Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
31 Cards in this Set
- Front
- Back
|
Draw phenylethylamine. What is this the structural backbone for and what do drugs derived from this do?
|
Phenylethylamine is the basic structural backbone for most sympathomimetics and mimics the actions of the sympathetic nervous system.
|
|
|
What are two variations of phenylethylamine?
|
(1) A methyl group substitued on the alpha carbon makes the compound more resistant to MAO and effective orally.
(2) Amphetamines - have greater lipophilicity (no hydroxyl groups on the phenyl group) which will have greater ability of getting into the CNS. |
|
|
Name three Amines wih primarily alpha receptor activity.
|
(1) Phenylephrine
(2) Metaraminol (3) Naphazoline |
|
|
In summary, what are the primary uses for Alpha Receptor Agonists?
|
Alpha receptor agonists primarily will cause contraction in smooth muscle.
|
|
|
What are the therapeutic uses for alpha receptor drugs (phenylephrine, Metaraminol, Naphazoline)?
|
(1) Over-the-counter decongestant
(2) Blood Shot Eyes (3) Hypotensive Crisis - hemorrhagic shock, low blood pressure in spinal cord victims, and to counteract hypertensives (4) Paraoxysmal Atria Tachycardia (5) Production of mydriasis |
|
|
Side- What are the three muscles in the eye mentioned in class and what receptors are on each?
|
Three muscles include radial, ciliary, and circular. Radial muscles have alpha receptors which when activated contract, causing pupil dilation. Ciliary muscles have muscarenic receptors and when blocked can accomodate near vision by preventing rounding up.
|
|
|
What is the prototypical beta agonist?
|
Isoproterenol.
|
|
|
What are the uses for isoproterenol? Is it still in use? Why or why not?
|
Isoproterenol is the prototypical Beta agonist. It is infrequently used now because its equivelant potency as a beta 1 and beta 2 agonist. The greatest use fof Beta agonists is for the treatment of asthma.
|
|
|
Name Beta 2 receptor agonists.
|
(1) Albuterol
(2) Metaproterenol (3) Terbutaline (4) Salmeterol (5) Dobutamine - actually this is only Beta 1 |
|
|
Out of all the beta 2 receptor agonist all are active for about 3-4 hours, except one which has activity that lasts for about 12 hours. Which beta 2 agonist is this?
|
Salmeterol.
|
|
|
Which beta 2 receptor is used to relax uterine smooth muscle in order to delay premature delivery?
|
Terbutaline.
|
|
|
Which drug is a beta 1 receptor agonist? How is this drug used?
|
Dobutamine has greater Beta 1 activity than Beta 2. It appears to have an inotropic effect on the heart with little effect on the heart rate or peripheral resistance. Thus, it is used to treat failing heart due to cardiogenic congestive heat failure. This drug is not used for the longterm.
|
|
|
side - What is positive and negative effects of inotropic?
|
Positive inotropic - the heart beats more forcefully
Negative inotropic - the heart beats less forcefully |
|
|
side - what is chronotropic and what are the positive and negative effects of chronotropic?
|
Chronotropic is the rate at which the heart beats. Positive - increases the heart rate and Negative - decreases the heart rate.
|
|
|
What is the drug most frequently used for increased alpha and beta activity?
|
EPI.
|
|
|
For cardiac stimulation during an emergency, which receptor would be activated?
|
Beta 1
|
|
|
For bronchial dilation, which receptor would be activated?
|
Beta 2
|
|
|
For anaphylactic shock, which receptor would be activated?
|
(1) Bronchospasms - beta 2
(2) Mast cell release of histamine - beta 2 (3) drop in blood pressure - beta 1 (4) Pharyngeal and glottal edema - alpha 1 |
|
|
For administration of Local Anesthetic, which receptor would be activated?
|
Alpha 1
|
|
|
For topical administration to control nosebleed, which receptor would be activated?
|
Alpha 1
|
|
|
For treatment of glaucoma, which receptor is used?
|
Alpha 1 - it reduces the blood flow in the ciliary body to reduce aqueous humor production and Beta 1 - this is desensitization of receptors that mediate aqueous humor production.
|
|
|
What amines have CNS activity?
|
(1) Amphetamine
(2) Methamphetamine (3) Methylphenidate (Retilin) |
|
|
What are Amphetamine, Methamphetamine, and methylphenidate used for?
|
They are applied for ADHD.
|
|
|
T/F: Amphetamine, Methamphetamine, Methylphenidate acts indirectly by releasing NE from nerves.
|
TRUE.
|
|
|
What drug do the CNS amine drugs have in common?
|
Tyramine by taking up space in the storage vesicle and displace NE.
|
|
|
What side effects do amphetamine, methamphetamine, and methylphenidate have?
|
(1) GI motility decreases
(2) Heart Rate Increases (3) Move around more (4) Euphoria (5) stereotpical behavior (6) Paranoia or aggressive behavior (7) Can cause bruxism. |
|
|
What is dopamine treated for?
|
Hypovolemic shock and cardiogenic shock.
|
|
|
What is hypovolemic shock and how is it treated?
|
Hypovolemic shock is when the body's blood volume goes down and the kidney, in response to the low blood volume, releases renin and angiotensin II which causes vasoconstriction - this is the wrong response. It can be treated with dopamine which stimulates beta 1 receptors in the heart and a d1 receptor which causes vasodilation in the kidney and prevents kidney damage.
|
|
|
What are two drugs that are agonists for the alpha 2 autoreceptors?
|
(1) Clonidine
(2) alpha-methyl dopa |
|
|
What is the mechanism for clonidine? What is it primarily used to treat?
|
Clonidine decreases the release of NE and thereby decreases the sympathetic outflow from the CNS and periphery. Clonidine is primarily used to treat hypertension.
|
|
|
What is the mechanism for alpha-methyl dopa?
|
In the terminal, alpha-mehtyl dopa is converted to alpha-mehtyl dopamine and is then converted to alpha-methyl NE. When released, the alpha-methyl NE binds to alpha 2 receptr and is its agonist and decreases the release of NE and therefore decreases the sympathetic ouflow.
|
