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THE PHARMACOLOGY OF ADRENERGIC RECEPTORS. M.T. Piascik PHA 824 December 11 & 16, 2008. Learning Objectives. The student should be able to explain or describe; The pharmacodynamic principles that aid in the understanding of adrenergic receptors and the actions of drugs on these receptors.

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THE PHARMACOLOGY OF ADRENERGIC RECEPTORS

M.T. Piascik

PHA 824

December 11 & 16, 2008


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Learning Objectives

The student should be able to explain or describe;

The pharmacodynamic principles that aid in the understanding of adrenergic receptors and the actions of drugs on these receptors.

The criteria upon which alpha and beta receptors are defined.

The second messenger systems utilized by alpha and beta receptors and how activation of these receptors leads to a change in physiologic function.


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Learning Objectives(cont.)

The student should be able to explain or describe;

The effects of alpha and beta receptor activation on the heart and blood vessels.

The effects of isoproterenol, epinephrine and norepinephrine on the cardiovascular system.

The clinical uses and potential toxicities of epinephrine, norepinephrine and isoproterenol with emphasis on epinephrine.



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Beta Adrenergic Receptors

DRUG KD BETA1 RECEPTORKD BETA2 RECEPTOR

Epinephrine 800 nM800 nM

Norepinephrine 1000 nM 10,000 nM

Isoproterenol 80 nM80 nM


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Which of the dose-response curves represents activation of the beta1 receptor and which represents activation of the beta2 receptor?


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Beta Adrenergic Receptor Systems the beta1 receptor and which represents activation of the beta2 receptor?

Tissue Receptor Subtype

Heart beta1

Adipose tissue beta1

Vascular smooth muscle beta2

Airway smooth muscle beta2

Kidney-renin release from JG cells beta1



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Rhythm disturbances are a major concern with drugs that activate the beta1 receptor.

Physiologic Consequences of Beta1 Receptor Activation


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The BETA1-Adrenergic Receptor as a Therapeutic Target activate the beta1 receptor.

  • Agonists- congestive heart failure

    2) Antagonists- hypertension, ischemic heart disease, congestive heart failure, supraventricular tachyarrhythmias.




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The Beta2-Adrenergic Receptor as a Therapeutic Target Muscle

Agonists- Airways dysfunction (asthma, chronic bronchitis emphysema), tocolytics

Antagonists- No therapeutic uses.


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The BETA2-Adrenergic Receptor as a Therapeutic Target Muscle

  • Agonists- congestive heart failure

    2) Antagonists- hypertension, ischemic heart disease, congestive heart failure, supraventricular tachyarrhythmias.


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Alpha Adrenergic Receptors Muscle

KD KDKD

BETA1 RECEPTOR BETA1 RECEPTORALPHA RECEPTOR

Epinephrine 800 nM 800 nM5000 nM

Norepinephrine 1000 nM 10,000 nM* 6000 nM

Isoproterenol 80 nM 80 nM 10,000 nM**

* At doses used in therapeutics, Norepinephrine is void of Beta2 activity

** At doses used in therapeutics, Isoproterenol is void of Alpha1 activity









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Therapeutic Uses of Epinephrine Norepinephrine

Oral dosing of epinephrine, norepinephrine or isoproterenol is not possible due to its rapid metabolism in the gut by MAO.

Epinephrine can be given topically, by injection (s.c., i.m. i.v) or inhalation


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Therapeutic Uses of Epinephrine Norepinephrine(cont.)

Actions at the Beta2 Receptor

  • The treatment of respiratory distress or bronchspasm caused for example by asthma (i.e. status asthmaticus) or anaphylaxis as a result of allergic responses.

    Actions at the Beta1 Receptor

  • Epinephrine is also used to provide rapid inotropic support in cardiopulmonary resuscitation


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Therapeutic Uses of Epinephrine Norepinephrine(cont.)

Actions at the Beta2 Receptor

  • The treatment of respiratory distress or bronchspasm caused for example by asthma (i.e. status asthmaticus) or anaphylaxis as a result of allergic responses.

    Actions at the Beta1 Receptor

  • Epinephrine is also used to provide rapid inotropic support in cardiopulmonary resuscitation


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Therapeutic Uses of Epinephrine Norepinephrine(cont.)

Actions at the Alpha1 Receptor

  • Epinephrine is often used in combination with local anesthetic agents (such as articaine, bupivacaine or lidocaine) to prolong the duration of anesthetic action.

  • Epinephrine is used in

    surgery to reduce bleed.


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Epinephrine Toxicities Norepinephrine

  • Arrhythmias

  • Hypertension

  • Toxicity can occur following systemic administration or systemic absorption following oral administration.


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Epinephrine Toxicities Norepinephrine

  • Arrhythmias

  • Hypertension

  • Toxicity can occur following systemic administration or systemic absorption following oral administration.


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Epinephrine Toxicities Norepinephrine

  • Toxicity can be potentiated in patients taking tricyclic antidepressants, nonselective beta blockers, cocaine and amphetamine-like drugs and those under general anesthesia.


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Beta1-AR Norepinephrine

Beta2-AR