Term
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Definition
| structurally related to the endogenous neurotransmitters/hormones of the sympathic nervous system. |
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Term
| MAO (Monoamine Oxidase) and COMT (Catechol-O-Methyl transferase |
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Definition
| 2 enzymes inactivate endogenous catecholamines and limit bioavailability and half life of synthetic analogs |
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Term
| Pathway of therapuetic effect of bronchodilators |
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Definition
| b2 receptor stimulation increases activity of Adenylyl Cyclase via Gs protein and induce formation of cAMP => PKA activation => relaxation of respiratory tract smooth muscle |
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Term
|
Definition
Stimulates Both beta receptor subtypes.
Cardio efx limits use
Substrate for COMT |
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Term
| B-receptor Agonist SAR: Amino-group substitution |
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Definition
| increases B-receptors binding vs Alpha-receptors |
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Term
| B-receptor Agonist SAR:adding a Beta-OH group |
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Definition
| Increases direct agonist activity and vesicular storage |
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Term
| B-receptor Agonist SAR: Catechol structure |
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Definition
| Promotes maximal Alpha and Beta receptor binding |
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Term
| B-receptor Agonist SAR: Non-Catechol structure (Ring lacks OH Substituents) |
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Definition
| prolongs duration of action because compound is no longer a substrate for metabolic enzyme COMT |
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Term
| B-receptor Agonist SAR:Substitutions of Alpha-Carbon |
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Definition
| Prolong duration of action - reduced metabolism by MAO |
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Term
| Reasons for beta-agonist treatment has improved? (3) |
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Definition
Use of b2-adrenoceptor selective agents (To decrease Cardiovascular efx)
increased Metabolic resistance (Prolong Duration of Axn)
Adminstration as aerosols in various devices (Limit systemic efx) |
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Term
| Bronchodilation is mediated by |
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Definition
| Beta2-receptors - localized on airway smooth muscle |
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Term
| Short/Intermediate acting beta-2-agonists |
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Definition
Albuterol
Levalbuterol
Pirbuterol |
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Term
|
Definition
Drug of choice for treatment of acute asthma symptoms.
Inhaled
Bronchodilation within 15min.
Duration 3-4 Hrs.
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|
|
Term
Adverse Drug Effects - Cardio
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|
Definition
| Tachycardia,palpitations, hyper-or hypotensio |
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Term
|
Definition
| Tremor, Weakness, Muscle Cramping |
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Term
|
Definition
| The hyperglycemic effect may become relevant in diabetic patients |
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Term
| Quaternary Anticholinergics |
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Definition
may be direct agonist especially at NM junctions. Do not pass BBB well
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Term
| Alkaloids Anticholinergics |
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Definition
Organic abses, most are pharmacologically active
Nicotine, muscarine, quinine, strychnine, morphine |
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Term
|
Definition
| Stimulation of a system by means other than agonist activity at a receptor |
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Term
|
Definition
| Usually used to indicate true agonist activity (binding affinity with resulting efficacy) |
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Term
|
Definition
| system refractory period following prolonged agonist occupancy/stimulation of a receptor |
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|
Term
Albuterol = Salbutamol
Brand name, Inhaled, Oral |
|
Definition
Ventolin: Drug of choice. Dilation with 15min, duration 3-4 hours when inhaled
Orally: Dilation in 30min Duration 4-8 Hours
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|
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Term
| Levalbuterol. Brand Name and What is it |
|
Definition
Xopenex: active R-enantiomer of racemic albuterol.
Higher Cost |
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|
Term
Pirbuterol
Brand name and what about it |
|
Definition
| Maxair, Chemically and Pharmacodynamically similar to albuterol |
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Term
| LABA Characteristic and why its important |
|
Definition
High Lipid Solubility
Allows drug to dissolve into smooth muscle cell membrane
Slow release depot
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Term
|
Definition
Servent
Longterm prevention
BID 12 hours. Not for acute, onset is 30min
good for Exercise induced bronchoconstriction |
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Term
|
Definition
Foradil
Dosing is BID 12 hours
good for Exercise induced bronchoconstriction |
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