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27 Cards in this Set

  • Front
  • Back
What is Asthma?
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)
What is COPD?
Chronic obstruction in expiratory airflow that may be accompanied by airway hyper-responsiveness and may be partially reversible
- includes asthma, emphysema and chronic bronchitis
What is emphysema?
abnormal, permanent enlargement of airspaces distal to the terminal bronchioles with destruction of walls
What is chronic bronchitis?
persistent cough and sputum production for most days out of 3 months, in at least 2 consecutive years
What is the pharmacological approach to treating asthma?
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)
What are the advantages to inhalation?
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
Muscarinic antagonists in asthma do what? beta agonists?
- inhibit bronchoconstriction

- encourage bronchodilatoin
Albuterol (Proventil®, Ventolin®)
- 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
What are long acting beta agonists used for?
- in asthma, used to limit the need for corticosteroid treatment, since corticosteroids have so many more side effects
How do corticosteroids work?
- they reduce the cellular production of inflammatory mediators
- this decreases the underlying inflammation in asthma
Triamcinolone (Azmacort®)
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
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
What are antihystamines used for?
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!!
What are the side effects of antihystamines?
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
Abnormally high LVEF (3)
IHSS and hypertrophic CM
hyperthyroidism
regurg (AI/MR/VSD)
What are immunosuppressants used for?
* 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
What are the drug classes of immunsuppressants?
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
Corticosteroids
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)
Hydrocortisone (Cortef®, SoluCortef®)
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;
Cyclosporine (Sandimmune®, GenGraf®, Neoral®)
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
talk about the bioavailability and dose of Cyclosporine.
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)
Tacrolimus (ProGraf®)
- 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
What are COX inhibitors and what are their therapeutic effects?
+ 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)
Aspirin
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
Ibuprofen (Motrin®, Advil®, others)
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®)
Celecoxib (Celebrex®)
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)
List the 3 types of anti-arthritic agents.
o DMARDS
o NSAIDs
o Corticosteroids