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74 Cards in this Set
- Front
- Back
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What are the types of histamine blockers?
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H1 blockers (1/2 generation)
H2 blockers |
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What 2 serotonin receptors do we use agonists for? antagonists?
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5-HT1 and 5-HT4
5-HT2 and 5-HT3 |
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___ is found in neurons, mast cells and is metabolized by monoamine oxidase.
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histamine
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Diphenhydramine?
Sumatriptan? |
First Generation H1
5-HT |
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Loratadine
dimenhydranate chlorpheniramine desloratadine |
2nd gen HI
1st gen H1 1st gen H1 2nd gen H1 |
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Fexofenadine and cetirizine?
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2nd gen H1
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Promethazine and hydroxyzine?
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1st gen H1
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The 4 places that histamine is stored/released?
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GI mucosa, CNS, mast cells, basophils
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What immunoglobulin triggers histamine release from mast cells?
What 3 drugs induce histamine release? |
IgE
Morphine, penicillin, vancomycin |
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What effect does histamine have on the Airway, GI, and Blood Vessels?
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Bronchoconstriction mainly
Acid secretion D/V VD/ increased vascular permability |
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Bronchoconstriction, Intestinal cramps, VD, edema, pain, itching?
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H1 receptor on SMOOTH MUSCLE
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Controls gastric acid secretion and stimulates cardiac muscle?
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H2 receptor
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Where are H3 and H4 receptors found?
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CNS
Immune system (eosinophils) |
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used to be used for testing of bronchial hyperactivity and testing gastric acid secretion, but NO LONGER used?
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histamine - we mainly used anti-histamines
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Histamine has opposite effects on smooth muscle than ___ which is used in life saving anaphylaxis?
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epi
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___ is useful in asthma prophylaxis (blocks degranulation of mast cells)
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cromolyn
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which H1 receptor is More lipophilic? 1st of 2nd generation?
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1st is more lipophilic
2nd is less lipophilic |
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Can be used as anti-emetic, parkinson's disease, type-1-hypersensitivity, allergic dermatoses?
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H1 receptor antagonists
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Can be used for antiparkinsonism (suppresses extrapyramidal symptoms associated with antipsychotic drugs)
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dephenhydramine (H1 1st gen)
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used to reduce allergic rxns and is very sedating?
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diphenhydramine (h1 1st gen)
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What drug can potentiate CNS depressants like opiates so you actually need less optiods?
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diphenhydramine (h1 1st gen)
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Used exclusively for prevention of motion sickness? It's salt anyways
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dimenhydranate (dramamine) 1st Gen h1
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a drug that is a potent local anesthetic, sedation, and anti-emetic. also weak dopamine antagonist?
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promethazine (H1 1st gen)
that is phenergan |
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SE include neuroleptic malignant syndrome; produces alpha-blockage; orthostatic HypoTension; tachy; dizz
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Promethazine (h1 1st gen)
it is phenergan |
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used mainly to treat general anxiety and reduce alcohol withdrawl?
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hydroxyzine (1st gen H1)
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What the major difference between H1 1st and 2nd gen antagonists?
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2nd generation has much less sedation effects
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Are 1st or 2nd generation antihistamines more selective for H1 receptors?
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2nd generations are - thats why less sedation b/c don't go to brain
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What drug has double the half-life of the 2nd gen H1 Loratadine (clairitin)?
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desloratadine (clarinex)
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Again where do H1 and H2 act?
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H1 = smooth muscle and CNS
H2 = gastric mucosa and cardiac stimulant |
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H2 receptors mainly act on ___ and have few side effects except what drug?
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GI mucosa (blocks g-acid)
cimetidine |
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Bulimia, panic, OCD, and depression would be associated with?
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decreased serotonin levels (5-HT)
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The 5-HT1 agonists end in " ----"
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tryptans
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DOC for acute migraine?
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sumatriptan - 5HT1 agonist
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inhibit vomiting reflex from chemo?
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ondansetron (5HT3) are the setrons
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i'm assuming i'm a trip if i don't my medication for my migraine?
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sumatriptan
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used for chronic constipation and is 5HT4 agonist but restricted use d/t CV toxicity?
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Tegaserod
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Ergot alkaloids are from wet/spoiled grains and responsible for ____?
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st. anthony's fire
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ergot alkaloids are partial ___ and ___ agonists?
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alpha and 5-HT (serotonin)
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an OD can cause ischemia and gangrene; causes VC
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ergotamine
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powerful uterine contraction and can cause abortion/miscarriage (ergot)
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ergonovine
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main stay for migraine treatment besides sumatriptan?
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ergotamine
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used in hyperprolactinemia to reduce prolactin secretion?
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bromocriptine
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nitropurusside can be used as an antagonist to what drug class?
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ergots
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What is one of the main effects of serotonin?
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bronchospasm
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most useful in treatment of carcinoid tumors?
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Sumatriptan
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what drug can reverse 1 or more smooth muscle effects of circulating histamine?
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Epinephrine
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many H1 blockers have nonhistamine effects including?
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anti-motion sickness effects
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if you block H2 receptors what happens to cAMP in the heart?
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decreases
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toxicities of H2 antihistamines include:
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p450 inhibition
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what drug is used to treat chemo induced vomiting?
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ondansetron
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cetirizine is used for? H1 2nd gen
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hay fever
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which drug is used to treat hyperprolactinemia?
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bromocriptine
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which drugs are used to treat peptic ulcers?
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cimetidine - H2 blocker
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cetrizine is used for __ and is a __
cimetidine is a ___ and used for __ |
2nd Gen H1 - hay fever
H2 - Peptic ulcers |
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what drug is used for migraines and is not fungus derived?
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sumatriptan - 5HT1
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what drug is used to reverse ergot induced vasospasm?
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nitroprusside
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what effect do theophylline, nitro, isoproterenol, and histamine have in common?
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Tachycardia
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does albuterol have a diuretic effect?
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NO
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does nedocromil or cromolyn have direct bronchodilator effects?
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no they are only prophylactic
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what does not play a role in asthma? histamine, leukotriene, antigens, PLA2
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histamine
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Theophylline is a bronchodilator active by the ___ route
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oral
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what drug is life saving in status asthmaticus and inhibits PLA2
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prednisone
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what asthmatic drug has OD toxicity that includes insomnia, arrhythmias, and convulsions?
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aminophylline
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anti IgE antibody keeps IgE from binding to mast cells; reduces frequency and severity of asthma exacerbations.
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omalizumab
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stabilizes mast cell and inhibits degranulation? NO use in acute attacks and is DOC for asthma in children
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cromolyn
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ADR is inhibition of P450; used for prophylactic asthma in children; reversible inhibitor of leukotriene receptors
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lukasts (montelukast and zifurlukast)
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inhibits 5-lipooxygenase but is extremely hepatotoxic?
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zileuton
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methylxanthine derivative inhibits phosphodiesterase leading to increased cAMP
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theophylline
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muscarinic receptor antagonist (m2/m3) used in asthma + COPD
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ipratropium
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stabilize mast cell and inhibit degranulation; increase mucociliary clearance; NO anti-inflammatory properties so not used for monotherapy in asthma?
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beta2 agonists
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___ do not effect bronchodilation, they work by decreasing inflammatory cascade; They also inhibit ___
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corticosteroids; PLA2
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budesonide; beclomethasone, fluticasone
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corticosteroid used in asthma
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most effective for cough?
most widely used for cough? |
opiods
non-opiods (DXM) |
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a non-narcotic antitussive derivative of procaine used to anesthetize the stretch receptors
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benzonatate
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