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Pharmacology -- Respiratory
Terms in this set (84)
MOA of diphenhydramine, dimenhydrinate, chlorpheniramine, loratadine, fexofenadine, desloratadine, cetrizine
Name 1st generation H1 blockers (3)
diphenhydramine, dimenhydrinate, chlorpheniramine (names containing en/ine, en/ate)
Name 2nd generation H1 blockers (4)
Loratadine, fexofenadine, desloratadine, cetrizine (name usually ends in -adine)
1st generation H1 blockers - uses
Allergy, motion sickness, sleep aid
2nd generation H1 blockers - uses
1st generation H1 blockers - toxicity
sedation, antimuscarinic, anti-alpha-adrenergic
2nd generation H1 blockers - toxicity compared to 1st generation. Why?
far less sedating than 1st generation because of decreased entry into CNS
name 1st generation H1 blocker drugs, uses, toxicity
diphenhydramine, dimenhydrinate, chlorpheniramine
- allergy, motion sickness, sleeping aid
- sedation, antimuscarinic, anti-alpha-adrenergic
name 2nd generation H1 blocker drugs, uses, toxicity
loratidine, fexofenadine, desloratadine, cetrizine
- far less sedating than 1st generation because of decreased entry into CNS
what is bronchoconstriction mediated by
- inflammatory processes
- parasympathetic tone
what are 6 types of asthma drugs
name B2 agonists
albuterol, salmeterol, formoterol
Short acting B2 agonist (1)
Long acting B2 agonist (2)
albuterol - mechanism
relaxes bronchial smooth muscle via B2 receptor
albuterol - use
use during acute exacerbation
salmeterol, formoterol - use
long-acting agents for prophylaxis
salmeterol, formoterol - adverse effects
tremor and arrhythmia
name a methylxanthine
theophyline - mechanism
- by inhibiting phosphodiesterase thereby decreasing cAMP hydrolysis.
- blocks action of adenosine
theophylline - use
narrow theraputic index (tachyarrhythmias, seizures) so limited use
Asthma drug with limited use b/c narrow therapeutic index and risk of tachyarrhythmias and seizures
Asthma drug that can cause seizures and tachyarrhythmias with toxicity
theophylline - metabolism
Muscarinic antagonists - drugs. Which one is long acting?
Corticosteroids - names
Corticosteriods - mechanism
- inhibit synthesis of almost all cytokines
- inactivate NF-kappaB the transcription factor that induces the production of TNF-alpha among other inflam agents
Corticosteriods - use
first line for chronic asthma
1st line for chronic asthma
Corticosteroids (beclomethasone, fluticasone)
Antileukotrienes - names
montelukast, zafirlukast, zileuton
montelukast, zafirlukast - mechanism and use
- block leukotriene receptors
- especially good in aspirin-induced asthma
Asthma drugs especially good for aspirin-induced asthma
zileuton - mechanism
- 5-lipoxygenase pathway inhibitor
- blocks conversion of arachidonic acid to leukotrienes
omalizumab - mechanism
- monoclonal anti-IgE antibody
- binds mostly unbound serum IgE
Omlizumab - use
- allergic asthma resistant to inhaled steroids and long-standing beta2-agonists
Asthma drugs that relax bronchial smooth muscle via B2 receptor
B2 agonists (albuterol, salmeterol, formoterol)
Asthma drugs that cause bronchodilation by inhibiting phosphodiesterase
Asthma drugs that prevent bronchoconstriction by blocking muscarinic receptors. Which one is long acting?
Tiotropium (long acting)
Asthma drugs that inactivate NF-kB and inhibit synthesis of virtually all cytokines. 1st line for chronic asthma.
Corticosteroids (beclomethasone, budesonide, fluticasone)
Asthma drugs that block leukotrienes. These are especially good for aspirin-induced asthma.
Antileukotrienes (montelukast, zafirlukast)
Asthma drug that inhibits 5-lipoxygenase pathway therefore inhibiting conversion of arachidonic acid to leukotrienes.
Asthma drug that is a monoclonal antibody to IgE. Used in allergic asthma resistant to inhaled steroids and long-acting B2-agonists.
Expectorants - names
Guaifenesin - mechanism
expectorant - thins respiratory secretions
guaifenesin - effect on cough reflex
n-acetylcysteine - mechanism
loosen mucous plug in CF patients by cleaving disulfide bonds within mucus glycoproteins
N-acetylcysteine - other uses
antidote for acetaminophen overdose
Mucolytic used in CF patients that works by cleaving disulfide bonds within mucus glycoproteins
It can also be used as an antidote for ______ toxicity
Bosentan - use
treat pulmonary arterial hypertension
Bosentan - mechanism
competetively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance
MOA is to competitively antagonize endothelin-1 receptors -> decrease pulmonary vascular resistance
Dextromethorphan - use
Dextromethorphan - mechanism
- antagonizes NMDA glutamate receptors
- synthetic codeine analog so mild opioid effect and mild abuse potential
Dextromothorphan - antidote for overdose
- for OD: naloxone
NMDA glutamate receptor antagonist used as an antitussive
Nasal decongestants - names
Nasal decongestants - mechanism
symapthomimetic alpha-agonistic nonprescription -> vasocontriction -> reduced secretions
Pseudoephedrine, phenylephrine - use
reduce hyperemia, edema, nasal congestion, open obstructed eustachian tubes
Pseudoephedrine also used to make what?
pseudoephedrine, phenylephrine - toxicity
hypertension, CNS stimulation/anxiety (pseudoephedrine)
Methacholine - mechanism and use
muscarinic receptor agonist
asthma challenge test
Muscarinic receptor agonist used in bronchial provocation challenge to help diagnose asthma
Anti-fungals that inhibit ergosterol synthesis to disrupt cell membranes, and inhibit CYP450 system
-Azole antifungals (ketoconazole, fluconazole, itraconazole, voriconazole)
Anti-fungal that is a polyene and binds ergosterol in cell membrane leading to pore formation and cell lysis
Anti-fungal that inhibits squalene-2,3-epoxidase which results in decreased synthesis of ergosterol, accumulates in skin and nails so used to treat dermatophyte infections
Anti-fungal that enters fungal cells and bind microtubules inhibiting mitosis
Anti-fungal that disrupt cell wall by blocking 1,3-beta-D-glucan synthesis
Anti-fungal that inhibits both DNA and RNA synthesis, synergistic with Amphotericin B, particularly important in treatment of cryptococcal meningitis
Anti-fungal that is a polyene and binds to ergosterol in fungal cell membrane leading to pore formation and cell lysis. It is used topically for oral thrush.
How does isoniazid induce neuropathy?
Causes vitamin B6 deficiency by increasing urinary excretion of B6 (they are structurally similar)
Anti-TB drug blocking DNA dependent RNA polymerase and can cause red urine. How does resistance develop?
Altered binding site on RNA polymerase
Anti-fungal with AE including nephrotoxicity, hypokalemia, and hypomagnesemia.
Toxic effects are due to drug binding to ______ in human cells.
Cholesterol (in human cell membranes)
When can rifampin be used as monotherapy?
Prophylaxis against meningitis for those exposed to Neisseria meningitidis
Which anti-TB drug must be metabolized to active form by mycobacterial catalase-peroxidase?
Mast cell stabilizers used for asthma (2)
What type of beta-blockers are preferred in indicated patients who also have COPD? Why?
Prevent bronchoconstriction by blocking B2 receptors
HIV patients with CD4 < 50 should be treated prophylactically to prevent what type of infection? What drug should be used?
Mycobacterium Avium Complex (MAC)
Which of the first-line TB drugs requires an acidic environment to kill TB and is thus most useful against intracellular organisms?
Pyrazinamide - "p"H is important
Anti-viral used for RSV
Smoking cessation drug that is a partial agonist of nicotinic acetylcholine receptors. It reduces withdrawal cravings while also decreasing rewarding effects of nicotine.
Anti-TB drugs with AE of optic neuritis including color blindness? What is its MOA?
Inhibits carbohydrate polymerization
Why should patients using inhaled corticosteroids rinse out their mouth after use?
Antibiotic of choice for treating lung abscesses. Why?
Covers both anaerobic AND aerobic flora
Streptomycin (second line anti-TB drug) is what type of antibiotic? Therefore, what is its MOA?
Inhibit 30s subunit of ribosome
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