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Histamine: Moderator: Dr. Pooja Shukla Resident: Fariha Fatima JR-2
Histamine: Moderator: Dr. Pooja Shukla Resident: Fariha Fatima JR-2
enterochromaffin-like cells.
The effect involves three separate cell types: smooth muscle in the
microcirculation, capillary or venular endothelium, and sensory nerve
endings.
At the site of injection, a reddening appears owing to dilation of small
vessels, followed soon by an edematous wheal at the injection site and a
red irregular flare surrounding the wheal.
first-generation second-
generation
Neutral at physiological pH
Cross bbb where they block
the actions of histaminergic Ionised at
neurons in the CNS. physiological pH
Do not cross bbb
Pharmacokinetics:
These agents are rapidly absorbed after oral
administration, with peak blood concentrations occurring in
1–2 hours.
The newer agents are considerably less lipid soluble than the
first-generation drugs and are substrates of the P-glycoprotein
transporter in the blood-brain barrier; as a result they enter the
central nervous system with difficulty or not at all.
Pharmacodynamics:
The first-generation H 1 -receptor antagonists have
many actions in addition to blockade of the actions of
histamine.
• Adrenoceptor-blocking actions
• Serotonin-blocking action
• Local anesthesia
Other actions