Chlorphenamine maleate, History, Best Uses, Side effects, and 12 Brands in Pakistan

Introduction

Chlorphenamine maleate, or chlorpheniramine, is an antihistamine medication commonly used to treat symptoms of allergies, hay fever, and the common cold. It belongs to the class of drugs called histamine H1 receptor antagonists, which work by blocking the action of histamine in the body. Histamine is a chemical released by the body’s immune system during an allergic reaction, causing symptoms such as itching, sneezing, runny nose, and watery eyes.

History of Chlorphenamine maleate

The journey of chlorphenamine maleate began with the discovery of antihistamine compounds in the 1920s. Scientists like Daniel Bovet and his team experimented with various chemical structures, synthesizing early antihistamines like diphenhydramine.

Pharmacology

In the 1930s, researchers at Rhône-Poulenc explored the properties of phenolic compounds, uncovering their potential as antihistamines. This knowledge paved the way for the development of chlorphenamine maleate.

Patent and Development

Schering-Plough patented chlorphenamine maleate in 1948, beginning its development as a medication. The company’s scientists refined the compound, testing its efficacy and safety for human use.

Clinical Trials

The 1950s saw the first clinical trials of chlorphenamine maleate, conducted to assess its effectiveness in treating allergies, hay fever, and the common cold. Positive results led to its approval by the FDA in 1951.

Marketing and Branding

Chlorphenamine maleate was first marketed under the brand name Chlor-Trimeton, which became synonymous with allergy relief. The medication’s popularity soared, making it a household name.

Impact and Legacy

Chlorphenamine maleate revolutionized the treatment of allergic symptoms, providing relief for millions worldwide. Its development paved the way for newer antihistamines and inspired further research into the treatment of allergies and related conditions.

Forms of Chlorphenamine Maleate

Chlorphenamine maleate is available in various forms for administration. These forms include:

1. Tablets and Capsules: It is commonly available in tablet or capsule form. These solid oral dosage forms are designed to be swallowed with water.
2. Syrups: It is also available in liquid form as a syrup. Syrups are often preferred for pediatric use or for individuals with difficulty swallowing tablets or capsules. The syrup form allows for easy measurement of the prescribed dose.
3. Injections: Chlorphenamine maleate can be administered via injection. This form is typically used in hospitals or when immediate relief is required.

Mechanism of Action

Chlorphenamine maleate is an antihistamine medication that works by:

1. Blocking histamine receptors: Chlorphenamine maleate binds to histamine H1 receptors in the body, preventing histamine from attaching and causing an allergic response.
2. Reducing histamine effects: By blocking histamine receptors, chlorphenamine maleate reduces the effects of histamine, including:
   • Vasodilation (widening of blood vessels)
   • Increased mucus production
   • Itching and pruritus (itching sensation)
   • Smooth muscle contraction
3. Sedating effects: It also has a sedating effect, which helps to relieve anxiety and insomnia associated with allergies.
4. Anticholinergic effects: Chlorphenamine maleate has anticholinergic properties, which help to dry up excess mucus and reduce secretions.

Chlorphenamine Maleate Uses

Chlorphenamine maleate is an antihistamine medication used to treat the following health conditions:

Allergic Rhinitis: It is commonly used to manage symptoms of allergic rhinitis, including sneezing, itching, nasal congestion, and rhinorrhea (runny nose). It provides relief by blocking the action of histamine, the primary mediator of allergic reactions.

Urticaria (Hives): Chlorphenamine maleate is effective in relieving itching and swelling associated with urticaria, a skin condition characterized by the sudden appearance of red, raised, and itchy welts.

Conjunctivitis: In cases of allergic conjunctivitis, characterized by redness, itching, and watering of the eyes due to allergen exposure, chlorphenamine maleate eye drops can help alleviate symptoms by blocking histamine receptors in the eye.

Pruritus (Itching): Its antipruritic properties make it useful in managing itching associated with various dermatological conditions, insect bites, and allergic reactions.

Motion Sickness: Chlorphenamine maleate is sometimes used to prevent and alleviate symptoms of motion sickness, including nausea, vomiting, and dizziness. Its sedative effects may also help individuals relax during travel.

Insomnia: Due to its sedative properties, chlorphenamine maleate is occasionally prescribed to promote sleep in individuals experiencing insomnia, particularly when insomnia is associated with allergies or itching.

Anaphylaxis: In emergencies such as anaphylaxis, a severe allergic reaction that can lead to life-threatening symptoms, chlorphenamine maleate is administered as part of the treatment regimen to help alleviate allergic symptoms.

Pruritic Dermatoses: It is also used topically in the form of creams or ointments to relieve itching associated with various pruritic dermatoses, including eczema, contact dermatitis, and allergic reactions.

Chlorphenamine Maleate use during pregnancy

• Pregnancy Safety: Chlorphenamine can be used in pregnancy. There is no good evidence that it is harmful to your baby, but it can have side effects such as feeling drowsy.
• Doctor’s Recommendation: Your doctor or pharmacist may recommend a non-drowsy antihistamine (loratadine) before chlorphenamine.
• Breastfeeding: If your doctor or health visitor says your baby is healthy, you can use chlorphenamine during breastfeeding. This is a drowsy antihistamine, so it is better to take occasional doses or only for a short time.
• Baby’s Health: It is not known how much chlorphenamine gets into breast milk, but it has been used for many years without causing babies to have side effects. However, chlorphenamine can cause drowsy symptoms, so may also make your baby sleepy too.

Dosage of Chlorphenamine Maleate

Adults:

• Allergic rhinitis: 4mg every 4-6 hours as needed, not to exceed 24mg in 24 hours
• Urticaria: 4mg every 4-6 hours as needed, not to exceed 24mg in 24 hours
• Insomnia: 8-12mg at bedtime
• Motion sickness: 8-12mg 30 minutes before travel, repeated every 4-6 hours as needed

Children:

• 2-5 years: 1mg every 4-6 hours as needed, not to exceed 6mg in 24 hours
• 6-11 years: 2mg every 4-6 hours as needed, not to exceed 12mg in 24 hours
• 12 years and older: adult dosage

Side effects

Chlorphenamine Maleate, like other antihistamines, can cause a range of side effects, some of which can be serious. It’s essential to be aware of these potential side effects and discuss any concerns with your doctor.

Common Side Effects:

• Drowsiness
• Dizziness
• Dry mouth
• Fatigue
• Headache
• Nausea
• Vomiting
• Constipation
• Blurred vision
• Difficulty urinating

Less Common Side Effects:

• Allergic reactions (rash, itching, swelling)
• Anxiety
• Confusion
• Hallucinations
• Increased heart rate
• Insomnia
• Loss of appetite
• Mood changes
• Muscle weakness
• Seizures (rare)
• Tremors

Serious Side Effects:

• Anaphylaxis (severe allergic reaction)
• Blood disorders (e.g., agranulocytosis, thrombocytopenia)
• Cardiovascular problems (e.g., hypertension, cardiac arrhythmias)
• Liver damage (rare)
• Respiratory depression (rare)
• Seizures (rare)
• Urinary retention (rare)

Precautions and Warnings

While using chlorphenamine maleate, it is important to be aware of certain precautions and warnings:

Warnings:

• Do not use it if you are allergic to chlorphenamine maleate or any other antihistamine.
• Do not use if you have narrow-angle glaucoma, urinary retention, or severe high blood pressure.
• Do not use if you are taking sedatives, tranquilizers, or antidepressants.
• Do not use it if you are pregnant or breastfeeding without consulting your doctor.

Precautions:

• Use with caution if you have kidney or liver disease, asthma, or heart problems.
• Use with caution if you are elderly or have prostate enlargement.
• Avoid driving or operating heavy machinery due to drowsiness.
• Avoid alcohol and other central nervous system depressants.
• Inform your doctor if you have any medical conditions or take any medications.
• Follow the recommended dosage and consult your doctor if necessary.

Chlorphenamine Maleate Drug Interactions

Major Interactions:

• Sedatives and tranquilizers (e.g., barbiturates, benzodiazepines): Increased sedation and respiratory depression.
• Antidepressants (e.g., MAOIs, SSRIs): Increased anticholinergic effects and sedation.
• Anticholinergics (e.g., atropine, scopolamine): Increased anticholinergic effects.
• Cardiovascular medications (e.g., beta-blockers, calcium channel blockers): Increased risk of hypotension and bradycardia.
• Macrolide antibiotics (e.g., erythromycin, clarithromycin): Increased risk of QT prolongation and cardiac arrhythmias.

Moderate Interactions:

• Opioid analgesics (e.g., morphine, hydrocodone): Increased sedation and respiratory depression.
• Muscle relaxants (e.g., carisoprodol, cyclobenzaprine): Increased sedation and muscle weakness.
• Anticonvulsants (e.g., carbamazepine, phenytoin): Increased risk of sedation and cognitive impairment.
• Bronchodilators (e.g., albuterol, ipratropium): Increased risk of anticholinergic effects.

Minor Interactions:

• Antacids: Reduced absorption of chlorphenamine maleate.
• Histamine H2 blockers (e.g., ranitidine, famotidine): Increased risk of sedation and anticholinergic effects.

Food Interactions:

• Alcohol: Increased sedation and respiratory depression.
• Grapefruit juice: Increased risk of QT prolongation and cardiac arrhythmias.

Brands in Pakistan

In Pakistan, chlorphenamine maleate is available under various brand names. Some of the common brands include:

1. ABENOL PLUS: (Popular Chemical Works (Pvt) Ltd)
2. PIRITON SYRUP 120ml: Manufactured by (GlaxoSmithKline) GSK
3. ALLERGIN: (Sami Pharmaceuticals Pvt Ltd)
4. BRONCODYL:(Zinta Pharmaceuticals Industries)
5. BRONCODYL-D:(Medicaids Pakistan (Pvt) Ltd)
6. CETRINE: Getz Pharma Pvt Ltd.
7. CHLOR-TRIMETON:(GlaxoSmithKline Pakistan Limited) GSK
8. COCIL: (Ethical Laboratories (Pvt) Ltd)
9. COFCINA-D: (Mediceena Pharma (Pvt) Ltd)
10. HISTAFEN: (Hilton Pharma (Pvt) Ltd)
11. PIRITON Tablet: Manufactured by (Glaxosmithkline)
12. POLAR-D: (KCI Pharma (Pvt) Ltd)
13. PULMONAL SYRUP 120ml :(Manufactured by C.C.L (Pvt) Ltd.)

Other Countries

Here are some brands of Chlorphenamine Maleate available in other countries:

1. Aller-Chlor: available in the U.S.
2. Aller-Chlor Syrup: available in the U.S.
3. Chlo-Amine: available in the U.S.
4. Chlor-Trimeton 12-Hour Allergy: available in the U.S.
5. Polaramine: available in the U.S.
6. Actifed Cold and Allergy: available in the U.S.
7. Actifed Cold and Sinus: available in the U.S.
8. Alka-Seltzer Plus Cold Medicine Liqui-Gels: available in the U.S.
9. Allerest Maximum Strength: available in the U.S.
10. Atrohist Pediatric: available in the U.S.
11. Brexin L.A.: available in the U.S.
12. Chlor-Phed Timecelles: available in the U.S.