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53 Cards in this Set
- Front
- Back
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Glucocorticoids induce____ (protein) which inhibits phospholipase A2.
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lipocortin
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Glucocorticoids inhibit expression of ______ cells to prevent leukocyte localization.
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endothelial (cell adhesion molecules)
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Long term systemic doses of corticosteroids can cause ______?
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iatrogenic Cushing syndrome
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PO corticosteroids are usually given for how long? inhalation corticosteroids?
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PO- short term, few days
inh- long term to minimize systemic effects |
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What are the 2 inhaled corticosteroids (ICS) that are prodrugs?
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beclomethasone dipropionate (BDP) and ciclesonide (CIC)
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Effects of structural changes in inhaled corticosteroids at:
double bond at C1-2? halogenation at C6 and/or 9? esterification at C17 or 21? |
DB - reduce MC activity
H - inc systemic effectiveness E - more lipophilic w/ inc permeability and stability |
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What are the names of the ICS?
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triamcinolone acetonide
budesonide flunisolide mometasone furoate fluticasone propionate CIC BDP |
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ADR of ICS?
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oral candidiasis, dysphonia, reflex cough, and maybe growth retardation in children
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What is the response time for ICS?
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1-2 wks and maxing after 8+ wks
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What is the most currently effective therapy for asthma control?
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combination ICS + long acting B2 agonists
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What are the name(s) of the mast cell stabilizers?
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cromolyn (intal)
nedocromil (tilade) |
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Mast cell stabilizers are useful when taken ________. What kind of response do they have?
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prophylactically
IAR |
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The early and late phase reaction to antigen challenge are inhibited and specific to lung. Which drugs are these?
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mast cell stabilizers
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5-LOX is the enzyme for what biosynthesis?
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leukotrienes
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What are the leukotriene receptors called? Most interest? and why?
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CysLT1 and CysLT2
CyLT1 bc most actions in lungs are mediated by this receptor |
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Name the leukotriene receptor antagonist drugs.
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zafirlukast (accolate)
montelukast (singular) pranlukast (not avail in US) |
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Which leukotriene has the most affinity for CysLT1?
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D4
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What is the steroid sparing effect? and which asthma drugs can do this?
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use of an agent to dec dependence on steroids to avoid ADRs
leukotriene receptor antagonists |
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What is 1 advantage of LT-modifiers?
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PO admin increases compliance
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Name a drug that is a 5-LOX inhibitor. Dose? ADRs?
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zileuton (zyflo) 600 mg BID
inc liver enzymes, substrate of CYP3A4 monitor liver function recommended |
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Name a drug that is an immune modulator. MOA? indications? administration?
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omalizumab (xolair)
anti-IgE antibody for mod-severe that isn't controlled on "standard" therapy SQ every 2-4 wks |
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PS innervates ___ and ____ muscle, ____ cells, and _______ using which NT? S?
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-cardiac and smooth muscle, gland cells and nerve terminal using ACh
-" " using NE |
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S innervates _____ glands using which NT?
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sweat glands, erector pili muslce using ACh (exception)
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S innervates ___ vascular and ____ muscle using which NT?
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renal vascular and smooth muscle using DA (exception)
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What are the co-transmitters for cholinergic synapse?
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NO and peptides
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M3 receptor can cause bronchoconstriction under which cranial nerve stimulation?
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vagal (CN X)
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What are the co-transmitters for adrenergic synapse?
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ATP and neuropeptide Y
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Methylxanthine drugs such as theophylline inhibit _____ enzyme to prolong which 2nd messenger?
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phosphodiesterase
cAMP |
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What are the 3 bronchodilators?
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B-adrenergic agonists
anticholinergics methylxanthines |
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B-adrenergic agonists are derived from _____ structure.
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catecholamines: Epi, NE, DA
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Catecholamines are metabolized by what enzymes?
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MAO and COMT
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What class of drugs is isoproterenol? What limit its ability to be effective?
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B-adrenergic agonist
both B but low alpha recep affinity, CV ADRs, short duration of action |
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T/F. If a drug is a substrate for COMT, it prolongs the duration of action.
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False. Non-catechol structures (lacking OH substituents) prolong duration of action.
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Beta-agonists as tx for asthma has improved by?
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1. B2 selective dec CV ADRs
2. inc resistance to be metabolized prolongs duration of action 3. aerosol delivery system localize tx to lungs (prevents systemic effects) |
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Explain the concepts of tolerance and "spare" receptors in inhaled B2 agonists.
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Tolerance: requires inc dose to get the same effect
SR: you have "left over" receptors that can cause an effect, i.e. you only need a small % of receptors to work to get the full effect. |
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B2 agonist + glucocorticoids can be used to _____.
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prevent downregulation of receptors due to prolonged admin of B2 agonists.
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How should SA B2 agonists be used?
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PRN only; maint for mod-severe is inappropriate.
Inc PRN usage may need re-eval of asthma tx |
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Sustained release PO B2 agonists may be used for what age group and why?
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children too young to use aerosol to prevent nocturnal asthma
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T/F. There is no evidence that B2 agonists have an effect on chronic inflammation associated with asthma.
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True.
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What forms do B2 agonist aerosols come in? hint: 3 forms
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1. MDI
2. DPI 3. sol. for nebulizer |
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What are the indications for SAB2 agonists?
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acute asthma sx and prophylaxis of exercise induced bronchospasm
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List the SAB2 agonists and the LAB2 agonists.
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SA - albuterol (ventolin), levalbuterol (xopenex), pirbuterol (maxair)
LA - salmeterol (serevent), formoterol (foradil) |
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What enantiomer is albuterol? levalbuterol?
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A - R/S
L - R |
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LAB2 agonists work for ___ hrs or more due to their high ____ _____ rather than ____ to ____.
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12
lipid solubility resistance to metabolism |
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Compare/contrast salmeterol and formoterol?
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sal onset of action >30 min and not good for acute attack; formo onset of action ~5 min
Both can be used for EIB if given in correct time interval before exercise. |
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ADRs of B2 agonists.
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(Sympathomimetic - fight/flight rxns)
CV: tachycardia, palpitation Neuromuscular: tremor, muscle cramping Metabolic: hyperglycemia in diabetics |
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What are some drugs that interact with B agonists?
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1. BB dec eff
2. anticholinergics inc therapeutic eff 3. MAO-I, TCA, sympathomimetic agents inc toxicity |
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Terminology of anticholinergics:
Quaternary, Alkaloids, Indirect and Direct Acting, Depolarizing blockade. |
Q: direct agonist, don't pass BBB, +charge on N
A: natural organic base, most are pharm. active I: stimulation not by agonist activity D: true agonist DB: sys refrac period after prolonged agonist stimulation of receptor |
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What is the difference between anticholinergic vs. B2 agonists when used as bronchodilators?
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AC requires vagal tone whereas B2 ag is a direct stimuli not dependent on tone.
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Name 2 useful asthma drugs that are anticholinergic. What are their differences?
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ipratropium and tiotropium: quaternary
-ipra is more selective and tio has a longer duration of action |
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Why is atropine not a therapeutically useful bronchodilator?
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too many systemic and CNS effects
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Which anticholinergic + B2 agonist has additive effects? Brand name?
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ipratropium/albuterol (Combivent)
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What are 3 proposed MOA of theophylline as a bronchodilator?
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1. non-selective PDE inhibitor (PDE III)
2. blockade of adenosine receptor 3. anti-inflammatory action |
