farmaka Flashcards
Are H1 blockers reversible or irreversible inhibitors?
Reversible
What are three first-generation H1 blockers?
Diphenhydramine, dimenhydrinate, and chlorpheniramine
Name four second-generation H1 blockers.
Loratadine, fexofenadine, cetirizine, and desloratadine
First-generation H1blockers usually end in ____, whereas second-generation H1blockers usually end in ____.
-en/-ine or -en/-ate, -adine
A patient has motion sickness on a flight and would like to fall asleep. What class of medication would be useful for this patient?
H1 blockers (e.g., diphenhydramine), which are useful for allergies, motion sickness, and as sleep aids
A patient takes chlorpheniramine for allergies. What side effects would you counsel the patient on?
Sedation, antimuscarinic symptoms, anti-α-adrenergic symptoms
What is the clinical use of second-generation H1 blockers?
Allergies
A truck driver has bad allergies. You want to prescribe a histamine blocker. Would diphenhydramine work for him?
No (although it treats allergies, it makes him too sleepy [second-generation H1-blockers are less sedating due to lower CNS activity])
How does guaifenesin help a patient with a severe cough productive of sputum?
It thins respiratory secretions, but it does not reduce the cough reflex
N-acetylcysteine is an expectorant. How does it work?
Dissolves mucous plugs by disrupting disulfide bonds (it is a mucolytic)
A patient with cystic fibrosis is prescribed a medication that would loosen mucous plugs. What is the mechanism of action of this drug?
Disrupts disulfide bonds (N-acetylcysteine is a mucolytic)
Which mucolytic is also used as an antidote for acetaminophen overdose?
N-acetylcysteine
By what mechanism does dextromethorphan suppress cough?
It antagonizes NMDA glutamate receptors
Dextromethorphan is a synthetic analog of what drug?
Codeine
Excess use of dextromethorphan can produce what side effect?
Mild opioid effect
A patient with a cough overdoses on an NMDA glutamate receptor antagonist. What drug can be used to treat the overdose?
Naloxone (dextromethorphan can cause opioid-like effects)
Why does dextromethorphan have mild abuse potential?
If used in excess, it has a mild opioid effect
A patient with depression takes a medication to suppress cough. She quickly becomes tachycardic & sweaty, & her fingers tremble. Diagnosis?
This is serotonin syndrome, seen when dextromethorphan is combined with another serotonergic agent such as certain antidepressants
What is the main clinical function of pseudoephedrine and phenylephrine? By what mechanism?
Nasal decongestants via α-adrenergic agonism
What are the clinical indications for pseudoephedrine and phenylephrine?
Reduce hyperemia, edema, nasal congestion; open obstructed eustachian tubes; and act as stimulant (pseudoephedrine only, used to make meth)
A patient takes α-adrenergic agonists for nasal congestion. What side effects can be expected?
Can cause hypertension and central nervous system stimulation/anxiety
Name the three types of drugs that are used for pulmonary hypertension.
Endothelin receptor antagonists, prostacyclin analogs, and PDE5 inhibitors
Name a competitive endothelin receptor antagonist that is used to decrease pulmonary vascular resistance for pulmonary hypertension.
Bosentan
A patient with COPD has a pulmonary artery pressure of 26 mmHg. He is prescribed an endothelin receptor antagonist. What must you monitor?
Monitor LFTs for hepatotoxic side effects (this patient has pulmonary hypertension from COPD, and the medication described is bosentan)
What is the mechanism of action of sildenafil?
Inhibits cGMP PDE5 and prolongs nitric oxide vasodilatory effects
A man with pulmonary hypertension and erectile dysfunction would benefit from which medication?
Sildenafil
Name two prostacyclin analog medications that directly vasodilate pulmonary and systemic vascular beds for pulmonary hypertension.
Epoprostenol and iloprost
A man with elevated pulmonary artery pressure is given a PGI2 analog that also works to inhibit platelet aggregation. Side effects?
Flushing and jaw pain (he has pulmonary artery hypertension, and the medication described is epoprostenol or iloprost)
Bronchoconstriction is mediated by which two processes?
Inflammation and parasympathetic tone (these are targets for therapy)
What is the mechanism of action of albuterol?
Albuterol relaxes bronchial smooth muscle through its agonism of β2-adrenergic receptors
A typical patient with asthma takes a combination of drugs that targets which two pathways mediating bronchoconstriction?
Inflammation and parasympathetic tone
Is albuterol used as a controller medication or for relief of symptoms during exacerbations?
Relief in acute asthma exacerbations
Salmeterol and formoterol are ____ (short/intermediate/long)-acting agents. What class of drugs are they?
Long; β2-agonist
List two adverse effects that a patient may experience while taking salmeterol.
Tremor and arrhythmias
Name two inhaled corticosteroids commonly used to treat asthma.
Fluticasone and budesonide
What mechanism of inhaled corticosteroids makes them useful to treat asthma?
They inhibit the synthesis of virtually all cytokines
Inhaled corticosteroids are useful in treating asthma by inactivating what transcription factor?
Nuclear factor κB
Nuclear factor κB induces the production of inflammatory agents including ____.
Tumor necrosis factor-α
A patient has chronic asthma. What class of drugs is considered first-line therapy for this patient?
Inhaled corticosteroids
Ipratropium is an example of what class of drugs?
Muscarinic antagonists
Does ipratropium cause a competitive or a noncompetitive receptor blockade? Mechanism?
Competitive; prevents endogenous acetylcholine from inducing bronchoconstriction
Ipratropium is used to treat chronic obstructive pulmonary disease, as is what other long-acting muscarinic antagonist?
Tiotropium
Name two clinical indications for the use of ipratropium.
Asthma and chronic obstructive pulmonary disease
A patient has both asthma and COPD. What is the mechanism of action of the drug that would be useful against both of his conditions?
Ipratropium is used against both, as it blocks muscarinic receptors competitively
Name three examples of antileukotriene drugs.
Zileuton, zafirlukast, and montelukast
Zileuton is an inhibitor of what pathway? Toxicity?
The 5-lipoxygenase pathway that produces leukotrienes from arachidonic acid; it is hepatotoxic
What medication is used for allergic asthma resistant to inhaled corticosteroids and β2-agonists? Its mechanism of action?
Omalizumab, a monoclonal anti-immunoglobulin E antibody that binds unbound immunoglobulin E and blocks FcεRI binding
Theophylline likely causes ____ by inhibiting phosphodiesterase and increasing what molecule?
Bronchodilation; cAMP
What is the effect on bronchial smooth muscle of increased cAMP concentration?
Decreased bronchial tone (i.e., it causes bronchodilation)
The use of what asthma drug is limited because of its narrow therapeutic index?
Theophylline, a methylxanthine
A patient wants to try theophylline but is worried about side effects. What two side effects do you counsel the patient on?
Cardiotoxicity and neurotoxicity
In addition to inhibiting phosphodiesterase, theophylline also blocks endogenous ____ from inducing bronchoconstriction.
Adenosine
In the pathogenesis of asthma, the binding of antigens to immunoglobulin E on mast cells results in what?
The release of mediators such as leukotrienes and histamine from mast cells
In the pathogenesis of asthma, the release of mediators from mast cells results in what two responses?
Bronchoconstriction (early) and inflammation (late)
In asthma, the early response to the release of mediators is ____, whereas the late response to the release of mediators is ____.
Bronchoconstriction; inflammation
In the treatment of asthma, what drug type prevents released mast cell mediators from inducing the late response of airway inflammation?
Steroids
What is the primary function of methacholine? By what mechanism does it work?
Bronchoconstriction via muscarinic (M3) receptor agonism
A physician cannot tell if a patient has asthma. What drug could be used in an asthma challenge test for this patient?
Methacholine
