What Is Chlorphenamine Maleate?
Chlorphenamine maleate is an antihistamine medication used to treat various allergy symptoms. It works by blocking the action of histamine, a substance in the body involved in allergic reactions. By inhibiting histamine, chlorphenamine helps relieve symptoms such as sneezing, itching, watery eyes, and runny nose associated with allergies.
This medication is commonly used to alleviate hay fever symptoms (allergic rhinitis), allergic conjunctivitis, and other allergic reactions. It may also be used to manage symptoms of insect bites or stings and certain skin rashes.
Chlorphenamine can cause drowsiness and is often included in over-the-counter cold and allergy medications. Sometimes, it may be combined with decongestants to relieve nasal congestion.
As with any medication, following the recommended dosage and usage instructions provided by a healthcare professional or as indicated on the product label is essential. Awareness of potential side effects and interactions with other medications is also essential.
If you have allergies or are experiencing symptoms that you believe may be related to an allergy, it’s advisable to consult a healthcare provider for proper diagnosis and guidance on the most appropriate treatment options for your specific situation.
Chlorphenamine maleate is absorbed relatively slowly from the gastrointestinal tract, with peak plasma concentrations occurring about 2.5 to 6 hours after oral doses. Bioavailability is low, with values of 25 to 50% having been reported. Chlorphenamine appears to undergo considerable first-pass metabolism. About 70% of chlorphenamine in the circulation is bound to plasma proteins. There is wide interindividual variation in the pharmacokinetics of chlorphenamine values ranging from 2 to 43 hours have been reported for the half-life. Chlorphenamine is widely distributed in the body and enters the CNS.
Chlorphenamine maleate is extensively metabolized. Metabolites include desmethyl- and desmethyl chlorphenamine. Unchanged drugs and metabolites are excreted primarily in the urine; excretion depends on urinary pH and flow rate. Only trace amounts have been found in the feces.
A duration of action of 4 to 6 hours has been reported. This is shorter than may be predicted from pharmacokinetic parameters.
More rapid and extensive absorption, faster clearance, and a shorter half-life have been reported in children.
Uses and Administration
Chlorphenamine maleate, an alkylamine derivative, is a sedating antihistamine that causes moderate sedation. It also has antimuscarinic activity. Chlorphenamine is a racemic mixture of the dextrorotatory isomer dexchlorpheniramine, which has about twice the activity of chlorphenamine by weight. Chlorphenamine maleate and dexchlorpheniramine maleate are used for the symptomatic relief of allergic conditions, including urticaria and angioedema, rhinitis, and conjunctivitis, and in pruritic skin disorders. They are common ingredients of compound preparations for symptomatic treatment of coughs and the common cold. However, such preparations should be used with caution in children and generally avoided in those under two years of age.
Chlorphenamine may be given intravenously as an adjunct in the emergency treatment of anaphylactic shock. Chlorphenamine maleate is given in oral doses of 4 mg every 4 to 6 hours up to a maximum of 24 mg daily. Doses for children, according to age, are 1 to 2 years, 1 mg twice daily for 2 to 5 years, 1 mg every 4 to 6 hours (maximum 6 mg daily) for 6 to 12 years, 2 mg every 4 to 6 hours (maximum 12 mg daily). Although not licensed in the UK, the BNFC suggests that children aged one month and over may be given 1 mg twice daily. Chlorphenamine maleate may be given by intramuscular, subcutaneous, or slow intravenous injection for 1 minute.
The usual dose is 10 to 20 mg, and the total dose given by these routes in 24 hours should be at most 40 mg. For children, doses of 87.5 micrograms/kg subcutaneously four times daily have been suggested. The following parenteral doses may also be used in children: the usual dose in those aged one month to 1 year is 250 micrograms/kg. Those aged 1 to 5 years may be given a dose of 2.5 to 5 mg, and those aged 6 to 12 years, 5 to 10 mg. Alternatively, children and adolescents aged 1 to 18 years may be given a dose of 200 micrograms/kg. The BNFC suggests that doses for children may be repeated, if necessary, up to 4 times in 24 hours.
Dexchlorpheniramine maleate is given in oral doses of 2 mg every 4 to 6 hours up to a maximum of 12 mg daily. Children aged 2 to 5 years may be given 0.5 mg every 4 to 6 hours (maximum 3 mg daily) and for those aged 6 to 12 years, 1 mg every 4 to 6 hours (maximum 6 mg daily).
Modified-release oral preparations of chlorphenamine maleate or dexchlorpheniramine maleate are available in some countries, and the dosage is specific to a particular formulation.
Dexchlorpheniramine maleate has been applied topically in some countries, although, as with other antihistamines, there is a risk of sensitization. Chlorphenamine polistirex (a sulfonated diethenylbenzene-ethenylben-zene copolymer complex), chlorphenamine tannate, and dexchlorpheniramine tannate are given orally and are used similarly to the maleate.
Chlorphenamine may be tried in patients with malaria who have chloroquine-induced pruritus. Still additionally, it has been shown to have some promise as an adjunct in the treatment of chloroquine-resistant malaria itself. Early studies indicated that chlorphenamine was only one of some drugs that reversed chloroquine resistance in vitro in isolates of Plasmodium falciparum. Later clinical studies in children in Nigeria showed enhanced efficacy when chlorphenamine was given with chloroquine. The overall management of malaria is discussed.
Adverse Effects and Precautions
As for the sedating antihistamines in general. Exfoliative dermatitis may develop as a side effect. Injections may be irritant and cause transient hypotension or stimulation of the CNS.
Effects on the Blood
There are several old and isolated reports of blood dyscrasias after the use of chlorphenamine maleate. These include agranulocytosis, thrombocytopenia, pancytopenia, and aplastic anemia. Hemolytic anemia has occurred after the use of dexchlorpheniramine maleate. The association with antihistamine use has been questioned in some of these cases.
Effects on the Senses
Chlorphenamine has been reported to affect the senses of smell and taste.
Facial dyskinesias have been reported after oral doses of chlorphenamine maleate.
Chlorphenamine maleate can interact with other medications, substances, or medical conditions. It’s crucial to inform your healthcare provider about all the medications you are taking, including prescription, over-the-counter, and herbal products, as well as any medical conditions you may have. Some potential interactions with chlorphenamine maleate include:
- Central Nervous System Depressants: Chlorphenamine can enhance the sedative effects of other central nervous system depressants, such as alcohol, benzodiazepines, and certain sleep medications. This can increase the risk of drowsiness and impairment.
- Monoamine Oxidase Inhibitors (MAOIs): Combining chlorphenamine with MAOIs, a class of antidepressants, can lead to serious side effects, including hypertensive crisis. It’s essential to wait a specific period after discontinuing an MAOI before starting chlorphenamine.
- Anticholinergic Medications: Concurrent use of medications with anticholinergic effects (drugs that block acetylcholine, a neurotransmitter) may increase the risk of side effects like dry mouth, blurred vision, constipation, and urinary retention.
- Certain Antifungal Medications: Some antifungal medications, particularly azole antifungals, may interact with chlorphenamine, affecting its metabolism and increasing the risk of side effects.
- Other Medications That Cause Drowsiness: Combining chlorphenamine with other medications that cause drowsiness can result in additive effects, increasing the risk of excessive sedation.
- Medical Conditions: Inform your healthcare provider if you have conditions such as glaucoma, prostate problems, urinary retention, or any other health issues, as these may be affected by chlorphenamine.
Always follow your healthcare provider’s advice and dosage recommendations. If you experience any unusual side effects or concerns about interactions, consult your healthcare provider promptly. This information is incomplete, and specific interactions can vary depending on individual circumstances.
(British Approved Name Modified, rINNM)
Synonyms: Chlorfenamin-maleinát; Chlorfenamino maleatas; Chlorphenamini Maleas; Chlorpheniramine Maleate; Chlorprophenpyridamine Maleate; Clorfenamina, maleato de; Klórfenamin-maleát; Kloorifenamiinimaleaatti; Klorfenaminmaleat
BAN: Chlorphenamine Maleate [BANM]
INN: Chlorphenamine Maleate [rINNM (en)]
INN: Maleato de clorfenamina [rINNM (es)]
INN: Chlorphénamine, Maléate de [rINNM (fr)]
INN: Chlorphenamini Maleas [rINNM (la)]
INN: Хлорфенамина Малеат [rINNM (ru)]
Chemical name: (±)-3-(4-Chlorophenyl)-NN-dimethyl-3-(2-pyridyl)propylamine hydrogen maleate
Molecular formula: C16H19ClN2,C4H4O4 =390.9
CAS: 132-22-9 (chlorphenamine); 113-92-8 (chlorphenamine maleate)
ATC code: R06AB04
Read code: y01tg
Pharmacopoeias. In China, Europe, Int., Japan, US
European Pharmacopoeia, 6th ed. (Chlorphenamine Maleate). A white or almost white crystalline powder. Freely soluble in water, soluble in alcohol. Protect from light.
The United States Pharmacopeia 31, 2008 (Chlorpheniramine Maleate). A white, odorless, crystalline powder. Soluble 1 in 4 of water and 1 in 10 of alcohol and chloroform, slightly soluble in ether and benzene. Its solutions in water have a pH between 4 and 5. Store in airtight containers. Protect from light.
Incompatibility. Chlorphenamine maleate has been reported to be incompatible with calcium chloride, kanamycin sulfate, noradrenaline acid tartrate, pentobarbital sodium, and meglumine adipiodone.
(British Approved Name Modified, rINNM)
Synonyms: Dekschlorfeniramino maleatas; Dekskloorifeniramiinimaleaatti; Dexchlorfeniramin-maleinát; Dexchlorphenamine Maleate; Dexchlorpheniramini Maleas; Dexclorfeniramina, maleato de; Dexklórfeniramin-maleát; Dexklorfeniraminmaleat
BAN: Dexchlorpheniramine Maleate [BANM]
INN: Dexchlorpheniramine Maleate [rINNM (en)]
INN: Maleato de dexclorfeniramina [rINNM (es)]
INN: Dexchlorphéniramine, Maléate de [rINNM (fr)]
INN: Dexchlorpheniramini Maleas [rINNM (la)]
INN: Дексхлорфенирамина Малеат [rINNM (ru)]
CAS: 25523-97-1 (dexchlorpheniramine); 2438-32-6 (dexchlorpheniramine maleate)
ATC code: R06AB02
Pharmacopoeias. In Europe, Japan, and US.
European Pharmacopoeia, 6th ed. (Dexchlorpheniramine Maleate). A white or almost white crystalline powder. Very soluble in water, freely soluble in alcohol, dichloromethane, and methyl alcohol. A 1% solution in water has a pH of 4.5 to 5.5. Protect from light.
The United States Pharmacopeia 31, 2008 (Dexchlorpheniramine Maleate). A white, odorless, crystalline powder. Soluble 1 in 1.1 water, 1 in 2 of alcohol, 1 in 1.7 of chloroform, and 1 in 2500 of ether slightly soluble in benzene. The pH of a 1% solution in water is between 4.0 and 5.0. Store in airtight containers. Protect from light.
BP2008: Chlorphenamine Injection Chlorphenamine Oral Solution Chlorphenamine Tablets
The United States Pharmacopeia 31, 2008: Chlorpheniramine Maleate and Phenylpropanolamine Hydrochloride Extended-release Capsules; Chlorpheniramine Maleate and Phenylpropanolamine Hydrochloride Extended-release Tablets; Chlorpheniramine Maleate and Pseudoephedrine Hydrochloride Extended-release Capsules; Chlorpheniramine Maleate and Pseudoephedrine Hydrochloride Oral Solution; Chlorpheniramine Maleate Extended-release Capsules; Chlorpheniramine Maleate Injection; Chlorpheniramine Maleate Syrup; Chlorpheniramine Maleate Tablets; Dexchlorpheniramine Maleate Syrup; Dexchlorpheniramine Maleate Tablets.
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
Argentina: Afeme; Alergidryl; Alergitrat; Isomerine¤; Qura Plus;
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Penntuss¤; Phena-Chlor¤; Phenacon¤; Phenahist-TR¤; Phenapap Sinus Headache & Congestion; Phenate¤; Phenchlor SHA¤; Phenhist DH with Codeine; Polaramine Expectorant; Poly-Tussin; Prehist D; Prehist; Primatuss Cough Mixture 4; Probahist¤; Protid; PSE CPM; Pseudo-Chlor; Pseudo-Gest Plus; QDALL; Quadra Hist¤; Quelidrine; R-Tanna S Pediatric; R-Tanna; R-Tannamine; R-Tannate; Ralix; Relacon-HC; Remcol Cold¤; Remcol-C¤; Rentamine Pediatric; Resaid¤; Rescon-DM; Rescon-ED¤; Rescon-Jr; Rescon-MX; Rescon¤; Respa-ARM¤; Rhinatate-NF; Rhinatate; Rhinogesic¤; Rhinolar-EX¤; Rhinolar¤; Rhinosyn-DM; Rhinosyn; Ricobid¤; Rinade BID¤; Robitussin PM Cough & Cold; Rolatuss Expectorant; Rolatuss Plain; Ru-Tuss II¤; Ru-Tuss¤; Ry-Tuss; Ryna-C¤; Ryna¤; Rynatuss; Ryneze; S-T Forte 2; Salphenyl¤; Scot-Tussin Cough & Cold Medicine¤; Scot-Tussin DM; Silaminic Cold¤; Simplet; Sinapils¤; Sinarest; Sine-Off Maximum Strength Allergy/Sinus; Sine-Off Sinus Medicine¤; Singlet; Sinulin¤; Sinutab Maximum Strength Sinus Allergy; Sinutrex Extra Strength¤; Snaplets-D¤; Snaplets-Multi¤; Spray-ur-Cold¤; Stahist; Sudafed Cold & Allergy; Sudafed Plus; Super Cold Tabs¤; Super Strength Sinadrin¤; T-Dry¤; T-Koff¤; Tanafed DM¤; Tanafed DMX; Tanafed DP; Tanafed¤; Tannic-12; Tanoral; Temazin Cold¤; Thera-Hist¤; TheraFlu Flu and Cold; TheraFlu Flu, Cold & Cough; TheraFlu Severe Cold; Threamine DM¤; Tri-Clear¤; Tri-Nefrin Extra Strength¤; Tri-Phen-Chlor TR¤; Tri-Tannate Plus Pediatric; Tri-Tannate; Triactin¤; Triaminic Allergy¤; Triaminic Chewable¤; Triaminic Cold & Allergy; Triaminic Cold & Cough; Triaminic Cold¤; Triaminic Flu, Cough & Fever; Triaminic Night Time Cough & Cold; Triaminic Softchews; Triaminic-12¤; Triaminic¤; Triaminicin Cold, Allergy, Sinus¤; Triaminicol Multi-Symptom Cough and Cold¤; Triaminicol Multi-Symptom Relief¤; Tricodene Forte¤; Tricodene NN¤; Tricodene Sugar Free; Tricom¤; Triminol Cough¤; Trind¤; Triotann; Tripalgen Cold¤; Triphenyl¤; Tritan; Tusquelin¤; Tuss-Tan; Tussanil DH; Tussanil Plain; Tussar DM; Tussend; Tussi-12; Tussionex Pennkinetic; Tussizone; Ty-Cold¤; Tylenol Allergy Complete Multi-Symptom; Tylenol Allergy Sinus Day & Night; Tylenol Children’s Cold Plus Cough; Tylenol Children’s Cold; Tylenol Childrens Plus Cold Nighttime; Tylenol Cold Complete Formula; Tylenol Cold Effervescent¤; Uni-Decon¤; Unituss HC; Vanex Forte-R¤; Vanex Forte¤; Vanex Grape¤; Vanex-HD; Vicks 44M Cold, Flu & Cough LiquiCaps; Vicks Children’s NyQuil Allergy/Head Cold; Vicks Children’s NyQuil Night-time Cold/Cough Liquid; Vicks Pediatric Formula 44M Multi-Symptom Cough & Cold; Viro-Med¤; Xiral; Xiratuss; Z-Cof HC
He knows everything about medications – to which pharmacological group the drug belongs, what components are included in its composition, how it differs from its analogs, what indications, contraindications, and side effects remedy has. John is a real pro in his field, so he knows all these subtleties and wants to tell you about them.