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Pharmacology
Sympathomimetics
| Question | Answer |
|---|---|
| What are sympathomimetics? | Agents which in general mimic responses due to stimulation of sympathetic nerves. |
| Which receptors are activated by sympathomimetics? | Adrenergic receptors |
| How do sympathomimetics activate directly or indirectly adrenergic receptors? | Increasing norepinephrine and epinephrine levels |
| What are the main mediators of the sympathoadrenal system? | Norepinephrine and Epinephrine |
| What conditions are most commonly treated with Sympathomimetics? | Cardiovascular pathology, hypersensitivity, COPD, adn glaucoma |
| What sympathomimetic drugs have direct-acting mode of action? | Alpha-adrenergic agonists, B-adrenergic agonists, and dopaminergic agonists |
| What are some common indirect acting sympathomimetics? | MAOIs, COMT inhibitors, release stimulants, and reuptake inhibits that increase levels of endogenous catecholamines |
| What are the main two categories of Direct-acting adrenergic agonists? | Selective and Nonselective |
| What are 4 common examples of a Selective direct-adrenergic agonists? | Phenylephrine, Clonidine, Dobutamine, and Terbutaline |
| What is a Direct-adrenergic agonist of alpha-1 receptor? | Phenylephrine |
| What is the overall or simple way to describe the mode of action of Indirect acting sympathomimetics? | Release NA from nerve endings |
| Directly act as agonist on a alpha & beta or both | Direct Acting sympathomimetic |
| On which type of neuron do Indirect acting sympathomimetic act on? | Adrenergic neurons to release N. A. |
| What does the classification of Direct acting sympathomimetics, selective or nonselective, describes? | Selective are drugs that only work in one receptor (alpha or beta), and nonselective act on more than one receptor, either alpha, beta, or both. |
| Selective Direct-acting alpha-2 sympathomimetic | Clonidine |
| On which receptor does Clonidine work? | alpha-2 |
| Which receptor is stimulated by Dobutamine? | Beta-1 |
| What is an important B-1 direct acting sympathomimetic? | Dobutamine |
| What type of adrenergic agonist is Terbutaline? | Selective Direct-Acting adrenergic agonist |
| Which receptors are stimulated by Isoproterenol? | Beta-1 and Beta-2 |
| Does Epinephrine or Norepinephrine, have B2 activity? | Epinephrine |
| List of Nonselective Direct-acting adrenergic agonists: | Oxymetazoline Isoproterenol Epinephrine Norepinephrine |
| Which sympathomimetic is known to have mixed-acting qualiteis? | Ephedrine |
| Which adrenergic receptors are stimulated by Epinephrine? | Alpha 1 , Alpha 2, Beta 1, and Beta-2 |
| What are the subcategories of Indirect-acting adrenergic agonists? | 1. Releasing agents 2. Uptake inhibitor 3. MOA inhibitors 4. COMT inhibitors |
| What is meant by saying that Ephedrine has mixed acting qualities? | It is both a direct acting agonist, and and indirect acting adrenergic agonist. |
| What is the Indirect form in which Ephedrine works? | As a releasing agent |
| What are common Indirect-acting adrenergic receptors, classified as releasing agents? | Amphetamine, and tyramine |
| Is cocaine a direct or indirect-acting sympathomimetic? | Indirect-Acting adrenergic agonist |
| MOA inhibitor: | 1. Selegiline 2. Indirect-Acting adrenergic agonist |
| What is the purpose of action for Indirect-acting sympathomimetics? | Increase the availability of NE and EPI to stimulate adrenergic receptors |
| Other than Ephedrine, what other hormone has mixed-acting sympathomimetic features? | Dopamine |
| List of muscles with alpha-1 adrenergic activity: | 1. Most vascular smooth muscle (innervated) 2. Pupillary dilator muscle 3. Pilomotor smooth muscle 4. Prostate 5. Heart |
| What is the action due to a-1 vascular smooth muscle stimulation? | Contraction |
| alpha 1 stimulation of the pupillary dilator muscle cause: | Contraction (dilates pupil) |
| If an alpha 1 receptor is stimulated will increase or decrease blood pressure? | Increase blood pressure |
| Dilation of the pupil can be achieved by stimulating which adrenergic receptor? | Alpha-1 |
| What is the effect/action on the heart as the alpha-1 adrenergic receptor is stimulated? | Increases force of contraction |
| Which receptor is stimulated in order to increase the heart force of contraction? | Alpha-1 |
| Which tissues are affected by alpha-2 stimulation? | 1. Postsynaptic CNS neurons 2. Platelets 3. Adrenergic and cholinergic nerve terminals 4. Fat cells 5. Some vascular smooth muscle |
| What is a hematologic effect of alpha-2 adrenergic receptor stimulation? | Platelet aggregation |
| Which adrenergic receptor can be blocked in order to prevent platelet aggregation? | Alpha-2 |
| What is the effect of agonism of alpha-2 receptor in fat cells? | Inhibits lipolysis |
| Which are the main tissues affected by B1-adrenoreceptors? | Heart and juxtaglomerular cells |
| What actions are associated by the stimulation of B1 adrenoreceptors? | Increases force and rate of contraction ; increase renin release |
| Which adrenoreceptor subtype is stimulated in order to increase heart rate? | Beta-1 |
| Will stimulation or inhibition of Beta-1 adrenoreceptor cause decrease in heart rate? | Inhibition |
| Increasing the activity of B-1 adrenoreceptors will increase or decrease renin release? | Increase renin release |
| What muscle tissues are affected by B2-adrenoreceptor stimulation? | Respiratory, uterine, and vascular smooth muscle |
| What is the effect on the muscle tissues that are affected by B-2 stimulation? | Promotes smooth muscle relaxation |
| What is the action produced by the skeletal muscle due to B2-adrenoreceptor activation? | Promotes potassium uptake |
| An uptake of potassium can be seen with increased activity of which adrenoceptor subtype? | B2 |
| What is the action produced by B2 activity on human liver cells? | Activates glycogenolysis |
| What is the effect of D1 activity on smooth muscle? | Dilates renal blood vessels |