Pharmacology Clemastine

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clemastine antihistamine anticholinergic , sedative effects. antihistamines competitively bind histamine receptor sites, reducing neurotransmitter s effects. effects of histamine (which countered antihistamines) include:



increased capillary permeability
increased capillary dilatation
edema (i.e., swelling)
pruritus (itch)
gastrointestinal/respiratory smooth muscle constriction

clemastine inhibits both vasoconstrictor , vasodilator effects of histamine. depending on dose, drug can produce paradoxical effects, including cns stimulation or depression.


most antihistamines exhibit type of anticholinergic activity. antihistamines act competitively binding h1-receptor sites, blocking binding endogenous histamine. antihistamines not chemically inactivate or prevent normal release of histamine.


clemastine act fiasma (functional inhibitor of acid sphingomyelinase).


clemastine rapidly absorbed gastrointestinal tract , peak plasma concentrations attained in 2–4 hours. antihistamines thought metabolized in liver, mono-/didemethylation , glucuronide conjugation. inhibitor of cytochrome p450 cyp2d6 , may interfere other drugs metabolized isozyme.








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