Antihistamine Flashcards
Histamine is released from what cells?
Basophil and mast cells
How is NO produced?
Arginine —(NO synthase)—>citrulline + NO
H1 receptor is __ coupled receptor, and activation of it would cause?
Gq Vasodilation via NO Increase capillary permeability Smooth muscle contraction Pain and itch
Where are H2 receptor cells located and activation causes what?
H2 receptors are found in gastric parietal cells
Activation–>increase acid secretion
H1 antagonists are competitive or noncompetitive blockers? and what are the 1st and 2nd gen drugs?
Competitive
1st gen—>diphenhydramine/promethazine/chlorpheniramine/meclizine
2nd gen—>cetirizine/loratadine/fexofenadine
What are the benefits of 2nd gen H1 blockers comparing with 1st gen?
2nd gen do not cross BBB—>non sedating
2nd gen do not block M—>unlike 1st gen
1st gen—>sedating/anti M
What are the 2 commonly used antiemetic H1 blockers? and what about nausea and vomiting in pregnancy?
Meclizine and promethazine
Meclizine
H1 or H2? Allergic reaction Motion sickness Preoperative sedation Sleep aid Parkinson Acute EPS
Allergic—>both H1 and H2
All the rest are for H1
What is the end product of 5HT metabolism?
5-HIAA
Which 5HT receptor that is directly coupled to an ion channel? and what are the rest of the 5HT receptor coupled with?
5HT3
The rest are G-protein coupled receptors
What is the mechanism of buspirone?
5HT1a partial agonist for chronic anxiety
What is the mechanism of “triptans” and what are they used for?
5HT1d agonist—>vasocontrict—>acute migraine
Are 5HT2 receptor inhibitory or excitatory in the CNS
Excitatory
What group of drugs that block 5HT2a receptor?
Atypical antipsychotic like olanzapine
What is the mechanism of cyproheptadine?
5HT2 blocker for serotonin syndrome
H1 blocker—>seasonal allergy