Adrenergic Agents Flashcards by Marialaina Tomolonis

What are the 4 sympathomimetic effects of the CV system

Heart rate, CO, Peripheral vascular resistance, and venous return

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What are the 2 potential mechanisms of Indirect-acting sympathomimetics?

Displace stored catecholamines

2. Inhibit reputake of released neurotransmitter by interfering with NET

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What are some examples of indirect acting sympathomimetics?

Amphetamines, Tyramine containing compounds, catecholamine reuptake inhibitors

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What does Amphetamine do?

Release of stored NE and DA

CNS stimulant: increased mood and alertness, and decrease appetite

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What does methamphetamine do?

Similar to Amphetamine, made from pseudo ephedrine

potent CNS action

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What is Methylamphenidate used in?

ADHD (Aka Ritalin) Reduces reuptake of NE and improves its function in the brain

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Name 2 additional indirect sympathomimetics other than amphetaimes and tyramine products.

Modafinil (Provigil)
inhibits NE and DA transporters in CNS
Exact mech is poorly understood
Use to increase wakefulness w/ narcolepsy
Armodafinil (nuvigil)
R-enantiomer of modafinil
Similar actions and uses to modafinil

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What is Tyramine metabolized by?

MAO

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What is the goal of catecholamine repute inhibitor?

Imbalance of NE and DA leads to different actions

Atomoxetine (stratera), ADHD
Sibutramine (Meridia) Serotonin and NE reuptake inhibitor, Approved as appetite suppressant
Duloxetine (Cymbalta)-Serotinin and NE reuptake inhibotor used as an antidepressent

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What is the action of Cocaine?

It is a catecholamine reuptake inhibitor

inhibits preipheral repute of NET
enters CNS produces amphetamine -like action but more intense
inhibition of DA repute in pleasure center (very rapid addiction)

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Therapeutic Application of Sympathomimetics: Hypotension

Goal increase BP and CO

A1 agonist to Raise BP (NE, phenylephrine)
Ionotropic agents in shock syndrome to increase CO (Dopamine, Dobutamine)

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Therapeutic Application of Sympathomimetics: Hypertension

Goal decrease BP

1. Central acting A2 agonist manage HTN: Clonidine (Catapres)

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Therapeutic Application of Sympathomimetics: Orthostatic HTN

Goal Increase BP

1. A1 agonist: Midrodine

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Therapeutic Application of Sympathomimetics: Emergency Cardiac Measures

Goal Cardiac resusciation

1. A1 and B2 mediated actions - redistribute blood flow from less important areas to more important areas

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Therapeutic Application of Sympathomimetics: Surgical

2 Goals-Reduce blood loss, Slow diffusion of anesthetics away from site of administration

Reduce blood loss A1 activity-Epinehphrine/cocaine
Slow diffiusion-Epi, NE, Phenylephrine

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Therapeutic Application of Sympathomimetics: Sinus Decongestant

Goal Decrease Nasal Stuffiness

1. A1 Vasoconstriction in nasal passageways (Phenylephrine and oxymetazoline)

Therapeutic Application of Sympathomimetics: Pulmonary uses

Improve pulmonary airflow

B2 very commonly used in inhalers and nebulizers (Albuterol, metaproterenol, pirbuterol etc.)

Therapeutic Application of Sympathomimetics: Anaphylaxis

Reversal of vascular complications of immune hypersensitivity: symptoms of exposure to allergen can include shock due to cardiovascular and respiratory hypersensitivy response-bronchospasm, mucus membrane contestion,
1. Activate a1, b1, and b2 to reverse all symptoms

Therapeutic Application of Sympathomimetics: ophthalmic applications

multiple goals
Mydriasis-A1 agonist
Decongestant-A1 agonist
Reduction of intraocular pressure-A2 against (apraclonidine (lopidine), and brimonidine; alphagan)

Therapeutic Application of Sympathomimetics: GU applications

Delay delivery of baby: (aka tocolysis)

1. B2 selective used to relax uterus in preterm labor-Ritadine and terbutaline

Therapeutic Application of Sympathomimetics: CNS

Goal 1: Narcolepsy, and increase alertness and defer sleep Amphetamine, modafinil
Goal 2: Appetite suppression
Goal 3: ADHD management-Methylphenidate (ritalin), Dextroamphetamine (Adderall), Lisdexamfetamine (Vynase) prodrug for amphetamine

Therapeutic Application of Sympathomimetics: ICU sedation

Goal Improve pt comfort in ICU

A2 agonist- in combination with opioids, benzos and propofol lowers reuquirements of other drugs: (Dexmedetomidine)

Name the types of adrenergic receptors?

Alpha, beta

What are the names of the two enzymes that metabolize norepinephrine, epinephrine, and dopamine

MAO-monoamine oxydase

COMT-catecholomethyltransferase

What is NET and what does it do?

Norepinephrine transporter protein re-uptake NE and decreases NE activity; terminates adrenergic action

``` What effect occurs when the following receptors are stimulated by an agonist in the cardiovascular by an agonist in the cardiovascular system? For what medical conditions can these agents be used? A1 A2 B1 B2 ```

A1-located in PVS: Vasoconstriction A2-Peripheral: vasoconstriction (only when given locally or in high doses), Central: vasodilation drop BP B1-located in heart: inc HR and CO B2-Located in the PVS: vasodilation drops BP

``` What actions occur with use of adrenergic antagonists in following: CV Pulm Ocular Glucose Lipids ```

CV: A1 antagonist-Vasodilation B1 antagonist- dec HR and dec CO B2 antagonist- vasoconstriction, Increase BP (not really) Lungs: B2 antagonist-Bronchoconstriction (careful with B blocker) Eye: Decreased IOP, Midriasis Glucose: Block breakdown of lipid , blocks glucose mobility, decreases body ability to make more energy stores - worsens hypoglycemia

What is ISA

Intrinsic sympathomimetic activity-partial agonist activity of what was designed as a antagonist.

Limitations of B Blocker use?

leads to hypoglycemia, drop blood sugar, can worsen asthma, can worsen heart function in those with heart failure.