Description

Simple

A medication used to treat allergy symptoms such as cough.

Clinical

A histamine-H1 receptor antagonist indicated for the management of symptoms associated with upper respiratory allergies.

Overview

A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine.

Pharmacology

Indication

For the treatment of rhinitis, urticaria, allergy, common cold, asthma and hay fever.

Pharmacodynamic

In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical m... Read more

Mechanism of action

Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.

Absorption

Well absorbed in the gastrointestinal tract.

Protein binding

72%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

21-27 hours

Route of elimination

Information currently not available.

Toxicity

Oral LD50 (rat): 306 mg/kg; Oral LD50 (mice): 130 mg/kg; Oral LD50 (guinea pig): 198 mg/kg [Registry of Toxic Effects of Chemical Substances. Ed. D. Sweet, US Dept. of Health & Human Services: Cincinatti, 2010.]
Also a mild reproductive toxin to women of childbearing age.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Avoid alcohol.
  • Take with food.

Interactions

Type in a drug name to check for interaction with Chlorpheniramine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of adverse effects can be increased when Chlorpheniramine is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of adverse effects can be increased when Chlorpheniramine is combined with (S)-Warfarin.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Chlorpheniramine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Chlorpheniramine.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Chlorpheniramine.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Chlorpheniramine.
4-hydroxycoumarin
The risk or severity of adverse effects can be increased when Chlorpheniramine is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Chlorpheniramine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Chlorpheniramine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Chlorpheniramine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Chlorpheniramine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Abatacept
The metabolism of Chlorpheniramine can be increased when combined with Abatacept.
Abexinostat
The risk or severity of QTc prolongation can be increased when Chlorpheniramine is combined with Abexinostat.
Abiraterone
The metabolism of Chlorpheniramine can be decreased when combined with Abiraterone.
Acalabrutinib
The metabolism of Chlorpheniramine can be decreased when combined with Acalabrutinib.
Acebutolol
The risk or severity of QTc prolongation can be increased when Chlorpheniramine is combined with Acebutolol.
Acenocoumarol
The risk or severity of adverse effects can be increased when Chlorpheniramine is combined with Acenocoumarol.
Acepromazine
The risk or severity of adverse effects can be increased when Chlorpheniramine is combined with Acepromazine.
Aceprometazine
The risk or severity of QTc prolongation can be increased when Chlorpheniramine is combined with Aceprometazine.
Acetazolamide
The risk or severity of adverse effects can be increased when Acetazolamide is combined with Chlorpheniramine.