Chlorpheniramine, Dexchlorpheniramine (Monograph)
Brand names: Advil Allergy Sinus, Alka-Seltzer Plus, Aller-Chlor, Chlor-Trimeton, Coricidin,
... show all 13 brands
Drug class: First Generation Antihistamines
Introduction
First generation antihistamine; a propylamine-derivative.
Uses for Chlorpheniramine, Dexchlorpheniramine
Allergic Rhinitis
Symptomatic relief of allergic symptoms (e.g., rhinorrhea, sneezing, oronasopharyngeal irritation or itching, lacrimation, red, irritated, or itching eyes) caused by histamine release.
Used in fixed combination with other agents (e.g., acetaminophen, dextromethorphan, guaifenesin, ibuprofen, phenylephrine, pseudoephedrine) for relief of rhinorrhea, sneezing, lacrimation, itching eyes, oronasopharyngeal itching, and/or other symptoms (e.g., nasal/sinus congestion, cough) associated with allergic rhinitis (e.g., hay fever).
Use fixed-combination preparations only when symptoms amenable to each ingredient are present concurrently.
Chlorpheniramine, Dexchlorpheniramine Dosage and Administration
Administration
Oral Administration
Administer orally.
May be administered as self-medication in adults and children >6 years of age.
Administer to children 2 to ≤6 years of age under the direction of a clinician.
Dosage
Individualize dosage according to patient’s response and tolerance.
Fixed-combination preparations do not permit individual titration of dosages. When used in fixed combination with other agents (e.g., acetaminophen, dextromethorphan, guaifenesin, ibuprofen, phenylephrine, pseudoephedrine), select a dosage that is within the usual therapeutic range for each ingredient. Lower maximum daily chlorpheniramine dosages may be necessary because of other ingredients included in the formulations. Because combinations and dosage strengths vary for fixed-combination preparations, consult manufacturer’s product labeling for appropriate dosage of the specific preparation.
Pediatric Patients
Allergic Rhinitis
Oral
Children 2 to <6 years of age: 1 mg every 4–6 hours (as conventional formulations).
Children 6 to <12 years of age: 2 mg every 4–6 hours (as conventional formulations) or 8 mg (as extended-release tablets) once daily at bedtime or during the day, as indicated.
Children ≥12 years of age: 4 mg every 4–6 hours (as conventional formulations) or 8 or 12 mg (as extended-release tablets) twice daily in the morning and evening.
Adults
Allergic Rhinitis
Oral
4 mg every 4–6 hours (as conventional formulations) or 8 or 12 mg (as extended-release tablets) twice daily in the morning and evening.
Prescribing Limits
Pediatric Patients
Allergic Rhinitis
Oral
Children 2 to <6 years of age: Maximum 6 mg daily (as conventional formulations).
Children 6 to <12 years of age: Maximum 12 mg daily (as conventional formulations) or maximum 8 mg daily (as extended-release tablets).
Children ≥12 years of age: Maximum 24 mg daily (as immediate-release formulations or extended-release tablets).
Adults
Allergic Rhinitis
Oral
Maximum 24 mg daily (as conventional formulations or extended-release tablets).
Cautions for Chlorpheniramine, Dexchlorpheniramine
Warnings/Precautions
Sensitivity Reactions
Tartrazine Sensitivity
Some commercially available preparations may contain the dye tartrazine (FD&C yellow No. 5); possible allergic reactions in susceptible individuals (e.g., those sensitive to aspirin).
General Precautions
CNS Effects
Possible CNS depression (e.g., drowsiness, dizziness, weakness).
Caution when driving a motor vehicle or operating machinery. (See CNS Depressants under Interactions.)
Anticholinergic Effects
Possible anticholinergic effects (e.g., dryness of mouth, nose, and throat; dysuria; urinary retention). Use with caution, if at all, in patients with angle-closure glaucoma, prostatic hypertrophy, stenosing peptic ulcer, pyloroduodenal obstruction, or bladder neck obstruction.
Bronchopulmonary Effects
Possible bronchopulmonary effects (e.g., tightness of the chest, thickening of bronchial secretions, wheezing). Use not recommended, unless under the direction of a clinician, in patients who have a breathing problem (e.g., emphysema, chronic bronchitis). Use generally not recommended in asthmatics who previously experienced a serious antihistamine-induced adverse bronchopulmonary effect.
Phenylketonuria
Some commercially available preparations may contain aspartame (e.g., NutraSweet) which is metabolized in the GI tract to phenylalanine.
Use of Fixed Combinations
When used in fixed combination with other agents (e.g., acetaminophen, dextromethorphan, guaifenesin, ibuprofen, phenylephrine, pseudoephedrine), consider the cautions, precautions, and contraindications associated with the concomitant agent(s).
Specific Populations
Pregnancy
Category B. Use not recommended during the third trimester.
Lactation
Not known whether chlorpheniramine is distributed into milk; discontinue nursing or chlorpheniramine because of potential risk to nursing infants.
Pediatric Use
Possible severe reactions (e.g., seizures) in neonates; use not recommended in premature or full-term neonates. Possible paradoxical excitement (e.g., restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures).
Use conventional and extended-release preparations only under the direction and supervision of a clinician in children <6 years of age and in those <12 years of age, respectively.
Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection. Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established. Therefore, FDA recommended not to use such preparations in children <2 years of age; safety and efficacy in older children under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of nonprescription cough/cold preparations to avoid overdosage.
Geriatric Use
Possible increased risk of dizziness, sedation, and hypotension.
Common Adverse Effects
Sedation (e.g., drowsiness, dizziness, weakness), CNS stimulation (e.g., restlessness, insomnia, nervousness).
Drug Interactions
CNS Depressants
Potential pharmacologic interaction (additive CNS depression) with alcohol and other CNS depressants (e.g., hypnotics, sedatives, tranquilizers).
Laboratory Test Interferences
Antihistamines may suppress inhalation-challenge testing with histamine or antigen as well as the wheal and flare reactions to antigen skin testing.
Specific Drugs
Drug |
Interaction |
Comments |
---|---|---|
MAO inhibitors |
MAO inhibitors prolong and intensify anticholinergic effects of antihistamines |
Chlorpheniramine, Dexchlorpheniramine Pharmacokinetics
Absorption
Bioavailability
Well absorbed following oral administration, but only 25–45% (conventional tablets) or 35–60% (solution) of a single oral dose reaches the systemic circulation as unchanged drug.
Bioavailability of extended-release preparations is reduced compared to conventional tablets or solution.
Peak plasma concentrations generally occur within 2–6 hours following oral administration of conventional tablets or solution.
Onset
Antihistamine effect is apparent within 6 hours after a single dose.
Duration
Antihistamine effect may persist for ≥24 hours.
Distribution
Extent
Undergoes rapid and extensive distribution; however, distribution has not been characterized fully.
Plasma Protein Binding
Approximately 69–72%.
Elimination
Metabolism
Undergoes substantial metabolism in the GI mucosa during absorption and on first pass through the liver. Rapidly and extensively metabolized principally to at least 2 unidentified metabolites and monodesmethylchlorpheniramine and didesmethylchlorpheniramine.
Elimination Route
Excreted in urine.
Half-life
Terminal elimination half-life of chlorpheniramine is about 12–43 hours.
Special Populations
Terminal elimination half-life in children is about 9.6–13.1 hours (range: 5.2–23.1 hours).
Terminal elimination half-life in patients with chronic renal failure undergoing hemodialysis is about 280–330 hours.
Stability
Storage
Oral
Tablets
Tight containers at 15–30°C.
Extended-release Tablets
Well-closed containers at 15–30°C.
Oral Solution
Tight, light-resistant containers at 15–30°C; avoid freezing.
Actions and Spectrum
-
Blocks H1-receptor sites and prevents the action of histamine on the cell.
-
Suppresses flare and pruritus that accompany the endogenous release of histamine.
-
Exhibits some activities common to anticholinergics, ganglionic and adrenergic blocking agents, local anesthetics, and antispasmodics.
-
Causes less drowsiness and more CNS stimulation than some other first generation antihistamines.
-
Antihistamines do not block the stimulating effect of histamine on gastric acid secretion, which is mediated by H2-receptors of the parietal cells.
Advice to Patients
-
Importance of informing individuals who perform potentially hazardous tasks requiring mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle) about possible drowsiness, dizziness, or weakness.
-
Importance of avoiding alcoholic beverages during antihistamine therapy.
-
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses. Importance of patients already receiving another CNS depressant (e.g., sedatives, tranquilizers) not undertaking self-medication without first consulting a clinician.
-
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
-
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Bulk |
Powder* |
|||
Oral |
Solution |
2 mg/5 mL* |
Aller-Chlor Syrup |
Rugby |
Chlorpheniramine Maleate Solution |
||||
Tablets |
4 mg* |
Aller-Chlor |
Rugby |
|
Chlorpheniramine Maleate Tablets |
||||
Chlor-Trimeton 4 Hour Allergy (scored) |
Schering-Plough |
|||
Tablets, extended-release |
8 mg* |
Chlorpheniramine Maleate Extended-release Tablets |
||
12 mg* |
Chlorpheniramine Maleate Extended-release Tablets |
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Oral |
Capsules, liquid-filled |
2 mg with Acetaminophen 325 mg, Dextromethorphan Hydrobromide 10 mg, and Phenylephrine Hydrochloride 5 mg |
Alka-Seltzer Plus Cold & Cough Formula |
Bayer |
Solution |
1 mg/5 mL with Acetaminophen 160 mg/5 mL and Dextromethorphan Hydrobromide 7.5 mg/5 mL |
Triaminic Multi-Symptom Fever |
Novartis |
|
1 mg/5 mL with Acetaminophen 160 mg/5 mL, Dextromethorphan Hydrobromide 5 mg/ 5 mL, and Phenylephrine Hydrochloride 2.5 mg/5 mL |
Children’s Tylenol Plus Multi-Symptom Cold |
McNeil |
||
1 mg/5 mL with Dextromethorphan Hydrobromide 7.5 mg/5 mL |
Dimetapp Long Acting Cough Plus Cold |
Pfizer |
||
Tablets |
2 mg with Acetaminophen 325 mg |
Coricidin HBP Cold & Flu |
Schering-Plough |
|
2 mg with Acetaminophen 500 mg and Phenylephrine Hydrochloride 5 mg |
Sine-Off Sinus/Cold Caplets |
Gemini |
||
4 mg with Dextromethorphan Hydrobromide 30 mg |
Coricidin HBP Cough & Cold |
Schering-Plough |
||
Tablets, extended-release |
8 mg with Acetaminophen 500 mg and Phenylephrine Hydrochloride 40 mg |
Protid |
Lunsco |
|
Tablets, film-coated |
2 mg with Acetaminophen 325 mg and Phenylephrine Hydrochloride 5 mg |
Dristan Cold |
Pfizer |
|
2 mg with Acetaminophen 325 mg and Pseudoephedrine Hydrochloride 30 mg |
Flu-Relief Caplets |
Pfeiffer |
||
Kolephrin Caplets |
Pfeiffer |
|||
2 mg with Ibuprofen 200 mg and Pseudoephedrine Hydrochloride 30 mg |
Advil Allergy Sinus Caplets |
Pfizer |
AHFS DI Essentials™. © Copyright 2024, Selected Revisions February 1, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.