Chlorpheniramine (Maleate)

Overview

Chlorpheniramine (Maleate) is the maleate salt of chlorpheniramine. Chlorpheniramine is an antihistaminic agent derived from pheniramine. Chemically it is gamma-(4-chlorophenyl)-N,N-dimethyl-2-pyridinepropanamin. Administered orally or by subcutaneous injection for therapy and prophylaxis in conditions in which antihistamines may be effective.

Category:

Primary Characterstics

Chlorpheniramine (Maleate) also known as Chlorphenamine Maleate. . It is of Synthetic origin and belongs to Alkylamine. It belongs to H1-antagonist pharmacological group on the basis of mechanism of action. The Molecular Weight of Chlorpheniramine (Maleate) is 390.90.
Its pKa is 9.2.

Pharmacokinetics

Oral absorption of Chlorpheniramine (Maleate) is found to be 40% ±40. Volume of distribution is found to be 1-10 l/kg and plasma protien binding is 69-72%. Presystemic metabolism is noted to be 10% ±10 and metabolism is reported moderate, hepatic. Renal Excretion accounts for 50% and plasma half life is 30 hr.

Indications

Contraindications

Chlorpheniramine (Maleate) is contraindicated in conditions like Hypersensitivity.

Drug Interactions

Chlorpheniramine (Maleate) is known to interact with other drugs, the details of drug interactions is as follows:

DrugDetailsSeverityOnsetManagement
AlcoholMajor
AstemizoleConcomitant use of chlorpheniramine maleate and astemizole increase the risk of arrythmias.MajorContraindicated
Azatadine (Maleate)
Fosphenytoin
OxymorphoneCentral nervous system- and/or respiratory-depressant effects may be additively or synergistically increased in patients taking multiple drugs that cause these effects, especially in elderly or debilitated patients.ModerateDuring concomitant use of these drugs, patients should be monitored for potentially excessive or prolonged CNS and respiratory depression. Ambulatory patients should be made aware of the possibility of additive CNS effects (e.g., drowsiness, dizziness, lightheadedness, confusion) and counseled to avoid activities requiring mental alertness until they know how these agents affect them. Patients should also be advised to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
ParegoricCentral nervous system- and/or respiratory-depressant effects may be additively or synergistically increased in patients taking multiple drugs that cause these effects, especially in elderly or debilitated patients.ModerateDuring concomitant use of these drugs, patients should be monitored for potentially excessive or prolonged CNS and respiratory depression. Ambulatory patients should be made aware of the possibility of additive CNS effects (e.g., drowsiness, dizziness, lightheadedness, confusion) and counseled to avoid activities requiring mental alertness until they know how these agents affect them. Patients should also be advised to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Phenytoin (Na)
TerfenadineConcomitant use of chlorpheniramine maleate and terfenadine increase the risk of palpitation.

These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Interference in Pathology

No data regarding the pathological interferences produced by Chlorpheniramine (Maleate) is available.

Side Effects

The severe or irreversible adverse effects of Chlorpheniramine (Maleate), which give rise to further complications include Sinus tachycardia, Jaundice, Seizures, Hypertension, CNS stimulation.

Chlorpheniramine (Maleate) produces potentially life-threatening effects which include Bone marrow suppression. which are responsible for the discontinuation of Chlorpheniramine (Maleate) therapy.

The signs and symptoms that are produced after the acute overdosage of Chlorpheniramine (Maleate) include Hypotension, Convulsions, Coma, Urinary retention, Unconsciousness, Fever, Dryness of mucous, Flushing membrane, Pupillary dilatation.

The symptomatic adverse reactions produced by Chlorpheniramine (Maleate) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Drowsiness, Nausea, Vomiting, Restlessness, Palpitation, Constipation, Abdominal pain, Dry mouth, Blurred vision, Sedation, Facial dyskinesias, Blood dyscrasias, Xerostomia.

Available Brands

Click on the appropriate strength of the dosage form to view its available brands.

Single Ingredient

Inj: 10 mg/ml,
Syrup: 2 mg/5ml, 2.5 mg/5ml,
Tabs: 4 mg, 10 mg,

Multi ingredient

Eye Drops: 0.1 %w/v,
Syrup: 1 mg/5ml, 2 mg/5ml, 4 mg/5ml, 5 mg/5ml, 20 mg/5ml, 3.75 mg/5ml,
Susp: 1 mg/5ml,
Liquid: 2 mg/5ml,
Elixir: 1 mg/15ml,
Linctus: 2 mg/5ml, 2.5 mg/5ml,
Tabs: 1 mg, 2 mg, 4 mg,

Dosage

Chlorpheniramine (Maleate)'s dosage details are as follows:
Dose Single Dose Frequency Route Instructions

Adult Dosage

10 to 20 mg15 (15)24 hourlyIV,IM,SCSlow IV over a period of 1 minute. total dose should not exceed 40 mg.
4 to 24 mg14 (14)6 hourlyPOMax. 24 mg daily

Paedriatic Dosage ( 20 Kg. )

0.25 to 0.5 mg/kg0.38 (0.375)24 hourlyIntra Muscular
0.25 to 10 mg5.1 (5.125)24 hourlyIntra VenousMaximum dose= 12mg
1 to 2 mg/kg1.5 (1.5)8 hourlyOral
87.5 to 0 mcg/kg44 (43.75)6 hourlySubcutaneous

Neonatal Dosage ( 3 Kg. )

0.1 mg/kg0.1 (0.1)8 hourlyoral

High Risk Groups

Drug should not be given to Paediatrics, Geriatrics, and Neonates.

If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.

Warning / Precautions

Chlorpheniramine should be used with caution in bone marrow depression. Patients should observe caution while driving or performing other task requiring alertness because it may cause drowsiness. It should be used with caution in patients with urinary retention, history of bronchial asthma, hyperthyroidism, cardiovascular or liver disease. It should be used with caution in person with acute or chronic respiratory impairment, especially in children. Do not administer subcutaneously because irritation or lesion may occur.

Storage Conditions

Syrup

Store in a well closed container, Below 40°C. Do not Freeze. Protect from Sunlight and Moisture.

Tab

Store in a well closed container, Below 40°C. Protect from Sunlight and Moisture.

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