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Examples of sedating antihistamines

Antihistamines are inhibitors of histamine receptors. H1-antihistamines, inhibit competitively H1 receptors and the corresponding effects i. They do not inhibit antigen/antibodies reactions, nor histamine release, they inhibit H1 effects.

H1-antihistamines have been used for more than fifty years in treating various allergic manifestations. H1-antihistamines which penetrate into brain elicit, by inhibiting stimulant effect of histamine, drowsiness.

The drugs of the first antihistamine generation are: promethazine, alimemazine, dexchlorpheniramine, brompheniramine, buclizine, carbinoxamine and doxylamine, are sedating and elicit a drowsiness which can be awkward.

The first-genaration antihistamines have alpha adrenolytic activity which can decrease the vasoconstrictive effect of adrenaline and noradrenaline and an antimuscarinic effect with the corresponding adverse effects.

Histamine carries its message to a large number of cells by attaching to a special receptor on the cells' surfaces.

Antihistamines have a broad range of functions -- they can ease allergy symptoms, alleviate gastrointestinal complaints, prevent motion sickness and aid in sleep, to name just a few.

Antihistamines accomplish these tasks by counteracting histamine, an important protein with diverse effects in the body.

The first antihistamines, developed a few decades after the discovery of histamine, block a receptor for histamine known as the H1-receptor.

These can be thought of as the "old-fashioned" group of antihistamines.


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