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Histamine

Histamine ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Histamine ballicule

What it isEndogenous amine acting at H1 to H4 receptors, mediating arousal, allergy and gastric acid.

Why this oneThe whole antihistamine and H2 blocker landscape is defined by which receptor is engaged and whether the drug enters the brain.

What limits itH1 blockade in the CNS causes sedation; peripherally restricted antihistamines exist precisely to avoid it.

Histamine molecular structure (skeletal formula)
Molecular structure: Histamine

NO BOXED WARNINGS

Principal riskEndogenous or dietary; no boxed warning applies

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger3 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilitySystemic vasodilation and bronchoconstriction with excessive diagnostic exposure

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