Pharmacology of Allergy and pulmonary drugs Flashcards
What are the 3 main symptoms of asthma or COPD
Bronchoconstruction, inflammation, mucus
What is the MOA for beta-2 agonists
bind to beta2-adrenergic receptors causing smooth muscle relaxation resulting in dilation of bronchial passages
What neurotransmitters bind to beta-2 agonists
epinephrine and norepinephrine
T/F: Beta-2 agonists work on the sympathetic path of the nervous system while muscarinic antagonists work on the parasympathetic path of the nervous system
True
T/F: S and R enatiomers of catecholamines are active Beta-adrenergic agents
False: Only R enatiomer is active
What are the three interaction points that allow catecholamines to bind to the beta-2 receptor
1) para and meta hydroxy groups, 2) hydroxy group at the beta carbon, 3) the amine group (primary or secondary) that is seperated by two carbons
What are the two enzymes that metabolize catecholamines, where do they attack
monoamine oxidase (MOA)- oxidizes the amine group, catechol o-methyltransferase (COMT)- attacks the hydroxy groups on the aromatic ring
What changes to amine group leads to better beta selectivity
adding bulk to N-substituent
What are the two amine groups that have the most beta-2 selectivity
N-tertiary butyl, and aromatic methylhydroxy substitution
T/F: A larger amino substituent is correlated to protection from MAO
True
What is the consequence of having an alpha carbon substitution in cathecholamines for beta-adrenergic agents
decreased alpha/beta activity but has MAO protection that increases the oral bioavailability
What is another way to position the hydroxy groups in catecholamine instead of para/meta, what is the consequence
ortho/para (resorcinol), protection from COMT metabolism
What are the short acting beta-2 agonists (SABAs)
albuterol, salbutamol, terbutaline, metaproterenol
How doe salbutamol and albuterol protect themselves from oxidation reaction, protection from MAI
Add a carbon in between hydroxy group and aromatic ring, bulky N-subistiuent
Which SABAs are based on para/meta hydroxy placement, which SABAs are based on ortho/para hydroxy placement
Albuterol and salbutamol/ terbutaline and metaproterenol
What are the long acting beta-2 agonists (LABAs)
Salmeterol, Formoterol, Bamuterol
What makes salmeterol, formoterol, and bambuter LABAs
long lipohillic side chain, pro drugs
What is the amount of time needed to be considered long acting
12 or more hours
What is MOA of muscarinic antagonists
bind the M3 receptor causing a decrease in forming of cGMP resulting in dilation of bronchonconstrictor muscles and decreased mucus secretion
What are the muscarinic antagonists derivatives of
naturally occuring tropine alkaloids
What is tropane, tropine
nitrogenous bicyclic compound, hydroxylated tropane
What is the long acting LAMA, short acting LAMA
tiotropium, Ipatropium
What is the key feature that makes muscarnic antagonists antagonists
chiral carbon connected to the aromatic ring points backwards
Why do muscarinic antagonists not cause systemic side effects, do not cross the blood barrier, and do not have central side effects
The quaternary amines are charged
