Adrenergic Agents Flashcards

1
Q

What are the 4 sympathomimetic effects of the CV system

A

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

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2
Q

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

A
  1. Displace stored catecholamines

2. Inhibit reputake of released neurotransmitter by interfering with NET

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3
Q

What are some examples of indirect acting sympathomimetics?

A

Amphetamines, Tyramine containing compounds, catecholamine reuptake inhibitors

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4
Q

What does Amphetamine do?

A

Release of stored NE and DA

CNS stimulant: increased mood and alertness, and decrease appetite

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5
Q

What does methamphetamine do?

A

Similar to Amphetamine, made from pseudo ephedrine

potent CNS action

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6
Q

What is Methylamphenidate used in?

A

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

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7
Q

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

A
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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8
Q

What is Tyramine metabolized by?

A

MAO

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9
Q

What is the goal of catecholamine repute inhibitor?

A

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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10
Q

What is the action of Cocaine?

A

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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11
Q

Therapeutic Application of Sympathomimetics: Hypotension

A

Goal increase BP and CO

  1. A1 agonist to Raise BP (NE, phenylephrine)
  2. Ionotropic agents in shock syndrome to increase CO (Dopamine, Dobutamine)
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12
Q

Therapeutic Application of Sympathomimetics: Hypertension

A

Goal decrease BP

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

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13
Q

Therapeutic Application of Sympathomimetics: Orthostatic HTN

A

Goal Increase BP

1. A1 agonist: Midrodine

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14
Q

Therapeutic Application of Sympathomimetics: Emergency Cardiac Measures

A

Goal Cardiac resusciation

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

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15
Q

Therapeutic Application of Sympathomimetics: Surgical

A

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

  1. Reduce blood loss A1 activity-Epinehphrine/cocaine
  2. Slow diffiusion-Epi, NE, Phenylephrine
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16
Q

Therapeutic Application of Sympathomimetics: Sinus Decongestant

A

Goal Decrease Nasal Stuffiness

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

17
Q

Therapeutic Application of Sympathomimetics: Pulmonary uses

A

Improve pulmonary airflow

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

18
Q

Therapeutic Application of Sympathomimetics: Anaphylaxis

A

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

19
Q

Therapeutic Application of Sympathomimetics: ophthalmic applications

A

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

20
Q

Therapeutic Application of Sympathomimetics: GU applications

A

Delay delivery of baby: (aka tocolysis)

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

21
Q

Therapeutic Application of Sympathomimetics: CNS

A

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

22
Q

Therapeutic Application of Sympathomimetics: ICU sedation

A

Goal Improve pt comfort in ICU

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

23
Q

Name the types of adrenergic receptors?

A

Alpha, beta

24
Q

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

A

MAO-monoamine oxydase

COMT-catecholomethyltransferase

25
Q

What is NET and what does it do?

A

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

26
Q
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
A

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

27
Q
What actions occur with use of adrenergic antagonists in following:
CV
Pulm
Ocular
Glucose
Lipids
A

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

28
Q

What is ISA

A

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

29
Q

Limitations of B Blocker use?

A

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