Pharm I Flashcards
What are some advantages to pulmonary delivery of drug?
The lung is more permeable to macromolecules and even more permeable to small molecules than the GI tract and has extremely fast onset of action
What are some disadvantages to pulmonary delivery of drug?
-inhaled corticosteroids can deposit a
significant portion of the drug dose in the oral cavity, with opportunistic infections
like candidiasis arising from diminished immune function.
Acidic powders are
also a concern for the integrity of tooth enamel.
What routes do drugs take for absorption in the lung?
para and trans-ceullar
How are lipid-soluble drugs absorbed?
They can dissolve in the lipid bilayer and are absorbed trans-cellularly
How are insoluble drugs absorbed?
para-cellularly via aqueos pores in the tight junctions
T or F. The less ionized a molecule, the faster its absorption rate
T. because it forms fewer interactions with the proteins and lipids lining the pore
What are the three major categories of disease that require treatment of the lung?
- inflammation
- infection
- cancer
What types of inflammation diseases require lung treatment?
- asthma
- COPD
- allergic rhinitis
- cystic fibrosis
What are some classes of drugs that act in the upper respiratory tract?
- mucolytics
- vasoconstrictors
- antihistamines
- drugs acting in the CNS cough center
What are some major uses of antihistamines?
- allergic rhinitis
- hay fever
What is the major use of vasoconstrictors in the URT?
permit someone to breath more easily, by
relieving nasal congestion.
What is ivacaftor?
Recently gained approval as the first in a new class of CTFR (cystic fibrosis transmembrane conductance regulator) potentiators.
What part of the ANS dominates lung function?
PNS, it provides direct innervation of smooth muscle and glandular tissue
T or F. In humans, bronchial smooth muscle has no direct neural connection from the SNS
T. SNS activity can only modulate the activity of the PNS via hetero-receptors
What other way can the SNS affect the lung?
beta-2 receptors can respond to circulating Epinephrine or to exogenous drug treatment
What classes of drugs can be used to control bronchospasm in asthma?
B2 adrenergic agonists and muscarinic anatgonists
What is the role of muscarinic M1 receptors?
They transduce vagal signal to both sub-mucosal glands and the airway smooth muscle AND increase glandular secretions in nasal mucosa
What is the role of muscarinic M2 receptors?
they are inhibitory auto receptors on the pre-synaptic membrane of PG fibers AND are found in bronchial smooth muscle where they oppose the increase in cAMP produced by B2 adrenergic stimulation
What is the role of muscarinic M3 receptors?
promotes bronchoconstriction of airway smooth muscle and mucus secretion
How do non-selective drugs, like atropine and ipratropium affect the lungs?
they non-selectively antagonize M-2 and M-3 receptors equally well
How does blockade of the M2 auto-receptors affect the release of endogenous Ach?
it increases the release, which serves to partially offset any bronchodilatory drug effects. (So the non-selective nature is not good)
How selective is Tiotropium?
it is selective for M1 and M3 receptors
T or F. Tiotropium has a longer duration of action than other muscarinic antagonists
T. But a slower onset of effect
How would anticholinergic drugs affect glandular secretions?
it dries them and potentially thickens them
