Autonomic Nervous System: Adrenergic Agonists Flashcards
What is the classifications of drugs that mimic the pharmacological and physiologic actions of endogenous catecholamines? What are their effects mediated by?
Drugs that mimic the pharmacological and physiological actions of the endogenous cathecolamines are classified as **sympathomimetic drugs. **Their effects are mediated by activation of adrenergic receptors located on effector cells and tissues
What mediates NE release from nerve terminals? When released what does NE bind to?
- Sympathetic nerve activity mediates NE release from nerve terminals
- Released NE binds to and activates adrenergic receptors located on postsynaptic effector
tissues and at presynaptic sites
What are the classifications of adrenergic agonists?
The adrenergic agonist are classified as: Direct-acting, indirect-acting, and mixed-acting
What does the capacity of the sympathomimetic drugs to produce physiological responses depend on?
Similarity of the chemical structure of sympathomimetic drugs to that of NE and EPI
What are direct acting adrenergic agonists?
Neurotransmitter and drug bind directly to and activate adrenergic receptor
What are indirect acting adrenergic agonists?
They mediate physiological response that involves increasing the synaptic levels of endogenous catecholamines
What are mixed acting adrenergic agonists?
Some drugs demostrate the capability to directly activate adrenergic receptors and also to increase the release of NE from adrenergic nerve terminals
Many adrenergic receptor agonists demostrate a level of ________ for specific _________.
Many adrenergic receptor agonists demostrate a level of selectivity for specific adrenergic receptors
True or False: An endogenous catecholamine or sympathomimetic drug only has a specificity for one type of adrenergic receptor.
An individual endogenous cathecolamine or sympathomimetic drug may exihibit a higher affinity
or selectivity for one or more subtypes of adrenergic receptors
What are pharmacologic interactions between agonists and adrenergic receptors influenced by?
- The tissue distribution of adrenergic receptors
- The number of adrenergic receptors expressed at specific sites * Interaractions between the sympathetic and parasympathetic nervous systems at target sites
- Pathophysiological and disease states
- The background level of sympathetic nerve activity
- Levels of endogenous catecholamines and /or sympathomimetic drugs
What is desensitization?
Prolonged exposure of adrenergic receptors to specific agonist reduces the responsiveness of these receptors, producing a progressive attenuation in the tissue‘s capacity to facilitate physiological responses
What are the 3 proposed mechanisms used to describe desensitization?
- Sequestration of receptors so that they are unavailable for interaction with the ligand
- Down-regulation, that is, a disappearence of the receptors by destruction or by decreased
synthesis - An inability to couple to G-protein, because the receptor has been phosphorylated on the
cytoplasmic side
What is the physiologic responses seen with stimulation of A1 receptor for the following tissues:
- Most vascular smooth muscle (innervated)
- Pupillary dilator muscle
- Urethral smooth muscle
- Splenic capsule
Most vascular smooth muscle (innervated) - Contraction
Pupillary dilator muscle- contraction ( pupil dialation)
Urethral smooth muscle- Contraction
Splenic capsule- contraction
What is the physiologic responses seen with stimulation of A2 receptor for the following tissues:
- Platelets
- Adrenergic and cholinergic nerve terminals
- Selected vascular smooth muscle
Platelets- Aggregation
Adrenergic and cholinergic nerve terminals - Inhibits transmitter release
Selected vascular smooth muscle- Contraction
What is the physiologic responses seen with stimulation of B1 receptor for the following tissues:
What is the physiologic responses seen with stimulation of B2 receptor for the following tissues:
What is the physiologic responses seen with stimulation of B3 receptor for the following tissues:
What is the physiologic responses seen with stimulation of D1 receptor for the following tissues:
What is the physiologic responses seen with stimulation of D2 receptor for the following tissues:
What would be the receptor you would like to influence in this case? What should this receptor do?
What is responsible for maintaining baseline airway tone? Activation of muscurinic receptor will cause what effect on bronchoal smooth muscle?
PSNS is responsible for maintaining baseline airway tone and activation of bronchial muscarinic receptors produces contraction of bronchial smooth muscle