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74 Cards in this Set

  • Front
  • Back
An endogenous substance synthesized, released and stored from mast cells, basophils, and neurons.
Histamine
These cells are found in skin, GI tract, and the respiratory tract.
Mast cells
These cells are found in the blood.
Basophils
These are found in the peripheral and central NS and release histamine.
Neurons.
___is synthesized from histidine (an amino acid) by the inducible enzyme l-histidine decarboxylase.
Histamine
Histmaine is metabolized via 2 pathways: name both.
1. Methylation to N-methyl histamine and then to N-methyl imidazole acetic acid (MAO) prior to urinary excretion.
2. Oxidative deamination to imidazole acetic acid (DAO) and them to imidazole acetic acid ribose prior to urinary exrcretion.
What drug will cause higher levels of histamine?
MAO-inhibitors b/c they inhibit MAO, part of the metabolic process of histamine.
Allergens rec. by ___cells and produces____towards that allergen.
plasma; antibodies.
Antibodies then attach to ___cells and cause release of ____.
Mast cells; histamine. Histamine then binds to histamine receptor.
Histamine receptors are are members of what receptor family?
G-protein coupled receptors.
What forms of histamine are r/t to ACUTE allergic reactions.
H1
This Histamine receptor is located bronchial smooth muscle, intestinal smooth muscle, cardiac endothelium, cardiac tissue and CNS.
H1
Allergens rec. by ___cells and produces____towards that allergen.
plasma; antibodies.
This type of histamine receptor is found in vascular SM, cardiac tissue, basophils, and parietal cells
H2
These histamine receptors are found t/o the CNS
H3
These histamine receptors are found in bone marrow and WBC
H4
This histamine receptor has a role in secretion of gastric acid
H2
This histamine receptor is important for modulating neurotransmission.
H3
These histamine receptors are important in regulating the immune response
H4
Mild cutaneous response to histamine
erythema, urticaria, and/or itching.
Mild to moderate histamine reactions
skin reactions, tachycardia, dysrhythmia, hypotension, mild resp. distress.
Severe anaphylactic symptoms include:
hypotension, ventricular fibrillation, cardiac arrest, bronchospasm, respiratory arrest.
What histamine receptors cause vasodilation of small blood vessels?
H1 and H2
This histamine receptor causes an increase in post-capillary venules.
H1
What is the are the "steps" in the triple response?
Localized red spot (w/n sec), Flare (due to reflexive vasodilation), wheal (as a result of inc. capillary permeability)
The binding of what 2 histamine receptors cause increase in inotropy (force)
H1 and H2
What receptor causes an increase of chronotropy?
H2
What receptor causes decreased AV conduction?
H1
What histamine receptor causes direct bronchoconstriction, and increased mucus viscosity?
H1
What histamine receptor causes SLIGHT bronchoDILATION, and increase mucous SECRETION?
H2
What histamine receptor causes a cough?
H1
What histamine receptor causes increased acid secrtion in the GI tract (parietal cells?/HCL)
H2
What two receptors cause cutaneous itching and PAIN.
H1 and H2
This histamine receptor causes presynaptic inhibition of histamine synthesis and release.
H3
This histamine causes regulation of DA, GABA, Ach, 5-HT, and NE.
H3
Food examples of direct histamine releasers:
peanuts, strawberries, eggs, milks...
Drug examples...
PCN, sulfonamides.
Fire ants, snake, bee
examples of venom that cause histamine release
examples of foreign proteins that cause histamine release:
non-human insulin/serum proteins.
What generation of H1 receptor antagonists is sedating?
1st generation is very sedating. 2nd generation non-sedating.
These drugs inhibit degranulation of mast cells and thereby prevent histamine release.
Mast cell stabilizers.
What is the #1 problem with H1 receptor antagonists?
Very Sedating.
What generation of H1 receptor antagonists is sedating?
1st generation is very sedating. 2nd generation non-sedating.
Diphenydramine
1st generation H1 antagonist
Hydroxyzine
1st generation H1 rec. antagonist.
Chlorpheniramine
1st generation H1 receptor antagonist.
Cyclizine
1st generation H1 recp. antagonist. Tx: motion sickness
Dimenhydrenate
1st genertion H1 recp. antagonist. Tx: motion sickness
Meclizine
1st generation H1 receptor blockers. Tx: motion sickness.
Promethazine
1st generation H1 recp. blocker. Tx: nausea.
1st generationg H1 recp. antagonists are ___/___antagonists.
reversible/competitive
1st gen. H1 Recp. Blockers also have mild___effects=anti-___
anticholinergic; anti-slude
1st generation H1 receptor blockers cross the___ and ____.
BBB and placenta. Careful in pregnant women.
Adjuvant to epi c/ anaphylactic, relief of allergy sx, sedation/sleep aid, prevention of motion sickness, vertigo, N/V, local anesthetic and anitussive.
Uses for 1st generation H1 blockers.
Sedation (c/ paradoxical effects in children; excitation), dizzy, fatigue, tacycardia, dysrhythmias, allergic rx w/ topical use, peripheral anti-msucarinic effects.
Adverse effects of H1 receptor blockers (antagonist).
Avoid what types of dugs with 1st generation oH1 receptor antagonist.
MAO-Inhibitors.
1st generation H1 blockers will cause synergystic AE when gvien with ___&___.
antimuscarinics and CNS depressants.
Acrivistine
2nd generation H1 blocker
Fexofenadine (allegra)
2nd generation H1 blocker
Loratidine (claritin)
2nd generation H1 blocker
Cetirizine (zyrtec)
2nd generation H1 blocker
Desloratadine
2nd generation H1 receptor blocker.
What 2nd generation H1 blocker has more of a CNS effect and therefore not recommended in pilots?
Cetrizine
What three 2nd generation H1 blockers are secreted in an unmetabolized form?
Cetrizine/Loratadine/Fexofenadine.
___/___are secreted in the urine.
Cetrizine and Loratadine
___is excreted in the feces.
Fexofenadine.
Cimetidine
H2 receptor antagonist
Nizatadine
H2 receptor antagonist
Famotiadine (pepcid)
H2 receptor antagonist.
Ranitidine (zantac)
H2 receptor blocker
H2 recptor blockers are used for what?
reduce gastric acid (HCL) production by parietal cells of GI tract. Tx: GERD.
Cromolyn Sodium and Nedocromil are examples of what?
Mast cell stabilizers.
Adveres effects of Mast cell stabilizers are?
cough and bitter taste, which decrease pt. compliance.
Use for mast cell stabilizers?
Prophylactic treatment of asthma and allergic rhinitis.