Autacoids Flashcards
Histamine receptors: H1R
Distribution: airway smooth muscle
Post receptor mechanism: Gq, ⬆️IP3, DAG
Function: ⬆️pruritus, pain, bronchoconstriction
Histamine receptor: H2R
Distribution: GI mucosa, heart muscle, mast cell
Post receptor mechanism: Gs, ⬆️ CAMP
Function: gastric acid production
Histamine receptor: H3
Distribution: brain
Post receptor mechanism: Gi, ⬇️CAMP
Function: ⬆️pruritus
Histamine receptor: H4R
Distribution: CD4 T cells
Post receptor mechanism: Gi, ⬇️ CAMP
Function: ⬆️pruritus
H1 blocker effects
Sedation
Anti nausea anti emetic
Anti muscarinic
Anti parkinson
Chlorphenamine
Paradoxical cns stimulation in children
Diphenhydramine, clemastine
Marked sedation, anti motion sickness
2nd generation h1 blockers
Cetirizine Fexofenadine Loratadine Desloratadine Ebastine Levocabastine Azelastine Olopatadine
PK of h1 blockers
Most are well absorbed orally
Peak 1-3 hrs after administration
Indications for antihistamine
Allergic rhinitis Allergic conjunctivitis Urticaria Atopic dermatitis Prophylaxis anti motion sickness
Adverse effects anti histamine
Cns depressive: fatigue, weakness
Cns stimulating: insomnia, irritability
Dry mouth
Less gi motility
Astemizole and terfenadine
⬆️QT interval (torsades de pointes)
Serotonin
Metabolized by MAO
Regulation of mood, sleep, temp control, vomitting, pain perception
Source of ergot alkaloid
Claviceps purpurea
Ergot alkaloids toxicity
Gi: diarrhea, vomitting