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27 Cards in this Set
- Front
- Back
What is Asthma?
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o Chronic inflammatory disorder of the airways with variable, and reversible obstruction
o Characterized by recurrent episodes of wheezing, breathlessness, cough, chest tightness – especially at night or early morning o Increased bronchial hyper-responsiveness to a variety of stimuli (exogenous, endogenous) |
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What is COPD?
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Chronic obstruction in expiratory airflow that may be accompanied by airway hyper-responsiveness and may be partially reversible
- includes asthma, emphysema and chronic bronchitis |
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What is emphysema?
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abnormal, permanent enlargement of airspaces distal to the terminal bronchioles with destruction of walls
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What is chronic bronchitis?
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persistent cough and sputum production for most days out of 3 months, in at least 2 consecutive years
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What is the pharmacological approach to treating asthma?
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Quick Relief: Beta 2-Agonists (albuterol), Anticholinergics (ipratropium)
Long-term Control: Corticosteroids, Leukotriene modifiers, Long-acting Beta 2-agonists, Theophylline, Mast cell stabilizers, Antibody Bronchodilation: Beta 2-Agonists (albuterol), Anticholinergics (ipratropium), Methylxanthines (theophylline) Anti-Inflammation: Antibody (omalizumab), Corticosteroids (beclomethasone), Mast cell stabilizers (cromolyn), Leukotriene modifiers (montelukast) |
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What are the advantages to inhalation?
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o Advantages – direct delivery to site of action, limited systemic effects, rapid relief possible
o Devices – MDIs, DPIs, nebulizer - a lot gets absorbed before it gets to the systemic level - has to get past the mouth and into the lungs, then has to get through the mucus, then has to get into the circulation, and then into the cells |
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Muscarinic antagonists in asthma do what? beta agonists?
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- inhibit bronchoconstriction
- encourage bronchodilatoin |
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Albuterol (Proventil®, Ventolin®)
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- prototype for short acting Beta agonists
Indication – reversible airway obstruction (asthma) MOA - 2 agonist at bronchial smooth muscle Dose – MDI (90 g/puff) 2 puffs q4-6h prn Neb 2.5 mg q4-6h prn Onset/Peak/Duration - < 2 min, ~30 min, 3-5 h Adverse effects – tachycardia, tremor, chest pain |
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What are long acting beta agonists used for?
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- in asthma, used to limit the need for corticosteroid treatment, since corticosteroids have so many more side effects
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How do corticosteroids work?
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- they reduce the cellular production of inflammatory mediators
- this decreases the underlying inflammation in asthma |
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Triamcinolone (Azmacort®)
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Indication – reversible airway obstruction (asthma)
MOA – decreased mediator synthesis, release, and infiltration of inflammatory cells Dose – MDI (100 g/puff) 4+ puffs daily Onset/Peak/Duration - < 2 min, ~30 min, 3-5 h Adverse effects – (limited via inhalation) oropharyngeal candidiasis, dysphonia, some adrenal suppression, some bone loss, cataract and glaucoma possible - NOT for acute wheezing!!! corticosteroids take 1-2 weeks before max anti-inflammatory effect |
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What does Histamine do in the body?
- use this to imply what effects antihistamines would have |
binds to histamine receptors:
o H1 CNS (neurotransmitter), blood vessels (vasodilation, capillary permeability), lungs (bronchoconstriction), skin (itching, pain) o H2 stomach (HCl acid secretion) * Associated with allergic reactions & upper GI disorders o Involves mast cell synthesis and release o Mild allergy - rhinitis, itching, local edema o Severe allergy - bronchoconstriction, hypotension, anaphylaxis - 1st time, allergen binds to a mast cell and it makes histamine inside itself; second time allergen comes, mast cell releases a ton of histamine |
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What are antihystamines used for?
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o Refers to H1-receptor antagonists
o Used for mild allergic symptoms, motion sickness and insomnia o Therapeutic effects similar, but side effects vary with agent - take the antihistamine drug BEFORE the release of histamine!! |
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What are the side effects of antihystamines?
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o 1st Generation – sedating (D, P > others), anticholinergic (clemastine, D, P > others), other (confusion, incoordination, paradoxical excitation)
o 2nd Generation – non-sedating, less adverse effects |
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Abnormally high LVEF (3)
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IHSS and hypertrophic CM
hyperthyroidism regurg (AI/MR/VSD) |
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What are immunosuppressants used for?
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* Used to limit or inhibit the immune response – treatment of auto-immune disease, prevention of transplant rejection
* Expect a down side – risk of infection, risk of malignancy |
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What are the drug classes of immunsuppressants?
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o Corticosteroids – prednisone, methylprednisolone
o Antiproliferatives (cytotoxics) – azathioprine, methotrexate, mycophenolate o Calcineurin inhibitors – cyclosporine, tacrolimus o Rapamycin derivatives – sirolimus o Antibodies (monoclonal; polyclonal) – basiliximab, daclizumab, muromonab |
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Corticosteroids
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MOA – inhibit mediator synthesis, suppress phagocyte infiltration, suppress lymphocyte proliferation
Absorption – PO > IM > Intra-articular DOA – dependent on dose, route, solubility Elimination – hepatic > other sites, renal excretion of inactives Adverse effects – (esp with long-term systemic use) adrenal suppression, infection, glucose intolerance, fat redistribution, myopathy, FEAB, osteoporosis, slow growth, cataracts, glaucoma, GI ulceration, perforation; avoid with live virus vaccine, systemic fungal infection; caution pregnancy, lactation, pediatric, and others; interaction digoxin, diuretics, NSAIDs, vaccines * Physiologic Effects – metabolic (gluconeogenesis, lipolysis), other (increased RBCs and PMNs) * Pharmacologic Effects – anti-inflammatory, immunosuppression, metabolic (hyperglycemia, Na-water retention, K excretion, decreased Ca absorption) |
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Hydrocortisone (Cortef®, SoluCortef®)
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Indication – adrenocortical insufficiency, other uses
Mechanism – glucocorticoid > mineralocorticoid Dose – 10-15 mg/m2 bid; 50-100 mg IV Onset/Duration – hours Adverse effects – adrenal suppression, hypokalemia; |
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Cyclosporine (Sandimmune®, GenGraf®, Neoral®)
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Indication – immunosuppression s/p transplantation
Mechanism – binds cyclophilin, then inhibits calcineurin required for IL-2 production and T-cell proliferation Dose – (depends on formulation, organ, other meds) Distribution – binds RBC > WBC and lipoproteins Elimination – hepatic metabolism, biliary excretion Adverse effects – infection risk, nephrotoxicity, hypertension, tremor, hirsutism, hepatotoxicity; avoid in pregnancy/lactation; interaction enzyme inducers and inhibitors, nephrotoxins - a calcineurin inhibitor |
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talk about the bioavailability and dose of Cyclosporine.
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Bioavailability varies with the formulation:
GenGraf and Neoral > Sandimmune Dose varies with transplant or disorder: Sandimmune LD: 15 mg/kg daily x 1-2 weeks MD: ~3-10 mg/kg/d (IV 5 mg/kg over 2-6 h) Neoral MD: 7-9 mg/kg/d (transplantation) MD: 2-4 mg/kg/d (rheumatoid arthritis) Monitor cyclosporine levels (whole bld, trough) |
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Tacrolimus (ProGraf®)
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- a calcineurin inhibitor (prevents T cells from secreting interleukin 2)
Indication – immunosuppression s/p transplantation Mechanism – binds FKBP12, then inhibits calcineurin required for IL-2 production and T-cell proliferation Dose – 75-150 g/kg q12h (50-100 g/kg/d IV by continuous infusion) Elimination – hepatic metabolism, biliary excretion Adverse effects – infection risk, nephrotoxicity, neurotoxicity, NVD, hypertension, hyperglycemia; avoid in pregnancy/lactation; interaction enzyme inhibitors - more risk of diarhea with this drug - can cause hyperkalemia and hypomagnesimia - even MORE than cyclosporin does = BAD |
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What are COX inhibitors and what are their therapeutic effects?
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+ Non-selective agents (e.g., aspirin, ibuprofen)
+ Selective agents (e.g., celecoxib) o Therapeutic effects + Pain relief (mild-moderate; dysmenorrhea) + Fever reduction + Anti-inflammation (arthritis) |
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Aspirin
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Indication – pain associated with inflammation
Mechanism – inhibits cyclo-oxygenase (COX) Dose – Acute pain, fever 650 mg q6h CVD prevention 80-160 mg daily Arthritis 1-1.25 g qid Onset/duration – within 60 min / 4-6 h Elimination – hepatic metab, then renal excretion Adverse effects – GI distress, tinnitus, altered hemostasis, renal dysfunction; avoid if allergic; interaction warfarin, corticosteroids, ethanol |
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Ibuprofen (Motrin®, Advil®, others)
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Indication – pain associated with inflammation
Mechanism – inhibits cyclo-oxygenase Dose – Acute pain, fever 400 mg q4h (5-10 mg/kg) Dysmenorrhea 400 mg q4-6h Arthritis 400-800 mg tid-qid Onset/duration – within 60 min / 4-6 h Elimination – hepatic, then renal Adverse effects – GI distress, tinnitus, renal dysfunction; avoid if allergic Celecoxib (Celebrex®) |
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Celecoxib (Celebrex®)
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Indication – acute pain, dysmenorrhea, arthritis
Mechanism – selectively inhibits COX-2 - (it's really good not to inhibit COX-1 because that reduces the side effects, esp GI a lot) Dose – Acute pain 400 mg x 1, then 200 mg bid Arthritis 100-200 mg bid Elimination – hepatic metabolism, renal excretion Adverse effects – dyspesia, abdominal pain; avoid if allergic; interaction warfarin, lithium; may be associated with increased cardiac risk (MI, thrombosis) - may be associated with increased cardiac risk (MI thrombosis) |
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List the 3 types of anti-arthritic agents.
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o DMARDS
o NSAIDs o Corticosteroids |