Antihistamines Flashcards
Histidine > Histamine {enzyme?}
HDC
Histidine decarboxylase
Histamine metabolites
N-methylhistamine (by Histamine N-methyltransferase)
N-methylimidazoleacetic acid (by MAO)
Imidazole acetic acid (by Diamine oxidase)
H1
Smooth muscle, Endothelium, Brain
Gq, IP3, DAG
H2
Gastric mucosa, cardiac muscle, mast cell, brain
Gs, cAMP
H1 action
Increase capillary permeability
Decrease lung airway
Increase sensory/ pain
Increase neurotransmitter release
H2 actions
Increase HR and contractility
Increase acid in stomach
Life saving drug for anaphylaxis
Epinephrine
1st generation H1 receptor antagonist
Chlorpheniramine
Diphendydramine
Hydroxyzine
Promethazine
2nd generation H1 receptor antagonist
Cetirizine
Loratadine
Fexofenadine
H1 receptor antagonist actions
Decrease vasodilation Decrease permeability Increased HR Reduce bronchoconstriction Acid secretion unchanged (H2 does) Puruirtis relief Decrease flares
Strongest muscarinic blocking H1 antagonist
Promethazine (1st gen)
2nd gen has no effect
Drug for motion sickness
Promethazine
H1 antagonist ADR
CNS stimulation CNS depression (1st gen) Antimuscarinic (1st gene) {dry mouth, urinary retention} GI side effects {anorexia, nausea, vomiting, constipation}
H1 antagonist use
Acute exudative allergy
Bronchial asthma
Systemic anaphylaxis {mostly Epinephrine}
Motion sickness (Promethazine)
H2 receptor antagonist
Cimetidine
Ranitidine
Famotidine