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