PAEDICOF

Dexchlorpheniramine, the d-isomer of the racemic compound chlorpheniramine, is two times more active than chlorpheniramine. Dexchlorpheniramine does not prevent the release of histamine, but rather, competes with free histamine for binding at the H₁-receptor sites, and competitively antagonizes the effects of histamine on H₁-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Blockade of H₁-receptors also suppresses the formation of oedema, flare, and pruritus that result from histaminic activity. Since dexchlorpheniramine binds to central and peripheral H₁-receptors, sedative effects are likely to occur. Dexchlorpheniramine has high antihistaminic activity, moderate anticholinergic effects and minimal sedative effects.

Dextromethorphan is a non-opioid antitussive drug. The major metabolite of dextromethorphan, dextrorphan, binds with high affinity to σ-receptors to produce its antitussive activity without exhibiting the classic opiate effects that occur from binding into μ- and δ-receptors. In larger than therapeutic doses, dextrorphan is also an antagonist of N-methyl-D-aspartate (NMDA) receptors.

Pseudoephedrine is a sympathomimetic agent with direct and indirect effects on adrenergic receptors. It has alpha and beta adrenergic activity and some stimulant effect on the central nervous system. The sympathomimetic effect of pseudoephedrine produces vasoconstriction which in turn relieves nasal congestion.