Autocoids & Anti-Histamines (final exam) Flashcards
Definition of autacoids
Chemical mediators that function in localized tissue and participate in physiological response to injury
Examples of autacoids
Histamines
Serotonin (5-HT)
Prostaglandin
Peptides
Where are histamines stored?
Throughout the body (lungs, skin, stomach), within mast cells
Histamine release is triggered by:
Immune-induced (type 1 hypersensitivity)
Insect sting / envenomation
Drug-induced
Physical injury
Antihistamines (H1 antagonists)
Diphenhydramine
Hydroxazine
Loratadine
Janus kinase inhibitor
Oclacitinib
Leukotriene inhibitor
Zafirlukast
5-HT inhibitor
Trazadone
Histamine receptors
Histamine-1 (H1)
Histamine-2 (H2)
Effects of H1 agonism
Inflammation
Bronchoconstriction - smooth muscle contraction
Vasodilation - vascular smooth muscle relaxation
Mediate signs of urticarial and pruritis
Effects of H2 agonism
Increased gastric HCl secretion
Vascular smooth muscle relaxation
Anti-histamine drug targets
Mast cell stabilizers (glucocorticoids)
Physiologic histamine antagonists (catecholamines)
Therapeutic histamine antagonists (histamine receptors antagonists)
Anti-histamine mechanism of action
Competitive H1 antagonism
Relaxation of bronchiolar smooth muscle
Inhibits vasodilation
Inhibits pruritis and itch stimulation
Anti-histamine pharmacokinetics
High bioavailability
High Vd
Adverse effects
Sedation is common (first gen more than second gen)
CNS depression
Antimuscarinic signs
Drug tolerance