Anti-Asthmatic Drugs Flashcards
What are the muscarinic antagonists used for asthma?
It is ipratropium, tiotropium, aclidinium, Umeclinidium
tropium ones are for Asthma+ COPD
What are the mediator release inhibitors?
Cromolyn and Nedocromolyn
What is the methyl xanthine medication used for asthma and what is its general mechanism?
Theophylline (PDE3 and PDE 4 inhibitor)
Anti-leukotriene agents are:
Zileuton, Zafirlukast, and Montelukast
What is anti-IgE antibody used for asthma?
Omalizumab
What is cetirizine used for?
non-FDA, seasonal rhinitis, seasonal allergic asthma
Roflumilast is a —-
PDE4 inhibitor
What are the IL-5 MAB?
IL-4 receptor MAB?
Reslizumab, Mepolizumab, Benralizumab
Dupilumab
For beta adrenergic agonists, what is important to keep note?
Whether long acting or short acting
What is the drug combination used for short acting acute management of tolerant asthma?
It is albuterol + ipratropium
SABA + SAMA
What are the long acting asthma management combination?
They are Umeclinidium+ Vilanterol (LAMA+LABA)
What is the LABA+ ICS combinations used to treat asthma?
They are Salmeterol + Fluticasone
Vilanterol+ Fluticasone
Formoterol+ Budenoside
What is the ULABA+LAMA combination used to treat asthma?
It is Olodetarol-Tiotropium
What is PDE? Function?
It is phosphodiesterase, and it is an enzyme that breaks down the second messenger cAMP to AMP
Mechanism of bronchial relaxation is what?
ATP –> cAMP via AC causes there to be relaxation.
Beta agonists do what? Theophylline does what?
Beta agonists activate AC, theophylline inhibits PDE4
What are the 3 factors that can increase broncho-constriction?
They are leukotrienes, Acetyl choline, and Adenosine
Epinephrine usage has what drawback?
it’s use should be limited for the lung (so you shouldn’t over dose it)
Why are sympathomimetics inhalational?
In order to reach mainly lung rather than other area.
Sympathomimetics clinical application is:
relaxation of bronchial smooth muscle, dialting airways, Airway diameter is the most important determinant.
They also facilitate mucociliary transport of secretions and thereby promote expectoration
What is the major structural difference between long acting and short acting agent?
They are more lipophilic.
Why are corticosteroid co-administered with LABAs?
In order to re-sensitize Beta-agonist receptors
What do Beta 2 agonistic drugs do?
They induce skeletal muscle tremor
Excessive use–> tachycardia, arrhythmias, loss of responsiveness to the drug
Corticosteroids are believed to restore the sensitivity
Albuterol and Terbutaline is NOT metabolized by
COMT
What does epinephrine target?
Alpha 1 and Alpha 2
What for corticosteroid do?
Corticosteroid inhibit synthesis of leukotrienes, prostaglandins, and thomboxanes–> reductions in brochial smooth muscle contraction, vascular permeability
What are side effects of inhalational corticosteroids?
Can change microflora of oropharygeal area causing candidiasis.
Anticholinergic Bronchodilator sprays are used how?
Nasal spray and oral inhalational
What is the MOA of ipratropium?
It is a synthetic quaternary anti-muscarinic agent and is a competitive antagonist at muscarinic cholinergic receptors
Decreases cGMP formation and decreases contractility of SM due to actions on Ca++.
Maintains basal tone.
What is the adverse effects of Ipratropium?
Xerostemia
What type of patients is ipratropium apt for?
COPD patients with psychogenic exacerbations
Tiotropium is used for?
COPD and Asthma .
Maintanance treatment of bronchospasm associated with COPD.
M3 receptor system is the major target
What is Aclinidium Bromide is used for what?
It is used for COPD, chronic bronchitis, and emphysema. M3 receptor antagonist.
What is the methyl xanthine name that is given injection?
It is Aminophyllin
What does PDE3 va PDE 4 function?
PDE3: bronchodilator
PDE4: anti-inflammatory
What are side effects of theophylline?
CNS: headache, anxiety restlessness
GI: nausea, diarrhea, vomiting, GI reflux
Cardiac: Large overdoses lethal. SVT, VT
Renal: Diuresis
What is the dose for theophyllin use?
Aminophyllin: is basically 250 mg/10 ml used for acute exacerbations. FDA no longer includes acute bronchospasm as an indication.
Inhibitors of mast cell degranulation are:
Crosmolyn sodium.
No bronchodialator activity, but is a non-prescription nasal solution for allergic rhinitis
Crosmolyn works how?
It inhibits mast cell degranulation by inhibiting IgE antibody-antigen induces Ca++ influx. Prevents the release of histamine. Ineffective for use of acute attack.
Nedocromil is more potent thatn Cromolyn sodium.
Used in Asthma for children.
Leukotriene Antagonists and Lipoxygenase Inhibitors ae given through which MOA? What are some names? They are not used for —- management.
They are given Orally.
Zileuton, Zafitleukast, Monteleukast
Acute
Zileuton has significant effect in —— processes.
CYP related metabolism
Zafirleukast inhibits the activity of ———. What is the alternative name?
Cytochrome Isoenzymes CYP3A4 and CYP2C9. Accolate
Monteleukast inhibits —– to what extent compared to Zafirleukast?
CYP2C9 and CYP3A4 to a much lesser extent
Monteleukast inhibits what?
They inhibit Leukotriene D4 and CysLT1, found in the human airway. Leukotrienes re released via mast cells and eosinophils.
Aspirin irreversibly acetylates
Cyclo-oxygenase enyzyme
Aspirin induced asthma can be prevented with ?
Monteleukast
What can Montelukast cause?
It can cause vasculitis due to systemic eosinophilia
Omalizumab is used for
IgE asthma/ allergic asthma , and is a monoclonal antibody that binds to IgE. late phase of allergic response is prevented.
Omalizumab is given
subcutaneously
What does Roflumilast help with?
Roflumilast is for treatment of COPD and asthma
Bronchodilator: PDE3 inhibition
Anti-inflammatory: PDE-4 inhibition
Magnesium Sulfate is given how, for what?
IV, to inhibit smooth muscle contraction
