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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

THE PHARMACOLOGY OF ADRENERGIC RECEPTORS

M.T. Piascik

PHA 824

December 11 & 16, 2008

learning objectives
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.

learning objectives cont
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.

beta adrenergic receptors
Beta Adrenergic Receptors

DRUG KD BETA1 RECEPTORKD BETA2 RECEPTOR

Epinephrine 800 nM800 nM

Norepinephrine 1000 nM 10,000 nM

Isoproterenol 80 nM80 nM

slide6
Which of the dose-response curves represents activation of the beta1 receptor and which represents activation of the beta2 receptor?
beta adrenergic receptor systems
Beta Adrenergic Receptor Systems

Tissue Receptor Subtype

Heart beta1

Adipose tissue beta1

Vascular smooth muscle beta2

Airway smooth muscle beta2

Kidney-renin release from JG cells beta1

the beta1 adrenergic receptor as a therapeutic target
The BETA1-Adrenergic Receptor as a Therapeutic Target
  • Agonists- congestive heart failure

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

the beta2 adrenergic receptor as a therapeutic target
The Beta2-Adrenergic Receptor as a Therapeutic Target

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

Antagonists- No therapeutic uses.

the beta2 adrenergic receptor as a therapeutic target14
The BETA2-Adrenergic Receptor as a Therapeutic Target
  • Agonists- congestive heart failure

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

alpha adrenergic receptors
Alpha Adrenergic Receptors

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

therapeutic uses of epinephrine
Therapeutic Uses of Epinephrine

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

therapeutic uses of epinephrine cont
Therapeutic Uses of Epinephrine(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
therapeutic uses of epinephrine cont25
Therapeutic Uses of Epinephrine(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
therapeutic uses of epinephrine cont26
Therapeutic Uses of Epinephrine(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.

epinephrine toxicities
Epinephrine Toxicities
  • Arrhythmias
  • Hypertension
  • Toxicity can occur following systemic administration or systemic absorption following oral administration.
epinephrine toxicities28
Epinephrine Toxicities
  • Arrhythmias
  • Hypertension
  • Toxicity can occur following systemic administration or systemic absorption following oral administration.
epinephrine toxicities29
Epinephrine Toxicities
  • Toxicity can be potentiated in patients taking tricyclic antidepressants, nonselective beta blockers, cocaine and amphetamine-like drugs and those under general anesthesia.
slide35

Beta1-AR

Beta2-AR

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