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ANTICHOLINERGIC AGENTS.
These drugs inhibit vagally mediated reflexes by antagonizing the action of acetylcholine at
muscarinic receptors. Of the available anticholinergic agents, ipratropium bromide is the
most commonly used
ANTIHISTAMINES.
Histamine exerts its effects through binding with one of its three receptors, referred to as H1-,
H2-, or H3-receptors. Histamine effects triggered through H1-receptor binding are those most
relevant to allergic inflammation and include pain, pruritus, vasodilation, increased vascular
permeability, smooth muscle contraction, mucus production, and the stimulation of
parasympathetic nerve endings and reflexes.
The H1-type antihistamines prevent the effects of H1-receptor activation through reversible,
competitive inhibition of histamine by binding to the H1-receptor. As a result, antihistamines
work best in preventing rather than reversing the actions of histamine and are most effective
when given at doses and dosing intervals resulting in the persistent saturation of target organ
tissue histamine receptors.
These antihistamines are further divided into 1st-generation antihistamines, which, because of
their lipophilicity, cross the blood-brain barrier to exert effects on the central nervous system,
and 2nd-generation antihistamines, which exert minimal, if any, central nervous system
effects because of their inability to cross the blood-brain barrier owing to their size, charge,
and lipophobicity.