also be used for symptomatic therapy in allergic reactions such as nettle fever or conjunctivitis .

Since the drug has an antidepressant effect, it could be used to treat depressive moods . However, this mode of action has not yet been demonstrated in humans.

Due to the relaxing and calming effect of the medicinal product, chlorphenamine is often misused as a sedative . This is particularly dangerous in combination with other dampening substances such as alcohol . Adverse effects of the drug can be intensified by taking it at the same time. In addition to alcohol, an interaction between chlorphenamine maleate and neuroleptics , benzodiazepines or antidepressants is possible.

Chlorphenamine must not be used medicinally if the patient suffers from hypersensitivity, bladder emptying disorders or a severely enlarged prostate . Furthermore, the substance should not be used to treat acute asthma attacks . In addition, the drug must not be taken during pregnancy and breastfeeding . Furthermore, young children should not be treated with chlorphenamine.

Risks & side effects

Chlorphenamine has different side effects. Undesirable effects include dry mouth, throat and nose , insomnia, tiredness, nervousness , drowsiness and poor eyesight . In addition, the drug can cause a glaucoma , a so-called glaucoma.

Because chlorphenamine has a tiring effect, avoid operating machinery and driving while taking it.

An overdose of the active substance can lead to a so-called anticholinergic syndrome . This is characterized by fever , cramps , dry mouth, reddening of the skin and hallucinations .

Muscle tension , low blood pressure , circulatory collapse and respiratory paralysis are other symptoms that can occur with an overdose of the drug. A fatal outcome cannot be ruled out if used incorrectly.

An American cohort study from 2015 also showed a positive correlation between long-term intake of chlorphenamine maleate and an increased risk of dementia such as Alzheimer’s .

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.