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76 Cards in this Set
- Front
- Back
Histamine: what is it?
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"a biologic amine"
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Histamine: what does it do?
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- Modulation of allergic and inflammatory reactions
- Stimulation of gastric acid secretions - Neurotransmitter in the CNS - Chemotaxis of WBC? |
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Histamine: where are they synthesized/stored?
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- Mast cells
- Basophils - CNS neurons - Enterochromaffin-like cells of the stomach. |
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Histamine: synthesized from what?
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Synthesized from L-histidine by histidine decarboxylase
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What is a good way to search for a histamine secreting tumor?
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Look for metabolites of histamine:
- N-methylhistamine - N-methyl-imidazole-acetic acid - Imidazole-5-acetic acid |
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What drugs can release histamine from mast cells wtihout degranulation or mast cell injury?
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Morphine, tubocurarine - these "displace" histamine without degranulation.
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What are some substances that can cause degranulation/mast cell injury?
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- Polypeptides
- Bradykinin - Substance P - Venoms - Radiocontrast agents - ABX (vancomycin) |
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Histamine: effects on gastric secretions?
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stimulates
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Histamine: non-vascular smooth muscle?
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vasoconstricts
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Histamine: vascular beds?
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vasodilates. Low doses stimulate H1 receptors and release NO. High doses activate H2 receptors on vascular smooth muscle.
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Histamine: cardiac effects?
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Causes reflex tachycardia and H2 receptors up (???)
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Histamine: CNS effects?
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wakefulness, decreased appetite
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H2 receptors: effects on gastric mucosa?
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stimulate secretion
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H2 receptors: effects on bronchial smooth muscle?
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weak relaxation
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H2 receptors: effects on cardiac muscle?
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generalized stimulation
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Histamine: clinical uses?
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- Used for allergy skin tests.
- Used to be used for airway hyperreactivity, but it has largely been replaced by methacholine. - Used to be used for gastric secretory capacity. |
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H1 receptor blocker
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Fexofenadine (Allegra)
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H2 receptor blocker
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Cimetidine
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What is one clinically relevant function that H1 receptor blockers do not block?
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Histamine induced gastric secretion.
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c/c the three different generations of histamine blockers: sedation
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- 1st generation agents have prominent CNS sedative effects (can cross BBB)
- 2nd and 3rd generation agents are much less sedating |
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Name 7 H1 receptor blockers
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1. Chlorpheniramine (Chlor-trimeton)
2. Diphenhydramine (Benadryl) 3. Dimenhydrinate (Dramamine) 4. Promethazine (Phenergan) 5. Cyproheptadine (Periactin) 6. Hydroxyzine (Atarax, Vistaril) 7. Meclizine (Antivert) |
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Name 2 H2 receptor blockers
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1. Loratadine (Claritin)
2. Cetirizine (Zyrtec) |
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Name 2 histamine releasing drugs
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1. Morphine
2. Vancomycin |
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Name a histamine release inhibitor
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Cromolyn (Intal)
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Name 4 decongestants
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1. Phenylephrine (Neo-synephrine)
2. Pseudoephedrine (Sudafed) 3. Oxymetazole (Afrin) 4. Ipratropium (Atrovent) |
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Name 2 expectorants
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1. Guaifenesin (Mucinex, Tussin)
2. Acetylcysteine (Mucomyst) |
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Name 3 cough supressants
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1. Codeine
2. Dextromethorphan 3. Hydrocodone |
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Dimenhydramine
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Strong anticholinergic activity. Marked sedation, anti-motion sickness activity.
(Dramamine), ethanolamine |
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Diphenhydramine
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Strong anticholinergic activity. Marked sedation, anti-motion sickness activity.
(Benadryl), Ethanolamine |
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Hydroxyzine
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Undetermined anticholinergic effects. Marked sedation. Injectable used as a tranquilizer.
(Atarax), Piperazine derivative |
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Meclizine
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Very little anticholinergic activity. Slight sedation, anti-motion sickness activity.
(Bonine), Piperazine derivative |
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Chlorpheniramine
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Slight anticholinergic activity. Common component of OTC "cold" medication.
(Chlor-Trimetron), Alkylamine |
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Promethazine
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Lots of anticholinergic activity. Marked sedation, antiemetic, alpha block, D2 receptor block.
(Phenergan), Alkylamine |
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Cyproheptadine
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Slight anticholinergic activity. Moderate sedation, also has anti-serotonin activity.
(Periactin) |
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What was the problem with the first 2nd generation H2 blockers?
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They caused QT prolongation
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Some "H1 antagonists" may actually be what?
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Inverse agonists
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Antihistamines: uses
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- Treatment of acute allergies
- Treatment of allergic dermatoses - Treatment of serum sickness/allergic drug reactions - Treatment of motion sickness and vertigo (1st generation) - As sedatives (1st generation) |
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Antihistamines: AE
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- Sedation, fatigue
- Dizziness, tinnitus - Blurred vision - Dry mouth, GI distress - Weight gain - Excitation - Overdoses may lead to convulsions - especially in children! - Drug allergies may develop when these agents are applied topically. |
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Dextromethorphan
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Robatussin
NMDA receptor antagonists - PCP like effects. Inhibit brainstem cough reflex. |
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Guaifenesin
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- Reduces viscosity of respiratory secretions
- AE: nephrolithiasis, nausea |
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Acetylcysteine
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- Reduces disulfide bonds in mucus, increasing fluidity
- SE: nausea, bronchospasm, hypersensitivity. |
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What are three different types of medications that you would give to someone who is having an asthma attack?
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Bronchodilator
Oxygen Antiinflammatory corticosteroid |
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Name three "short term relievers" of contracted airways.
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1. β-agonists
2. Theophylline 3. Antimuscarinics |
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Name four anti-inflammatory "long term controllers" for asthma.
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1. Inhaled corticosteroids
2. Inhaled mast-cell stabilizers 3. Leukotriene pathway inhibitors 4. Anti-IgE MAB |
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Inhalation route: dose at target organ? Total dose amount? AE? Duration of onset? What is important about the design of inhaled drugs?
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High dose at target organ, but total dose patient takes is much lower. Lower systemic exposure = lower AE. Generally has a very rapid onset (usually 5-10 min w/ inhalation, about as good as IV!). Particle size is very important.
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Nebulization: pros and cons
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Pros: good for infants and unconscious patients.
Cons: slow, high drug dose, exact dose pt received unknown |
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Metered dose inhaler: pros and cons
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Pros: portable, dose is low, rapid onset.
Cons: need education about proper use. Sometimes need to use spacer to get uniform dosing. |
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Dry powder inhaler: pros and cons.
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Pros: No CFCs, portable, rapid
Cons: dose depends on pt's ability to take a quick and deep breath. Specific ways to use. Feels like breathing rocks. Drug can be sensitive to humidity. |
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c/c albuterol and theophylline: mechanism of bronchodilation.
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Albu
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Elevated levels of cAMP do what to the bronchi?
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Dilate
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Elevated levels of acetylcholine do what to the bronchi?
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Constrict
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Name 2 "short acting" beta 2 agonists for asthma
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Albuterol, Terbutaline
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Terbutaline
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"Short acting" beta 2 agonist (3-4) hours, used for asthma rescue. Oral, injection
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Salmetrol
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Slow onset (12-24 hrs) beta 2 selective agonist used for long term control of asthma.
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Formetrol
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Somewhat fast onset beta 2 selective agonist. Not labeled for rescue, but has faster onset than salmetrol. 25x more potent than albuterol.
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Beta 2 agonists: AE
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Tremor
Tachycardia Palpitations Dizziness Bronchoconstriction (paradoxical effect) Heartburn Hypokalemia (K+ goes into skeletal muscle?) Prolonged QT Sudden cardiac death - Black box warning (esp long-acting agonists) |
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Name 2 antimuscarinics that are used as bronchodilators
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Ipratropium bromide, Tiotropium.
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Ipratropium bromide
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Antimuscarinic, very insoluble quaternary ammonium atropine derivative. Not intended for rescue, but fairly rapid action. 2-4x daily.
AE: urinary retention, glaucoma, blurry vision |
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Tiotropium
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Antimuscarinic used for bronchodilation.
1x daily, selective M1, M3 antagonism, because dissociates from prejunctional M2 receptor faster. AE: urinary retention, glaucoma, blurry vision. |
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Name three methylxanthines that are used for bronchodilation
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1. Theophylline
2. Aminophylline 3. Caffeine |
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Theophylline
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Oral, Inhibits PDE4, adenosine antagonist (causing bronchodilation), anti-inflammatory action.
AE: Low theraputic index - must monitor plasma levels. CNS stimulation Tremor, seizure Decreased sensitivity to CO2 GERD/heartburn/nausea Muscle activity Diuresis |
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Name 3 important corticosteroids used for anti-inflammation in asthma/COPD
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1. Fluticasone, MDI, PDI
2. Budesonide, MDI, PDI 3. Trimacinolone, MDI |
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What should you do immediately after using steriod inhalers?
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Rinse your mouth!
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Inhaled corticosteroids for asthma: AE
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AE:
Candidal infections Esophagitis Vocal chord changes Glaucoma, cataracts Adrenal suppression |
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What are "leukotriene modulators used for"?
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As anti-inflammatory agents in COPD
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Name 2 Leukotriene modulators (LTD4 receptor antagonists)
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1. Montelukast (Singulair)
2. Zafirlukast |
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Montelukast
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Leukotriene modulator (LTD4 receptor antagonist)
Oral 1x daily, children above 6 years. AE: drowsiness |
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Zafirlukast
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Leukotriene modulator (LTD4 receptor antagonist)
Oral 2x daily. AE: drowsiness. |
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Name a 5-lipoxygenase inhibitor used for anti-inflammation in asthma
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Zileuton
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Zileuton
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5-lipoxygenase inhibitor. Used for anti-inflammation in asthma.
SR oral, 2x daily Not that popular, less efficacious than corticosteroids AE: liver injury (reversible if you catch it in time) |
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Name a mast cell stabilizer used for treatment of asthma
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Cromolyn.
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Cromolyn
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A mast cell stabilizer used for treatment of asthma.
Inhibit the early response to allergen change and mast cell degranulation by altering the function of a delayed chloride channel. Very effective but not rapidly acting. Used for allergic rhinitides. Inhalation. AE: throat irritation, dry mouth, cough SAE: dermatitis, myositis, gastroenteritis. |
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Name an IgE monoclonal antibody used in the treatment of asthma
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Omalizumab
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Omalizumab
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An IgE monoclonal antibody used in the treatment of asthma.
Inhibits IgE binding to mast cells. 2x week for 10 weeks. Resevered for patients with poor pulmonary function and whose asthma cannot be controlled with corticosteroids. Very expensive! |
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Beta blocker use in COPDers?
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"Usually ok" (???)
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NSAIDs: cause asthma how often? What other symptoms to they cause?
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10-15%
Sampter's triad: asthma, aspirin sensitivity, and nasal polyp (usually seen in Haitians in their 20s???) |