E1- Adrenergic Stimulants Flashcards by Catherine sendek

What type of adrenergic agent acts on presynaptic neuron to increase synthesis, cause release, and inhibit re-uptake?

Indirect acting

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What type of adrenergic agent acts on adrenergic receptors on target tissues to mimic sympathetic stimulation?

Direct acting

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What type of adrenergic agent stops indirect acting and may enhance direct acting?

Denervation

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What is the relative affinity of EPI, NE, and Isoproterenol for both alpha 1 and alpha 2 receptors?

EPI and NE > Isoproterenol

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Between alpha, beta, and dopamine, what is the only inhibitory receptor?

Alpha 2

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What is the role of of alpha 1 receptors?

Vasoconstriction in skin, kidney, and mucous membranes

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What is the role of of alpha 2 receptors?

Presynaptic

Inhibit neurotransmitter release

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What is the relative affinity of EPI, NE, and Isoproterenol for beta 1 receptors?

Isoproterenol > EPI and NE

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What is the role of beta 1 receptors?

Increase force and rate of contraction of the heart

Increase renin secretion from the kidney

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What is the relative affinity of EPI, NE, and Isoproterenol for beta 2 receptors?

Isoproterenol > EPI > NE

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What is the role of beta 2 receptors?

Relax bronchioles and gut smooth muscles
Increase glycogenesis
Vasodilate blood vessels supplying skeletal muscles

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What is the relative affinity of EPI, NE, and Isoproterenol for beta 3 receptors?

Isoproterenol and NE > EPI

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What is the role of beta 3 receptors?

Increase lipolysis

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What is the role of D1 receptors?

Vasodilate renal vasculature

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What receptors does NE stimulate? With what affinity?

Stimulates alpha and beta receptors

a1 = B1 > B2

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What is the affect of NE on a1 and b1 receptors?

a1= Vasconstriction, increase BP
B1= Increase HR
Baroreflex responds and decreases HR, therefore CO is either unchanged or decreased

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What the the route of administration of NE?

Very short acting

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What is NE used for?

Rarely used to increase BP for severe hypotensive crisis

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Are cocaine, tyramine, amphetamine, and MAOIs indirect acting, direct acting, or denervation agents?

Indirect acting agents

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If atropine is given prior to NE, what will happen?

The vagal reflex is inhibited, the baroreceptor effect will not occur, and the HR will increase

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What receptors does EPI stimulate? With what affinity?

Activates all adrenergic receptors

B1 = B2 > a1

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What receptor does low dose EPI stimulate? What affect does this have?

B2 
Vasodilate blood vessels supplying skeletal muscle
- Decreased DBP
- Increased PP
- No change in MAP
- No baroreflex to slow HR
- HR stays increased

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What receptor does high dose EPI stimulate? What affect does this have?

a1 overrides B2 
Vasoconstriction
- Increased DBP
- Increased MAP
- Baroreflex responds
- HR slows

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What is EPI used for?

Anaphylactic shock
Decrease diffusion of anesthetics (vasoconstrictor)
Glaucoma
Emergency tx for cardiac arrest and complete heart block

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What are contraindications of NE?

Severe vasoconstriction at the infusion site that can lead to necrosis

What are contraindications of EPI?

Pts taking beta-blockers (unopposed alpha effects, so it can lead to severe HTN)

What are side effects of EPI?

``` Tremor Throbbing HA Increased BP Tachycardia Angina in pts with CAD ```

What can be used to reverse the effects of EPI?

Alpha blockers

What are the three drugs classified as alpha 1 agonist?

Phenylephrine Pseudeophedrine Oxymetazoline

What is Phenylephrine used for?

Hypotensive emergency Decongestant (vasoconstrict nasal mucosa) Mydriasis

What are contraindication of Phenylephrin?

Caution in pts with HTN and BPH

What is the main side effect of Phenylephrine?

Rebound decongestion

What drug is similar to Phenylephrine, but more effective?

Pseudeophedrine

What is Oxymetazoline used for?

Decrease redness in the eye | Decongestant

What are contraindications of Oxymetazoline?

Caution in pts with glaucoma and HTN

What are the three drugs classified as alpha 2 agonist?

Clonidine Methyldopa Tizanidine

What is Clonidine used for?

Decreases cravings in recovering addicts Decreases hot flashes Pre-anesthetic to sedate and dry secretions

What are side effects of Clonidine?

``` Xerostomia Sedation Erectile dysfunction Sudden withdraw can lead to HTN crisis Avoid getting patch hot, can lead to hypotension ```

What is Methyldopa used for?

HTN

What are contraindications of Methyldopa?

Not recommended for monotherapy b/c of CNS effects (only used fo refractory HTN pts)

What are side effects of Methyldopa?

``` Xerostomia Sedation Erectile dysfunction Hemolytic anemia Hepatotoxicity ```

What drug is recommended to tx HTN in pregnancy?

Methyldopa

What is Tizanidine used for?

Muscle spasticity in neurological conditions

What is the main side effect of Tizanidine?

Asthenia (dose-related effect defined as weakness, fatigue, and/or tiredness)

What is the one drug classified as a non-specific beta agonist?

Isoproterenol | B1 and B2 agonst

What is Isoproterenol used for?

Emergency tx for cardiac arrest and complete heart block

What are side effects of Isoproterenol?

Tachycardia Palpations Arrhythmias

What is the one drug classified as a beta1 agonist?

Dobutamine

How is Dobutamine administered?

What is Dobutamine used for?

Increase contractility and output in cardiogenic shock and low output heart failure Cardiac stress tests if pt cannot exercise

What should you watch out for when giving Dobutamine to a pt with HTN?

BP may increase if given too quickly

What is the one drug classified as a beta2 agonist?

Albuterol

What is Albuterol used for?

Athma

What are side effects of Albuterol?

H/A Tachycardia Palpitations Tremor

What is the one drug classified as a beta3 agonist?

Mirabegron

What is Mirabegron used for?

Overactive bladder (relaxes detrusor muscle to increase bladder capacity)

What are the side effects of Mirabegron?

HTN | Tachycardia

What is the two drug classified as dopamine agonist?

Dopamine | Fenoldopam

What is the effect/use of low dose dopamine?

Renal vasodilation via D1 receptors in the kidey

What is the effect/use of moderate dose dopamine?

Inotropic effect via B1 receptors in the heart

What is the effect/use of high dose dopamine?

Vasocontriction via alpha receptors in blood vessels

What are contraindications of dopamine?

Should not be used with a MAOI because they are metabolized by MAO

What are the side effects of dopamine?

Tachycardia, nausea, vomiting, angina, headache, and peripheral vasoconstriction

How are dopamine and fenoldopam administered?

What is fenoldopam used for?

Emergency HTN

What are then side effects of fenoldopam?

Reflex tachycardia, headache, and flushing

What is are the 5 drugs classified as indirect acting sympathoimetics agonist?

``` Amphetamine Methylphenidate Methamphetamine Cocaine Tyramine ```

What is the MOA of Amphetamine, Methylphenidate, and Methamphetamine?

Increase release of NE from neurons

What is the MOA of Cocaine?

Inhibits reuptake of DA and NE

What is the MOA of Tyramine?

Increases release of DA, NE from nerve terminals | Rapidly hydrolyzed by MAO

What are Amphetamine and Methylphenidate equal DOCs for?

ADHD

What are side effects of Amphetamine, Methylphenidate, and Methamphetamine?

Tremor Tachycardia HTN Psychosis

What is unique about Amphetamine, Methylphenidate, and Methamphetamine?

Only work on intact neurons

Why is Methamphetamine a major drug of abuse?

It has more central actions and fewer peripheral effects

What can cocaine be used for?

Local anesthetic and powerful vasoconstrictor | Rarely used for nasopharyngeal surgery (too addicting)

What are side effects of cocaine?

``` Severe HTN Stroke Tachycardia Arrhythmias MI Psychosis ```

What are contraindications of Tyramine?

Pts tx for depression with MAOI, tyramine can lead to severe HTN crisis

What is the specific agonist for alpha 1 receptors?

Phenylephrine

What is the specific agonist for alpha 2 receptors?

Clonidine

What is the specific agonist for B1 receptors?

Dobutamine

What is the specific agonist for B2 receptors?

Albuterol

What is the specific agonist for B3 receptors?

Mirabegron

What happens when you give epinephrine after an alpha blocker?

The effects of epinephrine are reversed (hypotension)

What is dopamine used to treat?

Severe refractory heart failure and is useful if an increase in BP is needed