Chlorphenamine


Generic Medicine Info
Indications and Dosage
Oral
Allergic conditions
Adult: As conventional tab: 4 mg 4-6 hourly. Max: 24 mg daily. As extended-release tab: 12 mg 12 hourly. Max: 24 mg daily.
Child: 1-<2 years 1 mg bid; 2-5 years 1 mg 4-6 hourly. Max: 6 mg daily; 6-<12 years 2 mg 4-6 hourly. Max: 12 mg daily; ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.
Elderly: Dose reduction may be needed. Max: 12 mg daily.

Parenteral
Allergic conditions
Adult: 10-20 mg via IM, SC or slow IV inj over 1 minute. Max: 40 mg daily.
Child: 1 month to <1 year 0.25 mg/kg; 1-5 years 0.2 mg/kg or 2.5-5 mg; 6-12 years 0.2 mg/kg or 5-10 mg; >12 years 0.2 mg/kg or 10-20 mg.
Administration
May be taken with or without food.
Incompatibility
Incompatible with Ca chloride, kanamycin sulfate, norepinephrine acid tartrate, pentobarbital Na and meglumine adipiodone.
Contraindications
Narrow-angle glaucoma, symptomatic prostate hypertrophy, acute asthma attacks, stenosing peptic ulcer, bladder neck or pyloroduodenal obstruction. Concomitant or within 14 days of MAOI use.
Special Precautions
Patient with CV disease (e.g. ischaemic heart disease, hypertension), increased intraocular pressure, thyroid dysfunction, asthma or other chronic breathing disorders (e.g. bronchitis), epilepsy, prostatic hyperplasia, genitourinary obstruction. Hepatic or renal impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Sedation; excitation (in young children).
Eye disorders: Blurred vision.
Gastrointestinal disorders: Dry mouth, nausea, vomiting, diarrhoea, epigastric pain.
General disorders and administration site conditions: Fatigue, lassitude.
Metabolism and nutrition disorders: Anorexia, increased appetite.
Nervous system disorders: Somnolence, disturbance in attention, abnormal coordination, dizziness, headache.
Patient Counseling Information
This drug may cause drowsiness, dizziness, blurred vision and psychomotor impairment, if affected, do not drive or operate machinery.
Overdosage
Symptoms: Sedation, paradoxical excitation of the CNS, toxic psychosis, apnoea, convulsions, anticholinergic effects, dystonic reactions, CV collapse (e.g. arrhythmias). Management: Symptomatic and supportive treatment. Gastric lavage or induced emesis using syrup of ipecacuanha may be considered. Activated charcoal can be given if overdosage is by the oral route, provided there are no contraindications for use and the overdose is recent (within 1 hour of ingestion). CNS convulsions may be treated with IV diazepam. Hypotension and arrhythmias should be treated vigorously. For severe cases, haemoperfusion may be used.
Drug Interactions
Enhanced sedative effect with other CNS depressants (e.g. barbiturates, hypnotics, opioid analgesics, sedatives, antipsychotics. Inhibits phenytoin metabolism which may lead to phenytoin toxicity.
Potentially Fatal: Increased anticholinergic effects with MAOIs.
Food Interaction
Enhanced CNS depression with alcohol.
Lab Interference
May suppress the wheal and flare reactions to skin test antigens.
Action
Description: Chlorphenamine, an alkylamine derivative, is a sedating antihistamine that competitively and reversibly inhibits histamine H1- receptor in the gastrointestinal and respiratory tract and blood vessels. This prevents the release of histamine, prostaglandins and leukotrienes, and also prevents the migration of inflammatory mediators.
Synonym: Chlorpheniramine.
Onset: Within 30 minutes.
Duration: 4-6 hours.
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract. Bioavailability: 25-50%. Time to peak plasma concentration: 2.5-6 hours.
Distribution: Widely distributed in the body, including the CNS. Enters breast milk. Volume of distribution: 6-12 L/kg. Plasma protein binding: Approx 70%.
Metabolism: Extensively metabolised in the liver by CYP enzymes, including CYP2D6 to active and inactive metabolites, including desmethyl- and didesmethylchlorphenamine; undergoes extensive first-pass metabolism.
Excretion: Mainly via urine (approx 22%, as unchanged drug); faeces (trace amounts). Elimination half-life: 2-43 hours.
Chemical Structure

Chemical Structure Image
Chlorphenamine

Source: National Center for Biotechnology Information. PubChem Database. Chlorpheniramine, CID=2725, https://pubchem.ncbi.nlm.nih.gov/compound/Chlorpheniramine (accessed on Jan. 21, 2020)

Storage
Store between 20-25°C. Protect from light.
MIMS Class
Antihistamines & Antiallergics
ATC Classification
R06AB04 - chlorphenamine ; Belongs to the class of substituted alkylamines used as systemic antihistamines.
References
Anon. Chlorphenamine [Chlorpheniramine]. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/02/2022.

Anon. Chlorpheniramine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 15/02/2022.

Buckingham R (ed). Chlorphenamine Maleate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/02/2022.

Chlorphen-12 Tablet, Film Coated, Extended Release (KVK-Tech, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 15/02/2022.

Chlorphenamine 10 mg/mL Solution for Injection (Macarthys Laboratories Ltd). MHRA. https://products.mhra.gov.uk. Accessed 15/02/2022.

Chlorphenamine 2 mg/5 mL Oral Solution (Dalkeith Laboratories Limited). MHRA. https://products.mhra.gov.uk. Accessed 15/02/2022.

Chlorphenamine 4 mg Tablets (Special Concept Development UK Limited T/A RxFarma). MHRA. https://products.mhra.gov.uk. Accessed 15/02/2022.

Chlorpheniramine Maleate Tablet (Reliable 1 Laboratories LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 15/02/2022.

Joint Formulary Committee. Chlorphenamine Maleate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/02/2022.

Disclaimer: This information is independently developed by MIMS based on Chlorphenamine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 MIMS. All rights reserved. Powered by MIMS.com
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