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28 Cards in this Set
- Front
- Back
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what are the three tissues that have large amount of histimine
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skin
respiratory GI |
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Where is histimine stored?
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mast cells and basophils
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How is histime metabolized/
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n-methylation + oxidation in the brain
oxidative deamination outside the brain. |
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What are the effects of histimine?
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smooth mm contraction
vasodilation mucas production platelet aggreagation complement activation eosinohphill and neutrolphil chemotactic factors which causes hay fever asthma rash anaphalaxis histime is not the only compound in the body that causes these symptoms. |
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what is the major cause of histimine release?
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antibody antigen response in allergic reactions.(main)
any chemical that cause tissues damage can release histimine organic bases -morphine -d-tubocurare |
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What are the histimine receptors and where are they found?
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H1
found in skin, smooth mm, endothelium, and brain. H2 gastric mucosa, and heart and vessels H3 CNS H4 bone marrow hemopoetic |
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What type of receptor is H1?
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G protein
activates phospholipase c(PLC) which activates IP3 which releases Ca which binds calmodulin to activate myosin light chain kinase. |
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What type of receptor is H2?
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G protein
upregulates CAMP |
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What are the major effects of H1 activations?
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Smooth muscle contraction in the bronchi
vaso dilation and decreased BP |
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What are the major effects of H2 activations
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positive chemotropic and inotropic effects on the heart
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How does H1 lead to vasodilation?
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activates the endothelial derived relaxation factor to release NO
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Where does H1 lead to vasoconstriction?
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in the veins because there is no NO pathway in veins only venules therefore they contract bc of the myosic light chain kinase effects.
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What does H1 do to vascular permiability?
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increases it allowing flow out of the vessels and causing swelling.
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What is the wheel and flare response caused by H1
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When tissue is damaged there is a primary vasodilation then H1 activates the nerves endings to produces vasodilation in a wider area then it produces swelling by increaseing vascular permeabilty.
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What are the effects of diphenhydramine?(benadryl)
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antihistimine
anticholinergic sedation antimotionsickness |
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dimenhydrinate(dramamine) has what effects?
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antihistimine
anticholinergic sedation antimotionsickness |
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Promethazine(phenergin) has what effects?
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antihistimine
anticholinergic sedation antimemetic(antinausea) |
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Chlorpheniramine has what effects
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antihistime
slight anticholinergic slight sedation less than other 1st gen antihistimines *** common component in cold medicine. |
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Fexofenadine(allegra) has what effects
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least sedating antihistime 2nd generation
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cetirazine(zirtec) has what effect?
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antihistimine fastest onset possibly sedating 2nd gen
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loratidine is also known as what?
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claritin
2nd gen antihistimine |
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desloratidine is also known as what?
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clarinex
2nd gen antihistimine |
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what are some differences btw the 1st and 2nd gen antihistimines?
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1st gen are much more sedating
1st gen dont last very long 4-24h as oppose to 24h+ in 2nd gen 2nd gen usually require only once a day dosing both are usually metabolized by CYP3A4 |
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What are the antihistimines used for/
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allergic rhinitis, conjunctivititis, and uticaria(hiives)
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What the first gen antihistimes better at than the second gen?
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drying up runny nose because of the presence of the anticholinegic properties.
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how is olipatadine used?
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topically in eye drops for allergic conjucntivitis
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how is azelastine used?
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topically as nasal spray.
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what are the side effects of the antihistimines?
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sedation
fatigue poor eyehand corridination GI irratation dry mouth,nose,throat blurred vision increased glaucoma all these only seen in the 1st gen. |
