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Pharm (Test 3)

What are the 4 roles and functions of histamine? 1)mediator of allergic reactions and inflammatory processes, 2)affects gastric secretion, 3)neurotransmitter, 4)neuromodulator
Where is bound histamine found? in vesicles in mast cells or basophils
Histamine is (active or inactive?) in bound form. inactive
Where are mast cells found? tissues -- nose, mouth, feet, internal body surfaces, blood vessels
Where is non-mast cells histamine found? in the brain as an endogenous NT
What type of cells store and release histamine from the fundus of the stomach? enterochromaffin-like cells (activates acid-production from parietal cells)
The major pathophysiologic mechanism of mast cells and basophil histamine release is _________________. immunologic
Negative feedback from ________ receptors found in skin and basophils limits reaction in the skin and blood. H2
What type of drugs (2 examples?) compete w/ histamine for sites within cells and displace histamine. amine drugs -- morphine and tubocurarine
H1 receptors are similar to _____________ receptors. muscarinic receptors
Where are H1 receptors located? presynaptic in the brain; endothelium, smooth muscle cells, nerve endings (brain)
H1 receptor activation causes: bronchoconstriction, slowed conduction through the AV node, coronary artery vasoconstriction
H2 receptors are similar to ______________ receptors. 5-HT1 receptors
Where are H2 receptors located? postsynaptic in the brain; gastric mucosa, cardiac muscle cells, and some immune cells
H2 receptor activation causes: CNS stimulation, increased myocardial contractility, increased HR, bronchodilation, increased secretion of H+ ions by gastric parietal cells (dec. pH)
H3 receptors are similar to _______________ receptors. H4
Where are H3 receptors located? heart presynaptic postganglionic SNS
Activation of H3 receptors causes: dec. NE release, dec. synthesis and release of histamine (negative feedback)
H4 receptors are similar to _______________ receptors. H3
Where are H4 receptors located? blood cells, bone marrow (eosinophils, neutrophils)
What are some cardiac effects caused by histamine on H1 and H2 receptors? dec. in SBP and DBP (vasodilation), inc. HR, vasodilation (nitric oxide), coronary vasoconstriction, edema, inc. capillary permeability
What are the direct effects of histamine on the myocardium? This is caused by stim. of which receptor? inc. contractility, inc. HR (result of H2 receptor stimulation)
How do H1 and H2 receptors differ in their vasodilatory effects? H1=rapid onset, transient; H2=slower onset, sustained
What effect does H1 receptor stim. have on pulmonary system? bronchoconstriction
What effect does H2 receptor stim. have on pulmonary system? bronchodilation
Asthma patients have ______-______X greater sensitivity when it comes to histamine-induced bronchoconstriction. 100-1000X
What effect does histamine have on the GI system? excessive secretion of gastric fluid with a low pH
What effect does histamine have on the CNS? Due to which receptor? CNS stimulation (agitation); H2 receptor
True or False: Histamine receptor blockers inhibit the release of histamine. False; it affects ability of histamine to get to receptors
What are some examples of H1 receptor blockers? diphenhydramine/Benadryl, dimenhydrinate/Dramamine, meclizine/bonine, promethazine/phenergan
How do H1 receptor blockers work? prevent activation of H1 receptors by histamine -- competitive antagonist; may activate muscarinic, 5HT3, alpha receptors
What are some examples of H2 receptor blockers? cimetidine/tagament, famotidine/Pepcid, ranitidine/zantac
How do H2 receptor blockers work? prevent inc. in intracellular cAMP which would activate the protein pump of the gastric parietal cell to secrete H+ ions
What is the drug of choice for anaphylaxis treatment? epinephrine
How does epi work to treat anaphylaxis? physiologic antagonist; has opposite effect on smooth muscle, but acts on different receptors
What drugs can be used to prevent the release of histamine? How do they work? cromolyn and beta2 agonists; dec. the degranulation of mast cells that occurs when immunologic triggering
Define anaphylaxis severe immediate hypersensitive reaction mediated by IgE antibodies formed in response to a foreign antigen
Define anaphylactic shock. the cardiovascular collapse that results from anaphylaxis
Define anaphylactoid reaction. non IgE mediated reaction that clinically resembles anaphylaxis
Drug reactions are frequent in anesthesia. Only _____% are true allergic reactions. 10%
How does re-exposure to an antigen trigger an anaphylactic reaction? re-exposure to the antigen causes the bridging of cell-surface IgE receptor molec. which activates enzymes which starts a cascade which leads to an introduction of extracellular Ca+ and mobilization of intracellular Ca+ and thus release of mediators
What are some examples of mast cell mediators? histamine, kinins, heparin, leukoagglutinis, leukotrienes, platelet-activating factor, prostaglandins, serotonin
What are some physiologic manifestations of anaphylaxis? bronchospasm, tachycardia, hypotension, edema, urticaria, excessive resp/GI secretions, inflammation, abdominal pain, N/V/D
What are some cutaneous signs of anaphylaxis? urticaria, angioedema, erythema, periorbital and facial edema
What are some resp signs of anaphylaxis? coughing, sneezing, hoarseness, intraoral edema, laryngeal edema, stridor, cyanosis, tachypnea, WHEEZING, dec. pulmonary compliance, pulm. edema, acute resp distress
define urticaria. skin wheals, pruritic
Define angioedema. deep nonpitting cutaneous edema from vasodilation and increased permeability of subq vessels. can involve the airway with compromise
What are some cardiovascular signs of anaphylaxis? diaphoresis, hypotension, tachycardia, arrhythmias, dec. SVR, cardiac arrest, pulm. HTN
Define Grade 1 anaphylaxis. Give epi? erythema, urticaria w/ or w/o angioedema; epi NOT given
Define Grade 2 anaphylaxis. moderate severity, cutaneous signs, hypotension and tachycardia, cough, diff. to ventilate
Define Grade 3 anaphylaxis. life-threatening severity, CV collapse, tachycardia or bradycardia, dysrhythmias, bronchospam
Define Grade 4 anaphylaxis. cardiac and/or resp arrest
What are some risk factors for anaphylaxis. receiving parenteral drugs, history of allergic rxn or atopy, asthma, women (2.5x-- cosmetics w/ quaternary ammonium), history of previous anesthetic
What are some examples of drugs associated w/ reactions? muscle relaxants (most frequent! usually non IgE), morphine, Demerol, codeine, induction agents (pentothal, ketamine, benzos, propofol), locals, ABX, blood, protamine, latex
True or False: Sugammadex is approved by the FDA for treatment of Roc-induced anaphylaxis. False-- not approved d/t hypersensitivity concerns
What is the treatment regimen for anaphylaxis? remove agent, airway mgmt., fluids, epi, vaso, d/c anesthetic agents, antihistamines (Benadryl/Pepcid), glucocorticoids (hydrocortisone)
How much fluid should you give to treat anaphylaxis? 25-50mL/kg (2-4L)
How much epi should you give for moderate hypotension during anaphylaxis? 10-100mcg
How much epi should you give for circulatory collapse/pulselessness during anaphylaxis? 1-3mg
What is an appropriate infusion dose of epi during anaphylaxis? 4-10mcg/min
How much vaso should you give for moderate hypotension during anaphylaxis? 0.5-2units
How much vaso should you give for circulatory collapse/pulselessness during anaphylaxis? 40 units
What dose of diphenhydramine should you give for anaphylaxis? 1mg/kg (max=50mg)
What dose of famotidine should you give for anaphylaxis? 20mg
What dose of hydrocortisone should you give for anaphylaxis? 5mg/kg (50-100mg)
What are some adjunct drugs used to treat anaphylaxis? aminophylline, albuterol inhaler, dopamine, norepi, NaBicarb
What can be done to prevent anaphylaxis? avoid risky practice, careful history taking, intradermal skin test, RAST test, leukocyte histamine release test, pharm. prophylaxis
What drugs should be given for anaphylaxis prophylaxis? Benadryl (H1), decadron, ranitidine (H2)