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35 Cards in this Set
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- Back
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diphenydramine
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1st gen H1 antagonist - reversible, competitive antagonist, mildly anticholinergic. uses: adjuvant to epi for anaphylaxis (vasoconstrict), allergy relief, sedation/sleep aid, prevent motion sickness, vertigo, nausea, and vomiting. local anesthetic, antitussive, crosses BBB and placenta (more lipid soluble so easily absorbed). Adverse effects - sedation (w/ paradoxal excitation in kids, dizzy, fatigue, tach/dysrhymias with OD, allergic rxn w/ topical use, peripheral anti-muscarinic effects. Additive w/ classic antimuscuranics as well as CNS depressants. Avoid MAOIs (MAO metabolizes H, so given together incr H
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Hydroxyzine
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1st gen H1 antagonist - reversible, competitive antagonist, mildly anticholinergic. uses: adjuvant to epi for anaphylaxis (vasoconstrict), allergy relief, sedation/sleep aid, prevent motion sickness, vertigo, nausea, and vomiting. local anesthetic, antitussive, crosses BBB and placenta (more lipid soluble so easily absorbed). Adverse effects - sedation (w/ paradoxal excitation in kids, dizzy, fatigue, tach/dysrhymias with OD, allergic rxn w/ topical use, peripheral anti-muscarinic effects. Additive w/ classic antimuscuranics as well as CNS depressants. Avoid MAOIs (MAO metabolizes H, so given together incr H
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Chlorpheniramine
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1st gen H1 antagonist - reversible, competitive antagonist, mildly anticholinergic. uses: adjuvant to epi for anaphylaxis (vasoconstrict), allergy relief, sedation/sleep aid, prevent motion sickness, vertigo, nausea, and vomiting. local anesthetic, antitussive, crosses BBB and placenta (more lipid soluble so easily absorbed). Adverse effects - sedation (w/ paradoxal excitation in kids, dizzy, fatigue, tach/dysrhymias with OD, allergic rxn w/ topical use, peripheral anti-muscarinic effects. Additive w/ classic antimuscuranics as well as CNS depressants. Avoid MAOIs (MAO metabolizes H, so given together incr H
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Cyclizine
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1st gen H1 antagonist - reversible, competitive antagonist, mildly anticholinergic. uses: (primarily for sedation) adjuvant to epi for anaphylaxis (vasoconstrict), allergy relief, sedation/sleep aid, prevent motion sickness, vertigo, nausea, and vomiting. local anesthetic, antitussive, crosses BBB and placenta (more lipid soluble so easily absorbed). Adverse effects - sedation (w/ paradoxal excitation in kids, dizzy, fatigue, tach/dysrhymias with OD, allergic rxn w/ topical use, peripheral anti-muscarinic effects. Additive w/ classic antimuscuranics as well as CNS depressants. Avoid MAOIs (MAO metabolizes H, so given together incr H
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Dimenhydrenate (Dramamine)
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1st gen H1 antagonist - reversible, competitive antagonist, mildly anticholinergic. uses: (primarily for sedation) adjuvant to epi for anaphylaxis (vasoconstrict), allergy relief, sedation/sleep aid, prevent motion sickness, vertigo, nausea, and vomiting. local anesthetic, antitussive, crosses BBB and placenta (more lipid soluble so easily absorbed). Adverse effects - sedation (w/ paradoxal excitation in kids, dizzy, fatigue, tach/dysrhymias with OD, allergic rxn w/ topical use, peripheral anti-muscarinic effects. Additive w/ classic antimuscuranics as well as CNS depressants. Avoid MAOIs (MAO metabolizes H, so given together incr H
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Meclizine
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1st gen H1 antagonist - reversible, competitive antagonist, mildly anticholinergic. uses: (primarily for sedation) adjuvant to epi for anaphylaxis (vasoconstrict), allergy relief, sedation/sleep aid, prevent motion sickness, vertigo, nausea, and vomiting. local anesthetic, antitussive, crosses BBB and placenta (more lipid soluble so easily absorbed). Adverse effects - sedation (w/ paradoxal excitation in kids, dizzy, fatigue, tach/dysrhymias with OD, allergic rxn w/ topical use, peripheral anti-muscarinic effects. Additive w/ classic antimuscuranics as well as CNS depressants. Avoid MAOIs (MAO metabolizes H, so given together incr H
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Promethazine
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1st gen H1 antagonist - reversible, competitive antagonist, mildly anticholinergic. uses: (primarily for nausea) adjuvant to epi for anaphylaxis (vasoconstrict), allergy relief, sedation/sleep aid, prevent motion sickness, vertigo, nausea, and vomiting. local anesthetic, antitussive, crosses BBB and placenta (more lipid soluble so easily absorbed). Adverse effects - sedation (w/ paradoxal excitation in kids, dizzy, fatigue, tach/dysrhymias with OD, allergic rxn w/ topical use, peripheral anti-muscarinic effects. Additive w/ classic antimuscuranics as well as CNS depressants. Avoid MAOIs (MAO metabolizes H, so given together incr H
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Acrivistine
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2nd gen H1 antagonist: useful as anti allergy due to non sedating properties. daytime drug of choice
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Fexofenadine (Allegra)
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2nd gen H1 antagonist: useful as anti allergy due to non sedating properties. daytime drug of choice. Excreted mainly in the unmetabolized form through the feces
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Loratadine (Claritin)
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2nd gen H1 antagonist: useful as anti allergy due to non sedating properties. daytime drug of choice. Excreted mainly in the unmetabolized form in the urine
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Cetirizine (Zyrtec)
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2nd gen H1 antagonist: useful as anti allergy due to non sedating properties. daytime drug of choice: Adverse Effects - more CNS actions than other 2nd gen antihistamines so not recommended for pilots. causes drowsiness. Excreted mainly in the unmetabolized form in the urine
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Desloratadine
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2nd gen H1 antagonist: useful as anti allergy due to non sedating properties. daytime drug of choic
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Cimetidine
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H2 Antagonist - GI - used to reduce gastric acid production by parietal cells of the GI tract. Used to treat GERD. Suppresses cyp450, so increases the conc of other drugs, especially Cimetidine
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Nizatidine
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H2 Antagonist - GI - used to reduce gastric acid production by parietal cells of the GI tract. Used to treat GERD. Suppresses cyp450, so increases the conc of other drugs, especially Cimetidine
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Famotadine (Pepcid)
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H2 Antagonist - GI - used to reduce gastric acid production by parietal cells of the GI tract. Used to treat GERD. Suppresses cyp450, so increases the conc of other drugs, especially Cimetidine
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Ranitidine (Zantac)
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H2 Antagonist - GI - used to reduce gastric acid production by parietal cells of the GI tract. Used to treat GERD. Suppresses cyp450, so increases the conc of other drugs, especially Cimetidine
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Cromolyn Sodium
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Mast Cell Stabilizer - doesn't work on receptors, inhibits histamine secretion, but doesn't inhibit directly. prevents the release of histamine from mast cells. used in Tx of asthma (prophylactic) and allergic rhinitis. Adverse effects include cough and bitter taste making patient compliance poor. Drug of choice for Chronic inflammation
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Nedocromil
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Mast Cell Stabilizer - doesn't work on receptors, inhibits histamine secretion, but doesn't inhibit directly. prevents the release of histamine from mast cells. used in Tx of asthma (prophylactic) and allergic rhinitis. Adverse effects include cough and bitter taste making patient compliance poor. Drug of choice for Chronic inflammation
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Histamine
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An endogenous biogenic amine which is synthesized, stored, and released from 1) Mast Cells - abundant in skin, GI tract, and reap tract and will trigger anaphylactic rxn, inflammation, and immune response. 2) Basophils - abundant in the blood. 3) Neurons - of both CNS & PNS
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H1 receptors
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Distributed in bronchial smooth muscle, intestinal smooth muscle, vascular endotheliium, cardiac tissue, and CNS
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H2 receptors
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Distributed in the vascular smooth muscle, cardiac tissue, basophils, and parietal cells
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H3 receptors
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Distributed non uniformly throughout the CNS
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H4 receptors
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Expressed within the bone marrow and white blood cells
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Pathological effects of histamine
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mild cutaneous response involves erythema, urticaria, and/or itching.
Mild to moderate Sx: skin rxn, tachy, dysrhythmias, hypotension, mild resp distress severe anaphylactic rxn: hypersensitivity rxn, hypotension, v-fib, cardiac arrest, bronchospasms, resp arrest |
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histamine vascular effects
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dilation of small blood vessels (H1 and 2 - reason for hypotension), increased permeability of post capillary venules (H1 - leads to edema)
Triple response from indradermal injection: localized red spot extending 1-2mm appearing within seconds due to vasodilation (inc blood flow), Flare (brighter red flush) develops more slowly, extending 1 cm beyond initial spot due to reflexive vasodilation, and Wheal is discernable in 1-2min at initial site of injection as a result of increased cap permeability (move of fluid and protein both ways). moves from local and propagates out. |
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Histamine cardiac effects
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increased isotropy H1 and 2
increased chronotropy H2 Decreased AV conduction H1 - leads to arrhythmias |
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Histamine Pulmonary effects
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Direct bronchoconstriction, increased mucus viscosity H1
slight bronchodilation, increased mucus secretion H2 Cough H1 |
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Histamine GI effects
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increased acid production H2 - H2 Blockers drugs of choice for peptic ulcers
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Histamine Neuronal effects
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cutaneous itching and pain H1 and 2
presynaptic inhibition of histamine synthesis and release - H3 regulation of dopamine, GABA, Ach, serotonin, and NE - H3 -CNS |
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Antibody/Antigen Immune releasers
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Food - eggs, peanuts, milk products, grains, strawberries
Drugs - penicillin, sulfa Venom - fire ants, snake bite, bee sting Foreign proteins - non-human insulin, serum proteins |
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Non-immune releasers
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Has Direct action on mast cells and releases antibodies
IV morphine or other opiods, ASA and NSAIDS in asthmatics, IV vanc (red man), X-ray contrast, succinylcholine, tubocurarine, compound 48/80, anaphylotoxins, Cold or UV |
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First generation H1 antihistamines
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Benadryl, chlorpheniramine, doxepin, hydroxyzine -
side effects most prominent, which cross BBB and cause sedation |
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2nd generation H1 antihistamines
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Levocetirizine, cetirizine, loratadine, desloratdine, fexofenadine - largely devoid of side effects b/c they do NOT penetrate CNS
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H2 receptor antagonists
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cimetidine, ranitidine - primarily are used to inhibit gastric acid secretion in the Tx of GI disorders
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Prophylaxis of allergic disorders
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Cromolyn and Nedocromil - mostly for asthmatic patients
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