Each mL contains Chlorphenamine (as Maleate) 10 mg.
Chlorphenamine is a propylamine derivative antihistamine. Chlorphenamine maleate has solubilities of approximately 250 mg/mL in water and 100 mg/mL in alcohol at 25°C.
Pharmacology: Pharmacokinetics: Distribution of chlorphenamine into human body tissues and fluids has not been fully characterized. Following IV administration in rabbits, highest concentration of the drug is attained in the lungs, heart, kidneys, brains, small intestine and spleen with lower concentrations in the large intestine, muscle, stomach, adrenal fat, liver and mesentery. Following IV administration in humans, chlorphenamine undergoes rapid and extensive distribution. Chlorphenamine is distributed into saliva and the drug and/or its metabolites appear to be distributed in small amounts into bile. Chlorphenamine and its metabolites are excreted almost completely in urine. Excretion is dependent on urinary pH and flow rate. Only trace amounts have been found in the faeces. More rapid and extensive absorption, faster clearance and a shorter half-life have been reported in children.
The chlorphenamine products are intended for the relief of some of the manifestations of allergic states such as in hay fever, urticaria, allergic eczema, vasomotor rhinitis, serum sickness, atopic dermatitis, contact dermatitis, and insect bites.
Chlorphenamine maleate injection is administered by subcutaneous, intramuscular or by slow intravenous injection, over a period of 1 minute. The usual dose is 10 to 20 mg and the total dose given by these routes in 24 hours should not normally exceed 40 mg. For children, dose of 87.5 mg/kg body weight subcutaneously four times daily have been suggested.
For the relief of allergic reactions to blood or plasma in adults and children 12 years of age and older, a single chlorphenamine maleate dose of 10-20 mg may be administered subcutaneously, IV or IM. For the adjunctive therapy of anaphylaxis in adults and children 12 years of age and older, a single dose of 10-20 mg may be administered IV. For the treatment of uncomplicated allergic conditions in adults and children 12 years of age and older (when oral therapy is not feasible or is contraindicated), 5-20 mg may be given parenterally as a single dose. The maximum parenteral dosage of chlorphenamine maleate in adults and children 12 years of age and older is 40 mg daily. Chlorphenamine maleate may be given by intramuscular, subcutaneous or diluted with 5 to 10 mL of blood, by slow intravenous injection over a period of 1 minute, or as prescribed by physician.
Chlorphenamine shares the toxic potentials of other antihistamines and the usual precaution of antihistamine therapy should be observed.
Safety and efficacy of chlorphenamine maleate injection in children younger than 12 years of age has not been established.
Like other antihistamine, chlorphenamine should not be used in premature or full term neonates.
There are no adequate and controlled studies to date using chlorphenamine in pregnant women and the drug should be used during the first 2 trimesters only when clearly needed. Because of the risk severe reaction (age seizures) to antihistamines in neonates, chlorphenamine should not be used during the third trimesters. It is not known that whether chlorphenamine is distributed in milk but other antihistamines have been detected in milk. Because of the potential for serious adverse reactions to antihistamines in nursing infants, a decision whether to discontinue chlorphenamine or not, taking into account the importance of the drug to the woman.
Chlorphenamine is well tolerated. Adverse effects which vary in incidence and severity are caused by all antihistamines, however serious toxicity rarely occurs.
Geriatric patients may be particularly susceptible to dizziness, sedation and hypotension. Most mild reactions may be relieved by a reduction in dosage or changing to another antihistamine. The most common side effects are sedation, lassitude, dizziness and incoordination. Anticholinergic effects common to all antihistamines like: dryness of mouth, nose and throat, dysuria and urinary retention, may be irritant and cause transient hypotension or stimulation of the CNS.
Store at temperatures not exceeding 25°C.
R06AB04 - chlorphenamine ; Belongs to the class of substituted alkylamines used as systemic antihistamines.
Soln for inj (amp) 10 mg/mL x 1 mL x 50's.