Final Exam - Histamine & Antihistamine Flashcards
What is the primary effect of histamine stimulation of H1 receptors on smooth muscle?
smooth muscle contraction.
How does histamine binding to H1 receptors lead to vasodilation?
stimulates the release of nitric oxide, which is a vasodilator. This relaxation of vascular smooth muscles causes vasodilation.
What is the consequence of histamine increasing the permeability of post-capillary venules?
allows fluids and cells to pass through the vessel walls, contributing to swelling and inflammation.
What sensation is induced by histamine binding to H1 receptors?
induce itch, leading to the sensation of itching.
What are the three components of the histamine triple response?
triple response consists of the reddening of the skin, the appearance of surrounding flare (swelling), and the presence of a weal, which is a raised, red, itchy area of skin.
Name two sedating antihistamines.
Doxylamine and Promethazine
Name three non-sedating antihistamines.
Fexofenadine, Loratadine, and Cetirizine
What is a characteristic of sedating antihistamines regarding their ability to cross the blood-brain barrier (BBB)?
can cross the BBB and cause central effects such as sedation and drowsiness
What prevents non-sedating antihistamines from crossing the BBB?
their high affinity for P-glycoprotein (P-gP) and their effects on other receptors.
What is the primary specificity of non-sedating antihistamines?
are specific for histamine at H1 receptors
How do the durations of action differ between sedating and non-sedating antihistamines?
shorter for sedating antihistamines (8-30 hours) and longer for non-sedating antihistamines (24 hours).
What potential drug interactions are associated with sedating antihistamines due to their ability to cross the BBB?
may interact with other medications or agents that cause sedation or central nervous system (CNS) depression, such as benzodiazepines, opioid analgesics, and alcohol
What distinguishes non-sedating antihistamines in terms of cardiac safety?
are considered cardiac safe
In addition to the treatment of allergies, what other uses are associated with sedating antihistamines?
short-term insomnia, as analgesics in combination with paracetamol and codeine, in cough preparations, and for the treatment of motion sickness.
What is the primary use of non-sedating antihistamines?
treatment of allergies